17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators

A heterocyclyl, halogen technology, applied in the field of tissue-selective androgen receptor modulators, can solve problems such as reduced ability
CN1849126AInactive Publication Date: 2006-10-18MERCK & CO INC
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
MERCK & CO INC
Publication Date
2006-10-18
Estimated Expiration
Not applicable · inactive patent

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Abstract

Compounds of formula I are modulators of the androgen receptor (AR) acting in a tissue-selective manner. These compounds alone or in combination with other active agents are effective in enhancing debilitating muscle tone and treating conditions caused by androgen deficiency or ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced bone Osteoporosis, periodontal disease, fractures, bone damage after bone reconstruction surgery, sarcopenia, frailty, aging skin, hypogonadism in men, postmenopausal syndrome in women, atherosclerosis, hypercholesterolemia, hyperlipidemia obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hypertrophy (BPH), abdominal obesity, metabolic syndrome, type II diabetes, cancer cachexia, al Alzheimer's disease, muscular dystrophy, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure and autoimmune diseases.
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Description

field of invention

[0001] The present invention relates to 17-heterocycle-4-azasteroid derivatives, their synthesis and their use as androgen receptor modulators. More specifically, the compounds of the present invention are tissue selective androgen receptor modulators and are thus useful in the treatment of conditions caused by androgen deficiency or ameliorated by the administration of androgens, such as osteoporosis, periodontal disease, bone fractures, Weakness and sarcopenia. In addition, the SARMs of the present invention can be used to treat psychiatric disorders associated with low testosterone, such as depression, sexual dysfunction, and cognitive decline. By being antagonists in specific tissues, SARMs are also effective in conditions where increased androgen stress or activity triggers symptoms, such as benign prostatic hypertrophy and sleep apnea. Background of the invention

[0002] The androgen receptor (AR) belongs to the superfamily of steroid / thyroid horm...

Claims

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