WO2003066637A1 - Polymorphs of clopidogrel hydrochloride and their use as antithrombic compounds - Google Patents

Polymorphs of clopidogrel hydrochloride and their use as antithrombic compounds Download PDF

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Publication number
WO2003066637A1
WO2003066637A1 PCT/HU2002/000157 HU0200157W WO03066637A1 WO 2003066637 A1 WO2003066637 A1 WO 2003066637A1 HU 0200157 W HU0200157 W HU 0200157W WO 03066637 A1 WO03066637 A1 WO 03066637A1
Authority
WO
WIPO (PCT)
Prior art keywords
dihydro
methyl
pyridine
thieno
chlorophenyl
Prior art date
Application number
PCT/HU2002/000157
Other languages
English (en)
French (fr)
Inventor
Péter KÓTAY NAGY
József Barkóczy
Gyula Simig
Zsuzsa SZENT KIRÁLLYI
Tamás GREGOR
Béla FARKAS
Györgyi VERECZKEYNÉ DONÁTH
Kálmán NAGY
Gyuláné KÖRTVÉLYESSY
Original Assignee
EGIS Gyógyszergyár Rt.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to HUP0200438 priority Critical
Priority to HU0200438A priority patent/HU0200438A3/hu
Application filed by EGIS Gyógyszergyár Rt. filed Critical EGIS Gyógyszergyár Rt.
Publication of WO2003066637A1 publication Critical patent/WO2003066637A1/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
PCT/HU2002/000157 2002-02-06 2002-12-20 Polymorphs of clopidogrel hydrochloride and their use as antithrombic compounds WO2003066637A1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
HUP0200438 2002-02-06
HU0200438A HU0200438A3 (en) 2002-02-06 2002-02-06 Novel clopidogrel hydrochloride polymorphs, process for the preparation thereof, their use and pharmaceutical compositions containing them

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
EP02788271A EP1474427A1 (en) 2002-02-06 2002-12-20 Polymorphs of clopidogrel hydrochloride and their use as antithrombic compounds
US10/504,042 US20050113406A1 (en) 2002-02-06 2002-12-20 Polymorphs of clopidogrel hydrochloride and their use as antithrombic compounds
SK336-2004A SK3362004A3 (sk) 2002-02-06 2002-12-20 Polymorfy hydrochloridu clopidogrelu a ich použitie ako antitrombotických zlúčenín
AU2002353251A AU2002353251A1 (en) 2002-02-06 2002-12-20 Polymorphs of clopidogrel hydrochloride and their use as antithrombic compounds
KR10-2004-7012110A KR20040079987A (ko) 2002-02-06 2002-12-20 클로피도그렐 히드로클로라이드의 다형체 및 이의 항혈전화합물로서의 용도
JP2003566010A JP2005522441A (ja) 2002-02-06 2002-12-20 クロピドグレル塩酸塩の多形体及び抗トロンビン化合物としての使用
EA200401025A EA007119B1 (ru) 2002-02-06 2002-12-20 Полиморфы клопидогреля гидрохлориа и их применение в качестве антитромботических соединений
IS7385A IS7385A (is) 2002-02-06 2004-08-05 Fjölgervingar klópídógrelhýdróklóríðs og notkun þeirra sem andsegaefnasambanda
HRP20040741 HRP20040741A2 (en) 2002-02-06 2004-08-17 Polymorphs of clopidogrel hydrochloride and their use as antithrombic compounds

Publications (1)

Publication Number Publication Date
WO2003066637A1 true WO2003066637A1 (en) 2003-08-14

Family

ID=10975791

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/HU2002/000157 WO2003066637A1 (en) 2002-02-06 2002-12-20 Polymorphs of clopidogrel hydrochloride and their use as antithrombic compounds

Country Status (15)

Country Link
US (1) US20050113406A1 (WO2017193030A1)
EP (1) EP1474427A1 (WO2017193030A1)
JP (1) JP2005522441A (WO2017193030A1)
KR (1) KR20040079987A (WO2017193030A1)
AU (1) AU2002353251A1 (WO2017193030A1)
BG (1) BG108868A (WO2017193030A1)
CZ (1) CZ2004901A3 (WO2017193030A1)
EA (1) EA007119B1 (WO2017193030A1)
HR (1) HRP20040741A2 (WO2017193030A1)
HU (1) HU0200438A3 (WO2017193030A1)
IS (1) IS7385A (WO2017193030A1)
PL (1) PL370038A1 (WO2017193030A1)
SK (1) SK3362004A3 (WO2017193030A1)
WO (1) WO2003066637A1 (WO2017193030A1)
YU (1) YU69604A (WO2017193030A1)

