CN100364991C - 2,4-二甲基-1h-吡咯-3-甲酰胺衍生物的苹果酸盐的晶体、其制备方法和其组合物 - Google Patents
2,4-二甲基-1h-吡咯-3-甲酰胺衍生物的苹果酸盐的晶体、其制备方法和其组合物 Download PDFInfo
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- CN100364991C CN100364991C CNB2005101286242A CN200510128624A CN100364991C CN 100364991 C CN100364991 C CN 100364991C CN B2005101286242 A CNB2005101286242 A CN B2005101286242A CN 200510128624 A CN200510128624 A CN 200510128624A CN 100364991 C CN100364991 C CN 100364991C
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- pyrrole
- dimethyl
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- carboxamide
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyrrole Compounds (AREA)
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| CNB02815892XA Ceased CN100439360C (zh) | 2001-08-15 | 2002-08-13 | 包括n-[2-(二乙氨基)乙基]-5-[(5-氟-2-氧代-3h-吲哚-3-亚基)甲基]-2,4-二甲基-1h-吡咯-3-甲酰胺的苹果酸盐的晶体、其制备方法和其组合物 |
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| CZ2004196A3 (cs) | 2001-08-15 | 2005-01-12 | Pharmacia & Upjohn Company | Krystaly obsahující sůl N-[2-(diethylamino)ethyl]-5-[(5-fluor-2-oxo-3H-indol-3-yliden) methyl]-2,4-dimethyl-1H-pyrrol 3-karboxamidu s kyselinou jablečnou, způsob jejich výroby a kompozice na jejich bázi |
| TW200418836A (en) * | 2002-09-10 | 2004-10-01 | Pharmacia Italia Spa | Formulations comprising an indolinone compound |
| PT1670785E (pt) * | 2003-10-02 | 2010-09-16 | Pharmacia & Upjohn Co Llc | Sais e polimorfos de um composto de indolinona substituída com pirrole |
| US20060009510A1 (en) * | 2004-07-09 | 2006-01-12 | Pharmacia & Upjohn Company Llc | Method of synthesizing indolinone compounds |
| MX2007000892A (es) * | 2004-07-22 | 2007-05-23 | Lilly Co Eli | Un hidrato variable cristalino de la sal de (s)-3-piridincarboxami da, 6-[4-[2-[[3-(9h-carbazol-4-iloxi)-2-hidroxipropil]amino]-2-met ilpropil]fenoxi]-hemisuccinato. |
| WO2006120557A1 (en) * | 2005-05-12 | 2006-11-16 | Pfizer Inc. | Anticancer combination therapy using sunitinib malate |
| CA2621569C (en) | 2005-09-19 | 2010-10-19 | Pfizer Products Inc. | Solid salt forms of a pyrrole substituted 2-indolinone |
| US20090004213A1 (en) | 2007-03-26 | 2009-01-01 | Immatics Biotechnologies Gmbh | Combination therapy using active immunotherapy |
| US20100256392A1 (en) * | 2007-11-21 | 2010-10-07 | Teva Pharmaceutical Industries Ltd. | Polymorphs of sunitinib base and processes for preparation thereof |
| EP2220071A2 (en) * | 2007-11-21 | 2010-08-25 | Teva Pharmaceutical Industries Ltd. | Sunitinib hemi-l-malate, polymorphs and preparation thereof, polymorphs of racemic sunitinib malate, compositins containing sunitinib base and malic acid and preparation thereof |
| US8389562B2 (en) * | 2007-12-12 | 2013-03-05 | Medichem, S.A. | Polymorphic forms of a 3-pyrrole substituted 2-indolinone |
| EP2113248A1 (en) | 2008-04-29 | 2009-11-04 | Ratiopharm GmbH | Pharmaceutical composition comprising N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2-,4-dimethyl-1H-pyrrole-3-carboxamide |
| EP2090306A1 (en) | 2008-02-13 | 2009-08-19 | Ratiopharm GmbH | Pharmaceutical compositions comprising N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide |
