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公开(公告)号：JPS60197663A
公开(公告)日：1985-10-07
申请号：JP5389184
申请日：1984-03-21
发明人： YANAGISAWA ISAO , OOTA MITSUAKI , TAKAGI TOKUICHI
IPC分类号： C07D295/08 , A61K31/445 , A61P1/04
摘要： NEW MATERIAL:The sulfamoylamidine derivative of formula I (R is H or lower alkyl; n is 2, 3 or 4) or its acid addition salt. EXAMPLE:4-[ m-( piperidinomethyl )phenoxy ]-N -sulfamoylbutylamidine dihydrochloride. USE:A gastric juice secretion suppressing agent based on histamine H2 receptor antagonistic activity, and free from the side effect caused by anticholine activity. PREPARATION:The compound of formula I can be prepared by reacting the imidate derivative of formula II (R' is lower alkyl) with the sulfamide derivative of formula III. When a compound of formula III wherein R is H is used as the starting material, the dimer of formula IV is also produced as a by-product, which is, however, separable easily from the compound of formula I taking advantage of the difference in the physical and chemical properties between the compound of formula I .
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公开(公告)号：JPS62209062A
公开(公告)日：1987-09-14
申请号：JP5168386
申请日：1986-03-10
IPC分类号： C07D237/00 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/47 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/519 , A61P1/04 , C07D213/00 , C07D213/68 , C07D215/00 , C07D215/36 , C07D215/40 , C07D241/00 , C07D401/12 , C07D475/02 , C07D491/056
摘要： NEW MATERIAL:A compound expressed by formula I [A, B, D, E and F are C or N; R and R are H, lower alkyl, lower alkoxy, nitro or lower alkyl substituted by a halogen; amino which may be substituted by OH, lower alkanoyl or toluenesulfonyl; R -R are H, lower alkyl, lower alkoxy or adjacent two groups together form a group expressed by formula IV (R is H or lower alkyl), n is 0 or 1] or salt thereof. EXAMPLE:2-{[(3,5-Dimethyl-4-methoxy-2-pyridyl)methyl]thio}quinoline. USE:A medicine, preventing agent and remedy for gastropathy, e.g. gastric acid secretion inhibitor, preventive agent and remedy for gastric ulcer, etc. PREPARATION:A condensed ring thiol expressed by formula II is reacted with a 2-halogenomethylpyridine expressed by formula III (X is halogen) in the presence of a base to give the compound expressed by formula I (n is 0), which is then oxidized with an oxidizing agent to afford the compound expressed by formula I (n is 1).
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3.发明专利
公开(公告)号：JPS62207270A
公开(公告)日：1987-09-11
申请号：JP4945286
申请日：1986-03-06
IPC分类号： C07D401/12 , A61K31/435 , A61K31/44 , A61K31/4427 , A61P1/04 , C07D213/00 , C07D233/00 , C07D249/00 , C07D257/00 , C07D263/00 , C07D413/12 , C07D491/056
摘要： NEW MATERIAL:An azole compound substituted with 2-pyridylmethylthio(or sulfinyl) group and expressed by formula I [ring A is azole ring having 1-3C atoms, 1-4N atoms and and 0-1O atom; R is phenyl or lower alkyl; m is 0, 1 or 2; n is 0 or 1; 2-3 of R -R are lower alkyl, lower alkoxy or adjacent two groups together form group of formula IV (R is H or lower alkyl) and the remaining 0-1 is H] or its salt. EXAMPLE:2-[[(3,5-Dimethyl-4-methoxy-2-pyridyl)methyl]thio]4,5-diphenyl oxazole. USE:An gastric acid secretion suppressing agent and antiulcer agent useful as a preventive and remedy for gastric diseases. PREPARATION:Reaction of the compound of formula II with the compound of formula III (X is halogen) gives the compound of formula Ia, which is treated with an oxidizing agent to obtain the compound of formula Ib.
