JP2002532503A5 - - Google Patents
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- Publication number
- JP2002532503A5 JP2002532503A5 JP2000588180A JP2000588180A JP2002532503A5 JP 2002532503 A5 JP2002532503 A5 JP 2002532503A5 JP 2000588180 A JP2000588180 A JP 2000588180A JP 2000588180 A JP2000588180 A JP 2000588180A JP 2002532503 A5 JP2002532503 A5 JP 2002532503A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- lower alkyl
- heteroaryl
- aryl
- cycloalkyl
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 description 52
- 125000003118 aryl group Chemical group 0.000 description 49
- 125000001072 heteroaryl group Chemical group 0.000 description 49
- 125000000623 heterocyclic group Chemical group 0.000 description 41
- 125000000753 cycloalkyl group Chemical group 0.000 description 40
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 description 23
- 150000001875 compounds Chemical class 0.000 description 16
- 229910052739 hydrogen Inorganic materials 0.000 description 10
- 239000001257 hydrogen Substances 0.000 description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 9
- -1 wherein -R 11 Chemical group 0.000 description 7
- 229910052736 halogen Inorganic materials 0.000 description 6
- 150000002367 halogens Chemical class 0.000 description 6
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 description 6
- IBVRNLCFTHSDEM-UHFFFAOYSA-N 6h-quinoxalin-5-one Chemical compound C1=CN=C2C(=O)CC=CC2=N1 IBVRNLCFTHSDEM-UHFFFAOYSA-N 0.000 description 5
- 125000005010 perfluoroalkyl group Chemical group 0.000 description 5
- 125000004093 cyano group Chemical group *C#N 0.000 description 4
- 206010028980 Neoplasm Diseases 0.000 description 3
- 125000004429 atom Chemical group 0.000 description 3
- 210000000481 breast Anatomy 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 125000005842 heteroatom Chemical group 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 230000004770 neurodegeneration Effects 0.000 description 2
- 208000015122 neurodegenerative disease Diseases 0.000 description 2
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 description 2
- 239000008194 pharmaceutical composition Substances 0.000 description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- CEIDHALHGCCINZ-SEYXRHQNSA-N (9z)-2,3-bis(furan-2-yl)-9-[(3-methoxy-1h-pyrrol-2-yl)methylidene]-7h-pyrrolo[3,2-f]quinoxalin-8-one Chemical compound C1=CNC(\C=C/2C3=C4N=C(C(C=5OC=CC=5)=NC4=CC=C3NC\2=O)C=2OC=CC=2)=C1OC CEIDHALHGCCINZ-SEYXRHQNSA-N 0.000 description 1
- 0 *C1=C(C=C([C@@]2C(N3)=CC=C4C(*)=C(*)C(*)=NC24)C3=O)N=C*1 Chemical compound *C1=C(C=C([C@@]2C(N3)=CC=C4C(*)=C(*)C(*)=NC24)C3=O)N=C*1 0.000 description 1
- LFMSWSZYGKVOMM-UHFFFAOYSA-N 1h-phenazin-2-one Chemical compound C1=CC=C2N=C(C=CC(=O)C3)C3=NC2=C1 LFMSWSZYGKVOMM-UHFFFAOYSA-N 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 210000001072 colon Anatomy 0.000 description 1
- 208000029742 colonic neoplasm Diseases 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 150000002431 hydrogen Chemical class 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 125000000547 substituted alkyl group Chemical group 0.000 description 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11265398P | 1998-12-17 | 1998-12-17 | |
