アンドロゲン受容体調節剤としての17-複素環-4-アザステロイド誘導体

Japanese Patent JP2007505118

A

Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive impairment, decreased libido, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

Robert Es Meissner
Helen Jei, Mitchell

JP2006526181A

March 08, 2007

September 02, 2004

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MERCK & COMPANY INCOPORATED

C07J73/00; A61K31/122; A61K31/473; A61K31/52; A61K31/5575; A61K31/565; A61K31/58; A61K31/585; A61K31/59; A61K31/663; A61K33/16; A61K38/00; A61K38/23; A61K38/27; A61K45/00; A61K45/06; A61P1/02; A61P3/04; A61P3/06; A61P3/10; A61P5/26; A61P5/28; A61P7/00; A61P9/10; A61P11/00; A61P13/08; A61P15/00; A61P15/12; A61P17/00; A61P19/00; A61P19/02; A61P19/10; A61P21/00; A61P25/24; A61P25/28; A61P29/00; A61P31/18; A61P35/00; A61P37/02; A61P43/00; C07D401/04; C07D471/04; C07D473/00

Yoshio Kawaguchi
Makoto Ono
Chihiro Watanabe
Kenkyo Kanayama
Katsuma Osaki
Mitsuaki Tsubokura

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