AR036261A1 - Cristales de una sal del acido malico de una 2-indolinona sustituida con 3-pirrol , sus composiciones y metodos para su preparacion - Google Patents
Cristales de una sal del acido malico de una 2-indolinona sustituida con 3-pirrol , sus composiciones y metodos para su preparacionInfo
- Publication number
- AR036261A1 AR036261A1 ARP020103088A ARP020103088A AR036261A1 AR 036261 A1 AR036261 A1 AR 036261A1 AR P020103088 A ARP020103088 A AR P020103088A AR P020103088 A ARP020103088 A AR P020103088A AR 036261 A1 AR036261 A1 AR 036261A1
- Authority
- AR
- Argentina
- Prior art keywords
- crystals
- malic acid
- salt
- carboxamide
- diethylamino
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- 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
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- 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)
Abstract
Cristales y composiciones, en las cuales los cristales incluyen una sal del ácido málico de N-[2-(dietilamino)etil]-5-[(5-fluoro-1,2-dihidro-2-oxo-3H-indol-3-iliden)metil]-2,4-dimetil-1H-pirrol-3-carboxamida de fórmula (1). También se describen métodos para la preparación de dichos cristales. Un método para preparar un cristal anhidro, el cristal anhidro comprende una sal del ácido málico de N-[2-(dietilamino)etil]-5-[(5-fluoro-1,2-dihidro-2-oxo-3H-indol-3-iliden)metil]-2,4-dimetil-1H-pirrol-3-carboxamida, el método comprende: combinar ácido málico; N-[2-(dietilamino)etil]-5-[(5-fluoro-1,2-dihidro-2-oxo-3H-indol-3-iliden)metil]-2,4-dimetil-1H-pirrol-3-carboxamida; y un solvente; e inducir la sal para que se cristalice bajo condiciones de cristalización que comprenden uno o más factores que incluyen: una diferencia entre la temperatura inicial y la temperatura final de la solución de cristalización de cómo máximo 100°C; una velocidad de enfriamiento de cómo máximo 50°C por hora; no contiene precipitante; una relación de súper saturación de por lo menos 10 y/o sus combinaciones. Este compuesto es activo como inhibidor de proteinquinasas y se relaciona con los receptores de factor de crecimiento.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31235301P | 2001-08-15 | 2001-08-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR036261A1 true AR036261A1 (es) | 2004-08-25 |
Family
ID=23211067
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020103088A AR036261A1 (es) | 2001-08-15 | 2002-08-15 | Cristales de una sal del acido malico de una 2-indolinona sustituida con 3-pirrol , sus composiciones y metodos para su preparacion |
Country Status (43)
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| HN2003000272A (es) * | 2002-09-10 | 2008-07-29 | Pharmacia Italia Spa | Formulaciones que comprenden un compuesto de indolinona |
| JP4933259B2 (ja) * | 2003-10-02 | 2012-05-16 | ファルマシア・アンド・アップジョン・カンパニー・エルエルシー | ピロール置換インドリノン化合物の塩および多形 |
| US20060009510A1 (en) * | 2004-07-09 | 2006-01-12 | Pharmacia & Upjohn Company Llc | Method of synthesizing indolinone compounds |
| DE602005023474D1 (en) * | 2004-07-22 | 2010-10-21 | Lilly Co Eli | Kristallines variables hydrat von (s)-6-(4-(2-((3-(9h-carbazol-4-yloxy)-2-hydroxypropyl)amino)-2-methylpropyl)phenoxy)-3-pyridincarbonsäureamid-hemisuccinatsalz |
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| AU2006293644B2 (en) | 2005-09-19 | 2012-05-31 | Zoetis Services Llc | 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 |
| CA2709083A1 (en) * | 2007-12-12 | 2009-06-18 | 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 |
| US20110112164A1 (en) * | 2008-02-21 | 2011-05-12 | 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 |
| PL2274303T3 (pl) * | 2008-03-31 | 2013-03-29 | Teva Pharma | Sposoby otrzymywania sunitynibu i jego soli |
| US8466190B2 (en) | 2008-04-16 | 2013-06-18 | Natco Pharma Limited | Polymorphic forms of Sunitinib base |
| EP2292613B1 (en) | 2008-05-23 | 2015-09-30 | Shanghai Institute of Pharmaceutical Industry | Dihydroindolinone derivatives |
| SI2313371T1 (sl) * | 2008-06-13 | 2013-02-28 | Medichem, S.A. | Postopek za pripravo soli 3-pirol substituirane 2-indolinonske jabolčne kisline |
| 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 |
