JP2004512328A5 - - Google Patents
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- JP2004512328A5 JP2004512328A5 JP2002537718A JP2002537718A JP2004512328A5 JP 2004512328 A5 JP2004512328 A5 JP 2004512328A5 JP 2002537718 A JP2002537718 A JP 2002537718A JP 2002537718 A JP2002537718 A JP 2002537718A JP 2004512328 A5 JP2004512328 A5 JP 2004512328A5
- Authority
- JP
- Japan
- Prior art keywords
- salt
- methylpiperazin
- ylamino
- pyrimidin
- ylmethyl
- 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 description 12
- 239000011780 sodium chloride Substances 0.000 claims description 12
- -1 4-methylpiperazin-1-ylmethyl Chemical group 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 239000002253 acid Substances 0.000 claims description 5
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims description 3
- 239000004480 active ingredient Substances 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 239000003814 drug Substances 0.000 description 5
- 150000001875 compounds Chemical class 0.000 description 2
- 241000272517 Anseriformes Species 0.000 description 1
- KXDAEFPNCMNJSK-UHFFFAOYSA-N benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 description 1
- 150000003936 benzamides Chemical class 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000012458 free base Substances 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-M methanesulfonate Chemical compound CS([O-])(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-M 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
Description
【特許請求の範囲】
【請求項１】
消化管間質腫瘍の処置のための、活性成分として式Ｉ
【化１】
で示される４−(４−メチルピペラジン−１−イルメチル)−Ｎ−[４−メチル−３−(４−ピリジン−３−イル)ピリミジン−２−イルアミノ)フェニル]−ベンズアミドまたは薬学的に許容されるその塩を含む医薬。
【請求項２】
４−(４−メチルピペラジン−１−イルメチル)−Ｎ−[４−メチル−３−(４−ピリジン−３−イル)ピリミジン−２−イルアミノ)フェニル]−ベンズアミドの薬学的に許容される塩が酸付加塩である、請求項１に記載の医薬。
【請求項３】
４−(４−メチルピペラジン−１−イルメチル)−Ｎ−[４−メチル−３−(４−ピリジン−３−イル)ピリミジン−２−イルアミノ)フェニル]−ベンズアミドの薬学的に許容される酸付加塩がモノメタンスルホン酸塩である、請求項２に記載の医薬。
【請求項４】
４−(４−メチルピペラジン−１−イルメチル)−Ｎ−[４−メチル−３−(４−ピリジン−３−イル)ピリミジン−２−イルアミノ)フェニル]−ベンズアミドのモノメタンスルホン酸塩がβ結晶形である、請求項３に記載の医薬。
【請求項５】
１日当たりの服用量が４−(４−メチルピペラジン−１−イルメチル)−Ｎ−[４−メチル−３−(４−ピリジン−３−イル)ピリミジン−２−イルアミノ)フェニル]−ベンズアミド遊離塩基の２００〜６００ｍｇに相当する、請求項１〜４のいずれかに記載の医薬。
【請求項６】
服用が３ヶ月以上にわたる、請求項５に記載の医薬。
【請求項１】
消化管間質腫瘍の処置のための、活性成分として式Ｉ
【化１】
【請求項２】
４−(４−メチルピペラジン−１−イルメチル)−Ｎ−[４−メチル−３−(４−ピリジン−３−イル)ピリミジン−２−イルアミノ)フェニル]−ベンズアミドの薬学的に許容される塩が酸付加塩である、請求項１に記載の医薬。
【請求項３】
４−(４−メチルピペラジン−１−イルメチル)−Ｎ−[４−メチル−３−(４−ピリジン−３−イル)ピリミジン−２−イルアミノ)フェニル]−ベンズアミドの薬学的に許容される酸付加塩がモノメタンスルホン酸塩である、請求項２に記載の医薬。
【請求項４】
４−(４−メチルピペラジン−１−イルメチル)−Ｎ−[４−メチル−３−(４−ピリジン−３−イル)ピリミジン−２−イルアミノ)フェニル]−ベンズアミドのモノメタンスルホン酸塩がβ結晶形である、請求項３に記載の医薬。
【請求項５】
１日当たりの服用量が４−(４−メチルピペラジン−１−イルメチル)−Ｎ−[４−メチル−３−(４−ピリジン−３−イル)ピリミジン−２−イルアミノ)フェニル]−ベンズアミド遊離塩基の２００〜６００ｍｇに相当する、請求項１〜４のいずれかに記載の医薬。
【請求項６】
服用が３ヶ月以上にわたる、請求項５に記載の医薬。
驚くべきことに、今回、ＧＩＳＴが「化合物I」または薬学的に許容されるその塩で成功裡に処置され得ることが証明された。
「化合物I」のモノメタンスルホン酸付加塩（以後、「塩I」と呼ぶ。）およびその好ましい結晶形は、１９９９年１月２８日に公開された国際公開第９９／０３８５４号に記載されている。
Claims (3)
- 消化管間質腫瘍の処置のための、活性成分として式Ｉ
