Hoffmann-la Roche Inc.

Apostolos Dermatakis

Kin-Chun Thomas Luk

Yi Heng Chen

Jin-Jun Liu

Pamela Loreen Rossman

Sung-Sau So

Steven Gregory Mischke

Paige Erin Mahaney

Wendy Lea Corbett

Christophe Michoud

Marek Michal Kabat

Frederick M Konzelmann

Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.

Pyrimido compounds having antiproliferative activity

Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases and are selective against LCK. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.

Naphthostyrils

Disclosed are novel 4-alkenyl- and 4-alkynyl oxindoles having the formula

4-alkenyl-and 4-alkynyloxindoles

Disclosed are novel 4-alkenyl- and 4-alkynyl oxindoles having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, a, b, and X are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer, more particularly, the treatment or control of breast and colon tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I and II as well as intermediates useful in the preparation of the compounds of formula I and II.

4-Alkenyl- and 4-alkynyloxindoles

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Parlin, NJ, United States of America

Apostolos Dermatakis