HUP0204141A2 - Pyrido[2,3d]pyrimidine-2,7-diamine inhibitors, pharmaceutical compositions containing them and their use - Google Patents
Pyrido[2,3d]pyrimidine-2,7-diamine inhibitors, pharmaceutical compositions containing them and their useInfo
- Publication number
- HUP0204141A2 HUP0204141A2 HU0204141A HUP0204141A HUP0204141A2 HU P0204141 A2 HUP0204141 A2 HU P0204141A2 HU 0204141 A HU0204141 A HU 0204141A HU P0204141 A HUP0204141 A HU P0204141A HU P0204141 A2 HUP0204141 A2 HU P0204141A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- unsubstituted
- substituted
- general formula
- compounds
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 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
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 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
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 101150020251 NR13 gene Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 abstract 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 208000035269 cancer or benign tumor Diseases 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 208000037803 restenosis Diseases 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
- 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)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (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
A jelen találmány tárgyát az (I) általános képletű vegyületek képezik,ahol az R2, az R7, az R13, az R14 és az R15 jelentése egymástólfüggetlenül hidrogénatom, vagy szubsztituálatlan/szubsztituált kisszénatomszámú alkil-, szubsztituálatlan/szubsztituált kisszénatomszámú alkenil- vagy szubsztituálatlan/szubsztituált kisszénatomszámú alkenil csoport, vagy a -(CH2)nR12 általános képletűcsoport, amely szubsztituálatlan vagy szubsztituált; az R5 jelentésehalogénatom, ciano- vagy nitrocsoport, illetve az -R, az -NR9R10 vagyaz -OR9 általános képletű csoport; az R6 jelentése halogénatom, ciano-vagy nitrocsoport, vagy az -R9, az -NR9R10, az -OR9, a -CO2R9, a -COR9, a -CON-R9R10 vagy az -NR9COR10 általános képletű csoport,illetve szubsztituálatlan/szubsztituált kis szénatomszámú alkenil-,vagy szubsztituálatlan/szubsztituált kis szénatomszámú alkinil-csoport; az R8 jelentése a -CO2R13, a -COR13, a -CONR13R14, a -CSNR13R14, a -C(NR13)NR14R15, az -SO3R13, az -SO2R13, az -SO2NR13R14,a PO3R13R14, a -POR13R14, vagy a -PO(NR13R14)a általános képletűcsoport; az R9 és az R10 jelentése egymástól függetlenül hidrogénatom,vagy szubsztituálatlan/szubsztituált kis szénatomszámú alkilcsoport;az R11 egy heteroarilcsoportot vagy egy heterociklusos csoportot elem;az R12 egy cikloalkilcsoportot, egy heterociklusos csoportot, egyaril- vagy egy heteroarilcsoportot jelent; valamint az n jelentése 0,1, 2 vagy 3. Ezek a vegyületek, és gyógyszerészeti készítményeikalkalmasak a sejtproliferáció zavaraival kapcsolatos betegségek (mintpéldául a rák vagy a restenosis) kezelésére. Ezek a vegyületekhatékonyan gátolják a cdk-kat és a növekedési faktorok általaktiválható tirozin-kinázokat. ÓThe subject of the present invention is the compounds of general formula (I), where R2, R7, R13, R14 and R15 are independently hydrogen, or unsubstituted/substituted lower alkyl, unsubstituted/substituted lower alkenyl, or unsubstituted/substituted a low-carbon alkenyl group, or a group of the general formula -(CH2)nR12, which is unsubstituted or substituted; R5 is a halogen atom, cyano or nitro group, or -R, -NR9R10 or -OR9; R6 is a halogen atom, a cyano or nitro group, or a group of the general formula -R9, -NR9R10, -OR9, -CO2R9, -COR9, -CON-R9R10 or -NR9COR10, or an unsubstituted/substituted small carbon number alkenyl or unsubstituted/substituted low carbon alkynyl; R8 is -CO2R13, -COR13, -CONR13R14, -CSNR13R14, -C(NR13)NR14R15, -SO3R13, -SO2R13, -SO2NR13R14, PO3R13R14, -POR13R14, or -PO (NR13R14) is a group of general formula; R9 and R10 are independently a hydrogen atom or an unsubstituted/substituted lower alkyl group; R11 is a heteroaryl group or a heterocyclic group; R12 is a cycloalkyl group, a heterocyclic group, a monoaryl or a heteroaryl group; and n is 0, 1, 2 or 3. These compounds and their pharmaceutical preparations are useful for the treatment of diseases associated with cell proliferation disorders (such as cancer or restenosis). These compounds effectively inhibit cdks and growth factor-activatable tyrosine kinases. HE
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 (2)
| Publication Number | Publication Date |
|---|---|
| HUP0204141A2 true HUP0204141A2 (en) | 2003-04-28 |