Cited By (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005026174A1 (en) * 2003-09-11 2005-03-24 Generics [Uk] Limited Novel crystalline polymorphs of clopidogrel
WO2005068471A1 (en) * 2004-01-13 2005-07-28 Zentiva, A.S. New crystalline forms of clopidogrel hydrobromide and methods of their preparation
WO2005097804A1 (en) * 2004-04-09 2005-10-20 Hanmi Pharm. Co., Ltd. Crystalline clopidogrel naphthalenesulfonate or hydrate thereof, method for preparing same and pharmaceutical composition containing same
WO2005103059A1 (en) * 2004-04-20 2005-11-03 Sanofi-Aventis Clopidogrel salt and polymorphic forms thereof
WO2005117866A1 (en) * 2004-06-01 2005-12-15 Ivax Pharmaceuticals S.R.O. Amorphous clopidogrel hydrochloride and its antithrombotic use
EP1674468A1 (en) * 2004-12-21 2006-06-28 Ratiopharm GmbH Polymorphs of clopidogrel hydrobromide
EP1693375A1 (en) * 2005-02-21 2006-08-23 KRKA, tovarna zdravil, d.d., Novo mesto Process for preparing clopidrogel hydrogen sulfate of form I
WO2005104663A3 (en) * 2004-03-05 2006-09-28 Sanjay Govind Barve Industrial process for preparation of clopidogrel hydrogen sulphate
WO2007029096A2 (en) * 2005-09-05 2007-03-15 Ranbaxy Laboratories Limited Novel polymorphic forms of clopidogrel hydrochloride
WO2007029080A1 (en) * 2005-09-05 2007-03-15 Ranbaxy Laboratories Limited Preparation of form i of clopidogrel hydrochloride
WO2007073095A1 (en) * 2005-12-22 2007-06-28 Sk Chemicals Co., Ltd. Process for the preparation of (s)-(+)-clopidogrel on a solid-phase
WO2007074995A1 (en) * 2005-12-26 2007-07-05 Sk Chemicals Co., Ltd. Process for the preparation of s-(+)-clopidogrel by optical resolution
JP2007533744A (ja) * 2004-04-20 2007-11-22 サノフイ−アベンテイス (+)−(S)−α−(2−クロロフェニル)−6,7−ジヒドロチエノ[3,2−C]ピリジン−5(4H)酢酸メチル臭化水素酸塩、クロピドロゲル(clopidrogel)臭化水素酸塩の多形体型
WO2008004249A2 (en) * 2006-07-04 2008-01-10 Msn Laboratories Limited An improved process for the preparation of clopidogrel and its pharmaceutically acceptable salts
WO2008060934A2 (en) * 2006-11-14 2008-05-22 Acusphere, Inc. Formulations of tetrahydropyridine antiplatelet agents for parenteral or oral administration
EP1970054A2 (en) 2007-03-14 2008-09-17 Ranbaxy Laboratories Limited Clopidogrel tablets
WO2008134600A1 (en) 2007-04-27 2008-11-06 Cydex Pharmaceuticals, Inc. Formulations containing clopidogrel and sulfoalkyl ether cyclodextrin and methods of use
EP2107061A1 (en) 2008-04-02 2009-10-07 Krka Tovarna Zdravil, D.D., Novo Mesto Process for the preparation of optically enriched clopidogrel
CN102120745A (zh) * 2011-01-31 2011-07-13 天津红日药业股份有限公司 一种盐酸氯吡格雷的晶型ⅰ及其制备方法和用途
CN102367257A (zh) * 2011-11-21 2012-03-07 天津红日药业股份有限公司 氯吡格雷盐酸盐的单晶晶型,它们的制备及应用
US8835407B2 (en) 2009-05-13 2014-09-16 Cydex Pharmaceuticals, Inc. Pharmaceutical compositions comprising prasugrel and cyclodextrin derivatives and methods of making and using the same

