Chemocentryx, Inc.

Amgen Inc.

Brian E McMaster

Daniel J Dairaghi

Thomas J Schall

James Bradley Aggen

Andrew M K Pennell

Subhabrata Bapi Sen

J J Kim Wright

J J Wright

Penglie Zhang

Wei Yu Chen

Mark Penfold

Subrabrata Sen

Jj Kim Wright

Julio Cesar Medina

Feng Xu

Anita Melikian

Valeri Martichonok

Jennifer M Burns

Xuemei Wang

Tassie Collins

Hossen Mahmud

Andrew Mk Pennell

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Substituted piperazines

Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Pharmaceutical compositions containing organic compounds or salts thereof that serve as modulators for the SDF-1 or I-TAC chemokines are disclosed. The compounds and compositions are useful in the treatment of cancer, especially in the inhibition of cancer proliferation, growth, and metastasis. Methods of interfering with SDF-1 and/or I-TAC binding to the CCXCKR2 receptor and treating cancer using the compounds and pharmaceutical compositions of the present invention are also disclosed.

Inhibitors of human tumor-expressed CCXCKR2

Compounds and compositions are provided that bind to the CCR4 chemokine receptor and which are useful for treating diseases associated with CCR4 activity, such as contact hypersensitivity.

Modulation of CCR4 function

Methods for treating CMV or a CMV-related disease are provided that use compounds having the formula: wherein Ar is a substituted or unsubstituted 5&#x2013;14 membered heteroaryl group having from 1 to 5 heteroatoms as ring members; Ris selected from the group consisting of substituted or unsubstituted aryl(C&#x2013;C)alkyl, heteroaryl(C&#x2013;C)alkyl, &#x2014;C(O)R, and &#x2014;C(O)NRR, wherein each Rand Rindependently is substituted or unsubstituted aryl, substituted or unsubstituted aryl(C&#x2013;C)alkyl, substituted or unsubstituted (C&#x2013;C)cycloalkyl(C&#x2013;C)alkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroaryl(C&#x2013;C)alkyl and substituted or unsubstituted hetero(C&#x2013;C)cycloalkyl(C&#x2013;C)alkyl; Ris H or (C&#x2013;C)alkyl; and Zis a substituted or unsubstituted hetero(C&#x2013;C)bicycloalkyl group.

Bicyclic compounds as inhibitors of chemokine binding to US28

The invention provides compounds and compositions of the formula:wherein, These compounds and compositions bind to the CXCR3 chemokine receptor and are useful for treating diseases and conditions responsive to the modulation of CXCR3 activity, such as multiple sclerosis, rheumatoid arthritis, psoriasis, cancer, infectious disease, angiogenesis, and graft rejection.

Compounds and methods for modulating CXCR3 function

Arylamines as inhibitors of chemokine binding to US28

The present invention is directed to pharmaceutical compositions containing active compounds, which inhibit the activity of the chemokines, MIP-1&agr; and RANTES. It also is directed to methods of treating inflammatory and immunoregulatory disorders and diseases using these pharmaceutical compositions.

Anti-inflammatory compositions and methods of use

Compounds and methods for modulating cxcr3 function

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Mountain View, CA, United States of America

Brian E McMaster