147083-36-1Relevant articles and documents
METHODS FOR THE PREPARATION OF ALCAFTADINE
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Page/Page column 17, (2014/10/15)
The invention relates to new and improved processes for the preparation of Alcaftadine and pharmaceutically acceptable salts thereof as well as an intermediate for the preparation of Alcaftadine. The new process saves a number of steps compared to the known process and results in a higher yield.
Imidazo[2,1-b]benzazepine derivatives, compositions and method of use
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, (2008/06/13)
The present invention is concerned with novel imidazo[2, 1-b][3]benzazepines of formula STR1 the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; R1 represents hydrogen, halo, C1-4 alkyl or C1-4 alkyloxy; R2 represents hydrogen, halo, C1-4 alkyl or C1-4 alkyloxy; R3 represents hydrogen, C1-4 alkyl, ethenyl substituted with hydroxycarbonyl or C1-4 alkyloxycarbonyl, C1-4 alkyl substituted with hydroxycarbonyl or C1-4 alkyloxycarbonyl, hydroxyC1-4 alkyl, formyl or hydroxycarbonyl; R4 represents hydrogen, C1-4 alkyl, hydroxyC1-4 alkyl, phenyl or halo; R5 represents hydrogen, C1-4 alkyl or halo; L represents hydrogen; C1-6 alkyl; C1-6 alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C1-4 alkyloxy, hydroxycarbonyl, C1-4 alkyloxycarbonyl, C1-4 alkyloxycarbonyl-C1-4 alkyloxy, hydroxycarbonylC1-4 alkyloxy, C1-4 alkyloxycarbonylamino, C1-4 alkylaminocarbonyl, C1-4 alkylaminocarbonylamino, C1-4 alkylaminothiocarbonylamino, aryl, aryloxy and arylcarbonyl; C1-6 alkyl substituted with both hydroxy and aryloxy; C3-6 alkenyl; C3-6 alkenyl substituted with aryl; or, L represents a radical of formula --Alk--Y--Het1 (a-1),--Alk--NH--CO--Het2 (a-2)or --Alk--Het3 (a-3); provided that 6,11-dihydro-11-(4-piperidinylidene)-5H-imidazo[2,1-b][3]benzazepine is ecxluded, which are useful antiallergic compounds. Compositions comprising said compounds, methods of using and processes for preparing the same.