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Aminoindan derivative or salt thereof

An alkyl and aryl technology, applied in the field of NMDA receptor antagonists, can solve the problems of narrow therapeutic safety range and use restrictions

Inactive Publication Date: 2009-07-22
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these drugs have a narrow range of therapeutic safety and limited clinical use (Eide PK et al., Pain, 58(1994) 347-354)

Method used

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  • Aminoindan derivative or salt thereof
  • Aminoindan derivative or salt thereof
  • Aminoindan derivative or salt thereof

Examples

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Embodiment

[0118] The compounds of the present invention are described below based on Examples. In addition, since novel compounds are also included in the raw material compounds of the compounds of the present invention, their production examples are described below as reference examples.

reference example 1

[0120] Under ice cooling, 55% oily sodium hydride (1.33 g) was added to a solution of 3-hydroxymethylindan-1-one (1.23 g) and iodomethane in THF (20 ml), and stirred at the same temperature for 1 hour . A saturated aqueous solution of ammonium chloride was added to the reaction liquid, extracted with ethyl acetate, washed with saturated brine, dried over anhydrous magnesium sulfate, and the solvent was removed under reduced pressure. The residue was purified by silica gel column chromatography (eluent: n-hexane: ethyl acetate = 10:1) to obtain the compound of Reference Example 1 as an oily substance.

reference example 2

[0122] At -20°C, a THF (2ml) solution of 3-oxoindane-1-carboxylic acid methyl ester (1.0g) was added to a THF (7ml) solution of t-BuOK (3.0g), and at the same temperature Stir for 30 minutes. Further, methyl iodide (4.5 g) was added thereto, and stirred while rising to room temperature for 30 minutes. The reaction solution was cooled with ice, and 1N hydrochloric acid and ethyl acetate were added for liquid separation, the organic layer was washed with saturated brine, then dried with anhydrous magnesium sulfate, and the solvent was removed under reduced pressure to obtain the compound of Reference Example 2 (1.2 g).

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Abstract

Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain. A novel compound or a salt thereof, which is characterized in that it has an amino group and R1 (lower alkyl, cycloalkyl, -lower alkylene-aryl, aryl which may be substituted, and the like) on carbon atoms of indane, cyclopenta[b]thiophene, cyclopenta[b]furan, cyclopenta[b]pyridine, or cyclopenta[c]pyridine ring, or 2, 3-dihydrdo-1-benzofuran, 2, 3-dihydrdo-1-benzothiophene, indoline ring, or the like, and has R2 and R3 (the same or different, each lower alkyl or aryl) on carbon atoms beside them, and an NMDA receptor antagonist comprising the same as an active component.

Description

technical field [0001] The present invention relates to aminoindan derivatives or salts thereof useful as medicines, especially NMDA receptor antagonists, and NMDA receptor antagonists containing the aminoindan derivatives or salts thereof as active ingredients. The aminoindane derivative or its salt of the present invention, and the NMDA receptor antagonist with said aminoindane derivative or its salt as active ingredients are effective against Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, Ischemic stroke, pain, etc. have therapeutic or preventive effects. Background technique [0002] Glutamate functions as a neurotransmitter in the mammalian central nervous system, and it regulates the activity of nerve cells or the release of neurotransmitters through glutamate receptors present in synapses. At present, many pharmacological and physiological studies have shown that glutamate receptors can be divided into ion channel type and metabolic regulation ty...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C211/42A61K31/13A61K31/381A61K31/404A61K31/435A61K31/4453A61P25/00A61P25/04A61P25/16A61P25/28A61P43/00C07C215/42C07C215/44C07C217/52C07C255/58C07D209/40C07D221/16C07D295/12C07D307/82C07D333/78
CPCC07C255/58C07D333/78C07D307/82C07C215/42C07C235/40C07D295/12C07D209/40C07C2102/08C07C215/44C07C211/42C07D221/16C07C217/52C07C2602/08A61P25/00A61P25/04A61P25/16A61P25/28A61P29/00A61P43/00A61P9/10C07D493/00C07D495/00A61K31/13A61K31/381A61K31/404A61K31/435A61K31/4453C07D211/16
Inventor 林边敏山崎真五渡边和志白石宜之铃木大辅星井博昭大森淳弥金山隆俊
Owner ASTELLAS PHARMA INC
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