发明名称 NICHT-STEROIDALE TETRACYCLISCHE VERBINDUNGEN FÜR ÖSTROGEN-VERWANDTE BEHANDLUNGEN
摘要 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 R<a >or R<b >is 'R<e>; R<e >and 'R<e >are 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>,&prop;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.
申请公布号 DE60130748(T2) 申请公布日期 2008.07.17
申请号 DE2001630748T 申请日期 2001.03.21
申请人 N.V. ORGANON 发明人 VEENEMAN, GERRIT;DE ZWART, EDUARD WILLEM;LOOZEN, HUBERT JAN;MESTRES, JORDI
分类号 C07D221/18;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 主分类号 C07D221/18
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