1576-46-1Relevant articles and documents
BISAMIDE SARCOMERE ACTIVATING COMPOUNDS AND USES THEREOF
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Paragraph 0235-0237, (2019/03/30)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
Design, synthesis, and pharmacological evaluation of highly potent and selective dipeptidyl peptidase-4 inhibitors
Jiang, Tao,Zhou, Yuren,Zhu, Jianming,Chen, Zhuxi,Sun, Peng,Zhang, Qiang,Wang, Zhen,Shao, Qiang,Jiang, Xiangrui,Li, Bo,Wang, Heyao,Zhu, Weiliang,Shen, Jingshan
, p. 399 - 407 (2015/06/08)
The optimization of a series of fused β-homophenylalanine inhibitors of dipeptidyl peptidase-4 (DPP-4) is described. Modification on the P2-binding moiety of 6 (IC50 = 10 nM) led to the discovery of β-homophenylalanine derivatives containing pyrrolidin-2-ylmethyl amides. The introduction of a sulfamine in the meta position of the phenyl ring improved the potency against DPP-4 (6-12-fold increase). Compound 14k showed DPP-4 inhibitory activity with an IC50 value of 0.87 nM. Meanwhile, in vivo experiments exhibited that 14h had an efficiency comparable to sitagliptin at the dose of 10 mg/kg.
NOVEL 1,2,4 OXADIAZOLE COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 60, (2009/12/28)
The invention relates to 1,2,4 oxadiazole compounds and analogs thereof, represented by formula (II), and compositions and methods of use thereof.
