KR20090023670A - 트롬빈 수용체 길항제의 즉시-방출형 정제 제형 - Google Patents
트롬빈 수용체 길항제의 즉시-방출형 정제 제형 Download PDFInfo
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- KR20090023670A KR20090023670A KR1020097000084A KR20097000084A KR20090023670A KR 20090023670 A KR20090023670 A KR 20090023670A KR 1020097000084 A KR1020097000084 A KR 1020097000084A KR 20097000084 A KR20097000084 A KR 20097000084A KR 20090023670 A KR20090023670 A KR 20090023670A
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- pharmaceutical formulation
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- formulation
- pharmaceutically acceptable
- disintegrant
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| JP2012529431A (ja) | 2009-06-08 | 2012-11-22 | メルク・シャープ・アンド・ドーム・コーポレーション | トロンビン受容体アンタゴニストおよびクロピドグレルの固定用量錠剤 |
| CN102442965B (zh) * | 2010-09-30 | 2013-12-11 | 天津药物研究院 | 用于治疗血栓性疾病的par-1拮抗剂及其制备方法和用途 |
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| US6858577B1 (en) | 1999-06-29 | 2005-02-22 | Ortho-Mcneil Pharmaceutical, Inc. | Indole peptidomimetics as thrombin receptor antagonists |
| US7488742B2 (en) | 2000-06-15 | 2009-02-10 | Schering Corporation | Thrombin receptor antagonists |
| AU6690001A (en) * | 2000-06-15 | 2001-12-24 | Schering Corp | Thrombin receptor antagonists |
| US7235567B2 (en) * | 2000-06-15 | 2007-06-26 | Schering Corporation | Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist |
| US20040192753A1 (en) * | 2000-06-15 | 2004-09-30 | Samuel Chackalamannil | Methods of use of thrombin receptor antagonists |
| WO2002068425A1 (en) * | 2001-02-23 | 2002-09-06 | Ortho-Mcneil Pharmaceutical, Inc. | Aminomethyl-pyrroloquinazoline compounds as thrombin receptor antagonists |
| EP1394152A4 (en) | 2001-04-19 | 2005-02-02 | Eisai Co Ltd | 2-IMINOIMIDAZOLE DERIVATIVES (1) |
| KR100960170B1 (ko) * | 2001-10-18 | 2010-05-26 | 쉐링 코포레이션 | 트롬빈 수용체 길항제로서의 힘바신 동족체 |
| BRPI0309309B8 (pt) * | 2002-04-16 | 2021-05-25 | Merck Sharp & Dohme | antagonistas de receptor de trombina tricíclicos |
| DE10317816A1 (de) * | 2003-04-16 | 2004-11-04 | Claas Selbstfahrende Erntemaschinen Gmbh | Feldhäcksler mit positionierbarer Fahrerkabine |
| CZ300438B6 (cs) * | 2003-11-25 | 2009-05-20 | Pliva Hrvatska D.O.O. | Zpusob prípravy orální pevné lékové formy s okamžitým uvolnováním úcinné látky obsahující jako úcinnou látku polymorfní formu finasteridu |
| JP2009521472A (ja) * | 2005-12-22 | 2009-06-04 | シェーリング コーポレイション | 心肺手術の合併症の予防としてのトロンビンレセプターアンタゴニスト |
| TW200812619A (en) * | 2006-04-06 | 2008-03-16 | Schering Corp | TRA combination therapies |
| US20080026050A1 (en) * | 2006-06-30 | 2008-01-31 | Rajan Gupta | Solid dose formulations of a thrombin receptor antagonist |
| TWI343262B (en) * | 2006-09-26 | 2011-06-11 | Schering Corp | Rapidly disintegrating lyophilized oral formulations of a thrombin receptor antagonist |
| EP2120879A2 (en) * | 2006-12-22 | 2009-11-25 | Schering Corporation | Disintegration promoters in solid dose wet granulation formulations |
