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1. 发明授权

US5374720A 2-(substituted pyrrolidinylthio)carbapenem derivatives 失效
标题翻译： 2-（取代的吡咯烷硫基）碳青霉烯衍生物
公开(公告)号：US5374720A
公开(公告)日：1994-12-20
申请号：US780142
申请日：1991-10-21
申请人： Susumu Nakagawa , Norikazu Ohtake , Fumio Nakano , Koji Yamada , Ryosuke Ushijima , Satoshi Murase , Hiroshi Fukatsu
发明人： Susumu Nakagawa , Norikazu Ohtake , Fumio Nakano , Koji Yamada , Ryosuke Ushijima , Satoshi Murase , Hiroshi Fukatsu
IPC分类号： C07D477/20 , C07D487/04 , A61K31/40
CPC分类号： C07D477/20
摘要： A compound of the formula: ##STR1## wherein R is a hydrogen atom or a methyl group, R.sup.1 is a hydrogen atom or a negative charge, each of R.sup.2 and R.sup.3 which may be the same or different, is a hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group, a formimidoyl group, an acetoimidoyl group, --COOR.sup.4, --CON(R.sup.5)R.sup.6, --N(R.sup.5)R.sup.6, --CH.sub.2 COOR.sup.4, --CH.sub.2 N(R.sup.5)R.sup.6 or --CH.sub.2 CON(R.sup.5)R.sup.6 (wherein R.sup.4 is a hydrogen atom or a lower alkyl group, each of R.sup.5 and R.sup.6 which may be the same or different, is a hydrogen atom or a lower alkyl group, or R.sup.5 and R.sup.6 form together with the adjacent nitrogen atom a heterocyclic group selected from the group consisting of an aziridinyl group, an azetidinyl group, a pyrrolidinyl group and a piperidyl group), A is .dbd.NR.sup.7, .dbd.N.sup.+ (R.sup.7)R.sup.8, wherein each of R.sup.7 and R.sup.8 which may be the same or different, is a hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group, a formimidoyl group, an acetoimidoyl group, --COOR.sup.4, --CON(R.sup.5)R.sup.6, --N(R.sup.5)R.sup.6, --CH.sub.2 COOR.sup.4, --CH.sub.2 N(R.sup.5)R.sup.6 or --CH.sub.2 CON(R.sup.5)R.sup.6 (wherein R.sup.4, R.sup.5 and R.sup.6 are as defined above), p is an integer of from 0 to 3, and q is an integer of from 1 to 3; or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：下式的化合物：其中R是氢原子或甲基，R 1是氢原子或负电荷，R 2和R 3可以相同或不同，为氢原子，低级烷基，羟基低级烷基，亚氨基，亚氨酰基，-COOR4，-CON（R5）R6，-N（R5）R6，-CH2COOR4，-CH2N（R5）R6或-CH2CON（ R5）R6（其中R4是氢原子或低级烷基，R5和R6各自可以相同或不同，是氢原子或低级烷基，或R5和R6与相邻的氮原子一起形成）选自氮丙啶基，氮杂环丁烷基，吡咯烷基和哌啶基的杂环基），A为= NR 7 = N +（R 7）R 8，其中R 7和R 8可以相同或不同，不同的是氢原子，低级烷基，羟基低级烷基，亚氨基，亚氨代乙酰基，-COOR4，-CON（R5）R6，-N（R5）R6，-CH2COOR4，-CH2N（R5 ）R6或-CH2CON（R5）R6（其中在R4中，R5和R6如上所定义），p是0-3的整数，q是1至3的整数; 或其药学上可接受的盐或酯。

