552885-77-5

Upstream product

• 405-50-5 p-Fluorophenylacetic acid 
• 385844-15-5 [1-(tert-butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl](4-fluorophenyl)acetic acid 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 
• 385844-14-4 (+/-)-[1-(tert-butoxycarbonyl)-4-hydroxypiperidin-4-yl](4-fluorophenyl)acetic acid 

Downstream Products

• 929268-62-2 4-{1-(4-fluoro-phenyl)-2-[4-(4-naphthalen-1-yl-butyl)-piperazin-1-yl]-2-oxo-ethyl}-piperidine-1-carboxylic acid tert-butyl ester 
• 385844-17-7 tert-butyl 4-(1-(4-fluorophenyl)-2-{4-[4-(2-methoxy-1-naphthyl)butyl]piperazin-1-yl}-2-oxoethyl)piperidine-1-carboxylate 
• 929268-72-4 3-(3'-fluoro-biphenyl-2-yl)-1-{4-[(4-fluoro-phenyl)-(1-isopropyl-piperidin-4-yl)-acetyl]-piperazin-1-yl}-propan-1-one 
• 929268-68-8 3-(3-fluoro-biphenyl-2-yl)-1-{4-[(4-fluoro-phenyl)-(1-isopropyl-piperidin-4-yl)-acetyl]-piperazin-1-yl}-propan-1-one 
• 929268-70-2 3-(2'-fluoro-biphenyl-2-yl)-1-{4-[(4-fluoro-phenyl)-(1-isopropyl-piperidin-4-yl)-acetyl]-piperazin-1-yl}-propan-1-one 
• 929268-66-6 3-(5-fluoro-biphenyl-2-yl)-1-{4-[(4-fluoro-phenyl)-(1-isopropyl-piperidin-4-yl)-acetyl]-piperazin-1-yl}-propan-1-one 
• 929268-67-7 3-(4-fluoro-biphenyl-2-yl)-1-{4-[(4-fluoro-phenyl)-(1-isopropyl-piperidin-4-yl)-acetyl]-piperazin-1-yl}-propan-1-one 
• 929268-65-5 3-(6-fluoro-biphenyl-2-yl)-1-{4-[(4-fluoro-phenyl)-(1-isopropyl-piperidin-4-yl)-acetyl]-piperazin-1-yl}-propan-1-one 
• 929268-74-6 1-[3-(4'-fluorobiphenyl-2-yl)propanoyl]-4-[(4-fluorophenyl)(1-isopropylpiperidin-4-yl)acetyl]piperazine 
• 385844-27-9 1-[(4-fluorophenyl)(1-isopropylpiperidin-4-yl)acetyl]-4-[4-(2-methoxy-1-naphthyl)butyl]piperazine 
• 838819-92-4 3-biphenyl-2-yl-1-[4-[2-(4-fluorophenyl)-2-(1-isopropylpiperidin-4-yl)acetyl]piperazin-1-yl]propane-1-one 
• 929268-63-3 2-(4-fluoro-phenyl)-2-(1-methyl-piperidin-4-yl)-1-[4-(4-naphthalen-1-yl-butyl)-piperazin-1-yl]-ethanone 
• 707542-35-6 1-[2-(4-fluorophenyl)-2-(1-isopropylpiperidin-4-yl)ethyl]-4-(3-biphenyl-2-ylpropyl)piperazine 

Relevant academic research and scientific papers

Novel piperazines: Potent melanocortin-4 receptor antagonists with anxiolytic-like activity

In the present study, we found that a novel piperazine compound, 11a, showed a moderate affinity (IC50 = 333 nM) for the MC4 receptor. We developed the new type of piperazine compounds and found that mono-piperazine 11b exhibited a high-affinity (IC50 = 40.3 nM) for the MC4 receptor. We also found that a series of biphenyl analogues exhibited a high-affinity for the receptor, and in particular, compound 11j exhibited the highest affinity for the MC4 receptor with an IC50 value of 14.5 nM. Furthermore, some of these compounds, when administered orally, significantly reversed the stress-induced anxiety-like behavior in rats. In this paper, we report the synthesis, structure-activity relationships, and oral activity of the novel mono-piperazines as MC4 receptor antagonists.

PIPERAZINE DERIVATIVE

A piperazine derivative represented by the formula (1): ???wherein n is an integer of 1 to 8; R1 represents hydrogen or C1-10 alkyl; A represents CH or nitrogen; Ar1 represents phenyl or substituted phenyl; and Y represents a group represented by the formula Y1-Y2-Ar2 or Y3-Y4(Ar5)-Ar6 or a pharmaceutically acceptable salt of the derivative. The novel piperazine derivative has MC4 receptor antagonistic activity.

Remedial agent for anxiety neurosis or depression and piperazine derivative

There are provided a therapeutic preparation for anxiety neurosis or depression which comprises a MC4 receptor antagonist as an effective ingredient; and a piperazine derivative represented by Formula [1]: [wherein Ar1 is a phenyl gr