| BRPI0809095A2 (pt) * | 2007-03-23 | 2014-09-09 | Schering Corp | Redução de eventos adversos após intervenção percutânea através de uso de um antagonista de receptor de trombina |
-
2007
- 2007-06-28 TW TW096123547A patent/TWI367112B/zh not_active IP Right Cessation
- 2007-06-29 MX MX2009000131A patent/MX2009000131A/es unknown
- 2007-06-29 AR ARP070102934A patent/AR061790A1/es not_active Application Discontinuation
- 2007-06-29 CL CL200701923A patent/CL2007001923A1/es unknown
- 2007-06-29 ES ES07796595.2T patent/ES2616405T3/es active Active
- 2007-06-29 CA CA2656395A patent/CA2656395C/en active Active
- 2007-06-29 WO PCT/US2007/015168 patent/WO2008005353A2/en not_active Ceased
- 2007-06-29 ES ES12159636.5T patent/ES2616354T3/es active Active
- 2007-06-29 US US11/771,520 patent/US20080031943A1/en not_active Abandoned
- 2007-06-29 KR KR1020097000084A patent/KR20090023670A/ko not_active Withdrawn
- 2007-06-29 JP JP2009518301A patent/JP5116764B2/ja not_active Expired - Fee Related
- 2007-06-29 CN CN201510409546.7A patent/CN104922054A/zh active Pending
- 2007-06-29 EP EP12159636.5A patent/EP2491922B1/en active Active
- 2007-06-29 AU AU2007269733A patent/AU2007269733B2/en not_active Ceased
- 2007-06-29 CN CNA2007800325694A patent/CN101511345A/zh active Pending
- 2007-06-29 EP EP07796595.2A patent/EP2034969B1/en active Active
- 2007-06-29 BR BRPI0713935-7A patent/BRPI0713935A2/pt not_active IP Right Cessation
- 2007-07-02 PE PE2007000840A patent/PE20080376A1/es not_active Application Discontinuation
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2009
- 2009-01-15 ZA ZA200900350A patent/ZA200900350B/xx unknown
- 2009-01-29 NO NO20090467A patent/NO20090467L/no not_active Application Discontinuation
- 2009-01-30 CO CO09008875A patent/CO6150126A2/es unknown
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2012
- 2012-03-30 JP JP2012082021A patent/JP2012126752A/ja not_active Withdrawn
-
2016
- 2016-03-10 US US15/066,726 patent/US20170224666A9/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0713935A2 (pt) | 2012-12-04 |
| EP2491922A1 (en) | 2012-08-29 |
| ZA200900350B (en) | 2010-01-27 |
| US20170224666A9 (en) | 2017-08-10 |
| WO2008005353A2 (en) | 2008-01-10 |
| CO6150126A2 (es) | 2010-04-20 |
| CA2656395A1 (en) | 2008-01-10 |
| WO2008005353A3 (en) | 2008-06-26 |
| EP2034969A2 (en) | 2009-03-18 |
| JP2009542678A (ja) | 2009-12-03 |
| CL2007001923A1 (es) | 2008-02-08 |
| EP2491922B1 (en) | 2017-01-04 |
| AU2007269733B2 (en) | 2013-02-21 |
| US20160193196A1 (en) | 2016-07-07 |
| JP2012126752A (ja) | 2012-07-05 |
| US20080031943A1 (en) | 2008-02-07 |
| MX2009000131A (es) | 2009-01-26 |
| CN101511345A (zh) | 2009-08-19 |
| AR061790A1 (es) | 2008-09-24 |
| JP5116764B2 (ja) | 2013-01-09 |
| TW200810792A (en) | 2008-03-01 |
| NO20090467L (no) | 2009-03-19 |
| CN104922054A (zh) | 2015-09-23 |
| CA2656395C (en) | 2016-12-13 |
| ES2616354T3 (es) | 2017-06-12 |
| ES2616405T3 (es) | 2017-06-13 |
| EP2034969B1 (en) | 2017-01-11 |
| AU2007269733A1 (en) | 2008-01-10 |
| TWI367112B (en) | 2012-07-01 |
| PE20080376A1 (es) | 2008-06-13 |
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