Eli Lilly and Company

Princeton University

Gerald B Grindey

Chuan Shih

Edward C Taylor

Dietmar G Kuhnt

John E Toth

Larry W Hertel

J Jeffry Howbert

Karen Lynn Lobb

James E Ray

George B Boder

Cora Sue Grossman

William J Ehlhardt

John L Zimmermann

John F Worzalla

This invention provides certain benzenesulfonamide derivatives and methods for using them in the treatment of susceptible neoplasms in mammals. Also provided are certain novel pharmaceutical formulations employing these benzenesulfonamide derivatives in combination with a carrier, and processes for preparing the benzenesulfonamide derivatives.

Antitumor compositions and methods of treatment

A method of treating susceptible neoplasms in mammals comprising administering to a mammal in need of such treatment a pharmaceutically effective amount of a compound of the formula ##STR1## wherein: R.sup.1 is hydrogen;

Method of treating tumors in mammals with 2',2'-difluoronucleosides

This invention provides the use of N-[[(3,4-dichlorophenyl)amino]carbonyl]-2,3-dihydrobenzofuran-5-sulfonamid e, and pharmaceutically acceptable salts thereof, in the treatment of susceptible neoplasms in mammals. This invention further provides the novel aforementioned compound and its pharmaceutical formulations.

Antitumor compositions and methods

3-Ethynylpyrrolo[2,3-d]pyrimidines are chemical intermediates for antineoplastic N-(acyl)glutamic acid derivatives. A typical embodiment is 3-ethynyl-4-hydroxy-6-pivaloylaminopyrrolo[2,3-d]pyrimidine.

Pyrrolo(2,3-d)pyrimidines

Administration of a folate binding protein binding agent in conjunction with use of an antitumor agent which is an inhibitor of glycinamide ribonucleotide transformylase or other antifolate reduces the toxic effects of such agent and provides an enhanced therapeutic index.

Method for treating gar-transformylase tumors in mammals and reducing

2'-deoxy-2',2'-difluoro-inosine and 5'-O alkyl derivatives are disclosed as inhibitors of neoplasms.

2-deoxy-2',2'-difluoro-inosine and 5'O-derivatives

N-(Acyl)glutamic acid derivatives in which the acyl group is substituted with 4-hydroxypyrrolo[2,3-d]-pyrimidin-3-yl group are antineoplastic agents. A typical embodiment is N-{5-[2-(4-hydroxy-6-aminopyrrolo[2,3-d]pyrimidin-3-yl)ethyl]thien-2-ylcar bonyl}-L-glutamic acid.

N-(6-Amino-(pyrrolo(2,3-d)pyrimidin-3-ylacyl) )-glutamic acid derivatives

N-(Acyl)glutamic acid derivatives in which the acyl group is substituted with 4-hydroxypyrrolo[2,3-d]pyrimidin-3-yl group are antineoplastic agents. A typical embodiment is N-[4-(2-{4-hydroxypyrrolo[2,3-d]pyrimidin-3-yl}ethyl)benzoyl]-L-glutamic acid.

Growing community of inventors

Indianapolis, IN, United States of America

Gerald B Grindey