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    • 10. 发明授权
    • 14.beta.-H-, 14-and 15-En-11.beta.-aryl-4-oestrenes
    • 14β-H,14和15-En-11β-芳基-4-盎司
    • US5426102A
    • 1995-06-20
    • US81269
    • 1993-06-22
    • Wolfgang SchwedeEckhard OttowGunter NeefArwed CleveKrzysztof ChwaliszHorst Michna
    • Wolfgang SchwedeEckhard OttowGunter NeefArwed CleveKrzysztof ChwaliszHorst Michna
    • A61K31/57A61K31/58A61K31/585A61P5/38C07J1/00C07J3/00C07J5/00C07J7/00C07J9/00C07J17/00C07J21/00C07J33/00C07J41/00C07J43/00
    • C07J1/0092C07J1/0088C07J1/0096C07J17/00C07J33/002C07J41/0094C07J43/003C07J9/00
    • Novel compounds of the general formula I ##STR1## and the pharmacologically tolerable addition salts thereof with acids are described, in which eitherIa) R.sup.11 represents a hydrogen atom in the .beta.-configuration and each of R.sup.12 and R.sup.13 represents a hydrogen atom, orIb) R.sup.11 represents a hydrogen atom in the .beta.-configuration and R.sup.12 and R.sup.13 together represent a second bond, orIc) R.sup.11 and R.sup.12 together represent a second bond and R.sup.13 represents a hydrogen atom, orId) R.sup.11 represents a hydrogen atom in the .alpha.-configuration and R.sup.12 and R.sup.13 together represent a second bond,and in Ia), Ib), Ic) or Id)X represents an oxygen atom, the hydroxyimino grouping >N.about.OH or two hydrogen atoms,R.sup.1 represents a hydrogen atom or a methyl group,R.sup.2 represents a hydroxy group, a C.sub.1 -C.sub.10 -alkoxy group or a C.sub.1 -C.sub.10 -acyloxy group, andR.sup.3 and R.sup.4 have the meanings customary for competitive progesterone antagonists specified in the description.The invention relates also to processes for the preparation of the novel compounds, to pharmaceutical compositions containing those compounds, to their use for the manufacture of medicaments, and to the novel intermediates required for the process.The novel compounds have a strong affinity for the gestagen receptor and exhibit pronounced antigestagenic and also antiglucocorticoid, antimineralocorticoid and antiandrogenic properties.
    • PCT No.PCT / EP91 / 02494 371日期:1993年6月22日 102(e)日期1993年11月1日PCT 1991年12月21日PCT PCT。 出版物WO92 / 11278 描述了通式I的新型化合物(Ⅰ)及其与酸的药理学上可以忍受的加成盐,其中Ia)R11表示β-构型中的氢原子, R 12和R 13表示氢原子,或Ib)R 11表示β构型中的氢原子,R 12和R 13一起表示第二键,或者Ic)R 11和R 12一起表示第二键,R 13表示氢原子,或 Id)R11表示α-构型中的氢原子,R 12和R 13一起表示第二键,并且在Ia),Ib),Ic)或Id)中X表示氧原子,羟基亚氨基> N不同OH或两个 氢原子,R 1表示氢原子或甲基,R 2表示羟基,C 1 -C 10 - 烷氧基或C 1 -C 10 - 酰氧基,R 3和R 4具有常规用于在 描述。 本发明还涉及制备新化合物的方法,含有这些化合物的药物组合物,其用于制备药物的方法以及该方法所需的新型中间体。 新化合物对于孕激素受体具有强烈的亲和力,并且具有显着的抗原成分和抗糖皮质激素,抗皮质激素和抗雄激素的特性。