| US60/112,653 | 1998-12-17 | ||
| PCT/EP1999/009806 WO2000035921A1 (en) | 1998-12-17 | 1999-12-11 | 4,5-pyrazinoxindoles as protein kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2002532503A JP2002532503A (ja) | 2002-10-02 |
| JP2002532503A5 true JP2002532503A5 (https=) | 2007-01-25 |
Family
ID=22345140
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000588180A Pending JP2002532503A (ja) | 1998-12-17 | 1999-12-11 | プロテインキナーゼ阻害剤としての４，５−ピラジノオキシンドール |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US6221867B1 (https=) |
| EP (1) | EP1149105B1 (https=) |
| JP (1) | JP2002532503A (https=) |
| KR (1) | KR20010108024A (https=) |
| CN (1) | CN1158283C (https=) |
| AR (1) | AR021695A1 (https=) |
| AT (1) | ATE387448T1 (https=) |
| AU (1) | AU767138B2 (https=) |
| BR (1) | BR9916324A (https=) |
| CA (1) | CA2354402A1 (https=) |
| DE (1) | DE69938258T2 (https=) |
| ES (1) | ES2301255T3 (https=) |
| PE (1) | PE20001385A1 (https=) |
| TR (1) | TR200101756T2 (https=) |
| UY (1) | UY25854A1 (https=) |
| WO (1) | WO2000035921A1 (https=) |
| ZA (1) | ZA200104505B (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0016454D0 (en) | 2000-07-04 | 2000-08-23 | Hoffmann La Roche | Thienopyrrolidinones |
| GB0108770D0 (en) | 2001-04-06 | 2001-05-30 | Eisai London Res Lab Ltd | Inhibitors |
| CN1300116C (zh) | 2001-04-16 | 2007-02-14 | 卫材株式会社 | 1h－吲唑化合物 |
| US7018999B2 (en) | 2001-05-16 | 2006-03-28 | Cephalon, Inc. | Methods for the treatment and prevention of pain |
| JP4414219B2 (ja) | 2001-07-23 | 2010-02-10 | メルク セローノ ソシエテ アノニム | Ｃ−ｊｕｎ−ｎ−末端キナーゼ（ｊｎｋ）インヒビターとしてのアリールスルホンアミド誘導体 |
| ATE465153T1 (de) | 2002-02-28 | 2010-05-15 | Eisai R&D Man Co Ltd | Neue indazolverbindungen mit kondensiertem ring |
| DE60316542T2 (de) | 2002-03-28 | 2008-07-03 | Eisai R&D Management Co., Ltd. | 7-azaindole als inhibitoren c-jun n-terminaler kinasen zur behandlung neurodegenerativer störungen |
| WO2003082869A1 (en) | 2002-03-28 | 2003-10-09 | Eisai Co., Ltd. | Azaindoles as inhibitors of c-jun n-terminal kinases |
| CA2486183C (en) * | 2002-05-23 | 2012-01-10 | Cytopia Pty Ltd. | Protein kinase inhibitors |
| US7429609B2 (en) | 2002-05-31 | 2008-09-30 | Eisai R & D Management Co., Ltd. | Pyrazole compound and medicinal composition containing the same |
| WO2003106455A1 (en) | 2002-06-14 | 2003-12-24 | Applied Research Systems Ars Holding N.V. | Azole methylidene cyanide derivatives and their use as protein kinase modulators |
| GB0305142D0 (en) | 2003-03-06 | 2003-04-09 | Eisai London Res Lab Ltd | Synthesis |
| BRPI0410071A (pt) * | 2003-05-08 | 2006-05-23 | Wyeth Corp | métodos para usar no diagnóstico e prognóstico da artrite em um paciente, para usar no monitoramento do curso da artrite em um paciente, para avaliar a eficácia de um tratamento para artrite em um paciente, para triar um composto capaz de inibir a artrite em um paciente e para tratar artrite em um paciente, e, molécula de sirna |
| US7612086B2 (en) | 2003-05-16 | 2009-11-03 | Eisai R & D Management Co. Ltd. | JNK inhibitors |
