Cardiome Pharma Corp.

Ucb Farchim Sa

Verona Pharma Plc

Bertrand M C Plouvier

Gregory N Beatch

Doug Ta Hung Chou

Tao Sheng

Grace Jung

Jeff Jiqun Zhu

Michael J A Walker

Richard A Wall

Sandro L Yong

Alexander B Zolotoy

Lewis Siu Leung Choi

Yuzhong Liu

James Gee Ken Yee

Anthony G M Barrett

Lewis S L Choi

Pirmin Ulmann

Alfred Hedinger

Cindy J Longley

Marco Silvio Passafaro

Allen Davidoff

Clive Pete Page

Allen I Bain

Martin Kurz

Daniel Moeckli

Aregahegn Yifru

Alexander R Zolotoy

Julian Scott Northen

Alan M Ezrin

Philippe Fernandes

Jeffery Jerome Wheeler

Peter Pang

Adewale Eniade

Elizabeth L S Cheu

Methods for the preparation of stereoisomerically substantially aminocyclohexyl ether compounds such as trans-(1R,2R)-aminocyclohexyl ether compounds and/or trans-(1S,2S)-aminocyclohexyl ether compounds as well as various intermediates and substrates are disclosed.

Synthetic process for aminocyclohexyl ether compounds

The current invention is directed towards a polymorph of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, at least 95% in the polymorphic form of a thermodynamically stable polymorph (I) of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, wherein said polymorph is determined by single crystal X-ray structural analysis and X-ray powder diffraction pattern. 

Crystalline form of pyrimido[6,1-A] isoquinolin-4-one compound

Methods for the preparation of stereoisomerically substantially aminocyclohexyl ether compounds such as trans-(1R,2R)-aminocyclohexyl ether compounds and/or trans-(1S,2S)-aminocyclohexyl ether compounds as well as various intermediates and substrates are disclosed. 

This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R, Rand Rare defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.

Synthetic processes for the preparation of aminocyclohexyl ether compounds

Aminocyclohexyl ether compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses uses for the compounds and compositions, including the treatment of arrhythmia.

Aminocyclohexyl ether compounds and uses thereof

Merged compounds of ion channel modulating compounds, including, for example, merged compounds of the ion channel modulating compound of the following formula: (I) are described herein, as well as methods of making and using such merged compounds and pharmaceutical compositions containing such merged compounds. 

Merged ion channel modulating compounds and uses thereof

This invention is directed to deuterated aminocyclohexyl ether compounds and processes for preparing same and methods of using same.

Deuterated aminocyclohexyl ether compounds and processes for preparing same

Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.

Ion channel modulating compounds and uses thereof

Prodrugs of ion channeling modulating compounds, including, for example, prodrugs of the ion channel modulating compound of the following formula: are described herein, as well as methods of making and using such prodrugs and pharmaceutical compositions containing such prodrugs. 

Prodrugs of ion channel modulating compounds and uses thereof

This invention is directed to drug conjugates of certain ion channel modulating compounds having the following formula: wherein A, X, R, R, R, R, R, LB, L and DM are defined herein, including isolated enantiomeric and diastereomeric isomers thereof, and mixtures thereof. Pharmaceutical compositions and methods of use are also disclosed.

Drug conjugates of ion channel modulating compounds

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Vancouver, Canada

Bertrand M C Plouvier