EP 1487783 A2 20041222 - IRREVERSIBLE SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF
Title (en)
IRREVERSIBLE SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF
Title (de)
IRREVERSIBLE, SELEKTIVE MODULATOREN DES ANDROGENREZEPTORS UND VERFAHREN ZU DEREN ANWENDUNG
Title (fr)
MODULATEURS IRREVERSIBLES SELECTIFS DE RECEPTEUR D'ANDROGENE ET PROCEDE D'UTILISATION ASSOCIES
Publication
Application
Priority
- US 0303121 W 20030224
- US 8467902 A 20020228
- US 42024802 P 20021023
Abstract (en)
[origin: WO03074473A2] In one embodiment, 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). The SARM compounds have unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. In one embodiment, the SARM compounds bind irreversibly to the androgen receptor. In another embodiment, the SARM compounds are androgen receptor antagonists which bind irreversibly to the androgen receptor. In another embodiment, the SARM compounds are alkylating agents. 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, osteoporosis, 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.
IPC 1-7
C07C 233/05; C07C 255/50; C07C 331/28; A61K 31/16; A61K 31/26; A61K 31/275
IPC 8 full level
A61K 31/16 (2006.01); A61K 31/26 (2006.01); A61K 31/275 (2006.01); A61P 5/28 (2006.01); A61P 15/16 (2006.01); A61P 27/02 (2006.01); A61P 35/00 (2006.01); C07C 233/05 (2006.01); C07C 255/50 (2006.01); C07C 261/02 (2006.01); C07C 265/12 (2006.01); C07C 331/10 (2006.01); C07C 331/28 (2006.01)
CPC (source: EP KR)
A61K 31/16 (2013.01 - EP); A61K 31/26 (2013.01 - EP); A61K 31/275 (2013.01 - EP); A61P 5/28 (2017.12 - EP); A61P 15/16 (2017.12 - EP); A61P 27/02 (2017.12 - EP); A61P 35/00 (2017.12 - EP); C07C 233/05 (2013.01 - KR); C07C 255/50 (2013.01 - KR); C07C 261/02 (2013.01 - EP); C07C 265/12 (2013.01 - EP); C07C 331/10 (2013.01 - EP); C07C 331/28 (2013.01 - EP KR)
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LI LU MC NL PT SE SI SK TR
DOCDB simple family (publication)
WO 03074473 A2 20030912; WO 03074473 A3 20031218; AU 2003214971 A1 20030916; CA 2476651 A1 20030912; CN 1646479 A 20050727; EA 200401121 A1 20051027; EP 1487783 A2 20041222; EP 1487783 A4 20060927; HR P20040851 A2 20050228; IL 163742 A0 20051218; JP 2005519111 A 20050630; KR 20040104463 A 20041210; MX PA04008412 A 20050517; TW 200304806 A 20031016
DOCDB simple family (application)
US 0303121 W 20030224; AU 2003214971 A 20030224; CA 2476651 A 20030224; CN 03804718 A 20030224; EA 200401121 A 20030224; EP 03710820 A 20030224; HR P20040851 A 20040916; IL 16374203 A 20030224; JP 2003572945 A 20030224; KR 20047013473 A 20030224; MX PA04008412 A 20030224; TW 92104206 A 20030227