2. 发明授权

US5373002A 2-(substituted pyrrolidinylthio) carbapenem derivatives 失效
标题翻译： 2-（取代的吡咯烷硫基）碳青霉烯衍生物
公开(公告)号：US5373002A
公开(公告)日：1994-12-13
申请号：US950717
申请日：1992-09-25
申请人： Susumu Nakagawa , Norikazu Ohtake , Fumio Nakano , Koji Yamada , Ryosuke Ushijima , Satoshi Murase , Hiroshi Fukatsu
发明人： Susumu Nakagawa , Norikazu Ohtake , Fumio Nakano , Koji Yamada , Ryosuke Ushijima , Satoshi Murase , Hiroshi Fukatsu
IPC分类号： C07D477/20 , A01N43/00 , A61K31/395 , C07D487/04
CPC分类号： C07D477/20
摘要： A compound of the formula: ##STR1## wherein R is a hydrogen atom or a methyl group, R.sup.1 is a hydrogen atom or a negative charge, R.sup.2 is a lower alkyl group, a lower alkyl group substituted with a hydroxyl group or --COOR.sup.3 (wherein R.sup.3 is a hydrogen atom or a lower alkyl group), A is .dbd.NH, .dbd.NR.sup.4 or .dbd.N(R.sup.4)R.sup.5 (wherein each of R.sup.4 and R.sup.5 which may be the same or different, is a lower alkyl group or a lower alkyl group substituted with a hydroxyl group), p is an integer of from 0 to 3, and each of q and r which may be the same or different, is an integer of from 0 to 5, provided that q and r are not simultaneously 0 and q +r.ltoreq.6; or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：下式的化合物：其中R是氢原子或甲基，R1是氢原子或负电荷，R2是低级烷基，被羟基取代的低级烷基或 -COOR 3（其中R 3为氢原子或低级烷基），A为= NH，= NR 4或= N（R 4）R 5（其中R 4和R 5可以相同或不同，为低级烷基或被羟基取代的低级烷基），p为0〜3的整数，q和r可以相同或不同，为0〜5的整数，条件是q和r 不同时为0和q + r为6; 或其药学上可接受的盐或酯。

3. 发明授权

US5438054A 2-(substituted pyrrolidinylthio) carbapenem derivatives 失效
标题翻译： 2-（取代的吡咯烷硫基）碳青霉烯衍生物
公开(公告)号：US5438054A
公开(公告)日：1995-08-01
申请号：US208046
申请日：1994-03-09
申请人： Susumu Nakagawa , Norikazu Ohtake , Fumio Nakano , Koji Yamada , Ryosuke Ushijima , Satoshi Murase , Hiroshi Fukatsu
发明人： Susumu Nakagawa , Norikazu Ohtake , Fumio Nakano , Koji Yamada , Ryosuke Ushijima , Satoshi Murase , Hiroshi Fukatsu
IPC分类号： C07D477/20 , A01N43/00 , A61K31/395 , C07D487/04
CPC分类号： C07D477/20
摘要： Carbapenem compounds of formula I and their pharmaceutically acceptable salts and esters are provided: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, p, q and r are as defined herein, which are useful as antibacterial agents.
摘要翻译：提供式I的碳青霉烯化合物及其药学上可接受的盐和酯：其中R，R 1，R 2，R 3，p，q和r如本文所定义，其可用作抗菌剂。

