“M/S. AJANTA PHARMA LTD.”
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Specifications of Approved Drug Compound Library
Annexure-I : Specifications of Approved drug compound library The compounds should be structurally diverse, medicinally active, and cell permeable Compounds should have rich documentation with structure, Target, Activity and IC50 should be known Compounds which are supplied should have been validated by NMR and HPLC to ensure high purity Each compound should be supplied as 10mM solution in DMSO and at least 100µl of each compound should be supplied. Compounds should be supplied in screw capped vial arranged as 96 well plate format. -
WO 2012/044761 Al
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date _ . 5 April 2012 (05.04.2012) WO 2012/044761 Al (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 47/48 (2006.01) kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, (21) International Application Number: CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, PCT/US201 1/053876 DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (22) International Filing Date: HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, 29 September 201 1 (29.09.201 1) KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, (25) Filing Language: English NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, (26) Publication Langi English RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, (30) Priority Data: ZM, ZW. 12/893,344 29 September 2010 (29.09.2010) US (84) Designated States (unless otherwise indicated, for every (71) Applicant (for all designated States except US): UNI¬ kind of regional protection available): ARIPO (BW, GH, VERSITY OF NORTH CAROLINA AT WILMING¬ GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, TON [US/US]; 601 South College Road, Wilmington, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, NC 28403 (US). -
Drug Name Plate Number Well Location % Inhibition, Screen Axitinib 1 1 20 Gefitinib (ZD1839) 1 2 70 Sorafenib Tosylate 1 3 21 Cr
Drug Name Plate Number Well Location % Inhibition, Screen Axitinib 1 1 20 Gefitinib (ZD1839) 1 2 70 Sorafenib Tosylate 1 3 21 Crizotinib (PF-02341066) 1 4 55 Docetaxel 1 5 98 Anastrozole 1 6 25 Cladribine 1 7 23 Methotrexate 1 8 -187 Letrozole 1 9 65 Entecavir Hydrate 1 10 48 Roxadustat (FG-4592) 1 11 19 Imatinib Mesylate (STI571) 1 12 0 Sunitinib Malate 1 13 34 Vismodegib (GDC-0449) 1 14 64 Paclitaxel 1 15 89 Aprepitant 1 16 94 Decitabine 1 17 -79 Bendamustine HCl 1 18 19 Temozolomide 1 19 -111 Nepafenac 1 20 24 Nintedanib (BIBF 1120) 1 21 -43 Lapatinib (GW-572016) Ditosylate 1 22 88 Temsirolimus (CCI-779, NSC 683864) 1 23 96 Belinostat (PXD101) 1 24 46 Capecitabine 1 25 19 Bicalutamide 1 26 83 Dutasteride 1 27 68 Epirubicin HCl 1 28 -59 Tamoxifen 1 29 30 Rufinamide 1 30 96 Afatinib (BIBW2992) 1 31 -54 Lenalidomide (CC-5013) 1 32 19 Vorinostat (SAHA, MK0683) 1 33 38 Rucaparib (AG-014699,PF-01367338) phosphate1 34 14 Lenvatinib (E7080) 1 35 80 Fulvestrant 1 36 76 Melatonin 1 37 15 Etoposide 1 38 -69 Vincristine sulfate 1 39 61 Posaconazole 1 40 97 Bortezomib (PS-341) 1 41 71 Panobinostat (LBH589) 1 42 41 Entinostat (MS-275) 1 43 26 Cabozantinib (XL184, BMS-907351) 1 44 79 Valproic acid sodium salt (Sodium valproate) 1 45 7 Raltitrexed 1 46 39 Bisoprolol fumarate 1 47 -23 Raloxifene HCl 1 48 97 Agomelatine 1 49 35 Prasugrel 1 50 -24 Bosutinib (SKI-606) 1 51 85 Nilotinib (AMN-107) 1 52 99 Enzastaurin (LY317615) 1 53 -12 Everolimus (RAD001) 1 54 94 Regorafenib (BAY 73-4506) 1 55 24 Thalidomide 1 56 40 Tivozanib (AV-951) 1 57 86 Fludarabine -
S1 Table. List of Medications Analyzed in Present Study Drug
