16,17-carbocyclic condensed steroid compounds having...

Organic compounds -- part of the class 532-570 series – Organic compounds – Cyclopentanohydrophenanthrene ring system containing

Reexamination Certificate

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C552S514000, C514S169000, C514S178000, C514S182000

Reexamination Certificate

active

07868193

ABSTRACT:
The invention discloses a steroid compound having the formula (1), wherein dotted bonds represent optional double bonds; R6is H, ═CH2, or —CH3, or —CH2—CH3; R7is H, C1-4-alkyl, C2-5alkenyl or C2-5-alkynyl, wherein the alkyl, alkenyl or alkynyl group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; R11is H, C1-4-alkyl, C2-4-alkenyl, C2-4-alkynyl or C1-4-alkylidene, wherein the alkyl, alkenyl, alkynyl or alkylidene group may be substituted with 1-3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; E represents together with carbon atoms 16 and 17 of the steroid skeleton a four to seven-membered ring, said ring being α and in cis-configuration with respect to the steroid skeleton, optionally comprising one or two endocyclic bonds; or a prodrug thereof. Such compounds can be used in therapy and for methods for selective modification of the activity of estrogen receptors.

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Mosselman, et al., “ERβ: Identification and Characterization of a Novel Human Estrogen Receptor,”FEBS Letters, 392, 1996, pp. 49-53.
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Ederveen, A.G.H., et al., “Tibolone, a Steroid with a Tissue-Specific Hormonal Profile, Completely Prevents Ovariectomy-Induced Bone Loss in Sexually Mature Rats,”J. Bone Min. Res. vol. 14, 1999, pp. 1963-1970.
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