3095-50-9

Upstream product

• 64-17-5 ethanol 
• 3095-38-3 3,5-dimethyl-4-nitrobenzoic acid 
• 108-67-8 1,3,5-trimethyl-benzene 
• 106567-41-3 2,4,6-trimethyl-3-nitrobenzoic acid 

Downstream Products

• 3095-47-4 4-amino-3,5-dimethylbenzoic acid ethyl ester 
• 1621681-50-2 ethyl 4-(4-chloro-3'-methoxybiphenyl-3-ylcarboxamido)-3,5-dimethylbenzoate 
• 1621680-91-8 4-(2-chloro-5-isobutoxybenzamido)-3,5-dimethylbenzoic acid 
• 1621680-68-9 4-(4-chloro-3'-methoxybiphenyl-3-ylcarboxamido)-3,5-dimethylbenzoic acid 
• 1621681-39-7 ethyl 4-(5-bromo-2-chlorobenzamido)-3,5-dimethylbenzoate 
• 1621681-31-9 4-(2-chloro-5-isobutoxy-N-methylbenzamido)-3,5-dimethylbenzoic acid 

Relevant academic research and scientific papers

Substituted benzamides with activity towards EP4 receptors

The present invention belongs to the field of EP4 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP4 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP4 receptor as well as to pharmaceutical compositions comprising them.

SUBSTITUTED BENZAMIDES WITH ACTIVITY TOWARDS EP4 RECEPTORS

The present invention belongs to the field of EP4 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP4 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP4 receptor as well as to pharmaceutical compositions comprising them.

Effect of the ortho modification of azobenzene on the photoregulatory efficiency of DNA hybridization and the thermal stability of its eis form

We synthesized various azobenzenes methylated at their ortho positions with respect to the azo bond for more effective photoregulation of DNA hybridization. Photoregulatory efficiency, evaluated from the change of T m (ΔTm) induced by trans-cis isomerization, was significantly improved for all ortho-modified azobenzenes compared with non-modified azobenzene due to the more stabilized trans form and the more destabilized cis form. Among the synthesized azobenzenes, 4-carboxy-2',6'- dimethylazobenzene (2',6'-Me-Azo), in which two ortho positions of the distal benzene ring with respect to carboxyl group were methylated, exhibited the largest ΔTm, whereas the newly synthesized 2,6-Me-Azo (4-carboxy-2,6- dimethylazobenzene), which possesses two methyl groups on the two ortho positions of the other benzene ring, showed moderate improvement of ΔTm. Both NMR spectroscopic analysis and computer modeling revealed that the two methyl groups on 2',6'-Me-Azo were located near the imino protons of adjacent base pairs; these stabilized the DNA duplex by stacking interactions in the trans form and destabilized the DNA duplex by steric hindrance in the cis form. In addition, the thermal stability of cis-2',6'-Me-Azo was also greatly improved, but not that of cis2,6-Me-Azo. Solvent effects on the half-life of the cis form demonstrated that cis-to-trans isomerization of all the modified azobenzenes proceeded through an inversion route. Improved thermal stability of 2',6'-Me-Azo but not 2,6-Me-Azo in the eis form was attributed to the retardation of the inversion process due to steric hindrance between lone pair electrons of the π orbital of the nitrogen atom and the methyl group on the distal benzene ring.

Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6- dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp]

A synthesis of the novel tyrosine analogue (2S)-2-methyl-3-(2,6-dimethyl-4- carbamoylphenyl)propanoic acid [(2S)-Mdcp] (15) was developed. In (2S)-Mdcp, the amino and hydroxyl groups of 2′,6′-dimethyltyrosine are replaced by a methyl and a carbamoyl group

Piperazine compounds and medicinal use thereof

The present invention relates to a piperazine compound of the formula wherein R1and R2are each hydrogen, halogen, lower alkyl, lower alkoxy, amino, substituted amino, nitro, hydroxy or cyano, R3, R4and R5are each hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, substituted amino or hydroxy, R6and R7are each hydrogen, lower alkyl, lower alkyl substituted by halogen, aralkyl, acyl or lower acyl substituted by halogen, R8and R9are each hydrogen or lower alkyl, Y is lower alkylene and the like, and ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazyl or imidazolyl, a pharmaceutically acceptable salt thereof and pharmaceutical agents containing these compounds. The compound of the present invention has superior TNF-α production inhibitory effect and/or IL-10 production promoting effect, and, since it is free of or shows only strikingly reduced expression of an effect on the central nervous system, the compound is useful as a highly safe and superior TNF-α production inhibitor an/or IL-10 production promoter and is useful as an agent for the prophylaxis or treatment of various diseases caused by abnormal TNF-α production, diseases curable with IL-10, such as chronic inflammatory diseases, acute inflammatory diseases, inflammatory diseases due to infection, autoimmune diseases, allergic diseases, and TNF-α mediated diseases.