[EN] POLYCYCLIC DERIVATIVE MODULATOR, AND PREPARATION METHOD THEREFOR AND USE THEREOF [FR] MODULATEUR DE DÉRIVÉ POLYCYCLIQUE, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION [ZH] 多环类衍生物调节剂、其制备方法和应用
This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.
[EN] INHIBITORS OF ADRENORECEPTOR ADRAC2<br/>[FR] INHIBITEURS DE L'ADRÉNORÉCEPTEUR ADRAC2
申请人:BAYER AG
公开号:WO2021089683A1
公开(公告)日:2021-05-14
The present application relates to novel substituted heterocyclic carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases and to their use for producing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of breathing difficulties including sleep-induced breathing difficulties such as central and obstructive sleep apnoea, snoring (primary and obstructive snoring), dysphagia, peripheral and cardiac vascular disorders including diabetic microangiopathies and disorders of the peripheral and central nervous system including neurodegenerative and neuroinflammatory disorders.
[EN] COMBINATION OF AN ALPHA2-ADRENOCEPTOR SUBTYPE C (ALPHA-2C) ANTAGONIST WITH A TASK1/3 CHANNEL BLOCKER FOR THE TREATMENT OF SLEEP APNEA<br/>[FR] COMBINAISON D'ANTAGONISTES D'UN SOUS-TYPE C DE RÉCEPTEUR α2-ADRÉNERGIQUE (ALPHA-2C) AVEC UN BLOQUEUR DE CANAL TASK1/3 POUR LE TRAITEMENT DE L'APNÉE DU SOMMEIL
申请人:BAYER AG
公开号:WO2022008426A1
公开(公告)日:2022-01-13
The present invention relates to a combination of selective blockers of TASK- 1 and TASK-3 channels, in particular substituted imidazo [ 1,2-a]pyrimidine and substituted imidazo [ 1,2-a]pyridine derivatives of formula (II) and α2 -Adrenoceptor subtype C (alpha-2C) antagonists, in particular substituted heterocyclic carboxamides of formula (I) for the treatment and/or prophylaxis of sleep-related breathing disorders, preferably obstructive and central sleep apneas and snoring.
[EN] POLYCYCLIC DERIVATIVE MODULATOR, AND PREPARATION METHOD THEREFOR AND USE THEREOF<br/>[FR] MODULATEUR DE DÉRIVÉ POLYCYCLIQUE, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION<br/>[ZH] 多环类衍生物调节剂、其制备方法和应用
The optimization of pyridazinone series of glucan synthase inhibitors
作者:Rongze Kuang、Heping Wu、Pauline C. Ting、Robert G. Aslanian、Jianhua Cao、David W. Kim、Joe F. Lee、John Schwerdt、Gang Zhou、R. Jason Herr、Andrew J. Zych、Jinhai Yang、Sang Q. Lam、David M. Jenkins、Samuel A. Sakwa、Samuel Wainhaus、Todd A. Black、Anthony Cacciapuoti、Paul M. McNicholas、Yiming Xu、Scott S. Walker
DOI:10.1016/j.bmcl.2012.06.091
日期:2012.8
A detailed structure-activity relationship study of a novel series of pyridazine-based small molecule glucan synthase inhibitors is described. The optimization of the PK profile of this series led to the discovery of compound 11g, which demonstrated in vivo potency ip in a lethal fungal infection model. (c) 2012 Elsevier Ltd. All rights reserved.