39887-54-2

Upstream product

• 75-31-0 isopropylamine 
• 38818-50-7 4-chloro-3-nitro-benzoyl chloride 

Downstream Products

• 1201900-87-9 C₁₉H₂₀N₂O₇ 
• 1403353-77-4 N-isopropyl-3-nitro-4-(piperazin-1-yl)benzamide 

Relevant academic research and scientific papers

Development and characterization of endocannabinoid hydrolases FAAH and MAGL inhibitors bearing a benzotriazol-1-yl carboxamide scaffold

A series of (1H-benzo[d][1,2,3]triazol-1-yl)(4-benzylpiperazin-1-yl) methanones and of (1H-benzo[d][1,2,3]triazol-1-yl)(4-phenylpiperazin-1-yl) methanones has been prepared and tested on human fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). In the benzylpiperazinyl series, compound 29 (ML30) exhibited an IC50 value of 0.54 nM on MAGL, combined with a 1000-fold selectivity versus FAAH, while compounds 11 and 16 acted as potent dual FAAH-MAGL inhibitors (IC50 50 values against MAGL in the nanomolar range, whilst being between one and two orders of magnitude less potent on the FAAH, while compounds 31 and 32 were potent FAAH inhibitors (IC50 20 nM) and over 12-fold selective versus MAGL. The key structural determinants driving the structure-activity relationships were explored by the minimization of the inhibitors inside the active site of both enzymes.

Discovery and optimization of CRTH2 and DP dual antagonists

A series of phenylacetic acid derivatives was discovered as CRTH2 antagonists. Modification of the series led to compounds that are also antagonists of DP. Since activation of CRTH2 and DP are believed to play key roles in mediating responses of asthma and other immune diseases, this series was optimized to increase the dual antagonistic activities and improve pharmacokinetic properties. These efforts led to selection of AMG 009 as a clinical candidate.

P2x7 receptor antagonists for use in the treatment of inflammatory, immune or cardiovascular diseases

The invention provides piperidine compounds of general formula (I) in which A, B, X, Y, Z, R, R1 and R2 are as defined in the specification, their use as medicaments, compositions containing them and processes for their for their preparation.