[EN] 4-FLUOROPIPERIDINE OREXIN RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES DES RÉCEPTEURS DE L'OREXINE DE TYPE COMPOSÉS DE 4-FLUOROPIPÉRIDINE
申请人:MERCK SHARP & DOHME
公开号:WO2014113303A1
公开(公告)日:2014-07-24
The present invention is directed to 4-fluoropiperidine compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
acid-catalyzed reductive α-alkylation of β-aminothiophenes was applied to the N-(thien-3-yl)acetamide and alkyl N-(thien-3-yl)carbamates. Without reduction, β-amino α-vinylthiophenes were obtained when α-branched aldehydes were used. β-(3-Aminothien-2-yl)α,β-unsaturatedketones, esters and nitriles were also prepared from the corresponding α-functionalized acetals. These amines are intermediates in the formation
Synthesis of quinolines and naphthyridines via catalytic retro-aldol reaction of β-hydroxyketones with ortho-aminobenzaldehydes or nicotinaldehydes
作者:Song-Lin Zhang、Zhu-Qin Deng
DOI:10.1039/c6ob01452f
日期:——
Cu(I)-catalyzed retro-aldol reaction of β-hydroxyketones with ortho-aminobenzaldehydes and nicotinaldehydes is reported that produces a range of quinolines and naphthyridines with high efficiency and selectivity. This reaction uses β-hydroxyketones as a regiospecific ketone-protected enolate source viacopper-catalyzed retro-aldol Cα–Cβ bond cleavage. The in situ generated copper enolate undergoes kinetically
Furopyridine, thienopyridine pyrrolopyridine useful in controlling
申请人:Abbott Laboratories
公开号:US06001849A1
公开(公告)日:1999-12-14
Novel heterocyclic ether compounds having the formula: ##STR1## wherein A, m, R, X, Y.sup.1, Y.sup.2 and Y.sup.3 are specifically defined, which are useful in selectively controlling chemical synaptic transmission; therapeutically-effective pharmaceutical compositions thereof; and use of said compositions to selectively control synaptic transmission in mammals.
Indoles having various activities, including indoles that are CRTH2 are described. The compounds are useful for treating asthma, neuropathic pain, allegic rhinitis and other disorders.