JP2008509147A5 - - Google Patents

Claims (32)

Use of N-desmethylclozapine in the preparation of a medicament for the treatment of psychosis due to any cause, wherein the administration pattern of the medicament is
Administering a first dose of N-desmethylclozapine; and subsequently administering a second dose of N-desmethylclozapine, wherein the second dose is higher than the first dose; Use, including process.   The use according to claim 1, wherein the administration pattern comprises identifying whether the patient is sensitive to the second administration after administering the first dose.   Use according to claim 1 or 2, wherein the first dose is 25% of the second dose.   Use according to claim 1 or 2, wherein the first dose is 50% of the second dose.   Use according to any of claims 1 to 4, wherein each dose is administered twice a day.   Use according to any of claims 1 to 5, wherein the psychosis is associated with schizophrenia.   Use according to any of claims 1 to 6, wherein the first dose is a break-in dose.   Use of N-desmethylclozapine in the preparation of a medicament for the treatment of psychosis due to any cause, wherein the administration pattern of the medicament comprises administering N-desmethylclozapine in progressively increasing doses .   Use of N-desmethylclozapine in the preparation of a medicament for the treatment of cognitive dysfunction, wherein the amount of any clozapine administered is net at muscarinic receptors by the combination of N-desmethylclozapine and clozapine. Use, low enough to result in agonism.   Use of N-desmethylclozapine in the preparation of a medicament for the treatment of psychosis, wherein the amount of any clozapine administered is net agonism at the muscarinic receptor by the combination of N-desmethylclozapine and clozapine Use low enough, which will result in use.   11. Use according to claim 10, wherein the psychosis is caused by administration of one or more drugs.   Use of N-desmethylclozapine in the preparation of a medicament for the treatment of affective disorders wherein the amount of any clozapine administered is net at the muscarinic receptor by the combination of N-desmethylclozapine and clozapine. Use, low enough to result in agonism.   13. Use according to claim 12, wherein the affective disorder is depression.   13. Use according to claim 12, wherein the affective disorder is mania.   Use of N-desmethylclozapine in the preparation of a medicament for the treatment of dementia, wherein the amount of any clozapine administered is net at the muscarinic receptor by the combination of N-desmethylclozapine and clozapine. Use, low enough to result in agonism.   16. Use according to claim 15, wherein the dementia comprises cognitive dysfunction.   16. Use according to claim 15, wherein the dementia comprises a behavioral disorder.   Use of N-desmethylclozapine in the preparation of a medicament for the treatment of neuropathic pain, wherein the amount of any clozapine administered is a combination of N-desmethylclozapine and clozapine at a muscarinic receptor. Use, low enough to result in a net agonism.   Use of N-desmethylclozapine in the preparation of a medicament for the treatment of glaucoma, wherein the amount of any clozapine administered is a net agonism at the muscarinic receptor by the combination of N-desmethylclozapine and clozapine. Use low enough, which will result in use.   Use of N-desmethylclozapine in the preparation of a medicament for the treatment of a condition where it is beneficial to increase the activity level of the M1 muscarinic receptor, wherein the amount of any clozapine administered is N- Use low enough to result in net agonism at the muscarinic receptor by the combination of desmethylclozapine and clozapine. 21. Use according to any of claims 1 to 20, wherein the medicament comprises an additional therapeutic agent selected from the group consisting of:
Monoamine reuptake inhibitor, selective serotonin reuptake inhibitor, norepinephrine reuptake inhibitor, double serotonin / norepinephrine reuptake inhibitor, dopamine agonist, antipsychotic, reverse serotonin agonist, serotonin antagonist, serotonin 2 reverse Agonists, serotonin 2 antagonists, serotonin 1A agonists, antiepileptics and peripherally acting muscarinic antagonists.   The use according to claim 21, wherein the additional therapeutic agent is selected from the group consisting of phenothiazine, phenylbutylpiperazine, debenzazapine, benzisoxidyl, and lithium salt.   The phenothiazine is selected from the group consisting of chlorpromazine (Sorazine®), mesoridazine (Selentil®), prochlorperazine (Compadin®), and thioridazine (Mereryl®). 23. Use according to claim 22.   23. Use according to claim 22, wherein the phenylbutyl piperazine is selected from the group consisting of haloperidol (Haldol (R)) and pimozide (Olap (R)).   23. The debenzazapine is selected from the group consisting of clozapine (clozalyl®), loxapine (Roxitan®), olanzapine (Ziprexa®), and quetiapine (Seroquel®). Use of description.   23. Use according to claim 22, wherein the benzoxydil is selected from the group consisting of resperidone (Resperidal®) and ziprasidone (Geodon®).   23. Use according to claim 22, wherein the lithium salt is lithium carbonate.   The additional therapeutic agents are aripiprazole (Abilify), clozapine, clozaril, compazine, etraphone, geodon, haldol, inapsin, roxitan, meryl, movan, navan, olanzapine (diplexa), olap, permityl, prolixin, fenagan, quetiapine (celloqueel) The use according to claim 21, selected from the group consisting of:), regran, rispadal, serentil, seroquel, stellazine, talatan, sorazine, triavir, trilafone, and diplexa, or pharmaceutically acceptable salts thereof.   21. Use according to any of claims 1 to 20, wherein administration of the medicament comprises administering at least a portion of N-desmethylclozapine by directly introducing N-desmethylclozapine to a subject.   30. The use according to claim 29, wherein introducing N-desmethylclozapine directly into the subject is administering N-desmethylclozapine orally.   30. The use of claim 29, wherein introducing N-desmethylclozapine directly into the subject is administering N-desmethylclozapine intravenously.   21. Use according to any of claims 1 to 20, wherein the medicament is substantially free of clozapine.