Novel retinoid-related orphan receptor gamma (RORϒ) modulators and their use in the treatment of diseases mediated by RORϒ provided by the present invention.
新型视黄醇相关孤儿受体γ(RORϒ)调节剂及其在通过RORϒ介导的疾病治疗中的应用,由本发明提供。
[EN] LACTAM DERIVATIVES USEFUL AS OREXIN RECEPTOR ANTAGONISTS<br/>[FR] DÉRIVÉS DE LACTAME UTILES EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE L'OREXINE
申请人:ACTELION PHARMACEUTICALS LTD
公开号:WO2012063207A1
公开(公告)日:2012-05-18
The present invention relates to lactam derivatives of formula (I) wherein Y, R1, R2 and R3 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.
A facile synthetic route to the new thiazol-5-ylboronic acid pinacol ester was described herein. Its reactivity toward Suzuki cross-coupling reaction was studied to provide various 5-arylthiazoles. A comparative study between Suzuki cross-coupling reactions and palladium-catalyzed C5–H direct arylation on thiazolering was achieved.
LACTAM DERIVATIVES USEFUL AS OREXIN RECEPTOR ANTAGONISTS
申请人:Aissaoui Hamed
公开号:US20130237525A1
公开(公告)日:2013-09-12
The present invention relates to lactam derivatives of formula (I)
wherein Y, R
1
, R
2
and R
3
are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.