Eisai Company, Limited

Eisai Inc.

Eisai R&d Management Co., Ltd.

James J Kowalczyk

Hu Yang

Mark Spyvee

Shawn Schiller

Boris M Seletsky

Galina Kuznetsov

Michael D Lewis

Ana Maria Garcia

Francis Gerard Fang

Ieharu Hishinuma

Takeshi Nagasu

Kentaro Yoshimatsu

Silvio A Campagna

Eric Schwartz

Rulin Fan

Edmund M Harrington

Amy E Christuk

Xiaoning C Sheng

The present invention provides compounds having formula (I): 

Hemiasterlin derivatives and uses thereof in the treatment of cancer

The present invention provides compounds having formula (I):  and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R-R, X, X, R, Q, and n are as defined herein.

Hemiasterlin derivatives and uses thereof

The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R&#x2013;R, X, X, R, Q, and n are as defined herein.

Provided are novel peptidomimetic isoprenyl transferase inhibitors, methods for synthesizing such inhibitors, and methods for the use of such inhibitors for the treatment of tumors.

Inhibitors of isoprenyl transferase

Peptidomimetic isoprenyl transferase inhibitors R6SCHR1&prime;CHR1WCHR2YC(:X)NR3CHR5COR4 wherein R1&equals;OH, H, alkyl, amino group or R1 and R6 together form a heterocyclic ring; R1&prime;&equals;H, alkyl, aryl; R2&equals;H, alkyl, arylalkyl, heteroarylalkyl; R3&equals;H, alkyl, arylalkyl; R4&equals;OH, alkoxy, amino group; R5&equals;natural amino acid residue or D&mdash;E&mdash;F, where D is alkyl or alkenyl, E is O, S, N, or null, F is H, alkyl, aryl, carboxy amino, etc.; R6&equals;H, alkyl, acyl, etc.; W&equals;alkyl, alkenyl; X&equals;O, S, Y is M&mdash;O&mdash;P, where M is C0-6 alkyl, O is oxygen-C0-4 alkyl, P is(un)substituted C6-20 aryl are disclosed.

Isoprenyl transferase inhibitors

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Andover, MA, United States of America

James J Kowalczyk