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 |
| ES2318041T3 (es) | 2001-07-23 | 2009-05-01 | Laboratoires Serono Sa | Derivados de arilsulfonamida como inhibidores de c-jun quinasas (jnk) n-terminales. |
| DE60332215D1 (de) | 2002-02-28 | 2010-06-02 | Eisai R&D Man Co Ltd | Neue indazolverbindungen mit kondensiertem ring |
| IL164082A0 (en) | 2002-03-28 | 2005-12-18 | Eisai Co Ltd | Azaindole derivatives and pharmaceutical compositions containing the same |
| EP1490364B1 (en) | 2002-03-28 | 2007-09-26 | Eisai R&D Management Co., Ltd. | 7-azaindoles as inhibitors of c-jun n-terminal kinases for the treatment of neurodegenerative disorders |
| DE60317198T2 (de) * | 2002-05-23 | 2008-12-04 | Cytopia Research Pty. Ltd., Richmond | Proteinkinaseinhibitoren |
| CA2482838A1 (en) | 2002-05-31 | 2003-12-11 | Eisai Co., Ltd. | Pyrazole compounds and pharmaceutical compositions containing the compound |
| EP1527070B1 (en) | 2002-06-14 | 2013-01-09 | Merck Serono SA | 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 |
| JP2007515940A (ja) * | 2003-05-08 | 2007-06-21 | ワイス | 関節炎及びその他の炎症性疾患の薬物標的としてのプロテインキナーゼｃゼータ |
| WO2004101565A2 (en) | 2003-05-16 | 2004-11-25 | Eisai Co., Ltd. | Jnk inhibitors |
| JP2007509173A (ja) | 2003-10-24 | 2007-04-12 | シエーリング アクチエンゲゼルシャフト | インドリノン誘導体類及び疾病状態、例えば癌の処理へのそれらの使用 |
| 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 |
| RU2008112691A (ru) | 2005-10-03 | 2009-10-10 | Оно Фармасьютикал Ко., Лтд. (Jp) | Азотсодержащее гетероциклическое соединение и его фармацевтическое применение |
| ZA200804717B (en) | 2005-12-29 | 2010-02-24 | Anthrogenesis Corp | Improved composition for collecting and preserving a 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 |
| ES2110965T3 (es) | 1989-07-25 | 1998-03-01 | Taiho Pharmaceutical Co Ltd | Derivado de oxoindol. |
| 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 |
| JPH11512708A (ja) | 1995-09-11 | 1999-11-02 | オステオアルスリィティス サイエンシズ，インコーポレイテッド | 変形性関節炎を治療するためのプロテインチロシンキナーゼインヒビター |
| 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 |
| KR100281867B1 (ko) | 1996-01-17 | 2001-02-15 | 고바야시 유키오 | 3-(비스-치환페닐메틸렌)옥신돌유도체 |
| ATE243034T1 (de) * | 1996-01-17 | 2003-07-15 | Taiho Pharmaceutical Co Ltd | Intimale verdickungsinhibitoren |
| 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 |
| WO1998007695A1 (en) * | 1996-08-23 | 1998-02-26 | Sugen, Inc. | Indolinone combinatorial libraries and related products and methods for the treatment of disease |
| WO1998024432A2 (en) | 1996-12-05 | 1998-06-11 | Sugen, Inc. | Use of indolinone compounds as modulators of protein kinases |
| EP0984930B1 (en) | 1997-05-07 | 2005-04-06 | Sugen, Inc. | 2-indolinone derivatives as modulators of protein kinase activity |
| 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 |
| EP1066257A2 (en) | 1998-03-26 | 2001-01-10 | Sugen, Inc. | Heterocylic 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 CN CNB998145971A patent/CN1158283C/zh not_active Expired - Fee Related
- 1999-12-11 ES ES99963496T patent/ES2301255T3/es not_active Expired - Lifetime
- 1999-12-11 WO PCT/EP1999/009806 patent/WO2000035921A1/en not_active Ceased
- 1999-12-11 DE DE69938258T patent/DE69938258T2/de not_active Expired - Fee Related
- 1999-12-11 TR TR2001/01756T patent/TR200101756T2/xx unknown
- 1999-12-11 JP JP2000588180A patent/JP2002532503A/ja active Pending
- 1999-12-11 AT AT99963496T patent/ATE387448T1/de not_active IP Right Cessation
- 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 KR KR1020017007570A patent/KR20010108024A/ko not_active Ceased
- 1999-12-11 CA CA002354402A patent/CA2354402A1/en not_active Abandoned
- 1999-12-11 EP EP99963496A patent/EP1149105B1/en not_active Expired - Lifetime
- 1999-12-15 AR ARP990106420A patent/AR021695A1/es unknown
- 1999-12-15 US US09/464,534 patent/US6221867B1/en not_active Expired - Fee Related
- 1999-12-16 PE PE1999001276A patent/PE20001385A1/es not_active Application Discontinuation
- 1999-12-16 UY UY25854A patent/UY25854A1/es not_active Application Discontinuation
-
2001
- 2001-05-31 ZA ZA200104505A patent/ZA200104505B/en unknown