BRPI0407381A - 4-aminopirimidino-5-ona - Google Patents
4-aminopirimidino-5-onaInfo
- Publication number
- BRPI0407381A BRPI0407381A BR0407381-9A BRPI0407381A BRPI0407381A BR PI0407381 A BRPI0407381 A BR PI0407381A BR PI0407381 A BRPI0407381 A BR PI0407381A BR PI0407381 A BRPI0407381 A BR PI0407381A
- Authority
- BR
- Brazil
- Prior art keywords
- aminopyrimidine
- compounds
- preparation
- cancer
- cyclin
- Prior art date
Links
- WYPGFVLAEWKLCO-UHFFFAOYSA-N 4-amino-4h-pyrimidin-5-one Chemical compound NC1N=CN=CC1=O WYPGFVLAEWKLCO-UHFFFAOYSA-N 0.000 title abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000013701 Cyclin-Dependent Kinase 4 Human genes 0.000 abstract 2
- 108010025464 Cyclin-Dependent Kinase 4 Proteins 0.000 abstract 2
- 201000011510 cancer Diseases 0.000 abstract 2
- 108091007914 CDKs Proteins 0.000 abstract 1
- 102000003903 Cyclin-dependent kinases Human genes 0.000 abstract 1
- 108090000266 Cyclin-dependent kinases Proteins 0.000 abstract 1
- 230000001028 anti-proliverative effect Effects 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- 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
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
4-AMINOPIRIMIDINO-5-ONA. Novos derivados 4-aminopirimidino-5-onas da formula I, em que R¬ 1¬ e R¬ 2¬ são como definidos no relatório descritivo, são como definidos no relatório descritivo, são revelados. Estes compostos inibem cinases ciclina-dependentes. em particular cinase ciclina-dependente 4 (Cdk4). Estes compostos e seus sais e ésteres farmaceuticamente aceitáveis têm atividade antiproliferativas e são úteis no tratamento ou controle de câncer, em particular tumores sólidos. Esta invenção é também direcionada às composições farmacêuticas contendo tais compostos, seus usos para tratar ou controlar câncer, a um processo de sua preparação e aos intermediários úteis em sua preparação.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US44627303P | 2003-02-10 | 2003-02-10 | |
| US51492603P | 2003-10-28 | 2003-10-28 | |
| PCT/EP2004/000971 WO2004069139A2 (en) | 2003-02-10 | 2004-02-03 | 4-aminopyrimidin-5-yl-methanone derivatives for inhibition of cdk4 activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0407381A true BRPI0407381A (pt) | 2006-02-07 |
Family
ID=32853425
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0407381-9A BRPI0407381A (pt) | 2003-02-10 | 2004-02-03 | 4-aminopirimidino-5-ona |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US7157455B2 (pt) |
| EP (1) | EP1628619A2 (pt) |
| JP (1) | JP2006523183A (pt) |
| KR (1) | KR100717099B1 (pt) |
| AR (1) | AR043693A1 (pt) |
| AU (1) | AU2004210408A1 (pt) |
| BR (1) | BRPI0407381A (pt) |
| CA (1) | CA2512915A1 (pt) |
| CL (1) | CL2004000226A1 (pt) |
| EA (1) | EA009412B1 (pt) |
| EC (1) | ECSP055958A (pt) |
| HR (1) | HRP20050689A2 (pt) |
| IL (1) | IL169626A0 (pt) |
| MA (1) | MA27716A1 (pt) |
| MX (1) | MXPA05008333A (pt) |
| MY (1) | MY137555A (pt) |
| NO (1) | NO20053410L (pt) |
| PL (1) | PL382309A1 (pt) |
| RS (1) | RS20050610A (pt) |
| TN (1) | TNSN05188A1 (pt) |
| TW (1) | TWI293881B (pt) |
| WO (1) | WO2004069139A2 (pt) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7211576B2 (en) * | 2004-04-20 | 2007-05-01 | Hoffmann-La Roche Inc. | Diaminothiazoles |
| US7405220B2 (en) | 2004-06-09 | 2008-07-29 | Hoffmann-La Roche Inc. | Pyrazolopyrimidines |
