DOCSLIB.ORG

(12) United States Patent (10) Patent No.: US 8.263,125 B2 Vaya Et Al

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
(12) United States Patent (10) Patent No.: US 8.263,125 B2 Vaya Et Al US008263125B2 (12) United States Patent (10) Patent No.: US 8.263,125 B2 Vaya et al. (45) Date of Patent: *Sep. 11, 2012 (54) DOSAGE FORM FOR HIGH DOSE-HIGH (52) U.S. Cl. ......... 424/469: 424/464; 424/465; 424/468 SOLUBLITY ACTIVE INGREDIENTS THAT (58) Field of Classification Search ........................ None PROVIDES FOR MIMEDIATE RELEASE AND See application file for complete search history. MODIFIED RELEASE OF THE ACTIVE INGREDIENTS (56) References Cited (75) Inventors: Navin Vaya, Gujarat (IN); Rajesh Singh Karan, Gujarat (IN); Sunil Sadanand U.S. PATENT DOCUMENTS Nadkarni, Gujarat (IN); Vinod Kumar 3,048,526 A * 8, 1962 Boswell ........................ 424,472 3,336,200 A 8, 1967 Krause et al. Gupta, Gujarat (IN) 4,139,589 A * 2/1979 Beringer et al. ... ... 264/250 4,503,031 A * 3/1985 Glassman ...... ... 424/467 (73) Assignee: Torrent Pharmaceuticals Limited, 4,996,061 A * 2/1991 Webb et al. ... ... 424/475 Ahmedabad (IN) 5,445,829 A * 8/1995 Paradissis et al. ... 424/480 5,738,874. A * 4/1998 Conte et al. ........ ... 424/472 (*) Notice: Subject to any disclaimer, the term of this 5,840,332 A * 1 1/1998 Lerner et al. .................. 424/464 5,985,843. A 1 1/1999 Higo et al. patent is extended or adjusted under 35 6,001,391 A 12/1999 Zeidler et al. U.S.C. 154(b) by 0 days. 6,238,699 B1 5, 2001 Rubin 6,372.254 B1 * 4/2002 Ting et al. ...... ... 424/473 This patent is Subject to a terminal dis 6,660,300 B1* 12/2003 Timmins et al. ... 424/469 claimer. 2004/0156902 A1* 8, 2004 Lee et al. ...................... 424/473 (21) Appl. No.: 11/134,633 FOREIGN PATENT DOCUMENTS WO WO/O 1/72286 10, 2001 (22) Filed: May 19, 2005 * cited by examiner (65) Prior Publication Data Primary Examiner — Anand Desai US 2006/OO24365A1 Feb. 2, 2006 Assistant Examiner — Melissa Mercier Related U.S. Application Data (74) Attorney, Agent, or Firm — Hedman & Costigan, P.C.: James V. Costigan (63) Continuation-in-part of application No. 10/630,446, filed on Jul. 29, 2003, now Pat. No. 7,985,422. (57) ABSTRACT (30) Foreign Application Priority Data A dosage form comprising of a high dose, high solubility active ingredient as modified release and a low dose active Aug. 5, 2002 (IN) ........................... 697 FMUMA2002 ingredient as immediate release where the weight ratio of Aug. 5, 2002 (IN) ........................... 699/MUMA2002 immediate release active ingredient and modified release Jan. 22, 2003 (IN) ............................. 8OfMUMA2003 active ingredient is from 1:10 to 1:15000 and the weight of Jan. 22, 2003 (IN) ............................. 82/MUMA2003 modified release active ingredient per unit is from 500 mg to 1500 mg; a process for preparing the dosage form. (51) Int. Cl. A6 IK 9/26 (2006.01) A6 IK9/20 (2006.01) 30 Claims, 10 Drawing Sheets -- U.S. Patent Sep. 11, 2012 Sheet 1 of 10 US 8,263,125 B2 FIGURE - - FIGURE 2 FIGURE 3 U.S. Patent Sep. 11, 2012 Sheet 2 of 10 US 8,263,125 B2 FIGURE 4 (a) 7 FIGURE 4 (b) U.S. Patent Sep. 11, 2012 Sheet 3 of 10 US 8,263,125 B2 FIGURE 5 20 OO 80 60 40 20 C. 2 g 6. 8 O 2 4 e. 8 20 22 24 26 Tite ho: U.S. Patent Sep. 11, 2012 Sheet 4 of 10 US 8,263,125 B2 FIGURE 6 2 O - O O 8 O 264 OOO O 2 4 6 8 O 2 1 4 16 8 2C 2 2 24 26 Time (hour) U.S. Patent Sep. 11, 2012 Sheet 5 of 10 US 8,263,125 B2 FIGURE 7 60 4 O 2 O O ----- -- --- O 2 4 6 8 O 12 4 6. 18 2O 22 24 26 Time (hour) U.S. Patent Sep. 11, 2012 Sheet 6 of 10 US 8,263,125 B2 FIGURE 8 O 4 8 12 6 2O 24 Tirne Hours) U.S. Patent Sep. 11, 2012 Sheet 7 of 10 US 8,263,125 B2 FIGURE 9 35OO 3OOO 25 OO 2OOO 5 OO 4 8 l2 6. 