Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT2C agonists
摘要:
A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1,2,3,6-tetrahydropyridines were synthesized and their biological activity at the 5-HT2C receptor studied to determine whether either series showed noteworthy agonist activity. Structure-activity relationships were developed from the performed receptor binding assays and functional studies, and the results of the analysis are presented herein. Crown Copyright (C) 2012 Published by Elsevier Ltd. All rights reserved.
Substituted anilinic piperidines as MCH selective antagonists
申请人:Synaptic Pharmaceutical Corporation
公开号:US06727264B1
公开(公告)日:2004-04-27
This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therepeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.
The present invention relates to compounds according to formula 1,
which exhibit cytotoxic activity. The compounds may be used in the treatment of cancer.
本发明涉及符合式1的化合物,具有细胞毒活性。这些化合物可用于治疗癌症。
Tetrahydrobenzindole compounds
申请人:Meiji Seika Kaisha, Ltd.
公开号:US06355642B1
公开(公告)日:2002-03-12
A compound of formula (I) for use in the treatment or prevention of mental diseases
A is N, CH, C having a double bond or CR5; each of B and Z is independently N, CH or CR1, with the proviso that A is N when B and/or Z is N; R1, R2, R3, R4 and R5 and n are as defined in the specification.
[EN] GAMMA-AMINOAMIDE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY<br/>[FR] MODULATEURS GAMMA-AMINOAMIDES DE L'ACTIVITE DE RECEPTEUR DE CHIMIOKINE
申请人:MERCK & CO INC
公开号:WO2004041279A1
公开(公告)日:2004-05-21
The present invention is directed to compounds of the formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R11, R12, W, X, and n are defined herein, which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.