EA006445B9 - Кристаллы, содержащие соль яблочной кислоты n-[2-(диэтиламино)этил]-5-[(5-фторо-2-оксо-1,2-дигидро-3h-индол-3-илиден)метил]-2,4-диметил-1h-пиррол-3-карбоксамида, способы их получения и их композиции - Google Patents
Кристаллы, содержащие соль яблочной кислоты n-[2-(диэтиламино)этил]-5-[(5-фторо-2-оксо-1,2-дигидро-3h-индол-3-илиден)метил]-2,4-диметил-1h-пиррол-3-карбоксамида, способы их получения и их композицииInfo
- Publication number
- EA006445B9 EA006445B9 EA200400183A EA200400183A EA006445B9 EA 006445 B9 EA006445 B9 EA 006445B9 EA 200400183 A EA200400183 A EA 200400183A EA 200400183 A EA200400183 A EA 200400183A EA 006445 B9 EA006445 B9 EA 006445B9
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- ylidene
- carboxamide
- diethylamino
- pyrrole
- oxo
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title abstract 4
- 150000004701 malic acid derivatives Chemical class 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title abstract 2
- -1 5-fluoro-2-oxo-3h-indole-3-ylidene Chemical group 0.000 title 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 title 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 title 1
- WINHZLLDWRZWRT-UHFFFAOYSA-N N-[2-(diethylamino)ethyl]-5-[(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide Chemical compound CCN(CC)CCNC(=O)C1=C(C)NC(C=C2C3=CC(F)=CC=C3NC2=O)=C1C WINHZLLDWRZWRT-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- 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)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31235301P | 2001-08-15 | 2001-08-15 | |
| PCT/US2002/025649 WO2003016305A1 (en) | 2001-08-15 | 2002-08-13 | Crystals including a malic acid salt of n-[2-(diethylamino) ethyl]-5-[(5-fluoro-2-oxo-3h-indole-3-ylidene) methyl]-2, 4-dimethyl-1h-pyrrole-3-carboxamide, processes for its preparation and compositions thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| EA200400183A1 EA200400183A1 (ru) | 2004-08-26 |
| EA006445B1 EA006445B1 (ru) | 2005-12-29 |
| EA006445B9 true EA006445B9 (ru) | 2017-02-28 |
Family
ID=23211067
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200400183A EA006445B9 (ru) | 2001-08-15 | 2002-08-13 | Кристаллы, содержащие соль яблочной кислоты n-[2-(диэтиламино)этил]-5-[(5-фторо-2-оксо-1,2-дигидро-3h-индол-3-илиден)метил]-2,4-диметил-1h-пиррол-3-карбоксамида, способы их получения и их композиции |
Country Status (42)
Families Citing this family (59)
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| DK3168218T3 (en) | 2001-08-15 | 2019-01-14 | Pharmacia & Upjohn Co Llc | Crystalline comprising an L-malic acid salt of N- [2- (DIETHYLAMINO) ETHYL] -5 - [(5-FLUOR-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDE) METHYL] -2,4 -DIMETHYL-1H-PYRROL-3-CARBOXAMIDE FOR USE AS A MEDICINE |
| TW200418836A (en) * | 2002-09-10 | 2004-10-01 | Pharmacia Italia Spa | Formulations comprising an indolinone compound |
| MXPA06003661A (es) * | 2003-10-02 | 2006-06-05 | Pharmacia & Upjohn Co Llc | Sales y polimorfos de un compuesto de indolinona sustituido con pirrol. |
| US20060009510A1 (en) * | 2004-07-09 | 2006-01-12 | Pharmacia & Upjohn Company Llc | Method of synthesizing indolinone compounds |
| EP1773811B1 (en) * | 2004-07-22 | 2010-09-08 | Eli Lilly And Company | A crystalline variable hydrate of (s)-6-(4-(2-((3-(9h-carbazol-4-yloxy)-2-hydroxypropyl)amino)-2-methylpropyl)phenoxy)-3-pyridinecarbox amide hemisuccinate salt |
| KR20070119745A (ko) * | 2005-05-12 | 2007-12-20 | 화이자 인코포레이티드 | 수니티닙 말레이트를 사용하는 항암 병행 요법 |
| DE602006008015D1 (de) | 2005-09-19 | 2009-09-03 | Pfizer Prod Inc | Feste salzformen eines pyrrolsubstituierten 2-indolinons |
| US20090004213A1 (en) | 2007-03-26 | 2009-01-01 | Immatics Biotechnologies Gmbh | Combination therapy using active immunotherapy |
| EP2220072A2 (en) * | 2007-11-21 | 2010-08-25 | Teva Pharmaceutical Industries Ltd. | Polymorphs of sunitinib base and processes for preparation thereof |
| US20100256392A1 (en) * | 2007-11-21 | 2010-10-07 | Teva Pharmaceutical Industries Ltd. | Polymorphs of sunitinib base and processes for preparation thereof |
| WO2009074862A1 (en) * | 2007-12-12 | 2009-06-18 | Medichem S.A. | Polymorphic forms of a 3-pyrrole substituted 2-indolinone |
| 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 |
| 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 |
| 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 |
| KR20100135910A (ko) * | 2008-04-16 | 2010-12-27 | 낫코 파마 리미티드 | 수니티닙 염기의 신규한 다형 형태 |
