Synthesis and salidiuretic activity of 2,3-dihydro-8-(1-pyrrolyl)-1,2,4-triazolo(4,3-a-)pyridines and 5,6-dihydro-4H-pyrido(2,3-c)pyrrolo(1,2-e)-1,2,5-triazepines.
Asymmetric 1,4-reductions of and 1,4-additions to enoates and related systems
申请人:——
公开号:US20030125563A1
公开(公告)日:2003-07-03
One aspect of the present invention relates to methods for the transition-metal-catalyzed asymmetric 1,4-addition of a nucleophile, e.g., hydride, to cyclic and acyclic enoates and enones. In certain embodiments of the methods of the present invention, the transition metal catalyst consists essentially of copper and an asymmetric bidentate bisphosphine ligand.
Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) wherein R
1
-R
3
and Ar are as defined herein are antagonists of chemokine CCR
5
receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR
5
antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I.
The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.