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21. 发明专利

ES2184731T3 未知
公开(公告)号：ES2184731T3
公开(公告)日：2003-04-16
申请号：ES92913257
申请日：1992-06-19
申请人： DAIICHI SEIYAKU CO
发明人： NISHI TOSHIYUKI , KODA HIROKO , SUGITA KAZUYUKI , ISHIDA YOHHEI , TAKEMURA MAKOTO , HAYANO TAKESHI
IPC分类号： A61K31/40 , A61K31/397 , A61K31/4025 , A61K31/496 , A61P31/04 , C07D20060101 , C07D477/00 , C07D477/20
摘要： Known carbapenem derivatives such as thienamycin have disadvantages that they are physicochemically unstable and readily decomposed by enzymes such as DHP of the kidney to bring about adverse effects such as nephrotoxicity, while 1- beta - methylcarbapenem compounds are stable and have potent antibacterial activities but are yet unsatisfactory as regards the stability and antibacterial activity against DHP. Under these circumstances the invention provides an antibiotic represented by general formula (I) which has a potent antibacterial activity against various bacteria including Pseudomonas aeruginosa and is excellent in safety and stable against hydrolases such as DHP, and a salt thereof (I), wherein R represents lower alkyl or optionally protected hydroxy lower alkyl; R , R and R represent each hydrogen or lower alkyl; R represents optionally esterified carboxy R , R , R and R represent each an amino-protective group, hydrogen or lower alkyl; R , R , R and R represent each hydrogen, hydroxyl, lower alkyl, hydroxy lower alkyl or halogen, or alternatively R and R and/or R and R may combine together to form alkylene; R represents hydrogen, lower alkyl, carboxyl, carbamoyl or -CONR R ; R and R represent each hydrogen or lower alkyl; R represents hydrogen, lower alkyl or hydroxy lower alkyl, or alternatively R may combine with R to form alkylene; Z represents a single bond, oxygen, sulfur, -CR R -, -NR CO-, -CONR - or -NR -; and m and n represent each an integer of 0 to 6.

22. 发明专利

DE69232791D1 CARBAPENEMDERIVATE 未知
公开(公告)号：DE69232791D1
公开(公告)日：2002-10-31
申请号：DE69232791
申请日：1992-06-19
申请人： DAIICHI SEIYAKU CO
发明人： NISHI TOSHIYUKI , KODA HIROKO , SUGITA KAZUYUKI , ISHIDA YOHHEI , TAKEMURA MAKOTO , HAYANO TAKESHI
IPC分类号： A61K31/40 , A61K31/397 , A61K31/4025 , A61K31/496 , A61P31/04 , C07D20060101 , C07D477/00 , C07D477/20
摘要： Known carbapenem derivatives such as thienamycin have disadvantages that they are physicochemically unstable and readily decomposed by enzymes such as DHP of the kidney to bring about adverse effects such as nephrotoxicity, while 1- beta - methylcarbapenem compounds are stable and have potent antibacterial activities but are yet unsatisfactory as regards the stability and antibacterial activity against DHP. Under these circumstances the invention provides an antibiotic represented by general formula (I) which has a potent antibacterial activity against various bacteria including Pseudomonas aeruginosa and is excellent in safety and stable against hydrolases such as DHP, and a salt thereof (I), wherein R represents lower alkyl or optionally protected hydroxy lower alkyl; R , R and R represent each hydrogen or lower alkyl; R represents optionally esterified carboxy R , R , R and R represent each an amino-protective group, hydrogen or lower alkyl; R , R , R and R represent each hydrogen, hydroxyl, lower alkyl, hydroxy lower alkyl or halogen, or alternatively R and R and/or R and R may combine together to form alkylene; R represents hydrogen, lower alkyl, carboxyl, carbamoyl or -CONR R ; R and R represent each hydrogen or lower alkyl; R represents hydrogen, lower alkyl or hydroxy lower alkyl, or alternatively R may combine with R to form alkylene; Z represents a single bond, oxygen, sulfur, -CR R -, -NR CO-, -CONR - or -NR -; and m and n represent each an integer of 0 to 6.

