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公开(公告)号:US4053609A
公开(公告)日:1977-10-11
申请号:US711858
申请日:1976-08-05
申请人: Mitsutaka Kawazu , Mitsuyoshi Wagatsuma , Masahiko Seto , Toshikazu Miyagishima , Totaro Yamaguchi , Satoshi Ohshima
发明人: Mitsutaka Kawazu , Mitsuyoshi Wagatsuma , Masahiko Seto , Toshikazu Miyagishima , Totaro Yamaguchi , Satoshi Ohshima
IPC分类号: C07C271/22 , C07D207/46 , C07D499/00 , C07D499/68 , A61K31/43
CPC分类号: C07C271/22 , C07D207/46 , C07D499/00
摘要: A compound of the formula: ##STR1## wherein R.sup.1 is hydrogen or hydroxy, R.sup.2 is a group of the formula: --CO-CH(NH.sub.2)-CH.sub.2 COR.sup.3 or --COCH.sub.2 -CH(NH.sub.2)-COR.sup.3, and R.sup.3 is selected from the group consisting of hydroxy, lower alkylamino, di-lower alkylamino, lower alkoxy and hydroxy-lower alkylamino, or R.sup.3 is amino when R.sup.2 is hydroxy. Several methods of preparing the compound [I] are also disclosed. The compound [I] and a pharmaceutically acceptable salt thereof are useful as antimicrobial agents.
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公开(公告)号:US4547494A
公开(公告)日:1985-10-15
申请号:US578380
申请日:1984-02-09
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。
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公开(公告)号:US4576938A
公开(公告)日:1986-03-18
申请号:US447809
申请日:1982-12-08
IPC分类号: C07D257/04 , C07D417/12 , C07D417/14 , C07D501/36 , A61K31/545 , C07D501/56
CPC分类号: C07D257/04 , C07D417/12 , C07D417/14
摘要: A cephalosporin compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a carboxy(lower)alkyl group, a hydroxy(lower)alkyl group, a carbamoyl(lower)alkyl group, an N-(lower)alkyl-carbamoyl(lower)alkyl group, a cycloalkyl group, a carboxycycloalkyl group, or a tetrazolylmethyl group, R.sup.2 is a hydrogen atom, a lower alkyl group, a formyl group or a lower alkanol group, R.sup.3 is a hydrogen atom, or R.sup.2 and R.sup.3 are combined together to form an aralkylidene group, or a pharmaceutically acceptable salt thereof which is useful as an antimicrobial agent, and process for their preparation.
摘要翻译: 下式的头孢菌素化合物:其中R1是氢原子,低级烷基,羧基(低级)烷基,羟基(低级)烷基,氨基甲酰基(低级)烷基,N-( 低级)烷基 - 氨基甲酰基(低级)烷基,环烷基,羧基环烷基或四唑基甲基,R2是氢原子,低级烷基,甲酰基或低级链烷醇基,R3是氢原子, 或R2和R3组合在一起形成可用作抗微生物剂的芳烷基或其药学上可接受的盐及其制备方法。
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公开(公告)号:US4786633A
公开(公告)日:1988-11-22
申请号:US56958
申请日:1987-06-03
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。
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公开(公告)号:US4784995A
公开(公告)日:1988-11-15
申请号:US59584
申请日:1987-06-08
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。
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公开(公告)号:US4866170A
公开(公告)日:1989-09-12
申请号:US98364
申请日:1987-09-18
IPC分类号: C07D499/04 , A61K31/43 , A61P31/04 , C07D499/00 , C07D499/18 , C07D499/64 , C07D499/68 , C07D499/70
CPC分类号: C07D499/00
摘要: A stable trihydrate of (2S, 5R, 6R)-6-{(2R)-2-[(2R)-2-amino-3-(N-methylcarbamoyl)propionamido]-2-(p-hydroxyphenyl)acetamido}-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid and process for preparing the same are disclosed.
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公开(公告)号:US5169946A
公开(公告)日:1992-12-08
申请号:US805561
申请日:1991-11-27
IPC分类号: A61K31/55 , A61K31/554 , A61P9/08 , A61P9/10 , A61P9/12 , C07D281/10
CPC分类号: C07D281/10
摘要: A process for preparing hydrochloride of 3-acetoxy-2,3-dihydro-5-[2-(dimethylamino)ethyl]-2-(p-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one which comprises reacting 3-hydroxy-2,3-dihydro-5-[2-(dimethylamino)ethyl]-2-(p-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one which acetyl chloride in acetic acid or a mixed solvent of acetic acid and acetic anhydride. According to the process, hydrochloride of 3-acetoxy-2,3-dihydro-5-[2-(dimethylamino)ethyl]-2-(p-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one is readily obtained in one step.
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