4. 发明授权

US5550121A Aminoalkylpyrrolidinylthiocarbapenem derivatives 失效
标题翻译：氨基烷基吡咯烷基硫代碳青霉烯衍生物
公开(公告)号：US5550121A
公开(公告)日：1996-08-27
申请号：US312619
申请日：1994-09-27
申请人： Susumu Nakagawa , Shinji Kato , Satoshi Murase , Osamu Okamoto , Ryuji Mitomo , Katsumi Yamamoto , Koji Yamada , Hiroshi Fukatsu
发明人： Susumu Nakagawa , Shinji Kato , Satoshi Murase , Osamu Okamoto , Ryuji Mitomo , Katsumi Yamamoto , Koji Yamada , Hiroshi Fukatsu
IPC分类号： C07D207/12 , C07D477/20 , C07D487/04 , A61K31/40
CPC分类号： C07D477/20 , C07D207/12
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a methyl group, R.sup.2 is a hydrogen atom or a negative charge, R.sup.3 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkoxy group, a lower alkanoyloxy group, an amino group, an N-lower alkylamino group, an N,N-di-lower alkylamino group, a lower alkanoylamino group, an aroylamino group, a (lower alkylsulfonyl)amino group, a sulfamoylamino group, a cyano group, a nitro group, a group of --COOR.sup.4 (wherein R.sup.4 is a hydrogen atom or a lower alkyl group) or a group of --CON(R.sup.5)R.sup.6 (wherein each of R.sup.5 and R.sup.6 which may be the same or different, is a hydrogen atom or a lower alkyl group, or R.sup.5 and R.sup.6 form together with the adjacent nitrogen atom a heterocyclic group selected from the group consisting of an aziridinyl group, an azetidinyl group, a pyrrolidinyl group, a piperidyl group, a piperazinyl group, a 4-lower alkyl piperazinyl group and a morpholino group), A is a linear or branched lower alkylene group, X is a group of --N(R.sup.7)R.sup.8 (wherein each of R.sup.7 and R.sup.8 which may be the same or different, is a hydrogen atom or a lower alkyl group) or a group of --N.sup.+ (R.sup.9)(R.sup.10)R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 which may be the same or different, is a lower alkyl group), provided that when A is a linear lower alkylene group, R.sup.3 is other than a hydrogen atom; or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：下式的化合物：其中R1是氢原子或甲基，R2是氢原子或负电荷，R3是氢原子，卤素原子，羟基，低级烷氧基低级烷酰氧基，氨基，N-低级烷基氨基，N，N-二低级烷基氨基，低级烷酰基氨基，芳酰氨基，（低级烷基磺酰基）氨基，氨磺酰氨基，氰基，硝基，-COOR 4（其中R 4是氢原子或低级烷基）或-CON（R 5）R 6（其中R 5和R 6可以相同或不同）的基团是氢原子或低级烷基，或者R 5和R 6与相邻的氮原子一起形成选自氮丙啶基，氮杂环丁烷基，吡咯烷基，哌啶基，哌嗪基的杂环基，4-低级烷基哌嗪基和吗啉代基），A为直链或支链低级亚烷基，X为杂环 -N（R 7）R 8（其中可以相同或不同的R7和R8各自为氢原子或低级烷基）或-N +（R 9）（R 10）R 11（其中每个 R 9，R 10和R 11可以相同或不同，为低级烷基），条件是当A为直链低级亚烷基时，R 3不是氢原子; 或其药学上可接受的盐或酯。

5. 发明授权

US5449672A Alkylaminoalkylpyrrolidinylthiocarbapenem derivatives 失效
标题翻译：烷基氨基烷基吡咯烷基硫代碳青霉烯衍生物
公开(公告)号：US5449672A
公开(公告)日：1995-09-12
申请号：US289547
申请日：1994-08-12
申请人： Susumu Nakagawa , Shinji Kato , Satoshi Murase , Osamu Okamoto , Ryuji Mitomo , Katsumi Yamamoto , Koji Yamada , Hiroshi Fukatsu
发明人： Susumu Nakagawa , Shinji Kato , Satoshi Murase , Osamu Okamoto , Ryuji Mitomo , Katsumi Yamamoto , Koji Yamada , Hiroshi Fukatsu
IPC分类号： A61K31/40 , A61K31/397 , A61P31/04 , C07D477/00 , C07D477/20 , C07D487/04
CPC分类号： C07D477/20 , Y02P20/55
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a methyl group, R.sup.2 is a hydrogen atom or a negative charge, X is a group of --N(R.sup.3)R.sup.4 (wherein R.sup.3 is a lower alkyl group, and R.sup.4 is a hydrogen atom or a lower alkyl group) or a group of --N.sup.+ (R.sup.5)(R.sup.6)R.sup.7 (wherein each of R.sup.5, R.sup.6 and R.sup.7 which may be the same or different, is a lower alkyl group), and n is an integer of from 2 to 4; or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：下式的化合物：其中R1是氢原子或甲基，R2是氢原子或负电荷，X是-N（R3）R4（其中R3是低级）烷基，R4为氢原子或低级烷基）或-N +（R5）（R6）R7（其中可相同或不同的R5，R6和R7各自为低级烷基）），n为2〜4的整数。或其药学上可接受的盐或酯。

