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HALOGENATED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF
专利权人:
发明人:
달톤 제임스 티.,밀러 듀안 디.,인 동후아,헤 얄리,스테이너 미첼 에스.,베베르카 카렌 에이.
申请号:
KR1020107029192
公开号:
KR1011070310000B1
申请日:
2003.10.14
申请国别(地区):
KR
年份:
2012
代理人:
摘要:
This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.본 발명은 안드로겐 수용체 표적 약제(ARTA)를 제공한다. 상기 약제는 선택적 안드로겐 수용체 모듈레이터(SARM)인 새로운 서브클래스의 화합물을 정의한다. 일부 SARM 화합물은 안드로겐 수용체에 대한 비스테로이드계 리간드의 예기치 않은 안드로겐 활성 및 동화 활성을 가지는 것으로 밝혀졌다. 다른 SARM 화합물은 안드로겐 수용체에 대한 비스테로이드계 리간드의 예기치 않은 항안드로겐 활성을 가지는 것으로 밝혀졌다. 상기 SARM 화합물은, 단독으로 또는 조성물로서, a) 남성 피임; b) 다양한 호르몬 관련 증상, 예컨대, 피곤함, 우울증, 감소된 성욕, 성적 장애, 발기 부전, 성선기능저하증(hypogonadism), 골다공증, 체모 손실, 빈혈, 비만, 사르코페니아(sarcopenia), 골다공증, 전립선비대증, 감정 및 인지 변화, 및
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http://www.ckcest.cn/home/
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