S1 Table. List of medications analyzed in present study Drug class Drugs Propofol, ketamine, etomidate, Barbiturate (1) (thiopental) Benzodiazepines (28) (midazolam, lorazepam, clonazepam, diazepam, chlordiazepoxide, oxazepam, potassium Sedatives clorazepate, bromazepam, clobazam, alprazolam, pinazepam, (32 drugs) nordazepam, fludiazepam, ethyl loflazepate, etizolam, clotiazepam, tofisopam, flurazepam, flunitrazepam, estazolam, triazolam, lormetazepam, temazepam, brotizolam, quazepam, loprazolam, zopiclone, zolpidem) Fentanyl, alfentanil, sufentanil, remifentanil, morphine, Opioid analgesics hydromorphone, nicomorphine, oxycodone, tramadol, (10 drugs) pethidine Acetaminophen, Non-steroidal anti-inflammatory drugs (36) (celecoxib, polmacoxib, etoricoxib, nimesulide, aceclofenac, acemetacin, amfenac, cinnoxicam, dexibuprofen, diclofenac, emorfazone, Non-opioid analgesics etodolac, fenoprofen, flufenamic acid, flurbiprofen, ibuprofen, (44 drugs) ketoprofen, ketorolac, lornoxicam, loxoprofen, mefenamiate, meloxicam, nabumetone, naproxen, oxaprozin, piroxicam, pranoprofen, proglumetacin, sulindac, talniflumate, tenoxicam, tiaprofenic acid, zaltoprofen, morniflumate, pelubiprofen, indomethacin), Anticonvulsants (7) (gabapentin, pregabalin, lamotrigine, levetiracetam, carbamazepine, valproic acid, lacosamide) Vecuronium, rocuronium bromide, cisatracurium, atracurium, Neuromuscular hexafluronium, pipecuronium bromide, doxacurium chloride, blocking agents fazadinium bromide, mivacurium chloride, (12 drugs) pancuronium, gallamine, succinylcholine -
Cross-Over Trial of Febuxostat and Topiroxostat for Hyperuricemia with Cardiovascular Disease (TROFEO Trial)
Circ J 2017; 81: 1707 – 1712 ORIGINAL ARTICLE doi: 10.1253/circj.CJ-17-0438 Preventive Medicine Cross-Over Trial of Febuxostat and Topiroxostat for Hyperuricemia With Cardiovascular Disease (TROFEO Trial) Akira Sezai, MD, PhD; Kazuaki Obata; Keisuke Abe; Sakie Kanno; Hisakuni Sekino, MD, PhD Background: We previously reported that febuxostat was more effective for hyperuricemia than allopurinol. The efficacy, however, of topiroxostat (a novel xanthine oxidase reductase inhibitor similar to febuxostat), for hyperuricemia is unknown. Methods and Results: Patients with cardiovascular disease and hyperuricemia, in whom serum uric acid (s-UA) was controlled at ≤6 mg/dL, were eligible for enrollment. Fifty-five patients were randomized to receive either febuxostat or topiroxostat for 6 months and were switched to the other drug for the following 6 months. The primary endpoint was s-UA. Secondary endpoints included serum creatinine, estimated glomerular filtration rate, urinary albumin, cystatin-C, oxidized low-density lipoprotein, eicosapentaenoic acid/ arachidonic acid ratio, lipid biomarkers, high-sensitivity C-reactive protein and B-type natriuretic protein. Although s-UA level was similar for both drugs, significantly more patients required dose escalation during treatment with topiroxostat. There were no differ- ences in renal function, inflammatory and lipid markers between the 2 drugs. A biomarker of oxidative stress was significantly lower after 3 months of febuxostat compared with topiroxostat. Conclusions: Febuxostat causes more marked and more rapid reduction of s-UA than topiroxostat. With regard to the antioxidant effect, febuxostat was superior to topiroxostat after 3 months. The renal protective and anti-inflammatory effects of both drugs were also similar after 6 months of treatment. -
United States Patent Office Patented Mar
