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FILE 'HOME' ENTERED AT 11:45:45 ON 09 SEP 2015

=> FILE Registry COST IN U.S. DOLLARS SINCE FILE TOTAL ENTRY SESSION FULL ESTIMATED COST 0.50 0.50

FILE 'REGISTRY' ENTERED AT 11:46:54 ON 09 SEP 2015 USE IS SUBJECT TO THE TERMS OF YOUR STN CUSTOMER AGREEMENT. COPYRIGHT (C) 2015 American Chemical Society (ACS)

Property values tagged with IC are from the ZIC/VINITI data file provided by InfoChem.

Page 2 of 37

STRUCTURE FILE UPDATES: 8 SEP 2015 HIGHEST RN 1803526-22-8 DICTIONARY FILE UPDATES: 8 SEP 2015 HIGHEST RN 1803526-22-8

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http://www.cas.org/legal/infopolicy

TSCA INFORMATION NOW CURRENT THROUGH JULY 10, 2015

Please note that search-term pricing does apply when conducting SmartSELECT searches.

REGISTRY includes numerically searchable data for experimental and predicted properties as well as tags indicating availability of experimental property data in the original document. For information on property searching in REGISTRY, refer to:

http://www.cas.org/training/stn/database-specific

=> s 139264-17-8 L1 1 139264-17-8 (139264-17-8/RN)

=> display L1 ENTER ANSWER NUMBER OR RANGE (1):1 ENTER DISPLAY FORMAT (IDE):all

L1 ANSWER 1 OF 1 REGISTRY COPYRIGHT 2015 ACS on STN RN 139264-17-8 REGISTRY ED Entered STN: 28 Feb 1992 CN 2-Oxazolidinone, 4-[[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl]-, (4S)- (CA INDEX NAME) OTHER CA INDEX NAMES: CN 2-Oxazolidinone, 4-[[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl]-, (S)- OTHER NAMES: CN (4S)-4-[[3-[2-(Dimethylamino)ethyl]-1H-indol-5-yl]methyl]-2- oxazolidinone CN (4S)-4-[[3-[2-(Dimethylamino)ethyl]-1H-indol-5-yl]methyl]oxazolidin-2- one CN (S)-4-[[3-[2-(Dimethylamino)ethyl]-1H-indol-5-yl]methyl]-2-oxazolidinone CN 311C90 CN Amigrawest CN Asco Top CN BW 311C90 CN No-migraine Z CN Xolnox CN Zipton CN Zolmitriptan CN Zomig CN Zominat FS STEREOSEARCH MF C16 H21 N3 O2 CI COM

Page 3 of 37 SR CA LC STN Files: ADISINSIGHT, ADISNEWS, ANABSTR, BIOSIS, BIOTECHNO, CA, CAPLUS, CASREACT, CBNB, CHEMCATS, CHEMLIST, CIN, DDFU, DRUGU, EMBASE, IMSPATENTS, IMSRESEARCH, IPA, MEDLINE, PATDPASPC, PS, RTECS*, TOXCENTER, USPAT2, USPATFULL (*File contains numerically searchable property data) DT.CA CAplus document type: Book; Conference; Dissertation; Journal; Patent RL.P Roles from patents: ANST (Analytical study); BIOL (Biological study); MSC (Miscellaneous); PREP (Preparation); PROC (Process); PRP (Properties); PRPH (Prophetic); RACT (Reactant or reagent); USES (Uses) RLD.P Roles for non-specific derivatives from patents: BIOL (Biological study); PREP (Preparation); PRP (Properties); USES (Uses) RL.NP Roles from non-patents: ANST (Analytical study); BIOL (Biological study); OCCU (Occurrence); PREP (Preparation); PROC (Process); PRP (Properties); RACT (Reactant or reagent); USES (Uses) RLD.NP Roles for non-specific derivatives from non-patents: ANST (Analytical study); FORM (Formation, nonpreparative)

Ring System Data

Elemental|Elemental| Size of |Ring System| Ring | RID Analysis |Sequence |the Rings| Formula |Identifier|Occurrence EA | ES | SZ | RF | RID | Count ======+======+======+======+======+======C3NO |NCOC2 |5 |C3NO |16.239.3 |1 C4N-C6 |NC4-C6 |5-6 |C8N |333.151.57|1

Absolute stereochemistry.

Experimental Property Tags (ETAG)

PROPERTY | NOTE ======+======ADME (Absorption, Distribution, Metabolism, Excretion)|(1) CAS 4 more tags shown in the MAX or ETAGFULL formats | Carbon-13 NMR Spectra |(2) CAS Crystal Structure |(3) CAS Half-Life (Biological) |(4) CAS 2 more tags shown in the MAX or ETAGFULL formats | Molecular Structure |(3) CAS Proton NMR Spectra |(2) CAS

(1) Moda, Tiago L.; Bioorganic & Medicinal Chemistry 2007 V15(24) P7738-7745 CAPLUS (2) Liu, Li-jun; Bopuxue Zazhi 2004 V21(1) P61-66 CAPLUS

Page 4 of 37 (3) Ravikumar, K.; Acta Crystallographica, Section E: Structure Reports Online 2007 V63(4) Po1774-o1776 CAPLUS (4) Uemura, Naoto; Clinical Drug Investigation 2005 V25(3) P199-208 CAPLUS

Predicted Properties (PPROP)

PROPERTY (CODE) | VALUE | CONDITION |NOTE ======+======+======+==== Bioconc. Factor (BCF) |1.0 |pH 1 25 deg C |(1) Bioconc. Factor (BCF) |1.0 |pH 2 25 deg C |(1) Bioconc. Factor (BCF) |1.0 |pH 3 25 deg C |(1) Bioconc. Factor (BCF) |1.0 |pH 4 25 deg C |(1) Bioconc. Factor (BCF) |1.0 |pH 5 25 deg C |(1) Bioconc. Factor (BCF) |1.0 |pH 6 25 deg C |(1) Bioconc. Factor (BCF) |1.0 |pH 7 25 deg C |(1) Bioconc. Factor (BCF) |1.0 |pH 8 25 deg C |(1) Bioconc. Factor (BCF) |1.0 |pH 9 25 deg C |(1) Bioconc. Factor (BCF) |1.07 |pH 10 25 deg C |(1) Boiling Point (BP) |563.3+/-38.0 deg C |760 Torr |(1) Density (DEN) |1.217+/-0.06 g/cm**3 |20 deg C |(1) | |760 Torr | Enthalpy of Vap. (HVAP) |84.66+/-3.0 kJ/mol |760 Torr |(1) Flash Point (FP) |294.5+/-26.8 deg C | |(1) Freely Rotatable Bonds (FRB) |5 | |(1) H acceptors (HAC) |5 | |(1) H donors (HD) |2 | |(1) Hydrogen Donors/Acceptors Sum|7 | |(1) (HDAS) | | | Koc (KOC) |1.0 |pH 1 25 deg C |(1) Koc (KOC) |1.0 |pH 2 25 deg C |(1) Koc (KOC) |1.0 |pH 3 25 deg C |(1) Koc (KOC) |1.0 |pH 4 25 deg C |(1) Koc (KOC) |1.0 |pH 5 25 deg C |(1) Koc (KOC) |1.0 |pH 6 25 deg C |(1) Koc (KOC) |1.0 |pH 7 25 deg C |(1) Koc (KOC) |1.80 |pH 8 25 deg C |(1) Koc (KOC) |12.90 |pH 9 25 deg C |(1) Koc (KOC) |34.49 |pH 10 25 deg C |(1) logD (LOGD) |-2.64 |pH 1 25 deg C |(1) logD (LOGD) |-2.64 |pH 2 25 deg C |(1) logD (LOGD) |-2.64 |pH 3 25 deg C |(1) logD (LOGD) |-2.64 |pH 4 25 deg C |(1) logD (LOGD) |-2.61 |pH 5 25 deg C |(1) logD (LOGD) |-2.45 |pH 6 25 deg C |(1) logD (LOGD) |-1.83 |pH 7 25 deg C |(1) logD (LOGD) |-0.91 |pH 8 25 deg C |(1) logD (LOGD) |-0.06 |pH 9 25 deg C |(1) logD (LOGD) |0.37 |pH 10 25 deg C |(1) logP (LOGP) |0.462+/-0.727 |25 deg C |(1) Mass Intrinsic Solubility |0.57 g/L |25 deg C |(1) (ISLB.MASS) | | | Mass Solubility (SLB.MASS) |713 g/L |pH 1 25 deg C |(1) Mass Solubility (SLB.MASS) |707 g/L |pH 2 25 deg C |(1) Mass Solubility (SLB.MASS) |707 g/L |pH 3 25 deg C |(1) Mass Solubility (SLB.MASS) |704 g/L |pH 4 25 deg C |(1) Mass Solubility (SLB.MASS) |670 g/L |pH 5 25 deg C |(1)

Page 5 of 37 Mass Solubility (SLB.MASS) |457 g/L |pH 6 25 deg C |(1) Mass Solubility (SLB.MASS) |110 g/L |pH 7 25 deg C |(1) Mass Solubility (SLB.MASS) |13 g/L |pH 8 25 deg C |(1) Mass Solubility (SLB.MASS) |1.8 g/L |pH 9 25 deg C |(1) Mass Solubility (SLB.MASS) |0.69 g/L |pH 10 25 deg C |(1) Mass Solubility (SLB.MASS) |0.63 g/L |Unbuffered Water|(1) | |pH 10.32 | | |25 deg C | Molar Intrinsic Solubility |0.0020 mol/L |25 deg C |(1) (ISLB.MOL) | | | Molar Solubility (SLB.MOL) |2.48 mol/L |pH 1 25 deg C |(1) Molar Solubility (SLB.MOL) |2.46 mol/L |pH 2 25 deg C |(1) Molar Solubility (SLB.MOL) |2.46 mol/L |pH 3 25 deg C |(1) Molar Solubility (SLB.MOL) |2.45 mol/L |pH 4 25 deg C |(1) Molar Solubility (SLB.MOL) |2.33 mol/L |pH 5 25 deg C |(1) Molar Solubility (SLB.MOL) |1.59 mol/L |pH 6 25 deg C |(1) Molar Solubility (SLB.MOL) |0.38 mol/L |pH 7 25 deg C |(1) Molar Solubility (SLB.MOL) |0.046 mol/L |pH 8 25 deg C |(1) Molar Solubility (SLB.MOL) |0.0064 mol/L |pH 9 25 deg C |(1) Molar Solubility (SLB.MOL) |0.0024 mol/L |pH 10 25 deg C |(1) Molar Solubility (SLB.MOL) |0.0022 mol/L |Unbuffered Water|(1) | |pH 10.32 | | |25 deg C | Molar Volume (MVOL) |236.1+/-3.0 cm**3/mol|20 deg C |(1) | |760 Torr | Molecular Weight (MW) |287.36 | |(1) pKa (PKA) |12.57+/-0.40 |Most Acidic |(1) | |25 deg C | pKa (PKA) |9.52+/-0.28 |Most Basic |(1) | |25 deg C | Polar Surface Area (PSA) |57.36 A**2 | |(1) Vapor Pressure (VP) |1.03E-12 Torr |25 deg C |(1)

This substance may exist in multiple tautomeric forms. The predicted property values in this table are calculated based upon the displayed form and may therefore differ from experimental values based on the actual tautomeric ratio at equilibrium.

(1) Calculated using Advanced Chemistry Development (ACD/Labs) Software V11.02 ((C) 1994-2015 ACD/Labs)

See HELP PROPERTIES for information about property data sources in REGISTRY. 882 REFERENCES IN FILE CA (1907 TO DATE) 16 REFERENCES TO NON-SPECIFIC DERIVATIVES IN FILE CA 893 REFERENCES IN FILE CAPLUS (1907 TO DATE)

REFERENCE 1

AN 163:323254 CA TI Novel extended release pharmaceutical formulations IN Sommer, Andreas; Zhang, Chengzhi; Carter, John; Arthur, John; Bradbury,

Page 6 of 37 Margaret PA Auspex Pharmaceuticals, Inc., USA SO PCT Int. Appl., 64pp. CODEN: PIXXD2 DT Patent LA English IPCI A61K0009-28 [I] CC 63-6 (Pharmaceuticals) FAN.CNT 1 PATENT NO. KIND DATE APPLICATION NO. DATE ------PI WO 2015120110 A2 20150813 WO 2015-US14545 20150205 W: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW RW: AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR, BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG, BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW, AM, AZ, BY, KG, KZ, RU, TJ, TM PRAI US 2014-61937189 P 20140207 US 2014-61990061 P 20140507 AB The present invention relates to new extended release pharmaceutical compns. and methods of use thereof for the treatment of disorders. A tetrabenazine gastro-erosional extended release tablet contained tetrabenazine 25, mannitol powder 177.9, microcryst. cellulose 59.3, PVP K29/32 14, Tween 80 (Polysorbate 80) 3.8, mannogemρ EZ (spray dried mannitol) 31.5, POLYOXρ N60K 35, and stearate 3.5 mg. ST extended release pharmaceutical formulation tetrabenazine IT Monoamine transporters RL: THU (Therapeutic use); BIOL (Biological study); USES (Uses) (VMAT1 (vesicle monoamine transporter 1), mediated disease; novel pharmaceutical formulations) IT Pharmaceutical excipients (binders, water-sol.; novel pharmaceutical formulations) IT Pharmaceutical tablets (controlled-release; novel pharmaceutical formulations) IT Pharmaceutical excipients (diluents; novel pharmaceutical formulations) IT Surfactants (novel pharmaceutical formulations) IT Polyoxyalkylenes RL: MOA (Modifier or additive use); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (novel pharmaceutical formulations) IT Polymers RL: MOA (Modifier or additive use); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (sustained-release; novel pharmaceutical formulations) IT Controlled-release drug delivery systems (tablets; novel pharmaceutical formulations) IT 9003-01-4D, crosslinked