23. 发明专利

NO934670L 未知
公开(公告)号：NO934670L
公开(公告)日：1994-02-18
申请号：NO934670
申请日：1993-12-17
申请人： DAIICHI SEIYAKU CO
发明人： NISHI TOSHIYUKI , KODA HIROKO , SUGITA KAZUYUKI , ISHIDA YOHHEI , TAKEMURA MAKOTO , HAYANO TAKESHI
IPC分类号： A61K31/40 , A61K31/397 , A61K31/4025 , A61K31/496 , A61P31/04 , C07D20060101 , C07D477/00 , C07D477/20
摘要： Known carbapenem derivatives such as thienamycin have disadvantages that they are physicochemically unstable and readily decomposed by enzymes such as DHP of the kidney to bring about adverse effects such as nephrotoxicity, while 1- beta - methylcarbapenem compounds are stable and have potent antibacterial activities but are yet unsatisfactory as regards the stability and antibacterial activity against DHP. Under these circumstances the invention provides an antibiotic represented by general formula (I) which has a potent antibacterial activity against various bacteria including Pseudomonas aeruginosa and is excellent in safety and stable against hydrolases such as DHP, and a salt thereof (I), wherein R represents lower alkyl or optionally protected hydroxy lower alkyl; R , R and R represent each hydrogen or lower alkyl; R represents optionally esterified carboxy R , R , R and R represent each an amino-protective group, hydrogen or lower alkyl; R , R , R and R represent each hydrogen, hydroxyl, lower alkyl, hydroxy lower alkyl or halogen, or alternatively R and R and/or R and R may combine together to form alkylene; R represents hydrogen, lower alkyl, carboxyl, carbamoyl or -CONR R ; R and R represent each hydrogen or lower alkyl; R represents hydrogen, lower alkyl or hydroxy lower alkyl, or alternatively R may combine with R to form alkylene; Z represents a single bond, oxygen, sulfur, -CR R -, -NR CO-, -CONR - or -NR -; and m and n represent each an integer of 0 to 6.

24. 发明专利

ES2238723T3 DERIVADOS DE AMINOCICLOPROPANO CIS-SUSTITUIDOS. 未知
公开(公告)号：ES2238723T3
公开(公告)日：2005-09-01
申请号：ES97930766
申请日：1997-07-11
申请人： DAIICHI SEIYAKU CO
发明人： TAKEMURA MAKOTO , KIMURA YOUICHI , TAKAHASHI HISASHI , ISHIDA YOHHEI
IPC分类号： C07D471/04 , A61K31/4375 , A61K31/47 , A61K31/4709 , C07D207/24 , C07D207/26 , C07D401/04 , C07D489/08 , C07D513/08 , C07D207/09 , C07D207/16
摘要： LA PRESENTE INVENCION PROPORCIONA UN AGENTE ANTIMICROBIANO QUE PRESENTA UNA ELEVADA SEGURIDAD, ASI COMO UNA POTENTE ACTIVIDAD ANTIMICROBIANA, SOBRE UNA AMPLIA VARIEDAD DE MICROORGANISMOS. DICHO AGENTE ES UN COMPUESTO REPRESENTADO POR LA SIGUIENTE FORMULA, SUS SALES E HIDRATOS: DONDE R 1 Y R 2 RE PRESENTAN CADA UNO INDEPENDIENTEMENTE UN ATOMO DE HIDROGENO O UN GRUPO ALQUILO; N REPRESENTA UN ENTERO DE 1 A 3; R 3 REPRESENTA UN GRUPO ALQUILO, UN GRUPO ALQUENILO, UN GRUPO HALOGENOALQUILO, UN GRUPO CICLOALQUILO, UN GRUPO ARILO, UN GRUPO HETEROARILO, UN GRUPO ALCOXILO O UN GRUPO ALQUILAMINO; R 4 R EPRESENTA UN ATOMO DE HIDROGENO O UN GRUPO ALQUILTIO; R 5 REPRESENTA UN ATOMO DE HIDROGENO, UN GRUPO AMINO, UN GRUPO HIDROXILO, UN GRUPO TIOL, UN GRUPO HALOGENOMETILO, UN GRUPO ALQUILO, UN GRUPO ALQUENILO, UN GRUPO ALQUINILO O UN GRUPO ALCOXILO; X 1 REPRESENTA UN ATOMO DE HALOGENO O UN ATOMO DE HIDROGENO; Y A REPRESENTA UN ATOMO DE HIDROGENO, O UNA ESTRUCTURA PARCIAL REPRESENTADA MEDIANTE LA FORMULA (II): DONDE X 2 RE PRESENTA UN ATOMO DE HIDROGENO, UN GRUPO AMINO, UN ATOMO DE HALOGENO, UN GRUPO CIANO, UN GRUPO HALOGENOMETILO, UN GRUPO HALOGENOMETOXILO, UN GRUPO ALQUILO, UN GRUPO ALQUENILO, UN GRUPO ALQUINILO O UN GRUPO ALCOXILO; E Y REPRESENTA UN ATOMO DE HIDROGNEO, UN GRUPO FENILO, UN GRUPO ACETOXIMETILO, UN GRUPO PIVALOILOXIMETILO, UN GRUPO ETOXICARBONILO, UN GRUPO DE COLINA, UN GRUPO DIMETILAMINOETILO, UN GRUPO 5 - INDANILO, UN GRUPO FTALIDINILO, UN GRUPO 5 ALQUIL - 2 - OXO - 1,3 - DIOXOL - 4 - ILMETILO, UN GRUPO 3 ACETOXI - 2 - OXOBUTILO, UN ALQUILO, UN GRUPO ALCOXIMETILO O UN GRUPO FENILALQUILO.

