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11. 发明授权

US4331665A Cephem and cepham compounds 失效
标题翻译： Cephem和cepham化合物
公开(公告)号：US4331665A
公开(公告)日：1982-05-25
申请号：US128260
申请日：1980-03-07
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 , C07D417/12 , C07D501/14 , C07D501/20 , C07D501/30 , C07D501/36 , A61K31/545
CPC分类号： C07D209/48 , C07C17/263 , C07D249/12 , C07D257/04 , C07D285/08 , C07D295/21
摘要： 7-Substituted-3-cephem and cepham-4-carboxylic acids represented by the following 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; and,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), and the heavy solid line means single or double bond, are useful as antibiotics.
摘要翻译：由下式（I）表示的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，可以被适当的取代基，被合适的取代基取代的低级烷基，低级烯基，低级炔基，可被适当取代基取代的环烷基，环（低级）烯基或含有5元杂环基的S或O 被氧代基取代，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; 低级烷基卤素; 或羟基; 并且当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-，可用作抗生素。

12. 发明授权

US4772682A Cephem compounds 失效
公开(公告)号：US4772682A
公开(公告)日：1988-09-20
申请号：US944229
申请日：1986-12-22
申请人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号： C07F9/6539 , C07D285/08 , C07D501/04 , C07D501/18 , C07D501/24 , C07D501/36 , C07D501/46 , C07F9/6561 , A61K31/545
CPC分类号： C07D285/08 , C07F9/65613
摘要： The invention relates to intermediates useful in the preparation of antimicrobial compounds, the intermediates being of the formula: ##STR1## wherein R.sup.A is --SCN or --S.sup..sym. (R.sup.3).sub.2, whereinR.sup.3 is lower alkyl, andR.sup.B is carboxy or --COO.sup..crclbar.,or a salt thereof, with the proviso that when R.sup.A is --SCN, then R.sup.B is carboxy and that when R.sup.A is --S.sup..sym. (R.sup.3).sub.2, then R.sup.B is --COO.sup..sym..

13. 发明授权

US4654422A Cephem intermediates 失效
标题翻译： Cephem中间体
公开(公告)号：US4654422A
公开(公告)日：1987-03-31
申请号：US785712
申请日：1985-10-09
申请人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号： C07F9/6539 , C07D285/08 , C07D501/04 , C07D501/18 , C07D501/24 , C07D501/36 , C07D501/46 , C07F9/6561 , C07F9/65
CPC分类号： C07D285/08 , C07F9/65613
摘要： The invention relates to novel cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is phosphono, dihalophosphoryl, di(lower) alkoxyphosphoryl, O-lower alkylphosphono, diaminophosphoryl, (amino) (hydroxy) phosphoryl or (lower alkoxy) (morpholino) phosphoryl,R.sup.2 is lower alkyl or lower alkenyl,R.sup.3 is a group of the formula: ##STR2## wherein X is hydrogen, halogen or lower alkoxy, or a group of the formula: ##STR3## wherein R.sup.4 is lower alkyl, and Y is N or CH; and pharmaceutically acceptable salts thereof.

14. 发明授权

US4567275A Cephem and cepham compounds and processes for preparation thereof 失效
标题翻译： Cephem和cepham化合物及其制备方法
公开(公告)号：US4567275A
公开(公告)日：1986-01-28
申请号：US619981
申请日：1984-06-12
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 , C07D501/20
CPC分类号： C07D209/48 , C07C17/26 , C07C17/263 , C07D257/04 , C07D285/08 , C07D295/21
摘要： The cephalosporin intermediate 2-(5-amino-1,2,4, thiadiazol-3yl)glyoxylic acid has been prepared.
摘要翻译：已经制备了头孢菌素中间体2-（5-氨基-1,2,4-噻二唑-3-基）乙醛酸。

15. 发明授权

US4563449A Cephem compounds 失效
公开(公告)号：US4563449A
公开(公告)日：1986-01-07
申请号：US511237
申请日：1983-07-06
申请人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号： C07F9/6539 , C07D285/08 , C07D501/04 , C07D501/18 , C07D501/24 , C07D501/36 , C07D501/46 , C07F9/6561 , C07D501/38 , A61K31/545
CPC分类号： C07D285/08 , C07F9/65613
摘要： The invention relates to novel cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is phosphono, dihalophosphoryl, di(lower) alkoxyphosphoryl, O-lower alkylphosphono, diaminophosphoryl, (anino) (hydroxy) phosphoryl or (lower alkoxy) (morpholino) phosphoryl,R.sup.2 is lower alkyl or lower alkenyl,R.sup.3 is a group of the formula: ##STR2## wherein X is hydrogen, halogen or lower alkoxy, or a group of the formula: ##STR3## wherein R.sup.4 is lower alkyl, and Y is N or CH; and pharmaceutically acceptable salts thereof.

16. 发明授权

US4447429A 7-[2-Alkoxyimino-2-(5-amino-1,2,4-thiadiazol-3-yl)acetamido]-3-cephems 失效
标题翻译： 7- [2-烷氧基亚氨基-2-（5-氨基-1,2,4-噻二唑-3-基）乙酰氨基] -3-头孢烯
公开(公告)号：US4447429A
公开(公告)日：1984-05-08
申请号：US213351
申请日：1980-12-05
申请人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号： C07D249/12 , C07D257/04 , C07D285/08 , C07D501/20 , C07D501/36 , A61K31/545 , C07D501/34
CPC分类号： C07D257/04 , C07D249/12 , C07D285/08 , Y02P20/55
摘要： This invention relates to novel cephem compounds of high antimicrobial activity of the formula ##STR1## wherein R.sup.1 is amino or a protected amino,R.sup.2 is lower alkyl,R.sup.3 is hydrogen or lower alkyl,R.sup.4 is hydrogen, acyloxy(lower)alkyl or acylthio(lower)alkyl andR.sup.5 is carboxy or a protected carboxy.

17. 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。

18. 发明授权

US4381299A 7-Amino-thiadiazole oxyimino derivatives of cephem and cepham 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：US4381299A
公开(公告)日：1983-04-26
申请号：US160904
申请日：1980-06-18
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 , A61K31/545
CPC分类号： C07D257/04 , C07C17/26 , C07D285/08 , C07D295/21
摘要： This invention relates to new cephem and cepham compounds of high antimicrobial activity, and more particularly to new 7-amino-thiadiazole oxyimino derivatives of cephem and cepham compounds.
摘要翻译：本发明涉及高抗微生物活性的新的头孢烯和头孢烯化合物，更具体地说，涉及头孢烯和头孢烯化合物的新的7-氨基 - 噻二唑氧基亚氨基衍生物。

19. 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。

20. 发明授权

US4463000A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4463000A
公开(公告)日：1984-07-31
申请号：US294291
申请日：1981-08-19
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 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 suitable substituents(s), cyclo(lower)alkyl or cyclo(lower)alkenyl; andR.sup.3 is a thiazolio group which may be substituted with suitable substituents(s) or a pyridinio group substituted with substituent(s) 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.
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是氨基或被保护的氨基; R2是氢，可被适当的取代基，环（低级）烷基或环（低级）烯基取代的低级脂族烃基; 并且R 3是可以被合适的取代基取代的噻唑基或被选自卤素，氰基，羟基，氨基，酰氨基，低级烷酰基，羟基氨基甲酰基，烷基氨基甲酰基，羧基的取代基取代的吡啶基。被保护的羧基，低级烷基，羟基（低级）烷基，磺基（低级）烷基，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）。

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