Page 7 of 37 RL: MOA (Modifier or additive use); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (Carbopol; novel pharmaceutical formulations) IT 851518-71-3 RL: MOA (Modifier or additive use); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (F 351; novel pharmaceutical formulations) IT 1004523-27-6, MK 8122 1004523-27-6D, MK 8122, deuterated analogs RL: THU (Therapeutic use); BIOL (Biological study); USES (Uses) (PPL 100; novel pharmaceutical formulations) IT 9005-63-4D, fatty acid ester RL: MOA (Modifier or additive use); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (Polysorbate; novel pharmaceutical formulations) IT 9004-34-6, Cellulose, biological studies RL: MOA (Modifier or additive use); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (microcryst.; novel pharmaceutical formulations) IT 63-42-3, Lactose 69-65-8, Mannitol 557-04-0, Magnesium stearate 9003-39-8, Polyvinylpyrrolidone 9007-20-9, Carbomer 25322-68-3 264876-68-8, Kollidon SR RL: MOA (Modifier or additive use); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (novel pharmaceutical formulations) IT 50-35-1, 57-27-2, , biological studies 58-46-8, Tetrabenazine 59-42-7, Phenylephrine 59-67-6, , biological studies 59-67-6D, Niacin, produgs, biological studies 59-92-7, Levodopa, biological studies 74-55-5, Ethambutol 76-42-6, Oxycodone 76-57-3, Codeine 90-34-6, Primaquine 99-66-1, Valproic acid 125- 29-1 , Hydrocodone 125-71-3, Dextromethorphan 442-52-4, Clemizole 502-85-2, 591-81-1 768-94-5, Amantadine 1028-33-7, Pentifylline 1200-22-2, Alpha-lipoic acid 3466-75-9, Dihydrotetrabenazine 3613-73-8, Dimeboline 5633-20-5, Oxybutynin 6493-05-6, Pentoxifylline 6740-88-1, Ketamine 19171-19-8, Pomalidomide 21187-98-4, Gliclazide 25451-15-4, Felbamate 28395-03-1, Bumetanide 28860-95-9, Carbidopa 34911-55-2, 38116-29-9 50847- 11-5 , Ibudilast 51322-75-9, Tizanidine 52328-98-0, Dimethylcurcumin 53179-13-8, Pirfenidone 55268-74-1, Praziquantel 58186-27-9, Idebenone 61422-45-5, Carmofur 61869-08-7, Paroxetine 73590-58-6, Omeprazole 73963-72-1, Cilostazol 78919-13-8, Iloprost 81846-19-7, Treprostinil 82626-48-0, 83015-26-3, Atomoxetine 92623-85-3, Milnacipran 93413-62-8 93413-69-5, Venlafaxine 95635-55-5, Ranolazine 102625-70-7, Pantoprazole 103577-45-3, Lansoprazole 103628-46-2, Sumatriptan 105816-04-4, Nateglinide 111974-69-7, Quetiapine 112885-41-3, Mosapride 116539-59-4, Duloxetine 116644-53-2, Mibefradil 117976-89-3, Rabeprazole 119141-88-7, Esomeprazole 120014-06-4, Donepezil 120511-73-1, Anastrozole 121679-13-8, Naratriptan 124937-51-5, Tolterodine 129722-12-9, Aripiprazole 133454-47-4, Iloperidone 133737-32-3, Pagoclone 133865-89-1, Safinamide 136199-02-5, Rolofylline 138112-76-2, Agomelatine 139264-17-8,

Page 8 of 37 Zolmitriptan 143322-58-1, Eletriptan 147536-97-8, Bosentan 152459-95-5, Imatinib 154323-57-6, Almotriptan 155974-00-8, Ivabradine 160970-54-7, Silodosin 162359-55-9, Fingolimod 165800-03-3, Linezolid 168273-06-1, Rimonabant 172732-68-2, Varespladib 175481-36-4, Lacosamide 177036-94-1, Ambrisentan 183321-74-6, Erlotinib 184036-34-8, Sitaxentan 184475-35-2, Gefitinib 191732- 72-6 , Lenalidomide 193275-84-2, Lonafarnib 198904-31-3, Atazanavir 206361-99-1, Darunavir 210101-16-9, Conivaptan 218600-44-3, Bardoxolone 219846-31-8, Radequinil 220620-09-7, Tigecycline 220991-20-8, Lumiracoxib 223673-61-8, Mirabegron 226256-56-0, Cinacalcet 231277-92-2, Lapatinib 252920-94-8, Solabegron 252977-51-8, TPA-023 257933-82-7, Pelitinib 268203-93-6, Udenafil 269055-15-4, Etravirine 274693-27-5, Ticagrelor 274901-16-5, Vildagliptin 284461-73-0, Sorafenib 286456-42-6, L 838417 288383-20-0, Cediranib 302962-49-8, Dasatinib 306296-47-9, Vicriviroc 313682-08-5, Brecanavir 325715-02-4, Indiplon 346688-38-8, Pridopidine 356057-34-6, Darapladib 357336-20-0, Brivaracetam 366789-02-8, Rivaroxaban 376348-65-1, Maraviroc 377727-87-2, Preladenant 389139-89-3, Omadacycline 394730-60-0, Boceprevir 412950-08-4, Rilapladib 443913-73-3, Vandetanib 444731-52-6, Pazopanib 475085-57-5, MRE-269 475086-01-2, NS 304 477600-75-2, Tofacitinib 486460-32-6, Sitagliptin 500287-72-9 503612-47-3, Apixaban 518048-05-0, Raltegravir 592542-59-1, Rigosertib 608141-41-9, Apremilast 616202-92-7, Lorcaserin 625115-55-1, Riociguat 641571-10-0, Nilotinib 656247-17-5, Nintedanib 697761-98-1, Elvitegravir 698387-09-6, Neratinib 698394-73-9, Vercirnon 781649-09-0, Telcagepant 839712-12-8, Cariprazine 841290-81-1, R 406 850649-61-5, Alogliptin 850876-88-9, ITMN-191 868540-17-4, Carfilzomib 871224-64-5, Almorexant 872363-17-2, Dipraglurant 873054-44-5, Ivacaftor 875446-37-0, Anacetrapib 877130-28-4, Filibuvir 877399-52-5, Crizotinib 901119-35-5 918504-65-1, PLX4032 936563- 96-1 , Ibrutinib 941678-49-5, Ruxolitinib 943319-70-8, Ponatinib 951650-22-9, NS 11394 1025504-45-3, NBI-98854 1051375-16-6, Dolutegravir 1088716-70-4 1187594-09-7, Baricitinib 1213669-91-0, CTP 354 1239918-14-9 1240215-77-3 1268605-91-9, CTP-499 1333312-39-2 1393801-57-4, JZP 386 1395951-84-4 1395951-95-7 1415108-06-3 1618086-90-0 1632490-59-5, biological studies 1803129-89-6 1803129-91-0 1803129-93-2 1803129-96-5 1803129-98-7 1803130-00-8 1803130-03-1 1803130-05-3 1803130-07-5 1803130-09-7 1803130-11-1 1803130-13-3 1803130-15-5 1803130-18-8 1803130-21-3 1803130-24-6 1803130-27-9 1803130-31-5 1803130-34-8 1803130-37-1 1803130-40-6 1803130-43-9 1803130-46-2 1803130-49-5 1803130-53-1 1803130-55-3 1803130-59-7 1803130-63-3 1803130-66-6 1803130-70-2 1803130-75-7 1803130-78-0 1803130-80-4 1803130-83-7 1803130-86-0 1803130-90-6 1803130-92-8 1803130-98-4 1803131-01-2 1803131-05-6 1803131-08-9 1803131-11-4 1803131-14-7 1803131-17-0 1803131-20-5 1803131-23-8 1803131-26-1 1803131-29-4 1803131-31-8 1803131-33-0 1803131-35-2 1803131-37-4 1803131-39-6 1803131-42-1 1803131-44-3 1803131-46-5 1803131-48-7 1803131-51-2 1803131-53-4 1803131-55-6 1803131-57-8 1803131-59-0 1803131-61-4 1803131-63-6 RL: THU (Therapeutic use); BIOL (Biological study); USES (Uses)

Page 9 of 37 (novel pharmaceutical formulations) IT 1803131-66-9 1803131-68-1 1803131-70-5 1803131-73-8 1803131-76-1 1803131-78-3 1803131-82-9 1803131-84-1 1803131-87-4 1803131-89-6 1803131-91-0 1803131-93-2 1803131-95-4 1803131-97-6 1803131-99-8 1803132-01-5 1803132-03-7 1803132-05-9 1803132-07-1 1803132-09-3 1803132-11-7 1803132-13-9 1803132-15-1 1803132-17-3 1803132-19-5 1803132-21-9 1803132-23-1 1803132-25-3 1803132-28-6 1803132-31-1 1803132-34-4 1803132-36-6 1803132-38-8 1803132-40-2 1803132-42-4 1803132-44-6 1803132-47-9 1803132-49-1 1803132-51-5 1803132-53-7 1803132-55-9 1803132-57-1 1803132-59-3 1803132-61-7 1803132-64-0 1803132-66-2 1803132-68-4 1803132-70-8 1803132-72-0 1803132-74-2 1803132-76-4 1803132-78-6 1803132-80-0 1803132-82-2 1803132-85-5 1803132-87-7 1803132-89-9 1803132-91-3 1803132-93-5 1803132-95-7 1803132-97-9 1803132-99-1 1803133-01-8 1803133-04-1 1803133-06-3 1803133-08-5 1803133-10-9 1803133-14-3 1803133-17-6 1803133-19-8 1803133-21-2 1803133-23-4 1803133-25-6 1803133-27-8 1803133-29-0 1803133-31-4 1803133-34-7 1803133-36-9 1803133-38-1 RL: THU (Therapeutic use); BIOL (Biological study); USES (Uses) (novel pharmaceutical formulations)

REFERENCE 2

AN 163:263348 CA TI Zolmitriptan nano freeze-dried powder and the production method thereof IN Xu, Jun; Yan, Qidong; Chen, Qi; Wu, Suoxia PA Taizhou Vocational & Technical College, Peop. Rep. China SO Faming Zhuanli Shenqing, 10pp. CODEN: CNXXEV DT Patent LA Chinese IPCI A61K0009-51; A61K0031-422; A61K0047-36; A61P0025-06 CC 63-6 (Pharmaceuticals) FAN.CNT 1 PATENT NO. KIND DATE APPLICATION NO. DATE ------PI CN 104800191 A 20150729 CN 2015-10221303 20150504 PRAI CN 2015-10221303 20150504 AB The invention discloses a kind of Zolmitriptan nano freeze-dried powder and the prepn. method thereof. The zolmitriptan nano freeze-dried powder is composed of Zolmitriptan 1 wt. part, carrier material 6-14 wt. parts and surfactant 90-130 wt. parts. The carrier material comprises one or more of lecithin, stearic acid, monoglyceride, chitosan and poloxamer. The surfactant comprises one or more of Tween 20, Tween 40, Tween 60, Tween 80 and polyoxyethylene castor oil. The prodn. method includes 1) dissolving zolmitriptan and carrier material in org. solvent under ultrasonic processing or stirring to obtain org. phase soln. A, 2) adding surfactant in purified water, stirring to obtain aq. soln. B, 3) slowly drop adding org. phase soln. A into aq. soln. B, mixing to obtain mixed soln. C, stirring to obtain emulsion D, 4) rotary evapg. emulsion D or evapg. org. solvent in 50-60°C bath to obtain zolmitriptan nanoparticle aq. soln., and 5) adding protecting agent into the zolmitriptan nanoparticle aq. soln., and freeze-drying to obtain zolmitriptan nanometer freeze-dried powder. The freeze-drying step

Page 10 of 37 includes prefreezing the zolmitriptan nanoparticle aq. soln. at -40°C for 6-12 h, turning on heating and vacuum system, sublimation drying, maintaining at -25°C for 4-6 h, maintaining at -15°C for 4-6 h, maintaining at 0°C for 4-6 h, maintaining at 15°C for 4-6 h, and drying at 25°C for 2-3 h. The org. solvent in step 1) is abs. ethanol, Et acetate or iso-Pr alc. The protecting agent comprises one or more of lactose, mannitol, dextran and sucrose. The carrier material and surfactant selected by the present invention, with good biocompatibility and low toxicity in vivo, is ideal adjuvant. By method of the present invention, Zolmitriptan is taken to load in solid lipid, and after being made into lyophilized powder so that it's dispersion is increased, and the stability is increased, and the bioavailability of Zolmitriptan is improved, and its drug effect can play at nanometer level. By removing org. solvent, it avoids org. solvent residual problem, gained Zolmitriptan nano freeze-dried powder of the present invention can be directly prepd. into oral freeze-dried powder prepn., and it is possible to make granule, tablet or capsule used in clin. medicine. ST zolmitriptan nano freeze dried powder prodn IT Castor oil RL: MOA (Modifier or additive use); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (ethoxylated; zolmitriptan nano freeze-dried powder and the prodn. method thereof) IT Freeze-dried drug delivery systems Migraine Pharmaceutical nanoparticles Pharmaceutical powders (zolmitriptan nano freeze-dried powder and the prodn. method thereof) IT Lecithins Monoglycerides RL: MOA (Modifier or additive use); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (zolmitriptan nano freeze-dried powder and the prodn. method thereof) IT 57-11-4, Stearic acid, biological studies 57-50-1, Sucrose, biological studies 63-42-3, Lactose 64-17-5, Ethanol, biological studies 67-63-0, Isopropyl , biological studies 69-65-8, D-Mannitol 141-78-6, Ethyl acetate, biological studies 9004-54-0, Dextran, biological studies 9005-64-5, Tween 20 9005-65-6, Tween 80 9005- 66-7 , Tween 40 9005-67-8, Tween 60 9012-76-4, Chitosan 106392-12-5, Poloxamer RL: MOA (Modifier or additive use); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (zolmitriptan nano freeze-dried powder and the prodn. method thereof) IT 139264-17-8, Zolmitriptan RL: THU (Therapeutic use); BIOL (Biological study); USES (Uses) (zolmitriptan nano freeze-dried powder and the prodn. method thereof)

