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1. 发明专利

JPH01287023A DIURETIC 失效
公开(公告)号：JPH01287023A
公开(公告)日：1989-11-17
申请号：JP2527389
申请日：1989-02-02
申请人： TANABE SEIYAKU CO
发明人： TAKAMURA NORIO , ODA KUNIYUKI , KOTADO SHINICHI , YAMAGUCHI ISAO , YANO KOJI
IPC分类号： C07D231/12 , A61K31/415
摘要： PURPOSE:To obtain a novel diuretic having excellent diuretic action, electrolyte- secretion promoting action and uric acid secretion promoting action, by using a phenoxyacetic acid derivative or its salt as an active component. CONSTITUTION:The objective agent can be produced by using a compound of formula I (R is H or lower alkyl; R is H or lower alkenyl; R is H, lower alkyl, lower alkoxy-substituted-lower alkyl, etc., X is halogen; Z is O or methyl ene) or its salt as an active component, compounding the component with a conventional drug carrier and converting to a drug preparation by conventional method. It can be administered orally or parenterally at a dose of 0.3-200mg/kg daily. The compound of formula I can be produced by reacting a phenol deriva tive of formula II with an acetic acid compound of formula Y-CH2COOR (Y is halogen) in a solvent in the presence of an acid acceptor (e.g. alkali metal hydroxide) at room temperature or under heating. The compound of formula I is e.g. {2,3-dichloro-4-[1-(1-ethoxymethyl-5-pyrazolyl)vinyl] phenoxy} acetic acid.

2. 发明专利

JPS6058909B2 失效
公开(公告)号：JPS6058909B2
公开(公告)日：1985-12-23
申请号：JP1183880
申请日：1980-02-01
申请人： TANABE SEIYAKU CO
发明人： NAGAO SHIGETO , GAINO MITSUNORI , TAKAMURA NORIO , SATO MASANORI
IPC分类号： A61K31/19 , A61K31/195 , A61K31/215 , A61K31/22 , A61P9/12 , C07C67/00 , C07C313/00 , C07C323/52

3. 发明专利

JPS5466668A NITROSOUREA DERIVATIVE AND ITS PREPARATION 失效
公开(公告)号：JPS5466668A
公开(公告)日：1979-05-29
申请号：JP13181777
申请日：1977-11-02
申请人： TANABE SEIYAKU CO
发明人： TAKAMURA NORIO , KAMIO MASAETSU , ARAI YOSHIHISA , MIZOGUCHI TOMISHIGE
IPC分类号： C07D333/48 , C07D333/36
摘要： NEW MATERIAL:Trans, and cis-3,4-bis[3-(2-chloroethyl)-3-nitrosoureido]sulfolane. of formula I. USE:Safe and effective anti-tumor agent. PROCESS:The compound I is prepared by reacting nitrous acid with a urea derivative IV obtained by the addition reaction of 2-chloroethyl isocyanate with an amino compound III in a solvent. The compound III is obtained by the catalytic reductions of a benzyl amine derivative II with H2 in a solvent in the presence of a hydrogenetion catalyst such as Pd-C, Raney nickel, etc.

4. 发明专利

JPH0733709A PRODUCTION OF OXALIC ACID MONOESTER COMPOUND 失效
公开(公告)号：JPH0733709A
公开(公告)日：1995-02-03
申请号：JP18466193
申请日：1993-07-27
申请人： TANABE SEIYAKU CO
发明人： TAKAMURA NORIO , ODA KUNIYUKI , SOFUGAWA MASAO
IPC分类号： C07C67/10 , C07C69/36 , C07C69/63
摘要： PURPOSE:To selectively produce an oxalic acid monoester from oxalic acid in one step and high yield under mild condition. CONSTITUTION:An oxalic acid monoester of formula II is produced by reacting oxalic acid with a compound of formula I [R is residue obtained by removing hydroxyl group from corresponding alcohol (ROH); X is a reactive residue] in the presence of a base preferably in a proper solvent. The reaction is effective for producing the compound in high efficiency even when the ester residue is originated from an alcohol unstable to acid, alkali, etc., especially an ester residue for getting a prodrug to promote the peroral absorption of beta-lactam antibacterial agent. The compound of formula II is easily converted to an oxalic acid monoester halide compound of formula III (Y is halogen) by reacting with a halogenating agent and is usable for the production of a penem or cephem compound of formula IV (R is OH-substituted alkyl; R is organic group; Z is CH2CH2, SCH2, OCH2, CH2, etc.; R is alkyl).

