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21. 发明专利

JPH05239058A 失效
公开(公告)号：JPH05239058A
公开(公告)日：1993-09-17
申请号：JP33623592
申请日：1992-12-16
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： CHIBA TOSHIYUKI , MATSUDA KEIJI , SAKURAI MINORU , AOKI SATOSHI , WASHITSUKA KENICHI
IPC分类号： A61K31/40 , A61K31/397 , A61K31/415 , A61K31/44 , A61K31/495 , A61P31/04 , C07D477/00
摘要： PURPOSE:To provide a new compound inhibiting the growth of a wide range of pathogenic bacteria including gram-positive bacteria and gram-negative bacteria and useful as an antibacterial agent. CONSTITUTION:A compound of formula I (R is carboxy, protected carboxy; R is hydroxy (lower) alkyl, etc.; R is H, lower alkyl; R is hydroxy, lower alkoxy, etc.; R is H, imino-protecting group; A is lower alkylene), e.g. (4R,5S,6 S)-3-[(2S,4S)-1-alluyoxycarbonyl-2-{(E)-3-t-butyldimethylsiloxy-1 propenyl}pyrolidin-4-ylthio]-6-[(R)-1-hydroxyethyl]-4-methyl-7-oxo-1- azabicyclo[3.2.0] hepto-2-ene-2-carboxylic acid allyl ester. The compound of formula I is obtained by reacting a compound of formula II with a compound of formula III in the presence of a base in a solvent under cooling to heating.

22. 发明专利

JPH02204490A 3-PYRROLIDINYLTHIO-1-AZABICYCLO(3.2.0)HEPT-2-ENE-2-CARBOXYLIC ACID DERIVATIVE AND PRODUCTION THEREOF 失效
公开(公告)号：JPH02204490A
公开(公告)日：1990-08-14
申请号：JP11914189
申请日：1989-05-12
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： MURATA MASAYOSHI , TSUTSUMI HIDEO , MATSUDA KEIJI , HATTORI KOJI , NAKAJIMA HISASHI
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61P31/04 , C07D207/12 , C07D477/20 , C07F7/18
摘要： NEW MATERIAL:A compound expressed by formula I [R is (protected) carboxy; R is (protected) hydroxy-lower alkyl; R3 is H or lower alkyl; R is monohalo- lower alkyl, mono-, di-lower alkylamino-lower alkyl, etc.; R is H, lower alkaneimidoyl, (substituted) lower cyloalkenyl or imino-protecting group; A is lower alkylene]. EXAMPLE:(4R,5S,6S)-3-[(2S,4S)-2-(2-Fluoroethyloxymethyl)pyrrolidin-4-y l]thio-6-[(1 R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carb oxylic acid. USE:An antimicrobial agent. PREPARATION:A compound expressed by formula II or a reactive derivative at the oxo group thereof, etc., are reacted with a compound expressed by formula III.

23. 发明专利

JPS63179875A 3-PYRROLIDINYLTHIO-1-AZABICYCLO(3.2.0)HEPT-2-ENE-2-CARB-OXYLIC ACID COMPOUND AND PRODUCTION THEREOF 失效
公开(公告)号：JPS63179875A
公开(公告)日：1988-07-23
申请号：JP29590087
申请日：1987-11-24
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： MURATA MASAYOSHI , TSUTSUMI HIDEO , MATSUDA KEIJI , HATTORI KOJI , NAKAJIMA HISASHI
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61K31/44 , A61P31/04 , C07D207/12 , C07D401/12 , C07D403/12 , C07D417/12 , C07D477/20
摘要： NEW MATERIAL:A compound expressed by formula I [R is (protected) carboxy; R is (protected) hydroxy (lower) alkyl; R is H or lower alkyl; R is (protected) ureido (lower) alkyl; R is H, lower alkanimidoyl or imide-protecting group; A is lower alkylene] and salts thereof. EXAMPLE:(4R,5S,6S)-6-[(1R)-1-Hydroxyethyl]-4-methyl-7-oxo-3-[(2S,4S)-2 -{(2-ureidoethyl)oxymethyl}pyrrolidin-4-yl]thio-1-azabicyclo[3.2.0]hep t-2-ene-2-carbo xylic acid. USE:An antimicrobial agent, extremely stable to dehydropeptidase and capable of exhibiting high discharge into urine. PREPARATION:For example, a compound expressed by formula II is reacted with a compound expressed by formula III to afford the aimed compound expressed by formula I.