- 式Ｉの４−(４−メチルピペラジン−１−イルメチル)−Ｎ−[４−メチル−３−(４−ピリジン−３−イル)ピリミジン−２−イルアミノ)フェニル]−ベンズアミドの薬学的に許容される塩が酸付加塩である、請求項１に記載の医薬組成物。
- 式Ｉの４−(４−メチルピペラジン−１−イルメチル)−Ｎ−[４−メチル−３−(４−ピリジン−３−イル)ピリミジン−２−イルアミノ)フェニル]−ベンズアミドの薬学的に許容される酸付加塩がそのモノメタンスルホン酸塩である、請求項２に記載の医薬組成物。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24381000P | 2000-10-27 | 2000-10-27 | |
| PCT/EP2001/012442 WO2002034727A2 (en) | 2000-10-27 | 2001-10-26 | Treatment of gastrointestinal stromal tumors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004512328A JP2004512328A (ja) | 2004-04-22 |
| JP2004512328A5 true JP2004512328A5 (ja) | 2009-02-19 |
| JP4386635B2 JP4386635B2 (ja) | 2009-12-16 |
Family
ID=22920224
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002537718A Expired - Lifetime JP4386635B2 (ja) | 2000-10-27 | 2001-10-26 | 消化管間質腫瘍の処置 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US6958335B2 (ja) |
| EP (1) | EP1332137B1 (ja) |
| JP (1) | JP4386635B2 (ja) |
| KR (1) | KR100885129B1 (ja) |
| CN (1) | CN1276754C (ja) |
| AT (1) | ATE321556T1 (ja) |
| AU (2) | AU1826202A (ja) |
| BR (1) | BRPI0114870B8 (ja) |
| CA (1) | CA2424470C (ja) |
| CY (1) | CY1105055T1 (ja) |
| CZ (1) | CZ303944B6 (ja) |
| DE (1) | DE60118430T2 (ja) |
| DK (1) | DK1332137T3 (ja) |
| ES (1) | ES2260317T3 (ja) |
| HK (1) | HK1058193A1 (ja) |
| HU (1) | HU229106B1 (ja) |
| IL (2) | IL155029A0 (ja) |
| MX (1) | MXPA03003703A (ja) |
| NO (1) | NO324948B1 (ja) |
| NZ (1) | NZ525254A (ja) |
| PL (1) | PL209733B1 (ja) |
| PT (1) | PT1332137E (ja) |
| RU (1) | RU2301066C2 (ja) |
| SK (1) | SK287335B6 (ja) |
| WO (1) | WO2002034727A2 (ja) |
| ZA (1) | ZA200302155B (ja) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP0400038A3 (en) * | 2001-05-16 | 2007-05-29 | Novartis Ag | Combination comprising n-{5-[4-{-methyl-piperazino-methyl)-benzoylamino]-2-methylphenyl}-4-(3-pyridyl)-2pyrimidine-amine and a chemotherapeutic agent |
| CA2452368A1 (en) * | 2001-06-29 | 2003-01-09 | Ab Science | New potent, selective and non toxic c-kit inhibitors |
| DE60216281T2 (de) * | 2001-06-29 | 2007-07-05 | Ab Science | Die verwendung von tyrosinkinasehemmer zur behandlung von allergischen erkrankungen |
| CA2452169A1 (en) * | 2001-06-29 | 2003-01-09 | Ab Science | Use of tyrosine kinase inhibitors for treating inflammatory diseases |
| EP1401416B1 (en) * | 2001-06-29 | 2006-10-25 | AB Science | Use of c-kit inhibitors for treating inflammatory bowel diseases (ibd) |
| WO2003004006A2 (en) * | 2001-06-29 | 2003-01-16 | Ab Science | Use of potent, selective and non toxic c-kit inhibitors for treating tumor angiogenesis |
| ATE401078T1 (de) * | 2001-09-20 | 2008-08-15 | Ab Science | Die verwendung von c-kithemmern zur förderung des haarwuchses |
| ATE404202T1 (de) * | 2001-09-20 | 2008-08-15 | Ab Science | Die verwendung von potenten, selektiven und nontoxischen c-kithemmern zur behandlung von interstitieller blasenentzündung |
