Title:
1-PHENYL-2-PHENYLETHANE DERIVATIVE
Document Type and Number:
WIPO Patent Application WO/2020/085373
Kind Code:
A1
Abstract:
The present invention provides a novel compound which has activating activity selective for ERβ. A compound represented by formula (1) or a salt thereof.
(In the formula, R1 represents a cycloalkyl group having 3-8 carbon atoms, an alkenyl group which may be substituted by a halogen atom and has 2-6 carbon atoms, a five-membered nitrogen-containing heteroaryl group, a four- to six-membered cyclic amino group, an alkanoylamino group which may be substituted by a halogen atom and has 2-6 carbon atoms, a 1-trifluoromethyl-1-hydroxymethyl group or a 1-methylpropyl group; R2-R5 may be the same or different and each represents a hydrogen atom or a fluorine atom; and R6 represents a hydrogen atom or an alkanoyl group having 2-5 carbon atoms.)
Inventors:
MISAWA KENSUKE (JP)
INOUE TAKAYOSHI (JP)
TSUNODA SHOTARO (JP)
INOUE TAKAYOSHI (JP)
TSUNODA SHOTARO (JP)
Application Number:
PCT/JP2019/041506
Publication Date:
April 30, 2020
Filing Date:
October 23, 2019
Export Citation:
Assignee:
KAO CORP (JP)
International Classes:
C07C39/16; A61K31/05; A61K31/165; A61K31/222; A61K31/397; A61K31/415; A61K31/4196; A61K31/421; A61K31/4245; A61P5/30; A61P13/08; A61P17/08; A61P17/10; C07C39/17; C07C39/21; C07C39/367; C07C39/373; C07C69/63; C07C233/18; C07D231/12; C07D249/08; C07D263/32; C07D271/06; C07D295/096
Domestic Patent References:
| WO2010030787A1 | 2010-03-18 | |||
| WO2016102472A1 | 2016-06-30 | |||
| WO2018049094A1 | 2018-03-15 | |||
| WO2010030787A1 | 2010-03-18 | |||
| WO2016102472A1 | 2016-06-30 |
Foreign References:
| US3123615A | 1964-03-03 | |||
| JP5990058B2 | 2016-09-07 |
Other References:
WAIBEL, MICHAEL ET AL.: "Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 44, no. 9, 2009, pages 3412 - 3424, XP026322164, DOI: 10.1016/j.ejmech.2009.02.006
TUCCINARDI, TIZIANO ET AL.: "Receptor-based virtual screening evaluation for the identification of estrogen receptor beta ligands", JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 30, no. 4, 2015, pages 662 - 670, XP055710230
NICHOLAS ET AL., AM J CLIN DERMATOL, vol. 4, 2003, pages 371 - 378
HALL ET AL., J AM ACAD DERMATOL, vol. 53, 2005, pages 555 - 68
RENDALL MJ ET AL., MATURITAS, vol. 60, 2008, pages 158 - 69
SATOR ET AL., MATURITAS, vol. 39, 2001, pages 43 - 55
PICRARD-FRANCHIMON ET AL., MATURITAS, vol. 22, 1995, pages 151 - 154
PETER ET AL., J INVEST DERMATOL, vol. 62, 1974, pages 191 - 201
VAN DE WEIJER PH ET AL., MATURITAS, vol. 42, 2002, pages 187 - 93
MUKHERJEE ET AL., PHARM RES, vol. 27, 2010, pages 1439 - 1468
POWELL ET AL., PROC NATL ACAD SCI U S A, vol. 105, 2008, pages 19012 - 19017
KULAKOSKY ET AL., J MOL ENDOCRINOL, vol. 29, 2002, pages 137 - 152
MICHAEL ET AL., GENES DEV, vol. 20, 2006, pages 1405 - 1428
LIU ET AL., PROC NATL ACAD SCI USA, vol. 105, 2008, pages 2604 - 2609
HELGUERO ET AL., ONCOGENE, vol. 24, 2005, pages 6605 - 6616
CHANG ET AL., MOL PHARMACOL, vol. 77, 2010, pages 744 - 750
MEYERS ET AL., J MED CHEM, vol. 44, 2001, pages 4230 - 4251
ENDOCRINOLOGY, vol. 148, 2007, pages 566 - 74
ANDROLOGIA, vol. 47, 2015, pages 1153 - 9
J ENDOCRINOL, vol. 163, 1999, pages 379 - 383
MEYERS ET AL., J. MED. CHEM., vol. 44, 2001, pages 4230 - 4251
THE REPORT OF ARCH DERMATOL RES, vol. 304, 2012, pages 499 - 510
See also references of EP 3872061A4
TUCCINARDI, TIZIANO ET AL.: "Receptor-based virtual screening evaluation for the identification of estrogen receptor beta ligands", JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 30, no. 4, 2015, pages 662 - 670, XP055710230
NICHOLAS ET AL., AM J CLIN DERMATOL, vol. 4, 2003, pages 371 - 378
HALL ET AL., J AM ACAD DERMATOL, vol. 53, 2005, pages 555 - 68
RENDALL MJ ET AL., MATURITAS, vol. 60, 2008, pages 158 - 69
SATOR ET AL., MATURITAS, vol. 39, 2001, pages 43 - 55
PICRARD-FRANCHIMON ET AL., MATURITAS, vol. 22, 1995, pages 151 - 154
PETER ET AL., J INVEST DERMATOL, vol. 62, 1974, pages 191 - 201
VAN DE WEIJER PH ET AL., MATURITAS, vol. 42, 2002, pages 187 - 93
MUKHERJEE ET AL., PHARM RES, vol. 27, 2010, pages 1439 - 1468
POWELL ET AL., PROC NATL ACAD SCI U S A, vol. 105, 2008, pages 19012 - 19017
KULAKOSKY ET AL., J MOL ENDOCRINOL, vol. 29, 2002, pages 137 - 152
MICHAEL ET AL., GENES DEV, vol. 20, 2006, pages 1405 - 1428
LIU ET AL., PROC NATL ACAD SCI USA, vol. 105, 2008, pages 2604 - 2609
HELGUERO ET AL., ONCOGENE, vol. 24, 2005, pages 6605 - 6616
CHANG ET AL., MOL PHARMACOL, vol. 77, 2010, pages 744 - 750
MEYERS ET AL., J MED CHEM, vol. 44, 2001, pages 4230 - 4251
ENDOCRINOLOGY, vol. 148, 2007, pages 566 - 74
ANDROLOGIA, vol. 47, 2015, pages 1153 - 9
J ENDOCRINOL, vol. 163, 1999, pages 379 - 383
MEYERS ET AL., J. MED. CHEM., vol. 44, 2001, pages 4230 - 4251
THE REPORT OF ARCH DERMATOL RES, vol. 304, 2012, pages 499 - 510
See also references of EP 3872061A4
Attorney, Agent or Firm:
THE PATENT CORPORATE BODY ARUGA PATENT OFFICE (JP)
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