[EN] PIPERIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR AGONISTS [FR] DERIVES DE PIPERIDINE UTILISES EN TANT QU'AGONISTES DU RECEPTEUR DE LA MELANOCORTINE 4
[EN] ACYLATED SPIROPIPERIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS [FR] DERIVES SPIROPIPERIDINES ACYLES CONVENANT COMME MODULATEURS DES RECEPTEURS DE LA MELANOCORTINE-4
NOVEL IMIDAZOLE COMPOUND AND USE THEREOF AS MELANOCORTIN RECEPTOR AGONIST
申请人:MITSUBISHI TANABE PHARMA CORPORATION
公开号:US20180258076A1
公开(公告)日:2018-09-13
The present invention relates to a novel imidazole compound or a pharmaceutically acceptable salt thereof having a melanocortin receptor agonistic activity, and medical use thereof. The present invention relates to an imidazole compound represented by general formula [I]
[wherein: Ring A represents an optionally substituted aryl group or the like; R
1
represents a hydrogen atom, an optionally substituted alkyl group, or the like; R
2
represents a hydrogen atom, a halogen atom, or the like; and R
3
represents an optionally substituted alkyl group] or a pharmaceutically acceptable salt thereof.
The present invention relates to a class of melanocortin MCR4 agonists of general formula (I)
wherein R
1
, R
2
, R
3
, R
4
and R
5
are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
[EN] BICYCLIC PIPERIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR AGONISTS<br/>[FR] DERIVES DE PIPERIDINE BICYCLIQUES UTILISES COMME AGONISTES DU RECEPTEUR 4 DE LA MELANOCORTINE
申请人:MERCK & CO INC
公开号:WO2004087159A1
公开(公告)日:2004-10-14
Certain novel bicyclic N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
A One-Pot Stereoselective Synthesis of Electron-Deficient 4-Substituted (E,E)-1-Arylsulfonylbuta-1,3-dienes and Their Chemoselective [3+2] Cycloaddition with Azomethine Ylides - A Simple Synthesis of 1,3,4-Trisubstituted Pyrrolidines and Pyrroles
A simple and efficient method for the synthesis of ( E , E )-1-(arylsulfonyl)buta-1,3-dienes bearing electron-withdrawing substituents like cyano and ethoxycarbonyl at position 4, involving a one-pot alkylation of bis(phenylsulfonyl)methane with trans -ethyl 4-bromocrotonate/ trans -4-bromocrotononitrile, and elimination of arylsulfinic acid, is described. These dienes undergo facile mono [3+2] cycloaddition
一种简单有效的合成 ( E , E )-1-(芳基磺酰基)buta-1,3-二烯的方法,该方法在 4 位带有吸电子取代基,如氰基和乙氧基羰基,包括双(苯磺酰基)的一锅烷基化) 甲烷与反式-4-溴巴豆酸乙酯/反式-4-溴巴豆腈,以及芳基亚磺酸的消除。这些二烯通过偶氮甲碱叶立德化学选择性进行简单的单 [3+2] 环加成,以提供功能化的 1,3,4-三取代吡咯烷。在温和条件下用MnO 2 ·SiO 2 氧化这些环加合物提供1,3,4-三取代的吡咯。