(p-Amylcinnamoyl)anthranilic acid (3a) had moderate antagonist activities against LTD4-induced smooth muscle contraction on guinea pig ileum and LTC4-induced bronchoconstriction in anesthetized guinea pigs. Modifications were made in the hydrophobic part (cinnamoyl moiety) and the hydrophilic part (anthranilate moiety) of 3a. A series of 8-(benzoylamino)-2-tetrazol-5-yl-1,4-benzodioxans and 8-(ben
Novel substituted 4-(1H-benzimidazol-2-yl) [1,4]diazepanes useful for the treatment of allergic diseases
申请人:——
公开号:US20010034343A1
公开(公告)日:2001-10-25
The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula
1
and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Substituted Phenoxy-and Phenylthio-Derivatives for Treating Proliferative Disorders
申请人:Reddy E. Premkumar
公开号:US20080058290A1
公开(公告)日:2008-03-06
Substituted phenol derivatives of Formula (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.
公式(I)的取代酚衍生物可用作抗增殖剂,包括例如抗癌剂,以及放射防护和化学防护剂。
Access to Saturated Thiocyano-Containing Azaheterocycles via Selenide-Catalyzed Regio- and Stereoselective Thiocyanoaminocyclization of Alkenes
作者:Wei Wei、Lihao Liao、Tian Qin、Xiaodan Zhao
DOI:10.1021/acs.orglett.9b02834
日期:2019.10.4
An efficient route for the synthesis of saturated thiocyano-containing azaheterocycles by selenide-catalyzed regio- and stereoselective thiocyanoaminocyclization of alkenes is disclosed. The desired products were obtained in moderate to highyields under mild conditions. The generality of this method was elucidated by its efficient application in thiocyano oxycyclization of alkenes.
cycloadditions of 2‐nitrosopyridine with various allylstannanes give 4‐stannyl‐substituted isoxazolidines. The use of [Cu(MeCN)4]PF6, in combination with a Walphos ligand, leads to excellent enantioselectivies and high yields. With cis‐2‐alkenylstannanes as nucleophiles, 3‐alkyl‐4‐stannyl‐substituted isoxazolidines are formed with excellent diastereo‐ and enantioselectivities.