CO5261549A1 - PIRIDO [2,3-d] PIRIMIDIN-2,7-DIAMINES INHIBITORS OF KINASES - Google Patents
PIRIDO [2,3-d] PIRIMIDIN-2,7-DIAMINES INHIBITORS OF KINASESInfo
- Publication number
- CO5261549A1 CO5261549A1 CO01005268A CO01005268A CO5261549A1 CO 5261549 A1 CO5261549 A1 CO 5261549A1 CO 01005268 A CO01005268 A CO 01005268A CO 01005268 A CO01005268 A CO 01005268A CO 5261549 A1 CO5261549 A1 CO 5261549A1
- Authority
- CO
- Colombia
- Prior art keywords
- substituted
- unsubstituted lower
- compounds
- group
- unsubstituted
- Prior art date
Links
- 108091000080 Phosphotransferase Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 102000020233 phosphotransferase Human genes 0.000 title abstract 2
- 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
- 101150020251 NR13 gene Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 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
- 230000003389 potentiating effect Effects 0.000 abstract 1
- 230000002062 proliferating effect Effects 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)
- 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
Se describen compuestos de fórmula: <EMI FILE="01005268_1" ID="1" IMF=JPEG >en la cual : R2, R7. R13, R14 y R15 son, independientemente, hidrógeno o alquilo inferior sustituido o sin sustituir, alquenilo inferior sustituido o sin sustituir, alquinilo inferior sustituido o sin sustituir, o bien -(CH2)nR12 sustituido o sin sustituir; R5 es halógeno, ciano, nitro, -R9, -NR9R10, o bien -OR9; R6 es halógeno, ciano, nitro, -R9, -NR9R10, -OR9, -C02R9, -COR9, -CONR9R10, NR9COR10, alquenilo inferior sustituido o sin sustituir, o alquinilo inferior sustituido o sin sustituir; R8 es -CO2R13, -COR13, -CINR13R14, -CSNR13R14, -C(NR13)NR14R15, -SO3R13, -SO2R13, -SO2NR13R14, -PO3R13R14, POR13R14, -PO(NR13R14)2; R9 Y R10 son, independientemente, hidrógeno o alquilo inferior sustituido o sin sustituir; R11 es un grupo heteroarilo o un grupo heterocíclico; R12 es un grupo cicloalquilo, un grupo heterociclico, un grupo arilo, o un grupo heteroarilo; y n vale 0, 1, 2 ó 3. Estos compuestos y sus composiciones farmacéuticas son útiles para tratar trastornos proliferativos celulares, tales como cáncer y restenosis. Estos compuestos son potentes inhibidores de cdks y de cinasas mediadas por factor de crecimiento.Compounds of formula are described: <EMI FILE = "01005268_1" ID = "1" IMF = JPEG> in which: R2, R7. R13, R14 and R15 are, independently, hydrogen or substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkynyl, or - (CH2) nR12 substituted or unsubstituted; R5 is halogen, cyano, nitro, -R9, -NR9R10, or -OR9; R6 is halogen, cyano, nitro, -R9, -NR9R10, -OR9, -C02R9, -COR9, -CONR9R10, NR9COR10, substituted or unsubstituted lower alkenyl, or substituted or unsubstituted lower alkynyl; R8 is -CO2R13, -COR13, -CINR13R14, -CSNR13R14, -C (NR13) NR14R15, -SO3R13, -SO2R13, -SO2NR13R14, -PO3R13R14, POR13R14, -PO (NR13R14) 2; R9 and R10 are, independently, hydrogen or substituted or unsubstituted lower alkyl; R11 is a heteroaryl group or a heterocyclic group; R12 is a cycloalkyl group, a heterocyclic group, an aryl group, or a heteroaryl group; and not worth 0, 1, 2 or 3. These compounds and their pharmaceutical compositions are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cdks and growth factor-mediated kinases.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17826100P | 2000-01-25 | 2000-01-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5261549A1 true CO5261549A1 (en) | 2003-03-31 |
Family
ID=22651853
