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A technology of cyclic amines and derivatives, which is applied in the field of NMDA receptor antagonists, and can solve the problems of unrecorded medical use of intermediates
Inactive Publication Date: 2007-08-22
ASTELLAS PHARMA INC
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However, there is no record at all about the medical use of this intermediate
Method used
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preparation example Construction
[0167] 1) Preparation of rat meninges specimens
[0168] After taking out the whole brains of 30 SD rats (available from Japan SLC Co., Ltd.) at 10 weeks after birth, the cerebellum was removed. A 0.32 M sucrose solution was added to the part containing the brain, and it was chopped with a blender, and then pulverized with a Teflon (registered trademark) homogenizer. Centrifuge at 2800 rpm at 4°C for 15 minutes, then centrifuge the supernatant at 15000 g at 4°C for 20 minutes. The resulting precipitate was suspended in 50 mM Tris-HCl (pH 7.5) containing 0.08% Triton X-100, allowed to stand on ice for 30 minutes, and then centrifuged at 15,000 g at 4° C. for 20 minutes. Add 50 mM Tris-HCl (pH 7.5) to the precipitate to suspend it, and then centrifuge at 15000 g at 4° C. for 20 minutes. After adding 50 mM Tris-HCl (pH 7.5) to the precipitate, centrifugation was performed in the same manner. 20 ml of 50 mM Tris-HCl (pH 7.5) was added to the precipitate to suspend it, and it wa...
Embodiment
[0187] Hereinafter, the compounds of the present invention will be described based on examples. In addition, novel compounds are also included in the raw material compounds of the compounds of the present invention, so these production examples are described below as reference examples.
reference example 1
[0189] 3-(3-Bromo-4-fluorophenyl)propanoic acid
[0190] Piperidine (1 ml) was added to a solution of 3-bromo-4-fluorobenzaldehyde (20 g) and malonic acid (51 g) in pyridine (250 ml), and the mixture was heated to reflux for 3 hours. After the reaction, the solvent was concentrated under reduced pressure, water was added, and 1N hydrochloric acid was added with stirring for neutralization. (2E)-3-(3-bromo-4-fluorophenyl)acrylic acid obtained by filtering the precipitate was dissolved in THF (200ml), and stirred at room temperature for 12 using 5% Rh-C (3g) under hydrogen atmosphere. Hour. After removing insoluble matter by filtration, the solvent was distilled off under reduced pressure to obtain the compound of Reference Example 1 (15 g).
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Abstract
Provided are compounds which are an NMDA antagonist having a broad safety margin and are useful as a treating agent or a preventing agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, pain, etc. Concretely provided are an amine derivative or its salt characterized in that the amine-containing structure A therein bonds to a 2- or 3-cyclic condensed ring (e.g., indane, tetralone, 4,5,6,7-tetrahydrobenzothiophene, 4,5,6,7-tetrahydrobenzofuran, 7,8-dihydro-6H-indeno[4,5-b]furan, 2,3-dihydro-1H-cyclopenta[1]naphthalene) via X 1 (bond or lower alkylene); and an NMDA antagonist containing it as an active ingredient thereof.A compound useful as an NMDA antagonist having a wide safety region which is a therapeutic agent for Alzheimer's disease, vascular dementia (vascular agnosia), Parkinson's disease, ischemic apoplexy, and pains or a preventive agent for these. The compound is an amine derivative or salt thereof characterized by comprising an amine-containing structure (A) and a di- or tricyclic fused ring (indane, tetralone, 4,5,6,7-tetrahydrobenzothiophene, 4,5,6,7-tetrahydrobenzofuran, 7,8-dihydro-6H-indeno[4,5-b]furan, 2,3-dihydro-1H-cyclopenta[a]naphthalene, etc.) bonded to the structure (A) through X<1> (a bond, lower alkylene, etc.). The NMDA antagonist contains the derivative or salt as an active ingredient.
Description
technical field [0001] The present invention relates to cyclic amine derivatives or salts thereof useful as medicines, particularly NMDA receptor antagonists, and NMDA receptor antagonists containing them as active ingredients. The cyclic amine derivatives of the present invention or their salts, and NMDA receptor antagonists using them as active ingredients are applicable to Alzheimer's disease, cerebrovascular dementia (cerebrovascular cognitive disease), Parkinson's Treatment and prevention of disease, ischemic stroke, pain and other diseases. Background technique [0002] Glutamate acts as a neurotransmitter in the central nervous system of mammals, and regulates the activity of nerve cells or the release of neurotransmitters through glutamate receptors present in synapses. At present, it is known from many pharmacological and physiological studies that glutamate receptors can be divided into two types: "ion channel built-in type" and "metabolism regulation type" (Hollm...
Claims
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