JP2005506982A5 - - Google Patents
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- Publication number
- JP2005506982A5 JP2005506982A5 JP2003526891A JP2003526891A JP2005506982A5 JP 2005506982 A5 JP2005506982 A5 JP 2005506982A5 JP 2003526891 A JP2003526891 A JP 2003526891A JP 2003526891 A JP2003526891 A JP 2003526891A JP 2005506982 A5 JP2005506982 A5 JP 2005506982A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- hydrogen
- piperazin
- hydroxyalkyl
- 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.)
- Withdrawn
Links
- -1 methylene, ethylene, carbonyl Chemical group 0.000 claims 33
- 150000001875 compounds Chemical class 0.000 claims 22
- 125000000217 alkyl group Chemical group 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 229910052757 nitrogen Inorganic materials 0.000 claims 9
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 9
- 125000004476 heterocycloamino group Chemical group 0.000 claims 5
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 4
- 102000001253 Protein Kinase Human genes 0.000 claims 4
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 4
- 108060006633 protein kinase Proteins 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- WRJZKSHNBALIGH-UHFFFAOYSA-N 2-piperazin-1-ium-1-ylacetate Chemical compound OC(=O)CN1CCNCC1 WRJZKSHNBALIGH-UHFFFAOYSA-N 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 3
- 125000005078 alkoxycarbonylalkyl group Chemical group 0.000 claims 3
- 125000004181 carboxyalkyl group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000005182 hydroxyalkylcarbonyl group Chemical group 0.000 claims 3
- 102000009076 src-Family Kinases Human genes 0.000 claims 3
- 108010087686 src-Family Kinases Proteins 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical group C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 239000005977 Ethylene Substances 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000003197 catalytic effect Effects 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31850801P | 2001-09-10 | 2001-09-10 | |
| PCT/US2002/025974 WO2003022815A1 (en) | 2001-09-10 | 2002-09-10 | 3-(4,5,6,7-tetrahydroindol-2-ylmethylidiene)-2-indolinone derivatives as kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005506982A JP2005506982A (ja) | 2005-03-10 |
| JP2005506982A5 true JP2005506982A5 (enExample) | 2006-01-05 |
Family
ID=23238468
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003526891A Withdrawn JP2005506982A (ja) | 2001-09-10 | 2002-09-10 | キナーゼ阻害剤としての３−（４，５，６，７−テトラヒドロインドール−２−イルメチリデン）−２−インドリノン誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US6777417B2 (enExample) |
| EP (1) | EP1436259A1 (enExample) |
| JP (1) | JP2005506982A (enExample) |
| BR (1) | BR0212435A (enExample) |
| CA (1) | CA2459879A1 (enExample) |
| MX (1) | MXPA04002242A (enExample) |
| WO (1) | WO2003022815A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE0101230L (sv) * | 2001-04-06 | 2002-10-07 | Innoventus Project Ab | Ny användning av en tyrosinkinasinhibitor |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| US20040266843A1 (en) * | 2003-03-07 | 2004-12-30 | Sugen, Inc. | Sulfonamide substituted indolinones as inhibitors of DNA dependent protein kinase (DNA-PK) |
| US7157577B2 (en) * | 2003-03-07 | 2007-01-02 | Sugen Inc. | 5-sulfonamido-substituted indolinone compounds as protein kinase inhibitors |
| US20050043233A1 (en) * | 2003-04-29 | 2005-02-24 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis |
| KR20120062863A (ko) * | 2003-07-30 | 2012-06-14 | 리겔 파마슈티칼스, 인크. | 자가면역 질환의 치료 또는 예방에 사용하기 위한 2,4-피리미딘디아민 화합물 |
| EP1680401A2 (en) | 2003-10-24 | 2006-07-19 | Schering Aktiengesellschaft | Indolinone derivatives and their use in treating disease-states such as cancer |
| ES2651349T3 (es) | 2005-06-08 | 2018-01-25 | Rigel Pharmaceuticals, Inc. | Composiciones y métodos para la inhibición de la ruta JAK |
