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Case Western Reserve University Patents
Show moreField of the invention: This invention relates to the treatment of patients suffering from therapy-resistant schizophrenia by administration of the drug melperone (4-fluoro-.gamma.-(4-methyl-piperidino) - butyrophenone). Background of the invention: The treatment of schizophrenia remains one of the major challenges of modern-day medicine. Even incremental advances in the safe and effective use of currently available treatments can have a major impact on the lives of schizophrenic individuals and their families. Reducing rates of relapse and rehospitalization by as little as 10 percent per year can have enormous public health implications. (J. M. Kane, Special Report: Schizophrenia, 1987, National Institute of Mental Health, in: Schizophrenia Bull., 13:133-156, 1987). It is estimated that about 2 million Americans suffer from classical schizophrenia. Approximately 200,000 to 400,000 (10-20 percent) of these schizophrenic patients do not respond to treatment with traditional neuroleptics (antipsychotic drugs) and are classified as therapy-resistant schizophrenics. Data gathered from maintenance medication trials indicate that 20 to 30 percent of patients initially responsive to antipsychotic drugs may relapse during the first year or two of maintenance drug treatment. A proportion of these relapsed patients may contribute to the number of patients refractory to treatment (J. M. Kane, J. Lieberman, Psychopharmacology. the Third Generation of Progress, 1987 Ravin Press, ed., H. Y. Meltzer, pp. 1103-1109). The term "treatment-(or therapy-)-resistant" schizophrenia used in this context describes a particular illness generally understood by a physician skilled in the art. The treatment-resistant schizophrenic patient may be minimally defined as a patient with schizophrenia without marked symptomatic relief from two treatment periods with two neuroleptic agents from different chemical classes. Clinical research has suggested that neuroleptic-resistant patients suffer from an illness which is characterized by pharmacodynamic, psychological, and physiological properties which differ from those of the neuroleptic-responsive patient. Thus, therapeutic agents known to be effective in the treatment of schizophrenia are not useful in the treatment of therapy-resistant schizophrenia. In general, the phenothiazines (e.g., chloropromazine) and the butyrophenones (e.g., haloperiodol) constitute the classical neuroleptics used in the treatment of schizophrenia to which the therapy-resistant patient does not respond. More effective pharmacotherapy for the treatment of therapy-resistant schizophrenia has not been developed in the more than three decades since the introduction of the first effective neuroleptic drugs. Thus far, the only drug approved for clinical use in treating therapy-resistant schizophrenic patients is clozapine, which was approved by the FDA in September 1989 for this particular use.
http://www.google.com/patents?vid=USPAT5221679
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