[EN] SUBSTITUTED PYRROLOPYRDINES AS INHIBITORS OF BROMODOMAIN<br/>[FR] PYRROLOPYRIDINES SUBSTITUÉES UTILISÉES EN TANT QU'INHIBITEURS DE BROMODOMAINES
申请人:GENENTECH INC
公开号:WO2016077378A1
公开(公告)日:2016-05-19
The present invention relates to compounds of formula (I) and to salts thereof, wherein R1, R2, and Q have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated disorders.
4-SUBSTITUTED PYRIDIN-3-YL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE
申请人:Wang Xiaojing
公开号:US20110059961A1
公开(公告)日:2011-03-10
The invention relates to compounds of formula (I) which are useful as kinase inhibitors, more specifically useful as PIM kinase inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same, either alone or in combination, to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
IMIDAZO[5,1-C][1,2,4]BENZOTRIAZINE DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASES
申请人:Stange Hans
公开号:US20100120763A1
公开(公告)日:2010-05-13
The invention relates to imidazo[5,1-c][1,2,4]benzotriazine derivatives of formula I:
which are inhibitors of phosphodiesterase 2 or 10 useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type 2 diabetes, metabolic syndrome, glucose intolerance, and pain.
BENZAMIDE FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
申请人:Priestley Eldon Scott
公开号:US20100227894A1
公开(公告)日:2010-09-09
The present invention provides novel benzamide derivatives of Formula (I):
or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, W, Y, Z, R
8
, and R
9
are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
Pyrido[3,2-E]Pyrazines, Process For Preparing The Same, And Their Use As Inhibitors Of Phosphodiesterase 10
申请人:Malamas Michael S.
公开号:US20090143361A1
公开(公告)日:2009-06-04
The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical compositions which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating central nervous system disorders, obesity, and metabolic disorders.