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41. 发明授权

US4868295A Process for the preparation of cefodizime 失效
标题翻译：头孢地嗪的制备方法
公开(公告)号：US4868295A
公开(公告)日：1989-09-19
申请号：US936187
申请日：1986-12-01
申请人： Ottmar Jaenicke , Hans Wagner , Manfred Worm
发明人： Ottmar Jaenicke , Hans Wagner , Manfred Worm
IPC分类号： C07D501/06 , A61K20060101 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/36 , C07D501/46 , C07D501/56
CPC分类号： C07D501/36 , Y02P20/55
摘要： A process for the preparation of cefodizime of the formula ##STR1## wherein (a) a compound of the formula II (ATS) ##STR2## wherein R.sub.1 represents hydrogen or an aminoprotective group and A represents a hydrogen atom or one equivalent of an alkali metal or alkaline earth metal, of ammonium or of an organic nitrogen base, is first reacted with a compound of the formula IIIR--SO.sub.2 Hal wherein R represents an optionally substituted alkyl, aryl or aralkyl radical and Hal represents a halogen atom, in an organic solvent and, if appropriate, in the presence of a base,(b) a compound of the formula I (TACS) ##STR3## in which A has the above meaning, is reacted with a silylating agent in an organic solvent and, if appropriate, in the presence of a base, and(c) the two products formed in (a) and (b) are reacted in their reaction solutions, and any protective group R.sub.1 present in the end product of the formula I is eliminated.
摘要翻译：制备式（II）的化合物其中（a）式II（ATS）的化合物其中R 1表示氢或氨基保护基，A表示氢原子或一个首先与式IIIR-SO2Hal的化合物反应，其中R表示任选取代的烷基，芳基或芳烷基，Hal表示卤素原子在有机溶剂中，如果合适，在碱的存在下，（b）式（I）所示的化合物（TACS），其中A具有上述含义，与甲硅烷基化剂在有机溶剂中反应和（c）在（a）和（b）中形成的两种产物在其反应溶液中反应，并且存在于式I的最终产物中的任何保护基R1是消除了

42. 发明授权

US4861769A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4861769A
公开(公告)日：1989-08-29
申请号：US828527
申请日：1986-02-12
申请人： Takao Takaya , Zenzaburo Tozuka , Nobuyoshi Yasuda , Shintaro Nishimura
发明人： Takao Takaya , Zenzaburo Tozuka , Nobuyoshi Yasuda , Shintaro Nishimura
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07C67/00 , C07C239/00 , C07C251/32 , C07C251/50 , C07D277/20 , C07D277/40 , C07D277/46 , C07D285/08 , C07D317/30 , C07D501/20 , C07D501/36 , C07D501/59 , C07D521/00
CPC分类号： C07D277/587 , C07D285/08 , C07D317/30
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl, lower alkanoyl, aryl, ar(lower)alkyl or a heterocyclic group, each of which may have suitable substituent(s),R.sup.2 is carboxy or protected carboxy,R.sup.3 is hydrogen, halogen, hydroxy, lower alkoxy, acyloxy, lower alkylthio, lower alkenyl, lower alkenylthio, lower alkynyl, heterocyclicthio or a heterocyclic group, in which lower alkylthio, lower alkenyl, lower alkenylthio, heterocyclicthio and a heterocyclic group may have suitable substituent(s),R.sup.4 and R.sup.5 are each hydrogen, halogen or arylthio,A is lower alkylene, andn is an integer of 0 or 1,and a pharmaceutically acceptable salt thereof, processes for preparation thereof and pharmaceutical composition comprising the same.
摘要翻译：下式的化合物，其中R 1是低级烷基，低级烷酰基，芳基，芳（低级）烷基或杂环基，其各自可以具有合适的取代基，R 2是羧基或被保护的羧基，R 3是氢，卤素，羟基，低级烷氧基，酰氧基，低级烷硫基，低级烯基，低级链烯硫基，低级炔基，杂环硫基或杂环基，其中低级烷硫基，低级烯基，低级链烯硫基，杂环硫基和杂环基可具有合适的取代基 s）中，R 4和R 5各自为氢，卤素或芳硫基，A为低级亚烷基，n为0或1的整数，及其药学上可接受的盐，其制备方法和包含其的药物组合物。