2O 24 Time Hours) U.S. Patent Sep. 11, 2012 Sheet 8 of 10 US 8,263,125 B2 FIGURE 10 O 2 4 6. 8 O 12 4 6. 18 2C 22 24 Time Hours) U.S. Patent Sep. 11, 2012 Sheet 9 of 10 US 8,263,125 B2 FIGURE 11 27 OO 2 4 O O 21 OO 1800 15OO 12OO 9 OO 6OO 3OO O 2 4 6 8 10 2 14 16 18 20 22 24 Time Hours) U.S. Patent Sep. 11, 2012 Sheet 10 of 10 US 8,263,125 B2 FIGURE 12 2OO 18O 16O 14 O 120 100 60 AO O 4 8 12 16 2O 24 Time Hours) US 8,263,125 B2 1. 2 DOSAGE FORM FOR HIGH DOSE-HIGH Block Jurgen et. al. describes in PCT application No. WO SOLUBILITY ACTIVE INGREDIENTS THAT 01/72286 A1 a formulation of vitamin composition whereas a PROVIDES FOR IMMEDIATE RELEASE AND beadlet comprises a slow release core coated by a controlled MODIFIED RELEASE OF THE ACTIVE release coating. The Sustained release core is coated with an INGREDIENTS immediate release layer. Richard Ting and Charles Hscao describes in U.S. Pat. No. This application is a continuation-in-part of Ser. No. 6,372.254B1 a press coated, pulsatile active ingredient deliv ery system which comprises a core of immediate release, 10/630,446, filed Jul. 29, 2003 now U.S. Pat. No. 7,985,422. enveloped by an extended release compartment. FIELD OF INVENTION 10 The need to use active ingredients with different and complementary mechanisms of action frequently arises in This invention relates to a dosage form comprising of a treatment of diabetes. There are several reasons to do this, high dose, high solubility active ingredient as modified namely, the disease itself is progressive, with deterioration of release and a low dose active ingredient as immediate release glycemic control over time; mono-therapeutic attempts to 15 achieve and maintain glycemic control often fail in the long where the weight ratio of immediate release active ingredient run; multiple defects in the disease and consequently primary and modified release active ingredient is from 1:1 to 1:15000 drug failures (1.2.3). and the weight of modified release high dose high solubility Current guidelines for combination therapy advise the use active ingredient per unit is from 500 mg to 1500 mg and the of agents with differing and complementary mechanisms of weight of immediate release active ingredient is up to 500mg: action in order to maximize therapeutic activity and reduce a process for preparing the formulation. Low dose active toxicity. Earlier introduction of combination therapy is ingredient in present invention can optionally be also in a increasingly being recommended. The commonly combined form of modified release. active ingredients include biguanides (metformin)+Sulpho nylureas, biguanides--PPAR2 agonists(thiazolidinediones), BACKGROUND OF THE INVENTION 25 Sulphonylureas--thiazolidinediones, non-Sulfonylurea secre tagogues (repaglinide)+biguanides etc. Fixed dose combina Combining two active ingredients in one pharmaceutical tions of many of the above mentioned co-administer active unit to improve patient compliance is known in literature. It ingredients have also been approved by the FDA. Most of can be either in the form of two or more active ingredients in these combinations are conventional formulations combined immediate release form or a combination of immediate 30 together into a single tablet. However, because of the dispar release and modified release form. There are various tech ity in the duration of action (half-life), these combinations are niques by which the combination of immediate release and given twice or thrice a day. modified release is formulated in single dosage form. To reduce this disparity in the duration of action, a novel Several examples of formulations having combination of strategy would be to combine a Sustained release formulation