Novel structural analogs of glyphosate based on azoles. 2*. N-Substituted imidazoles and pyrazoles obtained by alkylation of heterocycles containing carboxyl or phosphoryl groups in the ring
作者:N. V. Pavlenko、T. I. Oos、N. V. Kirij、Yu. L. Yagupolskii、A. van Almsick、L. Willms
DOI:10.1007/s10593-011-0777-1
日期:2011.7
Alkylation of 4(5)-substituted 1H-imidazoles using the corresponding reagents gave imidazole 1,4-isomers containing phosphoryl and carboxyl groups together in the ring and in the alkyl fragment. The alkylation of pyrazoles containing a carboxyl group at positions 3(5) and 4 of the ring using diethyl phosphonomethyltriflate has been studied.
The present invention provides a novel compound having a kininogenase-inhibitory action and its pharmaceutical use. The compounds are represented by the formulas (A), (B), (C), (E) and (H):
wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.
Inhibitors of ADAMTS4 or ADAMTS5 for use in preventing or treating cardiac remodeling and chronic heart failure
申请人:Universitetet i Oslo
公开号:US10322143B2
公开(公告)日:2019-06-18
The present invention provides an inhibitor of an ADAMTS proteoglycanase for use in treating or preventing cardiac remodeling or for use in treating or preventing heart failure in a subject. In particular, the present invention provides an inhibitor of ADAMTS4 or ADAMTS5 for use in treating or preventing cardiac remodeling or chronic heart failure in a subject with cardiac remodeling or with chronic heart failure, or with a condition that may lead to cardiac remodeling and/or chronic heart failure. Also provided is a method of treating or preventing cardiac remodeling or treating or preventing heart failure which method comprises administering to a subject in need thereof a therapeutically effective amount of an inhibitor of an ADAMTS proteoglycanase. Also provided is the use of an inhibitor of an ADAMTS proteoglycanase in the manufacture of a medicament for treating or preventing cardiac remodeling or treating or preventing heart failure.