Abstract: Quinazoline thiazolinone derivatives which demonstrate CDK1 antiproliferative activity and are useful as anti-cancer agents.

Abstract: The present invention provides compounds of formula I wherein R1, R2, R3, R4, and R5 are described herein. The invention also provides syntheses for preparation of such compounds and pharmaceutical compositions containing them. The invention further provides methods for inhibiting kinases, in particular CDK2, for inhibiting angiogenesis, and for treating cancers, in particular breast, colon, prostate, and lung cancer.

Abstract: Disclosed is a novel method for synthesizing pyrazolobenzodiazepines of formula I using intermediates of formula Pyrazolobenzodiazepines of formula I are useful in the treatment and control of solid tumors.

Abstract: Disclosed are novel pyrazolobenzodiazepines having the formula These compounds are useful in the preparation of the pyrazolobenzodiazepines of formula I, which are useful in the treatment and control of solid tumors.

Abstract: 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.

Abstract: Disclosed is a novel method for synthesizing pyrazolobenzodiazepines of formula I 1

Abstract: Disclosed are novel dihydropridinone 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.

Abstract: Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR an 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.

Abstract: Disclosed are novel naphthostyrils of formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing such compounds, methods for the treatment and/or prevention of cancer using such compositions, and intermediates useful in the preparation of the compounds of formula I.

Abstract: Disclosed are novel naphthostyrils of formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing such compounds, methods for the treatment and/or prevention of cancer using such compositions, and intermediates useful in the preparation of the compounds of formula I.

Abstract: Disclosed are novel pyrazolobenzodiazepines having the formula 1

Abstract: Disclosed are novel naphthostyrils of formula 1

Abstract: Disclosed are novel pyrazolobenzodiazepines having the formula and the pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 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, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I as well as intermediates useful in the preparation of the compounds of formula I.

Abstract: Disclosed are novel 4-alkenyl- and 4-alkynyl oxindoles having the formula and the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, 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.

Abstract: 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.

Abstract: The total synthesis of taxol employs a convergent synthetic plan. The synthetic plan may also be employed to produce a large number of taxol analogs. Taxol analogs having skeletal extensions are inaccessible by modification of the natural product but are readily produced by employing the convergent synthetic plan herein.

Abstract: A taxol intermediate selected from the group consisting of: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each selected from hydrogen, hydroxyl, or a protected hydroxyl; or R.sup.1 and R.sup.2 together form an oxo or a protected oxo; R.sup.3 is formyl, a protected formyl, or --CH(X)--OY wherein X is hydrogen or a monovalent metal and Y is hydrogen or a hydroxyl protecting group; and R.sup.4 and R.sup.5 are different and each selected from chloro or cyano; or R.sup.4 and R.sup.5 together form an oxo or a protected oxo, with the proviso that R.sup.1 and R.sup.2 are not both hydroxyl; R.sup.6 is hydroxyl or a protected hydroxyl; R.sup.7 is hydrogen, hydroxyl, or a protected hydroxyl; R.sup.8 is carboxyl, hydroxylmethyl, or a protected hydroxylmethyl; or R.sup.7 and R.sup.8 when taken together with carbon atoms 3 and 4, form an oxetane ring; or R.sup.6 and R.sup.8 when taken together with carbon atoms 1 and 4, form a bridged lactone; R.sup.9 is hydrogen or a hydroxyl protecting group; R.sup.