Title:
ESTROGEN RECEPTOR β PARTIAL AGONIST HAVING ESTROGEN RECEPTOR α INHIBITORY EFFECT, AND THERAPEUTIC AGENT FOR GYNECOLOGICAL DISORDERS USING SAME
Document Type and Number:
WIPO Patent Application WO2017010515
Kind Code:
A1
Abstract:
[Problem] To provide a therapeutic agent for estrogen-dependent gynecological disorders such as endometriosis, uterine fibroids, and adenomyosis. [Solution] An estrogen receptor α-inhibiting β partial agonist represented by structural formula (a), a pharmaceutically-acceptable salt thereof, or a hydrate of either of the aforementioned is used as an active ingredient.
Inventors:
NAKAO KENICHIRO (JP)
HARADA TASUKU (JP)
TANIGUCHI FUMINORI (JP)
HARADA TASUKU (JP)
TANIGUCHI FUMINORI (JP)
Application Number:
PCT/JP2016/070687
Publication Date:
January 19, 2017
Filing Date:
July 13, 2016
Export Citation:
Assignee:
NOBELPHARMA CO LTD (JP)
NAT UNIV CORP TOTTORI UNIV (JP)
NAT UNIV CORP TOTTORI UNIV (JP)
International Classes:
A61K31/573; A61P15/00; A61P43/00
Domestic Patent References:
| WO2010054758A1 | 2010-05-20 |
Other References:
MINUTOLO F. ET AL.: "Estrogen Receptor beta Ligands: Recent Advances and Biomedical Applications", MEDICINAL RESEARCH REVIEWS, vol. 31, no. 3, 2011, pages 364 - 442, XP055347261
KULAK J JR. ET AL.: "Treatment with Bazedoxifene, a Selective Estrogen Receptor Modulator, Causes Regression of Endometriosis in a Mouse Model", ENDOCRINOLOGY, vol. 152, no. 8, 2011, pages 3226 - 3232, XP055347267
CHUNG Y J. ET AL.: "The Effect of GnRH Agonist,Serm,Antiprogesterone in the Treatment of Uterine Myomas", ACTA OBSTETRICA ET GYNAECOLOGIA JAPONICA, vol. 65, no. 2, 2013, pages 994, XP055347270
MASAHIRO NOZAKI: "The effect of raloxifene on reproductive organs", OBSTETRICAL AND GYNECOLOGICAL THERAPY, vol. 94, no. 5, 2007, pages 967 - 972, XP009508381
TANIGUCHI F. ET AL.: "SR-16234, a selective estrogen receptor modulator, represses development of endemetriosis-like lesions in rat model", ACTA OBSTETRICA ET GYNAECOLOGIA JAPONICA, vol. 68, no. 2, February 2016 (2016-02-01), pages 567, XP009508384
See also references of EP 3323417A4
KULAK J JR. ET AL.: "Treatment with Bazedoxifene, a Selective Estrogen Receptor Modulator, Causes Regression of Endometriosis in a Mouse Model", ENDOCRINOLOGY, vol. 152, no. 8, 2011, pages 3226 - 3232, XP055347267
CHUNG Y J. ET AL.: "The Effect of GnRH Agonist,Serm,Antiprogesterone in the Treatment of Uterine Myomas", ACTA OBSTETRICA ET GYNAECOLOGIA JAPONICA, vol. 65, no. 2, 2013, pages 994, XP055347270
MASAHIRO NOZAKI: "The effect of raloxifene on reproductive organs", OBSTETRICAL AND GYNECOLOGICAL THERAPY, vol. 94, no. 5, 2007, pages 967 - 972, XP009508381
TANIGUCHI F. ET AL.: "SR-16234, a selective estrogen receptor modulator, represses development of endemetriosis-like lesions in rat model", ACTA OBSTETRICA ET GYNAECOLOGIA JAPONICA, vol. 68, no. 2, February 2016 (2016-02-01), pages 567, XP009508384
See also references of EP 3323417A4
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