Medarex Inc.

Chemocentryx, Inc.

Axys Pharmaceuticals, Inc.

Valeri Martichonok

Howard P Ng

Guoxian Wu

Oliver L Saunders

Danny P C McGee

David J King

Thomas Jay Lobl

Zhi-Hong Li

Sharon Elaine Boyd

Andrew M K Pennell

Zhihong Li

Penglie Zhang

Wei Yu Chen

Subhabrata Bapi Sen

John O Link

Sanjeev Gangwar

James Bradley Aggen

Sheila M Zipfel

John W Patterson

Geoffrey T Yarranton

Daniel J Dairaghi

Irina Astafieva

Kevin Lloyd Greenman

Jimmie L Moore

Lianfa Li

Brian E McMaster

Edward J Sullivan

J J Kim Wright

Danny Pc McGee

Arnold J Martelli

Oliver L Saunder

Geoffrey Thomas Yarranton

Danny P Mcgee

The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.

Methods of treating cancer with an antibody-drug conjugate

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.

Substituted piperazines

Peptidyl prodrugs and linkers and stabilizers useful therefor

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds 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.

4-phenylpiperdine-pyrazole CCR1 antagonists

Disulfide prodrugs and linkers and stabilizers useful therefor

Cytotoxic agents

The present invention relates to novel alkanoyl-substituted heterocyclic derivatives which are cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.

Compounds and compositions as protease inhibitors

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San Francisco, CA, United States of America

Valeri Martichonok