REFERENCE 3

AN 163:156891 CA TI Compositions and methods of treatment for mycosis fungoides comprising a tryptamine-based drug that acts as a 5-hydroxytryptamine-1 inhibitor

Page 11 of 37 IN Dascalu, Avi PA Israel SO PCT Int. Appl., 32pp. CODEN: PIXXD2 DT Patent LA English IPCI A61K0031-403 [I]; A61K0031-4045 [I]; A61K0031-4196 [I]; A61K0031-422 [I]; A61K0031-4439 [I]; A61K0031-506 [I]; A61P0035-00 [I] CC 1-6 (Pharmacology) FAN.CNT 1 PATENT NO. KIND DATE APPLICATION NO. DATE ------PI WO 2015101839 A1 20150709 WO 2014-IB3243 20141230 W: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW RW: AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR, BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG, BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW, AM, AZ, BY, KG, KZ, RU, TJ, TM PRAI US 2014-61922811 P 20140101 AB The present invention provides for a compn. and method comprising a tryptamine based drug that acts as a 5-hydroxytryptamine-1 inhibitor in an amt. sufficient to induce an improvement to mycosis fungoides and wherein the compn. is formulated into a gel, paste, cream, lotion, emulsion, aerosol or ointment for topical application. ST mycosis fungoides treatment hydroxytryptamine inhibitor IT Pharmaceutical excipients (antimicrobials; compns. and methods of treatment for mycosis fungoides comprising a tryptamine-based drug that acts as a hydroxytryptamine-1 inhibitor) IT Antitumor agents Homo sapiens Human Mycosis fungoides Oral drug delivery systems Pharmaceutical carriers Topical drug delivery systems (compns. and methods of treatment for mycosis fungoides comprising a tryptamine-based drug that acts as a hydroxytryptamine-1 inhibitor) IT Pharmaceutical excipients (emollients; compns. and methods of treatment for mycosis fungoides comprising a tryptamine-based drug that acts as a hydroxytryptamine-1 inhibitor) IT Pharmaceutical excipients (moisturizers; compns. and methods of treatment for mycosis fungoides comprising a tryptamine-based drug that acts as a hydroxytryptamine-1

Page 12 of 37 inhibitor) IT Preservatives (pharmaceutical; compns. and methods of treatment for mycosis fungoides comprising a tryptamine-based drug that acts as a hydroxytryptamine-1 inhibitor) IT Pharmaceutical excipients (preservatives; compns. and methods of treatment for mycosis fungoides comprising a tryptamine-based drug that acts as a hydroxytryptamine-1 inhibitor) IT Pharmaceutical excipients (surfactants; compns. and methods of treatment for mycosis fungoides comprising a tryptamine-based drug that acts as a hydroxytryptamine-1 inhibitor) IT Pharmaceutical excipients (thickeners; compns. and methods of treatment for mycosis fungoides comprising a tryptamine-based drug that acts as a hydroxytryptamine-1 inhibitor) IT 50-67-9, 5-Hydroxytryptamine, biological studies RL: BSU (Biological study, unclassified); BIOL (Biological study) (compns. and methods of treatment for mycosis fungoides comprising a tryptamine-based drug that acts as a hydroxytryptamine-1 inhibitor) IT 61-54-1D, Tryptamine, analogs 103628-46-2, Sumatriptan 121679-13-8, Naratriptan 139264-17-8, Zolmitriptan 143322-58-1, Eletriptan 144034-80-0, Rizatriptan 154323-57-6, Almotriptan 158747-02-5, Frovatriptan RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (compns. and methods of treatment for mycosis fungoides comprising a tryptamine-based drug that acts as a hydroxytryptamine-1 inhibitor) RE.CNT 3 THERE ARE 3 CITED REFERENCES AVAILABLE FOR THIS RECORD (1) SHARPE RICHARD J; WO 9102527 A1 1991 CAPLUS (2) Vermeer, M; Journal Of The American Academy Of Dermatology, 10.1016/S0190-9622(96)90696-9 1996, V35(4), P635 MEDLINE (3) YU RUEY J; US 20070161543 A1 2007

REFERENCE 4

AN 163:111307 CA TI Menstrual migraine: an updated review on hormonal causes, prophylaxis and treatment AU Silberstein, Stephen; Patel, Sumit CS Jefferson Headache Center, Philadelphia, PA, 19107, USA SO Expert Opinion on Pharmacotherapy (2014), 15(14), 2063-2070 CODEN: EOPHF7; ISSN: 1465-6566 PB Informa Healthcare DT Journal; General Review; (online computer file) LA English CC 1-0 (Pharmacology) AB Introduction: In this article, we will discuss pure menstrual migraine without aura (PMM) and menstrually related migraine without aura (MRM). Depending on the frequency and severity of their attacks, patients with

Page 13 of 37 PMM will likely need an acute treatment and/or short-term preventive plan. Of note, with the use of acute treatments and short-term preventive therapy there is risk of overuse if the patient does have pure menstrual migraine and is being treated for menstrually related migraine. Areas covered: A PubMed, Cochrane Central, Medline, Ovid search provided articles relating to menstrual migraine pathophysiol. and treatment. Expert opinion: Long-term daily preventive treatment should be considered for patients with MRM and those with severe PMM. Miniprophylaxis can be used in PMM rather than daily preventive treatment. When considering the use of short-term miniprophylaxis, sumatriptan, zolmitriptan, naratriptan, and frovatriptan have shown efficacy; however, frovatriptan appears to be the triptan of choice based on overall efficacy. Oral contraceptives may be considered if patients do not respond to or cannot tolerate typical migraine preventive . In patients with migraine with aura, oral contraceptives should be used with caution as this may add to the risk of stroke in this population. ST review menstrual migraine hormone prophylaxis IT Homo sapiens Human Menstruation Stroke (menstrual migraine: an updated review on hormonal causes, prophylaxis and treatment) IT Migraine (menstrual; menstrual migraine: an updated review on hormonal causes, prophylaxis and treatment) IT Contraceptives (oral; menstrual migraine: an updated review on hormonal causes, prophylaxis and treatment) IT 103628-46-2, Sumatriptan 121679-13-8, Naratriptan 139264-17-8, Zolmitriptan 158747-02-5, Frovatriptan RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (menstrual migraine: an updated review on hormonal causes, prophylaxis and treatment) RE.CNT 45 THERE ARE 45 CITED REFERENCES AVAILABLE FOR THIS RECORD (1) Allais, G; Cephalalgia 2011, V31, P144 (2) Allais, G; Neurol Sci 2006, V27(Suppl 2), PS193 (3) Allais, G; Neurol Sci 2007, V28(Suppl 2), PS225 (4) Allais, G; Neurol Sci 2008, V29(Suppl 1), PS186 (5) Allais, G; Neurol Sci 2011, V32(Suppl 1), PS99 (6) Bartolini, M; J Headache Pain 2012, V13, P401 CAPLUS (7) Brandes, J; Cephalalgia 2009, V29, P1133 MEDLINE (8) Casolla, B; Curr Pain Headache Rep 2012, V16(5), P445 (9) Coffee, A; J Womens Health (Larchmt) 2014, V23(4), P310 (10) De Lignieres, B; Br Med J(Clin Res Ed) 1986, V293(6561), P1540 MEDLINE (11) Diamond, M; Headache 2008, V48, P248

Page 14 of 37 (12) D'Alessandro, R; Cephalagia 1983, V3(Suppl 1), P156 (13) Facchinetti, F; Gynecol Endocrinol 2010, V26, P773 CAPLUS (14) Facchinetti, F; Headache 1991, V31(5), P298 MEDLINE (15) Goldstein, M; Advances in neurology 1982, P377 MEDLINE (16) Granella, F; Headache 1993, V33(7), P385 MEDLINE (17) Guidotti, M; J Headache Pain 2007, V8, P283 CAPLUS (18) Hu, Y; Headache Pain 2013, V14(1), P7 (19) LaGuardia, K; Fertil Steril 2005, V83(6), P1875 (20) Landy, S; Int J Clin Pract 2004, V58, P913 CAPLUS (21) Lipton, R; Neurology 1993, V43(6 Suppl 3), PS6 MEDLINE (22) Loder, E; Headache 2004, V44, P120 (23) MacGregor, E; Curr Med Res Opin 2004, V20(7), P1143 MEDLINE (24) MacGregor, E; Neurology 2006, V67, P2159 CAPLUS (25) Mannix, L; Headache 2007, V47, P1037 (26) Mannix, L; Obstet Gynecol 2009, V114, P106 (27) Martin, V; Headache 2008, V48, P226 (28) Massiou, H; Eur J Neurol 2005, V12, P774 MEDLINE (29) Moschiano, F; Neurol Sci 2005, V26(Suppl 2), PS162 (30) Negro, A; Expert Rev Neurother 2014, V14(5), P493 CAPLUS (31) Nett, R; Headache 2008, V48, P1194 (32) Nett, R; Obstet Gynecol 2003, V102, P835 CAPLUS (33) Newman, L; Headache 2001, V41, P248 MEDLINE (34) Newman, L; Neurology 1998, 51, P307 (35) Pfaffenrath, V; Cephalalgia 1993, V13(Suppl 13), P244 (36) Savi, L; J Headache Pain 2011, V12, P609 CAPLUS (37) Schreiber, C; Clin Ther 2007, V29(Suppl), P2511 (38) Silberstein, S; Headache 2002, V42, P917 (39) Silberstein, S; Neurology 1991, V41, P775 (40) Silberstein, S; Neurology 2004, V63, P261 CAPLUS (41) Silberstein, S; Obstet Gynecol 2000, P237 CAPLUS (42) Stewart, W; Neurology 2000, V55(10), P1517 MEDLINE (43) Tuchman, M; CNS Drugs 2006, V20, P1019 CAPLUS (44) Tuchman, M; CNS Drugs 2008, V22, P877 CAPLUS (45) Wade, A; Clin Drug Investig 2009, V29, P325 CAPLUS

REFERENCE 5

AN 162:663617 CA TI Identification and characterization of unknown impurity in zolmitriptan tablets by a sensitive HPLC method AU Reddy, A. S.; Reddy, R. C.; Venkateswarlu, P. CS Physico-Chemical Laboratory, Department of Chemistry, S.V. University, Tirupathi, Andhra Pradesh, India SO Journal of Chemical and Pharmaceutical Research (2014), 6(12), 548-553, 6 pp. CODEN: JCPRC5; ISSN: 0975-7384 URL: http://jocpr.com/vol6-iss12-2014/JCPR-2014-6-12-548-553.pdf PB Journal of Chemical and Pharmaceutical Research DT Journal; (online computer file) LA English CC 64-3 (Pharmaceutical Analysis) AB A sensitive and accurate high performance liq. chromatog. (HPLC) method was developed and validated to identify and characterize the unknown impurity found in zolmitriptan tablets during investigation of stability

Page 15 of 37 samples. The successful sepn. was achieved by using Inertsil ODS-3V, 150x4.6 mm, 5μm HPLC column with phosphate buffer (pH 3.0) as a mobile phase-A and methanol as mobile phase-B and detector wavelength at 225 nm. The gradient flow as delivered at a flow rate of 1.5 mL/min. The method was established by detg. limit of detection and limit of quantification. The linearity and accuracy has been demonstrated at a range of LOQ to 400% and 50 to 200% of specification level resp. The drug product was subjected to various stress conditions and proved the method stability indicating nature. ST zolmitriptan tablet high performance liq chromatog method IT HPLC Pharmaceutical tablets (identification and characterization of unknown impurity in zolmitriptan tablets by sensitive high performance liq. chromatog. method) IT 139264-17-8, Zolmitriptan RL: ANT (Analyte); ANST (Analytical study) (identification and characterization of unknown impurity in zolmitriptan tablets by sensitive high performance liq. chromatog. method) RE.CNT 12 THERE ARE 12 CITED REFERENCES AVAILABLE FOR THIS RECORD (1) Anon; ICH guidance on "Impurities in drug products" Q3B (R2) (2) Anon; Q2A, ICH Harmonized Tripartite Guideline 1994 (3) Anon; Q2B, ICH Harmonized Tripartite Guideline 1996 (4) Bhowmik, D; J Chem Pharm Res 2009, V1(1), P163 CAPLUS (5) Hu, Y; J Zhejiang Univ Med Sci 2004, V33, P37 CAPLUS (6) Mallikarjuna Rao, B; J Pharm Biomed Anal 2005, V39, P503 (7) Oldman, A; Pain 2002, V97, P247 CAPLUS (8) Reddy, A; J Chem Pharm Res 2012, V4(7), P3659 CAPLUS (9) Sampath kumar, K; J Chem Pharm Res 2009, V1(1), P72 (10) Srinivasu, M; J Pharm Biomed Anal 2005, V37, P453 CAPLUS (11) Srinivasu, T; Drug Inven Today 2012, V4(9), P450 (12) Yates, R; J Clin Pharmacol 2002, V42(11), P1237 CAPLUS

REFERENCE 6

AN 162:663467 CA TI Orally disintegrating porous film comprising pharmacological active ingredient and method for preparing the same IN Oh, Dong Hoon; Lee, Jin Hoo; Lee, So Yi; Kang, Jun Hyuk; Lim, Chae Yun; Jung, Kyung Tae; Yeon, Kyu Jeong; Park, Jin Gyu PA Seoul Pharma. Co., Ltd., S. Korea SO PCT Int. Appl., 30pp. CODEN: PIXXD2 DT Patent LA Korean IPCI A61K0009-70 [I]; A61P0003-10 [I]; A61P0003-04 [I] IPCR A61K0009-70 [I]; A61P0003-04 [I]; A61P0003-10 [I] CC 63-6 (Pharmaceuticals) FAN.CNT 2 PATENT NO. KIND DATE APPLICATION NO. DATE ------PI WO 2015072684 A1 20150521 WO 2014-KR10293 20141030

