The present invention provides compounds of the Formula below
wherein R, R1-R3 are as described herein; methods of treating patients for diabetes using the compounds, and processes for preparing the compounds.
The present disclosure provides, inter alia, RAF-Degrading Conjugate Compounds that are useful in the treatment of cancer and other RAF related diseases. Also provided are, pharmaceutical compositions, methods of treatment, and kits comprising a RAF-Degrading Conjugate Compound.
Discovery of LY3325656: A GPR142 agonist suitable for clinical testing in human
作者:Lian Zhu Liu、Tianwei Ma、Jingye Zhou、Zhi Long Hu、Xue Jun Zhang、Hai Zhen Zhang、Mi Zeng、Jia Liu、Lei Li、Yi Jiang、Zack Zou、Fan Wang、Lei Zhang、Jianfeng Xu、Jingru Wang、Fei Xiao、Xiankang Fang、Haixia Zou、Alexander M. Efanov、Melissa K Thomas、Hua V. Lin、Jiehao Chen
DOI:10.1016/j.bmcl.2019.126857
日期:2020.3
The discovery and optimization of a novel series of GPR142 agonists are described. These led to the identification of compound 21 (LY3325656), which demonstrated anti-diabetic benefits in pre-clinical studies and ADME/PK properties suitable for human dosing. Compound 21 is the first GPR142 agonist molecule advancing to phase 1 clinic trials for the treatment of Type 2 diabetes.
HETEROARYL SUBSTITUTED HETEROCYCLYL SULFONES
申请人:GRÜNENTHAL GMBH
公开号:US20170121314A1
公开(公告)日:2017-05-04
The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.