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1. 发明授权

US4267176A Amino or acylamino-substituted pyrimidinyl cephalosporanic acid derivatives and pharmaceutical compositions thereof 失效
标题翻译：氨基或酰氨基取代的嘧啶基头孢菌酸衍生物及其药物组合物
公开(公告)号：US4267176A
公开(公告)日：1981-05-12
申请号：US32778
申请日：1979-04-24
申请人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
发明人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
IPC分类号： C07D213/55 , A61K31/545 , A61K31/546 , A61P31/04 , C07D213/73 , C07D213/75 , C07D213/79 , C07D213/80 , C07D239/42 , C07D239/46 , C07D501/20 , C07D501/22 , C07D501/34 , C07D501/36 , C07D501/57 , C07D501/59 , C07D519/06 , C07F7/10 , C07D501/56
CPC分类号： C07D213/73 , C07D213/75 , C07D213/79 , C07D213/80 , C07D239/42 , C07D239/47 , C07F7/10
摘要： The invention relates to novel amino or acylamino-substituted pyrimidinyl cephalosporanic acid derivatives and pharmaceutically acceptable salts thereof, of antibacterial activity, to processes for the preparation thereof, and to pharmaceutical compositions comprising the novel cephalosporanic acid derivatives.
摘要翻译：本发明涉及具有抗菌活性的新型氨基或酰氨基取代的嘧啶基头孢菌酸衍生物及其药学上可接受的盐，其制备方法以及包含新型头孢烷酸衍生物的药物组合物。

2. 发明授权

US4395411A Pyrimidinyl cephalosporanic acid derivatives and pharmaceutical compositions 失效
标题翻译：嘧啶基头孢菌酸衍生物和药物组合物
公开(公告)号：US4395411A
公开(公告)日：1983-07-26
申请号：US213684
申请日：1980-12-05
申请人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
发明人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
IPC分类号： C07D213/55 , A61K31/545 , A61K31/546 , A61P31/04 , C07D213/73 , C07D213/75 , C07D213/79 , C07D213/80 , C07D239/42 , C07D239/46 , C07D501/20 , C07D501/22 , C07D501/34 , C07D501/36 , C07D501/57 , C07D501/59 , C07D519/06 , C07F7/10
CPC分类号： C07D213/73 , C07D213/75 , C07D213/79 , C07D213/80 , C07D239/42 , C07D239/47 , C07F7/10
摘要： This invention relates to novel 7-pyrimidinyl and pyridinyl acetamido cephem derivatives of high antibacterial activity.
摘要翻译：本发明涉及高抗菌活性的新型7-嘧啶基和吡啶基乙酰氨基头孢烯衍生物。

3. 发明授权

US4596869A Pyridinyl and pyrimidinyl derivatives 失效
标题翻译：吡啶基和嘧啶基衍生物
公开(公告)号：US4596869A
公开(公告)日：1986-06-24
申请号：US777867
申请日：1985-09-19
申请人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
发明人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
IPC分类号： C07D213/55 , A61K31/545 , A61K31/546 , A61P31/04 , C07D213/73 , C07D213/75 , C07D213/79 , C07D213/80 , C07D239/42 , C07D239/46 , C07D501/20 , C07D501/22 , C07D501/34 , C07D501/36 , C07D501/57 , C07D501/59 , C07D519/06 , C07F7/10 , C07D213/53 , C07D213/60 , C07D239/02
CPC分类号： C07D213/73 , C07D213/75 , C07D213/79 , C07D213/80 , C07D239/42 , C07D239/47 , C07F7/10
摘要： A novel compound, useful as an intermediate in the production of compounds of high antimicrobial activity, of the formula: ##STR1## wherein R.sub.a.sup.1 is hydrogen, amino or a protected amino group,R.sub.b.sup.1 and R.sub.c.sup.1 are each hydrogen, halogen, lower alkoxy or arylthio,R.sup.14 is carboxy or a protected carboxy group,X is lower alkylene or a group of the formula: ##STR2## in which R.sup.6 is hydrogen or an organic residue which may have suitable substituent(s), andZ is N or CH,or a salt thereof.
摘要翻译：一种新型化合物，其用作生产高抗微生物活性化合物的中间体，其具有下式：其中Ra1为氢，氨基或被保护的氨基，Rb1和Rc1各自为氢，卤素，低级烷氧基或芳硫基 R 14为羧基或被保护的羧基，X为低级亚烷基或下式基团：其中R 6为氢或可具有合适取代基的有机残基，Z为N或CH，或其盐。