| AU2009215377A1 (en) * | 2008-02-21 | 2009-08-27 | Generics [Uk] Limited | Novel polymorphs and processes for their preparation |
| EP2098521A1 (en) * | 2008-03-06 | 2009-09-09 | Ratiopharm GmbH | Crystal forms of N-[2-(diethylamino) ethyl]-5-[fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrolle-3-carboxamide and methods for their prepparation |
| CA2720164A1 (en) * | 2008-03-31 | 2009-10-08 | Teva Pharmaceutical Industries Ltd. | Processes for preparing sunitinib and salts thereof |
| EP2280960A1 (en) * | 2008-04-16 | 2011-02-09 | Natco Pharma Limited | Novel polymorphic forms of sunitinib base |
| US8829039B2 (en) | 2008-05-23 | 2014-09-09 | Shanghai Institute Of Pharmaceutical Industry | Dihydroindolinone derivatives |
| WO2009150523A1 (en) * | 2008-06-13 | 2009-12-17 | Medichem, S.A. | Process for preparing a 3-pyrrole substituted 2-indolinone malate salt |
| EP2138167A1 (en) | 2008-06-24 | 2009-12-30 | ratiopharm GmbH | Pharmaceutical composition comprising N-[2-(Diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene) methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide |
| WO2009156837A2 (en) * | 2008-06-26 | 2009-12-30 | Medichem, S.A. | Amorphous form of a 3-pyrrole substituted 2-indolinone malate salt |
| WO2010004339A1 (en) | 2008-07-10 | 2010-01-14 | Generics [Uk] Limited | Processes for the preparation of crystalline forms of sunitinib malate |
| WO2010011834A2 (en) * | 2008-07-24 | 2010-01-28 | Teva Pharmaceutical Industries Ltd. | Sunitinib and salts thereof and their polymorphs |
| CN102164913A (zh) * | 2008-07-24 | 2011-08-24 | 麦迪凯姆股份公司 | 一种3-吡咯替代的2-吲哚酮苹果酸盐的结晶体形式 |
| CN102197035A (zh) * | 2008-08-25 | 2011-09-21 | 基因里克斯(英国)有限公司 | 舒尼替尼的结晶形式及其制备方法 |
| JP2012500838A (ja) * | 2008-08-25 | 2012-01-12 | ジェネリクス・（ユーケー）・リミテッド | スニチニブの新規な多形およびその調製方法 |
| EP2350056A1 (en) * | 2008-10-10 | 2011-08-03 | Medichem, S.A. | Process for preparing a 3-pyrrole subsituted 2-indolinone malate salt |
| EP2181991A1 (en) | 2008-10-28 | 2010-05-05 | LEK Pharmaceuticals D.D. | Novel salts of sunitinib |
| EP2186809A1 (en) * | 2008-11-13 | 2010-05-19 | LEK Pharmaceuticals D.D. | New crystal form of sunitinib malate |
| EP2373643A4 (en) * | 2009-01-02 | 2013-08-07 | Hetero Research Foundation | NEW SUNITINIB MALATE POLYMORPHS |
| DK2387563T4 (da) | 2009-01-16 | 2022-07-18 | Exelixis Inc | Malatsalt af n-(4-{ [ 6, 7-bis(methyloxy)quinolin-4-yl]oxy}phenyl-n'-(4-fluorphenyl)cyclopropan-1,1-dicarboxamid, og krystallinske former deraf til behandling af cancer |
| EP2255792A1 (en) | 2009-05-20 | 2010-12-01 | Ratiopharm GmbH | Pharmaceutical compositions for N-[2-(Diethylamino)ethyl]5-[(fluoro-1,2-dihydro-2-oxo-3H-indole-3-ylidene) methyl]-2,4-dimenthyl-1H-pyrrole-3-carboxamide |
| WO2011004200A1 (en) | 2009-07-10 | 2011-01-13 | Generics [Uk] Limited | Novel pyrrole derivatives |
| AU2010296849A1 (en) | 2009-09-16 | 2012-05-03 | Ranbaxy Laboratories Limited | Salts of sunitinib |
| EP2499133A2 (en) | 2009-11-12 | 2012-09-19 | Ranbaxy Laboratories Limited | Process for the preparation of crystalline form i of l-malic acid salt of sunitinib |
| EP2501694A1 (en) | 2009-11-19 | 2012-09-26 | Ranbaxy Laboratories Limited | Process for the preparation of crystalline form ii of l-malic acid salt of sunitinib |
