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Pharmaceutical compositions of a 5-HT2a serotonin receptor modulator useful for the treatment of disorders related thereto

A pharmaceutical composition, composition technology, applied in the direction of drug combination, pharmaceutical formula, medical preparations of non-active ingredients, etc., can solve the problems of weak water solubility, low oral bioavailability, etc.

Inactive Publication Date: 2008-09-24
ARENA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, it is believed that 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl )-urea has very poor water solubility and is expected to provide very low oral bioavailability

Method used

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  • Pharmaceutical compositions of a 5-HT2a serotonin receptor modulator useful for the treatment of disorders related thereto
  • Pharmaceutical compositions of a 5-HT2a serotonin receptor modulator useful for the treatment of disorders related thereto
  • Pharmaceutical compositions of a 5-HT2a serotonin receptor modulator useful for the treatment of disorders related thereto

Examples

Experimental program
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Effect test

example 1

[0338]Example 1: 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl Solubility determination of )-urea in selected excipients

[0339] Add excess 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4- Difluoro-phenyl)-urea and excipients to give a suspension. For some excipients, no suspension was observed and therefore solubility was considered greater than a specific volume added, e.g. Transcutol TM P, PEG 300, PEG 600, Tween TM ) 20 and Softigen 767 (see table below). The contents of the bottle were mixed for 30 seconds using a VWR mini vortexter, followed by sonication (Branson 1510) for 1 minute. The bottle was placed in a constant temperature bath (ie, about 25°C) and allowed to equilibrate for no more than 12 hours. The resulting suspensions were transferred to eppendorf tubes each equipped with a 0.2 μm nylon filter (Costar 8168) and centrifuged at 14,000 rpm for 10 minutes. The supernatant from each Eppendorf tube was co...

example 2

[0350] 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2 , Pharmacokinetics of 4-difluoro-phenyl)-urea

[0351] 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4- Determination of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxyl in healthy male and female volunteers after difluoro-phenyl)-urea and Cremephor RH40 Plasma pharmacokinetics of phenyl-phenyl]-3-(2,4-difluoro-phenyl)-urea.

[0352] A single oral dose of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2 , 4-difluoro-phenyl)-urea

[0353]

example 3

[0355] 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl) in male Sprague-Dawley rats after oral administration with various excipients Pharmacokinetics of -4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea

[0356] After oral administration of 10 mg / kg of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4- Determination of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxyl in male Sprague-Dawley rats following difluoro-phenyl)-urea Plasma pharmacokinetics of phenyl-phenyl]-3-(2,4-difluoro-phenyl)-urea. 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)- Urea in polyethylene glycol 400 (PEG 400), Labrasol, Cremaphor RH40, 80% Tween 80 and 20% water (Tween), Cremaphor RH40: Labrasol (1:1, v / v), 40% hydroxypropyl- β-cyclodextrin (HPCD) and dimethylacetamide (DMAC) prepared as an aqueous suspension. Dosage formulations are administered via oral gavage tube.

[0357] 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-di Mean pharm...

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Abstract

The present invention relates to certain pharmaceutical compositions of a 5-HT2A serotonin receptor modulator and methods for preparing pharmaceutical composition related thereto. The pharmaceutical compositions are useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

Description

technical field [0001] The present invention relates to 5-HT 2A Certain pharmaceutical compositions and preparations of serotonin receptor modulators and 5-HT 2A Methods of pharmaceutical compositions related to serotonin receptor modulators. The pharmaceutical composition is useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of thrombosis, asthma or its symptoms, anxiety or symptoms, behavioral disorders , drug-induced psychosis, excited psychosis, Durett's syndrome, mania, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia, and related disorders, sleep disorders, diabetes-related disorders, progressive multifocal leukoencephalopathy, etc. Background technique [0002] It has recently been found that certain 1,3-disubstituted urea compounds are 5-HT 2A Modulators of serotonin r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K31/415
CPCA61K9/4866A61K9/4858A61K31/415A61P11/06A61P25/00A61P25/14A61P25/18A61P25/20A61P43/00A61P7/02A61P9/00A61P9/10A61P3/10Y02A50/30A61K47/30A61K9/48
Inventor 拉杰什·K·阿加瓦尔兰普尔纳·普拉萨德·古拉帕利迈克尔·马丁迈克尔·摩根丹尼斯·查普曼约瑟夫·贝利耶·斯皮尔单云
Owner ARENA PHARMA
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