Title:
アンドロゲン受容体調節剤としてのアンドロスタン17β-カルボキサミド類
Document Type and Number:
Japanese Patent JP4490689
Kind Code:
B2
Abstract:
Compounds of structural formula 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 activating the function of the androgen receptor in a patient, and in particular the method wherein the function of the androgen receptor is blocked in the prostate of a male patient or in the uterus of a female patient and activated 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, female sexual dysfunction, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents.
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Inventors:
One, Chiapin
Mark Gun, Dagan
Whitman, Debit Bee
Mark Gun, Dagan
Whitman, Debit Bee
Application Number:
JP2003532514A
Publication Date:
June 30, 2010
Filing Date:
September 27, 2002
Export Citation:
Assignee:
Merck Sharp End Dome Corporation
International Classes:
A61K45/00; C07J3/00; A61K31/56; A61K31/568; A61P1/02; A61P3/00; A61P3/06; A61P5/26; A61P7/06; A61P9/10; A61P15/08; A61P19/10; A61P21/00; A61P31/18; A61P35/00; A61P37/06
Domestic Patent References:
| JP11513981A | ||||
| JP10509188A | ||||
| JP6279487A |
Other References:
XIA, P.,Anti-AIDS Agents. Part 36: 17-Carboxylated Steroids as Potential Anti-HIV Agents,Bioorganic & Medicinal Chemistry,1999年,7(9),p. 1907-1911
XIA, P.,Synthesis of N-substituted 3-oxo-17β-carboxamide-4-aza-5α-androstanes and the tautomerism of 3-oxo-4-aza-5-androstanes,Heterocycles,1998年,47(2),p. 703-716
XIA, P.,Synthesis of N-substituted 3-oxo-17β-carboxamide-4-aza-5α-androstanes and the tautomerism of 3-oxo-4-aza-5-androstanes,Heterocycles,1998年,47(2),p. 703-716
Attorney, Agent or Firm:
Yoshio Kawaguchi
Akio Ichiiri
Makoto Ono
Katsuma Osaki
Mitsuaki Tsubokura
Akio Ichiiri
Makoto Ono
Katsuma Osaki
Mitsuaki Tsubokura