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4.发明专利
公开(公告)号：JPS62207271A
公开(公告)日：1987-09-11
申请号：JP4945386
申请日：1986-03-06
IPC分类号： C07D401/12 , A61K31/44 , A61K31/4427 , A61K31/52 , A61K31/522 , A61P1/04 , C07D209/00 , C07D213/00 , C07D277/00 , C07D417/12 , C07D471/04 , C07D473/22 , C07D473/24 , C07D473/38 , C07D487/04 , C07D491/056
摘要： NEW MATERIAL:A compound of formula I [2-4 of E and X-Z are C and the other 0-2 are H; 1-3 of A, B and D are C and the other 0-2 are N or S (provided that when A=D=N, then E and X-Z are not C at the same time); R and R are H, OH, halogen, lower alkyl, lower alkoxy, NH2, etc.; R -R are H, lower alkoxy, lower alkyl or adjacent two groups together form group of formula IV (R is H or lower alkyl)] or its pharmacologically permissible salt. EXAMPLE:2-[[( 3,5-Dimethyl-4-methoxy-2-pyridyl )methyl-thio-1H-imidazo[4,5-b] pyridine. USE:An gastric acid secretion suppressing agent and antiulcer agent useful as a preventive and remedy for gastric diseases. PREPARATION:Reaction of the compound of formula II with the compound of formula III (X is halogen) gives the compound of formula Ia, which is treated with an oxidizing agent to obtain the compound of formula Ib.
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公开(公告)号：JPS60228465A
公开(公告)日：1985-11-13
申请号：JP8590184
申请日：1984-04-26
发明人： YANAGISAWA ISAO , OOTA MITSUAKI , TAKAGI TOKUICHI
IPC分类号： C07D239/47 , A61K31/505 , A61P1/04
摘要： NEW MATERIAL:A 4(1H)-pyrimidone derivative shown by the formula I (R is 1-10C alkyl; R is lower alkyl; n is 2-4) or its acid addition salt. EXAMPLE:5-Heptyl-6-methyl-2-{ 3-[ m-(piperidinomethyl)phenoxy ]propylamine }- 4(1H)-pyrimidone. USE:An inhibitor against secretion of acid in the stomach. Having both histamine H2 acceptorantagonism and protecting action on stomach mucosa. PREPARATION:For example, a piperidinomethylphenoxyalkylamine shown by the formula II is reacted with a 2-nitroamino or 2-lower alkylthio-4(1H)-pyrimidone derivative shown by the formula III, to give a compound shown by the formula I.
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公开(公告)号：JPH0625153B2
公开(公告)日：1994-04-06
申请号：JP2420690
申请日：1990-02-02
发明人： OOTA MITSUAKI , KOIDE TOKUO , SUZUKI TAKESHI , MATSUHISA AKIRA , OOMORI JUNYA , MYATA KEIJI , YANAGISAWA ISAO
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/475 , A61K31/535 , A61K31/5355 , A61K31/54 , A61K31/541 , A61P1/00 , A61P1/08 , A61P23/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/20 , A61P43/00 , C07D235/20 , C07D235/26 , C07D235/30 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , C07D471/04
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公开(公告)号：JPS60202883A
公开(公告)日：1985-10-14
申请号：JP5755884
申请日：1984-03-26
发明人： YANAGISAWA ISAO , OOTA MITSUAKI , TAKAGI TOKUICHI
IPC分类号： C07D243/08 , A61K31/505 , A61P1/04 , A61P43/00 , C07D239/00 , C07D241/00 , C07D241/04 , C07D243/00 , C07D277/00 , C07D295/14 , C07D317/00 , C07D317/58 , C07D417/12 , C07D417/14
摘要： NEW MATERIAL:A compound of formula I [R , R are H, 1-6C alkyl, l is 1-6; m is 2, 3; R is formula II and III (n is 0-4; X is single bond, O, S; R , R are H, halogen, 1-5C alkyl; R is H, halogen)] or its salt. EXAMPLE:2-[ 2-[[ 2-[( Diaminomethylene )amino]-4-thiazolyl]methyl ]thio]ethyl]- 5-[3-[4-(p-fluorophenyl)-1-piperazino]propyl]-6-methyl-4(1H)-pyrimidone. USE:Remedy for gastropathies. PREPARATION:The reaction of a compound of formula IV or its salt such as 3-[[2-[(diaminomethylene)amino]-4-thiazolyl]methyl]thio]propion amidine hydrochloride with a compound of formula V such as ethylalpha-[3-[4-(p-fluorophenyl)-1- piperazino]propyl]acetoacetate gives the compound of formula I .
