[EN] FARNESOID X RECEPTOR AGONISTS AND USES THEREOF<br/>[FR] AGONISTES DU RÉCEPTEUR FARNÉSOÏDE X ET LEURS UTILISATIONS
申请人:METACRINE INC
公开号:WO2018170167A1
公开(公告)日:2018-09-20
Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
2-substituted 1,2-benzisothiazol-3(2H)-one 1,1-dioxide useful as an
申请人:American Home Products Corporation
公开号:US04859671A1
公开(公告)日:1989-08-22
There is disclosed the compound 2-[4-[4-(2,7-naphthyridin-1-yl)-1-piperazinyl]butyl]-1,2-benzisothiazol-3( 2H)-one 1,1-dioxide, and the method of producing said compound, and the pharmaceutically acceptable salts thereof, and the use of said compound as an anxiolytic agent having a low liability for extrapyramidal side effects.
[EN] PHENYLALANINE ENAMIDE DERIVATIVES<br/>[FR] DERIVES DE PHENYLALANINE ENAMIDE
申请人:CELLTECH R&D LTD
公开号:WO2004007494A1
公开(公告)日:2004-01-22
Phenylalanine enamide derivatives of formula (1) are described, wherein R1 is a -CH(CH3)2, -(CH2)2CH3; -CH2C(CH3)3, -CH2CH2OH, -CH2CH2OCH3, -CH2CH2OCH2CH2OH, -CH2CH2OCH2CH2OCH3, formula (A) group; and the salts, solvates and N-oxides thereof. Compounds according to the invention are potent and selective inhibitors of α4 integrins. The compounds are of use in modulating cell adhesion and in particular are of use in the prophylaxis and treatment of diseases or disorders including inflammation in which the extravasation of leukocytes plays a role and the invention extends to such a use and to the use of the compounds for the manufacture of a medicament for treating such diseases or disorders.
[EN] PROCESS FOR THE PREPARATION OF PHENYLALANINE ENAMIDE DERIVATIVES<br/>[FR] PROCEDE DE PREPARATION DE DERIVES DE PHENYLALANINE-ENAMIDE
申请人:CELLTECH R&D LTD
公开号:WO2004007428A1
公开(公告)日:2004-01-22
A process for the preparation of a class of phenylalanine enamide derivatives is described formula (1) wherein: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a linker group selected from -N(R4)- [where R4 is a hydrogen atom or an optionally substituted straight or branched C1-6alkyl group], -CON(R4)-, or -S(O)2N(R4)-; R1 is a carboxylic acid (-CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Rx, Ry and Rz which may be the same or different is each an atom or group -L1(Alk1)n(R3)v; and the salts, solvates, hydrates and N-oxides thereof; which comprises reacting a compound of formula (2): wherein: Qa is a group -N(R4)H; and the salts, solvates, hydrates and N-oxides thereof; with a compound Ar1W wherein W is a group selected from X1 (wherein X1 is a leaving atom or group), -COX2 (wherein X2 is a halogen atom or a -OH group) or -SO2 X3 (in which X3 is a halogen atom).