HUP0303737A2 - 6-helyzetben szubsztituált indolinonok és alkalmazásuk kináz inhibitorokként, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények - Google Patents
6-helyzetben szubsztituált indolinonok és alkalmazásuk kináz inhibitorokként, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0303737A2 HUP0303737A2 HU0303737A HUP0303737A HUP0303737A2 HU P0303737 A2 HUP0303737 A2 HU P0303737A2 HU 0303737 A HU0303737 A HU 0303737A HU P0303737 A HUP0303737 A HU P0303737A HU P0303737 A2 HUP0303737 A2 HU P0303737A2
- Authority
- HU
- Hungary
- Prior art keywords
- substituted
- indolinones
- preparation
- pharmaceutical compositions
- compositions containing
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- JYGFTBXVXVMTGB-UHFFFAOYSA-N indolin-2-one Chemical class C1=CC=C2NC(=O)CC2=C1 JYGFTBXVXVMTGB-UHFFFAOYSA-N 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005170 cycloalkyloxycarbonyl group Chemical group 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- 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
- 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
- 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
Abstract
A találmány tárgyát az általános képletű vegyületek - ahol X -O- vagy-S-; R1 H vagy egy prodrug csoport; R2 karboxi-, alkoxi-karbonil-,cikloalkoxi-karbonil- vagy aril-oxi-karbonilcsoport; R3 H, alkil-,cikloalkil-, trifluor-metil-, heteroaril-, adott esetben mono- vagydiszubsztituált fenil- vagy naftilcsoport; R4 szubsztituált fenil-,pirrolil- vagy furilcsoport; és R5 H vagy alkilcsoport - éshatóanyagként tartalmazó gyógyszerkészítmények, alkalmazásuk ésazelőállításukra szolgáló eljárás képezi. Ó
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 |
|---|---|
| HUP0303737A2 true HUP0303737A2 (hu) | 2004-03-01 |
| HUP0303737A3 HUP0303737A3 (en) | 2004-09-28 |
Family
ID=7680648
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0303737A HUP0303737A3 (en) | 2001-04-06 | 2002-03-30 | Indolinones, substituted in position 6, and their use as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US6858641B2 (hu) |
| EP (1) | EP1379501A1 (hu) |
| JP (1) | JP2004525173A (hu) |
| KR (1) | KR20030090712A (hu) |
| CN (1) | CN1509270A (hu) |
| AR (1) | AR035813A1 (hu) |
| BG (1) | BG108220A (hu) |
| BR (1) | BR0208900A (hu) |
| CA (1) | CA2442695A1 (hu) |
| CZ (1) | CZ20032975A3 (hu) |
| DE (1) | DE10117204A1 (hu) |
| EA (1) | EA200301005A1 (hu) |
| EC (1) | ECSP034776A (hu) |
| EE (1) | EE200300491A (hu) |
| HU (1) | HUP0303737A3 (hu) |
| IL (1) | IL158254A0 (hu) |
| MX (1) | MXPA03008896A (hu) |
| NO (1) | NO20034434D0 (hu) |
| PE (1) | PE20021058A1 (hu) |
| PL (1) | PL366458A1 (hu) |
| SK (1) | SK12412003A3 (hu) |
| WO (1) | WO2002081445A1 (hu) |
| ZA (1) | ZA200307306B (hu) |
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 |
| 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 |
| 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 |
| US8716296B2 (en) | 2007-10-12 | 2014-05-06 | Ingenium Pharmaceuticals Gmbh | Inhibitors of protein kinases |
| 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 |
| WO2010009166A1 (en) * | 2008-07-14 | 2010-01-21 | Gilead Colorado, Inc. | Oxindolyl inhibitor compounds |
| TW201011002A (en) | 2008-07-29 | 2010-03-16 | Boehringer Ingelheim Int | New compounds |
| EP2545037A1 (en) | 2010-03-10 | 2013-01-16 | Ingenium Pharmaceuticals GmbH | Inhibitors of protein kinases |
| 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 |
| EP3722291B1 (en) | 2015-12-24 | 2023-07-19 | Respivert Limited | Indolinone compounds and their use in the treatment of fibrotic diseases |
| 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 |
|---|---|---|---|---|
| EP1247803A3 (en) * | 1996-08-23 | 2002-10-16 | Sugen, Inc. | Indolinone compounds suitable for modulation of protein kinases |
| 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 |
| US6794395B1 (en) | 1999-08-27 | 2004-09-21 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Substituted indolinones, their manufacture and their use as medicaments |
| DE19940829A1 (de) | 1999-08-27 | 2001-03-01 | Boehringer Ingelheim Pharma | Neue 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 |
| 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 CZ CZ20032975A patent/CZ20032975A3/cs unknown
- 2002-03-30 KR KR10-2003-7013027A patent/KR20030090712A/ko not_active Application Discontinuation
- 2002-03-30 HU HU0303737A patent/HUP0303737A3/hu unknown
- 2002-03-30 EP EP02735201A patent/EP1379501A1/de not_active Withdrawn
- 2002-03-30 EE EEP200300491A patent/EE200300491A/xx unknown
- 2002-03-30 PL PL02366458A patent/PL366458A1/xx not_active Application Discontinuation
- 2002-03-30 JP JP2002579433A patent/JP2004525173A/ja not_active Ceased
- 2002-03-30 SK SK1241-2003A patent/SK12412003A3/sk unknown
- 2002-03-30 MX MXPA03008896A patent/MXPA03008896A/es unknown
- 2002-03-30 CN CNA028099184A patent/CN1509270A/zh active Pending
- 2002-03-30 BR BR0208900-9A patent/BR0208900A/pt active Pending
- 2002-03-30 IL IL15825402A patent/IL158254A0/xx unknown
- 2002-03-30 EA EA200301005A patent/EA200301005A1/ru unknown
- 2002-03-30 WO PCT/EP2002/003583 patent/WO2002081445A1/de 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 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 |
|---|---|
| ZA200307306B (en) | 2004-08-31 |
| CA2442695A1 (en) | 2002-10-17 |
| EE200300491A (et) | 2004-02-16 |
| NO20034434L (no) | 2003-10-03 |
| EP1379501A1 (de) | 2004-01-14 |
| PL366458A1 (en) | 2005-02-07 |
| KR20030090712A (ko) | 2003-11-28 |
| NO20034434D0 (no) | 2003-10-03 |
| AR035813A1 (es) | 2004-07-14 |
| ECSP034776A (es) | 2003-12-01 |
| CN1509270A (zh) | 2004-06-30 |
| US6858641B2 (en) | 2005-02-22 |
| JP2004525173A (ja) | 2004-08-19 |
| BR0208900A (pt) | 2004-04-20 |
| EA200301005A1 (ru) | 2004-04-29 |
| US20030092756A1 (en) | 2003-05-15 |
| HUP0303737A3 (en) | 2004-09-28 |
| WO2002081445A1 (de) | 2002-10-17 |
| DE10117204A1 (de) | 2002-10-10 |
| IL158254A0 (en) | 2004-05-12 |
| BG108220A (bg) | 2004-09-30 |
| MXPA03008896A (es) | 2003-12-08 |
| PE20021058A1 (es) | 2003-01-20 |
| SK12412003A3 (sk) | 2004-04-06 |
| CZ20032975A3 (cs) | 2004-02-18 |
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