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2. 发明申请

WO2004101594A1 NEW MONO-AND BISMETHYLENE-STEROID DERIVATIVES AND PROCESS FOR THEIR SYNTHESIS 审中-公开
标题翻译：新的单 - 和双甲硅烷基甾体衍生物及其合成方法
公开(公告)号：WO2004101594A1
公开(公告)日：2004-11-25
申请号：PCT/HU2004/000027
申请日：2004-03-25
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , TUBA, Zoltán , DANCSI, Lajosné , FRANCSICSNÉ CZINEGE, Erzsébet , FALKAY, György , ZUPKÓ, István , MÁRKI, Árpád , MOLNÁR, Csaba , CSÖRGEI, János , DUKÁTNÉ ABRÓK, Vilma , BALOGH, Gábor , MÁK, Marianna
发明人： TUBA, Zoltán , DANCSI, Lajosné , FRANCSICSNÉ CZINEGE, Erzsébet , FALKAY, György , ZUPKÓ, István , MÁRKI, Árpád , MOLNÁR, Csaba , CSÖRGEI, János , DUKÁTNÉ ABRÓK, Vilma , BALOGH, Gábor , MÁK, Marianna
IPC分类号： C07J7/00
CPC分类号： C07J7/00 , C07J11/00
摘要： The invention relates to new mono- and bismethylene-steroid derivatives of general formula (I) - wherein Z represents two hydrogen atoms or an oxo group; X and Y independently of each other represent either two hydrogen atoms of a CH 2 = group, with the restriction that at least one of them is CH 2 = group and if the meaning of Z is oxo group Y represents two hydrogen atoms, R represents a C 1 -C 4 alkyl group, as well as the pharmaceutical compositions containing the above compounds as active ingredients, and the processes for the synthesis of active ingredients and pharmaceutical compositions. The invention also relates to the methods of treatments with these compounds, which means administering to a mammal to be treated with progestogen - including human - effective amount/amounts of the active ingredients of the present invention as such or as medicament. The mono- and bismethylene-steroid derivatives of the general formula (I) have progestogen effect. They can be used as active ingredients of contraceptive medicaments as such or in combination with an estrogen component. Furthermore, they can be used in the treatment of endometriosis and in the substitution therapy of estrogen as gestagen agent beside the estrogen component. The mono- and bismethylene-steroid derivatives of the general formula (I) of the present invention can be synthesized by reacting a compound of the general formula (II), - wherein the meaning of Z, X and Y is as described for the compounds of formula (I) - with an acid anhydride of the general formula (R-CO) 2 O or with an acid chloride of the general formula R-CO-Cl - wherein R represents a C 1 -C 4 alkyl group - in the presence of a strong acid.
摘要翻译：本发明涉及通式（I）的新型单 - 和二亚甲基 - 类固醇衍生物 - 其中Z代表两个氢原子或氧代基; X和Y彼此独立地表示CH 2 =基团的两个氢原子，限制为它们中的至少一个是CH 2 =基团，如果Z的含义是氧代基团Y，则表示两个氢原子，R表示C1 -C4烷基，以及含有上述化合物作为活性成分的药物组合物，以及合成活性成分和药物组合物的方法。本发明还涉及用这些化合物治疗的方法，这意味着给哺乳动物施用孕激素 - 包括人有效量/本发明的活性成分本身或作为药物。通式（I）的单和二亚甲基类固醇衍生物具有孕激素作用。它们可以作为避孕药物的有效成分本身或与雌激素成分组合使用。此外，它们可用于治疗子宫内膜异位症和雌激素组分除外作为孕激素替代治疗。本发明的通式（I）的单和二亚甲基类固醇衍生物可以通过使通式（II）的化合物与其中Z，X和Y的含义如化合物式（I）的化合物与通式为（R-CO）2 O的酸酐或通式为R-CO-Cl的酰氯（其中R表示C1-C4烷基）在式强酸。

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