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Compounds and uses thereof

A technology for compounds and medicinal salts, applied in the field of compounds and their uses, can solve problems such as poor absorption, chemical instability, and inability to absorb drugs

Inactive Publication Date: 2009-12-23
ASTRAZENECA AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is therefore evident that these drugs are not absorbed in the stomach and do not absorb well in the intestine
Additionally, these amines are often good nucleophiles and may also have chemical instability issues in cases where the molecule has a labile group

Method used

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  • Compounds and uses thereof
  • Compounds and uses thereof
  • Compounds and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0182] Example 1: N-((4-(Dibenzo[b,f][1,4]thiazepine -11-yl)-piperazin-1-yl)methyl)-acetamide

[0183]

[0184] 11-(piperazin-1-yl)dibenzo[b,f][1,4]thiazepine ("PDBTZ", 1 mmol), a mixture of 37% aqueous formaldehyde (1 mmol) and acetamide (1 mmol) in ethanol (5 ml) was refluxed for 4 hours. The reaction mixture was evaporated, the residue resuspended in water and the resulting aqueous material extracted with chloroform. The organic portion was washed (water, brine), dried (sodium sulfate) and evaporated to dryness. The crude product was purified by flash chromatography to afford the title compound.

Embodiment 2

[0185] Example 2: N-[1-(4-(dibenzo[b,f][1,4]thiazepine -11-yl)-piperazin-1-yl)-ethyl]-2,2,2-trifluoro-acetamide

[0186]

[0187] A mixture of PDBTZ (1 mmol), acetaldehyde (1 mmol) and 2,2,2-trifluoro-acetamide (1 mmol) in ethanol (5 ml) was refluxed for 4 hours. The reaction mixture was evaporated, the residue resuspended in water and the resulting aqueous material extracted with chloroform. The organic portion was washed (water, brine), dried (sodium sulfate) and evaporated to dryness. The crude product was purified by flash chromatography to afford the title compound.

Embodiment 3

[0188] Embodiment 3: mouse animal assay

[0189] Dopamine antagonism of the compounds and compositions of the invention can be evaluated in rodent models. The methods and procedures used can be found in J. Med. Chem., 2001, 44, 372-389, which is hereby incorporated by reference in its entirety. Brain Serotonin 5-HT 2 Results of receptor binding affinity and for dopamine D 1 and D 2 Results of receptor binding affinity. It is hypothesized that a combination of serotonin receptor antagonism and dopamine receptor antagonism, where 5-HT 2 Receptor affinity relative to D 2 Receptor affinity was high, indicating that the compound is a potent atypical antipsychotic. J. Goldstein, "Quetiapine Fumarate (Seroquel): a new atypical antipsychotic," 35(2) Drugs of Today 1993-210 (1999), which is hereby incorporated by reference in its entirety.

[0190] Additionally, compounds and compositions of the invention can be tested for their activity according to the standard apomorphine cli...

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PUM

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Abstract

This invention relates to novel compounds having the structural Formula (I) below and their pharmaceutically acceptable salts or tautomers, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of at least one symptom or condition associated with schizophrenia and other psychotic disorders, dementia and other cognitive disorders, anxiety disorders, mood disorders, sleep disorders, disorders usually first diagnosed in infancy, childhood, or adolescence and neurodegenerative disorders.

Description

technical field [0001] The present invention relates to 11-(piperazin-1-yl)dibenzo[b,f][1,4]thiazepines Novel derivatives of , pharmaceutical compositions containing said derivatives, methods of preparing said derivatives and methods of treating at least one symptom or condition associated with schizophrenia and other Psychotic disorders (such as psychotic disorder, psychosis), dementia and other cognitive disorders, anxiety disorders (such as generalized anxiety disorder) anxiety disorder), mood disorders (such as depressive disorder, major depressive disorder), bipolar disorder (including bipolar I and II and II), bipolar mania, bipolar depression), sleep disorder, disorder usually first diagnosed in infancy, childhood, or adolescence (disorder usually first diagnosed in infancy, childhood, oradolescence) (e.g. attention deficit disorder (attention-deficit disorder) and disruptive behavior disorder (disruptive behavior disorder)) and neurodegenerative disease (neurodegene...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/535
CPCC07D281/16A61P9/00A61P13/00A61P25/00A61P25/04A61P25/06A61P25/08A61P25/16A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P43/00
Inventor 彼得·伯恩斯坦詹姆斯·B·坎贝尔
Owner ASTRAZENECA AB
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