The present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I:
wherein
R
1
to R
6
are as defmed in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
本发明涉及式I的芳基异噁唑-4-基咪唑衍生物:其中R1至R6如规范中定义,并且其药用酸盐。这类化合物具有高亲和力和选择性结合到GABA A α5受体结合位点,可能有助于作为认知增强剂或治疗认知障碍如阿尔茨海默病。
[EN] LIGANDS OF FOLLICLE STIMULATING HORMONE RECEPTOR AND METHODS OF USE THEREOF<br/>[FR] LIGANDS DU RECEPTEUR DE L'HORMONE FOLLICULO-STIMULANTE ET METHODES D'UTILISATION ASSOCIEES
申请人:ARENA PHARM INC
公开号:WO2005087765A1
公开(公告)日:2005-09-22
The present invention relates to compounds Formula I (I) that are modulators of the follicle stimulating hormone (FSH) receptor and are useful in the treatment of infertility and related disorders.
The present invention is concerned with aryl-isoxazole-4-carbonyl-pyrrole-2-carboxylic acid amide derivatives of formula
wherein
R
1
, R
2
, R
3
, R
4
, and R
5
, and m are as defined herein and with their pharmaceutically acceptable acid addition salts.
This class of compounds have high affinity and selectivity for GABA A α5 receptor binding sites and therefore may be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
本发明涉及一种芳基异噁唑-4-甲酰基-吡咯-2-羧酸酰胺衍生物,其化学式为其中R1、R2、R3、R4和R5以及m的定义如本文所述,并且涉及它们的药学上可接受的酸盐。这类化合物具有高亲和力和选择性,可结合到GABA A α5受体结合位点,因此可能用作认知增强剂或用于治疗像阿尔茨海默病这样的认知障碍。
1,3-Dipolar cycloaddition of nitrile oxides to methyl 3-(p-nitrobenzoyloxy)acrylate: Methyl 3-(p-nitrobenzoyloxy)acrylate as a methyl propiolate equivalent with reverse regioselectivity
作者:Kyukwan Zong、Seung Il Shin、Dong Ju Jeon、Jung No Lee、Eung K. Ryu
DOI:10.1002/jhet.5570370112
日期:2000.1
3-Aryl-4-methoxycarbonylisoxazoles were prepared from the reaction of a variety of substituted benzonitrile oxides with methyl 3-(p-nitrobenzoyloxy)acrylate in moderate to good yields.