Page 16 of 37 W: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW RW: AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR, BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG, BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW, AM, AZ, BY, KG, KZ, RU, TJ, TM KR 1407922 B1 20140617 KR 2013-138040 20131114 PRAI KR 2013-138040 A 20131114 AB The present invention relates to an orally disintegrating porous film and a method for prepg. the same, the film comprising a foaming agent, a foam stabilizing agent, a plasticizer, and pharmacol. active ingredient. The orally disintegrating porous film according to the present invention has micropores within the film and phys. properties suitable for a film, so that the film has an effect of significantly improving the dissoln. rate of a drug and has good processability since the film can be easily prepd. at low cost and through a simplified prepn. method. ST buccal porous film disintegration drug delivery IT Buccal drug delivery systems (films; orally disintegrating porous film comprising pharmacol. active substance and its manufg. method) IT Male reproductive system disease Sexual disorders (impotence; orally disintegrating porous film comprising pharmacol. active substance and its manufg. method) IT Analgesics Anti-inflammatory agents Antianemic agents Antiarthritics Antibiotics Anticonvulsants Antidepressants Antidiabetic agents Antiemetics Antihistamines Antiobesity agents Antiosteoporotic agents Antipsychotics Antipyretics Antitumor agents Antiulcer agents Bending strength Brain disease Cardiovascular agents Common cold Dissolution Expectorants

Page 17 of 37 Foaming agents Gastrointestinal agents Hypnotics and Sedatives Immunosuppressants Lactic acid bacteria Laxatives Mouthwashes Muscle relaxants Nervous system agents Nutrients Porosity Schizophrenia Vaccines (orally disintegrating porous film comprising pharmacol. active substance and its manufg. method) IT Alditols Enzymes Hormones, animal Lecithins Medium-chain fatty acids Polyoxyalkylenes Vitamins RL: THU (Therapeutic use); BIOL (Biological study); USES (Uses) (orally disintegrating porous film comprising pharmacol. active substance and its manufg. method) IT 50-02-2, Dexamethasone 50-58-8, Phendimetrazine tartrate 50-81-7, L-Ascorbic acid, biological studies 54-11-5, Nicotine 55-63-0, Nitroglycerin 56-81-5, Glycerin, biological studies 56-81-5D, Glycerin , fatty acid esters 57-50-1D, Sucrose, fatty acid esters 57-55-6, Propylene glycol, biological studies 58-08-2, Caffeine, biological studies 61-76-7, Phenylephrine hydrochloride 90-84-6, Diethylpropion 94-09-7, Benzocaine 102-76-1, Triacetin 103-90-2, Acetaminophen 113-92-8 123-03-5, Cetylpyridinium chloride 124-90-3, Oxycodone hydrochloride 125-69-9, Dextromethorphan 147-24-0, Diphenhydramine hydrochloride 345-78-8, Pseudoephedrine hydrochloride 357-08-4, hydrochloride 437-38-7, Fentanyl 562-10-7 569-65-3, Meclizine 797-63-7, 1134-47-0, 1197-21-3, Phentermine hydrochloride 1508-65-2, Oxybutynin hydrochloride 2216-51-5, L-Menthol 7232-21-5, Metoclopramide hydrochloride 7384-98-7, Propylene glycol dicaprylate 8050-81-5, Simethicone 9000-30-0, Guar gum 9000-40-2, Locust bean gum 9000-69-5, Pectin 9003-20-7, Polyvinyl acetate 9004-65-3, Hydroxypropyl methyl cellulose 9005-25-8, Starch, biological studies 9005-25-8D, Starch, derivs. 9005-32-7, Alginic acid 9057-02-7, Pullulan 11138-66-2, Xanthan gum 12441-09-7D, Sorbitan, fatty acid esters 14611-52-0, Selegiline hydrochloride 15307-86-5, Diclofenac 15687-27-1, Ibuprofen 16679-58-6, Desmopressin 22071-15-4, Ketoprofen 22232-71-9, Mazindol 23828-92-4, Ambroxol hydrochloride 25322-68-3, Polyethylene oxide 27848-84-6, Nicergoline 28911-01-5, Triazolam 28981-97-7, Alprazolam 31565-12-5, Propylene glycol monocaprylate 34552-83-5, Loperamide hydrochloride 37220-82-9, Glycerol oleate 41100-52-1, Memantine hydrochloride 51481-61-9, 52485-79-7, Buprenorphine 56211-40-6, Torasemide 59729-32-7, Citalopram hydrobromide 64461-82- 1, Tizanidine hydrochloride 66357-59-3, Ranitidine hydrochloride

Page 18 of 37 71125-38-7, Meloxicam 72797-41-2, Tianeptine 73590-58-6, Omeprazole 76824-35-6, Famotidine 77883-43-3, Doxazosin mesylate 79794-75-5, Loratadine 82248-59-7, Atomoxetine hydrochloride 82626-48-0, Zolpidem 83480-29-9, Voglibose 83881-52-1, Cetirizine hydrochloride 84057-84- 1, Lamotrigine 87333-19-5, Ramipril 90729-43-4, Ebastine 93479-97-1, Glimepiride 97240-79-4, 99614-01-4, Ondansetron hydrochloride 99614-02-5, Ondansetron 100299-08-9, Pemirolast potassium 100643-71-8, Desloratadine 103577-45-3, Lansoprazole 103628-46-2, Sumatriptan 106133-20-4, Tamsulosin 106266-06-2, Risperidone 109889-09-0, Granisetron 112885-41-3, Mosapride 119356-77-3, Dapoxetine 120011-70-3, Donepezil hydrochloride 129722-12-9, Aripiprazole 132539-06-1, Olanzapine 132907-72-3, Ramosetron hydrochloride 139264-17-8, Zolmitriptan 139755-83-2, Sildenafil 140462-76-6, Olopatadine hydrochloride 144034-80-0, Rizatriptan 144689-63-4, Olmesartan medoxomil 151767-02-1, Montelukast sodium 153439-40-8, Fexofenadine hydrochloride 158966-92-8, Montelukast 170729-80-3, Aprepitant 171596-29-5, Tadalafil 171599-83-0, Sildenafil citrate 219861-08-2, Escitalopram oxalate 224785-91-5, Vardenafil hydrochloride 242478-38-2, Solifenacin succinate 246852-12-0, Amlodipine mesylate 268203-93-6, Udenafil 286930-03- 8, Fesoterodine fumarate 385367-47-5, Tarafenacin 823178-28-5 862189-96-6 RL: THU (Therapeutic use); BIOL (Biological study); USES (Uses) (orally disintegrating porous film comprising pharmacol. active substance and its manufg. method) RE.CNT 6 THERE ARE 6 CITED REFERENCES AVAILABLE FOR THIS RECORD (1) Anon; KR 100627199 B1 2006 (2) Anon; KR 101320058 B1 2013 (3) BESS WILLIAM S; US 7067116 B1 2006 CAPLUS (4) GENERAL SASCHA; KR 20110044752 A 2011 (5) JEONG HYUN JUN; KR 20130100037 A 2013 CAPLUS (6) TALWAR MUNISH; US 20110086070 A1 2011

REFERENCE 7

AN 162:582739 CA TI Formulation, evaluation and optimization of taste masked zolmitriptan orally disintegrating tablets prepared by direct compression method using different super disintegrating agents AU Janakidevi, S.; Ramanamurthy, K. V. CS A.U. College of Pharmaceutical Sciences, Andhra University, Andhra Pradesh, 530003, India SO World Journal of Pharmacy and Pharmaceutical Sciences (2014), 3(7), 1480-1498, 19 CODEN: WJPPAJ; ISSN: 2278-4357 URL: http://www.wjpps.com/download/article/1404215149.pdf PB World Journal of Pharmacy and Pharmaceutical Sciences DT Journal; (online computer file) LA English

Page 19 of 37 CC 63-6 (Pharmaceuticals) AB The present investigation deals with the formulation of Taste masked orally disintegrating tablets of zolmitriptan that disintegrate in the oral cavity upon contact with saliva and there by improve therapeutic efficacy. It is a bitter drug, used in the treatment of migraine, in order to mask the taste of drug, and to get rapid action, with improved bioavailability, Taste masked orally disintegrating tablets were prepd. Amberlite IPR88 is a cation-exchange resin used to mask the taste by continuous sonication (about 6 h) method. Tablets were prepd. by direct compression method using super disintegrants like crospovidone (F1 to F3), croscarmellose sodium (F4 to F6) and sodium starch glycolate (F7 to F9), designated as nine different types of formulations at different concns. of 2%, 3% and 4% resp. Tablets were evaluated for wt. variation, thickness, disintegration time, drug content, in vitro dissoln., wetting time. Tablets contg. crospovidone 4% (F3) exhibit quick disintegration time than others. The in vitro disintegration time of the optimized tablet was within 30 s and shows 100% release within 15 min. It follows first order release kinetics with diffusion mechanism. ST taste masked zolmitriptan orally disintegrating tablet formulation IT Compressibility Compression Density Dissolution Drug bioavailability Flow Friability Friction Mechanical hardness Oral drug delivery systems Pharmaceutical tablets Saliva Size reduction Thickness Weight Wettability (formulation, evaluation and optimization of taste masked zolmitriptan orally disintegrating tablets prepd. by direct compression method using different super disintegrating agents) IT Flavoring materials (peppermint; formulation, evaluation and optimization of taste masked zolmitriptan orally disintegrating tablets prepd. by direct compression method using different super disintegrating agents) IT Pharmaceutical excipients (taste masking; formulation, evaluation and optimization of taste masked zolmitriptan orally disintegrating tablets prepd. by direct compression method using different super disintegrating agents) IT 9003-39-8D, Crospovidone, crosslinked RL: MOA (Modifier or additive use); PRP (Properties); THU (Therapeutic use); BIOL (Biological study); USES (Uses)

Page 20 of 37 (Crospovidone; formulation, evaluation and optimization of taste masked zolmitriptan orally disintegrating tablets prepd. by direct compression method using different super disintegrating agents) IT 7631-86-9, Aerosil, biological studies RL: MOA (Modifier or additive use); PRP (Properties); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (colloidal; formulation, evaluation and optimization of taste masked zolmitriptan orally disintegrating tablets prepd. by direct compression method using different super disintegrating agents) IT 63-42-3, Lactose 128-44-9, Sodium saccharine 557-04-0, Magnesium stearate 9063-38-1, Sodium starch glycolate 74811-65-7, Croscarmellose sodium 1703745-90-7, Amberlite IPR 88 RL: MOA (Modifier or additive use); PRP (Properties); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (formulation, evaluation and optimization of taste masked zolmitriptan orally disintegrating tablets prepd. by direct compression method using different super disintegrating agents) IT 139264-17-8, Zolmitriptan RL: THU (Therapeutic use); BIOL (Biological study); USES (Uses) (formulation, evaluation and optimization of taste masked zolmitriptan orally disintegrating tablets prepd. by direct compression method using different super disintegrating agents) IT 9004-34-6, Cellulose, biological studies RL: MOA (Modifier or additive use); PRP (Properties); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (microcryst.; formulation, evaluation and optimization of taste masked zolmitriptan orally disintegrating tablets prepd. by direct compression method using different super disintegrating agents) RE.CNT 19 THERE ARE 19 CITED REFERENCES AVAILABLE FOR THIS RECORD (1) Anon; PiaIvares Masters Thesis of formulation and evaluation of zolmitriptan fast disintegrating tablets prepared by direct compression (2) Asparo, M; US 20080306279 A1 2008 CAPLUS (3) Aurora, S; Headache: The journal of Head and Face Pain 2005, V46, P57 (4) Bhandari, S; Asian Journal of Pharmaceutics 2008, V2(1), P2 (5) Bhushan, S; Indian Drugs 2000, V37, P312 (6) Cooper, J; Tutorial pharmacy 1986, P211 (7) Dandagi, P; Indian Drugs 2005, V42(1), P52 (8) Glen, R; journal of Medicinal Chemistry 1995, V38, P3566 MEDLINE (9) Government of India ministry of health and family welfare; Indian pharmacopoeia, 6th Ed 2010, P185 (10) Higuchi, T; J Pharm Sci 1963, V52, P1145 CAPLUS (11) Korsmeyer, R; Ins J Pharm 1983, V15, P25 CAPLUS (12) Lachman, L; The theory and practice of industrial pharmacy, 3rd Edn 2003, P67 (13) Lindgreen, S; Med Clin North Am 1993, V77, P3 (14) Motohiro, O; US 20010014340 2001 CAPLUS

Page 21 of 37 (15) Rajitha, K; Int J Pharm Sci and Nanotechnol 2009, V1(4), P372 (16) Schiermeir, S; European journal of pharmaceutical sciences 2002, V15, P259 (17) Sreenivas, S; Indian Drugs 2006, V43(1), P35 (18) Wagner, J; J Pharm sci 1969, V58, P1253 CAPLUS (19) Watanabe, Y; Biol Pharm Bull 1995, V18, P1308 CAPLUS

