申请人:Ajinomoto Co., Inc.
公开号:US06555584B1
公开(公告)日:2003-04-29
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
wherein R1 is substituted/unsubstituted C2-C12 alkyl or alkoxy group or substituted/unsubstituted C2-C12 alkenyl or alkynyl group, R2 is hydrogen atom, hydroxyl group, mercapto group, substituted/unsubstituted C1-C6 alkoxy or alkylthio group, nitro group, halogen atom, trichloromethyl group, trifluoromethyl group or cyano group, R3 is substituted/unsubstituted C1-C20 alkyl or alkoxy group, substituted/unsubstituted C2-C20 alkenyl or alkynyl group, substituted/unsubstituted aromatic hydrocarbon or aromatic heterocyclic group, substituted amino group, substituted/unsubstituted C2-C20 alkenyloxy or alkynyloxy group or R4O— (wherein R4 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.
这项发明提供了一种新型的酰磺酰胺衍生物,可用作 ACC 活性抑制剂,有效用于治疗内脏脂肪综合征,该综合征成为成年人疾病的风险因素,如心肌梗塞、脑梗塞和糖尿病。特别地,它涉及一种由通式 1 表示的酰磺酰胺衍生物,其中 R1 是取代/未取代的 C2-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、卤原子、三氯甲基基团、三氟甲基基团或氰基,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/未取代的芳香烃或芳香杂环基、取代氨基、取代/未取代的 C2-C20 烯氧基或炔氧基或 R4O—(其中 R4 是取代/未取代的芳香烃或芳香杂环基),Y 是—CH═CH—、—N═CH—、—CH═N—、硫或氧,环 A 是芳香烃、芳香杂环环或环状烷基。