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1. 发明授权

US4608373A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4608373A
公开(公告)日：1986-08-26
申请号：US560412
申请日：1983-12-12
申请人： Tadao Shibanuma , Kohji Nakano , Noriaki Nagano , Yukiyasu Murakami , Ryuichiro Hara
发明人： Tadao Shibanuma , Kohji Nakano , Noriaki Nagano , Yukiyasu Murakami , Ryuichiro Hara
IPC分类号： C07D277/20 , C07D277/42 , C07D417/12 , C07D501/16 , C07D501/20 , C07D501/22 , C07D501/36 , C07D501/46 , C07D501/59 , C07D501/34 , A61K31/545
CPC分类号： C07D277/587 , C07D277/42 , C07D417/12
摘要： Novel cephem compounds are provided having the formula: ##STR1## wherein R represents lower alkyl, which may be substituted with lower acyloxy, lower alkylthio or certain 5 or 6-membered heterocyclic ring-containing groups. The cephem compounds and salts thereof exhibit antibacterial activity to many pathogens. A process for producing the cephem compounds is also provided.
摘要翻译：提供具有下式的新型头孢烯化合物：其中R代表低级烷基，其可以被低级酰氧基，低级烷硫基或某些含有5或6元杂环基团取代。头孢烯化合物及其盐对许多病原体表现出抗菌活性。还提供了产生头孢烯化合物的方法。

2. 发明授权

US3985758A 1,4-Dihydropyridine derivatives 失效
标题翻译： 1,4-二氢吡啶衍生物
公开(公告)号：US3985758A
公开(公告)日：1976-10-12
申请号：US584268
申请日：1975-06-06
申请人： Masuo Murakami , Kozo Takahashi , Masaru Iwanami , Masaharu Fujimoto , Tadao Shibanuma , Ryutaro Kawai , Toichi Takenaka
发明人： Masuo Murakami , Kozo Takahashi , Masaru Iwanami , Masaharu Fujimoto , Tadao Shibanuma , Ryutaro Kawai , Toichi Takenaka
IPC分类号： C07D211/90 , C07D213/55
CPC分类号： C07D211/90 , Y10S514/929
摘要： There are provided novel 1,4-dihydropyridine derivatives, particularly 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-.beta.-(N-benzyl-N-methylamino)ethyl ester and 5-methyl ester. The 1,4-dihydropyridine derivatives are characterized by cerebral vascular dilator activity.
摘要翻译：提供新的1,4-二氢吡啶衍生物，特别是2,6-二甲基-4-（3'-硝基苯基）-1,4-二氢吡啶-3,5-二羧酸3-β-（N-苄基-N- 甲基氨基）乙酯和5-甲酯。 1,4-二氢吡啶衍生物的特征在于脑血管扩张剂活性。

3. 发明授权

US4068074A Cephalosporin derivatives having at the 3-position of the cephem ring a heterocyclic thiomethyl group with a carboxy or sulfo group and at the 7-position of the cephem ring an .alpha.-heterocylic acylaminophenyl-acetamide group 失效
标题翻译：头孢菌素衍生物在头孢烯的3位具有羧基或磺基的杂环硫代甲基，并且在头孢烯环的7-位具有{60-环己基酰氨基苯基 - 乙酰胺基
公开(公告)号：US4068074A
公开(公告)日：1978-01-10
申请号：US695085
申请日：1976-06-11
申请人： Masuo Murakami , Ichiro Isaka , Norio Kawahara , Masaru Iwanami , Masaharu Fujimoto , Tetsuya Maeda , Tadao Shibanuma , Yoshinobu Nagano
发明人： Masuo Murakami , Ichiro Isaka , Norio Kawahara , Masaru Iwanami , Masaharu Fujimoto , Tetsuya Maeda , Tadao Shibanuma , Yoshinobu Nagano
IPC分类号： C07D501/36
CPC分类号： C07D501/36
摘要： A novel cephalosporin derivative having at the 3-position of the cephem ring a heterocyclic thiomethyl group having a carboxy group or a sulfo group and at the 7-position of the cephem ring, an .alpha.-heterocyclic acylaminophenylacetamide group. The compounds of this invention have excellent antibacterial activity against Pseudomonas and Proteus strains of bacteria.
摘要翻译：在头孢烯环的3位具有羧基或磺基的杂环硫甲基和头孢烯环的7-位的新型头孢菌素衍生物为α-杂环酰氨基苯基乙酰胺基。本发明的化合物对细菌的假单胞菌和变形菌菌株具有优异的抗菌活性。

