JP2004525173A5 - - Google Patents
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- Publication number
- JP2004525173A5 JP2004525173A5 JP2002579433A JP2002579433A JP2004525173A5 JP 2004525173 A5 JP2004525173 A5 JP 2004525173A5 JP 2002579433 A JP2002579433 A JP 2002579433A JP 2002579433 A JP2002579433 A JP 2002579433A JP 2004525173 A5 JP2004525173 A5 JP 2004525173A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- carbonyl
- amino
- phenyl
- 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.)
- Ceased
Links
- -1 C 1 -3 -Alkoxy Chemical group 0.000 claims description 28
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 24
- 125000000217 alkyl group Chemical group 0.000 claims description 21
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 16
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 15
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 15
- 229910052757 nitrogen Inorganic materials 0.000 claims description 11
- 150000003839 salts Chemical class 0.000 claims description 11
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 8
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims description 7
- 125000003545 alkoxy group Chemical group 0.000 claims description 7
- 125000004432 carbon atom Chemical group C* 0.000 claims description 7
- 125000001841 imino group Chemical group [H]N=* 0.000 claims description 7
- 229910052760 oxygen Inorganic materials 0.000 claims description 7
- 239000001301 oxygen Substances 0.000 claims description 7
- 229910052717 sulfur Inorganic materials 0.000 claims description 7
- 125000004434 sulfur atom Chemical group 0.000 claims description 7
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical compound BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 6
- KZBUYRJDOAKODT-UHFFFAOYSA-N Chlorine Chemical compound ClCl KZBUYRJDOAKODT-UHFFFAOYSA-N 0.000 claims description 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 4
- 239000000460 chlorine Substances 0.000 claims description 4
- 229910052801 chlorine Inorganic materials 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 229910052731 fluorine Inorganic materials 0.000 claims description 4
- 239000011737 fluorine Substances 0.000 claims description 4
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 125000003386 piperidinyl group Chemical group 0.000 claims description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 4
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical group [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims description 3
- 229910052794 bromium Inorganic materials 0.000 claims description 3
- 229910052740 iodine Inorganic materials 0.000 claims description 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 2
- 125000006164 6-membered heteroaryl group Chemical group 0.000 claims description 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 150000001721 carbon Chemical group 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims description 2
- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 16
- 125000006698 (C1-C3) dialkylamino group Chemical group 0.000 claims 12
- 125000006563 (C1-3) alkylaminocarbonyl group Chemical group 0.000 claims 9
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 8
- 125000006576 di-(C1-C3-alkyl)-aminocarbonyl group Chemical group 0.000 claims 7
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 7
- JYGFTBXVXVMTGB-UHFFFAOYSA-N indolin-2-one Chemical group C1=CC=C2NC(=O)CC2=C1 JYGFTBXVXVMTGB-UHFFFAOYSA-N 0.000 claims 5
- 150000001875 compounds Chemical class 0.000 claims 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims 4
- 125000006413 ring segment Chemical group 0.000 claims 4
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000004193 piperazinyl group Chemical group 0.000 claims 3
- 125000006603 (C1-C3) alkylaminosulfonyl group Chemical group 0.000 claims 2
- 125000006602 (C1-C3) alkylsulfonylamino group Chemical group 0.000 claims 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 2
