3,4-Disubstituted 1H-pyrazole compounds as cyclin-dependent kinase (CDK) modulators, their uses, process for their preparation and pharmaceutical composition
Adrian Liam Gill,Alison Jo-Anne Woolford,Andrew James Woodhead,Gary Trewartha,Maria Grazia Carr,Michael Alistair O'Brien,Paul Graham Wyatt,Theresa Rachel Early,Valerio Berdini
申请号：
BRPI0412259
公开号：
BRPI0412259B1
申请日:
2004.07.22
申请国别(地区):
BR
年份:
2019
代理人:
摘要：
"3,4-disubstituted 1h-pyrazole compounds and their use as modulators of cyclin-dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3)". The invention provides compounds of formula (O) or salts or tautomers or n-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and disorders, such as cyclin-dependent kinase-3 kinase-mediated cancers. glycogen synthase. formula (0). in formula (0): x is a group R 5 is -a-nr 4 R 4 or a 5 or 6 membered carbocyclic or heterocyclic ring； a is a bond, so ~ 2 ~, c = 0, nr ^ 9 ^ (c = o) or o (c = o), where r ^ g ^ is hydrogen or c 1-4-hydrocarbyl, optionally substituted by hydroxy or C1-4-alkoxy； y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length； R2 is hydrogen； a carbocyclic or heterocyclic group having from 3 to 12 ring members； or a C1-8-hydrocarbyl group, optionally substituted by one or more substituents chosen from halogen (e.g. fluorine), hydroxy, C1-4-hydrocarboxy, amino, mono- or di-C1- -4-hydrocarbylamino, and carbocyclic or heterocyclic groups having 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may be optionally substituted by an atom or group chosen from o, s, nh, s , s0 ~ 2 ~； R2 is hydrogen； halogen, C1-4 alkoxy (e.g. methoxy)； or a C1-4-hydrocarbyl group, optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy)； R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members； and R4 is hydrogen or a C1-4-hydrocarbyl group, optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4-alkoxy (e.g. methoxy). "3,4-disubstituted 1h-pyrazole compounds and their use as modulators of cyclin-dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3)". The invention provides compounds of formula (O) or salts or tautomers or n-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and disorders, such as cyclin-dependent kinase
