EA200200643A1 - PYRIDO [2,3-d] PYRIMIDIN-2,7-DIAMINE KINAZ INHIBITORS - Google Patents
PYRIDO [2,3-d] PYRIMIDIN-2,7-DIAMINE KINAZ INHIBITORSInfo
- Publication number
- EA200200643A1 EA200200643A1 EA200200643A EA200200643A EA200200643A1 EA 200200643 A1 EA200200643 A1 EA 200200643A1 EA 200200643 A EA200200643 A EA 200200643A EA 200200643 A EA200200643 A EA 200200643A EA 200200643 A1 EA200200643 A1 EA 200200643A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- substituted lower
- nrr
- cor
- compounds
- porr
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
Abstract
Раскрыты соединения формулы (I), где R, R, R, Rи Rпредставляют собой независимо водород или (не)замещенный низший алкил, (не)замещенный низший алкенил, (не)замещенный низший алкинил или (не)замещенный -(CH)R; Rпредставляет собой галоген, циано, нитро, -R, -NRRили -OR; Rпредставляет собой галоген, циано, нитро, -R, -NRR, -OR, -COR, -COR, -CONRR, -NRCOR, (не)замещенный низший алкенил или (не)замещенный низший алкинил; Rпредставляет собой -COR, -COR, -CONRR, -CSNRR, -C(NR)NRR, -SOR, -SOR, -SONRR, -PORR, PORR, -PO(NRR); Rи Rпредставляют собой независимо водород или (не)замещенный низший алкил; Rпредставляет собой гетероарильную или гетероциклическую группу; Rпредставляет собой циклоалкильную, гетероциклическую, арильную или гетероарильную группу; и n равно 0, 1, 2 или 3. Эти соединения и их фармацевтические композиции пригодны для лечения клеточных пролиферативных нарушений, таких как рак и рестеноз. Эти соединения являются сильными ингибиторами cdks и опосредованных фактором роста киназ.Международная заявка была опубликована вместе с отчетом о международном поиске.Compounds of formula (I) are disclosed, wherein R, R, R, R and R are independently hydrogen or (un) substituted lower alkyl, (un) substituted lower alkenyl, (un) substituted lower alkynyl, or (un) substituted - (CH) R ; R1 is halogen, cyano, nitro, -R, -NRR or -OR; R4 is halogen, cyano, nitro, -R, -NRR, -OR, -COR, -COR, -CONRR, -NRCOR, (un) substituted lower alkenyl or (un) substituted lower alkynyl; Is a -COR, -COR, -CONRR, -CSNRR, -C (NR) NRR, -SOR, -SOR, -SONRR, -PORR, PORR, -PO (NRR); R 4 and R 10 are independently hydrogen or (un) substituted lower alkyl; R4 is a heteroaryl or heterocyclic group; R5 is a cycloalkyl, heterocyclic, aryl or heteroaryl group; and n is 0, 1, 2, or 3. These compounds and their pharmaceutical compositions are suitable for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent cdks inhibitors and kinase growth factor mediated. The international application was published along with an international search report.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17826100P | 2000-01-25 | 2000-01-25 | |
| PCT/IB2001/000069 WO2001055147A1 (en) | 2000-01-25 | 2001-01-23 | PYRIDO[2,3-d]PYRIMIDINE-2,7-DIAMINE KINASE INHIBITORS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA200200643A1 true EA200200643A1 (en) | 2002-12-26 |
Family
ID=22651853
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200200643A EA200200643A1 (en) | 2000-01-25 | 2001-01-23 | PYRIDO [2,3-d] PYRIMIDIN-2,7-DIAMINE KINAZ INHIBITORS |
Country Status (34)
| Country | Link |
|---|---|
| EP (1) | EP1254137A1 (en) |
| JP (1) | JP4047010B2 (en) |
| KR (1) | KR20020065939A (en) |
| CN (1) | CN1395578A (en) |
| AP (1) | AP2002002586A0 (en) |
| AR (1) | AR030044A1 (en) |
| AU (1) | AU2542501A (en) |
| BG (1) | BG106850A (en) |
| BR (1) | BR0107751A (en) |
| CA (1) | CA2397961C (en) |
| CO (1) | CO5261549A1 (en) |
| CR (1) | CR6706A (en) |
| CZ (1) | CZ20022475A3 (en) |
| DZ (1) | DZ3266A1 (en) |
| EA (1) | EA200200643A1 (en) |
| EE (1) | EE200200405A (en) |
| GT (1) | GT200100016A (en) |
| HN (1) | HN2001000013A (en) |
| HU (1) | HUP0204141A3 (en) |
| IL (1) | IL150545A0 (en) |
| IS (1) | IS6443A (en) |
| MA (1) | MA26868A1 (en) |
