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US 2009/0221841 A1Published application
2-substituted estra-1,3,5(10)-triene-3-yl sulfamate with an anti-tumour action
AssigneeSterix Limited
InventorsAlexander HILLISCH, Olaf Peters, Christian Gege, Wilko Regenhardt, Dirk Kosemund, Gerhard Siemeister, Eberhard Unger, Ulrich Bothe
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Abstract
The invention relates to the use of 2-substituted estra-1,3,5(10)-triene-3-yl sulfamates of general formula I, in addition to their pharmaceutically acceptable salts for producing a medicament. Said compounds have an anti-tumour action.
Claims12
1-14. (canceled)
A 2-Substituted estra-1,3,5(10)-trien-3-yl sulfamates compound of formula I
- wherein
- R1 is hydrogen, C1-C8-alkyl-4 or C1-C5-acyl;
- R2 is C1-C8-alkoxy, C1-C5-alkyl or —O—CnFmHo, wherein n=1, 2, 3, 4, 5 or 6, m>1 and m+o=2n+1, wherein
- if R2 is C1-C5-alkyl, R17 is C1-C5-alkoxy;
- R6 is hydrogen;
- R7 is hydrogen, hydroxy, amino, acylamino, or
- if R6 and R7 are not hydrogen, then R17 is C1-C5-alkoxy and R6 and R7 together represent oxygen, oxime or O(C1-C5-alkyl)-oxime;
- R14 and R15 in each case is hydrogen or together a methylene group,
- R16 is hydrogen, C1-C5-alkyl, or fluorine;
- R17 is hydrogen, fluorine, or if R15 is hydrogen, R17 is a group CHXY, wherein
- X is hydrogen, fluorine, hydroxy, or C1-C4-alkyl, and
- Y is hydrogen or fluorine, wherein
- if X is fluorine, Y is hydrogen or fluorine, and
- if X is hydroxy, Y is hydrogen, or
- X and Y together are oxygen, or
- if R16 is fluorine, R17 is hydrogen or fluorine, or
- R16 and R17 together are a group ═CAB, wherein A and B, independently of one another, are hydrogen, fluorine or C1-C8-alkyl;
- and
- R18 is hydrogen atom, or methyl,
- wherein in the B- and D-rings of the steroid skeleton compound of formula I, the dotted lines represent 0, 1, or 2 double bonds, provided that when a double bond is present in the D ring, only one of R16 and R17 is present, or a pharmaceutically acceptable salt of the compound.
17 more elements
(canceled)
Dependencies are inferred from the claim text.