Abstract: To provide a compound which is useful as an NMDA receptor antagonist. The present inventors have studied a compound having an NMDA receptor antagonistic action, and confirmed that the fused indane compound of the present invention has an excellent NMDA receptor antagonistic action, thereby completed the present invention. The fused indane compound of the present invention has an excellent NMDA receptor antagonistic action and can be used as a prophylactic and/or therapeutic agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, intractable depression, attention deficit hyperactivity disorder, migraines, or the like.

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 -dihydro-1-benzofuran, 2,3-dihydro-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.

Abstract: [Problems] To provide a compound which is useful as an NMDA receptor antagonist. [Means for Solution] The present inventors have studied a compound having an NMDA receptor antagonistic action, and confirmed that the fused indane compound of the present invention has an excellent NMDA receptor antagonistic action, thereby completed the present invention. The fused indane compound of the present invention has an excellent NMDA receptor antagonistic action and can be used as a prophylactic and/or therapeutic agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, intractable depression, attention deficit hyperactivity disorder, migraines, or the like.

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.

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 X1 (bond or lower alkylene); and an NMDA antagonist containing it as an active ingredient thereof.

Abstract: This invention relates to the provision of novel aminomethyl-substituted thiazolobenzimidazole derivatives represented by the following general formula (I) or a salt thereof. The aforementioned derivative or a salt thereof has a metabotropic glutamate receptor action and excellent oral activity and is therefore useful as a medicament. (In the formula, R1: an oxygen-containing saturated hetero ring or the like, Alk1: a lower alkylene, m: 0 or 1, Alk2: a lower alkylene which may be substituted with oxo group, n: 0 or 1, X: a bond, O, S or NR5, R3: H or the like, and R2, R4, R5, R6 and R7: the same or different from one another and each represents H or the like. Provided that R3 does not represent a lower alkyl or a halogeno-lower alkyl when X is a bond and n is 1. Also, R4 represents a group other than Me when m is 1, R1 is OH or OMe and Alk1 is a C1-3 alkylene, and further 1) when X is a bond, n is 1 and R3 is H, or 2) when X is a bond, n is 0 and R3 is cyclohexane.

Abstract: This invention relates to the provision of novel aminomethyl-substituted thiazolobenzimidazole derivatives represented by the following general formula (I) or a salt thereof. The aforementioned derivative or a salt thereof has a metabotropic glutamate receptor action and excellent oral activity and is therefore useful as a medicament. (In the formula, R1: an oxygen-containing saturated hetero ring or the like, Alk1: a lower alkylene, m: 0 or 1, Alk2: a lower alkylene which may be substituted with oxo group, n: 0 or 1, X: a bond, O, S or NR5, R3: H or the like, and R2, R4, R5, R6 and R7: the same or different from one another and each represents H or the like. Provided that R3 does not represent a lower alkyl or a halogeno-lower alkyl when X is a bond and n is 1. Also, R4 represents a group other than Me when m is 1, R1 is OH or OMe and Alk1 is a C1-3 alkylene, and further 1) when X is a bond, n is 1 and R3 is H, or 2) when X is a bond, n is 0 and R3 is cyclohexane.

Abstract: This invention relates to pharmaceuticals for neuropathic pains comprising an mGluR1 receptor antagonist for systemic administration. Drugs efficacious in treating various neuropathic pain can be provided by the invention.

Abstract: This invention relates to pharmaceuticals for neuropathic pains comprising an mGluR1 receptor antagonist for systemic administration. Drugs efficacious in treating various neuropathic pain can be provided by the invention.

Abstract: This invention relates to novel thiazolo[3,2-a]benzoimidazole derivatives represented by the following general formula (I). The compounds provided by the invention act specifically on metabotropic glutamate receptors and are used as medicaments. The invention also provides novel compounds useful as intermediates for the synthesis of the compounds of the invention. (Symbols in the formula represent the following meanings. R1: carbamoyl, carbonyl, oxy, amino, carbonylamino or the like which may be substituted; R2: hydrogen, lower alkyl or the like; and R3, R4 and R5: hydrogen, lower alkyl and the like which may be the same or different from one another.

Abstract: This invention is to provide remedies for ischemic stroke which contain as an active ingredient a compound having mGluR1 antagonism, pharmaceutical compositions which are remedies for ischemic stroke at the acute stage, pharmaceutical compositions which contain as an active ingredient a compound having selective mGluR1 antagonism, and pharmaceutical compositions wherein the compound having selective mGluR1 antagonism is 6-amino-N-cyclohexyl-N,3 -dimethylthiazolo[3,2-a]benzoimidazole-2-carboxamide dihydrochloride.

Abstract: A morpholine derivative represented by formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 and R.sup.3, which may be the same or different, each represent a hydrogen atom or a lower alkyl group; R.sup.2 represents a halogen atom; and the dotted line indicates an optional double bond. These compounds exhibit a selective 5-HT reuptake inhibitory activity and a selective 5-HT.sub.2 receptor antagonistic activity and useful as a therapeutic agent for depression, anxiety, etc. with reduced side effects.

Abstract: A Maillard reaction inhibitor containing, as an active ingredient, an amidinoheterocyclic derivative or its pharmaceutically acceptable salt, which is useful for the prevention and/or cure of various complications of diabetes and maturity-onset disorders. The amidinoheterocyclic derivatives are also useful as Maillard reaction inhibitors for cosmetics, external endermic medicines, foods, drinks, luxury grocery items and functional foods.