188348-00-7Relevant articles and documents
Design, synthesis, and structure-activity relationship study of conformationally constrained analogs of indole-3-carboxamides as novel CB1 cannabinoid receptor agonists
Kiyoi, Takao,York, Mark,Francis, Stuart,Edwards, Darren,Walker, Glenn,Houghton, Andrea K.,Cottney, Jean E.,Baker, James,Adam, Julia M.
scheme or table, p. 4918 - 4921 (2010/11/04)
Novel tricyclic indole-3-carboxamides were synthesized as structurally restricted analogs of bicyclic indoles, and found to be potent CB1 cannabinoid receptor agonists. The CB1 agonist activity depended on the absolute configuration of the chiral center of the tricyclic ring. The preferred enantiomer was more potent than the structurally unconstrained lead compound. Structure-activity relationships in the amide side chain of the indole C-3 position were also investigated.
PYRIMIDINE-2, 4-DIONE DERIVATIVES AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS
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Page 36, (2010/02/10)
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
Asymmetric synthesis of 1,2-amino alcohols using tert-butanesulfinimines as chiral auxiliary
Ko, Chang Hong,Jung, Doo Young,Kim, Min Kyun,Kim, Yong Hae
, p. 304 - 308 (2007/10/03)
Facile and highly stereoselective synthesis of 1,2-amino alcohols has been achieved by the addition of [(dimethylphenyl-silyl)methyl] magnesium chloride to the tert-butanesulfinimines, followed by Fleming-Tamao oxidation of the silicon moiety.