4. 发明授权

US3951962A Novel N-alkenyltetracycline derivatives 失效
标题翻译：新型N-烯基四环素衍生物
公开(公告)号：US3951962A
公开(公告)日：1976-04-20
申请号：US560110
申请日：1975-03-19
申请人： Masuo Murakami , Masaru Iwanami , Tadao Shibanuma , Masaharu Fujimoto , Norio Sato , Ryutaro Kawai , Kuniichiro Yano
发明人： Masuo Murakami , Masaru Iwanami , Tadao Shibanuma , Masaharu Fujimoto , Norio Sato , Ryutaro Kawai , Kuniichiro Yano
IPC分类号： C07C233/00 , C07D307/02 , C07C103/19
CPC分类号： C07C233/00
摘要： N-alkenyltetracycline derivatives, for example, N-[1-methyl-2(2-thienyl)-1-butenyl]tetracycline represented by the formula ##SPC1##The compounds have excellent antibacterial action as compared with tetracycline.
摘要翻译： N-烯基四环素衍生物，例如由式表示的N- [1-甲基-2（2-噻吩基）-1-丁烯基]四环素与四环素相比，该化合物具有优异的抗菌作用。

5. 发明授权

US4414153A 1,3-Dithietane-2-carboxylic acid penicillin and cephalosporin derivatives 失效
标题翻译： 1,3-二硫戊环-2-羧酸青霉素和头孢菌素衍生物
公开(公告)号：US4414153A
公开(公告)日：1983-11-08
申请号：US304986
申请日：1981-09-23
申请人： Masaru Iwanami , Tetsuya Maeda , Yoshinobu Nagano , Masaharu Fujimoto , Noriaki Nagano , Atsuki Yamazaki , Kazaharu Tamazawa , Kiyoshi Murase , Tadao Shibanuma
发明人： Masaru Iwanami , Tetsuya Maeda , Yoshinobu Nagano , Masaharu Fujimoto , Noriaki Nagano , Atsuki Yamazaki , Kazaharu Tamazawa , Kiyoshi Murase , Tadao Shibanuma
IPC分类号： C07D339/00 , C07D499/76 , C07D501/06 , C07D501/20 , C07D501/36 , C07D501/57
CPC分类号： C07D339/00
摘要： Substituted 1,3-dithietane-2-carboxylic acid derivatives useful as intermediates for the preparation of highly effective penicillin and cephalosporin derivatives and the preparation thereof.
摘要翻译：用作制备高效青霉素和头孢菌素衍生物的中间体的1,3-二硫戊环-2-羧酸衍生物及其制备方法。

6. 发明授权

US4198339A 1,3-Dithietane-2-carboxylic acids and the preparation thereof 失效
标题翻译： 1,3-二噻吩-2-羧酸及其制备
公开(公告)号：US4198339A
公开(公告)日：1980-04-15
申请号：US913501
申请日：1978-06-07
申请人： Masaru Iwanami , Tetsuya Maeda , Yoshinobu Nagano , Masaharu Fujimoto , Noriaki Nagano , Atsuki Yamazaki , Kazaharu Tamazawa , Kiyoshi Murase , Tadao Shibanuma
发明人： Masaru Iwanami , Tetsuya Maeda , Yoshinobu Nagano , Masaharu Fujimoto , Noriaki Nagano , Atsuki Yamazaki , Kazaharu Tamazawa , Kiyoshi Murase , Tadao Shibanuma
IPC分类号： C07D339/00 , C07D499/76 , C07D501/06 , C07D501/20 , C07D501/36 , C07D501/57 , C07D333/38
CPC分类号： C07D339/00
摘要： Substituted 1,3-dithietane-2-carboxylic acid derivatives useful as intermediates for the preparation of highly effective penicillin and cephalosporin derivatives and the preparation thereof.
摘要翻译：用作制备高效青霉素和头孢菌素衍生物的中间体的1,3-二硫戊环-2-羧酸衍生物及其制备。

7. 发明授权

US3991111A N-alkenyltetracycline derivatives 失效
标题翻译： N-烯基四环素衍生物
公开(公告)号：US3991111A
公开(公告)日：1976-11-09
申请号：US574865
申请日：1975-05-06
申请人： Masuo Murakami , Masaru Iwanami , Tadao Shibanuma , Masaharu Fujimoto , Norio Sato , Ryutaro Kawai , Kuniichiro Yano
发明人： Masuo Murakami , Masaru Iwanami , Tadao Shibanuma , Masaharu Fujimoto , Norio Sato , Ryutaro Kawai , Kuniichiro Yano
IPC分类号： C07C233/00 , C07C103/19
CPC分类号： C07C233/00
摘要： N-alkenyltetracycline derivatives, for example, N-(1-methyl-2-.alpha.-naphthylethenyl)tetracycline represented by the formula ##SPC1##The compounds have excellent antibacterial action as compared with tetracycline.
摘要翻译： N-烯基四环素衍生物，例如由式表示的N-（1-甲基-2-甲酰基 - 乙烯基）四环素与四环素相比，该化合物具有优异的抗菌作用。

8. 发明授权

US5081116A Cephalosporin derivatives 失效
公开(公告)号：US5081116A
公开(公告)日：1992-01-14
申请号：US504926
申请日：1990-04-05
申请人： Noriaki Nagano , Masato Satoh , Masauki Komiya , Toshio Okazaki , Tetsuya Maeda , Tadao Shibanuma
发明人： Noriaki Nagano , Masato Satoh , Masauki Komiya , Toshio Okazaki , Tetsuya Maeda , Tadao Shibanuma
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/24 , C07D501/36
CPC分类号： C07D501/24 , Y02P20/55
摘要： A 7-[2-(2-amino-4-thiazolyl)-2-(hydroxyimino)-acetamido]-3-(1,3-dithiolan-2-yl)-3-cephem-4-carboxylic acid derivative is provided which can be represented by the general formula: ##STR1## wherein A represents a hydrogen atom, a 1-acetoxyethyl group, a 1-cyclohexylacetoxyethyl group or a pivaloyloxy-methyl group.