3,171,249 United States Patent Office Patented Mar. 2, 1965 i 2 fuel rocket engine. The above and other objects of this 3,171,249 PROPELLANT AND Rick |PROPULSSON METH invention will become apparent from the discussion OXD EMPLOYANG EYERAZINE WITH AMSNO which follows. TETRAZOLES The objects of this invention are accomplished by the Ronald E. Be, Canoga Park, Calif., assigner to use of compounds having the general formula: North American Aviatiosa, Bac. No Drawing. Fied Nov. 29, 1961, Ser. No. 155,803 NH2. (R) 8 Clains. (C. 60-35.4) N This invention relates to a novel rocket propellant. YS More particularly, this invention relates to a novel in 10 N--H proved rocket propellant and a method of operating a wherein x varies from 0 to 1 and R is selected from the rocket engine. class consisting of HCl, H2O, HNO3, and HCIO, as addi The criterion by which rocket propellants are classi tives to a hydrazine-based rocket fuel in an amount suffi fied is specific impulse, Is, defined as thrust in pounds 5 cient to depress the freezing point at least 40° C. while divided by the total mass flow of fuel and oxidizer in retaining about the same density impulse and specific pounds per second. Specific impulse is thus given in impulse. Hence, an embodiment of this invention com units of "seconds.” Oxidizer-fuel propulsion system prises a method of operating a rocket engine comprising compositions with a relatively high specific impulse are ejecting from the reaction chamber of the engine a gaseous known in the art. -
Rozprawa Doktorska
WOJSKOWA AKADEMIA TECHNICZNA im. Jarosława Dąbrowskiego WYDZIAŁ NOWYCH TECHNOLOGII I CHEMII ROZPRAWA DOKTORSKA Judyta REĆKO (imiona i nazwisko dyplomanta) Otrzymywanie i badanie koordynacyjnych związków wybuchowych zawierających 4,4’,5,5’-tetranitro-1H,1H’-2,2’- biimidazol (tytuł rozprawy doktorskiej) Nauki chemiczne, Chemia (dziedzina nauki, dyscyplina naukowa) prof. dr hab. inż. Stanisław CUDZIŁO (stopień wojskowy/naukowy, imię i nazwisko promotora pracy) WARSZAWA - 2020r Spis treści Wykaz stosowanych skrótów ................................................................................................. 4 Wprowadzenie ....................................................................................................................... 7 1. Związki koordynacyjne ...................................................................................................... 8 2. Koordynacyjne materiały wybuchowe ............................................................................ 10 2.1. Koordynacyjne materiały wybuchowe zawierające amoniak ....................................... 10 2.2.Koordynacyjne materiały wybuchowe zawierające hydrazynę ..................................... 11 2.3.Koordynacyjne materiały wybuchowe zawierające aminy alifatyczne ......................... 14 2.4. Koordynacyjne materiały wybuchowe zawierające karbohydrazyd ............................ 17 2.5. Koordynacyjne materiały wybuchowe z pochodnymi guanidyny ................................ 19 2.6. Koordynacyjne materiały wybuchowe zawierające imidazol ..................................... -
United States Patent Office Patented Aug
3,461,106 United States Patent Office Patented Aug. 12, 1969 1. 2 have insufficient fastness, frequently accompanied by 3,461,106 PGLYURETHANE FBERS insufficient absorption rates and depth of colour of the Harald Oertel and Heinrich Rinke, Leverkusen, Wilhelm dyeings, factors which also have a negative effect on the Thoma, Cologne-Flittard, and Friedrich-Karl Rosen fastness of such dyeings to abrasion. Further, the over dahl, Leverkusen-Schlebusch, Germany, assignors to dyeing properties are in many cases inadequate owing Farbenfabriken Bayer Aktiengeseischaft, Leverkusen, to the poor wash fastness of the dyeings. If, however, Germany, a corporation of Germany polyurethane elastomer fibres are to be widely used No Drawing. Fied May 21, 1965, Ser. No. 457,800 for textile purposes, the obtaining of deep