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EA200501233A1 - 4-аминопиримидин-5-он - Google Patents

4-аминопиримидин-5-он

Info

Publication number
EA200501233A1
EA200501233A1 EA200501233A EA200501233A EA200501233A1 EA 200501233 A1 EA200501233 A1 EA 200501233A1 EA 200501233 A EA200501233 A EA 200501233A EA 200501233 A EA200501233 A EA 200501233A EA 200501233 A1 EA200501233 A1 EA 200501233A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
treating
preparation
useful
cyclin
Prior art date
Application number
EA200501233A
Other languages
English (en)
Other versions
EA009412B1 (ru
Inventor
Дейвид Джозеф Барковиц
Синьцзи Чу
Цинцзи Дин
Нань Цан
Аллен Джон Лови
Джон Антони Молитерни
Джон Гилфойл Джр. Маллин
Бин Тан Ву
Питер Майкл Вовкулич
Original Assignee
Ф.Хоффманн-Ля Рош Аг
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ф.Хоффманн-Ля Рош Аг filed Critical Ф.Хоффманн-Ля Рош Аг
Publication of EA200501233A1 publication Critical patent/EA200501233A1/ru
Publication of EA009412B1 publication Critical patent/EA009412B1/ru

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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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (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

Описаны новые производные 4-аминопиримидин-5-она формулыгде Rи Rявляются такими, как определено в описании. Эти соединения ингибируют циклинзависимые киназы, в частности циклинзависимую киназу 4 (Cdk4). Эти соединения и их фармацевтически приемлемые соли и эфиры обладают антипролиферативной активностью и являются полезными для лечения или контроля рака, в частности, твердых опухолей. Данное изобретение также относится к фармацевтическим композициям, содержащим такие соединения, их применению для лечения или контроля рака, к способу их получения и к промежуточным соединениям, полезным для их получения.
EA200501233A 2003-02-10 2004-02-03 Производные 4-аминопиримидин-5-она, способ их получения и применение EA009412B1 (ru)

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 (2)

Publication Number Publication Date
EA200501233A1 true EA200501233A1 (ru) 2006-04-28
EA009412B1 EA009412B1 (ru) 2007-12-28

Family

ID=32853425

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200501233A EA009412B1 (ru) 2003-02-10 2004-02-03 Производные 4-аминопиримидин-5-она, способ их получения и применение

Country Status (22)

Country Link
US (2) US7157455B2 (ru)
EP (1) EP1628619A2 (ru)
JP (1) JP2006523183A (ru)
KR (1) KR100717099B1 (ru)
AR (1) AR043693A1 (ru)
AU (1) AU2004210408A1 (ru)
BR (1) BRPI0407381A (ru)
CA (1) CA2512915A1 (ru)
CL (1) CL2004000226A1 (ru)
EA (1) EA009412B1 (ru)
EC (1) ECSP055958A (ru)
HR (1) HRP20050689A2 (ru)
IL (1) IL169626A0 (ru)
MA (1) MA27716A1 (ru)
MX (1) MXPA05008333A (ru)
MY (1) MY137555A (ru)
NO (1) NO20053410L (ru)
PL (1) PL382309A1 (ru)
RS (1) RS20050610A (ru)
TN (1) TNSN05188A1 (ru)
TW (1) TWI293881B (ru)
WO (1) WO2004069139A2 (ru)

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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
ES2538714T3 (es) 2005-12-01 2015-06-23 F. Hoffmann-La Roche Ag Derivados de 2,4,5-trifenil-imidazolina como inhibidores de la interacción entre las proteínas p53 y MDM2 para el uso en calidad de agentes anticancerosos
WO2007113005A2 (en) * 2006-04-03 2007-10-11 European Molecular Biology Laboratory (Embl) 2-substituted 3-aminosulfonyl-thiophene derivatives as aurora kinase inhibitors
US9408848B2 (en) 2008-08-15 2016-08-09 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
WO2011133920A1 (en) 2010-04-23 2011-10-27 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
DK3164130T3 (da) * 2014-07-01 2019-10-28 Millennium Pharm Inc Heteroaryle forbindelser anvendelige som inhibatorer af sumo-aktiverende enzym
KR20220016909A (ko) 2019-06-06 2022-02-10 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 P2x3 및/또는 p2x2/3 수용체 길항제, 이를 함유하는 약학적 조성물 및 이의 용도
KR20230142504A (ko) * 2021-02-05 2023-10-11 상하이 치루 파마슈티컬 리서치 앤 디벨롭먼트 센터 리미티드 Cdk 억제제
WO2024063670A1 (ru) * 2022-09-22 2024-03-28 Акционерное общество "БИОКАД" Ингибиторы циклинзависимой киназы 7

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Also Published As

Publication number Publication date
WO2004069139A2 (en) 2004-08-19
WO2004069139A3 (en) 2007-04-26
US7615634B2 (en) 2009-11-10
TW200423940A (en) 2004-11-16
MY137555A (en) 2009-02-27
CL2004000226A1 (es) 2005-01-14
TNSN05188A1 (en) 2007-06-11
HRP20050689A2 (en) 2006-08-31
CA2512915A1 (en) 2004-08-19
AU2004210408A1 (en) 2004-08-19
AR043693A1 (es) 2005-08-10
EA009412B1 (ru) 2007-12-28
TWI293881B (en) 2008-03-01
KR100717099B1 (ko) 2007-05-10
BRPI0407381A (pt) 2006-02-07
ECSP055958A (es) 2006-01-16
KR20050099544A (ko) 2005-10-13
US7157455B2 (en) 2007-01-02
EP1628619A2 (en) 2006-03-01
JP2006523183A (ja) 2006-10-12
RS20050610A (en) 2007-12-31
IL169626A0 (en) 2007-07-04
US20060229330A1 (en) 2006-10-12
NO20053410L (no) 2005-09-08
PL382309A1 (pl) 2007-08-20
MA27716A1 (fr) 2006-01-02
MXPA05008333A (es) 2005-09-30
US20040162303A1 (en) 2004-08-19

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Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU