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Last Updated: April 24, 2024

Claims for Patent: 6,239,144


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Summary for Patent: 6,239,144
Title: Methods of treating bone loss
Abstract:The present invention provides methods of treating or preventing conditions associated with a lack of parathyroid hormone comprising administering to a mammal in need thereof an effective amount of a compound having activity as a tachykinin receptor antagonist. In a most preferred embodiment the present invention provides methods of increasing bone growth in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound having activity as a tachykinin receptor antagonist. Another embodiment of this invention provides methods of treating hyperparathyroidism in a mammal comprising administering to a mammal in need thereof an effective amount of a compound having activity as a tachykinin receptor antagonist.
Inventor(s): Galvin; Rachelle J (Indianapolis, IN), Gitter; Bruce D (Carmel, IN)
Assignee: Eli Lilly and Company (Indianapolis, IN)
Application Number:09/319,388
Patent Claims:1. A method for the treatment of a condition associated with a deficiency of parathyroid hormone in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound or composition having activity as a tachykinin receptor antagonist.

2. A method as claimed in claim 1 wherein the compound having activity as a tachykinin receptor antagonist is (R)-2-[N-(2-((4-cycdohexyl)piperazin-1-yl)acetyl)amino]-3-(1H-indol-3-yl)- 1-[N-(2-methoxybenzyl)acetylamino]propane, (R)-3-(1H-indol-3-yl)-1-[N-(2-methoxybenzyl)acetylamino]-2-[N-(2-(4-piperi din-1-yl)piperidin-1-yl)acetyl)amino]propane, (R)-3-(1H-indol-3-yl)-1-[N-(2-methoxybenzyl)acetylamio]-2-[N-(2-(4-(piperi din-1-yl)piperidin-1-yl)acetyl)amino]propane dihydrohloride trihydrate, 1-(2-bromobenzyl)-2-(3,5-dimethylphenyl)-6-[2-(N,N-dinethylamino)ethoxy]be nzidazole, RP 67580, (.+-.)CP 96345, 5-(3,5-bistrifuoromethylphenyl)-1-(3-indolyl)-2-((4-methylpiperazin-1-yl)a cetamido)-3-pentanone, (4-methylphenyl)methyl [R-(R*,S*)]-[1-(1H-indol-3-ylmethyl)-1-methyl-2-oxo-2-[(1-phenylethyl)amin o]ethyl]carbamate, (S)-1-(2-methoxybenzyl)-2-[(4-phenyl-1-piperazinyl)methyl]-4-(1H-indol-3-y lmethyl)-2-imidazoline, or 1-(3,5-dimethylbenzyloxy)-2-anmino-2-phenylcydohexane, or a pharmaceutically acceptable salt or solvate thereof.

3. A method as claimed in claim 2 employing (R)-3-(1H-indol-3-yl)-1-[N-(2-methoxybenzyl)acetylamino]-2-[N-(2-(4-(piper idin-1-yl)piperidin-1-yl)acetyl)amino]propane dihydrodhloride trihydrate.

4. A method for enhancing bone growth in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound or composition having activity as a tachykinin receptor antagonist.

5. A method as cained in claim 4 wherein the compound having activity as a tachykinin receptor antagonist is (R)-2-[N-(2-((4-cydohexyl)piperazin-1-yl)acetyl)amino]-3-(1H-indol-3-yl)-1 -[N-(2-methoxybenzyl)acetylamino]propane, (R)-3-(1H-indol-3-yl)-1-[N-(2-methoxybenzyl)acetylamino]-2-[N-(2-(4-(piper idin-1-yl)piperidin-1-yl)acetyl)amino]propane, (R)-3-(1H-indol-3-yl)-1-[N-(2-methoxybenzyl)acetylamino]-2-[N-(2-(4-piperi din-1-yl)piperidin-1-yl)acetyl)amino]propane dihydrocloride trihydrate, 1-(2-bromobenzyl)-2-(3,5-dimethylphenyl)-6-[2-(N,N-dimethylamino)ethoxy]be nzimidazole, RP 67580, (.+-.)CP 96345, 5-(3,5-bistifiuoromethylphenyl)-1-(3-indolyl)-2-((4-methylpiperazin-1-yl)a cetamido)-3-pentanone, (4-methylphenyl)methyl [R-(R*,S*)]-[1-(1H-indol-3-ylmethyl)-1-methyl-2-oxo-2-[(1-phenylethyl)amin o]ethyl]carbamate, (S)-1-(2-methoxybenzyl)-2-[(4-phenyl-1-piperazinyl)methyl]-4-(1H-indol-3-y lmethyl)-2-imidazoline, or 1-(3,5-dimethylbenzyloxy)-2-amino-2-phenylcyclohexane, or a pharmaceutically acceptable salt or solvate thereof.

6. A method as daimed in claim 5 employing (R)-3-(1H-indol-3-yl)-1-[N-(2-methoxybenzyl)acetylamio]-2-[N-(2-(4(piperid in-1-yl)piperidin-1-yl)acetyl)amino]propane dihydrochloride trihydrate.

7. A method for treating hyperparathyroidism in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound or composition having activity as a tachykinin receptor antagonist.

8. A method as daimed in claim 7 wherein the compound having activity as a tachykinin receptor antagonist is (R)-2-[N-(2-((4-cydohexyl)piperazin-1-yl)acetyl)amino]-3-(1H-indol-3-yl)-1 -[N-(2-methoxybenzyl)acetylamino]propane, (R)-3-(1H-indol-3-yl)-1-[N-(2-methoxybenzyl)acetylamino]-2-[N-(2-(4-piperi din-1-yl)piperidin-1-yl)acetyl)amino]propane, (R)-3-(1H-indol-3-yl)-1-[N-(2-methoxybenzyl)acetylamino]-2-[N-(2-(4-piperi din-1-yl)piperidin-1-yl)acetyl)amino]propane dihydrochloride trihydrate, 1-(2-bromobenzyl)-2-(3,5-dimethylphenyl)-6-[2-(N,N-dimethylamino)ethoxy]be nzimidazole, RP 67580, (.+-.)CP 96345, 5-(3,5-bistrifluoromethylphenyl)-1-(3-indolyl)-2-((4-methylpiperazin-1-yl) acetamido)-3-pentanone, (4-methylphenyl)methyl [R-(R*,S*)]-[1-(1H-indol-3-ylmethyl)-1-methyl-2-oxo-2-[(1-phenylethyl)amin o]ethyl]carbamate, (S)-1-(2-methoxybenzyl)-2-[(4-phenyl-1-piperazinyl)methyl]-4-(1H-indol-3-y lmethyl)-2-imidazoline, or 1-(3,5-dimethylbenzyloxy)-2-amino-2-phenylcyclohexane, or a pharmaceutically acceptable salt or solvate thereof.

9. A method as daimed in claim 8 employing (R)-3-(1H-indol-3-yl)-1-[N-(2-methoxybenzyl)acetylamino]-2-[N-(2-(4-(piper idin-1-yl)piperidin-1-yl)acetyl)amino]propane dihydrochloride trihydrate.

10. A method for inducing the secretion of parathyroid hormone in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound or composition having activity as a tachykinin receptor antagonist.

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