288104-81-4Relevant academic research and scientific papers
Novel pyrazole-3-carboxamide derivatives as cannabinoid-1 (CB1) antagonists: Journey from non-polar to polar amides
Sasmal, Pradip K.,Reddy, D. Srinivasa,Talwar, Rashmi,Venkatesham,Balasubrahmanyam,Kannan,Srinivas,Kumar, K. Shiva,Devi, B. Neelima,Jadhav, Vikram P.,Khan, Sanjoy K.,Mohan, Priya,Chaudhury, Hira,Bhuniya, Debnath,Iqbal, Javed,Chakrabarti, Ranjan
scheme or table, p. 562 - 568 (2011/02/25)
The synthesis and biological evaluation of novel pyrazole-3-carboxamide derivatives as CB1 antagonists are described. As a part of eastern amide SAR, various chemically diverse motifs were introduced. In general, a range of modifications were well tolerat
Imidazol-4-one and Imidazole-4-thione Compounds
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Page/Page column 15, (2010/05/13)
Imidazol-4-one or imidazole-4-thione compounds of formula (I): wherein X, R1, R2, R3, R4, R5, and R6 are defined herein. Also disclosed is a method for treating a cannabinoid receptor-mediated disorder with these compounds.
Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H- pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobes
Wu, Chien-Huang,Hung, Ming-Shiu,Song, Jen-Shin,Yeh, Teng-Kuang,Chou, Ming-Chen,Chu, Cheng-Ming,Jan, Jiing-Jyh,Hsieh, Min-Tsang,Tseng, Shi-Liang,Chang, Chun-Ping,Hsieh, Wan-Ping,Lin, Yinchiu,Yeh, Yen-Nan,Chung, Wan-Ling,Kuo, Chun-Wei,Lin, Chin-Yu,Shy, Horng-Shing,Chao, Yu-Sheng,Shia, Kak-Shan
experimental part, p. 4496 - 4510 (2010/03/01)
By using the active metabolite 5 as an initial template, further structural modifications led to the identification of the titled compound 24 (BPR-890) as a highly potent CB1 inverse agonist possessing an excellent CB2/1 selectivity and remarkable in vivo
Biphenyl-pyrazolecarboxamide compounds
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Page/Page column 30, (2008/06/13)
The present invention relates to biphenyl-pyrazole compounds and in particular biphenyl-pyrazolecarboxamides. The invention further provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by antagonism or inverse agonism of the CB1 receptor, such as obesity, smoking cessation, and normalization of blood lipid composition.
Pyrazolecarboxylic acid derivatives, their preparation, pharmaceutical compositions containing them
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, (2008/06/13)
N-Piperidino-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxamide and its salts and solvates are powerful antagonists of the CB1cannabinoid receptors. They are prepared by reacting a functional derivative of 5-(4-bromophenyl)-