and fast dye Claims priority, application Germany, May 23, 1964, ings is essential. This applies especially to the use of F 42,970 important groups of dyes such as acid dyes, metal com int. C. C08g 22/04, 22/06 O plex dyes or chrome dyes with which fast dyeings in U.S. C. 260-75 11 Claims deep colour tones can be obtained e.g. on polyamides which are used preferentially in conjunction with elastic polyurethane threads. The stability of polyurethane ABSTRACT OF THE DISCLOSURE 5 elastomer threads and foils to discolouration in light and Segmented polyurethane elastomers having improved to yellowing under the effect of atmospheric waste gases dyeability containing a repeating unit and having at least (especially nitrous gases and waste gases of combustion) one carboxylic acid hydrazide grouping and at least one still leaves room for improvement. -
Patent Application Publication ( 10 ) Pub . No . : US 2019 / 0192440 A1
US 20190192440A1 (19 ) United States (12 ) Patent Application Publication ( 10) Pub . No. : US 2019 /0192440 A1 LI (43 ) Pub . Date : Jun . 27 , 2019 ( 54 ) ORAL DRUG DOSAGE FORM COMPRISING Publication Classification DRUG IN THE FORM OF NANOPARTICLES (51 ) Int . CI. A61K 9 / 20 (2006 .01 ) ( 71 ) Applicant: Triastek , Inc. , Nanjing ( CN ) A61K 9 /00 ( 2006 . 01) A61K 31/ 192 ( 2006 .01 ) (72 ) Inventor : Xiaoling LI , Dublin , CA (US ) A61K 9 / 24 ( 2006 .01 ) ( 52 ) U . S . CI. ( 21 ) Appl. No. : 16 /289 ,499 CPC . .. .. A61K 9 /2031 (2013 . 01 ) ; A61K 9 /0065 ( 22 ) Filed : Feb . 28 , 2019 (2013 .01 ) ; A61K 9 / 209 ( 2013 .01 ) ; A61K 9 /2027 ( 2013 .01 ) ; A61K 31/ 192 ( 2013. 01 ) ; Related U . S . Application Data A61K 9 /2072 ( 2013 .01 ) (63 ) Continuation of application No. 16 /028 ,305 , filed on Jul. 5 , 2018 , now Pat . No . 10 , 258 ,575 , which is a (57 ) ABSTRACT continuation of application No . 15 / 173 ,596 , filed on The present disclosure provides a stable solid pharmaceuti Jun . 3 , 2016 . cal dosage form for oral administration . The dosage form (60 ) Provisional application No . 62 /313 ,092 , filed on Mar. includes a substrate that forms at least one compartment and 24 , 2016 , provisional application No . 62 / 296 , 087 , a drug content loaded into the compartment. The dosage filed on Feb . 17 , 2016 , provisional application No . form is so designed that the active pharmaceutical ingredient 62 / 170, 645 , filed on Jun . 3 , 2015 . of the drug content is released in a controlled manner. Patent Application Publication Jun . 27 , 2019 Sheet 1 of 20 US 2019 /0192440 A1 FIG . -
Report on the Deliberation Results May 8, 2013 Evaluation And
Report on the Deliberation Results May 8, 2013 Evaluation and Licensing Division, Pharmaceutical and Food Safety Bureau Ministry of Health, Labour and Welfare [Brand name] (a) Topiloric Tablets 20 mg, 40 mg, and 60 mg (b) Uriadec Tablets 20 mg, 40 mg, and 60 mg [Non-proprietary name] Topiroxostat (JAN*) [Applicant] (a) Fujiyakuhin Co., Ltd. (b) Sanwa Kagaku Kenkyusho Co., Ltd. [Date of application] June 26, 2012 [Results of deliberation] In the meeting held on April 26, 2013, the First Committee on New Drugs concluded that the product may be approved and that this result should be presented to the Pharmaceutical Affairs Department of the Pharmaceutical Affairs and Food Sanitation Council. The product is not classified as a biological product or a specified biological product, the re-examination period is 8 years, and neither the drug substance nor the drug product is classified as a poisonous drug or a powerful drug. *Japanese Accepted Name (modified INN) This English version of the Japanese review report is intended to be a reference material to provide convenience for users. In the event of