24. 发明专利

JPS63170379A 2-PYRROLIDINYLTHIO-1-AZABICYCLO-(3.2.0)HEPT-2-ENE-2-CAR-BOXYLIC ACID COMPOUND 失效
公开(公告)号：JPS63170379A
公开(公告)日：1988-07-14
申请号：JP29590287
申请日：1987-11-24
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： MURATA MASAYOSHI , TSUTSUMI HIDEO , MATSUDA KEIJI , HATTORI KOJI , NAKAJIMA HISASHI
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/425 , A61P31/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D477/20
摘要： NEW MATERIAL:The compound of formula I [R is (protected) carboxy; R is (proteced) hydroxyalkyl; R is H or alkyl; R is (substituted) heterocyclic group; R is H or imino-protecting group] and its salt. EXAMPLE:(4R,5S,6S)-3-[(2S,4S)-2-{2-(aminomethyl)thiazol-4-yl}-pyrrolid in-4-ylth io]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-e ne-2-carbox ylic acid. USE:It has high antibacterial activity against various pathogenic bacteria and is useful as a remedy for infectious diseases. PREPARATION:The compound of formula I can be produced e.g. by reacting a compound of formula II or its reactive derivative at the oxo group with a compound of formula III.

25. 发明专利

JPS63146894A AMINOGLYCOSIDE DERIVATIVE 失效
公开(公告)号：JPS63146894A
公开(公告)日：1988-06-18
申请号：JP29281687
申请日：1987-11-19
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： TAKATANI TAKAO , YASUDA NOBUSACHI , TSUTSUMI HIDEO , MATSUDA KEIJI
IPC分类号： C07H15/23 , A61K20060101 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , A61P31/12 , A61P37/04 , C07H20060101 , C07H15/22 , C07H15/234
摘要： NEW MATERIAL:The compound of formula I [at least one of R -R is higher alkanoylamino, higher alkenylamino, higher alkoxycarbonylamino, higher alkylaminocarboxylamino, higher alkoxy(lower)alkanoylamino or higher alkylthiocarbonylamino which may have substituent group and the others are amino or acylamino; Ra -Ra are acyloxy; R ' is OH, acyloxy, ar(lower)alkoxy or protected phosphonoxy]. EXAMPLE:1,3,6'-Tris-N-benzyloxycarbonyl-3''-N-trifluoroacetylkanamycin A. USE:Antiviral agent, immunoactivation agent and their production raw material. PREPARATION:The compound of formula III (Ra ' is acyloxy) can be produced e.g. by reacting a compound of formula II with a proper acylation agent in a solvent such as THF in the presence of a base such as triethylamine.

26. 发明专利

JPS611696A NOVEL AMINOGLYCOSIDE DERIVATIVE 失效
公开(公告)号：JPS611696A
公开(公告)日：1986-01-07
申请号：JP12275784
申请日：1984-06-13
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： TAKATANI TAKAO , YASUDA NOBUSACHI , TSUTSUMI HIDEO , MATSUDA KEIJI
IPC分类号： C07H15/236 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/00
摘要： NEW MATERIAL:A compound shown by the formula I [R is (substituted) higher alkanoylamino; R and R are amino, or acylamino; R is H, or lower alkyl; R and R are (substituted)amino] and its salt. EXAMPLE:1-N-Palmitoyl-3''-N-trifluoroacetylgentamicin C. USE:A preventive and remedy for infectious diseases of pathogenic microorganism. PREPARATION:A compound shown by the formula II (R is amino) or its reactive derivative (salt) at its amino group (e.g., 3,2',6'-tri-N-benzyloxycarbonyl-3''-N- trifluoroacetylgentamicin C, etc.) is acylated with an acylating agent shown by the formula R -OH.

