Ariad Pharmaceuticals, Inc.

Johnson Matthey Public Limited Company

Takeda Pharmaceutical Company Limited

Craig, Stuart Wilbert

Pradeep Kumar Sharma

Leonard W Rozamus

Christopher K Murray

John J Chaber

Jurjus Jurayj

Derek Wyndham Clissold

Rajendrakumar Reddy Gadikota

Min He

Shahrokh Kazerani

Erwin Rannala

Stuart Wilbert Craig

Jurjus Fayez Jurayj

Marianne Langston

Landon J Durak

Thai Hiep Nguyen

Xiaoguang Zhang

Shuanglian Li

The present disclosure relates to pharmaceutical salts and polymorphic forms of pyrimidine derivatives that have inhibitory activities against mutant epidermal growth factor receptor (EGFR). The present disclosure further relates to the processes for the preparation of the pyrimidine derivatives and to the pharmaceutical salts and the polymorphic forms of the pyrimidine derivatives.

Pharmaceutical salts of pyrimidine derivatives and method of treating disorders

Novel crystalline forms of brigatinib, pharmaceutical compositions comprising the same, and methods of their preparation and use of the same are disclosed herein.

Crystalline forms of 5-chloro-N4-[-2-(dimethylphosphoryl) phenyl]-N2-{2-methoxy-4-[4-(4-methylpiperazin-1-yl) piperidin-1-yl] phenyl} pyrimidine-2,4-diamine

Novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide free base and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, pharmaceutical compositions thereof and methods of their preparation and use are disclosed herein.

Crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-{4-[(4-methylpiperazin-1- yl)methyl]-3-(trifluoromethyl)phenyl}benzamide and its mono hydrochloride salt

Crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide and its mono hydrochloride salt

Crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide and its mono hydrochloride salt

Crystalline forms of brigatinib, pharmaceutical compositions comprising the same, and methods of their preparation and use of the same are disclosed herein.

Crystalline forms of 3-(imidazo[1,2-b)pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide and its mono hydrochloride salt

Crystalline forms of 5-chloro-N4-[-2-(dimethylphosphoryl)phenyl]-N2-{2-methoxy-4-[4-(4-methylpiperazin-1-YL) piperidin-1-YL]phenyl}pyrimidine-2,4-diamine

Crystalline forms of 3-(imidazo[1,2-B] pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide and its mono hydrochloride salt

Novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyljbenzamide free base and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methyl piperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, pharmaceutical compositions thereof and methods of their preparation and use are disclosed herein. The instant application is directed to novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl}phenyl}benzamide and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, compositions comprising such crystalline forms, and to methods of their preparation and use.

Crystalline forms of 3-(imidazo[1,2-B] pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl) methyl]-3-(trifluoromethyl)phenyl}benzamide and its mono hydrochloride salt

A process for the preparation of prostaglandin compounds having the formula (I): wherein A is selected from the group consisting of C&#x2013;Calkyl groups; C&#x2013;Caralkyl groups wherein an aryl portion thereof is unsubstituted or substituted with one to three substituents selected from the group consisting of C&#x2013;Calkyl groups, halo and CF; and (CH)OR' wherein n is an integer from 1 to 3 and R&#x2032; represents a C&#x2013;Caryl group which is unsubstituted or substituted with one to three substituents selected from the group consisting of C&#x2013;Calkyl groups, halo and CF; B is selected from OR&#x2033; and NHR&#x2033; wherein R&#x2033; is C&#x2013;Calkyl groups; andrepresents a double bond or a single bond, is disclosed. Novel intermediates are also disclosed.

Protected diols for prostaglandin synthesis

Protected and unprotected triols for prostaglandin synthesis

A process for the preparation of prostaglandin compounds having the formula (I): wherein A is selected from the group consisting of C&#x2013;Calkyl groups; C&#x2013;Caralkyl groups wherein an aryl portion thereof is unsubstituted or substituted with one to three substituents selected from the group consisting of C&#x2013;Calkyl groups, halo and CF; and (CH)OR' wherein n is an integer from 1 to 3 and R&#x2032; represents a C&#x2013;Caryl group which is unsubstituted or substituted with one to three substituents selected from the group consisting of C&#x2013;Calkyl groups, halo and CF; B is selected from OR&#x2033; and NHR&#x2033; wherein R&#x2033; is C&#x2013;Calkyl groups; and represents a double bond or a single bond, is disclosed. Novel intermediates are also disclosed.

Prostaglandin synthesis

Growing community of inventors

Westford, MA, United States of America

Pradeep Kumar Sharma