6. 发明授权

US5707987A Carbapenem derivatives 失效
标题翻译：卡巴培南衍生物
公开(公告)号：US5707987A
公开(公告)日：1998-01-13
申请号：US696910
申请日：1996-08-23
申请人： Susumu Nakagawa , Hiroshi Fukatsu , Ryosuke Ushijima
发明人： Susumu Nakagawa , Hiroshi Fukatsu , Ryosuke Ushijima
IPC分类号： A61K31/407 , A61K31/695 , A61P31/04 , C07D477/20 , C07D519/06 , C07F7/10 , A61K31/40 , C07D487/04
CPC分类号： C07D477/20
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl group, R.sup.2 is a hydrogen atom or a negative charge, R.sup.3 is a hydrogen atom or a lower alkyl group, Ar is a phenyl group, a naphthyl group or a group of: ##STR2## (wherein each of A.sub.4 and A.sub.5 is a single bond, --NHSO.sub.2 -- or the like, and Het is a pyrrolinyl group, a 1,4-diazabicyclo�2.2.2!octanyl group or the like which may be substituted with a hydroxyl group, a carbamoyl lower alkyl group or the like) which may be substituted with a lower alkyl group, a lower alkylsulfamoyl group or the like which may be substituted with a hydroxyl group, a di-lower alkylsulfonyl group or the like; a hydroxyl group; a di-lower alkylsulfamoyl group or the like, each of A.sub.1, A.sub.2 and A.sub.3 is a single bond or a lower alkylene group which may be substituted with a lower alkyl group, a lower alkylsulfamoyl group or the like which may be substituted with a hydroxyl group, a di-lower alkylsulfamoyl group or the like; a pyridyl group or a pyridino group; and W is a sulfur atom, a single bond; or a pharmaceutically acceptable salt or ester; a process for its production and an antibacterial agent containing it as an active ingredient.
摘要翻译： PCT No.PCT / JP95 / 00280 Sec。 371日期：1996年8月23日 102（e）日期1996年8月23日PCT提交1995年2月24日PCT公布。公开号WO95 / 23150 PCT 日期：1995年8月31日具有下式的化合物：其中R 1为氢原子或低级烷基，R 2为氢原子或负电荷，R 3为氢原子或低级烷基， Ar是苯基，萘基或基团，-NHSO 2 - 等，Het是可被取代的吡咯啉基，1,4-二氮杂双环[2.2.2]辛烷基等可以被可被羟基，二低级烷基磺酰基等取代的低级烷基，低级烷基氨磺酰基等取代的羟基，氨基甲酰基低级烷基等）。羟基; 二低级烷基氨磺酰基等，A1，A2和A3各自为可以被羟基取代的低级烷基，低级烷基氨磺酰基等取代的单键或低级亚烷基基，二低级烷基氨磺酰基等; 吡啶基或吡啶基; W是硫原子，单键; 或药学上可接受的盐或酯; 其生产方法和含有它作为活性成分的抗菌剂。

7. 发明授权

US4918070A Cephalosporin derivatives and antibacterial agents 失效
标题翻译：头孢菌素衍生物和抗菌剂
公开(公告)号：US4918070A
公开(公告)日：1990-04-17
申请号：US161100
申请日：1988-02-26
申请人： Susumu Nakagawa , Hiroshi Fukatsu , Yoshiaki Katoh , Satoshi Murase
发明人： Susumu Nakagawa , Hiroshi Fukatsu , Yoshiaki Katoh , Satoshi Murase
IPC分类号： A61K31/545 , C07D501/26 , C07D501/59
CPC分类号： C07D501/59
摘要： A cephalosporin derivative having the formula: ##STR1## wherein R.sup.1 is a substituted amino group, X is an alkylene group, R.sup.2 is an aryl or heterocyclic group which may be substituted and R.sup.3 is a hydrogen atom, a negative charge or a residue of an ester which can form a pharmaceutically acceptable ester hydrolyzable in a living body; or a pharmaceutically acceptable salt thereof.