| DK1478380T3 (da) * | 2002-02-27 | 2006-11-27 | Ab Science | Anvendelse af tyrosinkinase-inhibitorer til behandling af CNS-lidelser |
| FR2844452A1 (fr) * | 2002-09-18 | 2004-03-19 | Inst Gustave Roussy Igr | Utilisation d'inhibiteurs specifiques de tyrosine kinases pour l'immunomodulation |
| US7144911B2 (en) | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| US7279576B2 (en) | 2002-12-31 | 2007-10-09 | Deciphera Pharmaceuticals, Llc | Anti-cancer medicaments |
| US7202257B2 (en) | 2003-12-24 | 2007-04-10 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
| CN100467064C (zh) * | 2003-09-19 | 2009-03-11 | 诺瓦提斯公司 | 伊马替尼和米哚妥林在制备治疗胃肠道基质肿瘤药物中的应用 |
| US20100210596A1 (en) * | 2006-02-01 | 2010-08-19 | Bluestone Jeffrey A | Use of aminopyrimidine compounds in the treatment of immune disorders |
| AU2007296744A1 (en) * | 2006-09-11 | 2008-03-20 | Curis, Inc. | Multi-functional small molecules as anti-proliferative agents |
| US7888361B2 (en) * | 2006-09-11 | 2011-02-15 | Curis, Inc. | Tyrosine kinase inhibitors containing a zinc binding moiety |
| US8642067B2 (en) | 2007-04-02 | 2014-02-04 | Allergen, Inc. | Methods and compositions for intraocular administration to treat ocular conditions |
| US20090082361A1 (en) * | 2007-09-26 | 2009-03-26 | Protia, Llc | Deuterium-enriched imatinib |
| CN101584696A (zh) | 2008-05-21 | 2009-11-25 | 上海艾力斯医药科技有限公司 | 包含喹唑啉衍生物的组合物及制备方法、用途 |
| WO2010120386A1 (en) | 2009-04-17 | 2010-10-21 | Nektar Therapeutics | Oligomer-protein tyrosine kinase inhibitor conjugates |
| KR102061743B1 (ko) | 2011-03-04 | 2020-01-03 | 뉴젠 세러퓨틱스 인코포레이티드 | 알킨 치환된 퀴나졸린 화합물 및 그것의 사용 방법 |
| CN102918029B (zh) | 2011-05-17 | 2015-06-17 | 江苏康缘药业股份有限公司 | 4-苯胺-6-丁烯酰胺-7-烷醚喹唑啉衍生物及其制备方法和用途 |
| IN2014DN07898A (ja) | 2012-02-21 | 2015-04-24 | Ranbaxy Lab Ltd | |
| US8461179B1 (en) | 2012-06-07 | 2013-06-11 | Deciphera Pharmaceuticals, Llc | Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| CN104736144B (zh) | 2012-07-27 | 2019-02-01 | 艾祖米科技有限公司 | 外排抑制剂组合物和使用此组合物治疗的方法 |
| EP3027026A4 (en) | 2013-07-31 | 2017-05-03 | Windward Pharma, Inc. | Aerosol tyrosine kinase inhibitor compounds and uses thereof |
| US11285152B2 (en) | 2017-07-20 | 2022-03-29 | Kashiv Biosciences, Llc | Stable oral pharmaceutical composition of imatinib |
| SG11202007287XA (en) | 2018-01-31 | 2020-08-28 | Deciphera Pharmaceuticals Llc | Combination therapy for the treatment of mastocytosis |
| KR20240140193A (ko) | 2018-01-31 | 2024-09-24 | 데시페라 파마슈티칼스, 엘엘씨. | 위장관 기질 종양의 치료를 위한 병용 요법 |
| EP4007585A4 (en) | 2019-08-02 | 2023-11-08 | OneHealthCompany, Inc. | TREATMENT OF CANCER IN DOGS |
| TW202122082A (zh) | 2019-08-12 | 2021-06-16 | 美商迪賽孚爾製藥有限公司 | 治療胃腸道基質瘤方法 |
| CA3150433A1 (en) | 2019-08-12 | 2021-02-18 | Deciphera Pharmaceuticals, Llc | Ripretinib for treating gastrointestinal stromal tumors |
| KR20220123058A (ko) | 2019-12-30 | 2022-09-05 | 데시페라 파마슈티칼스, 엘엘씨. | 1-(4-브로모-5-(1-에틸-7-(메틸아미노)-2-옥소-1,2-디히드로-1,6-나프티리딘-3-일)-2-플루오로페닐)-3-페닐우레아의 조성물 |
