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US 8,273,716 B2Granted
Use of LHRH antagonists for intermittent treatments
AssigneeSpectrum Pharmaceuticals, Inc.
InventorJuergen Engel
Life of this patent
Estimating the term…
Abstract
The invention relates to methods of treatment or prophylaxis of physiological and/or pathological conditions with at least one LHRH antagonist, in particular at least one peptidomimetic LHRH antagonist such that the at least one LHRH antagonist is administered in a dose, which does not cause chemical (hormonal) castration.
Claims28
A method for treating a prostate cancer, the method comprising:
- administering at least one LHRH antagonist to a subject in need thereof in an amount sufficient to treat the prostate cancer and in a dose which does not cause a chemical or hormonal castration, wherein the at least one LHRH antagonist is a tetrahydrocarbazole derivative with the formula
- wherein V and W are each independently O, S, S+—O−, or geminally linked H2;
- R1 is O, S, or S+—O−;
- R2 is an optionally substituted cycloalkyl, cycloalkylakyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl, or —NHX1, wherein X1 is an optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl, and wherein R2 or X1 is optionally substituted with —F, —Cl, —Br, —I, —CF3, or —OCF3;
- R4m is an optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl, and wherein R4m is optionally substituted with —F, —Cl, —Br, —I, —CF3, or —OCF3;
- R8 is an optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl, and wherein R8 is optionally substituted with —F, —Cl, —Br, —I, —CF3, or —OCF3;
- R10 is an optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, or —C(O)X1004, wherein X1004 is an optionally substituted cycloalkyl, heterocyclyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl, and wherein R10 or X1004 is optionally substituted with —F, —Cl, —Br, —I, —CF3, or —OCF3;
- and
- R17, R18, R10, and R20 are each independently —H, —F, —Cl, —Br, —I, —CF3, or —OCF3.
6 more elements
Dependencies are inferred from the claim text.