Application of the QbD principles in the development of the casopitant mesylate manufacturing process. Process research studies for the definition of the control strategy of some drug substance-CQAs for stages 2a, 2b, and 2c
Casopitant was identified as a potent NK1 antagonist by GlaxoSmithKline (GSK). It was selected as part of a wide drug discovery programme within GSK for its potential activities on a number of therapeutic targets such as inflammatory bowel dise
Highly enantioselective formal aza-Diels-Alder reactions with acylhydrazones and Danishefsky's diene promoted by a silicon Lewis acid
Silicon Lewis acid 3 is effective for the promotion of highly enantioselective cycloaddition reactions of acylhydrazones with Danishefsky's diene (formal aza-Diels-Alder reactions). The reactions are conducted at ambient temperature for 15 min, and produc
Lee, Sharon K.,Tambar, Uttam K.,Perl, Nicholas R.,Leighton, James L.
experimental part
p. 4769 - 4774
(2010/08/07)
Chemical compounds
Formula (1) wherein R represents a halogen atom or a C1-4 alkyl group; R1 represents a C1-4 alkyl group; R2 represents hydrogen or a C1-4 alkyl group; R3 represents hydrogen, or a C1-4 alkyl group; R4 represents a trifluorometyl group; R5 represents hydrogen, a C1-4 alkyl group or C(0)R6; R6? represents C1-4 alkyl, C3-7 cycloalkyl, NH(C1-4 alkyl) or N(C1-4alkyl)2; m is zero or an integer from 1 to 3; n is an integer from 1 to 3 and pharmaceutically acceptable salts and solvates thereof; to processes for their preparation and their use in the treatment of conditions mediated bytachykinins.
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Page/Page column 13
(2010/02/05)
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