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO01005268A CO5261549A1 (en) | 2000-01-25 | 2001-01-24 | PIRIDO [2,3-d] PIRIMIDIN-2,7-DIAMINES INHIBITORS OF KINASES |
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 |
| JP4524072B2 (en) | 2000-10-23 | 2010-08-11 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | New compounds |
| PE20030008A1 (en) * | 2001-06-19 | 2003-01-22 | Bristol Myers Squibb Co | DUAL INHIBITORS OF PDE 7 AND PDE 4 |
| DE60315826T2 (en) | 2002-04-19 | 2008-05-21 | Smithkline Beecham Corp. | NEW CONNECTIONS |
| 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 |
| WO2006032452A1 (en) * | 2004-09-21 | 2006-03-30 | F. Hoffmann-La Roche Ag | 6-(2-alkyl-phenyl) - pyrido[2,3-d] pyrimidines useful as proteine kinase inhibitors |
| US20090137550A1 (en) | 2005-03-25 | 2009-05-28 | Glaxo Group Limited | Novel Compounds |
| 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 |
| TW200724142A (en) | 2005-03-25 | 2007-07-01 | Glaxo Group Ltd | Novel compounds |
| KR20080002865A (en) | 2005-03-25 | 2008-01-04 | 글락소 그룹 리미티드 | 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 |
| ATE449097T1 (en) * | 2005-07-21 | 2009-12-15 | Hoffmann La Roche | PYRIDOÄ2,3-DÜPYRIMIDINE-2,4-DIAMINE COMPOUNDS AS PTPIB INHIBITORS |
| JP2009504665A (en) | 2005-08-09 | 2009-02-05 | アイアールエム・リミテッド・ライアビリティ・カンパニー | Compounds and compositions as protein kinase inhibitors |
| 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 |
| 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 |
| 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 | 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 |
|---|---|---|---|---|
| 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 |
| AU763839B2 (en) * | 1998-05-26 | 2003-07-31 | Warner-Lambert Company | 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 YU YU50402A patent/YU50402A/en unknown
- 2001-01-23 EP EP01900591A patent/EP1254137A1/en not_active Withdrawn
- 2001-01-23 IL IL15054501A patent/IL150545A0/en unknown
- 2001-01-23 CN CN01804048A patent/CN1395578A/en active Pending
- 2001-01-23 CZ CZ20022475A patent/CZ20022475A3/en unknown
- 2001-01-23 WO PCT/IB2001/000069 patent/WO2001055147A1/en not_active Application Discontinuation
- 2001-01-23 JP JP2001561006A patent/JP4047010B2/en not_active Expired - Fee Related
- 2001-01-23 HU HU0204141A patent/HUP0204141A3/en unknown
- 2001-01-23 KR KR1020027009516A patent/KR20020065939A/en not_active Application Discontinuation
- 2001-01-23 MX MXPA02007221A patent/MXPA02007221A/en not_active Application Discontinuation
- 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 CA CA002397961A patent/CA2397961C/en not_active Expired - Fee Related
- 2001-01-23 AP APAP/P/2002/002586A patent/AP2002002586A0/en unknown
- 2001-01-23 EE EEP200200405A patent/EE200200405A/en unknown
- 2001-01-23 OA OA1200200213A patent/OA12161A/en unknown
- 2001-01-23 EA EA200200643A patent/EA200200643A1/en unknown
- 2001-01-23 PA PA20018510701A patent/PA8510701A1/en unknown
- 2001-01-23 GT GT200100016A patent/GT200100016A/en unknown
- 2001-01-23 PE PE2001000072A patent/PE20011066A1/en not_active Application Discontinuation
- 2001-01-23 DZ DZ013266A patent/DZ3266A1/en active
- 2001-01-23 BR BR0107751-1A patent/BR0107751A/en not_active IP Right Cessation
- 2001-01-23 SK SK1063-2002A patent/SK10632002A3/en not_active Application Discontinuation
- 2001-01-24 TN TNTNSN01014A patent/TNSN01014A1/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
-
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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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Application refused |