247035-14-9Relevant academic research and scientific papers
Tricyclic pharmacophore-based molecules as novel integrin αvβ3 antagonists. Part 1: Design and synthesis of a lead compound exhibiting αvβ3/ αIIbβ3 dual antagonistic activity
Kubota, Dai,Ishikawa, Minoru,Yamamoto, Mikio,Murakami, Shoichi,Hachisu, Mitsugu,Katano, Kiyoaki,Ajito, Keiichi
, p. 2089 - 2108 (2007/10/03)
In order to generate novel compounds with integrin α vβ3-antagonistic activity together with antiplatelet activity, tricyclic pharmacophore-based molecules were designed and synthesized. Although piperazine-containing compounds initially prepared were selective αIIbβ3 antagonists, replacement of piperazine with piperidine furnished a potent αvβ3/ αIIbβ3 dual antagonist. Structure-activity relationship (SAR) studies provided clues for further development of tricyclic pharmacophore-based integrin antagonists.
Aminopiperidine derivates as integrin αvβ3 antagonists
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, (2008/06/13)
An objective of the present invention is to provide compounds having integrin αvβ3antagonistic activity, cell adhesion inhibitory activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and, therapeutic agents for treating cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases and the like and for inhibiting platelet aggregation. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein A represents a five- to seven-membered heterocyclic group containing two nitrogen atoms or the like; D represents >NH2, >CH2or the like; X and Z represent CH or a nitrogen atom; R7and R8represent alkyl, halogen or the like; Q represents >C═O, >CH2or the like; R9represents H, alkyl, aralkyl or the like; R10represents H, alkynyl or the like; R11represents H, substituted amino or the like; R12represents H or alkyl; m is 0 to 5; n is 0 to 4; p and q are each 1 to 3; and r is 0 or 1.