4. 发明授权

US4407798A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4407798A
公开(公告)日：1983-10-04
申请号：US296301
申请日：1981-08-26
申请人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
发明人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D213/74 , C07D213/75 , C07D239/42 , C07D501/46 , C07D501/58
CPC分类号： C07D213/75 , C07D239/42
摘要： This invention relates to novel compounds having antimicrobial activity of the formula ##STR1## in which R.sup.1 is amino or a protected amino group,R.sup.2 is cyclo(lower)alkyl, cyclo(lower)alkenyl, lower alkyl, lower alkynyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl or lower alkylthio(lower)alkyl, andY is hydrogen, amino or a protected amino group, and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及具有式（IMAGE）的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是环（低级）烷基，环（低级）烯基，低级烷基，低级炔基，羧基（低级）烷基，保护的羧基（低级）烷基或低级烷硫基（低级）烷基，Y为氢，氨基或被保护的氨基，及其药学上可接受的盐。

5. 发明授权

US4425340A Cephem and cepham compounds 失效
标题翻译： Cephem和cepham化合物
公开(公告)号：US4425340A
公开(公告)日：1984-01-10
申请号：US314045
申请日：1981-10-22
申请人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号： C07C17/26 , C07D209/48 , C07D249/12 , C07D257/04 , C07D285/08 , C07D295/21 , C07D501/24 , A61K31/545
CPC分类号： C07D209/48 , C07C17/263 , C07D249/12 , C07D257/04 , C07D285/08 , C07D295/21
摘要： This invention relates to new cephem and cepham compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino,R.sup.2 is hydrogen, acyl, aryl which may be substituted with suitable substituent(s), lower alkyl substituted with suitable substituent(s), lower alkenyl, lower alkynyl, cycloalkyl which may be substituted with suitable substituent(s), cyclo(lower)alkenyl, or S or O containing 5-membered heterocyclic group substituted with oxo group(s),R.sup.3 is hydrogen or lower alkyl,R.sup.4 is hydrogen, acyloxy(lower)alkyl; acylthio(lower) alkyl; pyridinium(lower)alkyl which may be substituted with suitable substituent(s); a heterocyclicthio(lower)alkyl which may be substituted with suitable substituent(s); lower alkyl;l halogen; hydroxy; thiazolium(lower)alkyl which may be substituted with suitable substituent(s); or lower alkoxy; R.sup.5 is carboxy or a protected carboxy, wherein R.sup.5 is COO.sup.- when R.sup.4 is pyridinium(lower)alkyl which may be substituted with suitable substituent(s) or thiazolium(lower)alkyl which may be substituted with suitable substituent(s), and the heavy solid line means single or double bond; and 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的头孢烯和头孢烯化合物：其中R1是氨基或被保护的氨基，R2是氢，酰基，可被适当的取代基取代的芳基，低级烷基取代的具有合适的取代基，低级烯基，低级炔基，可被适当的取代基取代的环烷基，环（低级）烯基或含有被氧代基取代的5元杂环基的S或O，R 3 是氢或低级烷基，R 4是氢，酰氧基（低级）烷基; 酰基硫代（低级）烷基; 可用合适的取代基取代的吡啶鎓（低级）烷基; 可被适当的取代基取代的杂环硫基（低级）烷基; 低级烷基; l卤素; 羟基; 可被适当的取代基取代的噻唑鎓（低级）烷基; 或低级烷氧基; R5是羧基或被保护的羧基，其中当R 4是吡啶鎓（低级）烷基时，其中R 5是COO-，其可被合适的取代基取代，或可被适当的取代基取代的噻唑鎓（低级）烷基，重实线表示单键或双键; 及其药学上可接受的盐。