| RU2006117635A (ru) | 2003-10-24 | 2007-12-10 | Шеринг Акциенгезельшафт (De) | Производные индолинона и их применение для лечения патологических состояний, таких как злокачественное новообразование |
| US20060094753A1 (en) | 2004-10-29 | 2006-05-04 | Alcon, Inc. | Use of inhibitors of Jun N-terminal kinases for the treatment of glaucomatous retinopathy and ocular diseases |
| GB0516156D0 (en) | 2005-08-05 | 2005-09-14 | Eisai London Res Lab Ltd | JNK inhibitors |
| US7968572B2 (en) | 2005-10-03 | 2011-06-28 | Ono Pharmaceuticals Co., Ltd. | Nitrogen-containing heterocyclic compound and pharmaceutical application thereof |
| CA2633980A1 (en) | 2005-12-29 | 2007-07-12 | Anthrogenesis Corporation | Improved composition for collecting and preserving placental stem cells and methods of using the composition |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4556672A (en) | 1984-03-19 | 1985-12-03 | Pfizer Inc. | 3-Substituted 2-oxindole-1-carboxamides as analgesic and anti-inflammatory agents |
| DE3531678A1 (de) | 1985-09-05 | 1987-03-12 | Boehringer Mannheim Gmbh | Neue pyrrolo-benzimidazole, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
| KR930011300B1 (ko) | 1989-07-25 | 1993-11-29 | 다이호오 야꾸힌 고오교오 가부시끼가이샤 | 옥시인돌유도체 |
| WO1991009598A1 (en) | 1990-01-05 | 1991-07-11 | Pfizer Inc. | Azaoxindole derivatives |
| GB9004483D0 (en) | 1990-02-28 | 1990-04-25 | Erba Carlo Spa | New aryl-and heteroarylethenylene derivatives and process for their preparation |
| WO1992007830A2 (en) | 1990-10-29 | 1992-05-14 | Pfizer Inc. | Oxindole peptide antagonists |
| GB9115160D0 (en) | 1991-07-12 | 1991-08-28 | Erba Carlo Spa | Methylen-oxindole derivatives and process for their preparation |
| US5322950A (en) | 1991-12-05 | 1994-06-21 | Warner-Lambert Company | Imidazole with angiotensin II antagonist properties |
| FR2694004B1 (fr) | 1992-07-21 | 1994-08-26 | Adir | Nouvelles 3-(Hydroxybenzylidényl)-indoline-2-ones et 3-(hydroxybenzylidényl)-indoline-2-thiones, leurs procédés de préparation, et les compositions pharmaceutiques qui les contiennent. |
| GB9226855D0 (en) | 1992-12-23 | 1993-02-17 | Erba Carlo Spa | Vinylene-azaindole derivatives and process for their preparation |
| GB9313638D0 (en) | 1993-07-01 | 1993-08-18 | Erba Carlo Spa | Arylidene and heteroarylidene oxindole derivatives and process for their preparation |
| GB9326136D0 (en) | 1993-12-22 | 1994-02-23 | Erba Carlo Spa | Biologically active 3-substituted oxindole derivatives useful as anti-angiogenic agents |
| GB9412719D0 (en) | 1994-06-24 | 1994-08-17 | Erba Carlo Spa | Substituted azaindolylidene compounds and process for their preparation |
| GB9423997D0 (en) | 1994-11-28 | 1995-01-11 | Erba Carlo Spa | Substituted 3-arylidene-7-azaoxindole compounds and process for their preparation |
| GB9501567D0 (en) | 1995-01-26 | 1995-03-15 | Pharmacia Spa | Hydrosoluble 3-arylidene-2-oxindole derivatives as tyrosine kinase inhibitors |
| GB9507298D0 (en) * | 1995-04-07 | 1995-05-31 | Pharmacia Spa | Substituted indolylmethylene-oxindale analogues as tyrosine kinase inhibitors |
| US5880141A (en) | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