8. 发明授权

US5049665A Cephalosporin derivatives 失效
公开(公告)号：US5049665A
公开(公告)日：1991-09-17
申请号：US414389
申请日：1989-09-29
申请人： Susumu Nakagawa , Hiroshi Fukatsu , Yoshiaki Katoh , Satoshi Murase
发明人： Susumu Nakagawa , Hiroshi Fukatsu , Yoshiaki Katoh , Satoshi Murase
IPC分类号： A61K31/545 , C07D501/26 , C07D501/59
CPC分类号： C07D501/59
摘要： A cephalosporin derivative having the formula: ##STR1## wherein R.sup.1 is a substituted amino group, X is an alkylene group, R.sup.2 is an aryl or heterocyclic group which may be substituted and R.sup.3 is a hydrogen atom, a negative charge or a residue of an ester which can form a pharmaceutically acceptable ester hydrolyzable in a living body; or a pharmaceutically acceptable salt thereof.

9. 发明授权

US5100888A Cyclic amidinylthiocarbapenem derivatives 失效
标题翻译：环丙氨基噻吩衍生物
公开(公告)号：US5100888A
公开(公告)日：1992-03-31
申请号：US549574
申请日：1990-07-06
申请人： Susumu Nakagawa , Yoshiaki Kato , Hiroshi Fukatsu
发明人： Susumu Nakagawa , Yoshiaki Kato , Hiroshi Fukatsu
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61P31/04 , C07D207/24 , C07D477/20
CPC分类号： C07D477/20 , C07D207/24 , Y02P20/55
摘要： A compound represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a methyl group; R.sup.2 and R.sup.3, which may be the same or different, each represents a hydrogen atom or a lower alkyl group; and R.sup.4 represents a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a di-lower alkylcarbamoyl group, or a carbonyl group substituted with a heterocyclic group selected from the group consisting of an aziridinyl group, an azetidinyl group, a pyrrolidinyl group, a piperidino group, a morpholino group, a thio-morpholino group, a piperazinyl group, and a 4-lower alkyl-1-piperazinyl group, or a pharmaceutically acceptable salt or ester thereof. The compound of formula (I) and their salts or esters exhibit excellent antibacterial activity.

10. 发明授权

US5258509A Process for producing 2-carbon-substituted carbapenem derivatives 失效
标题翻译：制备2-碳取代的碳代青霉烯衍生物的方法
公开(公告)号：US5258509A
公开(公告)日：1993-11-02
申请号：US989150
申请日：1992-12-11
申请人： Susumu Nakagawa , Yoshiaki Kato , Hiroshi Fukatsu
发明人： Susumu Nakagawa , Yoshiaki Kato , Hiroshi Fukatsu
IPC分类号： C07D477/02 , C07D477/14 , C07D487/04
CPC分类号： C07D477/14 , C07D477/02
摘要： A process for producing a 2-(unsubstituted or carbon-substituted)-1-carbapen-2-em-3-carboxylic acid derivative, which comprises reacting a 2-trifluoromethanesulfonyloxy-1-carbapen-2-em-3-carboxylic acid derivative or the 1-carbapen-2-em-3-carboxylic acid derivative derived from a 2-oxo-1-carbapenam-3-carboxylic acid derivative and trifluoromethanesulfonic anhydride, and a stannane derivative in an inert solvent in the presence of a palladium compound and a salt.
摘要翻译： 2-（未取代或碳取代的）-1-碳代青霉-2-烯-3-羧酸衍生物的制备方法，其包括使2-三氟甲磺酰氧基-1-碳代青霉-2-烯-3-羧酸衍生物或衍生自2-氧代-1-碳青霉烯-3-羧酸衍生物的1-碳代青霉-2-烯-3-羧酸衍生物和三氟甲磺酸酐，以及在惰性溶剂中在钯化合物存在下的锡烷衍生物和盐。

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