New efficient asymmetric synthesis of taranabant, a CB1R inverse agonist for the treatment of obesity
Taranabant (1) is a cannabinoid-1 receptor (CB1R) inverse agonist that was recently in late-stage clinical development for the treatment of obesity. The previously employed synthesis exhibited a number of shortcomings for continuing development, and in th
Crump, Brian R.,Phenix, Brian D.,Spindler, Felix,Wallace, Debra J.,Campos, Kevin R.,Shultz, C. Scott,Klapars, Artis,Zewge, Daniel,McWilliams, J. Christopher,Krska, Shane,Sun, Yongkui,Chen, Cheng-Yi
scheme or table
p. 84 - 90
(2010/04/22)
COMBINATION OF DIPEPTIDYL PEPTIDASE-IV INHIBITOR AND A CANNABINOID CB1 RECEPTOR ANTAGONIST FOR THE TREATMENT OF DIABETES AND OBESITY
The present invention relates to pharmaceutical compositions comprising a combination of a particular dipeptidyl peptidase-IV (DPP-IV) inhibitor and a particular cannabinoid CB?1#191 receptor antagonist/inverse agonist, kits containing such combinations and methods of using such compositions for the treatment of diabetes, diabetes associated with obesity, diabetes-related disorders, obesity, and obesity-related disorders.
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(2008/06/13)
FORMATION OF TETRA-SUBSTITUTED ENAMIDES AND STEREOSELECTIVE REDUCTION THEREOF
The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compo
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Page/Page column 18; 25-26
(2008/06/13)
Cyanation of aromatic halides
A practical, ligand-free cyanation of aryl bromides employs Pd catalyst in combination with a non-toxic cyanide source, Mn[Fe(CN)6] (M=K or Na; n is 3 or 4), or a hydrate thereof, and a base. The reactions are performed in a polar aprotic solvents and provide the corresponding aryl nitrile in 83-96% yield, typically in less than 5 h.
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Page/Page column 4-5; 9
(2008/06/13)
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