immediate release active ingredient and modified release 35 of one active ingredient (shorter duration of action) with active ingredient are described below. conventional formulation (long duration of action) of another Shoichi Higo and Kazuo Igusa describes in U.S. Pat. No. active ingredient. This would make it possible to give the 5.985,843 various types of pharmaceutical formulations, active ingredients in same dosing frequency. which consists of a delayed release of sucralfate and an imme This type of combination will give better compliance and a diate release fraction of another active ingredient. The phar 40 relative freedom from mealtime drug administration, thus, maceutical dosage forms are a tablet formulation containing improving the quality of life. More importantly, because of immediate release and delayed release granules; a two or prolonged duration of action, it shall produce a strictercontrol three layer tablet; a tablet with delayed release core sur of blood glucose and consequently less diabetic complica rounded by immediate release shell; a delayed release tablet/ tions. granule coated with a film of immediate release active ingre 45 The techniques described above do not work well when the dient. difference in the dose of active ingredients are high for Similarly Jurgen Zeidler et. al describes in U.S. Pat. No. example where the weight ratio of active ingredients is from 6,001.391 a process for producing solid combination tablets, 1:1 to 1: 15000 and the dose of modified release active ingre which have at least two phases. The one of the two phases is dient per unit is from 500 mg to 1500 mg. The techniques processed by melt extrusion technique and contains a water 50 described in the prior art do not give good results when the soluble or swellable binder.
Load more

Recommended publications
  • Comparison of the Antiischaemic and Antianginal Effects of Nicorandil and Amlodipine in Patients with Symptomatic Stable Angina Pectoris: the SWAN Study
    Journal of Clinical and Basic Cardiology An Independent International Scientific Journal Journal of Clinical and Basic Cardiology 1999; 2 (2), 213-217 Comparison of the antiischaemic and antianginal effects of nicorandil and amlodipine in patients with symptomatic stable angina pectoris: the SWAN study The SWAN Study Group Homepage: www.kup.at/jcbc Online Data Base Search for Authors and Keywords Indexed in Chemical Abstracts EMBASE/Excerpta Medica Krause & Pachernegg GmbH · VERLAG für MEDIZIN und WIRTSCHAFT · A-3003 Gablitz/Austria ORIGINAL PAPERS, CLINICAL The SWAN study J Clin Basic Cardiol 1999; 2: 213 Comparison of the antiischaemic and antianginal effects of nicorandil and amlodipine in patients with symptomatic stable angina pectoris: the SWAN study The SWAN Study Group1 This multicentre, double-blind, randomised study compared the antiischaemic and antianginal effects of nicorandil and amlodipine in patients with symptomatic stable angina pectoris. Nicorandil is a new coronary and balanced peripheral vasodilating agent that operates through two mechanisms of action: activation of ATP-dependent K-channels and stimulation of guanylate cyclase. A total of 121 patients with symptomatic stable angina pectoris were randomised to receive nicorandil 10 mg twice daily (bd) or amlodipine 5 mg once daily (od) for 8 weeks (optional dosage increase after 2-4 weeks to 20 mg bd and 10 mg od, respec- tively). Symptom-limited exercise tolerance tests were performed at baseline, and after 2 and 8 weeks treatment, respectively. In addition, the number of anginal attacks, nitroglycerin (NTG) usage, blood pressure (BP), heart rate (HR) and adverse events were recorded, and a subjective assessment of quality of life performed.
