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1. 发明授权

US4958029A Process for the production of isoindoline derivatives, novel intermediates and process for their production 失效
标题翻译：生产异二氢吲哚衍生物的方法，新型中间体及其生产方法
公开(公告)号：US4958029A
公开(公告)日：1990-09-18
申请号：US140996
申请日：1988-01-05
申请人： Susumu Nakagawa , Satoshi Murase , Ryosuke Ushijima , Yoshiaki Kato
发明人： Susumu Nakagawa , Satoshi Murase , Ryosuke Ushijima , Yoshiaki Kato
IPC分类号： C07D209/44
CPC分类号： C07D209/44 , Y02P20/55
摘要： A process for producing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group or an aralkyl group, and R.sup.2 is a hydrogen atom or a hydroxyl-protecting group, or a salt thereof, which comprises removing from a compound of the formula: ##STR2## wherein R.sup.3 is a hydrogen atom or a hydroxyl-protecting group, R.sup.4 and R.sup.5 which may be the same or different are N-protecting groups selected from the group consisting of lower alkyl groups and aralkyl groups, and X.sup..crclbar. is an anion, the N-protecting group(s), if necessary, together with the hydroxyl-protecting group.

2. 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。

3. 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。

4. 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。

5. 发明授权

US5112818A 2-(2-cyclopropylpyrrolidin-4-ylthio)carbapenhem derivatives 失效
标题翻译： 2-（2-环丙基吡咯烷-4-基）乙酰胺衍生物
公开(公告)号：US5112818A
公开(公告)日：1992-05-12
申请号：US635218
申请日：1990-12-28
申请人： Susumu Nakagawa , Koji Yamada , Ryosuke Ushijima
发明人： Susumu Nakagawa , Koji Yamada , Ryosuke Ushijima
IPC分类号： C07D477/20
CPC分类号： C07D477/20
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a methyl group, each of R.sup.2 and R.sup.3 which may be the same or different, is a hydrogen atom or a lower alkyl group, or R.sup.2 and R.sup.3 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 piperidino group, a piperazinyl group and a morpholino group, A is a carbonyl group or a single bond, and n is an integer of from 0 to 3; or a pharmaceutically acceptable salt or ester thereof.

6. 发明授权

US5068322A Crystalline cephalosporin compounds 失效
标题翻译：晶体环磷酰胺化合物
公开(公告)号：US5068322A
公开(公告)日：1991-11-26
申请号：US522817
申请日：1990-05-14
申请人： Susumu Nakagawa , Ryosuke Ushijima , Fumio Nakano , Koji Yamada , Eiichi Mano
发明人： Susumu Nakagawa , Ryosuke Ushijima , Fumio Nakano , Koji Yamada , Eiichi Mano
IPC分类号： A61K31/545 , C07D501/46
CPC分类号： C07D501/46 , C07D501/18 , C07D501/38 , Y02P20/55
摘要： The present invention relates to stable crystalline (6R,7R)-7-(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxylimino)acetamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)methyl-3-cephem-4-carboxylate sulfate or its hydrate, a process for production of the compound and (6R,7R)-7-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)methyl-3-cephem-4-carboxylate hydrochloride or its hydrate which is a starting material useful for the production of the desired compound of the present invention.

7. 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。

8. 发明授权

US4959469A Crystalline cephalosporin compounds 失效
标题翻译：结晶头孢菌素化合物
公开(公告)号：US4959469A
公开(公告)日：1990-09-25
申请号：US315917
申请日：1989-02-27
申请人： Susumu Nakagawa , Ryosuke Ushijima , Fumio Nakano , Koji Yamada , Eiichi Mano
发明人： Susumu Nakagawa , Ryosuke Ushijima , Fumio Nakano , Koji Yamada , Eiichi Mano
IPC分类号： A61K31/545 , C07D501/46
CPC分类号： C07D501/46 , A61K31/545 , C07D501/18 , C07D501/38
摘要： The present invention relates to stable cyrstalline (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)-3-cephem-4-carboxylate sulfate or its hydrate, a process for production of the compound and (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxyl-1-methylethoxyimino)acetamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)methyl-3-cephem-4-carboxylate hydrochloride or its hydrate which is a starting material useful for the production of the desired compound of the present invention.
摘要翻译：本发明涉及稳定的cyrstalline（6R，7R）-7 - [（Z）-2-（2-氨基噻唑-4-基）-2-（1-羧基-1-甲基乙氧基亚氨基）乙酰氨基] -3-（ 5,6-二羟基-2-甲基-2-异二氢吲哚鎓）-3-头孢烯-4-羧酸甲酯硫酸盐或其水合物，该化合物的制备方法和（6R，7R）-7 - [（Z）-2 - （2-氨基噻唑-4-基）-2-（1-羧基-1-甲基乙氧基亚胺）乙酰胺基] -3-（5,6-二羟基-2-甲基-2-异二氢吲哚鎓）甲基-3-环丙基 - 4-羧酸盐酸盐或其水合物，其为可用于制备本发明所需化合物的原料。