REFERENCE 8

AN 162:520997 CA TI Pharmacological interventions in the treatment of trigeminal neuralgia (TN), glossopharyngeal neuralgia (GN) and trigeminal autonomic cephalalgias (TAC) - a systematic review AU Caroline, Sunitha K.; Arvind, M. CS Department of Oral Medicine and Radiology, Saveetha Dental College & Hospitals, Saveetha University, Chennai, India SO International Journal of Pharma and Bio Sciences (2014), 5(3), 329-335, 8 pp. CODEN: IJPBJ2; ISSN: 0975-6299 URL: http://www.ijpbs.net/current-issue.php PB Muthu Prasanna P. DT Journal; (online computer file) LA English CC 1-11 (Pharmacology) AB Assessing the pain relieving effect of various pharmacol. agents in the treatment of trigeminal neuralgia, glossopharyngeal neuralgia and trigeminal autonomic cephalalgias by carrying out a systematic review of literature. Materials and methods- Electronic search of the Pub Med - MeSH database was undertaken. Hand searches were taken from the back refs. The search yielded a total of 14 articles out of which 4 met articles met the inclusion criteria and the other 10 articles were eliminated. The available literature shows that there is use of intranasal zolmitriptan, sumatriptan and high flow oxygen in the management of pain in trigeminal autonomic cephalalgias. In the treatment of trigeminal neuralgia, oxcarbazepine is the latest drug of known efficacy and safety. In the management of glossopharyngeal neuralgia, no randomized controlled trials were done but exptl. studies reported better results with oxcarbazepine when compared to other drugs. ST trigeminal glossopharyngeal neuralgia autonomic cephalalgia pharmacol intervention IT Headache (chronic paroxysmal hemicrania; intranasal zolmitriptan, sumatriptan is used for treatment of trigeminal autonomic cephalalgias while oxcarbazepine is used for treatment of trigeminal neuralgia and glossopharyngeal neuralgia in human) IT Homo sapiens Human Pain Trigeminal neuralgia (intranasal zolmitriptan, sumatriptan is used for treatment of

Page 22 of 37 trigeminal autonomic cephalalgias while oxcarbazepine is used for treatment of trigeminal neuralgia and glossopharyngeal neuralgia in human) IT 28721-07-5, Oxcarbazepine 103628-46-2, Sumatriptan 139264-17-8, Zolmitriptan RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (intranasal zolmitriptan, sumatriptan is used for treatment of trigeminal autonomic cephalalgias while oxcarbazepine is used for treatment of trigeminal neuralgia and glossopharyngeal neuralgia in human) RE.CNT 21 THERE ARE 21 CITED REFERENCES AVAILABLE FOR THIS RECORD (1) Anis, S; Int J Pharm Bio Sci 2012, V3(3), PP32 (2) Anon; Neurology 2007, P69 (3) Anon; Trigeminal Autonomic Cephalalgias: Diagnosis and Management 2012, VXX(3) (4) Bahra, A; Neurology 2000, V54(9), P1832 CAPLUS (5) Cittadini, E; Arch Neurol 2006, V63(11), P1537 (6) Cohen, A; JAMA 2009, V302(22) CAPLUS (7) Debta, F; Journal of Indian Academy of Oral Medicine and Radiology 2010, V22(1), P10 (8) Hedlund, C; Headache, 10.1111/j.1526-4610.2009.01518.x 2009, V49(9), P1315 (9) Jadad, A; Control Clin Trials 1996, V17, P1 MEDLINE (10) Jorns, T; British Journal of Neurosurgery 2007, V21(3), P253 MEDLINE (11) Krafft, M; American Family Physician, www.aafp.org/afp 2008, V77(9) (12) Lemos, L; Clin J Pain 2008, V24(1), P64 (13) McQuay, H; Textbook of Pain, Ed 4 1999, P1125 (14) Perez, C; J Clin Pharmacol 2009, V49(5), P582 CAPLUS (15) Rozen, T; Headache 2001, V41(8), P813 MEDLINE (16) Shaikh, S; J Chin Med Assoc 2011, V74(6), P243 CAPLUS (17) Singh, P; Pain Med 2013, V14(1), P93 (18) Tolle, T; Pain Pract 2006, V6(3), P153 (19) van Vliet, J; Neurology 2003, V60, P630 MEDLINE (20) Zakrzewska, J; Expert Opin Pharmacother 2010, V11(9) (21) Zakrzewska, J; Pain 2002, V95(3), P259 CAPLUS

REFERENCE 9

AN 162:492166 CA TI Formulation development and in vivo evaluation of zolmitriptan oral dissolving films AU Kumar, S. Kishore; Nagabhushanam, M. V.; Sambasiva Rao, K. R. S.; Bhikshapathi, D. V. R. N. CS Department of Pharmaceutics, D.C.R.M. Pharmacy College, Andhra Pradesh, 523167, India SO International Journal of Pharma and Bio Sciences (2013), 4(3), 638-654 CODEN: IJPBJ2; ISSN: 0975-6299 URL: http://www.ijpbs.net/cms/php/upload/2459_pdf.pdf PB Muthu Prasanna P. DT Journal; (online computer file) LA English CC 63-6 (Pharmaceuticals) Section cross-reference(s): 1 AB The present study aimed at prepg. fast dissolving oral films of

Page 23 of 37 zolmitriptan as a model drug which is used for the migraine treatment. Fast dissolving dosage forms have acquired great importance in pharmaceutical industry because of their unique properties. In the present research work various trials were carried out using different grades of HPMC E3, E6, and E15, maltodextrin DE6 and other polymers by solvent casting method. The prepd. films were evaluated for film thickness, folding endurance, surface pH, morphol. properties, % drug content and content uniformity, tensile strength, percent elongation, in vitro disintegration time and in vitro dissoln. studies. The optimized formulation F23 prepd. using HPMC E15 showed min. disintegration time (10 s), highest dissoln. rate i.e. 99% of drug within 8 min and satisfactory physicochem. properties. The optimized film was evaluated for its bioavailability compared with pure drug as ref. std. Statistical anal. revealed that no significant difference between the bioavailability parameters of the film and the ref. std. indicated that they exhibited comparable plasma level-time profiles. These findings suggest that the fast dissolving film contg. zolmitriptan is considered to be potentially useful for the treatment of migraine where quick onset of action is desirable. ST migraine zolmitriptan fast dissolving oral film pharmacokinetics IT Blood plasma Dissolution Drug bioavailability Elongation, mechanical Flexibility Migraine Oral drug delivery systems Pharmaceutical films Pharmacokinetics Size reduction Stability Surface structure Tensile strength Thickness Weight pH (formulation of fast dissolving oral films of zolmitriptan which is used for migraine treatment and evaluation of pharmacokinetic properties of these films in rabbit in vivo) IT 9050-36-6, Maltodextrin RL: MOA (Modifier or additive use); PRP (Properties); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (DE6; formulation of fast dissolving oral films of zolmitriptan which is used for migraine treatment and evaluation of pharmacokinetic properties of these films in rabbit in vivo) IT 9004-65-3 RL: MOA (Modifier or additive use); PRP (Properties); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (E15 and E3; formulation of fast dissolving oral films of zolmitriptan which is used for migraine treatment and evaluation of pharmacokinetic properties of these films in rabbit in vivo) IT 57-55-6, Propylene glycol, biological studies 77-92-9, Citric acid, biological studies 121-33-5, Vanillin 915-67-3, Amaranth 11138-66- 2,

Page 24 of 37 Xanthan gum 22839-47-0, Aspartame RL: MOA (Modifier or additive use); PRP (Properties); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (formulation of fast dissolving oral films of zolmitriptan which is used for migraine treatment and evaluation of pharmacokinetic properties of these films in rabbit in vivo) IT 139264-17-8, Zolmitriptan RL: PKT (Pharmacokinetics); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (formulation of fast dissolving oral films of zolmitriptan which is used for migraine treatment and evaluation of pharmacokinetic properties of these films in rabbit in vivo) RE.CNT 18 THERE ARE 18 CITED REFERENCES AVAILABLE FOR THIS RECORD (1) Alpesh, R; Int J of Drug Dev & Res 2010, V2(2), P232 (2) Chugh, I; Int Res J of Phar 2010, V3(5), P57 (3) Galey, W; J Inves Dermatol 1976, V67(6), P713 CAPLUS (4) Kumar, G; Ind J Pharm Sci 2005, V67, P160 (5) Kunte, S; J Pharm Bioallied Sci 2010, V2(4), P325 CAPLUS (6) Lipton, R; Am J Med 2005, V11(8), PS3 (7) Mashru, R; Drug Dev Ind Pharm 2005, V31, P25 CAPLUS (8) Mital, S; Int J of Phar Res & Allied Sci 2012, V1(3), P60 (9) Nafee, N; Acta Pharm 2003, V53, P199 CAPLUS (10) Nagar, M; Der Phar Lettre 2012, V4(4), P1221 CAPLUS (11) Nagaraju, R; Ind J pharm edu and res 2012, V46(4), P318 (12) Nehal Siddiqui, M; Advances in Biological Research 2011, V5(6), P291 (13) Prabhu, P; Int J Pharm Inves 2011, V1(2), P99 CAPLUS (14) Rang, H; Rang And Dales Pharmacology, sixth edition P195 (15) Sheryl, R; Lancet Neurol 2006, V5, P148 (16) Shimoda, H; Eur J Pharm Biopharm 2009, V73(3), P361 CAPLUS (17) Silberstein, S; Lancet 2004, V363, P381 CAPLUS (18) Spencer, C; Drugs 1999, V58(2), P347 CAPLUS

REFERENCE 10

AN 162:468029 CA TI FDA-approved drugs and other compounds tested as inhibitors of human glutathione transferase P1-1 AU Musdal, Yaman; Hegazy, Usama M.; Aksoy, Yasemin; Mannervik, Bengt CS Department of Chemistry-BMC, Uppsala University, Uppsala, SE-75123, Swed. SO Chemico-Biological Interactions (2013), 205(1), 53-62 CODEN: CBINA8; ISSN: 0009-2797 PB Elsevier Ireland Ltd. DT Journal; (online computer file) LA English CC 1-4 (Pharmacology) AB Glutathione transferase P1-1 (GST P1-1) is often overexpressed in tumor cells and is regarded as a contributor to their drug resistance. Inhibitors of GST P1-1 are expected to counteract drug resistance and may therefore serve as adjuvants in the chemotherapy of cancer by increasing the efficacy of cytostatic drugs. Finding useful inhibitors among compds. used for other indications would be a shortcut to clin. applications and a

Page 25 of 37 search for GST P1-1 inhibitors among approved drugs and other compds. was therefore conducted. We tested 1040 FDA-approved compds. as inhibitors of the catalytic activity of purified human GST P1-1 in vitro. We identified chlorophyllide, merbromine, hexachlorophene, and ethacrynic acid as the most effective GST P1-1 inhibitors with IC50 values in the low micromolar range. For comparison, these compds. were even more potent in the inhibition of human GST A3-3, an enzyme implicated in steroid hormone biosynthesis. In distinction from the other inhibitors, which showed conventional inhibition patterns, the competitive inhibitor ethacrynic acid elicited strong kinetic cooperativity in the glutathione satn. of GST P1-1. Apparently, ethacrynic acid serves as an allosteric inhibitor of the enzyme. In their own right, the compds. investigated are less potent than desired for adjuvants in cancer chemotherapy, but the structures of the most potent inhibitors could serve as leads for the synthesis of more efficient adjuvants. ST recombinant glutathione transferase P11 inhibitor adjuvant chemotherapy IT Homo sapiens Human (FDA-approved drugs and other compds. were tested as potent inhibitors of recombinant human glutathione transferase P1-1) IT Tannins RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (FDA-approved drugs and other compds. were tested as potent inhibitors of recombinant human glutathione transferase P1-1) IT Quaternary ammonium compounds RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (alkylbenzyldimethyl, chlorides; FDA-approved drugs and other compds. were tested as potent inhibitors of recombinant human glutathione transferase P1-1) IT Chlorophyllides RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (chlorophyllide, merbromin, hexachlorophene and ethacrynic acid were most effective inhibitors of recombinant human glutathione transferase P1-1) IT 1418151-15-1, Glutathione S-transferase π RL: BSU (Biological study, unclassified); BIOL (Biological study) (FDA-approved drugs and other compds. were tested as potent inhibitors of recombinant human glutathione transferase P1-1) IT 50-02-2, Dexamethasone 50-03-3, Hydrocortisone acetate 50-04-4, Cortisone acetate 50-07-7, Mitomycin c 50-14-6, Ergocalciferol 50-23-7, Hydrocortisone 50-24-8, Prednisolone 50-27-1, Estriol 50-28-2, , biological studies 50-33-9, Phenylbutazone,

Page 26 of 37 biological studies 50-34-0, Propantheline bromide 50-35-1, Thalidomide 50-41-9, Clomiphene citrate 50-42-0, Adiphenine hydrochloride 50-44-2, Mercaptopurine 50-50-0, Estradiol benzoate 50-53-3, Chlorpromazine, biological studies 50-55-5, Reserpine 50-63-5, Chloroquine diphosphate 50-65-7, Niclosamide 50-76-0, Dactinomycin 50-78-2, Aspirin 50-81-7, L-Ascorbic acid, biological studies 50-91- 9, Floxuridine 51-05-8, Procaine hydrochloride 51-12-7, Nialamide 51-15-0, Pralidoxime chloride 51-21-8, Fluorouracil 51-30-9, Isoproterenol hydrochloride 51-41-2, Norepinephrine 51-42-3, Adrenaline bitartrate 51-48-9, Levothyroxine, biological studies 51-52-5, Propylthiouracil 51-56-9, Homatropine bromide 51-75-2, Mechlorethamine 51-83-2, Carbachol 51-84-3, Acetylcholine, biological studies 51-98-9, Norethindrone acetate 52-01-7, 52-21-1, Prednisolone acetate 52-24-4, Thiotepa 52-49-3, Trihexyphenidyl hydrochloride 52-67-5, Penicillamine 52-68-6, Trichlorfon 52-86-8, Haloperidol 52-88-0, Methylatropine nitrate 53-03-2, Prednisone 53-16-7, Estrone, biological studies 53-19-0, Mitotane 53-60-1, Promazine hydrochloride 53-84-9, Nadide 53-86-1, Indomethacin 54-21-7, Sodium salicylate 54-31-9, 54-64- 8, Thimerosal 54-85-3, Isoniazid 54-91-1, Pipobroman 54-95-5, 55-06-1, Liothyronine sodium 55-48-1, Atropine sulfate 55-56-1, Chlorhexidine 55-98-1, Busulfan 56-47-3, Desoxycorticosterone acetate 56-53-1, Diethylstilbestrol 56-75-7, Chloramphenicol 56-85-9, L-, biological studies 56-92-8, Histamine dihydrochloride 57-13-6, Urea, biological studies 57-24-9, Strychnine 57-33-0 57-57-8, β-Propiolactone 57-63-6, Ethinyl estradiol 57-64-7, Physostigmine salicylate 57-66-9, Probenecid 57-67-0, Sulfaguanidine 57-68-1, Sulfamethazine 57-83-0, Progesterone, biological studies 57-85-2, propionate 57-88-5, , biological studies 57-94-3, Tubocurarine chloride 57- 96-5 , Sulfinpyrazone 58-08-2, Caffeine, biological studies 58-14-0, Pyrimethamine 58-22-0, Testosterone 58-27-5, Menadione 58-28-6, Desipramine hydrochloride 58-32-2, Dipyridamole 58-33-3, Promethazine hydrochloride 58-39-9, Perphenazine 58-55-9, Theophylline, biological studies 58-58-2, Puromycin hydrochloride 58-61-7, Adenosine, biological studies 58-71-9 58-85-5, Biotin 58-89-9, 58-93-5, Hydrochlorothiazide 58-94-6, Chlorothiazide 58-95-7, α-Tocopheryl acetate 59-02-9, α-Tocopherol 59-05-2, Methotrexate 59-30-3, Folic acid, biological studies 59-33-6, Pyrilamine maleate 59-43-8, Thiamine, biological studies 59-47-2, Mephenesin 59-50-7, Chlorocresol 59-66-5, Acetazolamide 59-67-6, Niacin, biological studies 59-87-0, Nitrofurazone 59-92-7, Levodopa, biological studies 59-97-2, Tolazoline hydrochloride 60-02-6, Guanethidine sulfate 60-12-8, Phenylethyl alcohol 60-46-8, Aminopentamide 60-56-0, Methimazole 60-80-0, Antipyrine 61-12-1, Dibucaine hydrochloride 61-16-5, Methoxamine hydrochloride 61-19-8, Adenosine phosphate, biological studies 61-25-6, Papaverine hydrochloride 61-68-7, 61-73-4, Methylene blue 61-76-7, Phenylephrine hydrochloride 61-78-9 61-80-3, Zoxazolamine

