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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 the problems of non-absorption of drugs, chemical instability, poor absorption, etc.

Inactive Publication Date: 2009-12-30
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

[0188] Example 1: 1-(4-(Dibenzo[b,f][1,4]thiazepine -11-yl)-piperazin-1-yl)-2-methyl-propan-1-one

[0189]

[0190] 11-(piperazin-1-yl)dibenzo[b,f][1,4]thiazepine in ice bath ("PDBTZ", 1 mmol) and triethylamine (1.1 mmol) in dichloromethane (5 mL) were treated with 2-methylpropionyl chloride (1.1 mmol). The mixture was warmed to ambient temperature and stirred for 1 hour. Water was added, and the mixture was extracted with dichloromethane. The organic portion was washed (brine), dried (sodium sulfate) and evaporated. The crude material was purified by flash chromatography to afford the title compound.

Embodiment 2

[0191] Example 2: 1-(4-(Dibenzo[b,f][1,4]thiazepine -11-yl)-piperazin-1-yl)-propan-1-one

[0192]

[0193] A suspension of propionic acid (1 mmol) and 1-hydroxybenzotriazole (1 mmol) in dichloromethane (4 mL) was treated with 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (1.1 mmol) and triethylamine (1.2 mmol). A solution of PDBTZ (1 mmol) in dichloromethane (4 mL) was added and the mixture was stirred at ambient temperature for 20 hours. The reaction mixture was washed (water, brine), dried (sodium sulfate) and evaporated. The crude material was purified by flash chromatography to afford the title compound.

Embodiment 3

[0194] Example 3: 1-(4-(Dibenzo[b,f][1,4]thiazepine -11-yl)-piperazin-1-yl)-ethanone

[0195]

[0196] A solution of PDBTZ (1 mmol) in DMF (2 mL) was treated with acetic anhydride (2 mmol) and heated for 1 h. The reaction mixture was evaporated to dryness, made basic with aqueous potassium carbonate and extracted with dichloromethane. The organic portion was washed (water, brine), dried (sodium sulfate) and evaporated. The crude material was purified by flash chromatography to afford the title compound.

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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, 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): A01N43/00A61K31/553A61K31/554
CPCC07D281/16A61P1/00A61P25/00A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P43/00
Inventor 彼得·伯恩斯坦詹姆斯·B·坎贝尔
Owner ASTRAZENECA AB
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