5. 发明专利

JPH0616651A 1,5-BENZOTHIAZEPINE DERIVATIVE AND ITS PRODUCTION 失效
公开(公告)号：JPH0616651A
公开(公告)日：1994-01-25
申请号：JP8993793
申请日：1993-04-16
申请人： TANABE SEIYAKU CO
发明人： MORIMOTO MASAMICHI , NAGASAWA MASAAKI , TAKAMURA NORIO , INOUE HIROZUMI
IPC分类号： A61K31/55 , A61K31/554 , A61P7/02 , A61P9/08 , A61P9/10 , A61P9/12 , C07D281/10
摘要： PURPOSE:To obtain a new compound useful as a synthetic intermediate for a hypotensive and a cerebral vasolidator. CONSTITUTION:The compound of formula I (R , R and R are H or lower alkyl; either of X and X is H and the other is Cl), e.g. (-)-cis-2-(4- methoxyphenyl)-3-hydroxy-5-[2-(N-methylamino)ethyl]-8-chloro-2,3-dihyd ro-1,5- benzothiazepin-4(5H)-one hydrochloride. This compound is obtained by intramolecularly cyclizing a compound of formula II (R is lower alkyl) in the presence of a base (e.g. lithium diisopropylamide) in a solvent (e.g. THF) at -70 to -25 deg.C The compound of formula I can be reduced and converted into a hydroxy compound.

6. 发明专利

JPH03157331A DIURETIC 失效
公开(公告)号：JPH03157331A
公开(公告)日：1991-07-05
申请号：JP20039490
申请日：1990-07-26
申请人： TANABE SEIYAKU CO
发明人： TAKAMURA NORIO , INOUE ISAO , INAGE MASARU , YAMAGUCHI ISAO , YANO KOJI
IPC分类号： C07D405/06 , A61K31/415 , A61K31/44 , A61K31/443 , A61P7/10 , A61P19/06 , C07D405/14
摘要： NEW MATERIAL:The compound of formula I (R is lower alkyl, lower alkoxy- substituted lower alkyl, etc.; R is H or halogen; R is H or lower alkyl) and its salt. EXAMPLE:4,5-Dichloro-6-(1-methyl-5-pyrazolylcarbonyl)-1,3-benzodioxole-2- carboxylic acid. USE:A diuretic useful for the remedy and prevention of congestive heart, various edemata, etc. PREPARATION:The objective compound of formula I can be produced either by reacting a 1,2-benzenediol compound of formula II with an acetic acid compound of formula III (Y is reactive residue) or by oxidizing a benzodioxole compound of formula IV. The preferable daily dose of the compound of formula I is usually 0.1-200mg/kg, especially 0.3-100mg/kg.

7. 发明专利

JPH01211582A BENZODIOXOLE DERIVATIVE 失效
公开(公告)号：JPH01211582A
公开(公告)日：1989-08-24
申请号：JP3369388
申请日：1988-02-16
申请人： TANABE SEIYAKU CO
发明人： TAKAMURA NORIO , INOUE ISAO , INAGE MASARU , YAMAGUCHI ISAO , YANO KOJI
IPC分类号： C07D231/12 , A61K31/415 , A61K31/44 , A61K31/443 , A61P7/10 , C07D231/16 , C07D405/06 , C07D405/14
摘要： NEW MATERIAL:A compound shown by formula I (R is lower alkyl, lower alkoxy, substituted lower alkyl, phenyl or pyridyl; R is H or halogen; R is H or lower alkyl) or a salt thereof. EXAMPLE:4,5-Dichloro-6-(1-methyl-5-pyrazolylcarbonyl) -1,3-benzox-ole-2-carbo xylic acid. USE:A diuretic, electrolyte eliminate and uric acid eliminate. PREPARATION:A 1,2-benzenediol compound shown by formula II is reacted with an acetic acid compound shown by formula (Y)2CHCOOR (Y is reactive residue).