| CA2788709A1 (en) | 2010-01-29 | 2011-08-04 | Ranbaxy Laboratories Limited | Crystalline forms of l-malic acid salt of sunitinib |
| WO2011100325A2 (en) | 2010-02-09 | 2011-08-18 | Sicor Inc. | Polymorphs of sunitinib salts |
| WO2011104555A2 (en) | 2010-02-25 | 2011-09-01 | Generics [Uk] Limited | Novel process |
| US20130123511A1 (en) | 2010-03-04 | 2013-05-16 | Ranbaxy Laboratories Limited | Process for the direct preparation of malic acid salt of sunitinib |
| WO2011114246A1 (en) | 2010-03-18 | 2011-09-22 | Ranbaxy Laboratories Limited | Process for the preparation of malic acid salt of sunitinib |
| WO2011128699A2 (en) | 2010-04-16 | 2011-10-20 | Generics [Uk] Limited | Novel process |
| WO2012042421A1 (en) | 2010-09-29 | 2012-04-05 | Pfizer Inc. | Method of treating abnormal cell growth |
| CA3019531A1 (en) | 2011-04-19 | 2012-10-26 | Pfizer Inc. | Combinations of anti-4-1bb antibodies and adcc-inducing antibodies for the treatment of cancer |
| EP2828251B1 (en) | 2012-03-23 | 2018-10-31 | Laurus Labs Limited | An improved process for the preparation of sunitinib and its acid addition salts thereof |
| PL399027A1 (pl) | 2012-04-27 | 2013-10-28 | Instytut Farmaceutyczny | Sposób otrzymywania N-[2-(dietylamino)etylo]-5-formylo-2,4-dimetylo-1H-pirolo-3-karboksyamidu o wysokiej czystosci i jego zastosowanie do wytwarzania sunitynibu |
| NZ701324A (en) | 2012-05-04 | 2016-09-30 | Pfizer | Prostate-associated antigens and vaccine-based immunotherapy regimens |
| US9604968B2 (en) | 2013-10-18 | 2017-03-28 | Sun Pharmaceutical Industries Limited | Pure crystalline Form II of L-malic acid salt of sunitinib and processes for its preparation |
| CA2838585A1 (en) | 2013-10-18 | 2015-04-18 | Hari Babu Matta | An ascorbic acid salt of sunitinib |
| KR102196884B1 (ko) | 2013-11-01 | 2020-12-30 | 화이자 인코포레이티드 | 전립선-연관 항원의 발현을 위한 벡터 |
| CN104693187A (zh) * | 2013-12-10 | 2015-06-10 | 安杰世纪生物科技（北京）有限公司 | 一种舒尼替尼L-苹果酸盐晶型λ及其制备方法 |
| CN104744442B (zh) * | 2013-12-25 | 2019-05-28 | 江苏豪森药业集团有限公司 | 苹果酸舒尼替尼的制备方法 |
| RU2567535C1 (ru) * | 2014-10-01 | 2015-11-10 | Олег Ростиславович Михайлов | КРИСТАЛЛИЧЕСКАЯ ε-МОДИФИКАЦИЯ N-[2-(ДИЭТИЛАМИНО)ЭТИЛ]-5-[(Z)-(5-ФТОР-1,2-ДИГИДРО-2-ОКСО-3Н-ИНДОЛ-3-ИЛИДЕН)МЕТИЛ]-2,4-ДИМЕТИЛ-1Н-ПИРРОЛ-3-КАРБОКСАМИД МАЛАТА, СПОСОБ ЕЕ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ЕЕ ОСНОВЕ |
| CN105712979A (zh) * | 2014-12-05 | 2016-06-29 | 广州白云山医药集团股份有限公司白云山制药总厂 | 一种苹果酸舒尼替尼晶型ⅰ的制备方法 |
| EP3539536A1 (en) | 2018-03-15 | 2019-09-18 | MH10 Spolka z ograniczona odpowiedzialnoscia | A pharmaceutical composition of sunitinib or its salt thereof in its polymorphic form i |
| JP2022529290A (ja) * | 2019-04-18 | 2022-06-20 | メーター ヘルス インコーポレイテッド | 呼吸性不整脈を処置するための方法および組成物 |
| EP3958845A1 (en) | 2019-04-25 | 2022-03-02 | Synthon B.V. | Pharmaceutical composition comprising amorphous sunitinib |
| JP7633786B2 (ja) * | 2020-09-18 | 2025-02-20 | 日本化薬株式会社 | スニチニブリンゴ酸塩を有効成分とする医薬錠剤 |
| KR20240025990A (ko) | 2022-08-19 | 2024-02-27 | 주식회사 스카이테라퓨틱스 | 무정형 수니티닙, 그 제조방법 및 이를 포함한 의약 조성물 |
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| DE9190141U1 (de) | 1990-10-15 | 1993-07-15 | Pfizer Inc., New York, N.Y. | Indolderivate |
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