[EN] HYDRAZIDE, AMIDE, PHTHALIMIDE AND PHTHALHYDRAZIDE ANALOGS AS INHIBITORS OF RETROVIRAL INTEGRASE [FR] ANALOGUES D'HYDRAZIDE, D'AMIDE, DE PHTALIMIDE ET DE PHTALHYDRAZIDE EN TANT QU'INHIBITEURS DE L'INTÉGRASE RÉTROVIRALE
[EN] 4-HYDROXYPIPERIDINE DERIVATIVES AND THEIR USE AS INHIBITORS OF UBIQUITIN SPECIFIC PROTEASE 19 (USP19)<br/>[FR] DÉRIVÉS DE 4-HYDROXYPIPÉRIDINE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE LA PROTÉASE 19 SPÉCIFIQUE DE L'UBIQUITINE
申请人:ALMAC DISCOVERY LTD
公开号:WO2019150119A1
公开(公告)日:2019-08-08
Inhibitors of ubiquitin specific protease 19 (USP19) of Formula (I) are provided, together with pharmaceutical compositions comprising said inhibitors, and methods of use thereof. The compounds can be used in in the treatment of muscular atrophy, obesity, insulin resistance or type II diabetes or in reducing the loss of muscle mass.
The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.
The present invention relates to a compound of formula I
wherein
R
2
R
3
, R
4
, R
5
,
X, n, and o are as defined herein and to a pharmaceutically acceptable acid addition salt thereof which are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
本发明涉及一种具有如下式I的化合物
其中
R
2
R
3
,R
4
,R
5
,
X,n和o如本文所定义,并且其药学上可接受的酸盐,它们是治疗抑郁症、疼痛、精神病、帕金森病、精神分裂症、焦虑和注意力缺陷多动障碍(ADHD)的高潜力NK-3受体拮抗剂。
Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity
作者:Matthew E. Voss、Matthew P. Rainka、Mike Fleming、Lisa H. Peterson、David B. Belanger、M. Arshad Siddiqui、Alan Hruza、Johannes Voigt、Kimberly Gray、Andrea D. Basso
DOI:10.1016/j.bmcl.2012.03.051
日期:2012.5
The structure–activity relationships of new Aurora A/B kinase inhibitors derivedfrom the previously identified kinase inhibitor 12 are described. Introduction of aceticacidamides onto the pyrazole of compound 12 was postulated to influence Aurora A/B selectivity and improve the profile against off-target kinases. The SAR of the aceticacidamides was explored and the effect of substitution on enzyme
描述了源自先前鉴定的激酶抑制剂12的新型Aurora A / B激酶抑制剂的构效关系。假定将乙酰胺引入化合物12的吡唑中会影响Aurora A / B的选择性并改善针对脱靶激酶的作用。探索了乙酸酰胺的SAR,并研究了取代对酶抑制的影响以及基于机理的细胞活性。另外,筛选了几种更有效的抑制剂的脱靶激酶选择性。
SULTAM DERIVATIVES
申请人:Anderson Kevin W.
公开号:US20110124686A1
公开(公告)日:2011-05-26
The present invention relates to compounds according to formula 1,
which exhibit cytotoxic activity. The compounds may be used in the treatment of cancer.