Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Susan D Aster

Donald W Graham

James M Balkovec

Sherman Tim Waddell

Milana M Maletic

Xin Gu

Richard L Tolman

Aaron H Leeman

Gina M Santorelli

Derek J Von Langen

Gool F Patel

William K Hagmann

Mitree M Ponpipom

Nancy J Kevin

Steven H Olson

Rolf Thieringer

Steven S Mundt

Anne Hermanowski-Vosatka

2,5-Diaryl-1,2,4-triazole derivatives of structural formula I are selective inhibitors of the 11&#x3b2;-hydroxysteroid dehydrogenase Type 1 enzyme (11&#x3b2;-HSD-1). The compounds are useful for the treatment of diabetes, hyperglycemia, obesity, insulin resistance, atherosclerosis, dyslipidemia, hyperlipidemia, hypertension, and Metabolic Syndrome. Also disclosed are novel compounds of structural formula II which are inhibitors of 11&#x3b2;-HSD-1.

Diaryltriazoles as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1

Triazole derivatives of structural formula I are selective inhibitors of the 11&#x3b2;-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

Triazole derivatives as inhibitors of 11-&#x3b2; hydroxysteroid dehydrogenase-1

Triazole derivatives as inhibitors of 11-&#x3b2;-hydroxysteroid dehydrogenase-1

Compounds having Formula (I), including pharmaceutically acceptable salts and prodrugs thereof: are selective inhibitors of the 11&#x3b2;-HSD1 enzyme. They inhibit the 11&#x3b2;-HSD1-mediated conversion of cortisone and other 11-keto-glucocorticoids to cortisol and other 11&#x3b2;-hydroxy-glucocorticoids. The 11&#x3b2;-HSD1 inhibitors therefore decrease the amount of cortisol in target tissues, thereby modulating the effects of cortisol. Modulation of cortisol may be effective in controlling non-insulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM or with excess cortisol in the body 

11-&#x3b2;-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia

Triazole derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1

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

4-Aza-19-norandrostane derivatives

Described are new delta-17 and delta-20 olefic and saturated 17.beta.-substituted 4-aza-5.alpha.-androstan-3-ones and related compounds and the use of such compounds as 5.alpha.-reductase inhibitors for treatment of benign prostatic hyperplasia and other hyperandrogenic related disorders.

Delta-17 and delta-20 olefinic and saturated

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

Described are new 17.beta.-ester, amide and ketone 4-aza-5a-androstan-3-ones and related compounds and their use as 5a-reductase inhibitors for treatment of benign prostatic hyperplasia and other hyperandrogenetic related disorders.

17-ester, amide, and ketone derivatives of 3-oxo-4-azasteroids as

Delta-17 and delta-20 olefinic and saturated 17 beta-substituted 4-aza-5

Growing community of inventors

Teaneck, NJ, United States of America

Susan D Aster