9. 发明授权

US5225406A 1-carboxy-1-vinyloxyimino aminothiazole cephalosporin derivatives 失效
标题翻译： 1-羧基-1-乙烯氧基亚氨基氨基噻唑头孢菌素衍生物
公开(公告)号：US5225406A
公开(公告)日：1993-07-06
申请号：US753943
申请日：1991-09-03
申请人： Susumu Nakagawa , Ryuji Mitomo , Koji Yamada , Norikazu Otake , Fumio Nakano , Akira Asai , Satoru Kuroyanagi , Yoshiharu Tanaka , Moriaki Ishikawa , Ryosuke Ushijima
发明人： Susumu Nakagawa , Ryuji Mitomo , Koji Yamada , Norikazu Otake , Fumio Nakano , Akira Asai , Satoru Kuroyanagi , Yoshiharu Tanaka , Moriaki Ishikawa , Ryosuke Ushijima
IPC分类号： C07D235/28 , C07D263/46 , C07D263/58 , C07D271/10 , C07D271/113 , C07D277/20 , C07D277/36 , C07D277/56 , C07D285/12 , C07D285/125 , C07D501/20 , C07D501/36 , C07D501/46 , C07D501/59
CPC分类号： C07D263/58 , C07D235/28 , C07D263/46 , C07D271/113 , C07D277/36 , C07D277/56 , C07D277/587 , C07D285/125 , Y02P20/55
摘要： The present invention relates to a compound having the formula: ##STR1## wherein R is a hydrogen atom, a carboxyl-protecting group or a negative charge and Q is a hydrogen atom, a halogen atom, a hydroxyl group, an acetoxy group, a carbamoyloxy group, an azide group, a substituted or unsubstituted quarternary ammonio group or a substituted or unsubstituted heterocyclic thio group having at least one hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom, or a non-toxic salt or physiologically hydrolyzable non-toxic ester thereof; a process for producing it; and an antibacterial agent comprising it as an active ingredient.Further, the present invention also relates to a compound having the formula: ##STR2## wherein R.sup.3 is a hydrogen atom or an amino-protecting group, and each of R.sup.4 and R.sup.5 which may be the same or different is a hydrogen atom or a carboxyl-protecting group, or a salt thereof; and a process for producing it.
摘要翻译：本发明涉及具有下式的化合物：其中R是氢原子，羧基保护基或负电荷，Q是氢原子，卤原子，羟基，乙酰氧基基团，氨基甲酰氧基，叠氮基，取代或未取代的季铵基或具有至少一个选自氮原子，氧原子和硫原子的杂原子的取代或未取代的杂环硫基，或其无毒盐或其生理上可水解的无毒酯; 一个生产过程; 和含有它作为活性成分的抗菌剂。此外，本发明还涉及具有下式的化合物：其中R 3是氢原子或氨基保护基，并且R 4和R 5可以相同或不同的是氢原子或羧基保护基，或其盐; 及其生产工艺。

10. 发明授权

US4988687A 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：US4988687A
公开(公告)日：1991-01-29
申请号：US401747
申请日：1989-09-01
申请人： Susumu Nakagawa , Ryuji Mitomo , Ryosuke Ushijima
发明人： Susumu Nakagawa , Ryuji Mitomo , Ryosuke Ushijima
IPC分类号： C07D501/00 , C07D501/36
CPC分类号： C07D501/00
摘要： A compound having the formula: ##STR1## wherein R is a vinyl, phenyl or aralkyl group which may be substituted; or a pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.

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