Sigma Ligands For the Prevention or Treatment of Pain Induced by Chemotherapy
US-2016220575-A1 · Aug 4, 2016 · US
US9782483B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9782483-B2 |
| Application number | US-201113698718-A |
| Country | US |
| Kind code | B2 |
| Filing date | May 20, 2011 |
| Priority date | May 21, 2010 |
| Publication date | Oct 10, 2017 |
| Grant date | Oct 10, 2017 |
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The invention refers to the use of a sigma ligand, preferably a sigma ligand of formula (I), to prevent or treat emesis induced by a chemotherapeutic agent or radioactivity, especially emesis induced by taxanes, vinca alkaloids or platin chemotherapeutic drugs.
Opening claim text (preview).
The invention claimed is: 1. A method for treating a patient afflicted with or at risk of emesis induced by chemotherapy or by radiotherapy comprising administering to the patient a selective sigma-1 receptor ligand in an amount effective to treat the patient, wherein the patient has cancer and is undergoing chemotherapy or radiotherapy and wherein the selective sigma-1 receptor ligand is 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl} morpholine or a pharmaceutically acceptable salt or solvate thereof. 2. The method of claim 1 , for the simultaneous treatment of chemotherapy or radiotherapy-induced emesis, and pain. 3. The method of claim 1 , wherein the selective sigma-1 receptor ligand is 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl} morpholine hydrochloride. 4. A method for the treatment of cancer and simultaneous treatment of emesis induced by chemotherapy or radiotherapy in a patient, comprising administering to the patient a therapeutically effective amount of a combination of at least one selective sigma-1 receptor ligand and a least one chemotherapeutic drug simultaneously, separately or sequentially, wherein the selective sigma-1 receptor ligand is 4-{2[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl} morpholine or a pharmaceutically acceptable salt or solvate thereof. 5. The method of claim 4 , wherein the chemotherapeutic drug is selected from the group consisting of taxanes, vinca alkaloids and drugs derived from platinum. 6. The method of claim 4 , wherein the chemotherapeutic drug is selected from the group consisting of paclitaxel, oxaliplatin and vincristine. 7. The method of claim 4 , comprising administering to the patient 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl} morpholine or a pharmaceutically acceptable salt or solvate thereof and paclitaxel. 8. The method of claim 4 , comprising administering to the patient 4-{2-[5-Methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl} morpholine or a pharmaceutically acceptable salt or solvate thereof and oxaliplatin. 9. The method of claim 4 , comprising administering to the patient 4-{2-[5-Methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl} morpholine or a pharmaceutically acceptable salt or solvate thereof and vincristine. 10. The method of claim 4 , wherein the selective sigma-1 receptor ligand is 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl} morpholine hydrochloride. 11. The method of claim 4 , comprising administering to the patient 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl} morpholine hydrochloride and paclitaxel. 12. The method of claim 4 , comprising administering to the patient 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl} morpholine hydrochloride and oxaliplatin. 13. The method of claim 4 , comprising administering to the patient 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl} morpholine hydrochloride and vincristine.
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