公开(公告)号：US4743609A

公开(公告)日：1988-05-10

申请号：US827898

申请日：1986-02-10

申请人： Masaaki Hosoi ,  Fumio Nakano ,  Kenji Matsuyama ,  Hiroshi Takeshita ,  Kenji Niiyama ,  Susumu Nakagawa

发明人： Masaaki Hosoi ,  Fumio Nakano ,  Kenji Matsuyama ,  Hiroshi Takeshita ,  Kenji Niiyama ,  Susumu Nakagawa

IPC分类号： C07D401/12 ,  C07D401/14 ,  A61K31/405

CPC分类号： C07D401/12 ,  C07D401/14

摘要： This invention provides a class of new indole derivatives which are useful as medicinal compounds having a mild inhibitory effect on the gastric acid secretion as well as a remarkably cytoprotective effects on gastric muscosa, and which are represented by the general formula: ##STR1##

摘要翻译： 本发明提供了一类新的吲哚衍生物，其可用作对胃酸分泌具有温和抑制作用的药物化合物以及对胃肌肉的显着的细胞保护作用，其通过以下通式表示：

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。

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。

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.

公开(公告)号：US5095013A

公开(公告)日：1992-03-10

申请号：US562564

申请日：1990-08-03

申请人： Susumu Nakagawa ,  Fumio Nakano ,  Norikazu Otake ,  Ryosuke Ushijima

发明人： Susumu Nakagawa ,  Fumio Nakano ,  Norikazu Otake ,  Ryosuke Ushijima

IPC分类号： C07D477/00 ,  A61K31/397 ,  A61K31/40 ,  A61P31/04 ,  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 lower alkyl group, each of R.sup.3, R.sup.4 and R.sup.5 is a hydrogen atom or a lower alkyl group, or R.sup.3 and R.sup.4 together form a methylene group, an ethylene group or a propylene group, or R.sup.4 and R.sup.5 form together with the adjacent nitrogen atom an aziridinyl group, an azetidinyl group, a pyrrolidinyl group, a piperidino group, a piperazinyl group or a morpholino group; or a pharmaceutically acceptable salt or ester thereof.

公开(公告)号：US5084453A

公开(公告)日：1992-01-28

申请号：US265458

申请日：1988-10-13

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： A61K31/545 ,  C07D235/28 ,  C07D263/46 ,  C07D263/58 ,  C07D271/10 ,  C07D271/113 ,  C07D277/20 ,  C07D277/36 ,  C07D277/40 ,  C07D277/56 ,  C07D285/12 ,  C07D285/125 ,  C07D501/22 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46

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 carbamoyl 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.

公开(公告)号：US4883868A

公开(公告)日：1989-11-28

申请号：US64462

申请日：1987-06-22

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： A compound having the formula: ##STR1## wherein R.sup.1 is an amino group or a protected amino group, R.sup.2 is a hydrogen atom or a protecting group for a hydroxyl group, R.sup.3 represents negative charge, a hydrogen atom or a protecting group for a carboxyl group, and n is 0 or 1, and a salt thereof.

摘要翻译： 具有下式的化合物：其中R1是氨基或被保护的氨基，R2是氢原子或羟基的保护基，R3代表负电荷，氢原子或保护基 羧基，n为0或1，及其盐。

公开(公告)号：US5061794A

公开(公告)日：1991-10-29

申请号：US377086

申请日：1989-07-10

申请人： Susumu Nakagawa ,  Koji Yamada ,  Fumio Nakano ,  Norikazu Otake ,  Akira Asai ,  Satoru Kuroyanagi ,  Yoshiharu Tanaka ,  Moriaki Ishikawa ,  Ryosuke Ushijima ,  Ryuji Mitomo

发明人： Susumu Nakagawa ,  Koji Yamada ,  Fumio Nakano ,  Norikazu Otake ,  Akira Asai ,  Satoru Kuroyanagi ,  Yoshiharu Tanaka ,  Moriaki Ishikawa ,  Ryosuke Ushijima ,  Ryuji Mitomo

IPC分类号： C07D235/28 ,  C07D263/46 ,  C07D263/58 ,  C07D271/10 ,  C07D271/113 ,  C07D277/20 ,  C07D277/36 ,  C07D277/56 ,  C07D285/12 ,  C07D285/125 ,  C07D501/36

CPC分类号： C07D263/58 ,  C07D235/28 ,  C07D263/46 ,  C07D271/113 ,  C07D277/36 ,  C07D277/56 ,  C07D277/587 ,  C07D285/125

摘要： A compound having the formula: ##STR1## wherein R is a straight chain or branched chain lower alkyl, cyclic lower alkyl, lower alkenyl (except for 1-carboxy-1-vinyl), lower alkynyl, aralkyl, phenyl or 2-pyrrolidon-3-yl group which may be substituted, and Q is ##STR2## (wherein R.sup.1 is a hydrogen atom or an acetyl group, R.sup.2 is a hydrogen atom, a carboxyl group or a carboxymethyl group, Y is a sulfur atom or an oxygen atom, Z is a sulfur atom, an oxygen atom or an imino group which may be substituted by a lower alkyl group); or a pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.

摘要翻译： 具有下式的化合物：其中R是直链或支链的低级烷基，环状低级烷基，低级烯基（1-羧基-1-乙烯基），低级炔基，芳烷基，苯基或2 可以被取代的吡咯烷酮-3-基，Q是氢原子或乙酰基，R2是氢原子，羧基或羧甲基， Y是硫原子或氧原子，Z是硫原子，氧原子或可被低级烷基取代的亚氨基）; 或其药学上可接受的盐，生理上可水解的酯或其溶剂合物。

公开(公告)号：US4677100A

公开(公告)日：1987-06-30

申请号：US813614

申请日：1985-12-26

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 ,  C07D209/08 ,  C07D209/44 ,  C07D277/28 ,  C07D417/14 ,  C07D501/00 ,  C07D501/04 ,  C07D501/38 ,  C07D501/46 ,  C07D501/56

CPC分类号： C07D501/46 ,  C07D209/44

摘要： A compound having the formula: ##STR1## wherein R.sup.1 is a straight chain, branched chain or cyclic lower alkyl group which may be substituted by a carboxyl group, and each of R.sup.2 and R.sup.3 which may be the same or different, is a hydrogen atom, a hydroxyl group, a methoxy group or an acetoxy group, and R.sup.4 is a hydroxyl group, a methoxy group or an acetoxy group; or a pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.

摘要翻译： 具有下式的化合物：其中R 1是可以被羧基取代的直链，支链或环状低级烷基，R 2和R 3可以相同或相同， 不同的是氢原子，羟基，甲氧基或乙酰氧基，R4是羟基，甲氧基或乙酰氧基; 或其药学上可接受的盐，生理上可水解的酯或其溶剂合物。

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。