[EN] SORDARIN DERIVATIVES FOR PREVENTING OR TREATING INFECTIOUS DISEASES CAUSED BY PATHOGENIC MICROORGANISMS<br/>[FR] DÉRIVÉS DE SORDARINE POUR PRÉVENIR OU TRAITER DES MALADIES INFECTIEUSES CAUSÉES PAR DES MICRO-ORGANISMES PATHOGÈNES
申请人:ASTELLAS PHARMA INC
公开号:WO2009131246A1
公开(公告)日:2009-10-29
This invention relates to a new sordarin derivative or a pharmaceutically acceptable salt thereof, which has antimicrobial activities (especially, antifungal activities), to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases in a human being or an animal.
[EN] BIARYLTRIAZOLE INHIBITORS OF MACROPHAGE MIGRATION INHIBITORY FACTOR<br/>[FR] INHIBITEURS DE TRIAZOLE BIARYLE DU FACTEUR INHIBITEUR DE LA MIGRATION DES MACROPHAGES
申请人:UNIV YALE
公开号:WO2016130968A1
公开(公告)日:2016-08-18
The present disclosure describes biaryl triazole compounds, as well as their compositions and methods of use. The compounds inhibit the activity of macrophage migration inhibitory factor and are useful for the treatment of diseases, e.g., inflammatory diseases and cancer.
NICOTINAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
申请人:BERNHART Claude
公开号:US20100222319A1
公开(公告)日:2010-09-02
The disclosure relates to compounds of formula (I):
wherein A, Z, Z′, L, R
2
and R
3
are as defined in the disclosure, to compositions comprising said compounds, and to methods for the manufacture and therapeutic use thereof.
[EN] POLYCYCLIC TLR7/8 ANTAGONISTS AND USE THEREOF IN THE TREATMENT OF IMMUNE DISORDERS<br/>[FR] ANTAGONISTES DE TLR7/8 POLYCYLIQUES ET LEUR UTILISATION DANS LE TRAITEMENT DE MALADIES IMMUNES
申请人:MERCK PATENT GMBH
公开号:WO2017106607A1
公开(公告)日:2017-06-22
The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as toll-like receptor 7/8 (TLR7/8) antagonists. In Formula (I), Ring A is aryl or heteroaryl; Ring B is aryl or heteroary; and X is C(R4)2, O, NR4, S, S(R4), or S(R4)2.
Synthesis of Novel Succinamide Derivatives Having the 5,11-Dihydro-6H-pyrido(2,3-b)(1,4)benzodiazepin-6-one Skeleton as Potent and Selective M2 Muscarinic Receptor Antagonists. I.
116. Among them, 11-[3-[N-[2-(N-benzyl-N- methylamino)ethyl]-N-ethylcarbamoyl]propionyl]-5,11-dihydro-6H-pyr ido [2,3-b][1,4]benzodiazepin-6-one (68) was found to be the most potent and selective M2 muscarinic receptor antagonist in vitro. This compound also strongly inhibited the oxotremorine-induced bradycardia after intravenous administration and showed 130-fold selectivity for M2 muscarinic receptors