| MX (1) | MXPA02007221A (en) |
| NO (1) | NO20023527L (en) |
| OA (1) | OA12161A (en) |
| PA (1) | PA8510701A1 (en) |
| PE (1) | PE20011066A1 (en) |
| PL (1) | PL356802A1 (en) |
| SK (1) | SK10632002A3 (en) |
| SV (1) | SV2002000294A (en) |
| TN (1) | TNSN01014A1 (en) |
| WO (1) | WO2001055147A1 (en) |
| YU (1) | YU50402A (en) |
| ZA (1) | ZA200205879B (en) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7235551B2 (en) | 2000-03-02 | 2007-06-26 | Smithkline Beecham Corporation | 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases |
| KR100850812B1 (en) | 2000-10-23 | 2008-08-06 | 스미스클라인 비참 코포레이션 | Novel Compounds |
| PE20030008A1 (en) * | 2001-06-19 | 2003-01-22 | Bristol Myers Squibb Co | DUAL INHIBITORS OF PDE 7 AND PDE 4 |
| WO2003088972A1 (en) | 2002-04-19 | 2003-10-30 | Smithkline Beecham Corporation | Novel compounds |
| BR0316680A (en) * | 2002-11-28 | 2005-10-18 | Schering Ag | Chk, pdk and akt inhibitor pyrimidines, their production and use as pharmaceutical agents |
| US7157455B2 (en) * | 2003-02-10 | 2007-01-02 | Hoffmann-La Roche Inc. | 4-Aminopyrimidine-5-one derivatives |
| TW200502236A (en) * | 2003-03-28 | 2005-01-16 | Hoffmann La Roche | Novel pyrido[2,3-d]pyrimidin-7-carboxylic acid derivatives, their manufacture and use as pharmaceutical agents |
| FR2873118B1 (en) | 2004-07-15 | 2007-11-23 | Sanofi Synthelabo | PYRIDO-PYRIMIDINE DERIVATIVES, THEIR APPLICATION IN THERAPEUTICS |
| US7550589B2 (en) * | 2004-09-21 | 2009-06-23 | Hoffman-La Roche Inc. | 6-(2-alkyl-phenyl)-pyrido[2,3-D]pyrimidines useful as protein kinase inhibitors |
| UY29439A1 (en) | 2005-03-25 | 2006-10-02 | Glaxo Group Ltd | NEW COMPOUNDS |
| AU2006229995A1 (en) | 2005-03-25 | 2006-10-05 | Glaxo Group Limited | Process for preparing pyrido(2,3-d)pyrimidin-7-one and 3,4-dihydropyrimido(4,5-d)pyrimidin-2(1H)-one derivatives |
| WO2006110298A2 (en) | 2005-03-25 | 2006-10-19 | Glaxo Group Limited | 8-alkyl/aryl-4-aryl-2-n- (alkylamino)-n'-substituted-n'-cyanoguanidino-8h-pyrido[2,3-d]pyrimidin-7-one compounds and use thereof |
| PE20061351A1 (en) | 2005-03-25 | 2007-01-14 | Glaxo Group Ltd | 8H-PYRID [2,3-d] PYRIMIDIN-7-ONA 2,4,8-TRISUSTITUTED COMPOUNDS AS CSBP / RK / p38 KINASE INHIBITORS |
| FR2887882B1 (en) * | 2005-07-01 | 2007-09-07 | Sanofi Aventis Sa | PYRIDO [2,3-D] PYRIMIDINE DERIVATIVES, THEIR PREPARATION, THEIR THERAPEUTIC APPLICATION |
| ATE449097T1 (en) * | 2005-07-21 | 2009-12-15 | Hoffmann La Roche | PYRIDOÄ2,3-DÜPYRIMIDINE-2,4-DIAMINE COMPOUNDS AS PTPIB INHIBITORS |
| ES2351939T3 (en) * | 2005-08-09 | 2011-02-14 | Irm Llc | COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF PROTEIN KINASES. |
| FR2896246B1 (en) | 2006-01-13 | 2008-08-15 | Sanofi Aventis Sa | PYRIDO-PYRIMIDONE DERIVATIVES, THEIR PREPARATION, THEIR THERAPEUTIC APPLICATION |
| EP1914234A1 (en) | 2006-10-16 | 2008-04-23 | GPC Biotech Inc. | Pyrido[2,3-d]pyrimidines and their use as kinase inhibitors |
| JO2985B1 (en) | 2006-12-20 | 2016-09-05 | Takeda Pharmaceuticals Co | MAPK/ERK Kinase Inhibitors |
| FR2910813B1 (en) * | 2006-12-28 | 2009-02-06 | Sanofi Aventis Sa | NEW THERAPEUTIC USE FOR THE TREATMENT OF LEUKEMIA |
| EP2112150B1 (en) | 2008-04-22 | 2013-10-16 | Forma Therapeutics, Inc. | Improved raf inhibitors |
| JP5697601B2 (en) * | 2008-12-01 | 2015-04-08 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | 2,5-Diamino-substituted pyrido [4,3-D] pyrimidines as autotaxin inhibitors against cancer |
| GB201104267D0 (en) | 2011-03-14 | 2011-04-27 | Cancer Rec Tech Ltd | Pyrrolopyridineamino derivatives |
| GB201216018D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Pharmacologically active compounds |
| GB201216017D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Inhibitor compounds |
| EP2968331B1 (en) * | 2013-03-14 | 2020-07-01 | Icahn School of Medicine at Mount Sinai | Pyrimidine compounds as kinase inhibitors |
