申请人:Matsubara Koki
公开号:US20090048223A1
公开(公告)日:2009-02-19
A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G
1
represents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; G
2
represents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; G
3
represents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkoxycarbonyl group, an acyl group, an acyloxy group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; Y represents a single bond, or —C(R
3
)(R
4
)— (R
3
and R
4
represent hydrogen atom, or an alkyl group, or alkylene groups which combine together to form a saturated hydrocarbon ring group); G
4
represents hydroxyl group (Y is a single group), or —N(R
1
)(R
2
) (R
1
and R
2
represent hydrogen atom, an alkyl group, an aralkyl group, an alkenyl group, an alkynyl group, a saturated heterocyclic group, an alkylsulfonyl group, an acyl group, or an amidino group); G
5
is a substituent on a ring-constituting carbon atom of A, and represents hydrogen atom, fluorine atom, or an alkyl group] or a salt thereof, or a derivative thereof that is a prodrug, which potently inhibits Rho kinase.
一种化合物,其化学式为(1)[其中A代表含氮饱和环;m代表0至2的整数;n代表1至4的整数;G1代表氢原子、氯原子、羟基、烷氧基或氨基;G2代表卤素原子、羟基、氰基、羧基、烷基、烯基、炔基、烷氧基、烷硫基、氨基、烷氧羰基、酰基、酰氧基、烷基亚磺酰基、烷基磺酰基或芳基;G3代表氢原子、卤素原子、羟基、氰基、羧基、烷基、烯基、炔基、烷氧基、烷硫基、氨基、烷氧羰基、酰基、酰氧基、烷基亚磺酰基、烷基磺酰基或芳基;Y代表单键或- C(R3)(R4)-(R3和R4代表氢原子或烷基,或结合形成饱和碳氢化合物环基的烷基烯基);G4代表羟基(Y为单键)或- N(R1)(R2)(R1和R2代表氢原子、烷基、芳基烷基、烯基、炔基、饱和杂环基、烷基磺酰基、酰基或酰胺基);G5是A环上的环构成碳原子上的取代基,代表氢原子、氟原子或烷基]或其盐或是一种前药衍生物,能够有效抑制Rho激酶。