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1. 发明授权

US4479942A Tetrahydrofurnancarboxylic acid derivatives, processes for preparation thereof and pharmaceutical compositions thereof 失效
标题翻译：四氢呋喃羧酸衍生物，其制备方法及其药物组合物
公开(公告)号：US4479942A
公开(公告)日：1984-10-30
申请号：US403117
申请日：1982-07-29
申请人： Michio Yamashita , Tadaaki Komori , Junji Hosoda , Yoshio Kawai , Itsuo Uchida , Masanobu Kohsaka , Hiroshi Imanaka , Kazuo Sakane , Hiroyuki Setoi , Tsutomu Teraji
发明人： Michio Yamashita , Tadaaki Komori , Junji Hosoda , Yoshio Kawai , Itsuo Uchida , Masanobu Kohsaka , Hiroshi Imanaka , Kazuo Sakane , Hiroyuki Setoi , Tsutomu Teraji
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P31/04 , C07H19/16 , C12P19/40 , C07H17/00 , C07H19/06
CPC分类号： C12R1/645 , C07H19/16 , C12P19/40 , Y02P20/55
摘要： This invention relates to tetrahydrofuran-carboxylic acid derivatives, of antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group,R.sup.2 is amino or acylamino andR.sup.3 is carboxy or a protected carboxy groupor a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及抗微生物活性的四氢呋喃 - 羧酸衍生物，其具有下式：其中R1是氨基或被保护的氨基，R2是氨基或酰基氨基，R3是羧基或被保护的羧基或药学上可接受的盐其中。

2. 发明授权

US4585872A Cephem intermediates 失效
公开(公告)号：US4585872A
公开(公告)日：1986-04-29
申请号：US571380
申请日：1984-01-16
申请人： Tsutomu Teraji , Kazuo Sakane , Jiro Gotto
发明人： Tsutomu Teraji , Kazuo Sakane , Jiro Gotto
IPC分类号： C07D249/12 , C07D257/04 , C07D285/08 , C07D501/20 , C07D501/36
CPC分类号： C07D257/04 , C07D249/12 , C07D285/08 , Y02P20/55
摘要： Alkoxyimino-2-(5-amino-1,2,4-thiadiazol-3-yl) acetic acid compounds are intermediates for cephem compounds.

3. 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。

4. 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。

5. 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。

6. 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。

7. 发明授权

US4521413A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4521413A
公开(公告)日：1985-06-04
申请号：US414471
申请日：1982-09-02
申请人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号： C07C257/14 , C07D213/30 , C07D213/32 , C07D213/68 , C07D213/70 , C07D213/74 , C07D285/08 , C07D401/12 , C07D501/20 , C07D501/46 , C07D501/38 , A61K31/545
CPC分类号： C07D213/30 , C07D213/32 , C07D213/68 , C07D213/70 , C07D213/74 , C07D285/08 , C07D401/12 , Y02P20/55
摘要： The 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 lower alkyl which may be substituted with one carboxy, lower alkenyl, lower alkynyl, cyclo (lower) alkyl or cyclo (lower) alkenyl;R.sup.3 is lower alkylamino, N-(lower) alkanoyl (lower) alkylamino, di (lower) alkylamino, sulfo (lower) alkylamino, hydroxy (lower) alkylamino, N-(lower) alkanoylhydroxy (lower) alkylamino, alkanoyloxy (lower) alkyl, alkenoyloxy (lower) alkyl, lower alkoxy (lower) alkoxy (lower) alkyl, di (lower) alkylamino (lower) alkyl, lower alkylthio (lower) alkyl, lower alkylthio, lower alkoxy, lower alkoxy (lower) alkoxy, hydroxy (lower) alkoxy, lower alkanesulfonyl (lower) alkyl, hydroxy (lower) alkylthio, di (lower) alkylamino (lower) alkylthio, tetrazolyl, tetrazolylthio, tetrazolylthio (lower) alkyl or dihydrotriazinylthio (lower) alkyl substituted with oxo, hydroxy and lower alkyl; andR.sup.4 is hydrogen or lower alkyl; and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及高抗微生物活性的头孢烯化合物，其具有下式：其中R1是氨基或被保护的氨基; R2是可被一个羧基，低级烯基，低级炔基，环（低级）烷基或环（低级）烯基取代的低级烷基; R3是低级烷基氨基，N-（低级）烷酰基（低级）烷基氨基，二（低级）烷基氨基，磺基（低级）烷基氨基，羟基（低级）烷基氨基，N-（低级）烷酰基羟基（低级）烷基氨基，烷酰氧基（低级）烷基，低级烷氧基（低级）烷基，低级烷氧基（低级）烷基，低级烷基氨基（低级）烷基，低级烷硫基（低级）烷基，低级烷硫基，低级烷氧基，低级烷氧基低级烷基磺酰基（低级）烷基，羟基（低级）烷硫基，二（低级）烷基氨基（低级）烷硫基，四唑基，四唑基硫代，被氧代取代的四唑基硫基（低级）烷基或二氢三嗪基硫代（低级） ; R4为氢或低级烷基; 及其药学上可接受的盐。

8. 发明授权

US4390534A Cephem and cepham compounds 失效
标题翻译： Cephem和cepham化合物
公开(公告)号：US4390534A
公开(公告)日：1983-06-28
申请号：US255301
申请日：1981-04-17
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 , C07D501/56
CPC分类号： C07D209/48 , C07C17/263 , C07D249/12 , C07D257/04 , C07D285/08 , C07D295/21
摘要： This invention relates to novel 7-thiadiazol-oxyimino-3-cephem and cepham 4-carboxylic acid compounds of high antimicrobial activity.
摘要翻译：本发明涉及高抗微生物活性的新型7-噻二唑 - 氧亚氨基-3-头孢烯和头孢类4-羧酸化合物。

9. 发明授权

US4338313A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4338313A
公开(公告)日：1982-07-06
申请号：US180295
申请日：1980-08-22
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 , C07D257/04 , C07D285/08 , C07D295/21 , C07D501/46 , C07D501/20
CPC分类号： C07D209/48 , C07C17/263 , C07D257/04 , C07D285/08 , C07D295/21
摘要： The present invention relates to new cephem compounds, more particularly to new 7-alkoxyimino amino-substituted thiadiazolylacetamido 3-(1-pyridiniomethyl)-3-cephem-4-carboxylate compounds, of high antimicrobial activity, and to pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及新的头孢烯化合物，更具体地涉及高抗微生物活性的新的7-烷氧基亚氨基氨基取代的噻二唑基乙酰氨基-3-（1-吡啶基甲基）-3-头孢烯-4-羧酸酯化合物及其药学上可接受的盐。

10. 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。

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