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
- 239000003112 inhibitor Substances 0.000 title abstract 2
- QRRCMVPZJCHBLQ-UHFFFAOYSA-N pyrido[2,3-d]pyrimidine-2,7-diamine Chemical compound C1=NC(N)=NC2=NC(N)=CC=C21 QRRCMVPZJCHBLQ-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003102 growth factor Substances 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 230000003389 potentiating effect Effects 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 208000037803 restenosis Diseases 0.000 abstract 1
- -1 substituted Chemical class 0.000 abstract 1
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
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Neurology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Cardiology (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 |
| MXPA03003612A (en) | 2000-10-23 | 2003-06-19 | Smithkline Beecham Corp | Novel compounds. |
| PE20030008A1 (en) * | 2001-06-19 | 2003-01-22 | Bristol Myers Squibb Co | DUAL INHIBITORS OF PDE 7 AND PDE 4 |
| BR0309053A (en) | 2002-04-19 | 2005-02-22 | Smithkline Beecham Corp | Compounds |
| WO2004048343A1 (en) * | 2002-11-28 | 2004-06-10 | Schering Aktiengesellschaft | Chk-, pdk- and akt-inhibitory 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 |
| CN101014600A (en) * | 2004-09-21 | 2007-08-08 | 霍夫曼-拉罗奇有限公司 | 6-(2-alkyl-phenyl) - pyrido[2,3-d] pyrimidines useful as proteine kinase inhibitors |
| AR053450A1 (en) | 2005-03-25 | 2007-05-09 | Glaxo Group Ltd | DERIVATIVES OF 3,4-DIHYDRO-PYRIMID (4,5-D) PYRIMIDIN-2- (1H) -ONA 1,5,7 TRISUSTITUTED AS INHIBITORS OF QUINASE P38 |
| US7423042B2 (en) | 2005-03-25 | 2008-09-09 | Glaxo Group Limited | Compounds |
| PE20100737A1 (en) | 2005-03-25 | 2010-11-27 | Glaxo Group Ltd | NEW COMPOUNDS |
| CN101495475A (en) | 2005-03-25 | 2009-07-29 | 葛兰素集团有限公司 | Process for preparing pyrido[2,3-d]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one derivatives |
| FR2887882B1 (en) | 2005-07-01 | 2007-09-07 | Sanofi Aventis Sa | PYRIDO [2,3-D] PYRIMIDINE DERIVATIVES, THEIR PREPARATION, THEIR THERAPEUTIC APPLICATION |
| KR100962723B1 (en) * | 2005-07-21 | 2010-06-09 | 에프. 호프만-라 로슈 아게 | Pyrido[2,3-d]pyrimidine-2,4-diamine compounds as ptp1b 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 |
| MX2011005720A (en) * | 2008-12-01 | 2011-06-17 | Merck Patent Gmbh | 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 |
| GB201216017D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Inhibitor compounds |
| GB201216018D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Pharmacologically active compounds |
| WO2014151682A1 (en) * | 2013-03-14 | 2014-09-25 | 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 | Miscellaneous generation Pyridopyrimidinone derivatives are as CDK inhibitor and its application |
| 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 |
|---|---|---|---|---|
| GEP20012444B (en) * | 1994-11-14 | 2001-05-25 | Warner Lambert Company Us | 6-Aryl Pyrido[2,3-d]Pyrimidines and Naphthyridines, Pharmaceutical Composition on Their Basis and Application for Inhibiting Cellular Proliferation |
| 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 |
| ES2310039T3 (en) * | 1998-05-26 | 2008-12-16 | Warner-Lambert Company Llc | BICYCLE PYRIMIDINES AND BICYCLE 3,4-DIHYDROPIRIMIDINS AS INHIBITORS OF CELL PROLIFERATION. |
-
2001
- 2001-01-23 AR ARP010100285A patent/AR030044A1/en not_active Application Discontinuation
- 2001-01-23 AU AU25425/01A patent/AU2542501A/en not_active Abandoned
- 2001-01-23 MX MXPA02007221A patent/MXPA02007221A/en not_active Application Discontinuation
- 2001-01-23 PA PA20018510701A patent/PA8510701A1/en unknown
- 2001-01-23 CN CN01804048A patent/CN1395578A/en active Pending
- 2001-01-23 JP JP2001561006A patent/JP4047010B2/en not_active Expired - Fee Related
- 2001-01-23 OA OA1200200213A patent/OA12161A/en unknown
- 2001-01-23 GT GT200100016A patent/GT200100016A/en unknown
- 2001-01-23 WO PCT/IB2001/000069 patent/WO2001055147A1/en not_active Application Discontinuation
- 2001-01-23 AP APAP/P/2002/002586A patent/AP2002002586A0/en unknown
- 2001-01-23 BR BR0107751-1A patent/BR0107751A/en not_active IP Right Cessation
- 2001-01-23 KR KR1020027009516A patent/KR20020065939A/en not_active Application Discontinuation
- 2001-01-23 HU HU0204141A patent/HUP0204141A3/en unknown
- 2001-01-23 EA EA200200643A patent/EA200200643A1/en unknown
- 2001-01-23 CZ CZ20022475A patent/CZ20022475A3/en unknown
- 2001-01-23 SK SK1063-2002A patent/SK10632002A3/en not_active Application Discontinuation
- 2001-01-23 CA CA002397961A patent/CA2397961C/en not_active Expired - Fee Related
- 2001-01-23 EE EEP200200405A patent/EE200200405A/en unknown
- 2001-01-23 IL IL15054501A patent/IL150545A0/en unknown
- 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 DZ DZ013266A patent/DZ3266A1/en active
- 2001-01-23 YU YU50402A patent/YU50402A/en unknown
- 2001-01-23 PL PL01356802A patent/PL356802A1/en not_active Application Discontinuation
- 2001-01-24 TN TNTNSN01014A patent/TNSN01014A1/en unknown
- 2001-01-24 SV SV2001000294A patent/SV2002000294A/en not_active Application Discontinuation
- 2001-01-24 HN HN2001000013A patent/HN2001000013A/en unknown
- 2001-01-24 CO CO01005268A patent/CO5261549A1/en not_active Application Discontinuation
-
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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