申请人:AJINOMOTO CO. INC.
公开号:US20030162818A1
公开(公告)日:2003-08-28
This invention provides a novel acylsulfonamide derivative which can be used as an ACC activity inhibitor effective for the treatment of visceral fat syndrome that becomes the risk-factor of diseases of adult people such as myocardial infarction, cerebral infarction and diabetes.
Particularly, it relates to an acylsulfonamide derivative represented by a general formula 1
1
wherein R
1
is substituted/unsubstituted C
1
-C
12
alkyl or alkoxy group or substituted/unsubstituted C
2
-C
12
alkenyl or alkynyl group, R
2
is hydrogen atom, hydroxyl group, mercapto group, substituted/unsubstituted C
1
-C
6
alkoxy or alkylthio group, nitro group, halogen atom, trichloromethyl group, trifluoromethyl group or cyano group, R
3
is substituted/unsubstituted C
1
-C
20
alkyl or alkoxy group, substituted/unsubstituted C
2
-C
20
alkenyl or alkynyl group, substituted/unsubstituted aromatic hydrocarbon or aromatic heterocyclic group, substituted amino group, substituted/unsubstituted C
2
-C
20
alkenyloxy or alkynyloxy group or R
4
O— (wherein R
4
is substituted/unsubstituted aromatic hydrocarbon or aromatic heterocyclic group), Y is —CH═CH—, —N═CH—, —CH═N—, sulfur or oxygen, and ring A is aromatic hydrocarbon, aromatic heterocyclic ring or cyclic alkyl group.
本发明提供了一种新型的酰基磺酰胺衍生物,可用作有效的ACC活性抑制剂,用于治疗脂肪内脏综合征,该综合征成为成年人疾病的危险因素,如心肌梗死、脑梗死和糖尿病。特别地,它涉及到一种由通式11表示的酰基磺酰胺衍生物,其中R1是取代/未取代的C1-C12烷基或烷氧基或取代/未取代的C2-C12烯基或炔基,R2是氢原子、羟基、巯基、取代/未取代的C1-C6烷氧基或烷硫基、硝基、卤素原子、三氯甲基、三氟甲基或氰基,R3是取代/未取代的C1-C20烷基或烷氧基、取代/未取代的C2-C20烯基或炔基、取代/未取代的芳香族碳氢化合物或芳香族杂环基、取代的氨基、取代/未取代的C2-C20烯氧基或炔氧基或R4O-(其中R4是取代/未取代的芳香族碳氢化合物或芳香族杂环基),Y是-CH═CH-、-N═CH-、-CH═N-、硫或氧,环A是芳香族碳氢化合物、芳香族杂环环或环烷基。