Anormed, Inc.

Genzyme Corporation

Jason B Crawford

Renato Skerlj

Trevor R Wilson

Gary James Bridger

Ernest John McEachern

Yuanxi Zhou

David Earl Bogucki

Curtis Harwig

Dominique Schols

Al Kaller

Siqiao Nan

Bem Atsma

Christopher Dennis Smith

Maria Rosaria Di Fluri

Gang Chen

Christopher Dennis

Rosaria Maria Di Fluri

Bern Atsma

Ian R Baird

Ernest J Mceachern

Yongbao Zhu

Renato Tony Skerlj

Maria Rosario DiFluri

David Gauthier

Renato T Skelj

Trevor Wilson

Siquiao Nan

Renato T Skerlj

The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).

Chemokine receptor binding heterocyclic compounds with enhanced efficacy

Compounds which modulate chemokine receptor activities are disclosed. These compounds are preferably tertiary amines comprising tetrahydroquinoline and benzimidazole.

Chemokine receptor binding heterocyclic compounds

The present invention relates to chemokine-binding heterocyclic compound salts, methods of use thereof, and methods for preparing the same.

Chemokine-binding heterocyclic compound salts, and methods of use thereof

Heterocyclic compounds that bind chemokine receptors and inhibit the binding of their natural ligands are disclosed. The invention compounds are protective against infection by HIV and exert effects characteristic of antagonists to the CXCRreceptor.

Methods for preparing 2,6-diaryl piperidine derivatives are described. More particularly, 2,6-diaryl piperidines having formula 1-4 are prepared by cyclocondensation of an aryl or heteroaryl aldehyde with 1,3-acetonedicarboxylic acid.

Methods of making 2,6-diaryl piperidine derivatives

Tertiary amine compounds that bind chemokine receptors such as CXCR4 and CCR5 are disclosed.

This invention relates to a process for synthesizing heterocyclic pharmaceutical compound which binds to the CXCR4 chemokine receptor. In one embodiment, the process comprises: a) reacting a 5,6,7,8-tetrahydroquinolinylamine and an alkyl aldehyde bearing a phthalimide or a di-tertiary-butoxycarbonyl (di-BOC) protecting group to form an imine; b) reducing the imine to form a secondary amine; c) reacting the secondary amine with a haloalkyl substituted heterocyclic compound, to form a phthalimido-protected or di-tert-butoxycarbonyl protected tertiary amine; and d) hydrolyzing the protected amine to obtain a compound having Formula I' 

Process for the synthesis of CXCR4 antagonist

Tertiary amines containing a multiplicity of heteroaromatic substituents are useful as chemokine receptor modulators.

Heterocyclic compounds that bind chemokine receptors and inhibit the binding of their natural ligands are disclosed. The invention compounds are protective against infection by HIV and exert effects characteristic of antagonists to the CXCR4 receptor.

Novel compounds that are useful for targeting chemokine receptors are disclosed. These compounds are complex tertiary amines.

Compounds that bind to chemokine receptors such as CXCRand CCRdemonstrate protective effects against infection of cells by human immunodeficiency virus are disclosed. These compounds contain a tertiary amine[[s]] linked to a core nitrogen via an aromatic or heteroaromatic moiety.

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Burnaby, Canada

Jason B Crawford