Page 27 of 37 62-31-7, Dopamine hydrochloride 62-38-4, Phenylmercuric acetate 62-44-2, Phenacetin 62-51-1, Methacholine chloride 62-68-0, Proadifen hydrochloride 62-73-7, Dichlorvos 63-45-6, Primaquine diphosphate 63-56-9, Thonzylamine hydrochloride 63-92-3, Phenoxybenzamine hydrochloride 63-98-9, Phenacemide 64-72-2, Chlortetracycline hydrochloride 64-73-3, Demeclocycline hydrochloride 64-75-5, Tetracycline hydrochloride 64-77-7, Tolbutamide 64-86-8, Colchicine 65-19-0, Yohimbine hydrochloride 65-23-6, Pyridoxine 65-29-2, Gallamine triethiodide 65-45-2, Salicylamide 65-85-0, Benzoic acid, biological studies 66-76-2, Dicumarol 66-81-9, Cycloheximide 66- 84-2 , Glucosamine hydrochloride 67-20-9, Nitrofurantoin 67-43-6, Pentetic acid 67-48-1, Choline chloride 67-73-2, Fluocinolone acetonide 67-78-7, Triamcinolone diacetate 67-92-5, Dicyclomine hydrochloride 67-97-0, Cholecalciferol 68-22-4, Norethindrone 68-23-5, Norethynodrel 68-26-8, Retinol 68-35-9, Sulfadiazine 68-41-7, Cycloserine 68-88-2, Hydroxyzine 68-89-3, Dipyrone 69-05-6, Quinacrine hydrochloride 69-44-3, Amodiaquine dihydrochloride 69-52-3, Ampicillin sodium 70-00-8, Trifluridine 71-58-9, Medroxyprogesterone acetate 71-63-6, Digitoxin 71-73-8, Thiopental sodium 71-81-8, Isopropamide iodide 72-14-0, Sulfathiazole 72-33-3, Mestranol 72-69-5, Nortriptyline 73-05-2, Phentolamine hydrochloride 73-22-3, L-Tryptophan, biological studies 73-24-5, Adenine, biological studies 73-48-3, Bendroflumethiazide 73-78-9, Lidocaine hydrochloride 76-22- 2, Camphor 76-25-5, Triamcinolone acetonide 76-90-4, Mepenzolate bromide 77-09-8, Phenolphthalein 77-36-1, Chlorthalidone 77-46-3, Acedapsone 77-67-8, Ethosuximide 78-44-4, Carisoprodol 79-57-2, Oxytetracycline 79-81-2, Retinyl palmitate 80-08-0, Dapsone 80-13-7, Halazone 80-32-0, Sulfachlorpyridazine 80-35-3, Sulfamethoxypyridazine 80-49- 9, Homatropine methylbromide 80-74-0, Sulfisoxazole acetyl 81-07-2, Saccharin 81-13-0, Panthenol 81-23-2, Dehydrocholic acid 81-27-6, Sennoside A 81-81-2, Warfarin 82-92-8, Cyclizine 83-12-5, Phenindione 83-43-2, Methylprednisolone 83-67-0, Theobromine 83- 73-8 , Iodoquinol 83-88-5, Riboflavin, biological studies 84-17-3, Dienestrol 84-80-0, Phytonadione 85-73-4, Phthalylsulfathiazole 86-75-9, Benzoxiquine 87-17-2, Salicylanilide 87-33-2, Isosorbide dinitrate 87-89-8, myo-Inositol 88-04-0, Chloroxylenol 89-57-6, Mesalamine 89-78-1, Menthol 90-01-7, Salicyl alcohol 90-45-9, Aminacrine 90-80-2, Gluconolactone 91-33-8, Benzthiazide 91-64-5, Coumarin 93-14-1, Guaifenesin 94-09-7, Benzocaine 94-20-2, Chlorpropamide 94-25-7, Butamben 94-26-8, Butyl paraben 94-36-0, Benzoyl peroxide, biological studies 94-62-2, Piperine 95-25-0, Chlorzoxazone 96-83-3, Iopanoic acid 97-44-9, Acetarsol 97-53-0, Eugenol 97-59-6, Allantoin 97-77-8, Disulfiram 98-50-0, Arsanilic acid 98-92-0, Niacinamide 98-96-4, Pyrazinamide RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (FDA-approved drugs and other compds. were tested as potent inhibitors

Page 28 of 37 of recombinant human glutathione transferase P1-1) IT 100-97-0, Methenamine, biological studies 101-26-8, Pyridostigmine bromide 101-31-5, Hyoscyamine 102-29-4, Resorcinol monoacetate 102-76-1, Triacetin 103-84-4, Acetanilide 103-90-2, Acetaminophen 104-46-1, Anethole 106-48-9 107-35-7, 108-46-3, Resorcinol, biological studies 110-85-0, Piperazine, biological studies 112-38- 9, Undecylenic acid 113-38-2, Estradiol propionate 113-52-0, Imipramine hydrochloride 113-98-4, G potassium 114-07-8, Erythromycin 114-49-8, Scopolamine hydrobromide 114-80-7, Neostigmine bromide 115-67-3, Paramethadione 116-38-1, Edrophonium chloride 116-43-8, Succinylsulfathiazole 117-10-2, Danthron 117-37-3, Anisindione 117-96-4, Diatrizoic acid 118-10-5, Cinchonine 118-56-9, Homosalate 118-60-5, Octisalate 120-47-8, Ethyl paraben 120-51-4, Benzyl benzoate 121-19-7, Roxarsone 121-25-5, Amprolium 121-54-0, Benzethonium chloride 121-75-5, Malathion 121-81-3, Nitromide 122-09-8, Phentermine 122-11-2, Sulfadimethoxine 123-03-5, Cetylpyridinium chloride 123-31-9, Hydroquinone, biological studies 123-99-9, Azelaic acid, biological studies 124-94-7, Triamcinolone 125-02-0, Prednisolone sodium phosphate 125-33-7, Primidone 125-52-0, Oxyphencyclimine hydrochloride 125-69-9, Dextromethorphan hydrobromide 125-84-8, Aminoglutethimide 126-07-8, Griseofulvin 126-27-2, Oxethazaine 127-07-1, Hydroxyurea 127-69-5, Sulfisoxazole 127-71- 9, Sulfabenzamide 127-79-7, Sulfamerazine 128-13-2, Ursodiol 129-20- 4, Oxyphenbutazone 129-51-1, Ergonovine maleate 129-77-1, Piperidolate hydrochloride 130-16-5, Cloxyquin 130-26-7, Clioquinol 130-61-0, Thioridazine hydrochloride 131-53-3, Dioxybenzone 131-57-7, Oxybenzone 131-69-1, Phthalylsulfacetamide 132-20-7, Pheniramine maleate 132-65-0, Dibenzothiophene 132-69-4, Benzydamine hydrochloride 132-92-3, Methicillin sodium 132-93-4, Phenethicillin potassium 132-98-9, Penicillin V potassium 133-11-9, Phenyl aminosalicylate 133-67-5, Trichlormethiazide 134-62-3, Diethyltoluamide 134-71-4, Racephedrine hydrochloride 135-09-1, Hydroflumethiazide 135-23-9, Methapyrilene hydrochloride 136-40-3, Phenazopyridine hydrochloride 136-47-0, Tetracaine hydrochloride 136-77-6, Hexylresorcinol 137-26- 8, Thiram 137-66-6, Ascorbyl palmitate 138-14-7, Deferoxamine mesylate 138-37-4, Mafenide hydrochloride 138-52-3, Salicin 138-84-1, Potassium P-aminobenzoate 143-67-9, Vinblastine sulfate 144-80-9, Sulfacetamide 144-82-1, Sulfamethizole 145-41-5, Sodium dehydrocholate 145-63-1, Suramin 146-56-5, Fluphenazine hydrochloride 147-24-0, Diphenhydramine hydrochloride 147-94-4, Cytarabine 148-72-1, Pilocarpine nitrate 148-79-8, Thiabendazole 148-82-3, Melphalan 149-16-6, Butacaine 151-67-7, Halothane 151-73-5, Betamethasone sodium phosphate 152-11- 4, Verapamil hydrochloride 153-18-4, Rutin 154-41-6, Phenylpropanolamine

Page 29 of 37 hydrochloride 154-42-7, Thioguanine 154-68-7, Antazoline phosphate 154-93-8, Carmustine 155-41-9, Methscopolamine bromide 156-51-4, Phenelzine sulfate 156-57-0, Cysteamine hydrochloride 297-76-7, Ethynodiol diacetate 298-46-4, 298-57-7 298-59-9, Methylphenidate hydrochloride 298-81-7, Methoxsalen 299-39-8, Sparteine sulfate 300-08-3, Arecoline hydrobromide 302-22-7, 302-27-2, Aconitine 302-79-4, Tretinoin 304-20-1, Hydralazine hydrochloride 304-84-7, Ethamivan 305-03-3, Chlorambucil 306-07-0, Pargyline hydrochloride 313-06-4, Estradiol cypionate 314-19-2, Apomorphine hydrochloride 315-30-0, Allopurinol 318-98-9, Propranolol hydrochloride 319-89-1, Tetroquinone 320-67-2, Azacitidine 333-36-8, 337-47-3, Thiamylal sodium 338-98- 7, Isoflupredone acetate 343-55-5, Dicloxacillin sodium 345-78-8, Pseudoephedrine hydrochloride 356-12-7, Fluocinonide 357-08-4, Naloxone hydrochloride 357-57-3, Brucine 364-98-7, Diazoxide 378-44-9, Betamethasone 379-79-3, Ergotamine tartrate 382-67-2, Desoximetasone 389-08-2, Nalidixic acid 396-01-0, Triamterene 404-86-4, Capsaicin 426-13-1, Fluorometholone 427-51-0, acetate 434-03-7, 440-17-5, Trifluoperazine hydrochloride 443-48-1, Metronidazole 446-86-6, Azathioprine 466-06-8, Proscillaridin 474-25-9, Chenodiol 474-86-2, Equilin 479-18-5, Dyphylline 480-49-9, Filipin 483-18-1, Emetine 483-63-6, Crotamiton 485-71-2, Cinchonidine 486-56-6, Cotinine 502-85-2, Sodium oxybate 504-24-5, Fampridine 514-36-3, Fludrocortisone acetate 514-65-8, Biperiden 518-28-5, Podofilox 521-78-8, Trimipramine maleate 522-48-5, Tetrahydrozoline hydrochloride 523-87-5, Dimenhydrinate 530-43-8, Chloramphenicol palmitate 530-78-9, Flufenamic acid 532- 03-6 , Methocarbamol 536-33-4, Ethionamide 536-93-6, Eucatropine hydrochloride 537-12-2, Diperodon hydrochloride 541-15-1, Levocarnitine 541-22-0, Decamethonium bromide 546-88-3, Acetohydroxamic acid 548-62-9, Gentian violet 548-73-2, Droperidol 549-18-8, Amitriptyline hydrochloride 550-70-9, Triprolidine hydrochloride 550-99-2, Naphazoline hydrochloride 552-94-3, Salsalate 554-57-4, Methazolamide 554-92-7, Trimethobenzamide hydrochloride 555-30-6, Methyldopa 557-08-4, undecylenate 562-10-7 569-57- 3, Chlorotrianisene 579-56-6, Isoxsuprine hydrochloride 581-88-4, Debrisoquine sulfate 586-06-1, Metaproterenol 590-46-5, Betaine hydrochloride 590-63-6, Bethanechol chloride 595-33-5, 596-51-0, Glycopyrrolate 599-79-1, Sulfasalazine 603-50-9, Bisacodyl 606-17-7, Iodipamide 611-75-6, Bromhexine hydrochloride 614-39-1, Procainamide hydrochloride 616-91-1, Acetylcysteine 630- 56-8 , Hydroxyprogesterone caproate 630-60-4, Ouabain 630-93-3, sodium 635-41-6, Trimetozine 637-07-0, Clofibrate 637-32-1, Chloroguanide hydrochloride 637-58-1, Pramoxine hydrochloride 638- 94-8 , Desonide 642-78-4, Cloxacillin sodium 645-05-6, Altretamine 651-06-9, Sulfameter 661-19-8, Docosanol 665-66-7, Amantadine hydrochloride 695-53-4, Dimethadione 723-46-6, Sulfamethoxazole 738-70-5, Trimethoprim 747-36-4, Hydroxychloroquine sulfate 749-02- 0,

