公开(公告)号：US07964613B2

公开(公告)日：2011-06-21

申请号：US12071921

申请日：2008-02-27

申请人： Koki Matsubara ,  Atsushi Iesato ,  Akifumi Oomura ,  Koh Kawasaki ,  Rintaro Yamada ,  Minoru Seto

发明人： Koki Matsubara ,  Atsushi Iesato ,  Akifumi Oomura ,  Koh Kawasaki ,  Rintaro Yamada ,  Minoru Seto

IPC分类号： A01N43/42 ,  A01N43/00 ,  A61K31/47 ,  A61K31/00 ,  C07D217/00 ,  C07D217/22

CPC分类号： A61K31/55 ,  A61K31/47 ,  C07D401/12

摘要： 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; G1 represents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; G2 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; G3 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(R3)(R4)— (R3 and R4 represent hydrogen atom, or an alkyl group, or alkylene groups which combine together to form a saturated hydrocarbon ring group); G4 represents hydroxyl group (Y is a single group), or —N(R1)(R2) (R1 and R2 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); G5 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.

摘要翻译： 由式（1）表示的化合物[A表示含氮饱和环; m表示0〜2的整数。 n表示1〜4的整数， G1表示氢原子，氯原子，羟基，烷氧基或氨基; G 2表示卤素原子，羟基，氰基，羧基，烷基，烯基，炔基，烷氧基，烷硫基，氨基，烷基亚磺酰基，烷基磺酰基或芳基 组; G3表示氢原子，卤素原子，羟基，氰基，羧基，烷基，烯基，炔基，烷氧基，烷硫基，氨基，烷氧基羰基，酰基， 酰氧基，烷基亚磺酰基，烷基磺酰基或芳基; Y表示单键，或-C（R3）（R4） - （R3和R4表示氢原子，或烷基或结合在一起形成饱和烃环基的亚烷基）; G4表示羟基（Y为单一基团）或-N（R1）（R2）（R1和R2表示氢原子，烷基，芳烷基，烯基，炔基，饱和杂环基， 烷基磺酰基，酰基或脒基）; G5是A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，或其作为前体药物的衍生物，其有效抑制Rho激酶。

公开(公告)号：US20090048223A1

公开(公告)日：2009-02-19

申请号：US12071921

申请日：2008-02-27

申请人： Koki Matsubara ,  Atsushi Iesato ,  Akifumi Oomura ,  Koh Kawasaki ,  Rintaro Yamada ,  Minoru Seto

发明人： Koki Matsubara ,  Atsushi Iesato ,  Akifumi Oomura ,  Koh Kawasaki ,  Rintaro Yamada ,  Minoru Seto

IPC分类号： A61K31/397 ,  C07D401/14 ,  A61K31/4725 ,  C07D401/02 ,  A61K31/496 ,  A61K31/5377 ,  C07D413/14 ,  C07D487/02 ,  A61K31/5025

CPC分类号： A61K31/55 ,  A61K31/47 ,  C07D401/12

摘要： 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; G1 represents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; G2 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; G3 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(R3)(R4)— (R3 and R4 represent hydrogen atom, or an alkyl group, or alkylene groups which combine together to form a saturated hydrocarbon ring group); G4 represents hydroxyl group (Y is a single group), or —N(R1)(R2) (R1 and R2 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); G5 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.

摘要翻译： 由式（1）表示的化合物[A表示含氮饱和环; m表示0〜2的整数。 n表示1〜4的整数， G1表示氢原子，氯原子，羟基，烷氧基或氨基; G 2表示卤素原子，羟基，氰基，羧基，烷基，烯基，炔基，烷氧基，烷硫基，氨基，烷基亚磺酰基，烷基磺酰基或芳基 组; G3表示氢原子，卤素原子，羟基，氰基，羧基，烷基，烯基，炔基，烷氧基，烷硫基，氨基，烷氧基羰基，酰基， 酰氧基，烷基亚磺酰基，烷基磺酰基或芳基; Y表示单键，或-C（R3）（R4） - （R3和R4表示氢原子，或烷基或结合在一起形成饱和烃环基的亚烷基）; G4表示羟基（Y为单一基团）或-N（R1）（R2）（R1和R2表示氢原子，烷基，芳烷基，烯基，炔基，饱和杂环基， 烷基磺酰基，酰基或脒基）; G5是A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，或其作为前体药物的衍生物，其有效抑制Rho激酶。