A facile access to chalcogen and dichalcogen bearing dialkylamines and diols
摘要:
A highly practical procedure for the preparation of novel classes of chalcogen bearing diamines [{H2N(CH2)n}E] and diols [{HO(CH2)n}(2)E] (n = 2 or 3 and E = Se or Te) by the reaction of disodiumchalcogenide and haloalkylamines or haloalcohols is presented. (C) 2004 Elsevier Ltd. All rights reserved.
BENZAZEPINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
申请人:Takeda Chemical Industries, Ltd.
公开号:EP1422228A1
公开(公告)日:2004-05-26
The present invention provides a novel benzazepine derivative represented by formula :
wherein, R1 is a 5- or 6-membered aromatic ring, R2 is lower alkyl group, etc., Y is an optionally substituted imino group, ring A and ring B are independently an optionally substituted aromatic ring, W is formula -W1-X2-W2- (W1 and W2 are independently S(O)m1 (m1 is 0, 1 or 2), etc., and X2 is an optionally substituted alkylene groupetc. ), a preparation method and use thereof.
Synthesis of 5-methyl-4-oxo-quinolinecarboxylic acids
作者:Susan E. Hagen、John M. Domagala
DOI:10.1002/jhet.5570270616
日期:1990.9
A series of 5-methyl-4-oxo-3-quinolinecarboxylic acids was prepared in which the eight-position was substituted with fluorine, chlorine, methyl, or hydrogen. These quinolones were synthesized from the appropriate 2-methyl-3,4,6-trifluorobenzoic acids which were derived from oxazolines 8 and 16. The oxazoline moiety served as both an ortho-director (where feasible) and a protecting group; a trimethylsilyl
The present invention is directed to oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the oxazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
[EN] OXAZOLE OREXIN RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES DE RÉCEPTEUR D'OREXINE À BASE D'OXAZOLE
申请人:MERCK SHARP & DOHME
公开号:WO2015020930A1
公开(公告)日:2015-02-12
The present invention is directed to oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the oxazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
作者:Harshad K Rami、Mervyn Thompson、Paul Wyman、Jeffrey C Jerman、Julie Egerton、Stephen Brough、Alexander J Stevens、Andrew D Randall、Darren Smart、Martin J Gunthorpe、John B Davis
DOI:10.1016/j.bmcl.2004.05.028
日期:2004.7
Smallmolecule antagonists of the vanilloid receptor 1 (TRPV1, also known as VR1) are disclosed. Ureas such as 5 (SB-452533) were used to explore the structureactivityrelationship with several potent analogues identified. Pharmacological studies using electrophysiological and FLIPR Ca(2+) based assays showed compound 5 was an antagonist versus capsaicin, noxious heat and acid mediated activation