233283-14-2

Upstream product

• 451-46-7 4-fluorobenzoic acid ethyl ester 

Downstream Products

• 179488-71-2 4-[4-(pyrimidin-2-yl)piperazin-1-yl]benzaldehyde 
• 234080-97-8 (2S)-benzenesulfonylamino-3-[benzyl-[4-{4-(pyrimidin-2-yl)-piperazin-1-yl}-benzyl]-amino]-propionic acid 
• 234080-99-0 t-butyl (2S)-benzyloxycarbonylamino-3-[4-{4-(pyrimidin-2-yl)-piperazin-1-yl}-benzoylamino]-propionate 
• 234081-18-6 2-(benzenesulfonyl-methyl-amino)-3-[4-(4-pyrimidin-2-yl-piperazin-1-yl)-benzoylamino]-propionic acid tert-butyl ester 
• 234080-72-9 t-butyl (2S)-benzenesulfonylamino-3-[4-{4-(pyrimidin-2-yl)-piperazin-1-yl}-benzoylamino]-propionate 
• 234080-92-3 tert-butyl (2S)-benzenesulfonylamino-3-[4-{4-(pyrimidin-2-yl)piperazin-1-yl}benzylamino]propionate 
• 234081-00-6 (2S)-benzyloxycarbonylamino-3-[4-{4-(pyrimidin-2-yl)-piperazin-1-yl}-benzoylamino]-propionic acid 
• 234080-73-0 (2S)-benzenesulfonylamino-3-[4-{4-(pyrimidin-2-yl)-piperazin-1-yl}-benzoylamino]-propionic acid 
• 234081-19-7 2-(N-benzenesulfonyl-N-methylamino)-3-[4-{4-(pyrimidin-2-yl)piperazin-1-yl}benzoylamino]propionic acid 
• 234080-93-4 (2S)-benzenesulfonylamino-3-[4-{4-(pyrimidin-2-yl)-piperazin-1-yl}-benzylamino]-propionic acid 
• 234080-95-6 (2S)-benzenesulfonylamino-3-[methyl-[4-{4-(pyrimidin-2-yl)-piperazin-1-yl}-benzyl]-amino]-propionic acid 
• 234081-02-8 (2S)-amino-3-[4-{4-(1,4,5,6-tetrahydropyrimidin-2-yl)-piperazin-1-yl}-benzoylamino]-propionic acid 
• 882531-28-4 ethyl (3S)-[4-{4-(pyrimidin-2-yl)piperazin-1-yl}benzoylamino]pent-4-ynate 
• 234081-70-0 ethyl 3-[4-{4-(pyrimidin-2-yl)-piperazin-1-yl}-benzoylamino]-propionate 

Relevant 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

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.

Phenylpiperazine derivatives as integrin αvβ3 antagonists

An objective of the present invention is to provide compounds having integrin αvβ3 antagonistic activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and therapeutic agents for treating integrin αvβ3-mediated diseases 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 ring containing two nitrogen atoms or the like; X and Z represent CH or a nitrogen atom; R4 and R5 represent alkyl, halogen or the like; Q represents >C=O, >CH2 or the like; R6 represents H, alkyl, aralkyl or the like; R7 represents H, alkynyl or the like; R8 represents H, substituted amino or the like; R9 represents H or alkyl; m is 0 to 5; n is 0 to 4; p is 2 or 3; and q is 0 or 1.