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公开(公告)号：US4719206A
公开(公告)日：1988-01-12
申请号：US824969
申请日：1986-01-31
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D213/20 , C07D401/06 , C07D501/18 , C07D501/24 , A61K31/54
CPC分类号： C07D213/20 , C07D401/06
摘要： The invention relates to novel cephem compounds, of high antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 and R.sup.9 are amino or acylamino; andR.sup.9 is a group of the formula: ##STR2## where R.sup.2 is organic group,X is CH or N,Z is acid residueY is CH or N and n is O; orY is N.sup..sym. --R.sup.2 wherein R.sup.2 is as defined above and n is 1,or a group of the formula:--A--N.sup..sym. (R.sup.10).sub.3whereinR.sup.10 is lower alkyl andA is lower alkylene.
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公开(公告)号：US4584290A
公开(公告)日：1986-04-22
申请号：US556413
申请日：1983-11-30
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D213/20 , C07D401/06 , C07D501/18 , C07D501/24 , C07D501/38
CPC分类号： C07D213/20 , C07D401/06
摘要： The invention relates to novel compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or acylamino; andR.sup.9 is a group of the formula: ##STR2## wherein R.sup.2 is organic group,X is CH or N,Z is acid residueY is CH or N and n is O; orY is N.sup..sym. --R.sup.2 wherein R.sup.2 is as defined above and n is 1,or a group of the formula:--A--N.sup..sym. (R.sup.10).sub.3whereinR.sup.10 is lower alkyl andA is lower alkylene.
摘要翻译： 本发明涉及具有下式的高抗微生物活性的新化合物：其中R1是氨基或酰氨基; 并且R 9是下式的基团：其中R 2是有机基团，X是CH或N，Z是酸残基，Y是CH或N，n是0; 或Y是N（+） - R 2，其中R 2如上定义并且n是1，或下式基团-A-N（+）（R 10）3，其中R 10是低级烷基，A是低级亚烷基。
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3.发明授权7-Substituted-3-vinyl-3-cephem compounds and processes for production of the same 失效7-取代的3-乙烯基-3-头孢烯化合物及其制备方法
公开(公告)号：US4559334A
公开(公告)日：1985-12-17
申请号：US543880
申请日：1983-10-20
IPC分类号： A61K31/545 , C07D20060101 , C07D501/22 , C07D501/24
CPC分类号： C07D501/22
摘要： The invention relates to novel compounds of high antimicrobial activity of the formula: ##STR1## in which R.sup.1 is amino or a protected amino group, andR.sup.2 is carboxy or a protected carboxy group, and a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明涉及具有下式的高抗微生物活性的新化合物：其中R1是氨基或被保护的氨基，R2是羧基或被保护的羧基，及其药学上可接受的盐。
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4.发明授权
公开(公告)号：US4423213A
公开(公告)日：1983-12-27
申请号：US261618
申请日：1981-05-07
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
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 7-acylamino-3-vinylcephalosporanic acid derivatives of antimicrobial activity, and to methods of preparation thereof from novel intermediate compounds of the formula: ##STR1## in which R.sub.C is amino or a group of the formula: ##STR2## wherein R.sup.8 is aryl,A.sup.12 is lower alkylene having 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 substituent(s) 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 substituent(s),R.sup.a is a protected amino group,R.sup.b is a protected carboxy group,R.sup.c and R.sup.d are combined to form oxo or a protected oxo group, and X.sup.1 is halogen, andR.sup.2 is carboxy or a protected carboxy group, provided that, when R.sub.C is amino, then R.sup.2 is carboxy, or a salt thereof.
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5.发明授权7-acylamino-3-vinylcephalosporanic acid derivatives and processes for the preparation thereof 失效7-酰氨基-3-乙烯基头孢烷酸衍生物及其制备方法
公开(公告)号：US4960889A
公开(公告)日：1990-10-02
申请号：US462347
申请日：1990-01-03
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
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： Amino-pyridinyl and pyrimidinyl intermediates have been synthesized.
