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Oxopiperidina derivatives as Melanocortin Receptor agonists and / or MC3, MC4

机译:氧哌啶子基衍生物作为黑皮质素受体激动剂和 /或MC3,MC4

摘要

Referring to a oxopiperidina derived Compound of formula I, where n is 1; ra, ra and RB, Rb 'are h, cycloalkyl, among others; r1 is alkyl or cycloalkyl; R2 is heteroaryl; R3 is Halogen, alkyl, NO2, among others; R5 is alkyl or cycloalkyl Group; R4 is selected formulas (a) , (b) and (c), eventually replaced by an oxo Group,Or mono - or by an aryl or heteroaryl Group polisustituido; p is 0, 1, 2 or 3; M is 0, 1 or 2 - N; X is a link or a Link (R10) - C (r6) (R7); h R6, R7 is Halogen, among others; Halogen, alkyl, etc.; R10 is cycloalkyl, aryl, among others.Preferred compounds are: n {- (1R) - 1 - (4-chlorobenzyl) - 2 - [4 - (1H - Cyclohexyl - 4 - methyl - 1 - 1,2,4 - triazole) piperidin-1-yl] - 2-oxoethyl} - 1 - (2-phenylethyl) piperidin-4-yl Amine 4 - [4 - ((1R) - 1 - (4-chlorobenzyl) - 2 - [4 - (1H - Cyclohexyl - 4 - methyl - 1 - 1,2,4 - triazole) piperidin-1-yl] - 2-oxoethyl} amino phenol) cyclohexyl], among others. It also relates to a Pharmaceutical Composition and a preparation method.These compounds are agonists of Melanocortin MC3 and MC4 and / or are useful in the treatment of Obesity, diabetes, sexual dysfunction, among other
机译:指氧代哌啶子基衍生的式I化合物,其中n为1; n为1。 ra,ra和RB,Rb′是h,环烷基,等等。 r1是烷基或环烷基; R 2为杂芳基; R 3是卤素,烷基,NO 2等; R5是烷基或环烷基; R4是选择的式(a),(b)和(c),最终被氧代基团或单-或被芳基或杂芳基基团取代。 p是0、1、2或3; M为0、1或2-N; X是链接或链接(R10)-C(r6)(R7); h R6,R7为卤素等;卤素,烷基等; R 10是环烷基,芳基等。优选的化合物是:n {-(1R)-1-(4-氯苄基)-2-[4-(1H-环己基-4-甲基-1-1,2,4- (三唑)哌啶-1-基]-2-氧乙基}-1-(2-苯乙基)哌啶-4-基胺4-[4-(((R)-1-(4-氯苄基))-2-[4- (1H-环己基-4-甲基-1-1,2,4-三唑)哌啶-1-基]-2-氧代乙基}氨基苯酚)环己基],等等。它还涉及药物组合物和制备方法。这些化合物是黑皮质素MC3和MC4的激动剂和/或可用于治疗肥胖症,糖尿病,性功能障碍等。

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