| US20070203161A1 (en) * | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| ES2622493T3 (es) * | 2006-02-24 | 2017-07-06 | Rigel Pharmaceuticals, Inc. | Composiciones y métodos para la inhibición de la ruta de JAK |
| WO2008138184A1 (fr) * | 2007-05-14 | 2008-11-20 | Shanghai Hengrui Pharmaceutical Co.Ltd. | Dérivés de pyrrolo-azacycles, leur procédé de fabrication et leur utilisation en tant qu'inhibiteurs de protéine kinases |
| JP5711537B2 (ja) | 2008-02-15 | 2015-05-07 | ライジェル ファーマシューティカルズ， インコーポレイテッド | ピリミジン−２−アミン化合物およびｊａｋキナーゼの阻害剤としてのその使用 |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| AU2009244897B2 (en) | 2008-04-16 | 2014-11-13 | Alexion Pharmaceuticals, Inc. | 2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors |
| BRPI0910668A2 (pt) * | 2008-04-22 | 2019-09-24 | Portola Pharmaceutiacals Inc | inibidores de proteína quinases |
| US7897602B2 (en) * | 2009-01-12 | 2011-03-01 | Development Center For Biotechnology | Indolinone compounds as kinase inhibitors |
| EP2459195A1 (en) * | 2009-07-28 | 2012-06-06 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| CN103328471A (zh) * | 2010-10-13 | 2013-09-25 | 武田加利福尼亚股份有限公司 | 制备氮杂吲唑衍生物的方法 |
| US9102625B2 (en) | 2010-11-01 | 2015-08-11 | Portola Pharmaceuticals, Inc. | Nicotinamides as JAK kinase modulators |
| SG10201601352UA (en) | 2011-11-23 | 2016-03-30 | Portola Pharm Inc | Pyrazine kinase inhibitors |
| JP2015524400A (ja) | 2012-07-19 | 2015-08-24 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ９−［４−（３−クロロ−２−フルオロ−フェニルアミノ）−７−メトキシ−キナゾリン−６−イルオキシ］−１，４−ジアザ−スピロ［５．５］ウンデカン−５−オンのフマル酸塩、その薬物としての使用及び調製 |
| WO2014058921A2 (en) | 2012-10-08 | 2014-04-17 | Portola Pharmaceuticals, Inc. | Substituted pyrimidinyl kinase inhibitors |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5466823A (en) * | 1993-11-30 | 1995-11-14 | G.D. Searle & Co. | Substituted pyrazolyl benzenesulfonamides |
| US5633272A (en) * | 1995-02-13 | 1997-05-27 | Talley; John J. | Substituted isoxazoles for the treatment of inflammation |
| US6147106A (en) * | 1997-08-20 | 2000-11-14 | Sugen, Inc. | Indolinone combinatorial libraries and related products and methods for the treatment of disease |
| US5968974A (en) * | 1995-07-19 | 1999-10-19 | Merck & Co., Inc. | Method of treating colonic adenomas |
| JP3382624B2 (ja) * | 1996-04-12 | 2003-03-04 | ジー．ディー．サール アンド カンパニー | Ｃｏｘ―２阻害剤のプロドラッグとしての置換ベンゼンスルホンアミド誘導体 |
| ATE292623T1 (de) | 1997-05-07 | 2005-04-15 | Sugen Inc | 2-indolinonderivate als modulatoren der proteinkinase-ativität |
| US6114371A (en) * | 1997-06-20 | 2000-09-05 | Sugen, Inc. | 3-(cyclohexanoheteroarylidenyl)-2-indolinone protein tyrosine kinase inhibitors |
| US6130238A (en) * | 1997-06-20 | 2000-10-10 | Sugen, Inc. | 3-(cyclohexanoheteroarylidenyl)-2-indolinone protein tyrosine kinase inhibitors |
| CO4960662A1 (es) | 1997-08-28 | 2000-09-25 | Novartis Ag | Ciertos acidos 5-alquil-2-arilaminofenilaceticos y sus derivados |
| AU5468499A (en) * | 1998-08-04 | 2000-02-28 | Sugen, Inc. | 3-methylidenyl-2-indolinone modulators of protein kinase |
| DK1255752T3 (da) * | 2000-02-15 | 2007-11-26 | Sugen Inc | Pyrrolsubstituerede 2-indolinonproteinkinaseinhibitorer |
-
2002
- 2002-09-10 US US10/238,051 patent/US6777417B2/en not_active Expired - Fee Related
- 2002-09-10 MX MXPA04002242A patent/MXPA04002242A/es unknown
- 2002-09-10 CA CA002459879A patent/CA2459879A1/en not_active Abandoned
- 2002-09-10 JP JP2003526891A patent/JP2005506982A/ja not_active Withdrawn
- 2002-09-10 WO PCT/US2002/025974 patent/WO2003022815A1/en not_active Ceased
- 2002-09-10 EP EP02780264A patent/EP1436259A1/en not_active Withdrawn
- 2002-09-10 BR BR0212435-1A patent/BR0212435A/pt not_active IP Right Cessation
-
2004
- 2004-07-13 US US10/889,050 patent/US20040266855A1/en not_active Abandoned
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