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公开(公告)号：US4904652A
公开(公告)日：1990-02-27
申请号：US785048
申请日：1985-10-09
IPC分类号： C07D501/32 , 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 , C07D501/18 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36
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 compound 7[2-(aminothiazol-4-yl)-2-methyoxyiminoacetamido]-methylthiomethyl-3-cephem-4-carboxylic acid or carboxylic ester thereof, or a pharmaceutically acceptable salt thereof is disclosed as an antimicrobial agent.
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公开(公告)号：US4731443A
公开(公告)日：1988-03-15
申请号：US889189
申请日：1986-07-24
IPC分类号： 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 , C07D501/22 , C07D501/04 , A61K31/545
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 intermediates for the preparation of antimicrobial compounds, the intermediate being a compound of the formula: ##STR1## in which R.sup.2 is carboxy or a protected carboxy group,R.sup.8 is 2-hydroxyphenyl andZ is a group of the formula:--CH.dbd.CH.sub.2, --CH.sub.2 --X.sup.2, --CH.sub.2 P.sup.+ (R.sup.7).sub.3.X.sup.3-,--CH.dbd.P(R.sup.7).sub.3 OR--CH.sub.2 OH,wherein X.sup.2 and X.sup.3 are each halogen and R.sup.7 is selected from the group consisting of phenyl, tolyl, xylyl and naphthyl, or a salt thereof.
摘要翻译： 本发明涉及用于制备抗微生物化合物的新型中间体，其中间体为下式的化合物：其中R 2为羧基或被保护的羧基，R 8为2-羟基苯基，Z为下式基团： -CH = CH 2，-CH 2 -X 2，-CH 2 P +（R 7）3 X 3 - ， - CH = P（R 7）3 OR-CH 2 OH，其中X 2和X 3各自为卤素，R 7选自苯基， 甲苯基，二甲苯基和萘基，或其盐。
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8.发明授权7-acylamino-3-vinylcephalosporanic acid derivatives useful for treatment of infectious diseases in human beings and animals 失效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
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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9.发明授权7-Acylamino-3-substituted cephalosporanic acid derivatives and processes for the preparation thereof 失效7-酰氨基-3-取代头孢烷酸衍生物及其制备方法
公开(公告)号：US4462999A
公开(公告)日：1984-07-31
申请号：US261781
申请日：1981-05-08
IPC分类号： C07D501/32 , 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 , C07D501/18 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/56
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： Anti-microbial cephalosporins of the formula ##STR1## in which R.sup.2 is methoxymethyl or methylthiomethyl, and R.sup.6 is carboxy (lower) alkyl have been prepared.
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公开(公告)号：US5594132A
公开(公告)日：1997-01-14
申请号：US684194
申请日：1991-04-12
IPC分类号： C07D501/32 , 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 , C07D501/18 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36
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： A compound of the formula: ##STR1## in which R.sup.2 is lower alkoxymethyl, lower alkylthiomethyl or lower alkenylthiomethyl,R.sup.3 is carboxy or a protected carboxy group,A.sup.5 is lower alkylene which may have a group of the formula: .dbd.N.about.OR.sup.6, wherein R.sup.6 is hydrogen, lower alkenyl, lower alkynyl, lower alkyl or lower alkyl substituted by one or more substituent (s) selected from carboxy, a protected carboxy group, amino, a protected amino group and a heterocyclic group, andX.sup.1 is halogen,or a salt thereof.
摘要翻译： 下式的化合物，其中R 2是低级烷氧基甲基，低级烷硫基甲基或低级链烯硫基甲基，R 3是羧基或受保护的羧基，A5是可以具有下列基团的低级亚烷基：= N DIFFERENCE OR 6，其中 R6是氢，低级烯基，低级炔基，被一个或多个选自羧基，保护的羧基，氨基，保护的氨基和杂环基的取代基取代的低级烷基或低级烷基，X 1是卤素，或 其盐。
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