- 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 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 2
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 2
- 239000000969 carrier Substances 0.000 claims 2
- 125000002993 cycloalkylene group Chemical group 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- 125000003006 2-dimethylaminoethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- 239000005973 Carvone Substances 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 0 *C(N(*)*)=C1c(ccc(*)c2)c2N(*=I)C1=* Chemical compound *C(N(*)*)=C1c(ccc(*)c2)c2N(*=I)C1=* 0.000 description 1
- 125000003282 alkyl amino group Chemical group 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10117204A DE10117204A1 (de) | 2001-04-06 | 2001-04-06 | In 6-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| PCT/EP2002/003583 WO2002081445A1 (de) | 2001-04-06 | 2002-03-30 | In 6-stellung substituierte indoline und ihre verwendung als kinase-inhibitoren |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004525173A JP2004525173A (ja) | 2004-08-19 |
| JP2004525173A5 true JP2004525173A5 (enExample) | 2009-02-26 |
Family
ID=7680648
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002579433A Ceased JP2004525173A (ja) | 2001-04-06 | 2002-03-30 | ６位で置換されたインドリノン、それらのキナーゼインヒビターとしての使用 |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US6858641B2 (enExample) |
| EP (1) | EP1379501A1 (enExample) |
| JP (1) | JP2004525173A (enExample) |
| KR (1) | KR20030090712A (enExample) |
| CN (1) | CN1509270A (enExample) |
| AR (1) | AR035813A1 (enExample) |
| BG (1) | BG108220A (enExample) |
| BR (1) | BR0208900A (enExample) |
| CA (1) | CA2442695A1 (enExample) |
| CZ (1) | CZ20032975A3 (enExample) |
| DE (1) | DE10117204A1 (enExample) |
| EA (1) | EA200301005A1 (enExample) |
| EC (1) | ECSP034776A (enExample) |
| EE (1) | EE200300491A (enExample) |
| HU (1) | HUP0303737A3 (enExample) |
| IL (1) | IL158254A0 (enExample) |
| MX (1) | MXPA03008896A (enExample) |
| NO (1) | NO20034434L (enExample) |
| PE (1) | PE20021058A1 (enExample) |
| PL (1) | PL366458A1 (enExample) |
| SK (1) | SK12412003A3 (enExample) |
| WO (1) | WO2002081445A1 (enExample) |
| ZA (1) | ZA200307306B (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10233500A1 (de) * | 2002-07-24 | 2004-02-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 3-Z-[1-(4-(N-((4-Methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylen]-6-methoxycarbonyl-2-indolinon-Monoethansulfonat und dessen Verwendung als Arzneimittel |
| US7148249B2 (en) * | 2002-09-12 | 2006-12-12 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Indolinones substituted by heterocycles, the preparation thereof and their use as medicaments |
| JP4879492B2 (ja) * | 2002-11-27 | 2012-02-22 | アラーガン、インコーポレイテッド | 疾患の治療のためのキナーゼ阻害剤 |
| US20060154939A1 (en) * | 2004-12-24 | 2006-07-13 | Boehringer Ingelheim International Gmbh | Medicaments for the Treatment or Prevention of Fibrotic Diseases |
| PE20060777A1 (es) | 2004-12-24 | 2006-10-06 | Boehringer Ingelheim Int | Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas |
| PE20061155A1 (es) * | 2004-12-24 | 2006-12-16 | Boehringer Ingelheim Int | Derivados de indolinona como agentes para el tratamiento o la prevencion de enfermedades fibroticas |
| WO2007057397A1 (en) * | 2005-11-15 | 2007-05-24 | Boehringer Ingelheim International Gmbh | Treatment of cancer |
| CN101889004B (zh) | 2007-10-12 | 2014-09-10 | 阿斯利康公司 | 蛋白激酶抑制剂 |
| PE20091445A1 (es) * | 2007-12-03 | 2009-10-19 | Boehringer Ingelheim Int | Derivados de indolinona y procedimiento para su fabricacion |
| US20170065529A1 (en) | 2015-09-09 | 2017-03-09 | Boehringer Ingelheim International Gmbh | Pharmaceutical dosage form for immediate release of an indolinone derivative |
| EP2303841A1 (en) * | 2008-07-14 | 2011-04-06 | Gilead Sciences, Inc. | Oxindolyl inhibitor compounds |
