JP2007507482A5 - - Google Patents
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- Publication number
- JP2007507482A5 JP2007507482A5 JP2006530728A JP2006530728A JP2007507482A5 JP 2007507482 A5 JP2007507482 A5 JP 2007507482A5 JP 2006530728 A JP2006530728 A JP 2006530728A JP 2006530728 A JP2006530728 A JP 2006530728A JP 2007507482 A5 JP2007507482 A5 JP 2007507482A5
- Authority
- JP
- Japan
- Prior art keywords
- maleate
- powder
- salt
- pattern including
- ray diffraction
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 claims 6
- 239000011780 sodium chloride Substances 0.000 claims 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims 5
- 241000124008 Mammalia Species 0.000 claims 4
- 239000002775 capsule Substances 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 3
- VZCYOOQTPOCHFL-UPHRSURJSA-L maleate(2-) Chemical compound [O-]C(=O)\C=C/C([O-])=O VZCYOOQTPOCHFL-UPHRSURJSA-L 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 239000012458 free base Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 1
- -1 maleate carboxamide Chemical class 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
Images
Claims (12)
- 5-[(Z)-(5-フルオロ-2-オキソ-1,2-ジヒドロ-3H-インドール-3-イリデン)メチル]-N-[(2S)-2-ヒドロキシ-3-モルホリン-4-イルプロピル]-2,4-ジメチル-1H-ピロール-3-カルボキサミドの結晶性非吸湿性マレイン酸塩。
- 塩が、回折角(2θ)12.7および15.4にピークを含む粉末X線回折パターンを有する、請求項1に記載の塩。
- 塩が、回折角(2θ)13.1および15.9にピークを含む粉末X線回折パターンを有する、請求項1に記載の塩。
- 塩が、回折角(2θ)12.7, 13.1, 15.4および15.9にピークを含む粉末X線回折パターンを有する、請求項1に記載の塩。
- 図1に示すものと本質上同じ回折角(2θ)にピークを含む粉末X線回折パターンを持つ、請求項1に記載のマレイン酸塩。
- 図2に示すものと本質的に同一の回折角(2θ)にピークを含む粉末X線回折パターンを有する、請求項1に記載のマレイン酸塩。
- 請求項1〜6のいずれか１項に記載のマレイン酸塩および医薬として許容される担体を含む癌の治療用医薬組成物。
- カプセルの形態にある請求項7に記載の医薬組成物。
- 5〜75mg の遊離塩基相当量の5-[(Z)-(5-フルオロ-2-オキソ-1,2-ジヒドロ-3H-インドール-3-イリデン)メチル]-N-[(2S)-2-ヒドロキシ-3-モルホリン-4-イルプロピル]-2,4-ジメチル-1H-ピロール-3-カルボキサミドのマレイン酸塩を含む、請求項8に記載のカプセル剤。
- 10〜25mg の遊離塩基相当量の5-[(Z)-(5-フルオロ-2-オキソ-1,2-ジヒドロ-3H-インドール-3-イリデン)メチル]-N-[(2S)-2-ヒドロキシ-3-モルホリン-4-イルプロピル]-2,4-ジメチル-1H-ピロール-3-カルボキサミドのマレイン酸塩を含む、請求項8に記載のカプセル剤。
- 哺乳動物に、請求項7に記載の医薬組成物の治療有効量を投与することを含む、哺乳動物の癌を治療する方法。
- 哺乳動物に、請求項8に記載のカプセル剤を投与することを含む、哺乳動物の癌を治療する方法。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US50810403P | 2003-10-02 | 2003-10-02 | |
| US60/508,104 | 2003-10-02 | ||
| PCT/IB2004/003070 WO2005033098A1 (en) | 2003-10-02 | 2004-09-20 | Salts and polymorphs of a pyrrole-substituted indolinone compound |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007507482A JP2007507482A (ja) | 2007-03-29 |
| JP2007507482A5 true JP2007507482A5 (ja) | 2007-11-08 |
| JP4933259B2 JP4933259B2 (ja) | 2012-05-16 |
Family
ID=34421700
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006530728A Expired - Fee Related JP4933259B2 (ja) | 2003-10-02 | 2004-09-20 | ピロール置換インドリノン化合物の塩および多形 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US7247627B2 (ja) |
| EP (1) | EP1670785B1 (ja) |
| JP (1) | JP4933259B2 (ja) |
| KR (2) | KR20080007520A (ja) |
