Merrell Dow Pharmaceuticals

Merrell Pharmaceuticals, Inc.

Hoechst Marion Roussel

Sai P Sunkara

Roger A Parker

Winton D Jones

Paul S Liu

Michael L Edwards

David M Stemerick

Jules Freedman

Terry L Bowlin

Norton P Peet

Alan D Cardin

Robert A Farr

Shawn Christopher Miller

Nellikunja J Prakash

Jeffrey S Sabol

A Stanley Tyms

Barry L Rhinehart

Mohinder S Kang

Debra L Taylor

James R Mccarthy

##STR1## The present invention is directed to a class of novel carbocyclic derivatives having formulas (I) and (II) and their use as anti-viral and anti-neoplastic agents, wherein X.sub.1 and X.sub.2 are each independently hydrogen, fluorine, or chlorine, R is hydrogen or hydroxymethyl, J is a radical of formulas (a), (b) and (c). Y.sub.1 is a CH group, a CCl group, a CBr group or a CNH.sub.2 group, Y.sub.2 and Y.sub.3 are each independently nitrogen or a CH group, Y.sub.1 is a CH group, a CCl group, a CBr group or a CNH.sub.2 group, Y.sub.2 and Y.sub.3 are each independently nitrogen or a CH group, Y.sub.4 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen, Y.sub.5 is NH.sub.2 or C.sub.1 -C.sub.4 alkoxy, Q is NH.sub.2, NHOH, NHCH.sub.3, OH, or hydrogen, and V is hydrogen, halogen or NH.sub.2 ; or a pharmaceutically acceptable salt thereof.

Carbo-acyclic nucleoside derivatives as antiviral and antineoplastic

Certain triphenylpiperidines reverse drug resistance in multi-drug resistant tumors. These compounds apparently function by inhibiting a p-glycoprotein pump which becomes activated in late stage tumor development and which is inherently present in tumors from certain origins.

Reversal of multi-drug resistance by triphenyl-azacycloalkane derivatives

Certain tetraarylethylenes reverse drug resistance in multi-drug resistant tumors. These compounds apparently function by inhibiting a p-glycoprotein pump which becomes activated in late stage tumor development and which is inherently present in tumors from certain origins.

Reversal of multi-drug resistance by tetraarylethylenes

Diarylalkyl piperidines useful as multi-drug resistant tumor agents

A method for the inhibition of tumor metastases is described herein. The method makes use of the administration of an antimetastatic factor isolated from the leech Haementeria ghilianii.

Ghilanten antimetastatic principle from the south american leech,

Certain Castanospermine ester derivatives of the formula: ##STR1## wherein R, R.sub.1 and R.sub.2 are each independently hydrogen, C.sub.1-14 alkanoyl, C.sub.1-14 alkenoyl, cyclohexanecarbonyl, C.sub.1-8 alkoxyacetyl, ##STR2## naphthalenecarbonyl optionally substituted by methyl or halogen; phenyl (C.sub.2-6 alkanoyl) wherein the phenyl is optionally substituted by methyl or halogen; cinnamoyl; pyridinecarbonyl optionally substituted by methyl or halogen; dihydropyridine carbonyl optionally substituted by C.sub.1 -C.sub.10 alkyl; thiophenecarbonyl optionally substituted by methyl or halogen; or furancarbonyl optionally substituted by methyl or halogen; Y is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, trifluoromethyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylmercapto, cyano or dimethylamino; Y' is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or it is combined with Y to give 3,4-methylenedioxy; Y' is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or halogen; with R, R.sub.1 and R.sub.2 being selected in such a way that at least one of them, but not more than two of them, is hydrogen; are disclosed to be effective in treating diseases caused by Herpes Simplex Virus (HSV) Types 1 and 2.

Anti-herpes castanospermine esters

[4S-(4.alpha.,4a.beta.,5.beta.,6.alpha.,7.alpha.,7a.alpha.)]-Octahydro-1H-1 -pyrindine-4,5,6,7-tetrols and [4R-(4.alpha.,4a.alpha.,5.alpha.,6.beta.,7.beta.,7a.beta.)]-octahydro-1H-1 -pyrindine-4,5,6,7-tetrols are useful as inhibitors of alpha-mannosidase and are useful immunostimulants, chemoprotective and radioprotective agents and antimetastatic agents.

.alpha.-mannosidase inhibitors

This invention relates to quinolyloxazole-2-ones which are useful in the treatment of multi-drug resistant tumors. The quinoloyloxazole-2-ones act to prevent drug resistance and thus allow conventional chemotherapeutic agents to kill tumor cells as if drug resistance were not present.

Treatment of multi-drug resistant tumors with quinolyl-and

This invention relates to pyridinyloxazole-2-ones which are useful in the treatment of multi-drug resistant tumors. The pyridinyloxazole-2-ones act to prevent drug resistance and thus allow conventional chemotherapeutic agents to kill tumor cells as if drug resistance were not present.

Treatment of multi-drug resistant tumors with pyridyloxazole-2-ones

Aryloxyalkanol derivatives having the formula

Aryloxy alkanols as anti-retrovirus agents

This invention relates to pyridinyloxazole-2-ones which are useful anti-enveloped virus agents by virtue of their ability to act as protein kinase C inhibitors. These derivatives are disclosed to be effective in treating enveloped virus infections including HIV infections and are thus useful in the treatment of AIDS and ARC.

Prevention of glycoprotein enveloped virus infectivity by

This invention relates to quinolyloxazole-2-ones which are useful anti-enveloped virus agents by virtue of their ability to act as protein kinase C inhibitors. These derivatives are disclosed to be effective in treating enveloped virus infections including HIV infections and are thus useful in the treatment of AIDS and ARC.

Prevention of glycoprotein enveloped virus infectivity by quinolyl- and

Certain Castanospermine ester derivatives are disclosed to be effective in treating retroviral infections including HIV infections and are thus useful in the treatment of AIDS and ARC.

Growing community of inventors

Cincinnati, OH, United States of America

Sai P Sunkara