64201-30-5

Upstream product

• 4654-08-4 5-(4'-hydroxyphenyl)pentanoic acid 
• 18107-18-1 diazomethyl-trimethyl-silane 
• 67-56-1 methanol 
• 68486-77-1 3-(4-(benzyloxy)phenyl)propanal 
• 50463-48-4 3-(4-benzyloxyphenyl)propanoic acid 
• 501-97-3 4-hydroxyphenylpropionic acid 
• 129649-59-8 (E)-5-(4-Benzyloxy-phenyl)-pent-2-enoic acid methyl ester 

Downstream Products

• 1415712-24-1 methyl 5-(4-hydroxyphenyl)pentanoate 
• 1415712-00-3 C₂₄H₃₂N₂O₄*ClH 
• 955360-14-2 5-(4-[3-(hexahydro-1H-azepin-1-yl)propoxy]phenyl)pentyl methanesulfonate 
• 955360-13-1 5-(4-[3-(hexahydro-1H-azepin-1-yl)propoxy]phenyl)-1-pentanol 
• 1079821-75-2 C₁₄H₁₉BrO₃ 
• 4654-08-4 5-(4'-hydroxyphenyl)pentanoic acid 
• 113378-80-6 2-<3-(4-hydroxyphenyl)propyl>-1,3-indandione 
• 166959-43-9 5-(3-Allyl-4-trifluoromethanesulfonyloxy-phenyl)-pentanoic acid methyl ester 
• 955360-12-0 methyl 5-(4-[3-(hexahydro-1H-azepin-1-yl)propoxy]phenyl)pentanoate 

Relevant academic research and scientific papers

2,3,4-Trihydroxybenzyl-hydrazide analogues as novel potent coxsackievirus B3 3C protease inhibitors

Human coxsackievirus B3 (CVB3) 3C protease plays an essential role in the viral replication of CVB3, which is a non-enveloped and positive single-stranded RNA virus belonging to Picornaviridae family, causing acute viral myocarditis mainly in children. During optimization based on SAR studies of benserazide (3), which was reported as a novel anti-CVB3 3Cpro agent from a screening of compound libraries, the 2,3,4-trihydroxybenzyl moiety of 3 was identified as a key pharmacophore for inhibitory activity against CVB3 3Cpro. Further optimization was performed by the introduction of various aryl-alkyl substituted hydrazide moieties instead of the serine moiety of 3. Among the optimized compounds, 11Q, a 4-hydroxyphenylpentanehydrazide derivative, showed the most potent inhibitory activity (IC50 Combining double low line 0.07 μM). Enzyme kinetics studies indicated that 11Q exhibited a mixed inhibitory mechanism of action. The antiviral activity against CVB3 was confirmed using the further derived analogue (14b) with more cell permeable valeryl ester group at the 2,3,4-trihydroxy moiety.

Composition and kit comprising piperazine derivatives and metformin, and use thereof in the treatment of diabetes

The present invention relates to a composition comprising, in combination, metformin or a salt thereof, a pharmaceutically acceptable carrier or excipient and at least one compound of formula (I), the enantiomers, diastereoisomers or pharmaceutically acceptable salts thereof. Formula (I). The present invention also relates to the use of said composition for the treatment of diseases associated with insulin resistance syndrome.

PIPERAZINE DERIVATIVES, METHODS FOR PREPARING SAME, AND USES THEREOF IN THE TREATMENT OF INSULIN RESISTANCE

The invention relates to a compound of formula (I), where R1, R2, R3, m, n, and L1 are as defined in claim 1, to the methods for preparing same, to the pharmaceutical compositions containing same, and to the use

Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles

A nonpeptidyl GnRH receptor antagonist (1), with a unique 2-arylindole core, was identified through the Merck in-house screening for binding affinity on the rat GnRH receptor. SAR studies directed toward the alkoxy-ethanolamine and 2-aryl groups resulted in a simpler lead structure with improved activity. This compound 50 exhibits a 60-fold improvement in binding activity over our initial lead 1.