25. 发明专利

NO303636B1 未知
公开(公告)号：NO303636B1
公开(公告)日：1998-08-10
申请号：NO934670
申请日：1993-12-17
申请人： DAIICHI SEIYAKU CO
发明人： NISHI TOSHIYUKI , KODA HIROKO , SUGITA KAZUYUKI , ISHIDA YOHHEI , TAKEMURA MAKOTO , HAYANO TAKESHI
IPC分类号： A61K31/40 , A61K31/397 , A61K31/4025 , A61K31/496 , A61P31/04 , C07D20060101 , C07D477/00 , C07D477/20
摘要： Known carbapenem derivatives such as thienamycin have disadvantages that they are physicochemically unstable and readily decomposed by enzymes such as DHP of the kidney to bring about adverse effects such as nephrotoxicity, while 1- beta - methylcarbapenem compounds are stable and have potent antibacterial activities but are yet unsatisfactory as regards the stability and antibacterial activity against DHP. Under these circumstances the invention provides an antibiotic represented by general formula (I) which has a potent antibacterial activity against various bacteria including Pseudomonas aeruginosa and is excellent in safety and stable against hydrolases such as DHP, and a salt thereof (I), wherein R represents lower alkyl or optionally protected hydroxy lower alkyl; R , R and R represent each hydrogen or lower alkyl; R represents optionally esterified carboxy R , R , R and R represent each an amino-protective group, hydrogen or lower alkyl; R , R , R and R represent each hydrogen, hydroxyl, lower alkyl, hydroxy lower alkyl or halogen, or alternatively R and R and/or R and R may combine together to form alkylene; R represents hydrogen, lower alkyl, carboxyl, carbamoyl or -CONR R ; R and R represent each hydrogen or lower alkyl; R represents hydrogen, lower alkyl or hydroxy lower alkyl, or alternatively R may combine with R to form alkylene; Z represents a single bond, oxygen, sulfur, -CR R -, -NR CO-, -CONR - or -NR -; and m and n represent each an integer of 0 to 6.

27. 发明专利

AU4722197A Novel remedies for infectious diseases 未知
公开(公告)号：AU4722197A
公开(公告)日：1998-05-15
申请号：AU4722197
申请日：1997-10-22
申请人： DAIICHI SEIYAKU CO
发明人： OHTA TOSHIHARU , NAKAYAMA KIYOSHI , OHTSUKA MASAMI , INAGAKI HIROAKI , NISHI TOSHIYUKI , ISHIDA YOHHEI
IPC分类号： C07C237/42 , C07D207/14 , C07C211/34 , A61K31/40 , A61K31/425 , A61K38/05 , A61K38/06 , C07C211/39 , C07C211/44 , C07C211/57 , C07C225/16 , C07C237/10 , C07C317/32 , C07C323/31 , C07C323/40 , C07D207/48 , C07D243/08 , C07D255/02 , C07D295/12 , C07D295/14 , C07D405/06 , C07D417/06

