15997-90-7Relevant academic research and scientific papers
ADAMTS INHIBITORS, PREPARATION METHODS AND MEDICINAL USES THEREOF
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, (2021/08/13)
Compounds of formula (I) useful as inhibitors of ADAMTS-5 and/or ADAMTS-4, pharmaceutical compositions thereof, and use of them as therapeutic agents for the treatment of diseases involving degradation of cartilage or disruption of cartilage homeostasis, in particular osteoarthrosis and/or rheumatoid arthritis, are disclosed.
Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors
Tsai, Ting-Yueh,Coumar, Mohane Selvaraj,Hsu, Tsu,Hsieh, Hsing-Pang,Chien, Chia-Hui,Chen, Chiung-Tong,Chang, Chung-Nien,Lo, Yu-Kang,Wu, Ssu-Hui,Huang, Chung-Yu,Huang, Yu-Wen,Wang, Min-Hsien,Wu, Hsin-Yi,Lee, Hong-Jen,Chen, Xin,Chao, Yu-Sheng,Jiaang, Weir-Torn
, p. 3268 - 3272 (2007/10/03)
A series of substituted pyrrolidine-2,4-dicarboxylic acid amides were synthesized as potential antidiabetic agents, and many of them showed good in vitro DPP-IV inhibition (IC50 = 2-250 nM) with selectivity over DPP-II, DPP8, and FAP enzymes. Selected compounds 8c and 11a showed in vivo plasma DPP-IV inhibition after oral administration in Wistar rats.
COMPOUND INHIBITING DIPEPTIDYL PEPTIDASE IV
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Page/Page column 28, (2010/02/14)
The invention aims to provide a dipeptidyl peptidase IV inhibitor which is satisfactory in respect of activity, stability and safety and has an excellent action as a pharmaceutical agent. The invention is directed to a compound represented by the following general formula or a pharmaceutically acceptable salt thereof: wherein R1 and R2 each represents hydrogen, an optionally substituted C1-6 alkyl group, or -COOR5 whereupon R5 represents hydrogen or an optionally substituted C1-6 alkyl group, or R1 and R2, together with a carbon atom to which they are bound, represent a 3- to 6-membered cycloalkyl group, R3 represents hydrogen or an optionally substituted C6-10 aryl group, R4 represents a hydrogen or a cyano group, D represents -CONR6-, -CO- or -NR6CO-, R6 represents hydrogen or an optionally substituted C1-6 alkyl group, E represents -(CH2)m- whereupon m is an integer of 1 to 3, -CH2OCH2-, or -SCH2-, n is an integer of 0 to 3, and A represents an optionally substituted bicyclic heterocyclic group or bicyclic hydrocarbon group.
