Acadia Pharmaceuticals Inc.

Cinclus Pharma Holding Ab (publ)

Mikael Hillgren

Beat Theodor Weber

Marlon Carlos

Roger Olsson

Sagun Tandel

Matthew J Fleming

Andreas Philipp Boudier

Thomas Larsson

Dan Wang

Kjell Jarring

Xingbang Lin

The present invention relates to polymorphs of the hydrochloride salt of 5-{2-[({8-[(2,6-dimethylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyridine-6-yl}carbonyl)-amino]ethoxy}-5-oxopentanoic acid (linaprazan glurate), more specifically Form 1 and Form 2 of the HCl salt of linaprazan glurate. The invention also relates to a process for the preparation of such polymorphs, to pharmaceutical compositions comprising such polymorphs, and to the use of these polymorphs in the treatment or prevention of gastrointestinal inflammatory diseases or gastric acid related diseases, in particular erosive gastroesophageal reflux disease (eGERD).

Polymorphs of the hydrochloride salt of linaprazan glurate

Disclosed herein are methods for obtaining N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N-(4-(2-methylpropyloxy)phenylmethyl) carbamide (pimavanserin) comprising the step of contacting an intermediate according to Formula (A) or a salt thereof, with an intermediate Formula B, or a salt thereof, to produce pimavanserin or a salt thereof wherein Y is &#x2014;ORor &#x2014;NRR; Ris hydrogen or substituted or unsubstituted heteroalicyclyl, Ris substituted or unsubstituted aralkyl; X is &#x2014;ORor &#x2014;NRR; (wherein Ris hydrogen or substituted or unsubstituted Calkyl and one of Rand Ris hydrogen and the other is hydrogen or N-methylpiperidin-4-yl); and Ris &#x2014;OCHCH(CH)or F; Also disclosed herein is the tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide and methods for obtaining the salt.

Methods for preparing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and polymorphic form c

Disclosed herein are methods for obtaining N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (pimavanserin) comprising the step of contacting an intermediate according to Formula (A) or a salt thereof, with an intermediate Formula B, or a salt thereof, to produce pimavanserin or a salt thereof wherein Y is &#x2014;ORor &#x2014;NRR; Ris hydrogen or substituted or unsubstituted heteroalicyclyl, Ris substituted or unsubstituted aralkyl; X is &#x2014;ORor &#x2014;NRR; (wherein Ris hydrogen or substituted or unsubstituted Calkyl and one of Rand Ris hydrogen and the other is hydrogen or N-methylpiperidin-4-yl); and Ris &#x2014;OCHCH(CH)or F; Also disclosed herein is the tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N&#x2032;-(4-(2-methylpropyloxy)phenylmethyl) carbamide and methods for obtaining the salt. 

Methods for preparing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and polymorphic form

Methods for preparing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and polymorphic form C

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Orebro, Sweden

Mikael Hillgren