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1. 发明专利

JPH10330255A ANTTIPHLOGISTIC AND ANALGESIC AGENT 失效
公开(公告)号：JPH10330255A
公开(公告)日：1998-12-15
申请号：JP15735597
申请日：1997-06-02
申请人： LEDERLE JAPAN LTD , WAKO PURE CHEM IND LTD
发明人： YOMO YOSHIYUKI , KUMAGAI TOSHIO
IPC分类号： A61K31/19 , A61P25/04 , A61P29/00
摘要： PROBLEM TO BE SOLVED: To prepare a new medicine and a new antiphlogistic and analgesic agent by formulating a synthetic intermediate for 4-biphenylylacetic acid having strong antiphlogistic and analgesic actions as an active ingredient therein. SOLUTION: The medicine and antiphlogistic and analgesic agent contain 4-biphenyl-α-hydroxyacetic acid or its pharmacologically acceptable salt as an active ingredient. The 4-biphenyl-α-hydroxyacetic acid is an intermediate obtained from, i.e., a starting raw material 4-halogenated acetylbiphenyl of 4-biphenylaldehyde when synthesizing 4-biphenylacetic acid. The medicine and antiphlogistic and analgesic agent can orally or parenterally be administered. The daily dose thereof for an adult is usually 1-200 mg/kg in the case of the oral administration and 0.01-10 mg/kg in the case of the parenteral administration.

2. 发明专利

JPH09165386A DIAZABICYCLO COMPOUND 失效
公开(公告)号：JPH09165386A
公开(公告)日：1997-06-24
申请号：JP26913596
申请日：1996-09-20
申请人： LEDERLE JAPAN LTD
发明人： MATSUNAGA HIROSHI , KANEDA SOICHI , SHIMIZU HISASHI , YOMO YOSHIYUKI , KUMAGAI TOSHIO
IPC分类号： C07D471/04 , A61K31/435 , A61P9/00 , A61P9/08 , A61P9/10
摘要： PROBLEM TO BE SOLVED: To obtain a new derivative consisting of a specific 1,9- diazabicyclonona-3,8-diene derivative, having an improving action on circulatory disorders caused by ischemia, anoxia or hypoxia, and useful for medicines, especially circulatory disorder-improving medicines, etc. SOLUTION: This is a new 1,9-diazabicyclo[4.3.0]nona-3,8-diene derivative of formula I [R is H, a (substituted) lower alkyl, a lower alkenyl, a (substituted) lower acyl, a (substituted) heterocyclic alkyl, etc.; R is H, oxo, mercapto, amino, etc.; R is carboxy, a lower alkoxycarbonyl, etc.; R , R are each H, a lower alkyl, a lower alkoxy, etc.; R , R are each H, a lower alkyl; the broken line expresses the presence or absence of a double bond], which is useful for medicines for improving circulatory disorders caused by ischemia, anoxia or hypoxia, etc. The compound is obtained by the Diels Alder reaction of a 1,3,-bis(diaza-2-propanone compound of formula II (R is a lower alkyl)with a 1,3-butadiene derivative of formula III.

3. 发明专利

JP2592110B2 失效
公开(公告)号：JP2592110B2
公开(公告)日：1997-03-19
申请号：JP23963688
申请日：1988-09-27
申请人： LEDERLE JAPAN LTD
发明人： ABE TAKAO , MATSUNAGA HIROSHI , KUMAGAI TOSHIO , NAGASE JUNOSUKE
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61P31/04 , C07D519/00

