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    • 8. 发明授权
    • Pyrazole compounds
    • 吡唑化合物
    • US07612201B2
    • 2009-11-03
    • US10536899
    • 2003-12-18
    • Mandy Christine BeswickMartin James DrysdaleBrian William DymockEdward McDonald
    • Mandy Christine BeswickMartin James DrysdaleBrian William DymockEdward McDonald
    • C07D231/38C07D401/04C07D403/04C07D405/12C07D409/12C07D417/12
    • C07D231/38A61K31/415C07D401/04C07D401/12C07D403/04C07D403/12C07D405/10C07D405/12C07D409/12C07D413/12C07D417/12
    • Compounds of formula (IA) or (IB) or a salt, N-oxide, hydrate or solvate thereof are inhibitors of HSP90, and are of value in the treatment of diseases responsive to HSP90 inhibition such as cancers. In the formulae, Ar is an aryl, aryl(C1-C6 alkyl), aryl(C1-C6 alkyl), heteroaryl, heteroarylaryl(C1-C6 alkyl), or heteroarylaryl(C1-C6 alkyl) group, any of which being optionally substituted in the aryl or heteroaryl part thereof; R1, is hydrogen or optionally substituted C1-C6 alkyl; R2 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide or carboxyl ester group; and ring A is a non aromatic carbocyclic or heterocyclic ring wherein (i) a ring carbon is optionally substituted, and/or (ii) a ring nitrogen is optionally substituted by a group of formula -(Alk1)p (Cyc)n-(Alk3)m-(Z)r (Alk2)s Q where Alk1, Alk2 and Alk3 are optionally substituted C1-C3 alkyl, Cyc is an optionally substituted carbocyclic or heterocyclic radical; m, n, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C═O)—, —S02-, —C(═O)O—, —OC(═O)—, —NW—, —C(═O)NRA-, —NRAC(═O)—, —SO2NRA—, or —NRASO2— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical.
    • 式(IA)或(IB)化合物或其盐,N-氧化物,水合物或溶剂合物是HSP90的抑制剂,并且在治疗对HSP90抑制作用的疾病如癌症的治疗中具有价值。 在式中,Ar是芳基,(C 1 -C 6烷基),芳基(C 1 -C 6烷基),杂芳基,杂芳基芳基(C 1 -C 6烷基)或杂芳基芳基(C 1 -C 6烷基) 在其芳基或杂芳基部分取代; R1是氢或任选取代的C 1 -C 6烷基; R 2是氢,任选取代的环烷基,环烯基,C 1 -C 6烷基,C 1 -C 6烯基或C 1 -C 6炔基; 或羧基,羧酰胺或羧基酯基团; 环A是非芳族碳环或杂环,其中(i)环碳任选被取代,和/或(ii)环氮任选地被式 - (Alk1)p(Cyc)n-( Alk3)m-(Z)r(Alk2)sQ其中Alk1,Alk2和Alk3是任选取代的C 1 -C 3烷基,Cyc是任选取代的碳环或杂环基; m,n,p,r和s独立地为0或1,Z为-O - , - S - , - (CO) - , - SO2-,-C - ,-NW-, - C( - O)NRA - , - NRAC(-O) - , - SO2NRA-或-NRASO2-,其中RA是氢或C1-C6烷基,Q是氢或任选取代的碳环 或杂环基。