    [Show full text]
  • (12) United States Patent (10) Patent No.: US 9,498,481 B2 Rao Et Al
    USOO9498481 B2 (12) United States Patent (10) Patent No.: US 9,498,481 B2 Rao et al. (45) Date of Patent: *Nov. 22, 2016 (54) CYCLOPROPYL MODULATORS OF P2Y12 WO WO95/26325 10, 1995 RECEPTOR WO WO99/O5142 2, 1999 WO WOOO/34283 6, 2000 WO WO O1/92262 12/2001 (71) Applicant: Apharaceuticals. Inc., La WO WO O1/922.63 12/2001 olla, CA (US) WO WO 2011/O17108 2, 2011 (72) Inventors: Tadimeti Rao, San Diego, CA (US); Chengzhi Zhang, San Diego, CA (US) OTHER PUBLICATIONS Drugs of the Future 32(10), 845-853 (2007).* (73) Assignee: Auspex Pharmaceuticals, Inc., LaJolla, Tantry et al. in Expert Opin. Invest. Drugs (2007) 16(2):225-229.* CA (US) Wallentin et al. in the New England Journal of Medicine, 361 (11), 1045-1057 (2009).* (*) Notice: Subject to any disclaimer, the term of this Husted et al. in The European Heart Journal 27, 1038-1047 (2006).* patent is extended or adjusted under 35 Auspex in www.businesswire.com/news/home/20081023005201/ U.S.C. 154(b) by Od en/Auspex-Pharmaceuticals-Announces-Positive-Results-Clinical M YW- (b) by ayS. Study (published: Oct. 23, 2008).* This patent is Subject to a terminal dis- Concert In www.concertpharma. com/news/ claimer ConcertPresentsPreclinicalResultsNAMS.htm (published: Sep. 25. 2008).* Concert2 in Expert Rev. Anti Infect. Ther. 6(6), 782 (2008).* (21) Appl. No.: 14/977,056 Springthorpe et al. in Bioorganic & Medicinal Chemistry Letters 17. 6013-6018 (2007).* (22) Filed: Dec. 21, 2015 Leis et al. in Current Organic Chemistry 2, 131-144 (1998).* Angiolillo et al., Pharmacology of emerging novel platelet inhibi (65) Prior Publication Data tors, American Heart Journal, 2008, 156(2) Supp.
    [Show full text]
  • WO 2010/015655 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 11 February 2010 (11.02.2010) WO 2010/015655 Al (51) International Patent Classification: sham Research Centre, Wimblehurst Road, Horsham C07C 233/79 (2006.01) C07D 277/42 (2006.01) West Sussex RH 12 5AB (GB). SVIRIDENKO, Lilya C07C 255/58 (2006.01) A61K 31/166 (2006.01) [GB/GB]; Novartis Horsham Research Centre, Wimble C07C 311/39 (2006.01) A61K 31/427 (2006.01) hurst Road, Horsham West Sussex RH 12 5AB (GB). C07D 213/74 (2006.01) A61K 31/44 (2006.01) (74) Agent: VOEGELI-LANGE, Regina; Novartis Pharma C07D 213/75 (2006.01) A61P 1/00 (2006.01) Ag, Patent Department, CH-4002 Basel (CH). C07D 213/84' (2006.01) (81) Designated States (unless otherwise indicated, for every (21) International Application Number: kind of national protection available): AE, AG, AL, AM, PCT/EP2009/060150 AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, (22) International Filing Date: CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, 5 August 2009 (05.08.2009) DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, (25) Filing Language: English KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, (26) Publication Language: English ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, (30) Priority Data: SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, 08162006.4 7 August 2008 (07.08.2008) EP TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
    [Show full text]
  • Us 8530498 B1 3
    USOO853 0498B1 (12) UnitedO States Patent (10) Patent No.: US 8,530,498 B1 Zeldis (45) Date of Patent: *Sep. 10, 2013 (54) METHODS FORTREATING MULTIPLE 5,639,476 A 6/1997 OShlack et al. MYELOMAWITH 5,674,533 A 10, 1997 Santus et al. 3-(4-AMINO-1-OXO-1,3-DIHYDROISOINDOL- 395 A 22 N. 2-YL)PIPERIDINE-2,6-DIONE 5,731,325 A 3/1998 Andrulis, Jr. et al. 5,733,566 A 3, 1998 Lewis (71) Applicant: Celgene Corporation, Summit, NJ (US) 5,798.368 A 8, 1998 Muller et al. 5,874.448 A 2f1999 Muller et al. (72) Inventor: Jerome B. Zeldis, Princeton, NJ (US) 5,877,200 A 3, 1999 Muller 5,929,117 A 7/1999 Muller et al. 5,955,476 A 9, 1999 Muller et al. (73) Assignee: Celgene Corporation, Summit, NJ (US) 6,020,358 A 2/2000 Muller et al. - 6,071,948 A 6/2000 D'Amato (*) Notice: Subject to any disclaimer, the term of this 6,114,355 A 9, 2000 D'Amato patent is extended or adjusted under 35 SS f 1939. All et al. U.S.C. 154(b) by 0 days. 6,235,756 B1 5/2001 D'Amatoreen et al. This patent is Subject to a terminal dis- 6,281.230 B1 8/2001 Muller et al. claimer 6,316,471 B1 1 1/2001 Muller et al. 6,326,388 B1 12/2001 Man et al. 6,335,349 B1 1/2002 Muller et al. (21) Appl. No.: 13/858,708 6,380.239 B1 4/2002 Muller et al.
