【発明の名称】選択的エストロゲンとしての16-ヒドロキシエストラトリエン

Japanese Patent JP2002536455

A

3,16-Dihydroxy-1,3,5(10)-estratriene derivatives (I) are new. 3,16-Dihydroxy-1,3,5(10)-estratriene derivatives of formula (I) are new: [Image] thick black line in ring = single or double bond; R 1>H, halo, OH, Me, CF 3, OMe or OEt; R 2>H, halo, OH or 1-6C optionally saturated alkoxy; R 4>H, halo, 1-10C optionally saturated alkyl, CF 3, C 2F 5or 1-6C optionally saturated alkoxy; R 7>H, halo, 1-10C optionally saturated alkyl (optionally fully or partly fluorinated), 1-6C optionally saturated alkoxy or optionally substituted aryl or heteroaryl; R 8>H, , 1-10C optionally saturated alkyl (optionally fully or partly fluorinated) or CN; R 9>H, Me, Et, CF 3or C 2F 5; R 1>1>H, ONO 2, OH, SH, halo, CH 2Cl, 1-10C optionally saturated alkyl (optionally fully or partly fluorinated), 1-6C optionally saturated alkoxy, 1-6C optionally saturated alkylthio or optionally substituted aryl or heteroaryl; R 1>3>Me, Et, CF 3or C 2F 5; R 1>4>H or 1-10C optionally saturated alkyl (optionally fully or partly fluorinated); R 1>5>H, halo or 1-10C optionally saturated alkyl (optionally fully or partly fluorinated and optionally interrupted by O, S, SO, SO 2or NR 1>5>'); R 1>5>' : H or 1-3C alkyl; R 16>optionally saturated 1-10C alkyl (optionally partly or fully fluorinated), CF 3, or pentafluoroethyl, CN or H ; R 1>7>H, OH, halo or 1-10C optionally saturated alkyl (optionally fully or partly fluorinated); or R 1>4>+R 1>5>optionally mono- or dihalogenated methylene; wavy lines = alpha or beta configuration. Excluded are: 1,3,5(10)-estratriene-3,16alpha -diol (Ia); 1,3,5(10)-estratriene-3,16beta -diol (Ib); 1,3,5(10),7-estratetraene-3,16alpha -diol (Ic); and 1,3,5(10),7-estratetraene-3,16beta -diol (Id). Independent claims are also included for the following: (1) use of compounds (I), including (Ia)-(Id), for treating diseases caused by estrogen deficiency in women and men; (2) use of the partial structure of formula (II) as a component of the total structure of compounds exhibiting a dissociation in estrogenic activity in favor of bone over uterus. [Image] ACTIVITY : Gynecological; uropathic; antiulcer; hemostatic; osteopathic; cardiant; antiarteriosclerotic; nootropic; neuroprotective; antiinflammatory; antiinfertility; immunomodulatory. MECHANISM OF ACTION : Estrogen receptor ligand. The relative binding affinity (estradiol = 100) of (Ia) for rat prostate and uterus estrogen receptors was 50 and 9 respectively, and the ratio of its relative binding affinities for human estrogen receptors alpha and beta was 6 (estradiol = 1).

Hermann Künzer
Rudolph Knaute
Monica wrestle
Karl-Heinrich Fritzheimer
Christa Hegere-Hartung
Wolf Boehmer
Gerd Muller
Dirk Kosemund

JP2000598520A

October 29, 2002

February 09, 2000

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Schering Actien Gezershaft

A61P1/00; A61P5/30; A61P9/00; A61P9/10; A61P13/00; A61P13/02; A61P13/08; A61P19/08; A61P19/10; A61P25/00; A61P25/20; A61P25/28; A61P29/00; A61P35/00; A61P37/00; C07J1/00; C07J15/00; C07J31/00; A61K31/565; C07J33/00; C07J41/00; C07J53/00; (IPC1-7): C07J1/00; A61K31/565; A61P1/00; A61P5/30; A61P9/00; A61P9/10; A61P13/00; A61P13/02; A61P13/08; A61P19/08; A61P19/10; A61P25/00; A61P25/20; A61P25/28; A61P29/00; A61P35/00; A61P37/00

JPS5215592B1

1977-04-30

US2779773A	1957-01-29
GB823955A	1959-11-18
CH538460A	1973-06-30
US3622670A	1971-11-23
US3103524A	1963-09-10
GB804789A	1958-11-26
CH557805A	1975-01-15
US3166473A	1965-01-19
US3282786A	1966-11-01

Toshio Yano (4 outside)

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