| AU709191B2 (en) | 1995-09-11 | 1999-08-26 | Osteoarthritis Sciences, Inc. | Protein tyrosine kinase inhibitors for treating osteoarthritis |
| US5733920A (en) | 1995-10-31 | 1998-03-31 | Mitotix, Inc. | Inhibitors of cyclin dependent kinases |
| PL187516B1 (pl) | 1996-01-11 | 2004-07-30 | Smithkline Beecham Corp | Nowe podstawione pochodne imidazolu, sposób ich wytwarzania oraz kompozycja farmaceutyczna zawierająca te związki |
| WO1997025986A1 (en) * | 1996-01-17 | 1997-07-24 | Taiho Pharmaceutical Co., Ltd. | Intimal thickening inhibitors |
| DE69718968T2 (de) | 1996-01-17 | 2003-10-09 | Taiho Pharmaceutical Co. Ltd., Tokio/Tokyo | 3-(bis-substituierte-phenylmethylen)oxindol-derivate |
| GB9610964D0 (en) | 1996-05-24 | 1996-07-31 | Pharmacia & Upjohn Spa | Substituted tetralylmethylen-oxindole analogues as tyrosine kinase inhibitors |
| GB9611797D0 (en) | 1996-06-06 | 1996-08-07 | Pharmacia Spa | Substituted quinolylmethylen-oxindole analogues as tyrosine kinase inhibitors |
| DE69734521T9 (de) * | 1996-08-23 | 2006-12-07 | Sugen, Inc., South San Francisco | Kombinatorische indolinonbibliotheken und verwandte produkte und verfahren zur behandlung von erkrankungen |
| WO1998024432A2 (en) | 1996-12-05 | 1998-06-11 | Sugen, Inc. | Use of indolinone compounds as modulators of protein kinases |
| JP2002511852A (ja) | 1997-05-07 | 2002-04-16 | スージェン・インコーポレーテッド | 蛋白質キナーゼ活性の調節剤としての２−インドリノン誘導体 |
| GB9716557D0 (en) * | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
| GB9718913D0 (en) * | 1997-09-05 | 1997-11-12 | Glaxo Group Ltd | Substituted oxindole derivatives |
| WO1999048868A2 (en) | 1998-03-26 | 1999-09-30 | Sugen, Inc. | Heterocyclic classes of compounds for the modulating tyrosine protein kinase |
| CA2383623A1 (en) | 1998-08-04 | 2000-02-17 | Sugen, Inc. | 3-methylidenyl-2-indolinone modulators of protein kinase |
-
1999
- 1999-12-11 KR KR1020017007570A patent/KR20010108024A/ko not_active Ceased
- 1999-12-11 AU AU19773/00A patent/AU767138B2/en not_active Ceased
- 1999-12-11 BR BR9916324-1A patent/BR9916324A/pt not_active IP Right Cessation
- 1999-12-11 JP JP2000588180A patent/JP2002532503A/ja active Pending
- 1999-12-11 CA CA002354402A patent/CA2354402A1/en not_active Abandoned
- 1999-12-11 ES ES99963496T patent/ES2301255T3/es not_active Expired - Lifetime
- 1999-12-11 AT AT99963496T patent/ATE387448T1/de not_active IP Right Cessation
- 1999-12-11 CN CNB998145971A patent/CN1158283C/zh not_active Expired - Fee Related
- 1999-12-11 TR TR2001/01756T patent/TR200101756T2/xx unknown
- 1999-12-11 DE DE69938258T patent/DE69938258T2/de not_active Expired - Fee Related
- 1999-12-11 WO PCT/EP1999/009806 patent/WO2000035921A1/en not_active Ceased
- 1999-12-11 EP EP99963496A patent/EP1149105B1/en not_active Expired - Lifetime
- 1999-12-15 US US09/464,534 patent/US6221867B1/en not_active Expired - Fee Related
- 1999-12-15 AR ARP990106420A patent/AR021695A1/es unknown
- 1999-12-16 UY UY25854A patent/UY25854A1/es not_active Application Discontinuation
- 1999-12-16 PE PE1999001276A patent/PE20001385A1/es not_active Application Discontinuation
-
2001
- 2001-05-31 ZA ZA200104505A patent/ZA200104505B/en unknown
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