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100742134B1 (ko) * 2006-02-07 2007-07-24 경동제약 주식회사 결정성S-(+)-메틸-2-(2-클로로페닐)-2-(6,7-디히드로티에노[3,2-c]피리딘-5(4H)-일)아세테이트·캄실레이트를 포함하는약학적 조성물
US7985859B2 (en) * 2007-05-30 2011-07-26 Wockhardt Ltd. Processes for the preparation of clopidogrel
WO2012123958A1 (en) 2011-02-14 2012-09-20 Cadila Healthcare Limited Highly pure salts of clopidogrel free of genotoxic impurities
HU1400294A2 (hu) 2014-06-13 2015-12-28 Skillpharm Kft Clopidogrel új alkalmazása

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0099802A1 (fr) * 1982-07-13 1984-02-01 Elf Sanofi Nouveaux dérivés de la thiéno-(3,2-c) pyridine, leur procédé de préparation et leur application thérapeutique
EP0281459A1 (fr) * 1987-02-17 1988-09-07 Sanofi Enantiomère dextrogyre de l'alpha-(tétrahydro-4,5,6,7 thiéno (3,2-c)pyridyl-5) (chloro-2 phényl)-acétate de méthyle, son procédé de préparation et les compositions pharmaceutiques le renfermant
WO1999065915A1 (fr) * 1998-06-15 1999-12-23 Sanofi-Synthelabo Forme polymorphe de l'hydrogenosulfate de clopidogrel

Family Cites Families (4)

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Publication number Priority date Publication date Assignee Title
US5189170A (en) * 1989-09-29 1993-02-23 Sanofi Process for the preparation of phenylacetic derivatives of thieno-pyridines
FR2664596B1 (fr) * 1990-07-10 1994-06-10 Sanofi Sa Procede de preparation d'un derive n-phenylacetique de tetrahydrothieno [3,2-c] pyridine et son intermediaire de synthese.
HU225504B1 (en) * 1997-05-13 2007-01-29 Sanofi Aventis Novel halophenyl-(2-(2-thienyl)-ethylamino)-acetonitriles and process for producing them
HU226421B1 (en) * 1998-11-09 2008-12-29 Sanofi Aventis Process for racemizing optically active 2-(2-chlorophenyl)-2-(2-(2-thienyl)-ethylamino)-acetamides

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0099802A1 (fr) * 1982-07-13 1984-02-01 Elf Sanofi Nouveaux dérivés de la thiéno-(3,2-c) pyridine, leur procédé de préparation et leur application thérapeutique
EP0281459A1 (fr) * 1987-02-17 1988-09-07 Sanofi Enantiomère dextrogyre de l'alpha-(tétrahydro-4,5,6,7 thiéno (3,2-c)pyridyl-5) (chloro-2 phényl)-acétate de méthyle, son procédé de préparation et les compositions pharmaceutiques le renfermant
WO1999065915A1 (fr) * 1998-06-15 1999-12-23 Sanofi-Synthelabo Forme polymorphe de l'hydrogenosulfate de clopidogrel

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
HERBERT J-M: "CLOPIDOGREL AND ANTIPLATELET THERAPY", EXPERT OPINION ON INVESTIGATIONAL DRUGS, ASHLEY PUBLICATIONS LTD., LONDON, GB, vol. 3, no. 5, 1 May 1994 (1994-05-01), pages 449 - 455, XP000607616, ISSN: 1354-3784 *

