Merck + Co., Inc.

Jose Alexander

Joseph A Fix

A J Repta

Takeru Higuchi

Joseph P Vacca

Bruce D Dorsey

Arnold J Repta

Takeru Higuchi, Deceased

Chung Shih

Dilbir Bindra

Prodrugs of the HIV protease inhibitor L-735,524 are useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating ADS and methods of preventing or treating infection by HIV are also described.

Prodrugs of an inhibitor of HIV protease

This invention relates to novel acyloxyisopropyl carbamates as bioreversible prodrug moieties for amino drugs and to methods of synthesizng these compounds.

Acyloxyisopropyl carbamates as prodrugs for amine drugs

This invention relates to a the use of new oxodioxolenylmethyl carbamates to produce bioreversible neutral prodrugs from primary and secondary amines.

Dioxolenylmethyl carbamates pro moieties for amine drugs

The invention relates to pyroglutamic acid esters used as dermal penetration enhancers for therapeutic agents having poor skin permeation.

Pyroglutamic acid esters used as dermal penetration enhancers for drugs

Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.

Enhancment of absorption of drugs from gastrointestinal tract using

Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.

Acylcarnitines as absorption-enhancing agents for drug delivery through

Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.

Choline esters as absorption-enhancing agents for drug delivery through

This invention relates to a new one-step process for preparation of novel N-(acyloxyalkoxy)carbonyl derivatives useful as bioreversible prodrug moieties for drugs having a primary or secondary amine function thereon.

Process for preparing novel N-(acyloxy-alkoxy)carbonyl derivatives

Enhancement of absorption of drugs from gastrointestinal tract using

This invention relates to novel (acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs having a primary or secondary amine function thereon. Hydrolytic enzymes are used to trigger the regeneration of the parent amine drug of the carbamate prodrug moiety. The case also contains pharmaceutical composition, method of treatment and process claims.

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Lawrence, KS, United States of America

Jose Alexander