Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-[3-(3-pyridinyl)propyl]octanoic acid and analogs
摘要:
The title compound (10a) and its analogs were synthesized and found to possess two activities, the inhibition of the biosynthesis of thromboxane A2 and antagonism of its receptors. The in vitro and in vivo profile of these compounds as thromboxane receptor antagonists (TxRAs) and thromboxane synthase inhibitors (TxSIs) is described. 10a and its analogs displayed very potent TxRA activity in human washed platelets (IC50 almost-equal-to 10(-7)-10(-9) M) and dog saphenous vein (pA2 almost-equal-to 9) and also potent TxSI activity (IC50 almost-equal-to 10(-9) M). The good bioavailability and the long duration of action of some of these compounds was demonstrated using ex vivo measurement of the TxRA activity upon oral administration to guinea pigs. Compounds 10a, 20, and 33 potently inhibited arachidonic acid induced bronchoconstriction in guinea pigs.
[EN] PGD2 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES<br/>[FR] ANTAGONISTES DE RECEPTEUR DE LA PROSTAGLANDINE D2 POUR LE TRAITEMENT DE MALADIES INFLAMMATOIRES
申请人:MILLENNIUM PHARM INC
公开号:WO2005100321A1
公开(公告)日:2005-10-27
Disclosed herein are compounds represented by Structural Formula: (I) and (I-A). Also disclosed is the use of such compounds for inhibiting the G-protein coupled receptor referred to as chemoattractant receptor-homologous molecule expressed on Th2, or simply 'CRTH2' for the treatment of inflammatory disorders. The variables in Structural Formula (I) and (I-A) are defined herein.
Methods of making 2,6-diaryl piperidine derivatives
申请人:Chen Gang
公开号:US20050154201A1
公开(公告)日:2005-07-14
Methods for preparing 2,6-diaryl piperidine derivatives are described. More particularly, 2,6-diaryl piperidines having formula 1-4 are prepared by cyclocondensation of an aryl or heteroaryl aldehyde with 1,3-acetonedicarboxylic acid.
[EN] PREPARATION OF CATIONIC AND NEUTRAL FUSED N-HETEROCYCLES WITH OR WITHOUT ADDITIONAL HETEROATOMS<br/>[FR] PRÉPARATION DE N-HÉTÉROCYCLES FUSIONNÉS CATIONIQUES ET NEUTRES AVEC OU SANS HÉTÉROATOMES SUPPLÉMENTAIRES
申请人:NAT UNIV SINGAPORE
公开号:WO2021162633A1
公开(公告)日:2021-08-19
Disclosed herein is a process for the manufacture of a cationic fused N-heterocyclic ring system, comprising reaction of a compound of formula (I): with a base and with a material FF or only with a base to provide a compound of formula (II): where the symbols are defined herein.
PGD2 receptor antagonists for the treatment of inflammatory diseases
申请人:Ghosh Shomir
公开号:US20050256158A1
公开(公告)日:2005-11-17
Disclosed herein are compounds represented by Structural Formula (I) and (I-A):
Also disclosed is the use of such compounds for inhibiting the G-protein coupled receptor referred to as chemoattractant receptor-homologous molecule expressed on Th2, or simply “CRTH2” for the treatment of inflammatory disorders. The variables in Structural Formula (I) and (I-A) are defined herein.