    [Show full text]
  • (12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 De Juan Et Al
    US 200601 10428A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 de Juan et al. (43) Pub. Date: May 25, 2006 (54) METHODS AND DEVICES FOR THE Publication Classification TREATMENT OF OCULAR CONDITIONS (51) Int. Cl. (76) Inventors: Eugene de Juan, LaCanada, CA (US); A6F 2/00 (2006.01) Signe E. Varner, Los Angeles, CA (52) U.S. Cl. .............................................................. 424/427 (US); Laurie R. Lawin, New Brighton, MN (US) (57) ABSTRACT Correspondence Address: Featured is a method for instilling one or more bioactive SCOTT PRIBNOW agents into ocular tissue within an eye of a patient for the Kagan Binder, PLLC treatment of an ocular condition, the method comprising Suite 200 concurrently using at least two of the following bioactive 221 Main Street North agent delivery methods (A)-(C): Stillwater, MN 55082 (US) (A) implanting a Sustained release delivery device com (21) Appl. No.: 11/175,850 prising one or more bioactive agents in a posterior region of the eye so that it delivers the one or more (22) Filed: Jul. 5, 2005 bioactive agents into the vitreous humor of the eye; (B) instilling (e.g., injecting or implanting) one or more Related U.S. Application Data bioactive agents Subretinally; and (60) Provisional application No. 60/585,236, filed on Jul. (C) instilling (e.g., injecting or delivering by ocular ion 2, 2004. Provisional application No. 60/669,701, filed tophoresis) one or more bioactive agents into the Vit on Apr. 8, 2005. reous humor of the eye. Patent Application Publication May 25, 2006 Sheet 1 of 22 US 2006/0110428A1 R 2 2 C.6 Fig.
    [Show full text]
  • United States Patent (10) Patent No.: US 8,969,514 B2 Shailubhai (45) Date of Patent: Mar
    USOO896.9514B2 (12) United States Patent (10) Patent No.: US 8,969,514 B2 Shailubhai (45) Date of Patent: Mar. 3, 2015 (54) AGONISTS OF GUANYLATECYCLASE 5,879.656 A 3, 1999 Waldman USEFUL FOR THE TREATMENT OF 36; A 6. 3: Watts tal HYPERCHOLESTEROLEMIA, 6,060,037- W - A 5, 2000 Waldmlegand et al. ATHEROSCLEROSIS, CORONARY HEART 6,235,782 B1 5/2001 NEW et al. DISEASE, GALLSTONE, OBESITY AND 7,041,786 B2 * 5/2006 Shailubhai et al. ........... 530.317 OTHER CARDOVASCULAR DISEASES 2002fOO78683 A1 6/2002 Katayama et al. 2002/O12817.6 A1 9/2002 Forssmann et al. (75) Inventor: Kunwar Shailubhai, Audubon, PA (US) 2003,2002/0143015 OO73628 A1 10/20024, 2003 ShaubhaiFryburg et al. 2005, OO16244 A1 1/2005 H 11 (73) Assignee: Synergy Pharmaceuticals, Inc., New 2005, OO32684 A1 2/2005 Syer York, NY (US) 2005/0267.197 A1 12/2005 Berlin 2006, OO86653 A1 4, 2006 St. Germain (*) Notice: Subject to any disclaimer, the term of this 299;s: A. 299; NS et al. patent is extended or adjusted under 35 2008/0137318 A1 6/2008 Rangarajetal.O U.S.C. 154(b) by 742 days. 2008. O151257 A1 6/2008 Yasuda et al. 2012/O196797 A1 8, 2012 Currie et al. (21) Appl. No.: 12/630,654 FOREIGN PATENT DOCUMENTS (22) Filed: Dec. 3, 2009 DE 19744O27 4f1999 (65) Prior Publication Data WO WO-8805306 T 1988 WO WO99,26567 A1 6, 1999 US 2010/O152118A1 Jun. 17, 2010 WO WO-0 125266 A1 4, 2001 WO WO-02062369 A2 8, 2002 Related U.S.