27. 发明专利

JPS60166678A NOVEL QUINOLONE COMPOUND AND ITS PREPARATION 失效
公开(公告)号：JPS60166678A
公开(公告)日：1985-08-29
申请号：JP26913584
申请日：1984-12-19
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： TAKATANI TAKAO , TSUTSUMI HIDEO , MATSUDA KEIJI , SAKAI HIROYOSHI , MURATA MASAYOSHI
IPC分类号： C07D213/26 , A61K31/47 , A61P31/04 , C07D213/00 , C07D213/38 , C07D215/00 , C07D401/04
摘要： NEW MATERIAL:A quinolone compound shown by the formula I (R and R are halogen; R is lower alkyl; R is carboxy or epoxidized carboxy) and its salt. EXAMPLE:1-Ethyl-3-ethoxycarbonyl-6,8-difluoro-7-(3-pyridyl)-4-quinolone. USE:An antibacterial agent. Inhibiting growth of various pathogenic bacteria including Gram-positive and Gram-negative bacteria. PREPARATION:A novel compound shown by the formula II or its salt is heated to give a compound shown by the formula I or a compound shown by the formula III (R is esterified carboxy) or its salt is de-esterified to give a compound shown by the formula IV or its salt, and the compound shown by the formula I is obtained.

28. 发明专利

JP2512968B2 失效
公开(公告)号：JP2512968B2
公开(公告)日：1996-07-03
申请号：JP29590087
申请日：1987-11-24
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： MURATA MASAYOSHI , TSUTSUMI HIDEO , MATSUDA KEIJI , HATSUTORI KOJI , NAKAJIMA HISASHI
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61K31/44 , A61P31/04 , C07D207/12 , C07D401/12 , C07D403/12 , C07D417/12 , C07D477/20

29. 发明专利

JPH07196662A BICYCLIC COMPOUND AND ITS PRODUCTION 失效
公开(公告)号：JPH07196662A
公开(公告)日：1995-08-01
申请号：JP29943794
申请日：1994-12-02
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： CHIBA TOSHIYUKI , MATSUDA KEIJI , WASHITSUKA KENICHI , AZAMI HIDENORI
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/44 , A61P31/04
摘要： PURPOSE:To obtain a bicyclic compound useful for treating human and animal infectious diseases, having antimicrobial action by reacting plural compounds shown by specific formulas, respectively. CONSTITUTION:This compound of formula I [R is (protected) carboxyl; R is a (protected) hydroxy-lower alkyl; R is H or a lower alkyl; R is H, a lower alkyl or an amino protecting group; R is (substituted) pyrazolyl, imidazolyl or pyridyl; R is H or an imino protecting group; A is a lower alkylene]. The compound is obtained by reacting a compound of formula II or its reactive derivative at its oxo group or its salt with a compound of formula III or its salt. For example, (4R,5S,6S)6-[(1R)-1-hydroxyethyl]-3-[(2R,4S)-2-[2-(imidazol-2 ylamino)decylpyrrolidin-4-yllthio-4-methyl-7-oxo-azabicyclo[3,2,0]hept -2-ene-2- carboxylic acid hydrochloride may be cited as the compound.

30. 发明专利

JPH0672999A PRODUCTION OF AMINOALKYLPYRROLIDINE COMPOUND 失效
公开(公告)号：JPH0672999A
公开(公告)日：1994-03-15
申请号：JP25371192
申请日：1992-08-28
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： MATSUDA KEIJI , HATTORI KOJI , SAKANE KAZUO
IPC分类号： C07D207/09
摘要： PURPOSE:To industrially and advantageously obtain the high-purity subject compound useful as an intermediate for producing synthetic antifungal agents by reacting hydroxyalkylpyrrolidines with an alkali metal azide compound and then subjecting an azide group of the resultant reactional product to reduction reaction. CONSTITUTION:A 3-hydroxyalkylpyrrolidine compound expressed by formula I (R is imino protecting group; R is lower alkyl) {e.g. (3R-1-benzoyl-3-[(1R)-1- hydroxyethyl]pyrrolidine} or its reactive derivative(salt) in hydroxyl group is made to react with an azide compound of the formula X-N (X is alkali metal) to afford an azide compound of formula II and then tetrahydrofuran solution of triphenylphosphine is added thereto and the azide compound of formula II is made to react with triphenylphosphine at 50-60 deg.C for 4hr and then concentrated ammonia water is added to the reactional product and the solution is allowed to stand overnight and then the solvent is distilled away under reduced pressure to provide the objective aminoalkylpyrrolidine compound expressed by formula III.

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