Page 30 of 37 Spiperone 751-97-3, Rolitetracycline 773-76-2, Chloroxine 804-63- 7, Quinine sulfate 826-39-1, Mecamylamine hydrochloride 827-61-2, Aceclidine 829-74-3, Levonordefrin 834-28-6, Phenformin hydrochloride 849-55-8, Nylidrin hydrochloride 850-52-2, Altrenogest 859-18-7, Lincomycin hydrochloride 912-60-7, Noscapine hydrochloride 919-16-4, Lithium citrate 967-80-6, Sulfaquinoxaline sodium 968-81-0, Acetohexamide 969-33-5, hydrochloride 976-71-6, 979-32-8, Estradiol valerate 980-71-2, Brompheniramine maleate 985-16-0, Nafcillin sodium RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (FDA-approved drugs and other compds. were tested as potent inhibitors of recombinant human glutathione transferase P1-1) IT 987-24-6, Betamethasone acetate 987-78-0, Citicoline 1069-66-5, sodium 1070-11-7, Ethambutol hydrochloride 1094-08-2, Ethopropazine hydrochloride 1098-60-8, Triflupromazine hydrochloride 1104-22-9, Meclizine hydrochloride 1115-70-4, Metformin hydrochloride 1134-47-0, Baclofen 1143-38-0, Anthralin 1156-19-0, Tolazamide 1173-88-2, Oxacillin sodium 1177-87-3, Dexamethasone acetate 1195- 16-0 , Citiolone 1197-18-8, Tranexamic acid 1212-72-2, Mephentermine sulfate 1218-35-5, Xylometazoline hydrochloride 1220-83-3, Sulfamonomethoxine 1225-55-4, Protriptyline hydrochloride 1227-61-8, Mefexamide 1229-29-4, Doxepin hydrochloride 1257-78-9, Prochlorperazine edisylate 1263-89-4, Paromomycin sulfate 1264-62-6, Erythromycin ethylsuccinate 1264-72-8, Colistin sulfate 1319-77-3, Cresol 1319-82-0, Aminocaproic acid 1327-53-3, Arsenic trioxide 1393-48-2, Thiostrepton 1397-89-3, Amphotericin B 1400-61-9, Nystatin 1404-88-2, Tyrothricin 1405-10-3, Neomycin sulfate 1405-20-5, Polymyxin B sulfate 1405-37-4, Capreomycin sulfate 1405-41-0, Gentamicin sulfate 1405-87-4, Bacitracin 1405-97-6, Gramicidin 1476-53-5, Novobiocin sodium 1492-18-8, Leucovorin 1501-84- 4, Rimantadine hydrochloride 1508-65-2, Oxybutynin chloride 1508-75-4, Tropicamide 1508-76-5, Procyclidine hydrochloride 1524-88-5, Flurandrenolide 1622-61-3, Clonazepam 1642-54-2, Diethylcarbamazine citrate 1649-18-9, Azaperone 1665-48-1, Metaxalone 1684-40-8, Tacrine hydrochloride 1722-62-9, Mepivacaine hydrochloride 1786-81- 8, Prilocaine hydrochloride 1893-33-0, Pipamperone 1944-12-3, Fenoterol hydrobromide 1953-04-4, Galantamine hydrobromide 2002-29-1, Flumethasone pivalate 2016-88-8, hydrochloride 2022-85-7, Flucytosine 2030-63-9, Clofazimine 2062-78-4, Pimozide 2068-78-2, Vincristine sulfate 2078-54-8, 2135-17-3, Flumethasone 2152-44-5, Betamethasone valerate 2203-97-6, Hydrocortisone hemisuccinate 2259-96-3, 2315-02-8, Oxymetazoline hydrochloride 2321-07-5, Fluorescein 2375-03-3, Methylprednisolone sodium succinate 2392-39-4, Dexamethasone sodium phosphate 2398-96- 1, Tolnaftate 2438-32-6, Dexchlorpheniramine maleate 2447-57-6, Sulfadoxine 2508-79-4, Methyldopate hydrochloride 2668-66-8, Medrysone 2753-45-9, Mebeverine hydrochloride 2919-66-6, Melengestrol acetate

Page 31 of 37 2920-86-7, Prednisolone hemisuccinate 2971-90-6, Clopidol 3011-89-0, Aklomide 3093-35-4, Halcinonide 3105-97-3, Hycanthone 3198-07-0 3200-06-4, Nafronyl oxalate 3313-26-6, Thiothixene 3380-34-5, 3383-96-8, Temefos 3385-03-3, Flunisolide 3485-62-9, Clidinium bromide 3505-38-2, Carbinoxamine maleate 3521-62-8, Erythromycin estolate 3544-94-3, Chloramphenicol hemisuccinate 3546-41-6, Pyrvinium pamoate 3562-84-3, Benzbromarone 3598-37-6, Acepromazine maleate 3734-33-6, Denatonium benzoate 3736-81-0, Diloxanide furoate 3778-73-2, Ifosfamide 3810-74-0, Streptomycin sulfate 3818-50-6, Bephenium hydroxynaphthoate 3902-71-4, Trioxsalen 3963-95-9, Methacycline hydrochloride 4245-41-4, Estradiol acetate 4330-99-8, Trimeprazine tartrate 4342-03-4, Dacarbazine 4438-22-6, Atropine oxide 4598-67-8 4618-18-2, Lactulose 4682-36-4, Orphenadrine citrate 4759-48-2, Isotretinoin 4800-94-6, Carbenicillin disodium 5053-08-7, Fenspiride hydrochloride 5086-74-8, Tetramisole hydrochloride 5104-49-4, Flurbiprofen 5189-11-7, Pizotyline malate 5370-01-4, Mexiletine hydrochloride 5451-09-2, Aminolevulinic acid hydrochloride 5490-27-7, Dihydrostreptomycin sulfate 5534-09-8, Beclomethasone dipropionate 5536-17-4, Vidarabine 5560-59-8, Alverine citrate 5579-84-0, Betahistine hydrochloride 5588-16-9, Althiazide 5593-20-4, Betamethasone 17,21-dipropionate 5786-21-0, Clozapine 5870-29-1, Cyclopentolate hydrochloride 6055-19-2, Cyclophosphamide hydrate 6138-56-3, Tripelennamine citrate 6164-87-0, Nicotinyl alcohol tartrate 6190-39-2, Dihydroergotamine mesylate 6202-23-9, Cyclobenzaprine hydrochloride 6385-02-0, Meclofenamate sodium 6385-58-6, Bithionate sodium 6469-93-8, Chlorprothixene hydrochloride 6493-05-6, Pentoxifylline 6533-00-2, 6620-60-6, Proglumide 6724-53-4, Perhexiline maleate 6990-06-3, Fusidic acid 7054-25-3, Quinidine gluconate 7060-74-4, Oleandomycin phosphate 7232-21-5, Metoclopramide hydrochloride 7232-51-1, Pararosaniline pamoate 7235-40-7, β-Carotene 7279-75-6, Isoetharine mesylate 7280-37-7, Estropipate 7361-61-7, Xylazine 7414-83-7, Etidronate disodium 7421-40-1, Carbenoxolone sodium 7491-74-9, Piracetam 7527-91-5, Acrisorcin 7681-76-7, Ronidazole 7681-93-8, Natamycin 8025-81-8, Spiramycin 8068-28-8, Colistimethate sodium 9060-10-0, Bleomycin B2 10238-21-8, Glyburide 10246-75-0, Hydroxyzine pamoate 10347-81-6, Maprotiline hydrochloride 10457-90-6, Bromperidol 10592-13-9, Doxycycline hydrochloride 12192-57-3, Aurothioglucose 12650-69-0, Mupirocin 13071-11-9, Dexpropranolol hydrochloride 13292-46-1, Rifampin 13311-84-7, 13463-41-7, Pyrithione zinc 13492-01-8, Tranylcypromine sulfate 13523-86-9, Pindolol 13609-67-1, Hydrocortisone butyrate 13614-98-7, Minocycline hydrochloride 13655-52-2, Alprenolol 13669-70-0, Nefopam 13870-90-1, Coenzyme B12 13898-58-3, Benzoylpas 13909-09-6, Semustine 14028-44-5, Amoxapine 14362-31-3, Chlorcyclizine hydrochloride 14402-89-2, Sodium nitroprusside 14611-52-0, Selegiline hydrochloride 14663-23-1, Dantrolene sodium 14698-29-4, Oxolinic acid 14882-18-9, Bismuth subsalicylate 14919-77-8, Benserazide hydrochloride 14984-68-0, Cloperastine hydrochloride 15176-29-1, Edoxudine 15307-79-6, Diclofenac sodium 15318-45-3, Thiamphenicol 15500-66-0, Pancuronium bromide 15663-27-1, Cisplatin 15676-16-1, Sulpiride 15686-51-8, Clemastine 15686-71-2, Cefalexin 15687-27-1, Ibuprofen 15826-37-6, Cromolyn sodium 16051-77-7, Isosorbide mononitrate 16423-68-0,

Page 32 of 37 Erythrosine sodium 16676-29-2, hydrochloride 16773-42-5, Ornidazole 16846-24-5, Josamycin 17230-88-5, 17321-77-6, Clomipramine hydrochloride 17560-51-9, Metolazone 17575-22-3, Lanatoside C 18010-40-7, Bupivacaine hydrochloride 18507-89-6, Decoquinate 18559-94-9, Albuterol 19237-84-4, Prazosin hydrochloride 19387-91-8, Tinidazole 19767-45-4, Mesna 19774-82-4, Amiodarone hydrochloride 20559-55-1, Oxibendazole 20830-75-5, Digoxin 20830-81-3, Daunorubicin 21256-18-8, Oxaprozin 21434-91-3, Capobenic acid 21462-39-5, Clindamycin hydrochloride 21535-47-7, Mianserin hydrochloride 21736-83-4, Spectinomycin hydrochloride 21829-25-4, Nifedipine 22059-60-5, Disopyramide phosphate 22071-15-4, Ketoprofen 22204-24-6, Pyrantel pamoate 22204-53-1, Naproxen 22254-24-6, Ipratropium bromide 22260-51-1, Bromocriptine mesylate 22331-93-7, Sanguinarine sulfate 22373-78-0, Monensin sodium 22484-64-6, Sulfanilate zinc 22494-42-4, Diflunisal 22668-01-5, Etanidazole 22839-47-0, Aspartame 23031-32-5, Terbutaline hemisulfate 23142-01- 0, Carbetapentane citrate 23214-92-8, Doxorubicin RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (FDA-approved drugs and other compds. were tested as potent inhibitors of recombinant human glutathione transferase P1-1) IT 23239-51-2, Ritodrine hydrochloride 23256-50-0, Guanabenz acetate 23277-43-2, Nalbuphine hydrochloride 23288-49-5, Probucol 23593-75- 1, Clotrimazole 24169-02-6, Econazole nitrate 24280-93-1, Mycophenolic acid 24356-60-3, Cefapirin sodium 24356-94-3, Algestone acetophenide 25122-46-7, Clobetasol propionate 25155-18-4, Methylbenzethonium chloride 25301-02-4, Tyloxapol 25332-39-2, Trazodone hydrochloride 25389-94-0, Kanamycin sulfate 25507-04-4, Clindamycin palmitate hydrochloride 25717-80-0, Molsidomine 25812-30-0, Gemfibrozil 25953-17-7, Minaprine hydrochloride 26016-98-8, Fosfomycin calcium 26027-38-3, Nonoxynol-9 26159-36-4, Naproxol 26787-78-0, Amoxicillin 26807-65-8, Indapamide 26864-56-2, Penfluridol 26921-17-5, Timolol maleate 27164-46-1, Cefazolin sodium 27591-97-5, Tilorone 27833- 64-3 , Loxapine succinate 27848-84-6, Nicergoline 27912-14-7, Levobunolol hydrochloride 28094-15-7, Oxidopamine hydrochloride 28395-03-1, Bumetanide 28657-80-9, Cinoxacin 28721-07-5, Oxcarbazepine 28860-95-9, Carbidopa 29094-61-9, Glipizide 29122-68-7, Atenolol 29457-07-6, Ticarcillin disodium 29679-58-1, Fenoprofen 29767-20-2, Teniposide 29868-97-1, Pirenzepine hydrochloride 30034-03-8, Cefamandole sodium 30484-77-6, Flunarizine hydrochloride 30516-87-1, Zidovudine 31431-39-7, Mebendazole 31842-01-0, Indoprofen 32780- 64-6 , Labetalol hydrochloride 32795-47-4, Nomifensine maleate 32986-56- 4, Tobramycin 33069-62-4, Paclitaxel 33089-61-1, Amitraz 33125-97-2, 33286-22-5, Diltiazem hydrochloride 33386-08-2, Buspirone hydrochloride 33402-03-8, Metaraminol bitartrate 33419-42-0, Etoposide 33564-30-6, Cefoxitin sodium 34118-92-8, Acecainide hydrochloride 34183-22-7, Propafenone hydrochloride 34381-68-5, Acebutolol hydrochloride 34552-83-5, Loperamide hydrochloride 34552-84-6, Isoxicam 34580-14-8, Ketotifen fumarate 34911-55-2, Bupropion