| AU2020419197B2 (en) | 2019-12-30 | 2023-08-31 | Deciphera Pharmaceuticals, Llc | Amorphous kinase inhibitor formulations and methods of use thereof |
| KR102535840B1 (ko) | 2020-07-31 | 2023-05-23 | (주)파로스아이바이오 | 2,3,5-치환된 싸이오펜 화합물의 위장관기질종양 예방, 개선 또는 치료 용도 |
| US11779572B1 (en) | 2022-09-02 | 2023-10-10 | Deciphera Pharmaceuticals, Llc | Methods of treating gastrointestinal stromal tumors |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW225528B (ja) * | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| CO4940418A1 (es) * | 1997-07-18 | 2000-07-24 | Novartis Ag | Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso |
| WO2000012084A1 (en) * | 1998-08-31 | 2000-03-09 | Sugen, Inc. | Geometrically restricted 2-indolinone derivatives as modulators of protein kinase activity |
-
2001
- 2001-10-26 SK SK518-2003A patent/SK287335B6/sk not_active IP Right Cessation
- 2001-10-26 RU RU2003114752/15A patent/RU2301066C2/ru not_active IP Right Cessation
- 2001-10-26 PL PL362148A patent/PL209733B1/pl unknown
- 2001-10-26 ES ES01988712T patent/ES2260317T3/es not_active Expired - Lifetime
- 2001-10-26 CA CA002424470A patent/CA2424470C/en not_active Expired - Lifetime
- 2001-10-26 PT PT01988712T patent/PT1332137E/pt unknown
- 2001-10-26 JP JP2002537718A patent/JP4386635B2/ja not_active Expired - Lifetime
- 2001-10-26 AU AU1826202A patent/AU1826202A/xx active Pending
- 2001-10-26 EP EP01988712A patent/EP1332137B1/en not_active Expired - Lifetime
- 2001-10-26 AU AU2002218262A patent/AU2002218262B2/en not_active Expired
- 2001-10-26 CZ CZ20031152A patent/CZ303944B6/cs not_active IP Right Cessation
- 2001-10-26 IL IL15502901A patent/IL155029A0/xx unknown
- 2001-10-26 DE DE60118430T patent/DE60118430T2/de not_active Expired - Lifetime
- 2001-10-26 MX MXPA03003703A patent/MXPA03003703A/es active IP Right Grant
- 2001-10-26 KR KR1020037003903A patent/KR100885129B1/ko active IP Right Review Request
- 2001-10-26 WO PCT/EP2001/012442 patent/WO2002034727A2/en active IP Right Grant
- 2001-10-26 BR BR0114870-2 patent/BRPI0114870B8/pt active IP Right Grant
- 2001-10-26 DK DK01988712T patent/DK1332137T3/da active
- 2001-10-26 AT AT01988712T patent/ATE321556T1/de active
- 2001-10-26 HU HU0301512A patent/HU229106B1/hu unknown
- 2001-10-26 CN CNB018178952A patent/CN1276754C/zh not_active Ceased
- 2001-10-26 US US10/415,015 patent/US6958335B2/en not_active Expired - Lifetime
- 2001-10-26 NZ NZ525254A patent/NZ525254A/en not_active IP Right Cessation
-
2003
- 2003-03-18 ZA ZA200302155A patent/ZA200302155B/en unknown
- 2003-03-20 IL IL155029A patent/IL155029A/en active IP Right Grant
- 2003-04-24 NO NO20031833A patent/NO324948B1/no not_active IP Right Cessation
- 2003-12-29 HK HK03109439A patent/HK1058193A1/xx not_active IP Right Cessation
-
2006
- 2006-06-21 CY CY20061100839T patent/CY1105055T1/el unknown
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