Cited By (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7897613B2 (en) 2003-09-11 2011-03-01 Generics [Uk] Limited Crystalline polymorphs of clopidogrel
EP2149578A1 (en) * 2003-09-11 2010-02-03 Merck Generics (UK) Limited Novel crystalline polymorphs of clopidogrel
EP1772456A1 (en) * 2003-09-11 2007-04-11 Generics (UK) Limited Novel crystalline polymorphs of clopidogrel
EP1837337A1 (en) * 2003-09-11 2007-09-26 Merck Generics (UK) Limited Novel crystalline polymorphs of clopidogrel
WO2005026174A1 (en) * 2003-09-11 2005-03-24 Generics [Uk] Limited Novel crystalline polymorphs of clopidogrel
WO2005068471A1 (en) * 2004-01-13 2005-07-28 Zentiva, A.S. New crystalline forms of clopidogrel hydrobromide and methods of their preparation
EA008972B1 (ru) * 2004-01-13 2007-10-26 Зентива А.С. Новые кристаллические формы гидробромида клопидогреля и способы их получения
WO2005104663A3 (en) * 2004-03-05 2006-09-28 Sanjay Govind Barve Industrial process for preparation of clopidogrel hydrogen sulphate
JP2007532530A (ja) * 2004-04-09 2007-11-15 ハンミ ファーム. シーオー., エルティーディー. 結晶性クロピドグレルナフタレンスルホン酸塩又はその水和物、その製造方法及びそれを含む医薬組成物
WO2005097804A1 (en) * 2004-04-09 2005-10-20 Hanmi Pharm. Co., Ltd. Crystalline clopidogrel naphthalenesulfonate or hydrate thereof, method for preparing same and pharmaceutical composition containing same
JP2007533744A (ja) * 2004-04-20 2007-11-22 サノフイ−アベンテイス (+)−(S)−α−(2−クロロフェニル)−6,7−ジヒドロチエノ[3,2−C]ピリジン−5(4H)酢酸メチル臭化水素酸塩、クロピドロゲル(clopidrogel)臭化水素酸塩の多形体型
JP2007533746A (ja) * 2004-04-20 2007-11-22 サノフイ−アベンテイス クロピドグレル塩及びその多形型
WO2005103059A1 (en) * 2004-04-20 2005-11-03 Sanofi-Aventis Clopidogrel salt and polymorphic forms thereof
EA010829B1 (ru) * 2004-04-20 2008-12-30 Санофи-Авентис Клопидогрель и его полиморфные формы
WO2005117866A1 (en) * 2004-06-01 2005-12-15 Ivax Pharmaceuticals S.R.O. Amorphous clopidogrel hydrochloride and its antithrombotic use
EP1674468A1 (en) * 2004-12-21 2006-06-28 Ratiopharm GmbH Polymorphs of clopidogrel hydrobromide
EP1693375A1 (en) * 2005-02-21 2006-08-23 KRKA, tovarna zdravil, d.d., Novo mesto Process for preparing clopidrogel hydrogen sulfate of form I
WO2006087226A1 (en) * 2005-02-21 2006-08-24 Krka, Tovarna Zdravil, D.D., Novo Mesto Process for preparing clopidogrel hydrogen sulfate of form i
WO2007029096A3 (en) * 2005-09-05 2007-08-23 Kiran Kumar Gangakhedkar Novel polymorphic forms of clopidogrel hydrochloride
WO2007029080A1 (en) * 2005-09-05 2007-03-15 Ranbaxy Laboratories Limited Preparation of form i of clopidogrel hydrochloride
WO2007029096A2 (en) * 2005-09-05 2007-03-15 Ranbaxy Laboratories Limited Novel polymorphic forms of clopidogrel hydrochloride
WO2007073095A1 (en) * 2005-12-22 2007-06-28 Sk Chemicals Co., Ltd. Process for the preparation of (s)-(+)-clopidogrel on a solid-phase
WO2007074995A1 (en) * 2005-12-26 2007-07-05 Sk Chemicals Co., Ltd. Process for the preparation of s-(+)-clopidogrel by optical resolution
US7696351B2 (en) 2005-12-26 2010-04-13 Sk Chemicals Co., Ltd. Process for the preparation of S-(+)-clopidogrel by optical resolution
KR101235117B1 (ko) * 2005-12-26 2013-02-20 에스케이케미칼주식회사 광학분리에 의한 (s)-(+)-클로피도그렐의 제조방법
WO2008004249A3 (en) * 2006-07-04 2008-04-10 Msn Lab Ltd An improved process for the preparation of clopidogrel and its pharmaceutically acceptable salts