| GB201403536D0 (en) | 2014-02-28 | 2014-04-16 | Cancer Rec Tech Ltd | Inhibitor compounds |
| KR101671404B1 (en) * | 2014-09-02 | 2016-11-02 | 한국원자력의학원 | Pyrimidine derivatives having anti-cancer effect, combination therapeutic effect with radiation, and anti-diabetic effect, and PPAR activity, and medical use thereof |
| CN107286180B (en) * | 2016-04-11 | 2019-07-02 | 上海勋和医药科技有限公司 | Heteropyridopyrimidinone derivatives as CDK inhibitors and their applications |
| GB201709840D0 (en) | 2017-06-20 | 2017-08-02 | Inst Of Cancer Research: Royal Cancer Hospital | Methods and medical uses |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2146782T3 (en) * | 1994-11-14 | 2000-08-16 | Warner Lambert Co | 6-ARYL-PIRIDO (2,3-D) PIRIMIDINAS AND NAFTIRIDINAS FOR THE INHIBITION OF THE CELL PROLIFERATION INDUCED BY THE PROTEIN TIROSINA QUINASA. |
| IL115256A0 (en) * | 1994-11-14 | 1995-12-31 | Warner Lambert Co | 6-Aryl pyrido (2,3-d) pyrimidines and naphthyridines and their use |
| US5620981A (en) * | 1995-05-03 | 1997-04-15 | Warner-Lambert Company | Pyrido [2,3-D]pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation |
| EE200000706A (en) * | 1998-05-26 | 2002-06-17 | Warner-Lambert Company | Bicyclic pyrimidines and bicyclic 3,4-dihydropyrimidines as inhibitors of cell proliferation |
-
2001
- 2001-01-23 AR ARP010100285A patent/AR030044A1/en not_active Application Discontinuation
- 2001-01-23 PL PL01356802A patent/PL356802A1/en not_active Application Discontinuation
- 2001-01-23 CZ CZ20022475A patent/CZ20022475A3/en unknown
- 2001-01-23 BR BR0107751-1A patent/BR0107751A/en not_active IP Right Cessation
- 2001-01-23 OA OA1200200213A patent/OA12161A/en unknown
- 2001-01-23 IL IL15054501A patent/IL150545A0/en unknown
- 2001-01-23 PA PA20018510701A patent/PA8510701A1/en unknown
- 2001-01-23 CA CA002397961A patent/CA2397961C/en not_active Expired - Fee Related
- 2001-01-23 AU AU25425/01A patent/AU2542501A/en not_active Abandoned
- 2001-01-23 EE EEP200200405A patent/EE200200405A/en unknown
- 2001-01-23 AP APAP/P/2002/002586A patent/AP2002002586A0/en unknown
- 2001-01-23 YU YU50402A patent/YU50402A/en unknown
- 2001-01-23 DZ DZ013266A patent/DZ3266A1/en active
- 2001-01-23 SK SK1063-2002A patent/SK10632002A3/en not_active Application Discontinuation
- 2001-01-23 MX MXPA02007221A patent/MXPA02007221A/en not_active Application Discontinuation
- 2001-01-23 JP JP2001561006A patent/JP4047010B2/en not_active Expired - Fee Related
- 2001-01-23 CN CN01804048A patent/CN1395578A/en active Pending
- 2001-01-23 KR KR1020027009516A patent/KR20020065939A/en not_active Ceased
- 2001-01-23 EA EA200200643A patent/EA200200643A1/en unknown
- 2001-01-23 GT GT200100016A patent/GT200100016A/en unknown
- 2001-01-23 WO PCT/IB2001/000069 patent/WO2001055147A1/en not_active Ceased
- 2001-01-23 EP EP01900591A patent/EP1254137A1/en not_active Withdrawn
- 2001-01-23 PE PE2001000072A patent/PE20011066A1/en not_active Application Discontinuation
- 2001-01-23 HU HU0204141A patent/HUP0204141A3/en unknown
- 2001-01-24 HN HN2001000013A patent/HN2001000013A/en unknown
- 2001-01-24 SV SV2001000294A patent/SV2002000294A/en not_active Application Discontinuation
- 2001-01-24 CO CO01005268A patent/CO5261549A1/en not_active Application Discontinuation
- 2001-01-24 TN TNTNSN01014A patent/TNSN01014A1/en unknown
-
2002
- 2002-06-20 BG BG106850A patent/BG106850A/en unknown
- 2002-06-25 IS IS6443A patent/IS6443A/en unknown
- 2002-07-17 CR CR6706A patent/CR6706A/en not_active Application Discontinuation
- 2002-07-22 MA MA26736A patent/MA26868A1/en unknown
- 2002-07-23 ZA ZA200205879A patent/ZA200205879B/en unknown
- 2002-07-24 NO NO20023527A patent/NO20023527L/en not_active Application Discontinuation
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