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公开(公告)号:JPH07149765A
公开(公告)日:1995-06-13
申请号:JP19311694
申请日:1994-08-17
发明人: BABA YUTAKA , SUZUKI TOMOO , SUZUKI TSUNEMASA , HIROOKA KIYOTAKA , KURONO MASATSUNE , SAWAI KIICHI
IPC分类号: A61K31/00 , A61K31/40 , A61K31/407 , A61P25/00 , A61P25/02 , A61P25/18 , A61P25/28 , C07D487/04
摘要: PURPOSE:To obtain a new compound useful as a cerebral function improver such as an anti-dementia, showing strong muscarine receptor operation activity and a wide safe range, having a specific skeleton structure. CONSTITUTION:This compound has a skeleton structure of formula I [R1 is H, a 1-4C alkyl or an acyl; R2 and R3 are each H, a 1-4C alkyl, phenyl, a halogen, cyano, acyl, nitro, a 1-2C alkoxy or a (substituted) amido; (n) is 1-3; dotted line is a ring which occasionally exists], to be concrete, 1-[N-(1-azabicyclo [3.3.0] octan-5-yl) methyl-N-methylamino]-4-chloronaphthalene. For example, a compound of formula II is converted into a diazo compound, which is halogenated and cyanated and the prepared reaction product is converted into a salt to give the objective compound.
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公开(公告)号:JPH05139963A
公开(公告)日:1993-06-08
申请号:JP30222491
申请日:1991-11-19
发明人: KURONO MASATSUNE , BABA YUTAKA , SUZUKI TOMOO , SUZUKI TSUNEMASA , HIROOKA KIYOTAKA , SAWAI KIICHI
IPC分类号: A61K31/135 , A61P25/00 , A61P25/28 , C07C211/59
摘要: PURPOSE:To obtain an antidemential agent having high safety, applicable over a long period and suitable as an agent for improving cerebral function, e.g. treating agent for senile dementia by using an aminonitronaphthalene derivative as an active component. CONSTITUTION:The objective antidemential agent contains the compound of formula (the position of NH2 is 1 or 2-site; that of NO2 is 1, 2, 3, 4, 5, 6, 7 or 8-site) such as 1-amino-2-naphthalene as an active component. The daily dose of the compound is preferably 0.01-100mg for adult.
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公开(公告)号:JPH06184152A
公开(公告)日:1994-07-05
申请号:JP25354692
申请日:1992-08-31
发明人: KURONO MASATSUNE , BABA YUTAKA , SUZUKI TOMOO , SUZUKI TSUNEMASA , HIROOKA KIYOTAKA , SAWAI KIICHI
IPC分类号: A61K31/135 , A61K31/00 , A61K31/165 , A61K31/40 , A61K31/47 , A61K31/473 , A61P25/28 , C07C211/53 , C07C211/57 , C07C211/59 , C07C211/61 , C07C237/06 , C07C237/10 , C07D215/38 , C07D219/12 , C07D487/04 , A61K31/645
摘要: PURPOSE:To provide a new compound having brain function-improving activity, thus useful for the prevention or curing of Alzheimertype dementia. CONSTITUTION:The objective compound of formula I [A is CH, N or N oxide; R1 is nitro or amino; R2 is H, lower alkyl or acyl; R3 is formula II ((m) is 0 or 1; (n) is 0-3; R4 and R5 are each H or lower alkyl; R6 and R7 are each H, lower alkyl, etc.; dotted line is a ring present as the case may be], e.g. 4-(1-azabicyclo[3,3,0]octan-5-yl)methylamino-3-nitroquinoline. The compound of the formula I can be obtained by reaction between a compound of formula III (X is halogen or alkoxy) and a compound of formula IV in a solvent (e.g. DMF) or in the absence of a solvent at 0-180 deg.C. The compound of the formula I is low toxic and excellent in safety, and can be administered for a long period of time.
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公开(公告)号:JPS6422883A
公开(公告)日:1989-01-25
申请号:JP17717387
申请日:1987-07-17
发明人: KURONO MASATSUNE , SUZUKI TSUNEMASA , SUZUKI TOMOO , HIROOKA KIYOTAKA , MATSUMOTO KOJI , OZAWA HIROSHI , SAWAI KIICHI
IPC分类号: C07F7/10 , A61K31/695 , A61P25/28 , C07F7/08
摘要: NEW MATERIAL:A compound expressed by formula I [R1 represents H or trialkylsilyl; R2 and R3 represent H; R4 represents alkyl; R5 represents formulae II or III (R6 and R7 represent alkyl; n and m are 1-3), R4 and R5 may link with each other to represent N- or Si-containing heterocyclic ring or piperadine ring having formula IV as substituent group, when R1 is H; R2 and R4 as well as R3 and R5 represent heterocyclic ring linked through alkylene chain, when R1 is trialkylsilyl]. EXAMPLE:N-[2-[(Isopropyl)(trimethylsilylmethyl)amino]ethyl]-2-oxo-1-py rrolidine acetamide. USE:A prophylactic and remedial agent for cerebral dysfunction. PREPARATION:A compound expressed by formula V (R represents H or lower alkyl) is reacted with a compound expressed by formula VI and the reaction product, as necessary, is converted into a salt.
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