Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

John Lawson Roberts

Sung-Sau So

Dennis D Keith

Qingjie Ding

Norman Kong

Chung-Chen Wei

Kuo-Sen Huang

Anthony Neri

Paul Gillespie

Peter Michael Wovkulich

Allen John Lovey

Jin-Jun Liu

Giacomo Pizzolato

Binh Vu

Bradford Graves

Nan Jiang

Nicholas J S Huby

Pamela Loreen Rossman

Kevin W Anderson

Binh Thanh Vu

Bradford James Graves

Kevin William Anderson

The present invention relates to compounds according to formula 1, which exhibit cytotoxic activity. The compounds may be used in the treatment of cancer.

Sultam derivatives

There is provided a compound of formula I and the pharmaceutically acceptable salts and esters thereofwherein X, X, R, R, R, R, Rand Rare herein described. The compounds exhibit activity as anticancer agents.

4,4,5,5, tetrasubstituted imidazolines

The present invention provides a method for testing an agent for its ability to inhibit binding between fibroblast growth factor (FGF) and heparan sulfate, comprising the steps of: interacting in solution immobilized FGF on a solid support with the agent and labeled heparan sulfate, and detecting the presence or absence of label in the solution remote from the solid support.

Method for testing the ability of an agent to inhibit fibroblast growth factor binding with labeled heparan sulfate

Novel pyrazolopyrimidines of formula (I): are discussed. These pyrazolopyrimidines are capable of inhibiting the activity of cyclin-dependent kinases, most particularly cyclin-dependent kinase 1 (Cdk1), cyclin-dependent kinase 2 (Cdk2), and cyclin-dependent kinase 4 (Cdk4) and are thus useful, inter alia, in the treatment or control of cancer, in particular solid tumors. This invention also provides pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors.

Pyrazolopyrimidines

The present invention provides a method for testing an agent for its potential to inhibit heparanase catalytic activity, comprising the steps of: interacting immobilized heparanase substrate binding protein on a solid support with labeled heparanase substrate to provide immobilized labeled heparanase substrate, interacting a heparanase enzyme solution with the immobilized labeled heparanase substrate in the presence of the agent, and detecting the presence or absence of label in the solution remote from the solid support. The labeled heparanase substrate may be bound to an immobilization bridge which binds to immobilized molecules on a solid support, to provide bridge-immobilized labeled heparanase substrate. The present invention also provides a method for testing an agent for its ability to inhibit binding between fibroblast growth factor (FGF) and heparanase substrate, comprising the steps of: interacting in solution immobilized FGF on a solid support with the agent and labeled heparanase substrate, and detecting the presence or absence of label in the solution remote from the solid support.

Method for screening an agent for ability to inhibit heparanase activity

Antibacterial compounds of the formula ##STR1## in which R.sub.1 is a cyclic or secondary acyclic amino group which independently has antibacterial activity;

Cephalosporin antibacterial compounds

Antibacterial compounds of the formula ##STR1## in which R.sub.1 is a cyclic or secondary acyclic amino group which independently has antibacterial activity:

Penam antibacterial compounds

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Budd Lake, NJ, United States of America

John Lawson Roberts