| US8829039B2 (en) | 2008-05-23 | 2014-09-09 | Shanghai Institute Of Pharmaceutical Industry | Dihydroindolinone derivatives |
| US8153678B2 (en) * | 2008-06-13 | 2012-04-10 | 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 |
| JP2011527330A (ja) * | 2008-07-10 | 2011-10-27 | ジェネリクス・（ユーケー）・リミテッド | スニチニブリンゴ酸塩の結晶形の調製方法 |
| WO2010010454A2 (en) | 2008-07-24 | 2010-01-28 | Medichem, S.A. | Crystalline forms of a 3-pyrrole substituted 2-indolinone malate salt |
| CA2731605A1 (en) | 2008-07-24 | 2010-01-28 | Teva Pharmaceutical Industries Ltd. | Sunitinib and salts thereof and their polymorphs |
| 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 |
| CA2734965A1 (en) * | 2008-08-25 | 2010-03-04 | Generics [Uk] Limited | Novel crystalline form and processes for its preparation |
| 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 |
| WO2010076805A2 (en) | 2009-01-02 | 2010-07-08 | Hetero Research Foundation | Novel polymorphs of sunitinib malate |
| EA038195B1 (ru) | 2009-01-16 | 2021-07-22 | Экселиксис, Инк. | Малатная соль n-(4-{[6,7-бис-(метилокси)хинолин-4-ил]окси}фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида и ее применение для лечения рака почек и печени |
| 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 |
| WO2011033472A1 (en) | 2009-09-16 | 2011-03-24 | Ranbaxy Laboratories Limited | Salts of sunitinib |
| WO2011058521A2 (en) * | 2009-11-12 | 2011-05-19 | Ranbaxy Laboratories Limited | Process for the preparation of crystalline form i of l-malic acid salt of sunitinib |
| US8916716B2 (en) | 2009-11-19 | 2014-12-23 | Ranbaxy Laboratories Limited | Process for the preparation of crystalline form II of L-malic acid salt of sunitinib |
| EP2528913A1 (en) | 2010-01-29 | 2012-12-05 | 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 |
| EP2542550A1 (en) | 2010-03-04 | 2013-01-09 | 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 |
| EP2699598B1 (en) | 2011-04-19 | 2019-03-06 | Pfizer Inc | Combinations of anti-4-1bb antibodies and adcc-inducing antibodies for the treatment of cancer |
| ES2709110T3 (es) | 2012-03-23 | 2019-04-15 | Laurus Labs Ltd | Un proceso mejorado para la preparación de sunitinib y sus sales de adición de ácido |
| 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 |
| RU2737765C2 (ru) | 2012-05-04 | 2020-12-02 | Пфайзер Инк. | Простатоассоциированные антигены и иммунотерапевтические схемы на основе вакцин |
| 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 |
| US9278955B2 (en) | 2013-10-18 | 2016-03-08 | Sun Pharmaceutical Industries Limited | Ascorbic acid salt of sunitinib |
| HUE043042T2 (hu) | 2013-11-01 | 2019-07-29 | Pfizer | Vektorok prosztatához kapcsolódó antigének expressziójára |
| 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 |
| AU2020257415A1 (en) * | 2019-04-18 | 2021-11-11 | Meter Health, Inc. | Methods and compositions for treating respiratory arrhythmias |
| 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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2002
- 2002-08-13 DK DK16196036.4T patent/DK3168218T3/en active
- 2002-08-13 HR HR20040112A patent/HRP20040112B1/xx not_active IP Right Cessation
- 2002-08-13 CA CA002455050A patent/CA2455050C/en not_active Expired - Lifetime
- 2002-08-13 UA UA2004021084A patent/UA76483C2/uk unknown
- 2002-08-13 AU AU2002324684A patent/AU2002324684B2/en not_active Expired
- 2002-08-13 SK SK90-2004A patent/SK902004A3/sk unknown
- 2002-08-13 EA EA200400183A patent/EA006445B9/ru unknown
- 2002-08-13 DK DK02759342.5T patent/DK1419151T3/da active
- 2002-08-13 RS YU10304A patent/RS53251B/sr unknown
- 2002-08-13 JP JP2003521228A patent/JP4159988B2/ja not_active Expired - Lifetime
- 2002-08-13 MX MXPA04001452A patent/MXPA04001452A/es active IP Right Grant
- 2002-08-13 PT PT2759342T patent/PT1419151E/pt unknown
- 2002-08-13 NZ NZ531232A patent/NZ531232A/en not_active IP Right Cessation
- 2002-08-13 EP EP16196036.4A patent/EP3168218B1/en not_active Expired - Lifetime
- 2002-08-13 ES ES16196036T patent/ES2705063T3/es not_active Expired - Lifetime
- 2002-08-13 ES ES02759342.5T patent/ES2453164T3/es not_active Expired - Lifetime
- 2002-08-13 ME MEP-2008-520A patent/ME00414B/me unknown
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001037820A2 (en) * | 1999-11-24 | 2001-05-31 | Sugen, Inc. | Ionizable indolinone derivatives and their use as ptk ligands |
| WO2001060814A2 (en) * | 2000-02-15 | 2001-08-23 | Sugen, Inc. | Pyrrole substituted 2-indolinone protein kinase inhibitors |
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