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1. 发明授权

US4598154A Thiazole intermediates for cephalosporin compounds 失效
标题翻译：噻唑中间体用于头孢菌素化合物
公开(公告)号：US4598154A
公开(公告)日：1986-07-01
申请号：US692497
申请日：1985-01-18
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 , C07D277/42
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.

2. 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.

3. 发明授权

US4547494A Pyrrolidomoxine cephalosporins 失效
标题翻译：吡咯莫多因头孢菌素
公开(公告)号：US4547494A
公开(公告)日：1985-10-15
申请号：US578380
申请日：1984-02-09
申请人： Toyonari Oine , Yoshihisa Yamada , Mitsuyoshi Wagatsuma , Totaro Yamaguchi , Satoshi Ohshima
发明人： Toyonari Oine , Yoshihisa Yamada , Mitsuyoshi Wagatsuma , Totaro Yamaguchi , Satoshi Ohshima
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D257/04 , C07D417/12 , C07D501/36 , C07D501/60
CPC分类号： C07D257/04 , C07D417/12 , Y02P20/55
摘要： A 7.beta.-{(Z)-2-(2-aminothiazol-4-yl)-2-[(2-pyrrolidon-3-yl)oxyimino]acetamido}-3-(1-amino-1H-tetrazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid or a pharmaceutically acceptable salt thereof is useful as an antimicrobial agent.
摘要翻译：将7β-{（Z）-2-（2-氨基噻唑-4-基）-2 - [（2-吡咯烷酮-3-基）氧亚氨基]乙酰氨基} -3-（1-氨基-1H-四唑-5 - 基）硫代甲基-3-头孢烯-4-羧酸或其药学上可接受的盐可用作抗微生物剂。

4. 发明授权

US3966731A 2-Fluoromethyl-3-o-tolyl-6-amino-4(3H)-quinazolinone 失效
标题翻译： 2-氟甲基-3-邻甲苯基-6-氨基-4（3H） - 喹唑啉酮
公开(公告)号：US3966731A
公开(公告)日：1976-06-29
申请号：US510577
申请日：1974-09-30
申请人： Ichizo Inoue , Toyonari Oine , Yoshihisa Yamada , Junichi Tani , Ryuichi Ishida , Takashi Ochiai
发明人： Ichizo Inoue , Toyonari Oine , Yoshihisa Yamada , Junichi Tani , Ryuichi Ishida , Takashi Ochiai
IPC分类号： C07D239/91 , A61K31/505 , A61K31/517 , A61P25/08 , A61P25/20 , C07D20060101 , C07D239/88
CPC分类号： C07D239/91 , Y10S514/906
摘要： N-(2-amino-5-nitrobenzoyl)-o-toluidine is condensed with fluoroacetic acid or a functional derivative thereof. N-(2-fluoroacetamido-5-nitrobenzoyl)-o-toluidine obtained by said condensation reaction is dehydrated to produce 2-fluoromethyl-3-(o-tolyl)-6-nitro-4(3H)-quniazolinone, which is then subjected to reduction reaction. 2-fluoromethyl-3-(o-tolyl)-6-amino-4(3H)-quinazolinone thus obtained and a pharmaceutically acceptable acid addition salt thereof are useful as central muscle relaxants, minor tranquilizers, anti-convulsants, analgesics and/or anti-inflammatory agents.
摘要翻译： N-（2-氨基-5-硝基苯甲酰基） - 对 - 甲苯胺与氟乙酸或其功能性衍生物缩合。将通过所述缩合反应获得的N-（2-氟乙酰氨基-5-硝基苯甲酰基） - 邻甲苯胺脱水，得到2-氟甲基-3-（邻甲苯基）-6-硝基-4（3H） - 偶氮唑啉酮进行还原反应。由此获得的2-氟甲基-3-（邻甲苯基）-6-氨基-4（3H） - 喹唑啉酮和其药学上可接受的酸加成盐可用作中枢肌肉松弛剂，小镇静剂，抗惊厥药，止痛剂和/或抗炎剂。

5. 发明授权

US5294706A Process for preparing 1,5-benzothiazepine derivatives 失效
标题翻译：制备1,5-苯并硫氮杂衍生物的方法
公开(公告)号：US5294706A
公开(公告)日：1994-03-15
申请号：US979417
申请日：1992-11-19
申请人： Tadayuki Koumoto , Hironori Hayashi , Toshiya Kadowaki , Masahiko Seto , Toyonari Oine
发明人： Tadayuki Koumoto , Hironori Hayashi , Toshiya Kadowaki , Masahiko Seto , Toyonari Oine
IPC分类号： C07D281/10
CPC分类号： C07D281/10
摘要： There is disclosed a process for preparing 1,5-benzothiazepine derivatives of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group, or a salt thereof which comprises subjecting a propionate derivatives of the formula: ##STR2## wherein R.sup.2 is an ester residue and R.sup.1 is the same as defined above, to intramolecular cyclization in the presence of a sulfonic acid compound of the formula:R.sup.3 SO.sub.3 H (III)wherein R.sup.3 is a lower alkyl group or a substituted or unsubstituted phenyl group, in a non-halogenated organic solvent and, if desired, converting the product to a salt thereof.
摘要翻译：公开了一种制备下式的1,5-苯并硫氮杂衍生物的方法：其中R1是低级烷基或其盐，其包括使下式的丙酸酯衍生物：（II））其中R 2是酯残基并且R 1与上述定义相同，在下式的磺酸化合物存在下分子内环化：R3SO3H（Ⅲ）其中R3是低级烷基或取代或未取代的苯基，在非卤化有机溶剂中，如果需要，将产物转化成其盐。

6. 发明授权

US4727071A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US4727071A
公开(公告)日：1988-02-23
申请号：US835886
申请日：1986-03-04
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.