9. 发明授权

US4474779A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US4474779A
公开(公告)日：1984-10-02
申请号：US433247
申请日：1982-10-07
申请人： Noriaki Nagano , Kohji Nakano , Tadao Shibanuma , Yukiyasu Murakami
发明人： Noriaki Nagano , Kohji Nakano , Tadao Shibanuma , Yukiyasu Murakami
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D501/20 , C07D501/24 , C07D501/36 , C07D501/56
CPC分类号： C07D277/587 , Y02P20/55
摘要： Cephalosporin compounds represented by the general formula ##STR1## wherein R represents a group shown by formula ##STR2## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group of 1-3 carbon atoms and R.sup.2 represents a hydrogen atom, a lower alkyl group of 1-3 carbon atoms, a phenyl group which may be substituted by an amino or hydroxy group, a cyano group, a carboxy group, or a carboxymethyl group; said R.sup.1 and R.sup.2 may form a cycloalkylidene group of 4-6 carbon atoms together with the carbon atom to which they are bonded) or a group shown by formula --CH.sub.2 --R.sup.3 (wherein R.sup.3 represents a hydrogen atom, a halogenomethyl group, a carbamoyl group, a carboxymethyl group, .alpha.4-carboxy-3-hydroxyisothiazol-5-yl-thiomethyl group, or .alpha.2-carboxyphenylthiomethyl group); R' represents a group shown by formula ##STR3## (wherein R.sub.a represents a carboxy group, a cyano group, or a carbamoyl group which may be substituted by a lower alkyl group of 1-3 carbon atoms and R.sub.b represents a hydrogen atom or an amino group) or a group shown by formula ##STR4## (wherein R.sub.a and R.sub.b have the same significance as above); and the waveline .about. shows an anti-form or syn-form bond and the salts thereof. They possess excellent antibacterial activities against gram positive bacteria and gram negative bacteria, in particular, pseudomonas aeruginosa and are useful as anti-bacterial agents.
摘要翻译：由通式表示的头孢菌素化合物（其中R表示由式表示的基团，其中R1表示氢原子或1-3个碳原子的低级烷基，R2表示氢原子，低级烷基 1-3个碳原子的苯基，可以被氨基或羟基，氰基，羧基或羧甲基取代的苯基;所述R 1和R 2可以一起形成4-6个碳原子的亚环烷基与其结合的碳原子）或式-CH 2 -R 3（其中R 3表示氢原子，卤代甲基，氨基甲酰基，羧甲基，α4-羧基-3-羟基异噻唑-5 - 基 - 硫代甲基或α2-羧基苯硫基甲基）; R'表示式IMA图示的基团（其中，Ra表示羧基，氰基或可被1-3个碳原子的低级烷基取代的氨基甲酰基，Rb表示氢原子或氨基）或由式IMA IMA表示的基团（其中Ra和Rb具有与上述相同的含义）; 并且波纹差异显示出抗形式或顺式键及其盐。它们对革兰氏阳性细菌和革兰氏阴性细菌，特别是铜绿假单胞菌具有优异的抗菌活性，可用作抗菌剂。

10. 再颁专利

USRE33778E 1,3-dithietane-2-carboxylic acid penicillin and cephalosporin derivatives 失效
公开(公告)号：USRE33778E
公开(公告)日：1991-12-24
申请号：US449114
申请日：1989-12-08
申请人： Masaru Iwanami , Tetsuya Maeda , Yoshinobu Nagano , Masaharu Fujimoto , Noriaki Nagano , Atsuki Yamazaki , Kasaharu Tamazawa , Kiyoshi Murase , Tadao Shibanuma
发明人： Masaru Iwanami , Tetsuya Maeda , Yoshinobu Nagano , Masaharu Fujimoto , Noriaki Nagano , Atsuki Yamazaki , Kasaharu Tamazawa , Kiyoshi Murase , Tadao Shibanuma
IPC分类号： C07D339/00 , C07D499/76 , C07D501/06 , C07D501/20 , C07D501/36 , C07D501/57
CPC分类号： C07D339/00
摘要： Substituted 1,3-dithietane-2-carboxylic acid derivatives useful as intermediates for the preparation of highly effective penicillin and cephalosporin derivatives and the preparation thereof.

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