4. 发明专利

JPH07196659A 2-((SUBSTITUTED 1,3-THIAZOLIUM-3-YL)ALKYLTHIO)CARBAPENEM DERIVATIVE 失效
公开(公告)号：JPH07196659A
公开(公告)日：1995-08-01
申请号：JP34935493
申请日：1993-12-28
申请人： LEDERLE JAPAN LTD
发明人： TAMAI SEI , KUMAGAI TOSHIO , NAGASE YUUNOSUKE
IPC分类号： C07D477/00 , A61K31/397 , A61K31/425 , A61P31/04
摘要： PURPOSE:To obtain a carbapenem derivative useful as an antimicrobial agent, having excellent resistance to beta-lactase and renal dehydropeptidase and strongly antimicrobial activity, shown by a specific formula, containing a methyl group of beta-configuration on a carbapenem skeleton. CONSTITUTION:The compound of formula I (R1 and R2 each is H, a lower alkenyl, a halogen, hydroxy, a lower alkoxy or a lower alkyl which may be substituted with mercapto or a lower alkylthio; n is 1-4) such as (1R,5S,6 S)-6-[(R)-1-hydroxyethyl]-2-[2-[5-(2hydroxyethyl)-4-methyl-1,3-thiazol ium-3- yl]ethylthio]-1methylcarbapen-2-em-3-carboxylate, etc. The compound, for example, is preferably obtained by reacting a compound of formula II (R is an acyl) as a starting substance with a mercaptoalcohol of formula III in the presence of a solvent such as tetrahydrofuran.

5. 发明专利

JPH0770139A 2-(MONO-OR DI-SUBSTITUTED 6,7-DIHYDRO-5H-PYRAZOLO(1,2-A)PYRAZOLIUM-6-YL)THIOCARBAPENEM DERIVATIVE 失效
公开(公告)号：JPH0770139A
公开(公告)日：1995-03-14
申请号：JP17049794
申请日：1994-06-30
申请人： LEDERLE JAPAN LTD
发明人： TAMAI SEI , ISODA TAKETOSHI , MIHIRA ADO , KUMAGAI TOSHIO
IPC分类号： A61K31/415 , A61P31/04 , C07D519/00
摘要： PURPOSE:To obtain the subject compound exhibiting powerful antibacterial activity, also having high resistance to kidney dehydropeptidase and beta-lactamase. CONSTITUTION:A compound of formula I[R and R are such that one of them is H, the other being a (OH-, lower alkoxy-, SH- or NH2-substituted) lower alkyl, carbamoyl, a mono- or di-lower alkyl-substituted amide, or halogen] and a pharmacologically permissible salt thereof, e.g. (1R, 5S, 6S)-2-[(6,7- dihydro-1,3-dimethyl-5H--pyrazolo[1,2-a]pyrazolium-6-yl)thio]-6-[(R)-1- hydroxyethyl]-1-methyl-carbapen-2-em-3-carboxylate. The compound of formula I can be obtained by reaction of a compound of formula II with a 2-substituted or a 1,3-disubstituted 6,7-dihydro-6-mercapto-5H-pyrazolo[1,2-a]pyrazolium salt of formula III to form a compound of formula IV, and then eliminating whose carboxyl protecting group R .

6. 发明专利

JPH04356460A OPTICALLY ACTIVE BICYCLO(2,2,1)HEPTANE-2,3-DICARBOXYLIC ACID DERIVATIVE 失效
公开(公告)号：JPH04356460A
公开(公告)日：1992-12-10
申请号：JP41412690
申请日：1990-12-17
申请人： LEDERLE JAPAN LTD
发明人： KUMAGAI TOSHIO , NAGASE YUUNOSUKE
IPC分类号： A61K31/40 , A61K31/403 , A61P9/06 , C07D209/72 , C07D209/74 , C07D209/76 , C07D307/77 , C07D413/06 , C07D417/06
摘要： PURPOSE:To obtain a compound useful as an intermediate for an optically active bicyclo[2,2,1]heptane derivative having antiarrhythmic activity. CONSTITUTION:Compounds shown by formula I and formula II [R is H, lower alkyl or phenyl; E is group shown by formula III (G and L are O or S; R is lower alkyl or lower alkoxycarbonyl; R and R are H, lower alkyl, aryl, aralkyl, etc.), etc.]. The compounds are obtained by reacting a racemic compound shown by formula IV with an optically active heterocyclic compound shown by formula V and formula VI in an inert solvent (e.g. dichloromethane) in the presence of a base (e.g. triethylamine) and a carboxylic acid activating reagent (e.g. thionyl chloride or phosphoryl chloride) at -40 to 100 deg.C for 5 minutes to 24 hours. (4S) or (4R) 4-Methyl-1,3-thiazolidine-2-thione may be cited as the compound shown by formula V or formula VI.