7. 发明授权

US4794186A Thiazolylacetic acid derivative and processes for preparing the same 失效
标题翻译：噻唑乙酸衍生物及其制备方法
公开(公告)号：US4794186A
公开(公告)日：1988-12-27
申请号：US681252
申请日：1984-12-13
申请人： Toyonari Oine , Yoshihisa Yamada , Hiroshi Sugano
发明人： Toyonari Oine , Yoshihisa Yamada , Hiroshi Sugano
IPC分类号： C07D407/12 , C07D207/26 , C07D207/273 , C07D417/12
CPC分类号： C07D207/273 , C07D417/12 , Y02P20/55
摘要： Novel thiazolylacetic acid derivative of the formula: ##STR1## wherein R.sup.1.sub.N H-- is amino or a protected amino group, R.sup.2 is hydrogen or lower alkyl, --COOR.sup.3 is carboxy or a protected carboxy group and n is an integer of 2 or 3, and processes for preparing the same. The compound (I) is useful as an intermediate in the synthesis of cephalosporins.
摘要翻译：下式的新型噻唑乙酸衍生物：其中R 1 NH-是氨基或被保护的氨基，R 2是氢或低级烷基，-COOR 3是羧基或保护的羧基，n是2或3的整数，及其制备方法。化合物（I）可用作头孢菌素合成中的中间体。

8. 发明授权

US4786633A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US4786633A
公开(公告)日：1988-11-22
申请号：US56958
申请日：1987-06-03
申请人： Mitsuyoshi Wagatsuma , Toyonari Oine , Totaro Yamaguchi
发明人： Mitsuyoshi Wagatsuma , Toyonari Oine , Totaro Yamaguchi
IPC分类号： C07D519/06 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36 , C07D501/56 , C07D519/00
CPC分类号： C07D501/36
摘要： A cephalosporin compound of the formula: ##STR1## wherein: R.sup.2 is a group of the formula: ##STR2## R.sup.4 is a lower alkenyl group, a lower alkyl group or a lower alkyl group substituted with a member selected from the group consisting of cyano, lower alkylthio, 2-(lower alkyl)-1,3,4-thiadiazol-5-yl, carbamoyl, thiocarbamoyl, and N-lower alkyl(thiocarbamoyl) andR.sup.5 and R.sup.6 are each a hydrogen atom or a lower alkyl group, or a pharmaceutically acceptable salt thereof, is disclosed. These compounds have antimicrobial activity.
摘要翻译：下式的头孢菌素化合物：其中：R 2是下式的基团：R 4是低级烯基，低级烷基或被选自下组的基团取代的低级烷基由氰基，低级烷硫基，2-（低级烷基）-1,3,4-噻二唑-5-基，氨基甲酰基，硫代氨基甲酰基和N-低级烷基（硫代氨基甲酰基）组成，R5和R6分别为氢原子或低级烷基或其药学上可接受的盐。这些化合物具有抗菌活性。

9. 发明授权

US4784995A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US4784995A
公开(公告)日：1988-11-15
申请号：US59584
申请日：1987-06-08
申请人： Toyonari Oine , Mitsuyoshi Wagatsuma , Totaro Yamaguchi
发明人： Toyonari Oine , Mitsuyoshi Wagatsuma , Totaro Yamaguchi
IPC分类号： A61K31/545 , C07D20060101 , C07D501/00 , C07D501/24 , C07D501/38 , C07D501/44 , C07D501/46 , C07D501/56
CPC分类号： C07D501/46
摘要： A cephalosporin compound of the formula: ##STR1## wherein R.sup.1 is a protected or unprotected amino group;either one of R.sup.2 and R.sup.3 is a substituted or unsubstituted lower alkylthio group; sulfamoyl group; a lower alkylsulfonyl group; sulfo group; a substituted or unsubstituted amino group; a lower alkyl group; a lower alkyl group having a substituent selected from a lower alkylthio group, amino group and an acylamino group; a halogen atom; carboxy group or a lower alkoxy group; andthe other one of R.sup.2 and R.sup.3 is hydrogen atom; carbamoyl group; a substituted or unsubstituted amino group; a lower alkyl group or a hydroxy-lower alkyl group; orR.sup.2 and R.sup.3 are combined together to form a lower alkylene group;or a salt thereof and processes for preparing the same are disclosed. The cephalosporin compound (I) is useful as an antimicrobial agent.
摘要翻译：下式的头孢菌素化合物：其中R 1是被保护或未被保护的氨基; R2和R3中的任一个是取代或未取代的低级烷硫基; 氨磺酰基低级烷基磺酰基; 磺基; 取代或未取代的氨基; 低级烷基; 具有选自低级烷硫基，氨基和酰氨基的取代基的低级烷基; 卤素原子; 羧基或低级烷氧基; R2和R3中的另一个是氢原子; 氨基甲酰基; 取代或未取代的氨基; 低级烷基或羟基 - 低级烷基; 或R 2和R 3结合在一起形成低级亚烷基; 或其盐及其制备方法。头孢菌素化合物（I）可用作抗微生物剂。

10. 发明授权

US4742174A Cephalosporin compounds 失效
公开(公告)号：US4742174A
公开(公告)日：1988-05-03
申请号：US920180
申请日：1986-10-17
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
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.

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