| EP1726953B1 (en) * | 2005-05-25 | 2008-08-20 | F. Hoffmann-La Roche Ag | Biomarker for response monitoring of CDK inhibitors in the clinic |
| US7705009B2 (en) * | 2005-11-22 | 2010-04-27 | Hoffman-La Roche Inc. | 4-aminopyrimidine-5-thione derivatives |
| CN101316823B (zh) | 2005-12-01 | 2013-05-22 | 霍夫曼-拉罗奇有限公司 | 用作抗癌剂的作为p53和MDM2蛋白之间相互作用的抑制剂的2,4,5-三苯基咪唑啉衍生物 |
| WO2007113005A2 (en) * | 2006-04-03 | 2007-10-11 | European Molecular Biology Laboratory (Embl) | 2-substituted 3-aminosulfonyl-thiophene derivatives as aurora kinase inhibitors |
| WO2010019967A1 (en) * | 2008-08-15 | 2010-02-18 | Georgetown University | Fluorescent cdk inhibitors for treatment of cancer |
| AR081626A1 (es) | 2010-04-23 | 2012-10-10 | Cytokinetics Inc | Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos |
| AR081331A1 (es) | 2010-04-23 | 2012-08-08 | Cytokinetics Inc | Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos |
| US9133123B2 (en) | 2010-04-23 | 2015-09-15 | Cytokinetics, Inc. | Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use |
| SG11201610476VA (en) * | 2014-07-01 | 2017-01-27 | Millennium Pharm Inc | Heteroaryl compounds useful as inhibitors of sumo activating enzyme |
| JP7538153B2 (ja) * | 2019-06-06 | 2024-08-21 | ベイジン タイド ファーマシューティカル カンパニー リミテッド | Ｐ２ｘ３及び／又はｐ２ｘ２／３受容体アンタゴニスト、それを含む医薬組成物及びその使用 |
| CA3207392A1 (en) * | 2021-02-05 | 2022-08-11 | Xiaoxia Yan | Cdk inhibitor |
| IL319771A (en) * | 2022-09-22 | 2025-05-01 | Joint Stock Company «Biocad» | Cyclin-dependent kinase 7 inhibitors |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9012592D0 (en) | 1990-06-06 | 1990-07-25 | Smithkline Beecham Intercredit | Compounds |
| ES2301194T3 (es) * | 1997-02-05 | 2008-06-16 | Warner-Lambert Company Llc | Pirido 2,3-d pirimidinas y 4-aminopirimidinas como inhibidores de la proliferacion celular. |
| NZ503788A (en) | 1997-10-27 | 2002-11-26 | Agouron Pharma | 4-aminothiazole derivatives and their use as inhibitors of cyclin-dependent kinases |
| US6262096B1 (en) | 1997-11-12 | 2001-07-17 | Bristol-Myers Squibb Company | Aminothiazole inhibitors of cyclin dependent kinases |
| BR9908004A (pt) | 1998-02-17 | 2001-12-18 | Tularik Inc | Composto, composição e método para prevençãoou supressão de uma infecção viral |
| ES2274634T3 (es) | 1998-08-29 | 2007-05-16 | Astrazeneca Ab | Compuestos de pirimidina. |
| GB9828511D0 (en) | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| EP1409487A1 (en) | 1999-09-15 | 2004-04-21 | Warner-Lambert Company Llc | Pteridinones as kinase inhibitors |
| CA2386955A1 (en) | 1999-11-22 | 2001-05-31 | Warner-Lambert Company | Quinazolines and their use for inhibiting cyclin-dependent kinase enzymes |
| CZ20022475A3 (cs) * | 2000-01-25 | 2003-03-12 | Warner-Lambert Company | Pyrido[2,3-d]pyrimidin-2,7-diaminové inhibitory kinázy |
| KR20020070520A (ko) * | 2000-01-27 | 2002-09-09 | 워너-램버트 캄파니 | 신경퇴행성 질병의 치료를 위한 피리도피리미디논 유도체 |
| GB0004888D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004887D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004886D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| JP2004501083A (ja) | 2000-04-18 | 2004-01-15 | アゴーロン・ファーマシューティカルズ・インコーポレイテッド | プロテインキナーゼを阻害するためのピラゾール |
| EP1317450B1 (en) * | 2000-09-15 | 2006-11-22 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| NZ526472A (en) * | 2000-12-21 | 2004-04-30 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors |
| KR100874791B1 (ko) | 2001-05-29 | 2008-12-18 | 바이엘 쉐링 파마 악티엔게젤샤프트 | Ｃｄｋ-억제 피리미딘, 그의 제조방법 및 약제로서의 용도 |
