137075-32-2

Upstream product

• 67199-13-7 N-(2,2-diphenylacetyl)piperazine 
• 67199-20-6 1-Diphenylacetyl-4-formylpiperazine 
• 117-34-0 2,2-diphenylacetic acid 
• 137075-31-1 1-(diphenylacetyl)-4-<2-(3-pyridyl)-2-oxoethyl>piperidine 

Downstream Products

• 137074-71-6 1-(diphenylacetyl)-4-(2-(pyridin-3-yl)-2-cyanoethyl)-piperazine 
• 143840-91-9 1-[4-(2-Chloro-2-pyridin-3-yl-ethyl)-piperazin-1-yl]-2,2-diphenyl-ethanone 

Relevant academic research and scientific papers

(Pyridylcyanomethyl)piperazines as orally active PAF antagonists

A series of (pyridylcyanomethyl)piperazines was prepared and evaluated for PAF-antagonist activity. Compounds were tested in vitro in a PAF-induced platelet aggregation assay and in vivo in a PAF-induced hypotension test in normotensive rats. Oral activity was ascertained through a PAF-induced mortality test in mice. The main structure-activity trends of the series were established. Activity was mainly found in four skeletons: 1-acyl-4-(3- pyridylcyanomethyl)-piperazine, 1-acyl-4-(4-pyridylcyanomethyl)piperazine, 1- acyl-4-(3-pyridylcyanomethyl)piperidine, and 1-acyl-4-cyano-4-(3- pyridylamino)piperidine. The acyl substituents, diphenylacetyl and 3,3- diphenylpropionyl, provided the most active compounds, and the introduction of an amine or hydroxy group in the 3,3-diphenylpropionyl substituent led to further improvement in oral activity. As a result, three of the most active compounds (100, 114, and 115) have been selected for further pharmacological development.

(cyanomethyl)pyridines useful as PAF antagonists

57 The present invention relates to new (cyanomethyl)pyridines of general formula I: wherein Ais nitrogen and Bis -CH-, or Bis nitrogen and Ais -CH-; the group Y-W-represents a group of formula N-CR1(CN)-, N-CH2-CH(CN)-, CH-CH(CN)- or C=C(CN)- wherein R1 is hydrogen or a C1-C6 alkyl group; Rrepresents a group of formula R2CO-,R3R4N-(CH2)nCO- or R5-(CH2)m- wherein R2 represents C1-C15 alkyl, aryl, aryl-(C1-C6)-alkyl, aryl-(C1-C6)-alkenyl, diaryl-(C1-C6)-alkyl, diaryl-(C1-C6)-alkenyl, arylhydroxy-(C1-C6)-alkyl, diarylhydroxy-(C1-C6)-alkyl, aryl-(C1-C6)-alkoxy, diaryl-(C1-C6)-alkoxy, or heteroaryl-(C1-C6)-alkyl group; n is 0, 1, 2 or 3; R3 is hydrogen, C1-C6 alkyl, aryl or aryl-(C1-C6)-alkyl group; R4 is C3-C6 cycloalkyl, aryl, aryl-(C1-C6)-alkyl, diaryl-(C1-C6)-alkyl, aryl-(C1-C6)-alkylcarbonyl or diaryl-(C1-C6)-alkylcarbonyl group; m is 0, 1 or 2; and R5 is aryl-(C1-C6)-alkyl, diaryl-(C1-C6)-alkyl, diaryl-(C1-C6)-alkylcarbonylamino or diaryl-(C1-C6)-alkylaminocarbonyl group. These compounds are potent, orally active PAF antagonists and consequently, useful in the treatment of the diseases in which this substance is involved.