[EN] AZACYCLIC SPIRODERIVATIVES AS HSL INHIBITORS<br/>[FR] SPIRODÉRIVÉS AZACYCLIQUES EN TANT QU'INHIBITEURS DE LA HSL
申请人:HOFFMANN LA ROCHE
公开号:WO2010130665A1
公开(公告)日:2010-11-18
Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein n, m, A, R1 and R2 have the significance given in claim 1. The compounds are useful as HSL inhibitors for the treatment of diabetes dyslipidemia, atherosclerosis and obesity.
Compounds of formula (I)
as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A
1
, A
2
, R
1
, R
2
, R
3
and R
4
have the significance given in claim
1.
Synthesis and structure-activity relationships of 2-sulfonamido-1,3,4,6,7,11b.alpha.-hexahydro-2H-benzo[a]quinolizines as .alpha.2-adrenoceptor antagonists
作者:Terence J. Ward、John F. White、Norman Lattimer、Keith F. Rhodes、Shobna Sharma、John F. Waterfall
DOI:10.1021/jm00402a029
日期:1988.7
for alpha 2- and alpha 1-adrenoceptor antagonist activity on the rat vas deferens and anococcygeus muscle, respectively. A number of compounds in this series were shown to be potent and selective alpha 2-adrenoceptor antagonists. Studies on the resolved enantiomers of compounds 6, 10, and 16 showed that alpha 2-adrenoceptor antagonist activity resided primarily in the 2R,11bS isomers, related to the absolute
[EN] PYRIMIDINYL-PYRIDYLOXY-NAPHTHYL COMPOUNDS AND METHODS OF TREATING IRE1-RELATED DISEASES AND DISORDERS<br/>[FR] COMPOSÉS PYRIMIDINYL-PYRIDYLOXY-NAPHTYLE ET PROCÉDÉS DE TRAITEMENT DE MALADIES ET DE TROUBLES LIÉS À IRE1
申请人:GENENTECH INC
公开号:WO2018166528A1
公开(公告)日:2018-09-20
Described herein are pyrimidinyl-pyridyloxy-naphthyl compounds with inositol requiring enzyme 1 (IRE1) modulation activity or function having the Formula (I) or (I') structure : or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula (I) or (I') compounds, as well as methods of using such IRE1 modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.