43. 发明授权

US4841044A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4841044A
公开(公告)日：1989-06-20
申请号：US943037
申请日：1986-12-18
申请人： Yoshiaki Watanabe , Chihiro Yokoo , Masami Goi , Akira Onodera , Mitsuo Murata , Hiroshi Fukushima , Minoru Taguchi , Kaoru Sota
发明人： Yoshiaki Watanabe , Chihiro Yokoo , Masami Goi , Akira Onodera , Mitsuo Murata , Hiroshi Fukushima , Minoru Taguchi , Kaoru Sota
IPC分类号： A61K31/545 , C07D501/36 , C07D501/59
CPC分类号： C07D501/59
摘要： Cephalosporin derivatives represented by the general formula ##STR1## wherein R is a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, R' is a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 5 or 6 carbon atoms or a benzyl group, or R and R' together with the nitrogen atom to which they are attached form a tetrahydropyridinyl group, a morpholinyl group or pyrroridinyl group, and the non-toxic salts thereof are disclosed. These compounds are useful as antibacterial agents.
摘要翻译：其中R为氢原子或碳原子数为1〜4的低级烷基，R'为氢原子，碳原子数1〜4的低级烷基，，具有5或6个碳原子的环烷基或苄基，或R和R'与它们所连接的氮原子一起形成四氢吡啶基，吗啉基或吡咯烷基，其无毒盐是披露这些化合物可用作抗菌剂。

44. 发明授权

US4810702A Antibacterial agent for mammal use comprising cephalosporin derivatives as an effective ingredient 失效
标题翻译：哺乳动物用抗菌剂包括头孢菌素衍生物作为有效成分
公开(公告)号：US4810702A
公开(公告)日：1989-03-07
申请号：US131779
申请日：1987-12-11
申请人： Seiji Shibahara , Tsuneo Okonogi , Yasushi Murai , Toshiaki Kudo , Takashi Yoshida , Ken Nishihata , Shinichi Kondo
发明人： Seiji Shibahara , Tsuneo Okonogi , Yasushi Murai , Toshiaki Kudo , Takashi Yoshida , Ken Nishihata , Shinichi Kondo
IPC分类号： A61K31/435 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36
CPC分类号： C07D501/36
摘要： Cephalosporin compounds having 2-(2-aminothiazol-4-yl)-2{(1S)-carboxyethoxyimino}acetyl group on the side chain at the 7-position thereof and 1-ethylpyridinium-4-ylthiomethyl group on the side chain at the 3-position thereof or non-toxic salts thereof are excellent antibacterial agents for mammals including human. The cephalosporin derivatives have low toxicity.

45. 发明授权

US4695639A Thiazole derivatives 失效
标题翻译：噻唑衍生物
公开(公告)号：US4695639A
公开(公告)日：1987-09-22
申请号：US568921
申请日：1984-01-06
申请人： Kunio Takanohashi , Tsuneaki Yoshida , Shoichiro Fujii
发明人： Kunio Takanohashi , Tsuneaki Yoshida , Shoichiro Fujii
IPC分类号： C07D277/20 , C07D277/40 , C07D277/74 , C07D277/76 , C07D417/12 , C07D501/36
CPC分类号： C07D277/587 , C07C317/00 , C07C323/00 , C07D277/74 , C07D417/12
摘要： A novel aminothiazoleacetic acid derivative which is an advantageous synthetic intermediate for .beta.-lactam antibiotics, and its production method and use. Starting with diketene, the production method comprises the following squence of steps. ##STR1## (In the above formulas, R is lower alkyl or phenyl; R.sub.1 and R.sub.2 each are hydrogen or lower alkyl; X and X' each are halogen; W is S or SO.sub.2 ; and W' is OH or ##STR2##
摘要翻译：一种新颖的氨基噻唑乙酸衍生物，其是β-内酰胺抗生素的有利合成中间体及其制备方法和用途。从双烯酮开始，生产方法包括以下步骤。（图像） + TR （在上式中，R为低级烷基或苯基; R 1和R 2各自为氢或低级烷基; X和X'各自为卤素; W为S或SO 2; W'为OH或“IMAGE”