6. 发明授权

US4332798A 7-Amino-thia-diazole oxyimino derivatives of cephem and cephem compounds 失效
标题翻译：头孢烯和头孢烯化合物的7-氨基 - 噻二唑氧基亚氨基衍生物
公开(公告)号：US4332798A
公开(公告)日：1982-06-01
申请号：US116984
申请日：1980-01-30
申请人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号： C07C17/26 , C07D209/48 , C07D249/12 , C07D257/04 , C07D285/08 , C07D295/21 , C07D501/20 , A61K31/545 , C07D501/56
CPC分类号： C07D209/48 , C07C17/26 , C07C17/263 , C07D249/12 , C07D257/04 , C07D285/08 , C07D295/21
摘要： 7-Substituted-3-cephem and cepham-4-carboxylic acids of formula (I) ##STR1## wherein R.sup.1 is amino or a protected amino, R.sup.2 is hydrogen, acyl, aryl which may be substituted with suitable substituent(s), lower alkyl substituted with suitable substituent(s), lower alkenyl, lower alkynyl, cycloalkyl which may be substituted with suitable substituent(s), cyclo(lower)alkenyl, or S- or O-containing 5-membered heterocyclic group substituted with oxo group(s).R.sup.3 is hydrogen or lower alkyl,R.sup.4 is hydrogen; acyloxy(lower)alkyl; acylthio(lower)alkyl pyridinium(lower)alkyl which may be substituted with suitable substituent(s); a heterocyclicthio(lower)alkyl which may be substituted with suitable substituent(s); lower alkyl; halogen; or hydroxy; andR.sup.5 is carboxy or a protected carboxy wherein R.sup.5 is COO-- when R.sup.4 is pyridinium(lower)alkyl which may be substituted with suitable substituent(s), and the heavy solid line means single or double bond, have useful antibiotic properties.
摘要翻译：（I）的7-取代的3-头孢烯和头孢烯-4-羧酸其中R1是氨基或被保护的氨基，R2是氢，酰基，可被适当取代基取代的芳基），被合适的取代基取代的低级烷基，低级链烯基，低级炔基，可被适当的取代基取代的环烷基，环（低级）烯基或被S或O取代的5-或氧代基团。 R3是氢或低级烷基，R4是氢; 酰氧基（低级）烷基; 可以用合适的取代基取代的酰硫基（低级）烷基吡啶鎓（低级）烷基; 可被适当的取代基取代的杂环硫基（低级）烷基; 低级烷基卤素; 或羟基; 当R 4是可被适当的取代基取代的吡啶鎓（低级）烷基，并且重实线表示单键或双键时，R 5为羧基或被保护的羧基，其中R 5为COO-，具有有用的抗生素性质。

7. 发明授权

US4550102A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4550102A
公开(公告)日：1985-10-29
申请号：US415910
申请日：1982-09-08
申请人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/38 , C07D501/46
CPC分类号： C07D501/46
摘要： The invention relates to novel cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or lower alkanoylamino,R.sup.2 is lower alkyl, lower alkynyl, carboxy (lower) alkyl or esterified carboxy (lower) alkyl,R.sup.3 is amino or lower alkanoylamino, andX is hydrogen or halogen; and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及具有下式的高抗微生物活性的新型头孢烯化合物：其中R1是氨基或低级烷酰氨基，R2是低级烷基，低级炔基，羧基（低级）烷基或酯化的羧基（低级）烷基，R3是氨基或低级烷酰氨基，X为氢或卤素; 和其药学上可接受的盐。

