首页> 外国专利> Heterocyclic pyrrolidines Melanocortin Receptor agonists, Pharmaceutical compositions containing them and Use thereof in the treatment of Obesity, Diabetes and erectile dysfunction.

Heterocyclic pyrrolidines Melanocortin Receptor agonists, Pharmaceutical compositions containing them and Use thereof in the treatment of Obesity, Diabetes and erectile dysfunction.

机译:杂环吡咯烷类黑皮质素受体激动剂,含有它们的药物组合物及其在肥胖症,糖尿病和勃起功能障碍的治疗中的用途。

摘要

Claim 1: a compound of the formula (1) wherein: R1 represents h, alkyl or cycloalkyl - 10 represents C1, C3 C6 - 10 - 7, aryl or heteroaryl, a heterocycle, each of which is insustituido or substituted with at least one Substituent selected from the Group C Consists in Halogen, c1-4 alkyl amino, Hydroxy, alkoxy, trifluoromethyl, c1-4,Ciano and oxo; R2 represents phenyl or heteroaryl 6 members, each of whom is insustituido or mono - or alkylated with one or more substituents selected from the group consisting of halogen, Hydroxy, c1-4 alkyl, c1-4 alkoxy, amino and cyano; R3 represents h, alkyl or represents Cycloalkyl or C1 - C3 - 6 or 7,Each of which is insustituido or substituted with one or more substituents selected from the group consisting of halogeno, trifluoromethyl Methyl, Hydroxy and amino; R4 represents cycloalkyl C4 - 7 or a monocyclic heterocycle, each of which is insustituido or mono - or Poly sust Ituido with one or more substituents selected from the group consisting of halogen, Hydroxy,C1-4 alkyl, trifluoromethyl, c1-4 alkoxy and oxo represents phenyl or heteroaryl; or a six member, each of which is insustituido or mono - or di substituted with one or more substituents selected from the group consisting of halogen, Hydroxy, trifluoromethyl, c1-4 alkyl, alkoxy C1-4 alkyl, amino, and R5 represents 6 difluorometilo C1, C3, trifluoromethyl, cycloalkyl - 6Amino alquilamino c1-4 alkyl 4amino C1 -, di -, a monocyclic heteroaryl phenyl or a monocyclic heterocycle where alkyl is insustituido or substituted with at least one Substituent selected from the group consisting of fluoro, Hydroxy, mercapto, c1-4 alkoxy, acetoxy amino, ACET Ilamino, cyano, carbamoilo,Dimethyl carbamoilo and oxo and phenyl or heteroaryl is insustituido or mono - or di substituted with one or more substituents selected from the group consisting of halogeno, trifluoromethyl Methyl, Hydroxy, amino, methoxy and, or a pharmaceutically acceptable Salt or an isomer thereof.
机译:1.权利要求1的式(1)化合物,其中:R 1代表h,烷基或环烷基-10代表C 1,C 3 -C 6-10-7,芳基或杂芳基,杂环,其各自是工业上的或被至少一个取代的选自C组的取代基包括卤素,c1-4烷基氨基,羟基,烷氧基,三氟甲基,c1-4,Ciano和羰基。 R2代表苯基或杂芳基6元,它们各自被一个或多个选自卤素,羟基,c1-4烷基,c1-4烷氧基,氨基和氰基的取代基取代或被一个或多个烷基取代。 R 3代表h,烷基或代表环烷基或C 1 -C 3-6或7,其中的每个被取代或被一个或多个选自卤代,三氟甲基甲基,羟基和氨基的取代基取代; R 4代表环烷基C 4-7或单环杂环,其各自为具有两个或多个选自卤素,羟基,C 1-4烷基,三氟甲基,c 1-4烷氧基和/或取代基的单取代或单取代或多取代。氧代代表苯基或杂芳基;或六个成员,分别被一个或多个选自卤素,羟基,三氟甲基,c1-4烷基,烷氧基C1-4烷基,氨基和R5的取代基取代或取代成一个或多个二氟metilo C1,C3,三氟甲基,环烷基-6氨基Alquilamino c1-4烷基4氨基C1-,二-,单环杂芳基苯基或单环杂环,其中烷基为取代基或被至少一种选自氟,羟基的取代基取代,巯基,c1-4烷氧基,乙酰氧基氨基,ACET二氨基,氰基,氨基甲酰基,二甲基氨基甲酰基和氧代,并且苯基或杂芳基是被一个或多个选自卤代,三氟甲基甲基的取代基取代或单取代或二取代的,羟基,氨基,甲氧基和/或其药学上可接受的盐或其异构体。

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