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公开(公告)号：JPS60197673A
公开(公告)日：1985-10-07
申请号：JP5389284
申请日：1984-03-21
发明人： YANAGISAWA ISAO , OOTA MITSUAKI , TAKAGI TOKUICHI
IPC分类号： C07D233/64 , A61K31/505 , A61P1/04 , A61P43/00 , C07D213/00 , C07D233/00 , C07D239/00 , C07D401/14 , C07D403/12
摘要： NEW MATERIAL:The pyrimidone derivative of formula I [R and R are lower alkyl; R is 1-10C alkyl, aralkyl, or di(lower alkyl)amino(lower alkyl); m and n are 1-3] and its acid addition salt. EXAMPLE:6-Ethyl-2-{2-[( 5-methyl-4-imidazolyl )methyl]thio]ethyl}-5-pentyl-4(1H)- pyrimidone. USE:Useful as a remedy for gastric diseases. It has histamine H1 and H2 receptor antagonistic activity and cytoprotective activity, and is used as an agent for suppressing the secretion of gastric juice. It has excellent durability, and administered orally or parenterally. PREPARATION:The compound of formula I can be prepared e.g. by reacting the amidine derivative of formula II or its acid addition salt with the acylacetic acid ester derivative of formula III (R is lower alkyl) in an inert organic solvent such as methanol at room temperature or under heating.
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公开(公告)号：JPS6013768A
公开(公告)日：1985-01-24
申请号：JP11954583
申请日：1983-07-01
发明人： YANAGISAWA ISAO , OOTA MITSUAKI , TAKAGI TOKUICHI
IPC分类号： C07D239/36 , A61K31/505 , A61P1/04 , A61P43/00
摘要： NEW MATERIAL:The 4(1H)-pyrimidone compound of formula I (R is alkyl which may be interrupted with O or S or substituted with cyano; R is alkyl) or its salt. EXAMPLE:5-Hexyl-6-methyl-2-[ 3-( m-piperidinomethylphenoxy )propyl ]-4(1H)-pyrimidone. USE:Gastric acid secretion suppressing agent and remedy for gastric diseases. It has antagonistic effect to histamine H1 and H2 and has gastric membrane protecting action. PREPARATION:The compound of formula I can be produced e.g. by the condensation cyclization reaction of the amidine derivative of formula II or its acid addition salt with the acylacetic acid ester derivative of formula III (R is lower alkyl) in an organic solvent at room temperature or under heating.
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公开(公告)号：JPS604182A
公开(公告)日：1985-01-10
申请号：JP11337183
申请日：1983-06-22
发明人： YANAGISAWA ISAO , OOTA MITSUAKI , TAKAGI TOKUICHI
IPC分类号： C07D417/12 , A61K31/505 , A61P1/04 , A61P43/00 , C07D277/20 , C07D277/48
摘要： NEW MATERIAL:The compound of formula I (R is H or lower alkyl; R is H, alkyl which may be interrupted with O or S or substituted with cyano, or alkenyl; R is alkyl; m and n are 1-3) and its salt. EXAMPLE:2-[2-[[[2-[(diaminomethylene)amino]-4-thiazolyl]methyl]thio]- ethyl]-6- ethyl-5-pentyl-4(1H)-pyrimidone. USE:A gastric juice secretion suppressing agent and a remedy for gastric diseases. It has antagonistic activity to histamine H1 and H2 receptors. Also effective to protect the gastric mucosa. PREPARATION:The compound of formula I can be prepared by condensing and cyclizing the amidine derivative of formula II with the acylacetic acid lower alkyl ester of formula III in a solvent such as methanol, dimethylformamide, etc. at room temperature or under heating.
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