7. 发明专利

JPH0471917B2 失效
公开(公告)号：JPH0471917B2
公开(公告)日：1992-11-16
申请号：JP1752683
申请日：1983-02-07
申请人： LEDERLE JAPAN LTD
发明人： FUJITA EIICHI , NAGAO YOSHIMITSU , KUMAGAI TOSHIO , ABE TAKAO , TAMAI SEI
IPC分类号： C07C67/20 , C07B31/00 , C07B51/00 , C07B53/00 , C07C27/00 , C07C29/132 , C07C29/147 , C07C45/00 , C07C45/41 , C07C67/00 , C07C231/00 , C07C231/02 , C07C325/00 , C07C327/20 , C07F9/653 , C07F9/6539

8. 发明专利

JPH04169584A CARBAPENEM COMPOUND 失效
公开(公告)号：JPH04169584A
公开(公告)日：1992-06-17
申请号：JP29352090
申请日：1990-11-01
申请人： LEDERLE JAPAN LTD
发明人： HATANO TOSHIMITSU , ISODA TAKETOSHI , KUMAGAI TOSHIO
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61P31/04
摘要： NEW MATERIAL:(5S,6S)-2-[(6,7-dihydro-5H-pyrazolo[1,2-a] [1,2,4]triazolium-6-yl) thio]-6-[(R)-l-hydroxyethyl]-carbapen-2-em-3-carboxylate. USE:An antibacterial agent and beta-lactamase inhibitor. PREPARATION:The objective compound can be produced by reacting a compound of formula II (R is carboxy-protecting group; R is acyl) with a mercapto reagent of formula III (R is amino-protecting group), eliminating the protecting groups R and R from the obtained compound of formula VI and reacting the resultant compound of formula V with a formimidic acid ester derivative.

9. 发明专利

JPH04154758A PRODUCTION OF 2-AZETIDINONE DERIVATIVE 失效
公开(公告)号：JPH04154758A
公开(公告)日：1992-05-27
申请号：JP27519590
申请日：1990-10-16
申请人： LEDERLE JAPAN LTD
发明人： NAGAO YOSHIMITSU , MATSUNAGA HIROSHI , KUMAGAI TOSHIO
IPC分类号： C07D205/08 , C07C235/08
摘要： PURPOSE:To readily and highly stereoselectively obtain the subject compound which is a synthetic raw material for carbapenem compounds useful as an antimicrobial agent in good yield by subjecting a new compound as a raw material to condensation cyclizing reaction and then, as necessary, eliminating protecting groups of OH, etc. CONSTITUTION:Carboxylic acids expressed by formula I (R is protecting group of OH) are made to react with a compound expressed by formula II (R is lower alkyl) to produce a compound expressed by formula III, which is subsequently reacted with a tin(II) triflate in the presence of a base to provide an enolate. The resultant enolate is then reacted with acetaldehyde to afford a compound expressed by formula IV. The OH of the obtained compound expressed by formula IV is subsequently protected to afford a compound expressed by formula V (R is R ), which is then allowed to react with a 4-lower alkoxyphenylamine to produce a compound expressed by formula VI (R is R ). The protecting group R of the OH is subsequently eliminated therefrom to form a new compound expressed by formula VII which is a raw material. The resultant compound expressed by formula VII is then subjected to condensing reaction and, as necessary, the protecting group of OH or the 4-lower alkoxyphenyl group or both are eliminated to afford the objective compound expressed by formula VIII.

10. 发明专利

JPH03861B2 失效
公开(公告)号：JPH03861B2
公开(公告)日：1991-01-09
申请号：JP3725583
申请日：1983-03-09
申请人： LEDERLE JAPAN LTD
发明人： FUJITA EIICHI , NAGAO YOSHIMITSU , KUMAGAI TOSHIO , ABE TAKAO , TAMAI SEI
IPC分类号： C07D205/08 , C07D205/085 , C07D403/12 , C07D409/12 , C07D417/12

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