| US7288547B2 (en) | 2002-03-11 | 2007-10-30 | Schering Ag | CDK-inhibitory 2-heteroaryl-pyrimidines, their production and use as pharmaceutical agents |
| BR0316680A (pt) | 2002-11-28 | 2005-10-18 | Schering Ag | Pirimidinas inibidoras de chk, pdk e akt, sua produção e uso como agentes farmacêuticos |
| BRPI0407174A (pt) | 2003-02-10 | 2006-02-07 | Pfizer | Regime de administração para nelfinavir |
| JP4828405B2 (ja) * | 2003-02-10 | 2011-11-30 | バイエル・シェーリング・ファルマ・アクチェンゲゼルシャフト | 呼吸器官の細菌性疾患の処置 |
| DE10349423A1 (de) | 2003-10-16 | 2005-06-16 | Schering Ag | Sulfoximinsubstituierte Parimidine als CDK- und/oder VEGF-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel |
-
2004
- 2004-02-02 US US10/770,379 patent/US7157455B2/en not_active Expired - Fee Related
- 2004-02-03 EA EA200501233A patent/EA009412B1/ru not_active IP Right Cessation
- 2004-02-03 BR BR0407381-9A patent/BRPI0407381A/pt not_active IP Right Cessation
- 2004-02-03 HR HR20050689A patent/HRP20050689A2/xx not_active Application Discontinuation
- 2004-02-03 PL PL382309A patent/PL382309A1/pl not_active Application Discontinuation
- 2004-02-03 WO PCT/EP2004/000971 patent/WO2004069139A2/en not_active Ceased
- 2004-02-03 RS YUP-2005/0610A patent/RS20050610A/sr unknown
- 2004-02-03 EP EP04707513A patent/EP1628619A2/en not_active Withdrawn
- 2004-02-03 MX MXPA05008333A patent/MXPA05008333A/es active IP Right Grant
- 2004-02-03 CA CA002512915A patent/CA2512915A1/en not_active Abandoned
- 2004-02-03 JP JP2006500021A patent/JP2006523183A/ja active Pending
- 2004-02-03 AU AU2004210408A patent/AU2004210408A1/en not_active Abandoned
- 2004-02-03 KR KR1020057014717A patent/KR100717099B1/ko not_active Expired - Fee Related
- 2004-02-06 MY MYPI20040366A patent/MY137555A/en unknown
- 2004-02-06 TW TW093102771A patent/TWI293881B/zh active
- 2004-02-06 AR ARP040100381A patent/AR043693A1/es not_active Application Discontinuation
- 2004-02-09 CL CL200400226A patent/CL2004000226A1/es unknown
-
2005
- 2005-07-11 IL IL169626A patent/IL169626A0/en unknown
- 2005-07-13 NO NO20053410A patent/NO20053410L/no not_active Application Discontinuation
- 2005-08-02 TN TNP2005000188A patent/TNSN05188A1/en unknown
- 2005-08-09 EC EC2005005958A patent/ECSP055958A/es unknown
- 2005-08-30 MA MA28472A patent/MA27716A1/fr unknown
-
2006
- 2006-06-20 US US11/471,001 patent/US7615634B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| AU2004210408A1 (en) | 2004-08-19 |
| WO2004069139A2 (en) | 2004-08-19 |
| TW200423940A (en) | 2004-11-16 |
| EP1628619A2 (en) | 2006-03-01 |
| US20060229330A1 (en) | 2006-10-12 |
| JP2006523183A (ja) | 2006-10-12 |
| MXPA05008333A (es) | 2005-09-30 |
| CA2512915A1 (en) | 2004-08-19 |
| KR100717099B1 (ko) | 2007-05-10 |
| US7615634B2 (en) | 2009-11-10 |
| EA200501233A1 (ru) | 2006-04-28 |
| MY137555A (en) | 2009-02-27 |
| WO2004069139A3 (en) | 2007-04-26 |
| HRP20050689A2 (hr) | 2006-08-31 |
| TWI293881B (en) | 2008-03-01 |
| IL169626A0 (en) | 2007-07-04 |
| RS20050610A (sr) | 2007-12-31 |
| ECSP055958A (es) | 2006-01-16 |
| MA27716A1 (fr) | 2006-01-02 |
| NO20053410L (no) | 2005-09-08 |
| PL382309A1 (pl) | 2007-08-20 |
| US7157455B2 (en) | 2007-01-02 |
| TNSN05188A1 (en) | 2007-06-11 |
| AR043693A1 (es) | 2005-08-10 |
| US20040162303A1 (en) | 2004-08-19 |
| CL2004000226A1 (es) | 2005-01-14 |
| EA009412B1 (ru) | 2007-12-28 |
| KR20050099544A (ko) | 2005-10-13 |
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