89664-09-5Relevant articles and documents
CuCl/bipyridine-catalyzed addition reactions of arylboroxines with aldehydes, α,β-unsaturated ketones, and N-tosyl aldimines
Liao, Yuan-Xi,Hu, Qiao-Sheng
experimental part, p. 7602 - 7607 (2011/11/12)
CuCl/bipyridine-catalyzed addition reactions of arylboroxines with aldehydes and α,β-unsaturated ketones at elevated temperatures were described. By using the microwave energy, CuCl/bipyridine-catalyzed addition reactions of arylboroxines with aldimines were also realized.
Design, synthesis and biological evaluation of piperazine analogues as CB1 cannabinoid receptor ligands
Song, Kwang-Seop,Lee, Sung-Han,Chun, Hyun Ji,Kim, Jong Yup,Jung, Myung Eun,Ahn, Kwangwoo,Kim, Soo-Un,Kim, Jeongmin,Lee, Jinhwa
, p. 4035 - 4051 (2008/09/21)
After the CB1 receptor antagonist SR141716 (rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. Several series of urea, carbamate, amide, sulfonamide and oxalamide derivatives based on 1-benzhydrylpiperazine scaffold were synthesized and tested for CB1 receptor binding affinity. The SAR studies to optimize the CB1 binding affinity led to the potent urea derivatives. After the additional SAR studies to optimize the substituents of diphenyl rings, the combination of 2-chlorophenyl and 4-chlorophenyl turned out to be the most potent scaffold. The CB2 binding affinity assay as well as functional assay was also conducted on these compounds. Herein we wish to introduce several novel CB1 antagonists with IC50 values less than 100 nM for the CB1 receptor binding.
AZETIDINECARBOXAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CB1 RECEPTOR MEDIATED DISORDERS
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Page 52, (2008/06/13)
Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors such as obesity: Formuila (I) wherein: R1 and R2 are independently selected from aryl; and R3 is hydrogen or alkyl; or a pharmaceutically acceptable salt or prodrug thereof, wherein at least one of R1 and R2 has a non-hydrogen substituent in the ortho-position(s) thereof relative to the point of attachment to the [-CH-0-] group.