8. 发明授权

US4495182A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4495182A
公开(公告)日：1985-01-22
申请号：US382763
申请日：1982-05-27
申请人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号： C07D213/61 , C07D213/70 , C07D213/73 , C07D285/08 , C07D501/36 , A61K31/545
CPC分类号： C07D213/70 , C07D213/61 , C07D213/73 , C07D285/08
摘要： This invention relates to cephem compounds of high antimicrobial activity of the formula ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is hydrogen, lower aliphatic hydrocarbon group selected from lower alkyl, alkenyl and alkynyl which may be substituted with carboxy, protected carboxy, lower alkylthio or phenyl, cyclo(lower)alkyl, or cyclo(lower)alkenyl;R.sup.3 is lower alkyl which may be substituted with carboxy, carbamoyl, hydroxy, amino or protected amino;R.sup.3a is hydrogen, lower alkyl or amino; andR.sup.3b is hydrogen or lower alkyl; andpharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及具有下式的高抗微生物活性的头孢烯化合物：其中R1是氨基或被保护的氨基; R2是氢，可以被羧基取代的低级烷基，烯基和炔基的低级脂族烃基，保护的羧基，低级烷硫基或苯基，环（低级）烷基或环（低级）烯基; R3是可被羧基，氨基甲酰基，羟基，氨基或被保护的氨基取代的低级烷基; R3a是氢，低级烷基或氨基; 和R3b是氢或低级烷基; 及其药学上可接受的盐。

9. 发明授权

US4468515A 2-Substituted oxyimino-2-(5-amino-1,2,4-thiadiazol-3-yl)acetic acids 失效
标题翻译： 2-取代的氧亚氨基-2-（5-氨基-1,2,4-噻二唑-3-基）乙酸
公开(公告)号：US4468515A
公开(公告)日：1984-08-28
申请号：US325027
申请日：1981-11-25
申请人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号： C07C17/26 , C07D209/48 , C07D257/04 , C07D285/08 , C07D295/21
CPC分类号： C07D209/48 , C07C17/26 , C07C17/263 , C07D257/04 , C07D285/08 , C07D295/21
摘要： This invention relates to thiadiazolyl compounds useful as intermediates in the preparation of novel cephem compounds of high antimicrobial activity.
摘要翻译：本发明涉及可用作制备高抗微生物活性的新型头孢烯化合物的中间体的噻二唑基化合物。

10. 发明授权

US4457928A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4457928A
公开(公告)日：1984-07-03
申请号：US330465
申请日：1981-12-14
申请人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号： C07C17/26 , C07D257/04 , C07D285/08 , C07D295/21 , C07D501/46 , A61K31/545
CPC分类号： C07D257/04 , C07C17/26 , C07D285/08 , C07D295/21
摘要： This invention relates to novel cephem compounds of high antimicrobial activity, to processes for preparation of said compounds, and to pharmaceutical compositions comprising said compounds, the novel cephem compounds being of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is hydrogen, lower aliphatic hydrocarbon group which may be substituted with a substituent selected from the group consisting of carboxy and protected carboxy, cyclo (lower) alkyl or cyclo (lower) alkenyl; andR.sup.3 is a thiazolio group which may be substituted with a substituent selected from the group consisting of lower alkyl and hydroxy (lower) alkyl, or a pyridinio group substituted with a substituent selected from the group consisting of halogen, cyano, hydroxy, amino, acylamino, lower alkanoyl, hydroxycarbamoyl, alkylcarbamoyl, carboxy, protected carboxy, lower alkyl, hydroxy (lower) alkyl, sulfo (lower) alkyl, protected amino (lower) alkyl, amino (lower) alkyl, carboxy (lower) alkyl and hydroxyimino (lower) alkyl;and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及高抗微生物活性的新型头孢烯化合物，所述化合物的制备方法以及包含所述化合物的药物组合物，所述新型头孢烯化合物具有下式：其中R 1为氨基或被保护的氨基; R2是氢，可以被选自羧基和保护的羧基，环（低级）烷基或环（低级）烯基的取代基取代的低级脂族烃基; 或者可以被选自低级烷基和羟基（低级）烷基的取代基取代的噻唑基，或被选自卤素，氰基，羟基，氨基，酰基氨基，低级烷酰基，羟基氨基甲酰基，烷基氨基甲酰基，羧基，保护的羧基，低级烷基，羟基（低级）烷基，磺基（低级）烷基，被保护的氨基（低级）烷基，氨基（低级）烷基，羧基（低级）烷基和羟基亚氨基低级）烷基; 及其药学上可接受的盐。

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