46. 发明授权

US4691014A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US4691014A
公开(公告)日：1987-09-01
申请号：US782567
申请日：1985-10-01
申请人： Takanobu Naito , Masaaki Yokoyama , Kazuya Sasaki , Makoto Yamamoto , Kouji Amemiya
发明人： Takanobu Naito , Masaaki Yokoyama , Kazuya Sasaki , Makoto Yamamoto , Kouji Amemiya
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D263/48 , C07D501/20 , C07D501/34 , C07D501/36 , C07D501/59 , C07D501/22
CPC分类号： C07D263/48 , Y02P20/55
摘要： A cephalosporin compound having the formula: ##STR1## wherein R.sub.1 is a hydroxy group, a lower alkanoyloxy group or a lower alkoxycarbonyloxy group, R.sub.2 is a hydrogen atom, a hydroxy group, a lower alkanoyloxy group or a lower alkoxycarbonyloxy group, R.sub.3 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkenyl group, a lower alkoxy group or --CH.sub.2 R.sub.7 (wherein R.sub.7 is a hydrogen atom, an azido group, a lower alkanoyloxy group, a carbamoyloxy group, a substituted or unsubstituted pyridinium group or a substituted or unsubstituted heterocyclic thio group), R.sub.4 is a hydrogen atom or a carboxy-protecting group, each of R.sub.5 and R.sub.6 is a hydrogen atom or a lower alkyl group, or R.sub.5 and R.sub.6 form a cycloalkylidene group together with the carbon atom to which they are attached, and m is 0 to 1, or a pharmaceutically acceptable salt thereof.
摘要翻译：具有下式的头孢菌素化合物：其中R1是羟基，低级烷酰氧基或低级烷氧基羰基氧基，R2是氢原子，羟基，低级烷酰氧基或低级烷氧羰基氧基， R3是氢原子，卤素原子，低级烷基，低级烯基，低级烷氧基或-CH2R7（其中R7是氢原子，叠氮基，低级烷酰氧基，氨基甲酰氧基，取代的或未取代的吡啶鎓基或取代或未取代的杂环硫基），R 4为氢原子或羧基保护基，R 5和R 6各自为氢原子或低级烷基，或者R 5和R 6一起形成亚环烷基与其连接的碳原子，m为0-1，或其药学上可接受的盐。

47. 发明授权

US4647556A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4647556A
公开(公告)日：1987-03-03
申请号：US471649
申请日：1983-03-03
申请人： Rudolf Lattrell , Reiner Kirrstetter , Wilfried Schwab , Walter Durckheimer , Gerhard Seibert
发明人： Rudolf Lattrell , Reiner Kirrstetter , Wilfried Schwab , Walter Durckheimer , Gerhard Seibert
IPC分类号： C07D501/36 , A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D501/34 , C07D501/46 , C07D501/38
CPC分类号： C07D277/587
摘要： The invention relates to cephem derivatives of the general formula I ##STR1## and their physiologically acceptable acid addition salts, to pharmaceutical formulations active against bacterial infections, to processes for preparing the compounds and formulations, and to the use of the compounds for combating bacterial infections.
摘要翻译：本发明涉及通式Ⅰ的头孢烯衍生物及其生理上可接受的酸加成盐，对抗细菌感染的药物制剂，制备化合物和制剂的方法，以及该化合物用于抗菌感染的用途。

48. 发明授权

US4599426A Amino thiazole compounds 失效
标题翻译：氨基噻唑化合物
公开(公告)号：US4599426A
公开(公告)日：1986-07-08
申请号：US531669
申请日：1983-09-13
申请人： Takashi Kamiya , Kunihiko Tanaka , Tsutomu Teraji , Yoshiharu Nakai
发明人： Takashi Kamiya , Kunihiko Tanaka , Tsutomu Teraji , Yoshiharu Nakai
IPC分类号： C07D501/34 , A61K31/545 , A61K31/546 , A61P31/04 , C07D209/48 , C07D213/75 , C07D277/20 , C07D277/38 , C07D277/40 , C07D277/42 , C07D277/44 , C07D277/46 , C07D277/48 , C07D417/12 , C07D501/24 , C07D501/36 , C07D521/00 , C07F9/40 , C07F9/553 , C07F9/6539 , C07F9/6561
CPC分类号： C07D209/48 , C07D213/75 , C07D277/46 , C07D277/587 , C07F9/4006 , C07F9/5537 , C07F9/65613 , Y02P20/55
摘要： The present invention relates to new 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof which have antimicrobial activities and to processes for preparation thereof, to pharmaceutical compositions comprising the same, and to a method of using the same therapeutically in the treatment of infectious diseases in humans and animals.This division relates to intermediate compounds, namely amino or amido-thiazolyl, substituted oxyimino disubstituted acetic acid of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is --CONH--R.sup.5 or --HNCO--R.sup.5,R.sup.5 is aryl or heterocyclic, either of which may be substituted, andA is lower alkylene, or a salt thereof.

