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Acylguanidine derivative

An alkyl and phenyl technology, applied in the field of substituted guanidine derivatives, can solve the problems of undisclosed dementia, schizophrenia, cognitive impairment, etc.

Inactive Publication Date: 2010-01-13
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in these gazettes, there is no disclosure of uses for dementia, schizophrenia, cognitive impairment, etc.

Method used

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  • Acylguanidine derivative
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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0193] (Preparation of raw material compound)

[0194] The raw material compounds (1) to (4) in the above production methods can be produced, for example, by the following methods, known methods or modified methods thereof.

[0195] (Raw material synthesis 1)

[0196] [chemical 15]

[0197]

[0198] (In the formula, Q and U represent leaving groups respectively, and any one represents -Br, -Cl, -I or -O-SO 2 -CF 3 etc., the other side means -B(OH) 2 or B(O-lower alkyl) 2 Wait. R 10 Represents a protecting group for a carboxyl group such as a lower alkyl group or benzyl group. )

[0199] In the raw material compound (1), R 4 The compound that is H can be directly prepared by the above-mentioned reaction route, or by the -OR of the thus prepared compound (1a) 10 Prepared by converting to a leaving group.

[0200] Among them, the coupling reaction can be passed through "Synthetic Communications", (UK), 1981, Volume 11, p.513-519; "Synlett", (Germany), 2000, Volume 6...

Embodiment

[0220] Hereinafter, a method for producing a compound contained in formula (I), which is an active ingredient of the present invention, will be described as an example. In addition, the production method of the compound used as a raw material is demonstrated as a production example. The production method of compound (I) is not limited to the production methods shown in the specific examples below, and can also be produced by a combination of these production methods, known production methods or their improved methods.

[0221] In the description of the following preparation examples and the tables described later, the following abbreviations are used for the measured values ​​by mass spectrometry.

[0222] ESI+:ESI-MS[M+H] + ;ESI-:ESI-MS[M-H] - ;FAB+: FAB-MS[M+H] + or FAB-MS[M] + ;FAB-:FAB-MS[M-H] - ;APCI+:APCI-MS[M+H] + ;APCI-:APCI-MS[M-H] - ;EI+:EI[M] + .

preparation example 1

[0224] By reacting methyl 3-nitro-4-{[(trifluoromethyl)sulfonyl]oxy}benzoate with phenylboronic acid, potassium phosphate, tetrakis(triphenylphosphine)palladium in DMF with heating , to obtain methyl 2-nitrobiphenyl-4-carboxylate. FAB+: 258.

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PUM

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Abstract

An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia and the like, based on the 5-HT 5A receptor modulating action. It was confirmed that a compound characterized by a structure that a tricyclic hetero ring having a pyrrole ring at the center and guanidine are bonded via a carbonyl group has a potent 5-HT 5A receptor modulating action and an excellent pharmacological action based thereon, and thus, it was found that the compound can be an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder, particularly for memory-related functional disorders such as cognitive impairments including dementia and schizophrenia, thereby completing the present invention.

Description

technical field [0001] The present invention relates to substituted guanidine derivatives having medicinal properties, especially 5-HT 5A It can be used as a pharmaceutical composition for the treatment or prevention of dementia, schizophrenia and the like due to its receptor regulating effect. Background technique [0002] Dementia is a syndrome based on decreased brain function, memory impairment, and judgment impairment caused by acquired brain disorders, and vascular dementia and Alzheimer's dementia are representative causative diseases. In the past, drugs for the treatment of these diseases have been studied, but the clinical needs could not be fully met. For example, it is reported that cholinesterase inhibitors such as Aricept, which are widely used as a therapeutic drug for Alzheimer's dementia, have insufficient effects (Curr.Neurol.Neurosci.rep., 5(6) , 455-457, 2005; Eur. J. Pharmacol., 346, 1-13, 1998). In addition, side effects produced by stimulation of the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/88A61K31/403A61K31/407A61K31/4155A61K31/437A61K31/4439A61K31/454A61K31/496A61K31/506A61K31/5377A61P25/00A61P25/14A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P43/00C07D401/04C07D401/06C07D401/14C07D403/04C07D405/04C07D405/14C07D409/04C07D409/06C07D409/14C07D413/06C07D471/04C07D491/048C07D495/04
CPCC07D471/04C07D403/04C07D401/06C07D405/04C07D409/14C07D409/06C07D413/06C07D401/04C07D401/14C07D495/04C07D409/04C07D405/14C07D491/048C07D403/06C07D209/88A61P25/00A61P25/14A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P43/00A61K31/403
Inventor 木野山功宫本聪星井博昭宫崎壮宏山崎真也子
Owner ASTELLAS PHARMA INC
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