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1. (WO2003011302) ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF

Pub. No.:    WO/2003/011302    International Application No.:    PCT/US2002/023761
Publication Date: 2003. 2. 13 International Filing Date: 2002. 7. 26
IPC: A61K 31/435
A61K 31/473
A61K 31/58
C07D 221/18
C07D 401/12
C07D 405/12
C07D 409/12
Applicants: MERCK & CO., INC.
HUTCHINSON, John, H.
BRESLIN, Michael, J.
HALCZENKO, Wasyl
DUGGAN, Mark, E.
HARADA, Shun-ichi
SCHMIDT, Azriel
TOWLER, Dwight
SAHOO, Soumya, P.
RODAN, Gideon, A.
Inventors: HUTCHINSON, John, H.
BRESLIN, Michael, J.
HALCZENKO, Wasyl
DUGGAN, Mark, E.
HARADA, Shun-ichi
SCHMIDT, Azriel
TOWLER, Dwight
SAHOO, Soumya, P.
RODAN, Gideon, A.
Title: ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF
Abstract:
Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the androgen receptor in a patient, and in particular the method wherein the androgen receptor is antagonized in the prostate of a male patient or in the uterus of a female patient and agonized in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, arthritis and joint repair, alone or in combination with other active agents. In addition, these compounds are useful as pharmaceutical composition ingredients alone and in combination with other active agents.