EA200301005A1 - Замещенные в положении 6 индолиноны и их применение в качестве ингибиторов киназ - Google Patents
Замещенные в положении 6 индолиноны и их применение в качестве ингибиторов киназInfo
- Publication number
- EA200301005A1 EA200301005A1 EA200301005A EA200301005A EA200301005A1 EA 200301005 A1 EA200301005 A1 EA 200301005A1 EA 200301005 A EA200301005 A EA 200301005A EA 200301005 A EA200301005 A EA 200301005A EA 200301005 A1 EA200301005 A1 EA 200301005A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- application
- compounds
- indolinons
- substituted
- salts
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 102000016736 Cyclin Human genes 0.000 abstract 1
- 108050006400 Cyclin Proteins 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 210000002889 endothelial cell Anatomy 0.000 abstract 1
- JYGFTBXVXVMTGB-UHFFFAOYSA-N indolin-2-one Chemical class C1=CC=C2NC(=O)CC2=C1 JYGFTBXVXVMTGB-UHFFFAOYSA-N 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 230000035755 proliferation Effects 0.000 abstract 1
- 102000027426 receptor tyrosine kinases Human genes 0.000 abstract 1
- 108091008598 receptor tyrosine kinases Proteins 0.000 abstract 1
- 210000004881 tumor cell Anatomy 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/32—Oxygen atoms
- C07D209/34—Oxygen atoms in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
Abstract
В заявке описаны замещенные в положении 6 индолиноны общей формулы (I)в которой R-Rи X имеют указанные в п.1 формулы изобретения значения, их изомеры и их соли, прежде всего их физиологически приемлемые соли, которые обладают ценными фармакологическими свойствами, прежде всего ингибирующим действием на различные рецепторные тирозинкиназы и циклин/CDK-комплексы, а также на пролиферацию эндотелиальных клеток и различных опухолевых клеток, а также описаны содержащие эти соединения лекарственные средства, применение этих соединений и способ их получения.Международная заявка была опубликована вместе с отчетом о международном поиске.
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 (1)
Publication Number | Publication Date |
---|---|
EA200301005A1 true EA200301005A1 (ru) | 2004-04-29 |
Family
ID=7680648
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200301005A EA200301005A1 (ru) | 2001-04-06 | 2002-03-30 | Замещенные в положении 6 индолиноны и их применение в качестве ингибиторов киназ |
Country Status (23)
Country | Link |
---|---|
US (1) | US6858641B2 (ru) |
EP (1) | EP1379501A1 (ru) |
JP (1) | JP2004525173A (ru) |
KR (1) | KR20030090712A (ru) |
CN (1) | CN1509270A (ru) |
AR (1) | AR035813A1 (ru) |
BG (1) | BG108220A (ru) |
BR (1) | BR0208900A (ru) |
CA (1) | CA2442695A1 (ru) |
CZ (1) | CZ20032975A3 (ru) |
DE (1) | DE10117204A1 (ru) |
EA (1) | EA200301005A1 (ru) |
EC (1) | ECSP034776A (ru) |
EE (1) | EE200300491A (ru) |
HU (1) | HUP0303737A3 (ru) |
IL (1) | IL158254A0 (ru) |
MX (1) | MXPA03008896A (ru) |
NO (1) | NO20034434D0 (ru) |
PE (1) | PE20021058A1 (ru) |
PL (1) | PL366458A1 (ru) |
SK (1) | SK12412003A3 (ru) |
WO (1) | WO2002081445A1 (ru) |
ZA (1) | ZA200307306B (ru) |
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 |
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 |
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 |
WO2007057397A1 (en) * | 2005-11-15 | 2007-05-24 | Boehringer Ingelheim International Gmbh | Treatment of cancer |
SI2212297T1 (sl) | 2007-10-12 | 2011-09-30 | Ingenium Pharmaceuticals Gmbh | Inhibitorji protein kinaz |
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 |
US8344018B2 (en) * | 2008-07-14 | 2013-01-01 | Gilead Sciences, Inc. | Oxindolyl inhibitor compounds |
NZ590560A (en) * | 2008-07-29 | 2012-12-21 | Boehringer Ingelheim Int | Indolinone Inhibitors of cell cycle kinases |