Page 33 of 37 35189-28-7, Norgestimate 35554-44-0, Enilconazole 35711-34-3, Tolmetin sodium 36282-47-0, Tramadol hydrochloride 36322-90-4, Piroxicam 36330-85-5, Fenbufen 36791-04-5, Ribavirin 37091-65-9, Azlocillin sodium 37321-09-8, Apramycin 37661-08-8, Bacampicillin hydrochloride 38194-50-2, Sulindac 38260-01-4, Trientine hydrochloride 38274-54-3, Benurestat 38304-91-5, Minoxidil 38821-53-3, Cefradine 39562-70-4, Nitrendipine 39831-55-5, Amikacin sulfate 40828-46-4, Suprofen 41100-52-1, Memantine hydrochloride 41340-25-4, Etodolac 41575-94-4, Carboplatin 41621-49-2, Ciclopirox olamine 41859-67-0, Bezafibrate 42200-33-9, Nadolol 42461-84-7, Flunixin meglumine 42540-40-9, Cefamandole nafate 42835-25-6, Flumequine 42924-53-8, Nabumetone 42971-09-5, Vinpocetine 43210-67-9, Fenbendazole 43218-56-0, Midodrine hydrochloride 49562-28-9, Fenofibrate 49745-95-1, Dobutamine hydrochloride 50293-90-8, Levalbuterol hydrochloride 50370-12-2, Cefadroxil 50679-08-8, Terfenadine 50700-72-6, Vecuronium bromide 51012-33-0, Tiapride hydrochloride 51022-69-6, Amcinonide 51264-14- 3, Amsacrine 51333-22-3, Budesonide 51411-04-2, Alrestatin 51481-61- 9, Cimetidine 52152-93-9, Cefsulodin sodium 53123-88-9, Sirolimus 53179-09-2, Sisomicin sulfate 53230-10-7, Mefloquine 53716-49-7, Carprofen 53885-35-1, Ticlopidine hydrochloride 53902-12-8, Tranilast 53994-73-3, Cefaclor 54527-84-3, hydrochloride 54767-75- 8, Suloctidil 54910-89-3, 54965-21-8, Albendazole 54965- 24-1 , Tamoxifen citrate 55268-74-1, Praziquantel 56038-13-2, Sucralose 56180-94-0, Acarbose 56238-63-2, Cefuroxime sodium 56390-09-1, Epirubicin hydrochloride 56391-57-2, Netilmicin sulfate 56392-17-7, Metoprolol tartrate 56796-39-5, Cefmetazole sodium 56824-20-5, Amiprilose 57432-61-8, Methylergonovine maleate 57524-89-7, Hydrocortisone valerate 58579-51-4, Anagrelide hydrochloride 59277-89-3, Acyclovir 59703-84-3, Piperacillin sodium 59729-33-8, Citalopram 59803-98-4, Brimonidine 59804-37-4, Tenoxicam 59865-13- 3, Cyclosporine 60142-96-3, Gabapentin 60200-06-8, Clorsulon 60560- 33-0 , Pinacidil 60628-96-8, Bifonazole 60719-82-6, Alaproclate 61036-62-2, Teicoplanin 61270-78-8, Cefonicid sodium 61318-91-0, Sulconazole nitrate 61413-54-5, Rolipram 62013-04-1, Dirithromycin 62571-86-2, Captopril 62893-20-3, Cefoperazone sodium 62929-91-3, Procaterol hydrochloride 63585-09-1, Foscarnet sodium 63612-50-0, 63675-72-9, Nisoldipine 64092-48-4, Zomepirac sodium 64211-46-7, Oxiconazole nitrate 64485-93-4, Cefotaxime sodium 64544-07-6, Cefuroxime axetil 64953-12-4, Moxalactam disodium 65277-42-1, 65899-73-2, Tioconazole 66085-59-4, Nimodipine 66104-23-2, Pergolide mesylate 66357-35-5, Ranitidine 66575-29-9, Colforsin 68099-86-5, Bepridil hydrochloride 68506-86-5, Vigabatrin 68693-11-8, Modafinil 68813-55-8, Oxantel pamoate 68844-77-9, Astemizole 69004-03-1, Toltrazuril 69525-81-1, Morantel citrate 70288-86-7, 70356-09-1, Avobenzone 70458-95-6, Pefloxacin mesylate 70458-96-7, Norfloxacin 71125-39-8, Meloxicam sodium 71751-41-2, Abamectin 72432-03-2, Miglitol 72558-82-8, Ceftazidime 72956-09-3, Carvedilol 73231-34-2, Florfenicol

Page 34 of 37 73590-58-6, Omeprazole 73816-42-9, Meclocycline sulfosalicylate 73963-72-1, Cilostazol 74011-58-8, Enoxacin 74103-07-4, Ketorolac tromethamine 74610-55-2 75330-75-5, Lovastatin 75444-65-4, Pirenperone 75607-67-9, Fludarabine phosphate 76095-16-4, Enalapril maleate 76547-98-3, Lisinopril 76824-35-6, Famotidine 76963-41-2, Nizatidine 77337-73-6, Acamprosate calcium 77883-43-3, Doxazosin mesylate 78110-38-0, Aztreonam 78246-49-8, Paroxetine hydrochloride 78628-80-5, Terbinafine hydrochloride 78755-81-4, 79307-93-0, Azelastine hydrochloride 79559-97-0, Sertraline hydrochloride 79794-75-5, Loratadine 79902-63-9, Simvastatin 80214-83-1, Roxithromycin 80621-81-4, Rifaximin 81103-11-9, Clarithromycin 81131-70-6, Pravastatin sodium 81403-80-7, Alfuzosin 82248-59-7, Atomoxetine hydrochloride 82419-36-1, 82586- 55-8 , Quinapril hydrochloride 82640-04-8, Raloxifene hydrochloride 83881-52-1, Cetirizine hydrochloride 83905-01-5, Azithromycin 84057-84-1, Lamotrigine 84485-00-7, Sibutramine hydrochloride 84625-61-6, Itraconazole 85721-33-1, 86386-73-4, Fluconazole 86541-74-4, Benazepril hydrochloride 87051-43-2, Ritanserin 87239-81-4, Cefpodoxime proxetil 87333-19-5, Ramipril 89778-27-8, Toremifene citrate 91296-87-6, Sarafloxacin hydrochloride 91374-21-9, Ropinirole 91832-40-5, Cefdinir 92665-29-7, Cefprozil 93413-69-5, Venlafaxine 93957-55-2, Fluvastatin sodium 95233-18-4, Atovaquone 95635-55-5, Ranolazine 96829-58-2, Orlistat RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (FDA-approved drugs and other compds. were tested as potent inhibitors of recombinant human glutathione transferase P1-1) IT 97240-79-4, Topiramate 97519-39-6, Ceftibuten 98079-52-8, Lomefloxacin hydrochloride 98319-26-7, Finasteride 100643-71-8, Desloratadine 100986-85-4, 102625-70-7, Pantoprazole 103577-45-3, Lansoprazole 104227-87-4, Famciclovir 104344-23-2, Bisoprolol fumarate 104987-11-3, Tacrolimus 105816-04-4, Nateglinide 107133-36-8, Perindopril erbumine 107868-30-4, 108050-54-0, Tilmicosin 111406-87-2, Zileuton 111470-99-6, Amlodipine besylate 111974-69-7, Quetiapine 112529-15-4, Pioglitazone hydrochloride 114798-26-4, Losartan 117467-28-4, Cefditoren pivoxil 117976-90-6, Rabeprazole sodium 120011-70-3, Donepezil hydrochloride 120068-37-3, 120202-66-6, Clopidogrel sulfate 124832-27-5, Valacyclovir hydrochloride 124937-52-6, Tolterodine tartrate 129318-43-0, Alendronate sodium 129722-12-9, Aripiprazole 132539-06-1, Olanzapine 133099-07-7, Darifenacin hydrobromide 134523-03-8, Atorvastatin calcium 135062- 02-1 , Repaglinide 136434-34-9, Duloxetine hydrochloride 137862-53-4, Valsartan 138402-11-6, Irbesartan 139264-17-8, Zolmitriptan 139755-83-2, Sildenafil 144689-63-4, Olmesartan medoxomil 144701-48- 4, Telmisartan 145040-37-5, Candesartan cilexetil 145202-66-0, Rizatriptan benzoate 147098-20-2, Rosuvastatin calcium 148553-50-8, Pregabalin 151767-02-1, Montelukast sodium 153439-40-8, Fexofenadine hydrochloride 162011-90-7, Rofecoxib 169590-41-4, Deracoxib 169590-42-5, Celecoxib 173334-58-2, Aliskiren hemifumarate 177834- 92-3

Page 35 of 37 , Eletriptan hydrobromide 181695-72-7, Valdecoxib 182815-44-7, Colesevelam hydrochloride 186826-86-8, Moxifloxacin hydrochloride 191114-48-4, Telithromycin 210353-53-0, Gemifloxacin mesylate 220119-17-5, Selamectin 224785-91-5, Vardenafil hydrochloride 353228-19-0, Risedronate sodium hydrate RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (FDA-approved drugs and other compds. were tested as potent inhibitors of recombinant human glutathione transferase P1-1) IT 144-83-2, Sulfapyridine RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (FDA-approved drugs and other compds. were tested as potent inhibitors of recombinant human glutathione transferase P1-1sulfaquinoxaline sodium) IT 70-30-4, Hexachlorophene 129-16-8, Merbromin RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (chlorophyllide, merbromin, hexachlorophene and ethacrynic acid were most effective inhibitors of recombinant human glutathione transferase P1-1) IT 58-54-8, Ethacrynic acid RL: PAC (Pharmacological activity); THU (Therapeutic use); BIOL (Biological study); USES (Uses) (ethacrynic acid was most effective and allosteric inhibitor of recombinant human glutathione transferase P1-1) RE.CNT 50 THERE ARE 50 CITED REFERENCES AVAILABLE FOR THIS RECORD (1) Adler, V; EMBO J 1999, V18, P1321 CAPLUS (2) Ang, W; J Am Chem Soc 2005, V127, P1382 CAPLUS (3) Awasthi, S; Biochim Biophys Acta 1993, V1164, P173 CAPLUS (4) Burg, D; Drug Metab Rev 2002, V34, P821 CAPLUS (5) Caccuri, A; J Biol Chem 1996, V271, P16193 CAPLUS (6) Cameron, A; Structure 1995, V3, P717 CAPLUS (7) Castro, V; Carcinogenesis 1990, V11, P1569 CAPLUS (8) Chou, T; Eur J Biochem 1981, V115, P207 CAPLUS (9) Dahllof, B; Anticancer Res 1987, V7, P65 MEDLINE (10) Guthenberg, C; Acta Chem Scand B 1979, V33, P595 MEDLINE (11) Guthenberg, C; Biochim Biophys Acta 1981, V661, P255 CAPLUS (12) Habig, W; J Biol Chem 1974, V249, P7130 CAPLUS (13) Hansson, J; Cancer Res 1991, V51, P94 CAPLUS (14) Hayes, J; Crit Rev Biochem Mol Biol 1995, V30, P445 CAPLUS (15) Hayeshi, R; Food Chem Toxicol 2007, V45, P286 CAPLUS (16) Hegazy, U; J Mol Biol 2013, V425, P1509 CAPLUS (17) Johansson, A; J Biol Chem 2001, V276, P33061 CAPLUS (18) Josephy, P; Molecular Toxicology, 2nd ed 2006 (19) Keleti, T; Math Biosci 1971, V12, P197 CAPLUS (20) Kolm, R; Protein Expr Purif 1995, V6, P265 CAPLUS (21) Lacreta, F; J Pharmacol Exp Ther 1994, V270, P1186 CAPLUS (22) Litwack, G; Nature 1971, V234, P466 CAPLUS (23) Mannervik, B; CRC Crit Rev Biochem 1988, V23, P283 CAPLUS (24) Mannervik, B; Carcinogenesis 1987, V8, P1929 CAPLUS (25) Mannervik, B; FEBS Lett 1978, V93, P225 CAPLUS (26) Mannervik, B; Methods Enzymol 1981, V77, P231 CAPLUS (27) Mannervik, B; Methods Enzymol 2005, V401, P1 CAPLUS

Page 36 of 37 (28) Mannervik, B; Proc Natl Acad Sci U.S.A 1985, V82, P7202 CAPLUS (29) Marcus, C; Arch Biochem Biophys 1978, V188, P287 CAPLUS (30) Mukanganyama, S; Int J Cancer 2002, V97, P700 CAPLUS (31) Muller, J; Int J Cancer 2008, V123, P1797 CAPLUS (32) Oakley, A; Biochemistry 1997, V36, P576 CAPLUS (33) O'Brien, M; J Pharmacol Exp Ther 1999, V291, P1348 CAPLUS (34) O'Dwyer, P; Cancer Res 1991, V51, P6059 MEDLINE (35) Parker, L; J Mol Biol 2008, V380, P131 CAPLUS (36) Phillips, M; Biochem J 1991, V275(3), P703 CAPLUS (37) Ploemen, J; Biochem Pharmacol 1990, V40, P1631 CAPLUS (38) Quesada-Soriano, I; J Mol Recognit 2011, V24, P220 CAPLUS (39) Raffalli-Mathieu, F; Biochem J 2008, V414, P103 CAPLUS (40) Schenker, P; J Theor Biol 2009, V261, P318 CAPLUS (41) Sidler, D; Oncogene 2012, V31, P4095 CAPLUS (42) Tew, K; Adv Drug Deliv Rev 1997, V26, P91 (43) Tew, K; Cancer Res 1988, V48, P3622 CAPLUS (44) Tew, K; Mol Pharmacol 1996, V50, P149 CAPLUS (45) Townsend, D; Oncogene 2003, V22, P7369 CAPLUS (46) Turella, P; Cancer Res 2005, V65, P3751 CAPLUS (47) Yang, X; J Med Chem 2010, V53, P1015 CAPLUS (48) Yonetani, T; Arch Biochem Biophys 1964, V106, P243 CAPLUS (49) Yu, S; Anticancer Drugs 2009, V20, P382 CAPLUS (50) Zhao, G; Bioorg Med Chem 2005, V13, P4056 CAPLUS

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