| EA201100254A1 (ru) * | 2008-07-29 | 2011-08-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Новые соединения |
| KR20130016244A (ko) | 2010-03-10 | 2013-02-14 | 인게니움 파르마코이티칼스 게엠베하 | 단백질 키나아제의 억제제 |
| CN102267934B (zh) * | 2010-06-02 | 2013-04-17 | 金凯美(大连)医药科技有限公司 | 一种6-甲氧羰基吲哚酮的制备方法 |
| KR20180128390A (ko) | 2015-12-24 | 2018-12-03 | 레스피버트 리미티드 | 인돌리논 화합물과 섬유성 질환의 치료에서 이의 용도 |
| WO2017153748A1 (en) * | 2016-03-08 | 2017-09-14 | Respivert Limited | Indole derivatives and their use as protein kinase inhibitors |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998007695A1 (en) * | 1996-08-23 | 1998-02-26 | Sugen, Inc. | Indolinone combinatorial libraries and related products and methods for the treatment of disease |
| GB9718913D0 (en) * | 1997-09-05 | 1997-11-12 | Glaxo Group Ltd | Substituted oxindole derivatives |
| US6043254A (en) * | 1998-04-03 | 2000-03-28 | Boehringer Ingelheim Pharma Kg | Indolinones having kinase-inhibiting activity |
| US6169106B1 (en) * | 1998-04-15 | 2001-01-02 | Boehringer Ingelheim Pharma Kg | Indolinones having kinase inhibitory activity |
| DE19816624A1 (de) | 1998-04-15 | 1999-10-21 | Boehringer Ingelheim Pharma | Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| US6319918B1 (en) * | 1998-06-04 | 2001-11-20 | Boehringer Ingelheim Pharma Kg | Substituted indolinones with kinase inhibitory activity |
| DE19824922A1 (de) * | 1998-06-04 | 1999-12-09 | Boehringer Ingelheim Pharma | Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| DE19924401A1 (de) | 1999-05-27 | 2000-11-30 | Boehringer Ingelheim Pharma | Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| DE19940829A1 (de) | 1999-08-27 | 2001-03-01 | Boehringer Ingelheim Pharma | Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| CA2381821A1 (en) | 1999-08-27 | 2001-03-08 | Boehringer Ingelheim Pharma Kg | Substituted indolinones, their manufacture and their use as medicaments |
| DE10042696A1 (de) | 2000-08-31 | 2002-03-14 | Boehringer Ingelheim Pharma | In 6-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| UA75054C2 (uk) | 1999-10-13 | 2006-03-15 | Бьорінгер Інгельхайм Фарма Гмбх & Ко. Кг | Заміщені в положенні 6 індолінони, їх одержання та їх застосування як лікарського засобу |
-
2001
- 2001-04-06 DE DE10117204A patent/DE10117204A1/de not_active Withdrawn
-
2002
- 2002-03-30 WO PCT/EP2002/003583 patent/WO2002081445A1/de not_active Ceased
- 2002-03-30 SK SK1241-2003A patent/SK12412003A3/sk unknown
- 2002-03-30 CN CNA028099184A patent/CN1509270A/zh active Pending
- 2002-03-30 EA EA200301005A patent/EA200301005A1/ru unknown
- 2002-03-30 KR KR10-2003-7013027A patent/KR20030090712A/ko not_active Withdrawn
- 2002-03-30 HU HU0303737A patent/HUP0303737A3/hu unknown
- 2002-03-30 EE EEP200300491A patent/EE200300491A/xx unknown
- 2002-03-30 EP EP02735201A patent/EP1379501A1/de not_active Withdrawn
- 2002-03-30 CZ CZ20032975A patent/CZ20032975A3/cs unknown
- 2002-03-30 BR BR0208900-9A patent/BR0208900A/pt not_active Application Discontinuation
- 2002-03-30 IL IL15825402A patent/IL158254A0/xx unknown
- 2002-03-30 JP JP2002579433A patent/JP2004525173A/ja not_active Ceased
- 2002-03-30 MX MXPA03008896A patent/MXPA03008896A/es unknown
- 2002-03-30 PL PL02366458A patent/PL366458A1/xx not_active Application Discontinuation
- 2002-03-30 CA CA002442695A patent/CA2442695A1/en not_active Abandoned
- 2002-04-04 US US10/116,365 patent/US6858641B2/en not_active Expired - Lifetime
- 2002-04-05 AR ARP020101257A patent/AR035813A1/es not_active Application Discontinuation
- 2002-04-05 PE PE2002000279A patent/PE20021058A1/es not_active Application Discontinuation
-
2003
- 2003-09-18 ZA ZA200307306A patent/ZA200307306B/xx unknown
- 2003-09-24 EC EC2003004776A patent/ECSP034776A/es unknown
- 2003-10-01 BG BG108220A patent/BG108220A/bg unknown
- 2003-10-03 NO NO20034434A patent/NO20034434L/no not_active Application Discontinuation
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