Merck + Co., Inc.

Derek J Von Langen

Richard L Tolman

Alan D Adams

Donald W Graham

Gary H Rasmusson

Soumya P Sahoo

William K Hagmann

Philippe L Durette

Thomas J Lanza, Jr

Hiroo Koyama

Joel Peter Berger

Kun Liu

James Francis Dropinski

Susan D Aster

A Brian Jones

Alexander Elbrecht

Gaochao Zhou

Karen Lamb MacNaul

Guo-Qiang Shi

Arthur A Patchett

Malcolm MacCoss

Thomas F Walsh

Mark T Goulet

Feroze Ujjainwalla

Anthony K Ogawa

Richard B Toupence

Kenneth J Fitch

Conrad Santini

Jeffrey P Bergman

Gregory D Berger

David E Moller

Mark D Leibowitz

John D Karkas

Anthony B Jones

This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.

Anti-hypercholesterolemic compounds

A class of 2-aryloxy-2-arylalkanoic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.

2-aryloxy-2-arylalkanoic acids for diabetes and lipid disorders

The instant invention is concerned with aryl and heteroaryl acetic acid and oxyacetic acid compounds, which are useful as antidiabetic compounds. Compositions and methods for their use in the treatment of diabetes and related diseases and for lowering triglyceride levels are disclosed.

Antidiabetic agents based on aryl and heteroarylacetic acids

16-substituted-4-aza-androstane 5-&agr;-reductase isozyme 1 inhibitors

The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compounds which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.

Antidiabetic agents

The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.

Benzisoxazole-derived antidiabetic compounds

The novel compounds of the present invention are those of structural formula I: ##STR1## or a pharmaceutically acceptable salt, ester, or stereoisomer thereof, which are inhibitors of 5.alpha.-reductase. The compounds of formula I are useful in the oral, systemic, parenteral or topical treatment of hyperandrogenic conditions. Methods of using the compounds of formula I for the treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia, male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as the treatment of prostatitis the treatment of sweat-related conditions such as apocrine gland sweating, hyperhidrosis, and hydradenitis suppurativa, the treatment of polycystic ovary syndrome, the prevention and treatment of bone loss and related diseases, and the prevention and treatment of premature labor are provided, as well as pharmaceutical compositions for the compounds of formula I.

Tricyclic compounds

Compounds of the Formula I ##STR1## are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.

16-pyrazinyl-substituted-4-aza-androstane 5-.alpha.-reductase isozyme 1

Compounds of the formula I ##STR1## are inhibitors of 5.alpha.-reductase, and are useful for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, prostatic carcinoma, prostatitis and benign prostatic hyperplasia.

16-substituted-6-aza-androsten-4-ene-3-ones as 5-.alpha.-reductase

16-substituted-4-aza-3-oxo-androstane as 5-alpha-reductase isozyme 1

16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors

Certain prodrugs such as ##STR1## are useful in the inhibition of herpes virus thymidine kinase, the prevention or treatment of recurrent infection by herpes virus, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing or treating recurrent infection by herpes virus are also described.

Prodrugs of herpes TK inhibitors

Compounds of the formula ##STR1## are inhibitors of 5 .alpha.-reductase and are useful alone or in combination with other active agents for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.

17.beta.-substituted-6-azasteroid derivatives useful as

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Fanwood, NJ, United States of America

Derek J Von Langen