28. 发明专利

AU3459797A Cis-substituted aminocyclopropane derivatives 未知
公开(公告)号：AU3459797A
公开(公告)日：1998-02-09
申请号：AU3459797
申请日：1997-07-11
申请人： DAIICHI SEIYAKU CO
发明人： TAKEMURA MAKOTO , KIMURA YOUICHI , TAKAHASHI HISASHI , ISHIDA YOHHEI
IPC分类号： C07D471/04 , A61K31/4375 , A61K31/47 , A61K31/4709 , C07D207/24 , C07D207/26 , C07D401/04 , C07D489/08 , C07D513/08
摘要： The present invention is to provide an antimicrobial agent having high safety as well as potent antimicrobial activity on broad range of microorganisms. A compound represented by the following formula, its salt and their hydrates: wherein R and R each independently represents a hydrogen atom or an alkyl group; n represents an integer of 1 to 3; R represents an alkyl group, an alkenyl group, a halogenoalkyl group, a cycloalkyl group, an aryl group, a heteroaryl group, an alkoxyl group or an alkylamino group; R represents a hydrogen atom or an alkylthio group; R represents a hydrogen atom, an amino group, a hydroxyl group, a thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group or an alkoxyl group; X represents a halogen atom or a hydrogen atom; and A represents a nitrogen atom or a partial structure represented by formula (II): wherein X represents a hydrogen atom, an amino group, a halogen atom, a cyano group, a halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group or an alkoxyl group; and Y represents a hydrogen atom, a phenyl group, an acetoxymethyl group, a pivaloyloxymethyl group, an ethoxycarbonyl group, a choline group, a dimethylaminoethyl group, a 5-indanyl group, a phthalidinyl group, a 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl group, a 3-acetoxy-2-oxobutyl group, an alkyl, an alkoxymethyl group or a phenylalkyl group.

29. 发明专利

AU659172B2 Carbapenem derivative 未知
公开(公告)号：AU659172B2
公开(公告)日：1995-05-11
申请号：AU2000292
申请日：1992-06-19
申请人： DAIICHI SEIYAKU CO
发明人： NISHI TOSHIYUKI , KODA HIROKO , SUGITA KAZUYUKI , ISHIDA YOHHEI , TAKEMURA MAKOTO , HAYANO TAKESHI
IPC分类号： A61K31/40 , A61K31/397 , A61K31/4025 , A61K31/496 , A61P31/04 , C07D20060101 , C07D477/00 , C07D477/20
摘要： Known carbapenem derivatives such as thienamycin have disadvantages that they are physicochemically unstable and readily decomposed by enzymes such as DHP of the kidney to bring about adverse effects such as nephrotoxicity, while 1- beta - methylcarbapenem compounds are stable and have potent antibacterial activities but are yet unsatisfactory as regards the stability and antibacterial activity against DHP. Under these circumstances the invention provides an antibiotic represented by general formula (I) which has a potent antibacterial activity against various bacteria including Pseudomonas aeruginosa and is excellent in safety and stable against hydrolases such as DHP, and a salt thereof (I), wherein R represents lower alkyl or optionally protected hydroxy lower alkyl; R , R and R represent each hydrogen or lower alkyl; R represents optionally esterified carboxy R , R , R and R represent each an amino-protective group, hydrogen or lower alkyl; R , R , R and R represent each hydrogen, hydroxyl, lower alkyl, hydroxy lower alkyl or halogen, or alternatively R and R and/or R and R may combine together to form alkylene; R represents hydrogen, lower alkyl, carboxyl, carbamoyl or -CONR R ; R and R represent each hydrogen or lower alkyl; R represents hydrogen, lower alkyl or hydroxy lower alkyl, or alternatively R may combine with R to form alkylene; Z represents a single bond, oxygen, sulfur, -CR R -, -NR CO-, -CONR - or -NR -; and m and n represent each an integer of 0 to 6.

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