Title:
【発明の名称】エストロゲン関連治療用のノンステロイド系四環式化合物
Document Type and Number:
Japanese Patent JP2003528858
Kind Code:
A
Abstract:
The invention provides non-steroidal estrogenic compounds with estrogenic and anti-estrogenic compounds effects for treatment of estrogen-deficiency related disorders, which compounds are having formula (I) wherein, one of Ror Ris 'R; Rand 'Rare OH, optionally independently etherified or esterified; X is N or -C(R<1>)-, wherein R<1 >is H1 halogen, CN, optionally substituted aryl, (1C-4C)alkyl, (2C-4C)alkenyl, (2C-4C)alkynyl or (3C-6C)cycloalkyl, which alkyl, alkenyl, alkynyl and cycloalkyl groups can optionally be substituted with one or more halogens; Y is N or -C(R<2>)-, with the proviso that X and Y are not both N, wherein R<2 >has the same meaning as defined for R<1>; Z is C(R<3>,'R<3>)- or -C(R<4>,∝R<4>)-C(R<5>,'R<5>)-, wherein R<3>, 'R<3>, R<4>, 'R<4>, R<5>, and 'R<5>, independently arc H, (1C-4C)alkyl, (2C-4C)alkenyl or (3C-6C) cycloalkyl, which alkyl, alkenyl and cycloalkyl groups can optionally be substituted with one or more halogens. These compounds are useful for estrogen-receptor related treatments in view of a desirable profile of activity for estrogen alpha and estrogen beta receptors.
Inventors:
Huenemann, Heritage
Deswald, Ed Walt
Rosen, Hiyu Belt
Mestress, jjorday
Deswald, Ed Walt
Rosen, Hiyu Belt
Mestress, jjorday
Application Number:
JP2001570626A
Publication Date:
September 30, 2003
Filing Date:
March 21, 2001
Export Citation:
Assignee:
Akzo Novel N B
International Classes:
A61K31/047; A61K31/05; A61K31/09; A61K31/473; A61P5/30; A61P15/08; A61P19/10; A61P35/00; C07C33/36; C07C33/38; C07C33/50; C07C39/17; C07C39/23; C07C39/42; C07C43/21; C07C43/215; C07C43/225; C07C43/23; C07C69/017; C07C69/28; C07D221/18; (IPC1-7): C07C39/17; A61K31/05; A61K31/473; A61P15/08; A61P19/10; A61P35/00; C07C39/23; C07C39/42; C07C43/21; C07C43/215; C07C43/225; C07C43/23; C07C69/28; C07D221/18
Domestic Patent References:
| JP2001501197A | 2001-01-30 | |||
| JP2001501197A | 2001-01-30 |
Foreign References:
| EP1559707A1 | 2005-08-03 | |||
| WO1992021661A1 | 1992-12-10 | |||
| EP1559707A1 | 2005-08-03 | |||
| WO1992021661A1 | 1992-12-10 |
Other References:
JPN6009003679, 生化学辞典, 19891120, 第３版, ｐ．１８６−１８７
JPN6009003676, Ａｎｎｉｅ Ｂａｒｓａｌｏｕ， ｅｔ ａｌ．, Ｊｏｕｒｎａｌ ｏｆ Ｂｉｏｌｏｇｉｃａｌ Ｃｈｅｍｉｓｔｒｙ, 1998, Ｖｏｌ．２７３， Ｎｏ．２７, ｐ．１７１３８−１７１４６
JPN6009003674, Ｃｈａｒｌｅｓ Ｅ． Ｍｏｒｒｅａｌ， ｅｔ ａｌ．, Ｊｏｕｒｎａｌ ｏｆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ, 1982, Ｖｏｌ．２５， Ｎｏ．３, ｐ．３２３−３２６
JPN6009003681, Ｊ．Ａ．Ｂｅｉｓｌｅｒ, Ｊｏｕｒｎａｌ ｏｆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ, 1971, Ｖｏｌ．１４， Ｎｏ．１１, ｐ．１１１６−１１１８
JPN6009045024, Ｂａｒａｎ Ｋ．Ｍｅｈｔａ， ｅｔ ａｌ．, Ｔｅｔｒａｈｅｄｒｏｎ, 1999, Ｖｏｌ．５５， Ｎｏ．４４, ｐ．１２８４３−１２８５２
JPN6009003676, Ａｎｎｉｅ Ｂａｒｓａｌｏｕ， ｅｔ ａｌ．, Ｊｏｕｒｎａｌ ｏｆ Ｂｉｏｌｏｇｉｃａｌ Ｃｈｅｍｉｓｔｒｙ, 1998, Ｖｏｌ．２７３， Ｎｏ．２７, ｐ．１７１３８−１７１４６
JPN6009003674, Ｃｈａｒｌｅｓ Ｅ． Ｍｏｒｒｅａｌ， ｅｔ ａｌ．, Ｊｏｕｒｎａｌ ｏｆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ, 1982, Ｖｏｌ．２５， Ｎｏ．３, ｐ．３２３−３２６
JPN6009003681, Ｊ．Ａ．Ｂｅｉｓｌｅｒ, Ｊｏｕｒｎａｌ ｏｆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ, 1971, Ｖｏｌ．１４， Ｎｏ．１１, ｐ．１１１６−１１１８
JPN6009045024, Ｂａｒａｎ Ｋ．Ｍｅｈｔａ， ｅｔ ａｌ．, Ｔｅｔｒａｈｅｄｒｏｎ, 1999, Ｖｏｌ．５５， Ｎｏ．４４, ｐ．１２８４３−１２８５２
Attorney, Agent or Firm:
Yoshio Kawaguchi (4 outside)
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