[EN] ARYLAMINE SUBSTUTUTED BICYCLIC HETEROAROMATIC COMPOUNDS AS P38 KINASE INHIBITORS<br/>[FR] COMPOSES BICYCLIQUES HETEROAROMATIQUES ARYLAMINE SUBSTITUEE UTILISES EN TANT QU'INHIBITEURS DE KINASE P38
申请人:CELLTECH R&D LTD
公开号:WO2004000846A1
公开(公告)日:2003-12-31
Bicyclic heteroaromatic derivatives of formula (1) are described: F (1) where: the dashed line joining A and C(Ra) is present and represents a bond and A is a -N= atom or a -C(Rb)= group, or the dashed line is absent and A is a -N(Rb)-, or -C(Rb)(Rc)- group; X is an -O-, -S- or substituted nitrogen atom or a -S(O)-, -S(O2)- or -NH-group; Y is a nitrogen or substituted carbon atom or a -CH= group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain L1 is a covalent bond or a linker atom or group; Cy1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the remaining substituents are defined in the specification. The compounds are potent and selective inhibitors of p38 kinase and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
[EN] THIENOPYRIDONE DERIVATIVES AS KINASE INHIBITORS<br/>[FR] DERIVES DE THIENOPYRIDONE EN TANT QU'INHIBITEURS DE KINASE
申请人:CELLTECH R&D LTD
公开号:WO2004113347A1
公开(公告)日:2004-12-29
A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 2-position by a carbonyl- or sulfonyl-linked pyrrolidin-1-yl or related moiety, being inhibitors of p38 MAP kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.
[EN] PROCESS FOR PREPARING 3-AMINOTHIENOPYRIDONE DERIVATIVES<br/>[FR] PROCEDE SERVANT A PREPARER DES DERIVES DE 3-AMINOTHIENOPYRIDONE
申请人:CELLTECH R&D LTD
公开号:WO2004113349A1
公开(公告)日:2004-12-29
This invention provides a class of 3-amino-7H-thieno[2,3-b]pyridin-6-one derivatives, substituted in the 7-position by an aryl, heteroaryl, cycloalkyl or heterocycloalkyl moiety, and in the 2-position by a specified range of substituent groups; also provided is a process for preparing those compounds, and the use thereof as intermediates in the manufacture of certain p38 MAP kinase inhibitors.
[EN] GLYT2 MODULATORS<br/>[FR] MODULATEURS DU GLYT2
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2005044810A1
公开(公告)日:2005-05-19
α-, β-, and Ϝ-amino acid derivatives of formula I are disclosed as selective GlyT2 inhibitors for the treatment of central nervous system (CNS) conditions such as muscle spasticity, tinnitus, epilepsy and neuropathic pain. Formula I
This invention relates to substituted indacene molecules that specifically inhibit one or both of the checkpoint kinases Wee1 and Chk1 and are useful in the treatment of proliferative disorders.