BRPI0412259A - composto de 1h-pirazol 3,4-dissubstituìdos e seu uso como modulares de quinases dependentes de ciclina (cdk) e quinase-3 de sintase de glicogênio (gsk-3) - Google Patents

composto de 1h-pirazol 3,4-dissubstituìdos e seu uso como modulares de quinases dependentes de ciclina (cdk) e quinase-3 de sintase de glicogênio (gsk-3)

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Publication number
BRPI0412259A
BRPI0412259A BRPI0412259-3A BRPI0412259A BRPI0412259A BR PI0412259 A BRPI0412259 A BR PI0412259A BR PI0412259 A BRPI0412259 A BR PI0412259A BR PI0412259 A BRPI0412259 A BR PI0412259A
Authority
BR
Brazil
Prior art keywords
hydrogen
optionally substituted
alkoxy
group
halogen
Prior art date
Application number
BRPI0412259-3A
Other languages
English (en)
Inventor
Valerio Berdini
Michael Alistair O'brien
Maria Grazia Carr
Theresa Rachel Early
Adrian Liam Gill
Gary Trewartha
Alison Jo-Anne Woolford
Andrew James Woodhead
Paul Graham Wyatt
Original Assignee
Astex Therapeutics Ltd
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
Priority claimed from GBGB0317127.9A external-priority patent/GB0317127D0/en
Application filed by Astex Therapeutics Ltd filed Critical Astex Therapeutics Ltd
Publication of BRPI0412259A publication Critical patent/BRPI0412259A/pt
Publication of BRPI0412259B1 publication Critical patent/BRPI0412259B1/pt

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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Abstract

"COMPOSTOS DE 1H-PIRAZOL 3,4-DISSUBSTITUìDOS E SEU USO COMO MODULARES DE QUINASES DEPENDNETES DE CICLINA (CDK) E QUINASE-3 DE SINTASE DE GLICOGêNIO (GSK-3)". A invenção põe à disposição compostos da fórmula (0) ou sais ou tautómeros ou N-óxidos ou solvatos do mesmo para uso na profilaxia ou tratamento de estados de doença e afecções, tal como cânceres mediados por quinase dependente de ciclina e quinase-3 de sintase de glicogênio. Fórmula (0). Na fórmula (0): X é um grupo R¬ 1¬-A-NR¬ 4¬ ou um anel carbocíclico ou heterocíclico de 5 ou 6 membros; A é uma ligação, SO~ 2~, C=O, NR¬ 9¬(C=O) ou O(C=O), sendo que R¬ g¬ é hidrogênio ou C~ 1-4~-hidrocarbila, opcionalmente substituída por hidróxi OU C~ 1-4~-alcóxi; Y é uma ligação ou uma cadeia de alquileno com o comprimento de 1, 2 ou 3 átomos de carbono; R¬ 1¬ é hidrogênio; um grupo carbocíclico ou heterocíclico, com 3 a 12 membros anelares; ou um grupo C~ 1-8~-hidrocarbila, opcionalmente substituído por um ou mais substituintes escolhidos de halogênio (por exemplo, flúor), hidróxi, C~ 1-4~-hidrocarbilóxi, amino, mono- ou di-C~ 1-4~-hidrocarbilamino, e grupos carbocíclicos ou heterocíclicos, com 3 a 12 membros anelares, e sendo que 1 ou 2 dos átomos de carbono do grupo hidrocarbila podem estar opcionalmente substituídos por um átomo ou grupo escolhido de O, S, NH, SO, SO~ 2~; R¬ 2¬ é hidrogênio; halogênio, C~ 1-4~-alcóxi (por exemplo, metóxi); ou um grupo C~ 1-4~-hidrocarbila, opcionalmente substituído por halogênio (por exemplo, flúor), hidroxila ou C~ 1-4~-alcóxi (por exemplo, metóxi); R¬ 3¬ é escolhido de hidrogênio e grupos carbocíclicos e heterocíclicos, com 3 a 12 membros anelares; e R¬ 4¬ é hidrogênio ou um g rupo C~ 1-4~-hidrocarbila, opcionalmente substituído por halogênio (por exemplo, flúor), hidroxila ou C~ 1-4~-alcóxi (por exemplo, metóxi).
BRPI0412259-3A 2003-07-22 2004-07-22 Compostos de 1H-pirazol 3,4-dissubstituídos como moduladores de quinases dependentes de ciclina (CDK), seus usos, processo para a preparação dos mesmos e composição farmacêutica BRPI0412259B1 (pt)

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US56976304P 2004-05-10 2004-05-10
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PCT/GB2004/003179 WO2005012256A1 (en) 2003-07-22 2004-07-22 3, 4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators

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