8. 发明专利

JPH05306286A 失效
公开(公告)号：JPH05306286A
公开(公告)日：1993-11-19
申请号：JP10741192
申请日：1992-04-27
申请人： TANABE SEIYAKU CO
发明人： TAKAMURA NORIO , YASUNAKA MASAYUKI , YASUDA KOUSUKE , MATSUOKA YUZO , IWATA HIROSHI
IPC分类号： A61K31/40 , A61K31/675 , A61P25/00 , A61P25/28 , A61P27/02 , A61P43/00 , C07D495/04 , C07F9/6561
摘要： PURPOSE:To provide the subject new compound having excellent cholinesterase- inhibitory activity, suitable for curing or preventing various diseases due to the decline in cholinergic functions, esp. Arzheimer-type senile dementia because of its large maximum tolerance dose and low toxicity. CONSTITUTION:The objective compound of formula I [R is H, aminocarbonyl, etc.; R is lower alkyl; X and X are such that one of them is S, the other being of formula II (R is the same as R ); n is 1 or 2] or a salt thereof, e.g. a compound of formula III. The compound of the formula I can be obtained by the following process: a compound of formula IV (R is the same as R except H; R is thiol-protecting group) is made to react with a lower alkyl halide to form a compound of formula V, which is then dethiolated through e.g. zinc-acetic acid treatment followed by reaction with a compound of formula Br-(CH2)n+1-X (X is halogen), and the resulting intermediate is made to react with an alkali metal salt of thio-lower alkanoic acid to produce a compound of formula VI (R is lower alkanoyl), which is finally put to intramolecular ring closure in the presence of a reducing agent such as metallic sodium.

9. 发明专利

JPH0577650B2 失效
公开(公告)号：JPH0577650B2
公开(公告)日：1993-10-27
申请号：JP3088189
申请日：1989-02-09
申请人： TANABE SEIYAKU CO
发明人： TAKAMURA NORIO , ODA KUNYUKI , KOTADO SHINICHI , YAMAGUCHI ISAO , YANO KOJI
IPC分类号： C07D231/12 , A61K31/415 , A61P9/12

10. 发明专利

JPH05202062A ANTIBACTERIAL AGENT 失效
公开(公告)号：JPH05202062A
公开(公告)日：1993-08-10
申请号：JP5304592
申请日：1992-01-27
申请人： TANABE SEIYAKU CO
发明人： TAKAMURA NORIO , SAITO KUNIO , MATSUSHITA TADAHIRO , YAMAGUCHI TOTARO
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/22 , C07D501/34 , C07D501/36 , C07D501/46
摘要： PURPOSE:To provide the subject antibacterial agent containing a cephalosporin compound excellent in antibacterial effect, especially on Gram positive bacteria as the active component and very stable to beta-lactamase-producing bacteria. CONSTITUTION:The objective antibacterial agent contains, as the active component, a cephalosporin compound (salt) of the formula [R is (protected)amino; R is (protected)OH or a lower alkoxy; R is (protected)carboxyl; R is H, a lower alkyl or a lower alkenyl; Formula CH2R is a nucleophilic compound residue; R is (protected)carboxyl or COO ; R is H or a lower alkyl; Dotted line shows existence or absence of a double bond], e.g. 7beta-{(Z)-2-(2- tritylaminothiazol-4-yl)-2-[(8-diphenyloxy-2-oxo-1 H-quinolin-5- yl)(diphenylmethyloxycarbonyl) methyloxyimino] acetamide} cephalosporanic acid.

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