    [Show full text]
  • Bibliography & Appendix
    Bibliography Abou-Sleiman, P. M., Muqit, M. M. K. & Wood, N. W. 2006. Expanding insights of mitochondrial dysfunction in Parkinson's disease. Nature reviews neuroscience. 7: 207- 219. Agid, Y., Destée, A., Durif, F., Montastruc, J. L. & Pollak, P. 1997. Tolcapone, romocriptine, and Parkinson’s disease. The lancet . 350: 712-713. Anderson, M. C., Hasan, F., Mccrodden, J. M. & Tipton, K. F. 1993. Monoamine oxidase inhibitors and the cheese effect. Neurochemical research. 18 : 1145-1149. Avner, D. L. 2000. Clinical experience with pantoprazole in gastroesophageal reflux disease. Clinical therapeutics . 22: 1169-1185. Bach, A. W., Lan, N. C., Johnson, D. L., Abell, C. W., Bembenek, M. E., Kwan, S. W., Seeburg, P. H. & Shih, J. C. 1988. cDNA cloning of human liver monoamine oxidase A and B: molecular basis of differences in enzymatic properties. Proceedings of the national academy of sciences of the United States of America . 85: 4934-4938. Baker, G. B., Coutts, R. T., Mckenna, K. F. & Sherry-Mckenna, R. L. 1992. Insights into the mechanisms of action of the MAO inhibitors phenelzine and tranylcypromine: a review. Journal of psychiatry and neuroscience. 17 : 206-214. Barden, T. P., Peter, J. B. & Merkatz, I. R. 1980. Ritodrine hydrochloride: a betamimetic agent for use in preterm labor. Journal of the American college of obstetricians and gynecologists . 56: 1-6. Bergström, M., Westerberg, G., Németh, G., Traut, M., Gross, G., Greger, G., Müller- Peltzer, H., Safer, A., Eckernäs, S. Å., Grahnér, A. & Långström, B. 1997. MAO-A inhibition in brain after dosing with esuprone, moclobemide and placebo in healthy volunteers: in vivo studies with positron emission tomography.
    [Show full text]
  • Tricyclic Antidepressant Drug Immunogens, Antibodies, Labeled Conjugates, and Related Derivatives
    Patentamt JEuropaischesEuropean Patent Office @ Publication number; 0107134 ^ ^ Office europeen des brevets EUROPEAN PATENT APPLICATION © Application number: 83110063.1 © Int. CI.3: G 01 N 33/54, G 01 N 33/58, C07G 7/00, C 07 H 21/02, ®^ Date of 08.10.83 filing: C 07 H 17/06, C 07 D 223/28, C07C 93/00 (§) Priority: 21.10.82 US 435633 © Applicant: MILES LABORATORIES, INC., 1127 Myrtle Street, Elkhart Indiana 46514 (US) @ Inventor: Buckler, Robert Thomas, 23348 May Street, @ Dateof publication of application: 02.05.84 Edwardsburg, MI49112(US) Bulletin 84/18 Inventor: Ward, Frederick Edmund, 57342 Necedah Drive, Elkhart, IN 4651 6 (US) @ Representative : Jesse, Ralf-Riidiger, Dr. et al, Bayer AG @ Designated Contracting States : CH DE FR GB IT LI NL Zentralbereich Patente Marken und Lizenzen, SE D-5090 Leverkusen 1 Bayerwerk (DE) @ Tricyclic antidepressant drug immunogens, antibodies, labeled conjugates, and related derivatives. Tricyclic antidepressant drug (e.g., imipramine, desi- pramine, amitriptyline, or nortriptyline) immunogens, anti- bodies prepared therefrom, labeled conjugates, synthetic intermediates, and the use of such antibodies and labeled conjugates in immunoassays for determining such drug. The immunogens comprise the drug coupled at its 2'- position to an immunogenic carrier material. Similarly, the labeled conjugates and synthetic intermediates are 2'- derivatives of the drug or a precusor thereof. The antibodies and labeled reagents are particularly useful in certain ho- mogeneous nonradioisotopic immunoassays for measuring tricyclic antidepressant drugs in biological fluids such as serum. BACKGROUND OF THE INVENTION 1. FIELD OF THE INVENTION This invention relates to novel derivatives of tricyclic antidepressant drugs. The derivatives per- tain to immunoassays for determining tricyclic anti- depressant drugs in liquid media such as biological fluids and include immunogens used to stimulate produc- tion of antibodies to the drugs in host animals by conventional techniques.
