2-AMINOBENZOXAZOLE CARBOXAMIDES AS 5HT3 MODULATORS
申请人:Yang Zhicai
公开号:US20080255114A1
公开(公告)日:2008-10-16
Compounds of formulae I, II and III:
are disclosed as 5-HT3 inhibitors. The compounds are useful in treating CINV, IBS-D and other diseases and conditions.
[EN] ANTIMICROBIALS AND METHODS OF MAKING AND USING SAME<br/>[FR] ANTIMICROBIENS ET LEURS PROCÉDÉS DE PRÉPARATION ET D'UTILISATION
申请人:MELINTA THERAPEUTICS INC
公开号:WO2017193023A1
公开(公告)日:2017-11-09
The present disclosure relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, reducing the risk of, and delaying the onset of microbial infections in humans and animals. In some embodiments, the present disclosure provides a compound of Formula (I): or a tautomer thereof or a pharmaceutically acceptable salt of the compound or tautomer.
Compounds of formula IA and IB are new
1
where the variables R
1
through R
10
have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.
Three-Component Reaction of Diamines with Triethyl Orthoformate and Diethyl Phosphite and Anti-Proliferative and Antiosteoporotic Activities of the Products
A three-component reaction between diamines (diaminobenzenes, diaminocyclohexanes, and piperazines), triethyl orthoformate, and diethylphosphite was studied in some detail. In the case of 1,3- and 1,4-diamines and piperazines, products of the substitution of two amino moieties—the corresponding tetraphosphonic acids—were obtained. In the cases of 1,2-diaminobenzene, 1,2-diaminocyclohexanes and 1,
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists
作者:Zhicai Yang、David J. Fairfax、Jun-Ho Maeng、Liaqat Masih、Alexander Usyatinsky、Carla Hassler、Soshanna Isaacson、Kevin Fitzpatrick、Russell J. DeOrazio、Jianqing Chen、James P. Harding、Matthew Isherwood、Svetlana Dobritsa、Kevin L. Christensen、Jonathan D. Wierschke、Brian I. Bliss、Lisa H. Peterson、Cathy M. Beer、Christopher Cioffi、Michael Lynch、W. Martin Rennells、Justin J. Richards、Timothy Rust、Yuri L. Khmelnitsky、Marlene L. Cohen、David D. Manning
DOI:10.1016/j.bmcl.2010.09.038
日期:2010.11
A new class of 2-substitutedbenzoxazole carboxamides are presented as potent functional 5-HT3 receptor antagonists. The chemical series possesses nanomolar in vitro activity against human 5-HT3A receptors. A chemistry optimization program was conducted and identified 2-aminobenzoxazoles as orally active 5-HT3 receptor antagonists with good metabolic stability. These novel analogues possess drug-like