626219-95-2

Upstream product

• 146137-78-2 2-fluoro-5-trifluoromethylbenzaldehyde 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 914347-13-0 C₁₂H₁₃F₃N₂O 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 869478-23-9 4-{2-[((S_S)-2-methyl-propane-2-sulfinylimino)-methyl]-4-trifluoromethyl-phenyl}-piperazine-1-carboxylic acid tert-butyl ester 
• 910300-22-0 4-{2-[1-(2-methyl-propane-2-sulfinylamino)-pentyl]-4-trifluoromethyl-phenyl}-piperazine-1-carboxylic acid tert-butyl ester 
• 626212-09-7 2-{4-[3-(2,4-dichlorophenyl)propionyl]-1-piperazinyl}-1-[1S-amino-3-methbutyl]-5-trifluoromethylbenzene 
• 626212-33-7 1-{4-[2-((S)-1-Amino-2-methyl-butyl)-4-trifluoromethyl-phenyl]-piperazin-1-yl}-3-(2,4-dichloro-phenyl)-propan-1-one 

Relevant academic research and scientific papers

(2-benzylphenyl)piperazine derivatives and use thereof

The invention discloses (2-benzylphenyl)piperazine derivatives, a use thereof, and a medicinal composition comprising above compounds. The derivatives and the medicinal composition are used for inhibiting serotonin reuptake. The invention also relates to

CHEMICAL COMPOUNDS 251

The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.

Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor

Benzylamine and pyridinemethylamine derivatives were synthesized and characterized as potent and selective antagonists of the melanocortin-4 receptor (MC4R). These compounds were also profiled in rodents for their pharmacokinetic properties. Two compounds with diversified profiles in chemical structure, pharmacological activities, and pharmacokinetics, 10 and 12b, showed efficacy in an established murine cachexia model. For example, 12b had a Ki value of 3.4 nM at MC4R, was more than 200-fold selective over MC3R, and had a good pharmacokinetic profile in mice, including high brain penetration. Moreover, 12b was able to stimulate food intake in the tumor-bearing mice and reverse their lean body mass loss. Our results provided further evidence that a potent and selective MC4R antagonist with appropriate pharmacokinetic properties might potentially be useful for the treatment of cancer cachexia.

Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor

A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was found to be increased by replacing the α-methyl substituent of the initial lead 11 with a larger s-Bu or i-Bu group. Further potency enhancement was observed when a glycine or β-alanine was incorporated onto the benzylamine. Some compounds demonstrated good potency, moderate selectivity, and oral bioavailability.

Practical asymmetric synthesis of α-branched 2- piperazinylbenzylamines by 1,2-additions of organometallic reagents to N-tert-butanesulfinyl imines

2-[4-(tert-Butoxycarbonyl)piperazinyl] benzylidene-tert-butanesulfinamides underwent nucleophilic 1,2-addition with different organometallic reagents to give highly diastereomerically enriched adducts. X-ray crystallography of the resulting α-branched N-B

LIGANDS OF MELANOCORTIN RECEPTORS AND COMPOSITIONS AND METHODS RELATED THERETO

Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders. The compounds have the following structure (I): (R4)s (R 2)n N~ X1-X2 (CR1aCRlb)q 1~ N R1-lm 1 O R3 (I) including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein m, n, q, s, R1, R1a, R1b, R2, R3, R4, X1 X2 and X3 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.

LIGANDS OF MELANOCORTIN RECEPTORS AND COMPOSITIONS AND METHODS RELATED THERETO

Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders. The compounds have the following structure (I): (I) including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein m, n, q, s, R1, R1a, R1b, R2, R3, R4a, R4b, R5a, R5b, X1, X2, X3, X4 and Ar are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.