    [Show full text]
  • (19) United States (12) Patent Application Publication (10) Pub
    US 20050181041A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2005/0181041 A1 Goldman (43) Pub. Date: Aug. 18, 2005 (54) METHOD OF PREPARATION OF MIXED Related US. Application Data PHASE CO-CRYSTALS WITH ACTIVE AGENTS (60) Provisional application No. 60/528,232, ?led on Dec. 9, 2003. Provisional application No. 60/559,862, ?led (75) Inventor: David Goldman, Portland, CT (US) on Apr. 6, 2004. Correspondence Address: Publication Classi?cation LEYDIG VOIT & MAYER, LTD (51) Int. Cl.7 ....................... .. A61K 31/56; A61K 38/00; TWO PRUDENTIAL PLAZA, SUITE 4900 A61K 9/64 180 NORTH STETSON AVENUE (52) US. Cl. ............................ .. 424/456; 514/179; 514/2; CHICAGO, IL 60601-6780 (US) 514/221 (73) Assignee: MedCrystalForms, LLC, Hunt Valley, (57) ABSTRACT MD This invention pertains to a method of preparing mixed phase co-crystals of active agents With one or more materials (21) Appl. No.: 11/008,034 that alloWs the modi?cation of the active agent to a neW physical/crystal form With unique properties useful for the delivery of the active agent, as Well as compositions com (22) Filed: Dec. 9, 2004 prising the mixed phase co-crystals. Patent Application Publication Aug. 18, 2005 Sheet 1 0f 8 US 2005/0181041 A1 FIG. 1a 214.70°C z.m."m.n... 206.98°C n..0ao 142 OJ/g as:20m=3: -0.8 -1.0 40 90 1:10 2110 Temperture (°C) FIG. 1b 0.01 as:22“.Km: 217 095 24221.4 39Jmum/Q -0.8 35 155 255 255 Temperture (°C) Patent Application Publication Aug.
    [Show full text]
  • Tepzz¥Z8 4A T
    (19) TZZ¥Z_ _ T (11) EP 3 081 214 A2 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.: 19.10.2016 Bulletin 2016/42 A61K 31/4178 (2006.01) A61K 31/422 (2006.01) A61P 25/28 (2006.01) (21) Application number: 16000020.4 (22) Date of filing: 30.08.2004 (84) Designated Contracting States: • Yuan, Junying, AT BE BG CH CY CZ DE DK EE ES FI FR GB GR Newton, HU IE IT LI LU MC NL PL PT RO SE SI SK TR MA 02468 (US) • Jagtap, Prakash, (30) Priority: 29.08.2003 US 498882 P North Andover, MA 01845 (US) (62) Document number(s) of the earlier application(s) in • Degterev, Alexei, accordance with Art. 76 EPC: Brookline, 10011481.8 / 2 384 753 MA 02445 (US) 04821344.1 / 1 663 184 (74) Representative: Bösl, Raphael Konrad (71) Applicants: Isenbruck Bösl Hörschler LLP • THE BRIGHAM AND WOMEN’S HOSPITAL, INC. Patentanwälte Boston, MA 02115 (US) Prinzregentenstraße 68 • President and Fellows of Harvard College 81675 München (DE) Cambridge, MA 02138 (US) Remarks: (72) Inventors: •This application was filed on 05-01-2016 as a • Cuny, Gregory D., divisional application to the application mentioned Houston, under INID code 62. TX 77004 (US) •Claims filed after the date of filing of the application (Rule 68(4) EPC). (54) INHIBITORS OF CELLULAR NECROSIS (57) The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis.
