摘要:
(1S,5R,6S)- or (1SR,5RS,6SR)-3-fluoro-2-oxobicylo[3.1.0]-hex-3-ene-6-carboxylic acid derivatives represented by general formula (1); a process for producing the same; and a process for efficiently producing a fluorine-containing amino acid compound acting on group 2 metabotropic glutamate receptor which has therapeutic and preventive effects on psychiatric diseases or neurological diseases, characterized by hydrogenating the above compound (1) and then further converting the same into hydantoin or amino cyanide followed by hydrolysis. In formula (1), R represents OR?1 or NR1R2¿ (wherein R?1 and R2¿ are the same or different and each represents hydrogen, C¿1-6? alkyl, C3-6 cycloalkyl, (C3-6 cycloalkyl)(C1-6 alkyl), aryl, aryl(C1-6 alkyl), (C1-6 alkoxy)(C1-6 alkyl), C1-6 hydroxyalkyl, (C1-6 alkylthio)(C1-6 alkyl) or C1-6 mercaptoalkyl).
摘要:
Fluorine-containing amino acid derivatives represented general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, wherein X represents hydrogen or fluorine; and R and R are the same or different and each represents hydrogen or lower C1-10 alkyl. These compounds are useful as drugs, in particular, group 2 metabotropic glutamate receptor agonists for treating and preventing psychiatric disorders such as schizophrenia, anxiety and associated diseases, depression, dipolar disturbance and epilepsy, and neurological diseases such as drug addiction, cognition disorder, Alzheimer's disease, Huntington's chorea, Parkinson's disease, motility disturbance associating muscular stiffness, cerebral ischemia, cerebral insufficiency, spinal cord lesion and head disturbance.
摘要:
A novel compound which is a 1,3-dihydro-2H-indol-2-one derivative represented by the formula (1): (1) (wherein R1 represents halogeno, C1-4 alkyl, etc. and R2 represents hydrogen, halogeno, etc., or R2 is present in the 6-position of the indol-2-one and is bonded to R1 to form C3-6 alkylene; R3 represents halogeno, hydroxy, etc. and R4 represents hydrogen, halogeno, C1-4 alkyl, etc., or R4 is present in the 3-position of the phenyl and is bonded to R3 to form methylenedioxy; R5 represents hydrogen or fluorine; R6 represents ethylamino, dimethylamino, etc.; R7 represents C1-4 alkoxy; and R8 represents C1-4 alkoxy) or a pharmaceutically acceptable salt of the derivative. The compound has antagonistic activity against an aruginine-vasopressin V1b receptor.
摘要:
A 2-fluoro-2-(3-oxocyclopentyl)acetate derivative represented by the formula (1). The compound is useful in the efficient synthesis of a 2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative.
摘要:
Compounds which are useful in the efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acid. The compounds are 2-oxobicyclo[3.1.0]hexane-6-carboxylic acid derivatives represented by formula (1) [wherein R1 represents hydrogen, C¿1-6? alkyl, C3-6 cycloalkyl, C1-6 alkyl substituted by C3-6 cycloalkyl, aryl, C1-6 alkyl substituted by aryl, C1-6 alkyl substituted by C1-6 alkoxy, C1-6 hydroxyalkyl, C1-6 alkyl substituted by C1-6 alkylthio, C1-6 mercaptoalkyl, tetrahydrofuranyl, or tetrahydropyranyl; R?2 and R3¿ are the same or different and each represents C¿1-6? alkyl, C3-6 cycloalkyl, C1-6 alkyl substituted by C3-6 cycloalkyl, aryl, or C1-6 alkyl substituted by aryl, or R?2 and R3¿ in combination represent -(CH¿2?)n- (n is 2 or 3); and Y?1 and Y2¿ are the same or different and each represents sulfur, oxygen, or nitrogen].
摘要:
A tetrahydropyridino or piperidino heterocyclic derivative represented by the formula [I]: A-Het [I]has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.
摘要:
Fluorobicyclo[3.1.0]hexane derivatives represented by general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same wherein R?1 and R2¿ represent each hydrogen, alkyl, cycloalkyl, etc.; and Y?1 and Y2¿ represent each hydrogen, alkylthio, cycloalkylthio, alkoxy, etc., or one of Y?1 and Y2¿ represents hydrogen and the other represents hydroxy, alkoxy, cycloalkoxy, etc., or Y?1 and Y2¿ together represent oxygen or -X(CH¿2?)nX- (wherein X represents oxygen or sulfur; and n is 2 or 3). These compounds are useful as drugs, in particular, group 2 metabotropic glutamate receptor agonists, in treating and preventing psychiatric disorders such as schizophrenia, anxiety, depression and bipolar disturbance, and neurologic diseases such as drug addiction, cognition disorder, Alzheimer's disease, Huntington's disease, Parkinson's disease, movement disorder in association with muscular rigidity, brain ischemia, brain insufficiency, spinal cord lesion and head disorder.
摘要:
4-Tetrahydropyridylpyrimidine derivatives of general formula (I); and medicinally acceptable salts thereof, wherein Ar is phenyl optionally substituted with one to three groups selected from among halogeno, C1-C5 alkyl, C1-C5 alkoxy and trifluoromethyl, thienyl or furanyl; R1 is hydrogen, C¿1?-C5 alkyl or amino optionally substituted with one or two C1-C5 alkyl groups; R?2 is C¿1-C5 alkyl, C4-C7 cycloalkylalkyl, C2-C5 alkenyl or C2-C5 alkynyl; and X?1, X2 and X3¿ are each independently hydrogen, halogeno, C¿1?-C5 alkyl, C1-C5 alkoxy, C1-C5 alkylthio or amino optionally substituted with one or two C1-C5 alkyl groups. These compounds are efficacious against diseases in which CRF is believed to be concerned, for example, melancholia, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, digestive diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immunologic diseases and so on.