EA201201274A1 (ru) | 2010-03-10 | 2013-04-30 | Инджениум Фармасьютиклз Гмбх | Ингибиторы протеинкиназ |
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 |
ES2796358T3 (es) * | 2015-12-24 | 2020-11-26 | Respivert Ltd | Compuestos de indolinonas y su uso en el tratamiento de enfermedades fibróticas |
ES2836255T3 (es) * | 2016-03-08 | 2021-06-24 | Respivert Ltd | Derivados de indol y su uso como inhibidores de proteína cinasa |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2001503736A (ja) * | 1996-08-23 | 2001-03-21 | スージェン・インコーポレーテッド | 疾病の治療のためのインドリノンのコンビナトリアルライブラリーおよび関連する生成物および方法 |
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 |
DE19816624A1 (de) | 1998-04-15 | 1999-10-21 | Boehringer Ingelheim Pharma | Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
US6169106B1 (en) | 1998-04-15 | 2001-01-02 | Boehringer Ingelheim Pharma Kg | Indolinones having kinase inhibitory activity |
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 |
WO2001016130A1 (de) | 1999-08-27 | 2001-03-08 | Boehringer Ingelheim Pharma Kg | Substituierte indolinone als tyrosinkinase inhibitoren |
DE19940829A1 (de) | 1999-08-27 | 2001-03-01 | Boehringer Ingelheim Pharma | Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
UA75054C2 (ru) | 1999-10-13 | 2006-03-15 | Бьорінгер Інгельхайм Фарма Гмбх & Ко. Кг | Замещенные в положении 6 индолиноны, их получение и их применение как лекарственного средства |
DE10042696A1 (de) | 2000-08-31 | 2002-03-14 | Boehringer Ingelheim Pharma | In 6-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
-
2001
- 2001-04-06 DE DE10117204A patent/DE10117204A1/de not_active Withdrawn
-
2002
- 2002-03-30 CA CA002442695A patent/CA2442695A1/en not_active Abandoned
- 2002-03-30 HU HU0303737A patent/HUP0303737A3/hu unknown
- 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 MX MXPA03008896A patent/MXPA03008896A/es unknown
- 2002-03-30 WO PCT/EP2002/003583 patent/WO2002081445A1/de not_active Application Discontinuation
- 2002-03-30 CZ CZ20032975A patent/CZ20032975A3/cs unknown
- 2002-03-30 EP EP02735201A patent/EP1379501A1/de not_active Withdrawn
- 2002-03-30 PL PL02366458A patent/PL366458A1/xx not_active Application Discontinuation
- 2002-03-30 CN CNA028099184A patent/CN1509270A/zh active Pending
- 2002-03-30 IL IL15825402A patent/IL158254A0/xx unknown
- 2002-03-30 JP JP2002579433A patent/JP2004525173A/ja not_active Ceased
- 2002-03-30 BR BR0208900-9A patent/BR0208900A/pt active Pending
- 2002-03-30 EE EEP200300491A patent/EE200300491A/xx unknown
- 2002-03-30 SK SK1241-2003A patent/SK12412003A3/sk unknown
- 2002-04-04 US US10/116,365 patent/US6858641B2/en not_active Expired - Lifetime
- 2002-04-05 AR ARP020101257A patent/AR035813A1/es not_active Withdrawn
- 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 active Pending
- 2003-10-03 NO NO20034434A patent/NO20034434D0/no not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
CN1509270A (zh) | 2004-06-30 |
CA2442695A1 (en) | 2002-10-17 |
WO2002081445A1 (de) | 2002-10-17 |
AR035813A1 (es) | 2004-07-14 |
US6858641B2 (en) | 2005-02-22 |
EE200300491A (et) | 2004-02-16 |
NO20034434L (no) | 2003-10-03 |
NO20034434D0 (no) | 2003-10-03 |
PE20021058A1 (es) | 2003-01-20 |
SK12412003A3 (sk) | 2004-04-06 |
JP2004525173A (ja) | 2004-08-19 |
HUP0303737A2 (hu) | 2004-03-01 |
EP1379501A1 (de) | 2004-01-14 |
IL158254A0 (en) | 2004-05-12 |
HUP0303737A3 (en) | 2004-09-28 |
PL366458A1 (en) | 2005-02-07 |
BR0208900A (pt) | 2004-04-20 |
DE10117204A1 (de) | 2002-10-10 |
US20030092756A1 (en) | 2003-05-15 |
ECSP034776A (es) | 2003-12-01 |
BG108220A (bg) | 2004-09-30 |
CZ20032975A3 (cs) | 2004-02-18 |
KR20030090712A (ko) | 2003-11-28 |
ZA200307306B (en) | 2004-08-31 |
MXPA03008896A (es) | 2003-12-08 |
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