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Conjugated psychotropic drugs and uses thereof

A technology for neuroleptics, uses, applied in the field of chemical sensitization, and can solve problems such as harmful side effects, limitations, etc.

Inactive Publication Date: 2009-06-03
RAMOT AT TEL AVIV UNIV LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0017] However, while the teachings in WO 02 / 43652, in particular regarding the antiproliferative and chemosensitizing activities of psychostimulants in the treatment of MDR cancers, are beneficial, the use of these psychostimulants is limited by side effects

Method used

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  • Conjugated psychotropic drugs and uses thereof
  • Conjugated psychotropic drugs and uses thereof
  • Conjugated psychotropic drugs and uses thereof

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Embodiment

[0197] Reference is made to the following examples which, together with the foregoing description, illustrate the invention in a non-limiting manner.

[0198] Chemical Synthesis and Analysis

[0199] Exemplary chemical conjugates of the present invention were synthesized by combining the neuroleptics phenothiazine and fluphenazine with the short-chain fatty acids propionate, butyrate and valerate and with 4-phenylbutyrate and γ-aminobutyrate ( GABA) response. The compound was prepared in high yield and a crystalline solid was isolated and dissolved in 1% aqueous lactic acid.

[0200] Synthesis of chemical conjugates prepared by phenothiazine or fluphenazine and organic acids—general method: neuroleptic phenothiazine or fluphenazine (1 equivalent), acid chloride derivatives of short-chain fatty acids ( 1.1 equiv) and optional Et 3 A mixture of N (2 equivalents) (for freeing the hydrochloride salt of the starting material) in 5-10 ml of dimethylamide (DMF) was stirred at room...

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Abstract

The present invention relates to a conjugated psychotropic drugs and uses thereof. The present invention discloses novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and / or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses. The organic acids are selected to reduce side effects induced by the psychotropic drugs and / or to exert an anti-proliferative activity.

Description

[0001] This application is a divisional application of the application with the filing date of September 29, 2002, the application number of 02823600.9, and the invention title of "conjugated neuroleptic drugs and their uses". technical field [0002] The present invention relates to novel chemical conjugates of antipsychotics and organic acids and uses thereof. More specifically, the present invention relates to the combination of neuroleptics (which may also have antiproliferative and / or chemosensitizing activity) with organic acids selected for reducing side effects caused by neuroleptics and / or for producing antiproliferative activity. Novel chemical conjugates and their use in the treatment of psychiatric and / or proliferative disorders and diseases and in chemosensitization. The novel chemical conjugates of the present invention are characterized by minimizing deleterious side effects compared to prior art neuroleptics. Background technique [0003] Neuroleptics, also ...

Claims

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Application Information

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IPC IPC(8): C07D279/18A61K31/541A61K31/54A61P25/18A61P35/00C07D417/00C07D279/28A61K31/5415A61K47/48A61P25/14
CPCA61K47/48038A61K31/5415A61K47/481A61K47/542A61K47/55A61P25/00A61P25/02A61P25/14A61P25/18A61P35/00A61P35/04A61K47/50A61K31/4965
Inventor A·努德曼A·雷哈里I·吉-阿德A·维兹曼
Owner RAMOT AT TEL AVIV UNIV LTD
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