Merrell Dow Pharmaceuticals

Richardson-Merrell Inc.

Hoechst Marion Roussel

Aventis Pharmaceuticals Inc.

Winton D Jones

Richard A Schnettler

Richard C Dage

George P Claxton

Francis P Miller

Sai P Sunkara

Hsien C Cheng

William L Albrecht

Phillip J Robinson

John M Kane

Keith A Diekema

Robert J Dinerstein

Fred L Ciske

Richard A Schenttler

Richard A Dage

The present invention describes certain alkyloxyamino-substituted fluorenones which inhibit protein kinase C, as well as pharmaceutical compositions including these compounds and methods of using these compounds to control protein kinase C activity in mammals, including humans. More specifically, the present compounds are useful for the treatment of neoplastic disease states, disorders associated with abnormal blood flow (including hypertension, ischemia, atherosclerosis, coagulation disorders), and inflammatory diseases (including immune disorders, asthma, lung fibrosis, and psoriasis).

Alkyloxyamino substituted fluorenones and their use as protein kinase-C

Novel 5-acyl-2-(1H)pyridinones and their use as cardiotonic agents. Typical of the compounds is 5-acetyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile which is prepared by condensing anionic cyano acetamide with 3-[(dimethylamino)methylenyl]-2,4-pentanedione in an inert organic solvent.

5-acyl-2-(1H)-pyridinoes

This invention relates to alkoxyimino ether derivatives of 5-acyl-2(1H)-pyridinones and to their use as cardiotonic agents useful in treating cardiac failure, and to the process useful in the preparation thereof.

Alkoxyimino ether derivatives of 5-acyl-2(1H)-pyridinones

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

Novel 5-acyl-2-(1H)pyrdinones and their use as cardiotonic agents. Typical of the compounds is 5-acetyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile which is prepared by condensing anionic cyano acetamide with 3-[(dimethylamino)methylenyl]-2,4-pentanedione in an inert organic solvent.

5-Acyl-2-(1H)-pyridinones useful for treating cardiac failure

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 alkoxyimino ether derivatives of 5-acyl-2(1H)-pyridinones

This invention relates to novel quinolyloxazole-2-ones which are useful as protein kinase C inhibitors, effective in the treatment of hypertension and asthma. This invention also includes a novel procedure for producing an intermediate ketone compound involving the reaction of a bromo-quinoline compound with butyl lithium and further reacting the lithiated compound with N-methyl-N-methoxyalkanamide.

Process for preparing quinoline aldehyde and ketone derivatives

Novel 5-acyl-2-(1H)-pyridinones and their use as cardiotonic agents. Typical of the compounds is 5-acetyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile which is prepared by condensing anionic cyano acetamide with 3-[(dimethylamino)methylenyl]-2,4-pentanedione in an inert organic solvent.

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Cincinnati, OH, United States of America

Winton D Jones