32177-89-2Relevant academic research and scientific papers
Discovery of N-{(1S,2S)-2-(3-cyanophenyl)-3-[4-(2-[18F] fluoroethoxy)phenyl]-1-methylpropyl}-2-methyl-2-[(5-methylpyridin-2-yl)oxy] propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use
Liu, Ping,Lin, Linus S.,Hamill, Terence G.,Jewell, James P.,Lanza Jr., Thomas J.,Gibson, Raymond E.,Krause, Stephen M.,Ryan, Christine,Eng, Waisi,Sanabria, Sandra,Tong, Xinchun,Wang, Junying,Levorse, Dorothy A.,Owens, Karen A.,Fong, Tung M.,Shen, Chun-Pyn,Lao, Julie,Kumar, Sanjeev,Yin, Wenji,Payack, Joseph F.,Springfield, Shawn A.,Hargreaves, Richard,Burns, H. Donald,Goulet, Mark T.,Hagmann, William K.
, p. 3427 - 3430 (2008/02/10)
The discovery of a structurally distinct cannabinoid-1 receptor (CB1R) positron emission tomography tracer is described. Starting from an acyclic amide CB1R inverse agonist (1) as the lead compound, an efficient route to introduce 18F to the mo
PRO-DRUGS OF TERTIARY ALCOHOLS
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Page/Page column 42, (2008/06/13)
The compounds of the present invention are prodrugs of modulators of the Cannabinoid-1 (CB 1 ) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the Cannabinoid- 1 (CB 1) receptor. In particular, compounds of the
Discovery of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1- methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity
Lin, Linus S.,Lanza Jr., Thomas J.,Jewell, James P.,Liu, Fing,Shah, Shrenik K.,Qi, Hongbo,Tong, Xinchun,Wang, Junying,Xu, Suoyu S.,Fong, Tung M.,Shen, Chun-Pyn,Lao, Julie,Xiao, Jing Chen,Shearman, Lauren P.,Stribling, D. Sloan,Rosko, Kimberly,Strack, Alison,Marsh, Donald J.,Feng, Yue,Kumar, Sanjeev,Samuel, Koppara,Yin, Wenji,Van Der Ploeg, Lex H. T.,Goulet, Mark T.,Hagmann, William K.
, p. 7584 - 7587 (2007/10/03)
The discovery of novel acyclic amide cannabinoid-1 receptor inverse agonists is described. They are potent, selective, orally bioavailable, and active in rodent models of food intake and body weight reduction. A major focus of the optimization process was to increase in vivo efficacy and to reduce the potential for formation of reactive metabolites. These efforts led to the identification of compound 48 for development as a clinical candidate for the treatment of obesity.
ACYCLIC HYDRAZIDES AS CANNABINOID RECEPTOR MODULATORS
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Page/Page column 44, (2010/11/08)
The acyclic hydrazides of the invention are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present inventio
RADIOLABELED CANNABINOID-1 RECEPTOR MODULATORS
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Page/Page column 38, (2010/02/10)
The present invention relates to particular radiolabeled Cannabinoid-1 (CB1) receptor modulators, and methods of using these modulators for labeling and diagnostic imaging of Cannabinoid-1 receptors in mammals, particularly humans. In addition, intermediates useful for the synthesis of the radiolabeled Cannabinoid-1 receptor modulators are also disclosed, as well as the processes for synthesizing the radiolabeled Cannabinoid-1 receptor modulators. Still further, formulations of the radiolabeled Cannabinoid-1 receptor compounds are described.
SUBSTITUTED AMIDES ACTIVE AT THE CANNABINOID-1 RECEPTOR
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Page 40-41, (2010/02/07)
Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
