A KHSO4 promoted tandem synthesis of 1,3,4-thiadiazoles from thiohydrazides and DMF derivatives
摘要:
An efficient, simple and environmentally benign method for the construction of 1,3,4-thiadiazole skeletons via the tandem coupling and cyclization of thiohydrazides with DMF derivatives in the presence of KHSO4 has been reported. This method reveals good reactivity and functional group tolerance, and a broad series of 1,3,4-thiadiazoles were obtained in moderate to good yields. (C) 2020 Elsevier Ltd. All rights reserved.
Quinuclidine Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands
申请人:Bristol-Myers Squibb Company
公开号:US20130131064A1
公开(公告)日:2013-05-23
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
申请人:BRISTOL-MYERS SQUIBB COMPANY
公开号:US20150094309A1
公开(公告)日:2015-04-02
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
Compounds having an activity to enhance the expression of apoAI are provided, which are used as medicaments.
Compounds of formula (I):
in which ring A and Ar
1
are independently a monocyclic or bicyclic aromatic carbocyclic group or aromatic heterocyclic group, each of which may be optionally substituted, or the like; R is a hydrogen or the like; Z is oxygen or the like; Y
1
and Y
2
are a hydrogen, a lower alkyl, or the like; n is an integer of 0 to 2; the broken line is the presence or absence of a bond; and the wavy line represents a cis- or trans-geometrical isomerism with respect to the double bond; are disclosed.