WO2008004249A2 (en) * 2006-07-04 2008-01-10 Msn Laboratories Limited An improved process for the preparation of clopidogrel and its pharmaceutically acceptable salts
WO2008060934A2 (en) * 2006-11-14 2008-05-22 Acusphere, Inc. Formulations of tetrahydropyridine antiplatelet agents for parenteral or oral administration
WO2008060934A3 (en) * 2006-11-14 2008-09-12 Acusphere Inc Formulations of tetrahydropyridine antiplatelet agents for parenteral or oral administration
EP1970054A2 (en) 2007-03-14 2008-09-17 Ranbaxy Laboratories Limited Clopidogrel tablets
US8853236B2 (en) 2007-04-27 2014-10-07 Cydex Pharmaceuticals, Inc. Formulations containing clopidogrel and sulfoalkyl ether cyclodextrin and methods of use
US9125945B2 (en) 2007-04-27 2015-09-08 Cydex Pharmaceuticals, Inc. Formulations containing clopidogrel and sulfoalkyl ether cyclodextrin and methods of use
US10512697B2 (en) 2007-04-27 2019-12-24 Cydex Pharmaceuticals, Inc. Formulations containing clopidogrel and sulfoalkyl ether cyclodextrin and methods of use
US8343995B2 (en) 2007-04-27 2013-01-01 Cydex Pharmaceuticals, Inc. Formulations containing clopidogrel and sulfoalkyl ether cyclodextrin and methods of use
WO2008134600A1 (en) 2007-04-27 2008-11-06 Cydex Pharmaceuticals, Inc. Formulations containing clopidogrel and sulfoalkyl ether cyclodextrin and methods of use
US9623045B2 (en) 2007-04-27 2017-04-18 Cydex Pharmaceuticals, Inc. Formulations containing clopidogrel and sulfoalkyl ether cyclodextrin and methods of use
US10034947B2 (en) 2007-04-27 2018-07-31 Cydex Pharmaceuticals, Inc. Formulations containing clopidogrel and sulfoalkyl ether cyclodextrin and methods of use
EP3766493A1 (en) 2007-04-27 2021-01-20 CyDex Pharmaceuticals, Inc. Method for improving the stability of clopidogrel using sulfoalkyl ether cyclodextrin
EP2107061A1 (en) 2008-04-02 2009-10-07 Krka Tovarna Zdravil, D.D., Novo Mesto Process for the preparation of optically enriched clopidogrel
US9399067B2 (en) 2009-05-13 2016-07-26 Cydex Pharmaceuticals, Inc. Pharmaceutical compositions comprising prasugrel and cyclodextrin derivatives and methods of making and using the same
US8835407B2 (en) 2009-05-13 2014-09-16 Cydex Pharmaceuticals, Inc. Pharmaceutical compositions comprising prasugrel and cyclodextrin derivatives and methods of making and using the same
US10111863B2 (en) 2009-05-13 2018-10-30 Cydex Pharmaceuticals, Inc. Pharmaceutical compositions comprising prasugrel and cyclodextrin derivatives and methods of making and using the same
CN102120745B (zh) * 2011-01-31 2013-04-10 天津红日药业股份有限公司 一种盐酸氯吡格雷的晶型ⅰ及其制备方法和用途
CN102120745A (zh) * 2011-01-31 2011-07-13 天津红日药业股份有限公司 一种盐酸氯吡格雷的晶型ⅰ及其制备方法和用途
CN102367257B (zh) * 2011-11-21 2014-05-07 天津红日药业股份有限公司 氯吡格雷盐酸盐的单晶晶型,它们的制备及应用
CN102367257A (zh) * 2011-11-21 2012-03-07 天津红日药业股份有限公司 氯吡格雷盐酸盐的单晶晶型,它们的制备及应用

Also Published As

Publication number Publication date
HU0200438A3 (en) 2003-10-28
IS7385A (is) 2004-08-05
AU2002353251A1 (en) 2003-09-02
JP2005522441A (ja) 2005-07-28
EA200401025A1 (ru) 2004-12-30
HRP20040741A2 (en) 2004-12-31
HU0200438A2 (hu) 2003-09-29
PL370038A1 (xx) 2005-05-16
YU69604A (sh) 2006-08-17
KR20040079987A (ko) 2004-09-16
HU0200438D0 (en) 2002-04-29
CZ2004901A3 (cs) 2005-02-16
BG108868A (en) 2005-09-30
EA007119B1 (ru) 2006-06-30
US20050113406A1 (en) 2005-05-26
SK3362004A3 (sk) 2005-03-04
EP1474427A1 (en) 2004-11-10

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