| CN (1) | CN100432072C (ja) |
| AR (1) | AR047762A1 (ja) |
| AT (1) | ATE473223T1 (ja) |
| AU (1) | AU2004277464B2 (ja) |
| BR (1) | BRPI0415022A (ja) |
| CA (1) | CA2540639C (ja) |
| CY (1) | CY1110771T1 (ja) |
| DE (1) | DE602004028028D1 (ja) |
| DK (1) | DK1670785T3 (ja) |
| ES (1) | ES2348623T3 (ja) |
| HK (1) | HK1093068A1 (ja) |
| IL (1) | IL174414A (ja) |
| MX (1) | MXPA06003661A (ja) |
| NO (1) | NO20061246L (ja) |
| NZ (1) | NZ546001A (ja) |
| PL (1) | PL1670785T3 (ja) |
| PT (1) | PT1670785E (ja) |
| RU (1) | RU2319702C2 (ja) |
| SI (1) | SI1670785T1 (ja) |
| TW (1) | TW200524921A (ja) |
| WO (1) | WO2005033098A1 (ja) |
| ZA (1) | ZA200602691B (ja) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050182122A1 (en) * | 2003-11-20 | 2005-08-18 | Bello Carlo L. | Method of treating abnormal cell growth using indolinone compounds |
| BRPI0607579A2 (pt) * | 2005-03-23 | 2009-09-15 | Pfizer Prod Inc | uso de anticorpo anti-ctla4 e indolinona para a preparação de medicamentos para o tratamento de cáncer |
| CA2622870A1 (en) * | 2005-09-20 | 2007-03-29 | Pfizer Products Inc. | Dosage forms and methods of treatment using a tyrosine kinase inhibitor |
| TWI384986B (zh) * | 2007-01-17 | 2013-02-11 | Lg Life Sciences Ltd | 抗病毒劑之順丁烯二酸單鹽以及含有該單鹽之醫藥組成物 |
| ES2682283T3 (es) * | 2007-04-04 | 2018-09-19 | Otsuka Chemical Co., Ltd. | Titanato de potasio, procedimiento de producción del mismo, materiales de fricción y composiciones de resina |
| KR20120015363A (ko) * | 2008-09-17 | 2012-02-21 | 노파르티스 아게 | Ｎ-［6-(시스-2,6-디메틸모르폴린-4-일)피리딘-3-일］-2-메틸-4'-(트리플루오로메톡시)［1,1'-비페닐］-3-카르복스아미드의 염 |
| WO2012042421A1 (en) | 2010-09-29 | 2012-04-05 | Pfizer Inc. | Method of treating abnormal cell growth |
| US9851313B2 (en) * | 2015-03-03 | 2017-12-26 | Panalytical B.V. | Quantitative X-ray analysis—ratio correction |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5534522A (en) * | 1995-06-07 | 1996-07-09 | Warner-Lambert Company | (R)-(Z)-1-azabicyclo [2.2.1] heptan-3-one,O-[3-(3-methoxyphenyl)-2-propynyl] oxime maleate as a pharmaceutical agent |
| DE19622489A1 (de) * | 1996-06-05 | 1997-12-11 | Hoechst Ag | Salze des 3-(2-(4-(4-(Amino-imino-methyl)-phenyl)-4- methyl-2,5-dioxo-imidazolidin-1-yl)-acetylamino)-3- phenyl-propionsäure-ethylesters |
| UA73976C2 (uk) * | 2000-02-15 | 2005-10-17 | Суджен, Інк. | Заміщені піролом 2-індолінони, фармацевтична композиція, спосіб модуляції каталітичної активності протеїнкінази та спосіб лікування або профілактики захворювання, пов'язаного з протеїнкіназою |
| AR042586A1 (es) * | 2001-02-15 | 2005-06-29 | Sugen Inc | 3-(4-amidopirrol-2-ilmetiliden)-2-indolinona como inhibidores de la protein quinasa; sus composiciones farmaceuticas; un metodo para la modulacion de la actividad catalitica de la proteinquinasa; un metodo para tratar o prevenir una afeccion relacionada con la proteinquinasa |