inconsistency between the Japanese original and this English translation, the former shall prevail. The PMDA will not be responsible for any consequence resulting from the use of this English version. Review Report April 15, 2013 Pharmaceuticals and Medical Devices Agency The results of a regulatory review conducted by the Pharmaceuticals and Medical Devices Agency on the following pharmaceutical product submitted for registration are as follows. [Brand name] (a) Topiloric Tablets 20 mg, 40 mg, and 60 mg (b) Uriadec Tablets 20 mg, 40 mg, and 60 mg [Non-proprietary name] Topiroxostat [Applicant] (a) Fujiyakuhin Co., Ltd. -
Download Product Insert (PDF)
PRODUCT INFORMATION Polmacoxib Item No. 17509 OO CAS Registry No.: 301692-76-2 Formal Name: 4-[3-(3-fluorophenyl)-4,5-dihydro-5,5-dimethyl- S NH 4-oxo-2-furanyl]-benzenesulfonamide 2 MF: C H FNO S 18 16 4 O FW: 361.4 Purity: ≥98% F UV/Vis.: λmax: 238, 320 nm Supplied as: A crystalline solid O Storage: -20°C Stability: ≥2 years Information represents the product specifications. Batch specific analytical results are provided on each certificate of analysis. Laboratory Procedures Polmacoxib is supplied as a crystalline solid. A stock solution may be made by dissolving the polmacoxib in the solvent of choice. Polmacoxib is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of polmacoxib in ethanol is approximately 5 mg/ml and approximately 20 mg/ml in DMSO and DMF. Polmacoxib is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, polmacoxib should first be dissolved in DMSO and then diluted with the aqueous buffer of choice. Polmacoxib has a solubility of approximately 0.5 mg/ml in a 1:8 solution of DMSO:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day. Description Polmacoxib is an inhibitor of cyclooxygenase 2 (COX-2) and the carbonic anhydrase subtypes I (CAI) and 1 CAII. It inhibits COX-2 in the absence of carbonic anhydrase II with an IC50 value of 40 nM, which increases by approximately 4- and 17-fold in the presence of a CAII at a molar ratio of 1:1 and 1:5, respectively.2 It also inhibits CAI and CAII (IC50s = 210 and 95 nM, respectively). -
Analgesic & Rheumatology
Recommendations of the SEC (Analgesic & Rheumatology) made in its 72nd meeting held on 24.06.2021 & 25.06.2021 at CDSCO HQ New Delhi. File Name & Recommendations Agenda Drug Name, Firm Name No Strength New Drugs Division ND/MA/21/000076 M/s Hetero Labs Ltd. The firm presented their proposal of Polmacoxib 2 mg Fresh Application Phase III clinical trial protocol capsules along with BE study protocol before committee. After detailed deliberation, the 1. committee recommended for grant of permission to conduct the BE study. The firm should present the results of BE study before committee for further consideration of phase III clinical trial protocol. Biological Division BIO/CT- The firm presented their proposal 18/FF/2021/24609- for marketing authorization and Belimumab (Marketing Authorization)- local clinical trial waiver based on Belimumab the results of GCT including sub set analysis on 66 Indian patients. The committee noted that the drug is not an unmet need in the country. M/s. GSK Further, the data presented by the 2. Pharmaceuticals firm in Indian sub-set is limited and Ltd. in different route of administration (intravenous) while the firm is seeking MA for subcutaneous route. After detailed deliberation, the committee did not recommend for grant of approval for marketing authorization. BIO/CT21/FF/2021/246 M/s Reliance Life The firm presented their proposal 79- Denosumab Sciences Pvt ltd for marketing authorization along 60mg/ml with the results of Phase-III clinical trial. 3. The committee noted that the Phase III trial was approved