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Invention Publication
CN1842532A 嘧啶并噻吩化合物 失效 - 权利终止 转让

嘧啶并噻吩化合物
Abstract:
式(I)的化合物是体外或体内HSP90活性抑制剂，其尤其用于治疗癌症其中，R2是式－(Ar1)m－(Alk1)p－(Z)r－(Alk2)s－Q的基团，其中，Ar1是任选取代的芳基或杂芳基，Alk1和Alk2是任选取代的二价C1－C3亚烷基或C2－C3亚烯基，m、p、r和s独立为0或1，Z是－O－、－S－、－(C＝O)－、－(C＝S)－、－SO2－、－C(＝O)O－、－C(＝O)NRA－、－C(＝S)NRA－、－SO2NRA－、－NRAC(＝O)－、－NRASO2－或－NRA－，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；R3是氢、任选取代基或任选取代的(C1－C6)烷基、芳基或杂芳基；且R4是羧酸酯、羧酰胺或磺酰胺基。
Abstract(English):

Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of cancer: wherein R2 is a group of formula -(Ar<1>)m-(Alk<1>)P-(Z)r-(Alk2)S-Q wherein Ar<1> is an optionally substituted aryl or heteroaryl radical, Alk' and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is -0-, -S-, -(C=O)-, -(C=S)-, -S02-, -C(=O)O-, -C(=O) NR - , -C(=S)NR -, -S02NR -, -NR C(=O)_, -NR S02- or-NR -wherein R is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.

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