49. 发明授权

US4598075A Cephalosporin compounds 失效
公开(公告)号：US4598075A
公开(公告)日：1986-07-01
申请号：US516053
申请日：1983-07-21
申请人： Toyonari Oine , Hiroshi Sugano , Yoshihisa Yamada , Totaro Yamaguchi , Satoshi Ohshima
发明人： Toyonari Oine , Hiroshi Sugano , Yoshihisa Yamada , Totaro Yamaguchi , Satoshi Ohshima
IPC分类号： C07D501/06 , A61K31/545 , A61K31/546 , A61P31/04 , C07D417/12 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/46 , C07D499/44
CPC分类号： C07D501/24 , C07D417/12 , Y02P20/55
摘要： A cephalosporin compound of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl;R.sup.2 is acetoxy or (1-methyl-1H-tetrazol-5-yl)thio, andR.sup.3 is carboxy; orR.sup.2 is a group of the formula: ##STR2## R.sup.3 is --COO.sup.- and Y is hydrogen, hydroxymethyl or carbamoyl; andn is an integer of 2 or 3,or a pharmaceutically acceptable salt thereof and processes for their preparation are disclosed. Said cephalosporin compound is useful as an antimicrobial agent.

50. 发明授权

US4585860A 7-acylamino-3-vinylcephalosporanic acid derivatives useful for treatment of infectious diseases in human beings and animals 失效
标题翻译：用于治疗人类和动物感染性疾病的7-酰基氨基-3-乙烯基头孢烷酸衍生物
公开(公告)号：US4585860A
公开(公告)日：1986-04-29
申请号：US493051
申请日：1983-05-09
申请人： Takao Takaya , Hisashi Takasugi , Takashi Masugi , Hideaki Yamanaka , Kohji Kawabata
发明人： Takao Takaya , Hisashi Takasugi , Takashi Masugi , Hideaki Yamanaka , Kohji Kawabata
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D209/48 , C07D213/75 , C07D239/42 , C07D257/06 , C07D271/06 , C07D271/07 , C07D277/20 , C07D277/46 , C07D277/48 , C07D277/56 , C07D285/08 , C07D417/12 , C07D501/06 , C07D501/18 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/36 , C07F9/6561 , A01N43/84
CPC分类号： C07D209/48 , C07D213/75 , C07D239/42 , C07D257/06 , C07D271/06 , C07D271/07 , C07D277/20 , C07D277/46 , C07D277/48 , C07D277/56 , C07D277/587 , C07D285/08 , C07D417/12
摘要： The invention relates to novel compounds of high antimicrobial activity of the formula: ##STR1## in which R.sup.1 is amino-substituted-heterocyclic group which may have halogen, protected amino-substituted-heterocyclic group which may have halogen, or a group of the formula: ##STR2## wherein R.sup.3 is lower alkyl,R.sup.2 is carboxy or a protected carboxy group, andA is lower alkylene which may have a substituent selected from the group consisting of amino, a protected amino group, hydroxy, oxo and a group of the formula: .dbd.N.about.OR.sup.4, wherein R.sup.4 is hydrogen, cyclo(lower)alkenyl, lower alkynyl, lower alkenyl, lower alkenyl substituted by carboxy or a protected carboxy group, lower alkyl, or lower alkyl substituted by one or more substituents selected from carboxy, a protected carboxy group, amino, a protected amino group, cyano, phosphono, a protected phosphono group and a heterocyclic group which may have suitable substituents.

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