The Dupont Merck Pharmaceutical Company

Erbamont Inc.

Bristol-myers Squibb Pharma Company

Bristol-myers Squibb Compnay

Pharmacia Corporation

Dupont Pharmaceuticals Company

Jung-Hui Sun

Mimi Lifen Quan

Hui-Yin Li

Karen Anita Rossi

Steven P Seitz

Christopher A Teleha

David J Meloni

Luigi Anzalone

Celia Dominguez

Fuqiang Jin

Daniel Lednicer

Thomas E Smyser

Brian Lloyd Wells

Chih-Yun Johnny Tu

James David Rodgers

Jiacheng Zhou

Thomas P Maduskuie, Jr

Robert J Cherney

Robert J Ardecky

Robert A Galemmo, Jr

Chung-Ho Park

Petrus Fredericus Stouten

Jose Ricardo Matos

Arthur D Patten

Robert Frank Kaltenbach, Iii

Lucius T Rossano

Thomas Peter Maduskuie, Jr

Robert Anthony Galemmo, Jr

Robert G Clifton, Jr

Jia C Zhou

Petrus Fredericus Wilhelmus Stouten

Efficient process for the preparation of a factor Xa inhibitor

N-(amidinophenyl)cyclourea analogs as factor Xa inhibitors

The present application describes N-(amidinophenyl)cyclourea analogs of formula I: ##STR1## which are useful as inhibitors of factor Xa.

N-(amidinophenyl) cyclourea analogs as factor XA inhibitors

A method for alleviating emesis caused by chemotherapy which comprises administering an antiemetic agent or a pharmaceutically acceptable salt thereof to a patient in conjunction with the administration of a chemotherapeutic agent, said antiemetic agent being represented by the formula (I) ##STR1## wherein Z represents a substituent such as a lower alkyl group, a methoxyethoxymethyl group, or a benzoylmethyl group; or Z in conjunction with the adjacent position represents the atoms necessary to complete a 5 to 7 membered saturated or unsaturated oxygen-containing ring; R represents a hydrogen atom, a halogen atom, a lower alkyl group, a cycloalkyl group, a lower alkoxy group, an amino group, a lower alkyl-substituted amino group, an acylamido group, a sulfamoyl group, a sulfonamido group or a nitro group; n is an integer of 1 to 3; W is a straight chain or branched chain alkylene group of 1 to 4 carbon atoms; and X represents the atoms necessary to complete a 5 or 6 membered ring; said antiemetic agent being administered in an amount and in a manner which alleviates emesis associated with said chemotherapeutic agent; and certain new antiemetic agents useful in said method.

Method for controlling emesis caused by chemotherapeutic agents and

This invention relates to 3-Pyrimidinyl Bisnaphthalimides as Anticancer Agents and pharmaceutically acceptable salts thereof, of the formula: ##STR1## and processes for the preparation of such compounds, pharmaceutical composition containing such compounds, and methods of using such compounds to treat cancer, particularly solid tumor carcinomas, in mammals.

3-aromatic and 3-heteroaromatic substituted bisnaphthalimides

The present invention relates generally to methods for the preparation of unsymmetrically substituted cyclic ureas of the formulae ##STR1## which are useful as HIV protease inhibitors. The methods provided go through an isourea intermediate.

Method for preparing N-monosubstituted and N,N'-disubstituted

This invention relates to bis-naphthalimides, including 2,2'-[1,2-ethanediylbis(methylimino-2,1-ethanediyl)]-bis[5-nitro-1H-benz[d e]isoquinoline-1,3(2H)-dione], 2-[2-[N-methyl-N-[2-[[2-(5-nitro-1,3-dioxo-1H-benz[de]isoquinoline-2(3H)-y l)ethyl]amino]ethyl]amino]ethyl]-5-nitro-1H-benz[de]isoquinoline-1,3(2H)-di one, 2,2'-[1,2-ethanediylbis(imino-2,1-ethanediyl)]-bis[5-nitro-1H-benz[de]isoq uinoline-1,3(2H)-dione], pharmaceutical compositions containing them, and methods of using them to treat solid tumor carcinomas in mammals.

Highly water soluble bis-naphthalimides useful as anticancer agents

This invention relates to bis-naphthalimides, including 2,2'-[1,2-ethanediylbis[imino(1-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione] and 2,2'-[1,2-ethanediylbis[imino(2-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione], processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer in mammals.

Processes for preparing bis-naphthalimides containing amino-acid derived

This invention relates to unsymmetrical mono-3-nitro bis-naphthalimides of formula ##STR1## including (R,R)-2-{2-[2-((2-(1,3-dioxo-1H-benz[de]isoquinolin-2-(3H)-yl)-propylamino ))ethylamino]-1-methylethyl}-5-nitro-1H-benz[de]isoquinolin-1,3-(2H)-dione, processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer, particularly solid tumor carcinomas, in mammals.

Unsymmetrical mono-3-nitro bis-naphthalimides as anticancer agents

This invention relates to bis-naphthalimides, including 2,2'-[1,2-ethanediylbis[imino(1-methy1-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione] and 2,2'-[1,2-ethanediylbis[imino(2-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione], processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer in mammals.

Process of preparing tetraamino intermediates

There are provided novel bis-naphthalimide compounds useful as antitumor agents, pharmaceutical compositions containing them and processes for preparing such compounds.

Bis-naphthalimides containing amide and thioamide linkers as anticancer

Bis-naphthalimides containing amino-acid derived linkers as anticancer

The compound (R) (-)-4-amino-5-chloro-N-(2-pyrrolidinylmethyl)-2,3-dihydrobenzo[b]furan-7-c arboxamide; the S isomer thereof, and pharmaceutical compositions containing the same.

4-amino-5-chloro-n-(2-pyrrolidinylmethyl)-2,3-dihydrobenzo[b]fura

There are provided novel bis-napthalimide compounds useful as antitumor agents, pharmaceutical compositions containing them and processes for preparing intermediates to such compounds.

Bis-naphthalimides as anticancer agents

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Hockessin, DE, United States of America

Jung-Hui Sun