[EN] COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY [FR] COMPOSÉS ET COMPOSITIONS POUR TRAITER DES ÉTATS ASSOCIÉS À UNE ACTIVITÉ DE STING
Pyrrolidine derivatives, pharmaceutical compositions and uses thereof
申请人:FLECK Martin
公开号:US20140213568A1
公开(公告)日:2014-07-31
The invention relates to new pyrrolidine derivatives of the formula
to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
Aminodiol HIV Protease Inhibitors. Synthesis And Structure−Activity Relationships Of P<sub>1</sub>/P<sub>1</sub>‘ Compounds: Correlation between Lipophilicity and Cytotoxicity
作者:Ping Chen、Peter T. W. Cheng、Masud Alam、Barbara D. Beyer、Gregory S. Bisacchi、Tamara Dejneka、Adelaide J. Evans、Jill A. Greytok、Mark A. Hermsmeier、W. Griffith Humphreys、Glenn A. Jacobs、Octavian Kocy、Pin-Fang Lin、Karen A. Lis、Michael A. Marella、Denis E. Ryono、Amy K. Sheaffer、Steven H. Spergel、Chong-qing Sun、Joseph A. Tino、Gregory Vite、Richard J. Colonno、Robert Zahler、Joel C. Barrish
DOI:10.1021/jm950717a
日期:1996.1.1
A series of novel aminodiol inhibitors of HIV protease based on the lead compound 1 with structural modifications at P1' were synthesized in order to reduce the cytotoxicity of 1. We have observed a high degree of correlation between the lipophilicity and cytotoxicity of this series of inhibitors. It was found that appropriate substitution at the para position of the P1' phenyl group of 1 resulted
[EN] DOPAMINE D2 RECEPTOR LIGANDS<br/>[FR] LIGANDS DES RÉCEPTEURS DOPAMINERGIQUES D2
申请人:BROAD INST INC
公开号:WO2016100940A1
公开(公告)日:2016-06-23
The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity. The present invention relates to novel compounds that modulate dopamine D2 receptors. In particular, compounds of the present invention show functional selectivity at the dopamine D2 receptors and exhibit selectivity downstream of the D2 receptors, on the 0- arrestin pathway and/or on the cAMP pathway.
[EN] 2-THIO-IMIDAZOLE DERIVATIVES AS TGR5 MODULATORS<br/>[FR] DÉRIVÉS DE 2-THIOL-IMIDAZOLE UTILES COMME MODULATEURS DE TGR5
申请人:CADILA HEALTHCARE LTD
公开号:WO2013054338A1
公开(公告)日:2013-04-18
The present invention relates to compounds of the general Formula I their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, their N-oxide, metabolites, polymorphs, use of these compounds in medicine for treating diabetes (TGR5 modulators) and the intermediates involved in their preparation.
[EN] DOPAMINE D2 RECEPTOR LIGANDS<br/>[FR] LIGANDS DU RÉCEPTEUR D2 DE LA DOPAMINE
申请人:BROAD INST INC
公开号:WO2016100823A1
公开(公告)日:2016-06-23
The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.