| EP1419151B1 (en) * | 2001-08-15 | 2014-02-26 | Pharmacia & Upjohn Company LLC | Chrystals including a malic acid salt of n-[2-(diethylamino)ethyl] -5-[(5-fluoro-1,2-dihydro-2-oxo-3h-indole-3-ylidene)methyl] -2,4-dimethyl-1h-pyrrole-3-carboxamide, processes for its preparation and compositions thereof |
| YU67702A (sh) | 2001-09-28 | 2004-12-31 | Pfizer Products Inc. | Postupak za dobijanje alkansulfonil piridina |
| TWI259081B (en) * | 2001-10-26 | 2006-08-01 | Sugen Inc | Treatment of acute myeloid leukemia with indolinone compounds |
| JP2005528344A (ja) * | 2002-02-15 | 2005-09-22 | 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 | インドリノン誘導体の製造法 |
| TW200418836A (en) * | 2002-09-10 | 2004-10-01 | Pharmacia Italia Spa | Formulations comprising an indolinone compound |
-
2004
- 2004-09-20 PT PT04769435T patent/PT1670785E/pt unknown
- 2004-09-20 ES ES04769435T patent/ES2348623T3/es not_active Expired - Lifetime
- 2004-09-20 CN CNB2004800287364A patent/CN100432072C/zh not_active Expired - Fee Related
- 2004-09-20 JP JP2006530728A patent/JP4933259B2/ja not_active Expired - Fee Related
- 2004-09-20 AT AT04769435T patent/ATE473223T1/de active
- 2004-09-20 MX MXPA06003661A patent/MXPA06003661A/es active IP Right Grant
- 2004-09-20 NZ NZ546001A patent/NZ546001A/en unknown
- 2004-09-20 DE DE602004028028T patent/DE602004028028D1/de not_active Expired - Lifetime
- 2004-09-20 RU RU2006110541/04A patent/RU2319702C2/ru not_active IP Right Cessation
- 2004-09-20 AU AU2004277464A patent/AU2004277464B2/en not_active Ceased
- 2004-09-20 CA CA2540639A patent/CA2540639C/en not_active Expired - Fee Related
- 2004-09-20 KR KR1020087000428A patent/KR20080007520A/ko not_active Application Discontinuation
- 2004-09-20 SI SI200431486T patent/SI1670785T1/sl unknown
- 2004-09-20 PL PL04769435T patent/PL1670785T3/pl unknown
- 2004-09-20 BR BRPI0415022-8A patent/BRPI0415022A/pt not_active IP Right Cessation
- 2004-09-20 KR KR1020067006363A patent/KR20060058728A/ko active Search and Examination
- 2004-09-20 DK DK04769435.1T patent/DK1670785T3/da active
- 2004-09-20 EP EP04769435A patent/EP1670785B1/en not_active Expired - Lifetime
- 2004-09-20 WO PCT/IB2004/003070 patent/WO2005033098A1/en active Application Filing
- 2004-09-30 US US10/956,420 patent/US7247627B2/en not_active Expired - Fee Related
- 2004-10-01 AR ARP040103580A patent/AR047762A1/es not_active Application Discontinuation
- 2004-10-01 TW TW093129924A patent/TW200524921A/zh unknown
-
2006
- 2006-03-17 NO NO20061246A patent/NO20061246L/no not_active Application Discontinuation
- 2006-03-20 IL IL174414A patent/IL174414A/en not_active IP Right Cessation
- 2006-03-31 ZA ZA200602691A patent/ZA200602691B/en unknown
- 2006-12-15 HK HK06113815.0A patent/HK1093068A1/xx not_active IP Right Cessation
-
2010
- 2010-09-03 CY CY20101100810T patent/CY1110771T1/el unknown
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