Approach to dual-acting platelet activating factor (PAF) receptor antagonist/thromboxane synthase inhibitor (TxSI) based on the link of PAF antagonists and TxSIs
摘要:
A series of compounds (22-36) which possess dual-acting PAF antagonist/TxSI have been generated by the approach of linking the known PAF antagonists and TxSIs, such as Ridogrel (1). (C) 2002 Elsevier Science Ltd. All rights reserved.
Heterocyclisch substituierte Cycloalkano[b]-indolsulfonamide können durch Umsetzung von entsprechenden N-unsubstituierten Indolen mit Acrylnitril, anschließende Verseifung, Veresterung oder Amidierung, oder durch Umsetzung von heterocyclisch substituierten Hydrazinen mit Cycloalkanonen oder durch nachträgliches Einführen der heterocyclischen Gruppe in entsprechende Indolderivate hergestellt werden. Die heterocyclisch substituierten Cycloalkano[b]-indolsulfonamide können zur Behandlung von thromboembolischen Erkrankungen, Ischämien, Arteriosklerose, Asthma, Allergien sowie zur Prophylaxe von Myocardinfarkten eingesetzt werden.
SUBSTITUTED PYRAZOLES AS HUMAN PLASMA KALLIKREIN INHIBITORS
申请人:BioCryst Pharmaceuticals, Inc.
公开号:EP3828173A1
公开(公告)日:2021-06-02
Disclosed are compounds of formula (I), as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention and the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
Disclosed are compounds of formula I
as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also disclosed are pharmaceutical compositions comprising at least one such compound, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
公开了式 I 的化合物
及其药学上可接受的盐类。这些化合物是血浆激肽的抑制剂。此外,还公开了包含至少一种此类化合物的药物组合物,以及涉及使用这些化合物和组合物治疗和预防以不需要的血浆激肽活性为特征的疾病和病症的方法。
HUMAN PLASMA KALLIKREIN INHIBITORS
申请人:Biocryst Pharmaceuticals, Inc.
公开号:EP3113772A1
公开(公告)日:2017-01-11
TRIFLUOROMETHYL SUBSTITUTED PYRAZOLES AS HUMAN PLASMA KALLIKREIN INHIBITORS