681291-92-9Relevant articles and documents
Process development of the synthetic route to R116301
Guillaume, Michel,Cuypers, Jef,Dingenen, Jul
, p. 1079 - 1086 (2012/12/30)
We describe in this paper the synthesis of compound 1 (R116301), which was developed to prepare pilot scale quantities (20-50 kg) of drug substance. The synthesis involves the sBuLi deprotonation of Boc-protected piperidone acetal 2, followed b
SUBSTITUTED 4-(4-PIPERIDIN-4-YL-PIPERAZIN-1-YL)-AZEPANE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS
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, (2008/06/13)
The invention concerns substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in pa
SUBSTITUTED 1-PIPERIDIN-4-YL-4-AZETIDIN-3-YL-PIPERAZINE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS
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, (2010/02/07)
The invention concerns substituted 1-piperidin-4-yl-4-azefdin-3-yl-piperazine having neurokinin antagonistic activity, in particular NK1 and NK1/NK3- antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in pa