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Details for Patent: 7,005,452

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Details for Patent: 7,005,452

Title:Use of the dextrogyral enantiomer of milnacipran for the preparation of a drug
Abstract: The present invention concerns the use of a mixture of enantiomers enriched in the dextrogyral enantiomer of milnacipran and/or of at least one of its metabolites, as well as their pharmaceutically-acceptable salts, for the preparation of a drug intended to prevent or to treat disorders that can be managed by double inhibition of serotonin (5-HT) and norepinephrine (NE) reuptake, while limiting the risks of cardiovascular disturbances and/or organ and/or tissue toxicity.
Inventor(s): Deregnaucourt; Jean (Paris, FR), Grosse; Richard (Gidy, FR)
Assignee: Pierre Fabre Medicament (Boulogne Billancourt, FR)
Filing Date:Jun 03, 2003
Application Number:10/453,574
Claims:1. A method for treating a patient afflicted with a condition or disorder which may be treated by double inhibition of serotonin (5-HT) and norepinephrine (NE) reuptake, while limiting the risks of cardiovascular disturbances and/or the risks of organ and/or tissue toxicity, comprising the step of administering to the patient an amount of a mixture of enantiomers of milnacipran hydrochloride (Z(.+-.)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropanecarboxamide hydrochloride), such mixture being substantially pure in the dextrogyral enantiomer, effective for alleviation of the condition or disorder, wherein the administration of said mixture limits the risks of cardiovascular disturbances and/or the risks of organ and/or tissue toxicity, relative to administration of racemic milnacipran hydrochloride.

2. The method of claim 1, wherein the cardiovascular disturbance corresponds to an increase in blood pressure and/or an increase in heart rate.

3. The method of claim 2, wherein the increase in blood pressure corresponds to an increase in diastolic blood pressure.

4. The method of claim 1, wherein the organ toxicity is cardiac toxicity and the tissue toxicity is hepatic and/or renal toxicity.

5. The method of claim 1, wherein mass/mass ratio between the dextrogyral enantiomer and levogyral enantiomer in the mixture is greater than 95:5 (dextrogyral:levogyral).

6. The method of claim 1, wherein mass/mass ratio between the dextrogyral enantiomer and levogyral enantiomer in the mixture is greater than 99:1 (dextrogyral:levogyral).

7. The method of claim 1, wherein mass/mass ratio between the dextrogyral enantiomer and levogyral enantiomer in the mixture is greater than 99:5:0.5 (dextrogyral:levogyral).

8. The method of claim 1, wherein the disorder or condition is selected from depression, bi-polar disease, schizophrenia, generalised anxiety, morose and marasmic states, stress-related diseases, panic attacks, phobias, obsessive-compulsive disorders, behavioural disorders, oppositional disorders, post-traumatic stress disorder, depression of the immune System, fatigue and the associated pain syndromes, chronic fatigue syndrome, fibromyalgia, and other functional somatic disorders, autism, disorders characterised by attention deficit due to general health status, attention disorders due to hyperactivity, eating disorders, neurotic bulimia, neurotic anorexia, obesity, psychotic disorders, apathy, migraine, pain, irritable bowel syndrome, cardiovascular diseases, neuro-degenerative diseases and the associated anxiety-depressive syndromes (Alzheimer's disease, Huntington's chorea, Parkinson's disease), urinary incontinence and drug addiction.

9. The method of claim 8, wherein depression is selected from deep depression, resistant depression, depression in the elderly, psychotic depression, depression induced by treatments with interferon, depressive state, manic-depressive syndrome, seasonal depressive episodes, depressive episodes related to general health status, depression related to mood-altering substances.

10. The method of claim 8, wherein the phobia is agoraphobia.

11. The method of claim 8, wherein the pain is chronic pain.

12. The method of claim 8, wherein the cardiovascular disease is selected from anxiety-depressive syndrome in myocardial infarct or in hypertension.

13. The method of claim 8, wherein the urinary incontinence is selected from urinary incontinence related to stress and enuresis.

14. The method of claim 8, wherein the drug addiction is selected from anxiety addiction to tobacco, to nicotine, to alcohol, to narcotics, to drugs, and to an analgesic used in weaning-off from these addictive states.

15. The method of claim 1, wherein the patient is selected from children, the elderly, patients with hepatic and/or renal insufficiency, patients receiving treatment that induces hepatic or renal organ and/or tissue toxicity, patients receiving treatment for a heart condition, patients receiving treatment that induces cardiovascular side-effects, patients having a history of cardiovascular disease and/or suffering from cardiovascular disorders.

16. The method of claim 15, wherein the history of cardiovascular disease and/or cardiovascular disorders are chosen among myocardial infarct, cardiac rhythm disorders (tachycardia, bradycardia, palpitations), blood pressure disorders (hypo- or hypertensive patients) and heart disease.

17. A method for treating a patient afflicted with depression, while limiting the risks of cardiovascular disturbances and/or the risks of organ and/or tissue toxicity, comprising the step of administering to the patient an amount of: a) a mixture of enantiomers substantially pure in the dextrogyral enantiomer of milnacipran hydrochloride (Z(.+-.)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropanecarboxamide hydrochloride), wherein the administration of said mixture limits the risks of cardiovascular disturbances and/or the risks of organ and/or tissue toxicity, relative to administration of racemic milnacipran hydrochloride, and b) at least one active compound selected from the psychotropics, as associated products for use simultaneously, separately or staggered in time, effective for alleviation of depression.

18. The method of claim 17, wherein the psychotropics are selected from antidepressants and antimuscarinic agents.

19. The method according to claim 17, wherein the depression is selected from deep depression, resistant depression, depression in the elderly, psychotic depression, depression induced by treatments with interferon, depressive state, manic-depressive syndrome, seasonal depressive episodes, depressive episodes related to general health status, depression related to mood-altering substances.

20. A method for treating a patient afflicted with a condition or disorder which may be treated by double inhibition of serotonin (5-HT) and norepinephrine (NE) reuptake, while limiting the risks of cardiovascular disturbances and/or the risks of organ and/or tissue toxicity, comprising the step of administering to the patient an amount of: a) a mixture of enantiomers substantially pure in the dextrogyral enantiomer of milnacipran hydrochloride (Z(.+-.)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropanecarboxamide hydrochloride), wherein the administration of said mixture limits the risks of cardiovascular disturbances and/or the risks of organ and/or tissue toxicity, relative to administration of racemic milnacipran hydrochloride, and b) at least one other active substance selected from the active compounds that induce organ toxicity and the active compounds that induce cell toxicity, as associated products for use simultaneously, separately or staggered in time, effective for alleviation of the condition or disorder.

21. The method of claim 20, wherein the cell toxicity is hepatic and/or renal toxicity.

22. A method for treating a patient afflicted with a condition or disorder which may be treated, by double inhibition of serotonin (5-HT) and norepinephrine (NE) reuptake while limiting the risks of cardiovascular disturbances and/or the risks of organ and/or tissue toxicity, comprising the step of administering to the patient an amount of: a) a mixture of enantiomers substantially pure in the dextrogyral enantiomer of milnacipran hydrochloride (Z(.+-.)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropanecarboxamide hydrochloride), wherein the administration of said mixture limits the risks of cardiovascular disturbances and/or the risks of organ and/or tissue toxicity, relative to administration of racemic milnacipran hydrochloride, and b) at least one other active substance selected from the active compounds that induce cardiovascular side-effects, as associated products for use simultaneously, separately or staggered in time, effective for alleviation of the condition or disorder.
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