Treatment of dementia and neurodegenerative diseases with intermediate doses of LHRH antagonists
View Patent ↗The present invention relates to the treatment of dementia and neurodegenerative diseases like Alzheimer's disease with intermediate doses of LHRH antagonists which do not cause a castration. A preferred LHRH antagonist is cetrorelix.
1. A method of treatinig Alzheimer's disease in humans comprising the administration of an LHRH antagonist at a monthly dose of about 60 mg to about 100 mg to an Alzheimer's disease patient, wherein said monthly dose is administered as a single dose, and wherein said LHRH antagonist is selected from the group consisting of cetrorelix, teverelix, antide, abarelix, D-63153 and peptidomimetics, wherein said peptidomimetic is selected from the group consisting of:
1-[7-Chloro-3-(3,5-dimethyl-phenyl)-2-oxo-4-(2-piperidin-2-yl-ethoxy)-1,2-dihydro-quinolin-6-yl]-3-pyridin-2-yl-urea;
3-[Benzyl-methyl-amino)-methyl]-2-tert-butyl-8-(2-fluoro-benzyl)-6-(3-methoxyphenyl)-7-methyl-8H-imidazo[1,2-a]pyrimidin-5-one;
2-(2,5-Dimethyl-furan-3-yl)-8-(2-fluoro-benzyl)-3-([methyl-(2-pyridin-2-yl-ethyl)-amino]-methyl)-5-oxo-5,8-dihydro-imidazo[1,2-a]pyrimidine-6-carboxylic acid 1-ethyl-propylester; and
3-((2-[2-(3,5-Difluoro-phenyl)-1-(2-methoxy-benzoyl)-2-oxo-ethylidene]-2,3-dihydro-1H-benzoimidazol-5-yl-amino)-methyl)-benzonitrile.
2. The method of claim 1 , wherein said monthly dose is about 60 mg.
3. The method of claim 1 , wherein the administration Is continued for a month, two months or several months.
4. The method of claim 1 , wherein said monthly dose is administered as a single dose.
5. The method of claim 1 , wherein the treatment leaves sex hormone levels in the human receiving the treatment above the chemical castration threshold.
6. A method of treating Alzheimer's disease in humans comprising administration to a human in need thereof a single dose of about 60mg of cetrorelix per month.
7. The method of claim 6 , wherein the treatment is continued for two or more months.
8. The method of claim 1 , wherein said LHRH antagonist is cetrorelix.
9. The method of claim 1 , wherein the LHRH antagonist is D-63153.
10. The method of claim 1 , wherein said monthly dose is about 100 mg.
11. A method of treating Alzheimer's disease in humans comprising administering to a human need thereof a single dose of about 100mg of D-63153 per month.
12. The method of claim 11 wherein treatment is continued for two or more months.
13. A method of treating Alzheimer's disease in humans comprising administering to a human in need thereof a single dose of about 60mg of D-63153 per month.
14. A method of treating Alzheimer's disease in humans comprising the administration of an LHRH antagonist at a monthly dose of about 30 mg to about 100 mg to an Alzheimer's disease patient, wherein said monthly dose is administered as a single dose, and wherein said LHRH antagonist is selected from the group consisting of cetrorelix, teverelix, antide, abarelix, D-63153 and peptidomimetics, wherein said peptidomimetics is selected from the group consisting of:
1-[7-Chloro-3-(3,5-dimethyl-phenyl)-2-oxo-4-(2-piperidin-2-yl-ethoxy)-1,2-dihydro-quinolin-6-yl]-3-pyridin-2-yl-urea;
3-[Benzyl-methyl-amino)-methyl]-2-tert-butyl-8-(2-fluoro-benzyl)-6-(3-methoxyphenyl)-7-methyl-8H-imidazo[1,2-a]pyrimidin-5-one;
2-(2,5-Dimethyl-furan-3-yl)-8-(2-fluoro-benzyl)-3-([methyl-(2-pyridin-2-yl-ethyl)-amino]-methyl)-5-oxo-5,8-dihydro-imidazo[1,2-a]pyrimidine-6-carboxylic acid 1-ethyl-propylester; and
3-((2-[2-(3,5-Difluoro-phenyl)-1-(2-methoxy-benzoyl)-2-oxo-ethylidene]-2,3-dihydro-1H-benzoimidazol-5-yl-amino)-methyl)-benzonitrile.