Novel 17beta hydroxysteroid dehydrogenase type I inhibitors

    公开(公告)号:AU2004289459A1

    公开(公告)日:2005-05-26

    申请号:AU2004289459

    申请日:2004-11-11

    Abstract: The present invention relates to novel 3, 15 substituted estrone derivatives which represent inhibitory compounds of the 17beta-hydroxysteroid dehydrogenase type I (17beta-HSD1), to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel 3, 15 substituted estrone derivatives, particularly their use in the treatment or prevention of steroid hor­mone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17beta-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17beta-estradiol concentration. In addition, the present invention relates to the general use of selective 17beta-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment and prevention of benign gynaecological disorders, in particular endometriosis.

    19.
    发明专利
    未知

    公开(公告)号:TR200402391T4

    公开(公告)日:2004-12-21

    申请号:TR200402391

    申请日:2002-06-22

    Abstract: 7-Alkyl-3-(substituted phenyl)-9,9-(dialkyl or alkylene)-3,7-diazabicyclo (3.3.1) nonane derivatives (I) are new. Diazabicyclononane derivatives of formula (I) and their acid addition salts are new. R1 = 1-6C alkyl or 4-7C cycloalkylalkyl; R2, R3 = 1-4C alkyl; or R2 + R3 = 3-6C alkylene; and R4 = phenyl (monosubstituted in the ortho- or para-position by NO2, CN or 2-5C alkanoyl) or 2,4-dinitrophenyl. An Independent claim is also included for the preparation of (I).

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