    [Show full text]
  • (12) Patent Application Publication (10) Pub. No.: US 2012/0115729 A1 Qin Et Al
    US 201201.15729A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2012/0115729 A1 Qin et al. (43) Pub. Date: May 10, 2012 (54) PROCESS FOR FORMING FILMS, FIBERS, Publication Classification AND BEADS FROM CHITNOUS BOMASS (51) Int. Cl (75) Inventors: Ying Qin, Tuscaloosa, AL (US); AOIN 25/00 (2006.01) Robin D. Rogers, Tuscaloosa, AL A6II 47/36 (2006.01) AL(US); (US) Daniel T. Daly, Tuscaloosa, tish 9.8 (2006.01)C (52) U.S. Cl. ............ 504/358:536/20: 514/777; 426/658 (73) Assignee: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF 57 ABSTRACT ALABAMA, Tuscaloosa, AL (US) (57) Disclosed is a process for forming films, fibers, and beads (21) Appl. No.: 13/375,245 comprising a chitinous mass, for example, chitin, chitosan obtained from one or more biomasses. The disclosed process (22) PCT Filed: Jun. 1, 2010 can be used to prepare films, fibers, and beads comprising only polymers, i.e., chitin, obtained from a suitable biomass, (86). PCT No.: PCT/US 10/36904 or the films, fibers, and beads can comprise a mixture of polymers obtained from a suitable biomass and a naturally S3712). (4) (c)(1), Date: Jan. 26, 2012 occurring and/or synthetic polymer. Disclosed herein are the (2), (4) Date: an. AO. films, fibers, and beads obtained from the disclosed process. O O This Abstract is presented solely to aid in searching the sub Related U.S. Application Data ject matter disclosed herein and is not intended to define, (60)60) Provisional applicationpp No. 61/182,833,sy- - - s filed on Jun.
    [Show full text]
  • Stems for Nonproprietary Drug Names
    USAN STEM LIST STEM DEFINITION EXAMPLES -abine (see -arabine, -citabine) -ac anti-inflammatory agents (acetic acid derivatives) bromfenac dexpemedolac -acetam (see -racetam) -adol or analgesics (mixed opiate receptor agonists/ tazadolene -adol- antagonists) spiradolene levonantradol -adox antibacterials (quinoline dioxide derivatives) carbadox -afenone antiarrhythmics (propafenone derivatives) alprafenone diprafenonex -afil PDE5 inhibitors tadalafil -aj- antiarrhythmics (ajmaline derivatives) lorajmine -aldrate antacid aluminum salts magaldrate -algron alpha1 - and alpha2 - adrenoreceptor agonists dabuzalgron -alol combined alpha and beta blockers labetalol medroxalol -amidis antimyloidotics tafamidis -amivir (see -vir) -ampa ionotropic non-NMDA glutamate receptors (AMPA and/or KA receptors) subgroup: -ampanel antagonists becampanel -ampator modulators forampator -anib angiogenesis inhibitors pegaptanib cediranib 1 subgroup: -siranib siRNA bevasiranib -andr- androgens nandrolone -anserin serotonin 5-HT2 receptor antagonists altanserin tropanserin adatanserin -antel anthelmintics (undefined group) carbantel subgroup: -quantel 2-deoxoparaherquamide A derivatives derquantel -antrone antineoplastics; anthraquinone derivatives pixantrone -apsel P-selectin antagonists torapsel -arabine antineoplastics (arabinofuranosyl derivatives) fazarabine fludarabine aril-, -aril, -aril- antiviral (arildone derivatives) pleconaril arildone fosarilate -arit antirheumatics (lobenzarit type) lobenzarit clobuzarit -arol anticoagulants (dicumarol type) dicumarol
    [Show full text]