[EN] CASPASE 6 INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE CASPASE 6 ET LEURS UTILISATIONS
申请人:UNIV CALIFORNIA
公开号:WO2021102361A1
公开(公告)日:2021-05-27
Disclosed herein, inter alia, are compounds and methods for inhibiting Caspase 6 and the treatment of diseases, pharmaceutical composition including a compound as described herein and a pharmaceutically acceptable excipient and methods of inhibiting human Caspase 6 protein activity, the method including: contacting the human Caspase 6 protein with a compound as described herein.
Development of 5-hydroxypyrazole derivatives as reversible inhibitors of lysine specific demethylase 1
作者:Daniel P. Mould、Ulf Bremberg、Allan M. Jordan、Matthis Geitmann、Alba Maiques-Diaz、Alison E. McGonagle、Helen F. Small、Tim C.P. Somervaille、Donald Ogilvie
DOI:10.1016/j.bmcl.2017.05.018
日期:2017.7
A series of reversibleinhibitors of lysinespecificdemethylase1 (LSD1) with a 5-hydroxypyrazole scaffold have been developed from compound 7, which was identified from the patent literature. Surface plasmon resonance (SPR) and biochemical analysis showed it to be a reversibleLSD1inhibitor with an IC50 value of 0.23 µM. Optimisation of this compound by rational design afforded compounds with Kd
已经从化合物7开发了具有5-羟基吡唑支架的一系列赖氨酸特异性脱甲基酶1(LSD1)的可逆抑制剂,其已从专利文献中鉴定。表面等离子体共振(SPR)和生化分析表明,它是可逆的LSD1抑制剂,IC 50值为0.23 µM。通过合理设计优化该化合物,可得到K d <10 nM的化合物。在人类THP-1细胞中,发现这些化合物上调替代细胞生物标志物CD86的表达。发现化合物11p在小鼠中具有中等的口服生物利用度,表明其可用作体内工具化合物的潜力。
[EN] MACROCYCLIC INHIBITORS OF PEPTIDYLARGININE DEIMINASES<br/>[FR] INHIBITEURS MACROCYCLIQUES DE PEPTIDYLARGININE DÉIMINASES
申请人:GILEAD SCIENCES INC
公开号:WO2021222353A1
公开(公告)日:2021-11-04
The present disclosure relates to novel compounds for use in therapeutic treatement of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.
[EN] KINASE INHIBITORS<br/>[FR] INHIBITEURS DE KINASES
申请人:GB005 INC
公开号:WO2021247748A1
公开(公告)日:2021-12-09
Disclosed herein are lH-indole-7-carboxamide derivatives as protein kinase inhibitors, in particular Bruton's tyrosine kinase (BTK) inhibitors, pharmaceutical compositions comprising them, processes for preparing them and uses of such protein kinase inhibitors to treat or prevent diseases, disorders and conditions associated with kinase function. In particular, the present invention relates to selective BTK inhibitors.