Brian Austad - Tewksbury MA, US Farid Benayoud - North Andover MA, US Trevor Calkins - Stoughton WI, US Silvio Campagna - Candia NH, US Charles E. Chase - Londonderry NH, US William Christ - Andover MA, US Francis G. Fang - Andover MA, US Yongbo Hu - Westborough MA, US Bryan M. Lewis - North Brunswick NJ, US Marc Pesant - Saint-Colomban, CA Matthew Schnaderbeck - Methuen MA, US Gordon Wilkie - North Andover MA, US Xiaojie Zhu - Andover MA, US
Taiju Nakamura - Kamisu, JP Masaaki Matsuda - Tsukuba, JP Yongbo Hu - Chestnut Hill MA, US Daiju Hasegawa - Tsukuba, JP Yorihisa Hoshino - Tsukuba, JP Kazato Inanaga - Kamisu, JP Minetaka Isomura - Kamisu, JP Nobuaki Sato - Tsukuba, JP Kazuhiro Yoshizawa - Kamisu, JP George A. Moniz - Cambridge MA, US Gordon D. Wilkie - North Andover MA, US Francis G. Fang - Andover MA, US Yoshihiro Nishikawa - Kamisu, JP
Assignee:
EISAI R&D MANAGEMENT CO., LTD. - Tokyo
International Classification:
C07D 471/04 C07C 257/06 C07D 401/14 C07D 401/04
US Classification:
546119, 558 6, 546194, 5462741
Abstract:
This invention relates to a new synthesis, intermediates and precursors leading to a mixture of the compounds 11 and 12 as shown below. It also relates to the resolution of the stereoisomeric mixture to provide in substantial stereochemical purity compound 12. The synthesis of the invention involves preparation of compound 7 and compound 10 as shown below and their reaction to prepare a mixture of compound 11 and compound 12.
Salt And Crystal Forms Of An Activin Receptor-Like Kinase Inhibitor
- Cambridge MA, US Debra Mazaik - Cambridge MA, US Gordon Wilkie - Cambridge MA, US Joshua D. Waetzig - Cambridge MA, US Brian Heinrich - Cambridge MA, US Lauren MacEachern - Dartmouth, CA Dominik Siegel - Dottikon, CH Harald Ohmer - Dottikon, CH Steven C. Johnston - Woburn MA, US
International Classification:
C07D 487/04
Abstract:
Various salt forms of Compound (I) represented by the following structural formula, and their corresponding pharmaceutical compositions, are disclosed. Particular single crystalline forms of 1:1.5 Compound (I) succinate, 1:1 Compound (I) hydrochloride salt, and 1:1 Compound (I) fumarate salt are characterized by a variety of properties and physical measurements. Methods of preparing specific crystalline forms are also disclosed. The present disclosure also provides methods of treating or ameliorating fibrodysplasia ossificans progressive in a subject.
Crystalline Forms Of (S)-1-(4-Fluorophenyl)-1-(2-(4-(6-(1-Methyl-1H-Pyrazol-4-Yl)Pyrrolo[2,1-F][1,2,4]Triazin-4-Yl)Piperazinyl)-Pyrimidin-5-Yl)Ethan-1-Amine And Methods Of Making
- Cambridge MA, US Brenton Mar - Cambridge MA, US Brian Heinrich - Cambridge MA, US Gordon Wilkie - Cambridge MA, US Lauren MacEachern - Dartmouth, CA
International Classification:
C07D 487/04 A61P 35/00 A61P 17/00
Abstract:
Crystalline Forms of Compound (I):pharmaceutically acceptable salts thereof and solvates of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating disorders and conditions associated with oncogenic KIT and PDGFRA alterations using the same, and methods for making Compound (I) and crystalline forms thereof are also disclosed.