Design, synthesis and pharmacological evaluation of 4-(piperazin-1-yl methyl)-N1-arylsulfonyl indole derivatives as 5-HT6 receptor ligands
摘要:
4-(Piperazin-1-yl methyl)-N-1-arylsulfonyl indole derivatives were designed and synthesized as 5-HT6 receptor (5-HT6R) ligands. The lead compound 6a, from this series shows potent in vitro binding affinity, good PK profile, no CYP liabilities and activity in animal models of cognition. (c) 2012 Elsevier Ltd. All rights reserved.
Substituted 1,3-thiazole compounds, their production and use
申请人:——
公开号:US20040053973A1
公开(公告)日:2004-03-18
(1) A 1,3-thiazole compound of which the 5-position is substituted with a 4-pyridyl group having a substituent including no aromatic group or (2) a 1,3-thiazole compound of which the 5-position is substituted with a pyridyl group having at the position adjacent to a nitrogen atom of the pyridyl group a substituent including no aromatic group has an excellent p38 MAP kinase inhibitory activity.
Compounds of formula (I)
1
are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
式(I)的化合物是新颖的VR1拮抗剂,可用于治疗疼痛、炎症性热性过敏、尿失禁和膀胱过度活动。
Substituted 7-aza[2.2.1]bicycloheptanes for the treatment of disease
申请人:——
公开号:US20030105089A1
公开(公告)日:2003-06-05
The invention provides compounds of Formula I:
1
which may be in the form of pharmaceutical acceptable salts or compositions, are useful in treating diseases or conditions in which &agr;7 nicotinic acetylcholine receptors (nAChRs) are known to be involved.
Monocyclic L-Nucleosides, analogs and uses thereof
申请人:ICN Pharmaceuticals, Inc.
公开号:US06130326A1
公开(公告)日:2000-10-10
Novel monocyclic L-Nucleoside compounds have the general formula ##STR1## Embodiments of these compounds are contemplated to be useful in treating a wide variety of diseases including infections, infestations, neoplasms, and autoimmune diseases. Viewed in terms of mechanism, embodiments of the novel compounds show immunomodulatory activity, and are expected to be useful in modulating the cytokine pattern, including modulation of Th1 and Th2 response.
1,4-disubstituted piperazines (or homopiperazines) as
申请人:Takeda Chemical Industries, Ltd.
公开号:US04880809A1
公开(公告)日:1989-11-14
Novel 1,4-disubstituted piperazine compounds represented by the formula (I): ##STR1## wherein A is a condensed polycyclic hydrocarbon group; R is a phenyl group substituted with a lower alkoxy group; X is methylene group, carbonyl group or thiocarbonyl group; and m is 2 or 3, and their salts are useful as a platelet activating factor antagonist.