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Title:
17β-HSD1、17β-HSD3、および17β-HSD10の阻害剤
Document Type and Number:
Japanese Patent JP2014508784
Kind Code:
A
Abstract:
The present application discloses 17β hydroxy steroid dehydrogenase (17β HSD) type 1, 3, 10 inhibitors and use thereof (alone and in combination) in the treatment of cancer and other afflictions. 17β HSD1 inhibitors include estradiol derivatives with a nieta-carbamoylbenzyl substituent at C 16. 17β HSD3/HSD10 inhibitors include androsterone derivatives substituted at the C3 position with a sulfonamide piperazine. Also disclosed are compounds that are inhibitors of both 17β HSD1 and 17β HSD3 that have a spiro-morpholine substituent at C20.

Inventors:
Donald Polier
Rene Marte
Junie Roy
Application Number:
JP2014500216A
Publication Date:
April 10, 2014
Filing Date:
March 26, 2012
Export Citation:
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Assignee:
UNIVERSITE LAVAL
International Classes:
C07J1/00; A61K31/565; A61K31/566; A61K31/567; A61K31/58; A61K51/00; A61P13/08; A61P15/00; A61P25/28; A61P35/00; A61P35/04; A61P43/00; C07J5/00; C07J43/00
Domestic Patent References:
JPH01132523A1989-05-25
JP2010503718A2010-02-04
JP2008545678A2008-12-18
JP2007510697A2007-04-26
Foreign References:
WO2008065100A12008-06-05
Other References:
MEDICINAL CHEMISTRY, vol. 7(2), JPN6016008805, 2011, pages 80 - 91, ISSN: 0003270383
BIOORGANIC & MEDICINAL CHEMISTRY, vol. 16, JPN6016008807, 2008, pages 1849 - 1860, ISSN: 0003270384
BIOCHEMICAL JOURNAL, vol. 424, JPN6016008809, 2009, pages 357 - 366, ISSN: 0003270385
MOLECULES, vol. (15), JPN6016008811, 2010, pages 1590 - 1631, ISSN: 0003270386
JOURNAL OF STEROID BIOCHEMISTRY, vol. 36(6), JPN6016008812, 1990, pages 617 - 629, ISSN: 0003270387
JOURNAL OF MEDICINAL CHEMISTRY, vol. 45(3), JPN6016008813, 2002, pages 640 - 653, ISSN: 0003270388
ACS MEDICINAL CHEMISTRY LETTERS, vol. 2, JPN6016008814, 17 June 2011 (2011-06-17), pages 678 - 681, ISSN: 0003270389
Attorney, Agent or Firm:
Yasuhiko Murayama
Masatake Shiga
Takashi Watanabe
Shinya Mitsuhiro