| HUP0204141A3 HUP0204141A3 (en) | 2005-03-29 |
Family
ID=22651853
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0204141A HUP0204141A3 (en) | 2000-01-25 | 2001-01-23 | Pyrido[2,3d]pyrimidine-2,7-diamine inhibitors, pharmaceutical compositions containing them and their use |
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 |
| CZ20031125A3 (en) | 2000-10-23 | 2003-10-15 | Smithkline Beecham Corporation | Novel compounds |
| PE20030008A1 (en) * | 2001-06-19 | 2003-01-22 | Bristol Myers Squibb Co | DUAL INHIBITORS OF PDE 7 AND PDE 4 |
| PL373339A1 (en) | 2002-04-19 | 2005-08-22 | Smithkline Beecham Corporation | Novel compounds |
| JP2006508997A (en) * | 2002-11-28 | 2006-03-16 | シエーリング アクチエンゲゼルシャフト | Chk-, Pdk- and Akt-inhibiting pyrimidines, their preparation and use as pharmaceuticals |
| 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 |
| AR053346A1 (en) | 2005-03-25 | 2007-05-02 | Glaxo Group Ltd | COMPOSITE DERIVED FROM 8H -PIRIDO (2,3-D) PIRIMIDIN -7 ONA 2,4,8- TRISUSTITUTED PHARMACEUTICAL COMPOSITION AND USE TO PREPARE A COMPOSITION FOR TREATMENT AND PROFILXIS OF A DISEASE MEDIATED BY KINASE CSBP / RK / P38 |
| JP2008535822A (en) | 2005-03-25 | 2008-09-04 | グラクソ グループ リミテッド | New compounds |
| EA200702073A1 (en) | 2005-03-25 | 2008-12-30 | Глэксо Груп Лимитед | Method of producing pyrido [2,3-d] pyrimidine-7-bp and 3,4-dihidropyrimido [4,5-d] pyrmidin-2 (1h) -onovy derivatives |
| UY29439A1 (en) | 2005-03-25 | 2006-10-02 | Glaxo Group Ltd | NEW COMPOUNDS |
| 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 |
| US8530650B2 (en) * | 2008-12-01 | 2013-09-10 | 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 |
| EP3733184B1 (en) * | 2013-03-14 | 2023-08-30 | Icahn School of Medicine at Mount Sinai | Pyrimidine compounds for use in the treatment of cancer |
| 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 |
|---|---|---|---|---|
| IL115256A0 (en) * | 1994-11-14 | 1995-12-31 | Warner Lambert Co | 6-Aryl pyrido (2,3-d) pyrimidines and naphthyridines and their use |
| TJ342B (en) * | 1994-11-14 | 2002-10-06 | Warner Lambert Co | Derivatives of 6-aryl pyrido Ä2,3-dÜ pyrimidines and naphthyridines pharmaceutical composition possess inhibiting effect of cellular proliferation pr ovoking protein tyrosine kinase and method of inhibiting cellular proliferation |
| US5620981A (en) * | 1995-05-03 | 1997-04-15 | Warner-Lambert Company | Pyrido [2,3-D]pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation |
| EP1080092B1 (en) * | 1998-05-26 | 2008-07-23 | Warner-Lambert Company LLC | Bicyclic pyrimidines and bicyclic 3,4-dihydropyrimidines as inhibitors of cellular proliferation |
-
2001
- 2001-01-23 PL PL01356802A patent/PL356802A1/en not_active Application Discontinuation
- 2001-01-23 AU AU25425/01A patent/AU2542501A/en not_active Abandoned
- 2001-01-23 BR BR0107751-1A patent/BR0107751A/en not_active IP Right Cessation
- 2001-01-23 EP EP01900591A patent/EP1254137A1/en not_active Withdrawn
- 2001-01-23 PA PA20018510701A patent/PA8510701A1/en unknown
- 2001-01-23 AP APAP/P/2002/002586A patent/AP2002002586A0/en unknown
- 2001-01-23 WO PCT/IB2001/000069 patent/WO2001055147A1/en not_active Application Discontinuation
- 2001-01-23 PE PE2001000072A patent/PE20011066A1/en not_active Application Discontinuation
- 2001-01-23 HU HU0204141A patent/HUP0204141A3/en unknown
- 2001-01-23 DZ DZ013266A patent/DZ3266A1/en active
- 2001-01-23 AR ARP010100285A patent/AR030044A1/en not_active Application Discontinuation
- 2001-01-23 KR KR1020027009516A patent/KR20020065939A/en not_active Application Discontinuation
- 2001-01-23 SK SK1063-2002A patent/SK10632002A3/en not_active Application Discontinuation
- 2001-01-23 IL IL15054501A patent/IL150545A0/en unknown
- 2001-01-23 GT GT200100016A patent/GT200100016A/en unknown
- 2001-01-23 CN CN01804048A patent/CN1395578A/en active Pending
- 2001-01-23 EA EA200200643A patent/EA200200643A1/en unknown
- 2001-01-23 MX MXPA02007221A patent/MXPA02007221A/en not_active Application Discontinuation
- 2001-01-23 EE EEP200200405A patent/EE200200405A/en unknown
- 2001-01-23 YU YU50402A patent/YU50402A/en unknown
- 2001-01-23 CZ CZ20022475A patent/CZ20022475A3/en unknown
- 2001-01-23 OA OA1200200213A patent/OA12161A/en unknown
- 2001-01-23 JP JP2001561006A patent/JP4047010B2/en not_active Expired - Fee Related
- 2001-01-23 CA CA002397961A patent/CA2397961C/en not_active Expired - Fee Related
- 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
- 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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