| CA2731605A1 (en) * | 2008-07-24 | 2010-01-28 | Teva Pharmaceutical Industries Ltd. | Sunitinib and salts thereof and their polymorphs |
| EP2342195B1 (en) * | 2008-07-24 | 2014-09-10 | Medichem, S.A. | Crystalline forms of a 3-pyrrole substituted 2-indolinone malate salt |
| US20120029046A1 (en) * | 2008-08-25 | 2012-02-02 | Generics (Uk) Limited | Crystalline form of sunitinib and processes for its preparation |
| CN102197034A (zh) * | 2008-08-25 | 2011-09-21 | 基因里克斯(英国)有限公司 | 舒尼替尼的新型多晶型物及其制备方法 |
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| EP2186809A1 (en) * | 2008-11-13 | 2010-05-19 | LEK Pharmaceuticals D.D. | New crystal form of sunitinib malate |
| EP2896618A1 (en) | 2009-01-02 | 2015-07-22 | Hetero Research Foundation | Polymorphs of sunitinib malate |
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| 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 |
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| US20120271056A1 (en) | 2009-11-12 | 2012-10-25 | Ranbaxy Laboratories Limited | Process for the preparation of crystalline form i of l-malic acid salt of sunitinib |
| WO2011061613A1 (en) | 2009-11-19 | 2011-05-26 | Ranbaxy Laboratories Limited | Process for the preparation of crystalline form ii of l-malic acid salt of sunitinib |
| US20130210885A1 (en) | 2010-01-29 | 2013-08-15 | 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 |
| AU2011222470A1 (en) | 2010-03-04 | 2012-09-27 | Ranbaxy Laboratories Limited | Process for the direct preparation of malic acid salt of sunitinib |
| US20160185760A1 (en) | 2010-03-18 | 2016-06-30 | 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 |
| US20140178368A1 (en) | 2011-04-19 | 2014-06-26 | Leslie Lynne SHARP | 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 |
| RU2609651C2 (ru) | 2012-05-04 | 2017-02-02 | Пфайзер Инк. | Простатоассоциированные антигены и иммунотерапевтические схемы на основе вакцин |
| CA2838585A1 (en) | 2013-10-18 | 2015-04-18 | Hari Babu Matta | An ascorbic acid salt of sunitinib |
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| 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 |
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| 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 |
| KR20240025990A (ko) | 2022-08-19 | 2024-02-27 | 주식회사 스카이테라퓨틱스 | 무정형 수니티닙, 그 제조방법 및 이를 포함한 의약 조성물 |
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2002
- 2002-08-13 CZ CZ2004196A patent/CZ2004196A3/cs unknown
- 2002-08-13 SI SI200231043T patent/SI1419151T1/sl unknown
- 2002-08-13 PL PL368317A patent/PL216524B1/pl unknown
- 2002-08-13 CN CNB2005101286242A patent/CN100364991C/zh not_active Expired - Lifetime
- 2002-08-13 EP EP16196036.4A patent/EP3168218B1/en not_active Expired - Lifetime
- 2002-08-13 ES ES11156767.3T patent/ES2623094T3/es not_active Expired - Lifetime
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- 2002-08-13 ME MEP-2008-520A patent/ME00414B/me unknown
- 2002-08-13 KR KR1020047002173A patent/KR100639281B1/ko active IP Right Grant
- 2002-08-13 US US10/218,985 patent/US20030069298A1/en not_active Abandoned
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- 2002-08-13 AU AU2002324684A patent/AU2002324684B2/en not_active Expired
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- 2002-08-13 UA UA2004021084A patent/UA76483C2/uk unknown
- 2002-08-13 CA CA002455050A patent/CA2455050C/en not_active Expired - Lifetime
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- 2002-08-13 ES ES16196036T patent/ES2705063T3/es not_active Expired - Lifetime
- 2002-08-13 EP EP02759342.5A patent/EP1419151B1/en not_active Expired - Lifetime
- 2002-08-13 ES ES02759342.5T patent/ES2453164T3/es not_active Expired - Lifetime
- 2002-08-13 EA EA200400183A patent/EA006445B9/ru unknown
- 2002-08-13 HU HU0700036A patent/HU229206B1/hu unknown
- 2002-08-13 BR BR0211612-0A patent/BR0211612A/pt not_active Application Discontinuation
- 2002-08-13 TR TR2019/00509T patent/TR201900509T4/tr unknown
- 2002-08-13 IL IL16009702A patent/IL160097A0/xx active IP Right Grant
- 2002-08-13 DK DK16196036.4T patent/DK3168218T3/en active
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