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1. 发明授权

US4618606A Antibiotic 7-(thiazolyl)-3-(pyrazinylmethyl) or (pyridazinylmethyl) cephalosporins 失效
标题翻译：抗生素7-（噻唑基）-3-（吡嗪基甲基）或（哒嗪基甲基）头孢菌素
公开(公告)号：US4618606A
公开(公告)日：1986-10-21
申请号：US552468
申请日：1983-11-16
申请人： Hiroshi Sadaki , Hiroyuki Imaizumi , Takashi Nagai , Kenji Takeda , Isao Myokan , Takihiro Inaba , Yasuo Watanabe , Yoshikazu Fukuoka , Shinzaburo Minami , Isamu Saikawa
发明人： Hiroshi Sadaki , Hiroyuki Imaizumi , Takashi Nagai , Kenji Takeda , Isao Myokan , Takihiro Inaba , Yasuo Watanabe , Yoshikazu Fukuoka , Shinzaburo Minami , Isamu Saikawa
IPC分类号： C07D241/18 , C07D405/04 , C07D501/18 , C07D501/46 , A61K31/545
CPC分类号： C07D405/04 , C07D241/18 , Y02P20/55
摘要： The invention relates to antibiotic compounds of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl-protecting group; R.sup.2 represents a group of the formula: ##STR2## R.sup.3 represents a hydrogen atom or an alkoxy group; R.sup.4 represents a hydrogen atom or a halogen atom; R.sup.5 represents a hydrogen atom or a protected or unprotected amino group; A represents a group of the formula, --CH.sub.2 -- or a group of the formula, ##STR3## or a group of the formula, ##STR4## and the bond means that the compound may be a synisomer or an anti-isomer or a mixture thereof.
摘要翻译：本发明涉及下式的抗生素化合物：其中R 1表示氢原子或羧基保护基; R 2表示下式的基团：R 3表示氢原子或烷氧基; R4表示氢原子或卤素原子; R5表示氢原子或被保护或未被保护的氨基; A代表下式的基团-CH 2 - 或下式的基团或下式的基团和键意指化合物可以是异构体或反式异构体或混合物其中。

2. 发明授权

US5300497A Penam derivatives and salts thereof, process for producing the same and antibacterial agent comprising the same 失效
标题翻译： Penam衍生物及其盐，其制备方法和含有它们的抗菌剂
公开(公告)号：US5300497A
公开(公告)日：1994-04-05
申请号：US957372
申请日：1992-10-07
申请人： Hirokazu Ochiai , Yasuo Watanabe , Yoshiharu Murotani , Hirohiko Fukuda , Osamu Yoshino , Shinzaburo Minami , Toshio Hayashi , Kaishu Momonoi
发明人： Hirokazu Ochiai , Yasuo Watanabe , Yoshiharu Murotani , Hirohiko Fukuda , Osamu Yoshino , Shinzaburo Minami , Toshio Hayashi , Kaishu Momonoi
IPC分类号： C07D499/00 , C07D499/21 , C07D499/87 , C07D519/06 , A61K31/425
CPC分类号： C07D499/00 , Y02P20/55
摘要： A penam derivative represented by the following general formula or a salt thereof: ##STR1## wherein R.sup.1 represents a hydrogen atom, an amino-protecting group or an acyl group; R.sup.2 represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a lower alkoxy group, a lower alkylthio group or a formamido group; R.sup.4 represents an protected or unprotected carboxyl group or a carboxylato group; R represents a group of the formula, --NHR.sup.5 or --NR.sup.5 R.sup.6 (in which R.sup.5 and R.sup.6, which may be the same or different, represent protected or unprotected hydroxyl groups, cyano groups, sulfo groups, or unsubstituted or substituted lower alkyl, aryl, acyl, carbamoyl, sulfamoyl, lower alkylsulfonyl or heterocyclic groups) or a group of the formula, --N.dbd.CR.sup.7 R.sup.8 (in which R.sup.7 and R.sup.8, which may be the same or different, represent hydrogen atoms or protected or unprotected carboxyl groups, cyano groups or unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl, aryl, amino, acyl, acyloxy, carbamoyl, carbamoyloxy, sulfamoyl, lower alkylthio, ureido or heterocyclic groups, or R.sup.7 and R.sup.8 may form a cycloalkene or a heterocyclic ring with the carbon atom to which R.sup.7 and R.sup.8 are attached); and n represents 1 or 2. The above penam derivative or its salt is very effective as antibacterial agents.
摘要翻译：由以下通式表示的penam衍生物或其盐：其中R 1表示氢原子，氨基保护基或酰基; R2表示氢原子或低级烷基; R3表示氢原子，低级烷氧基，低级烷硫基或甲酰氨基; R4代表受保护或未保护的羧基或羧基; R表示式-NHR 5或-NR 5 R 6基团（其中R 5和R 6可以相同或不同，表示保护或未被保护的羟基，氰基，磺基或未取代或取代的低级烷基，芳基，酰基，氨基甲酰基，氨磺酰基，低级烷基磺酰基或杂环基）或下式基团-N = CR7R8（其中R7和R8可以相同或不同，表示氢原子或被保护或未被保护的羧基，氰基或未取代或取代的低级烷基，低级烯基，低级炔基，芳基，氨基，酰基，酰氧基，氨基甲酰基，氨基甲酰氧基，氨磺酰基，低级烷硫基，脲基或杂环基，或者R7和R8可以与碳形成环烯或杂环 R7和R8所连接的原子）; 并且n表示1或2.上述阳am衍生物或其盐作为抗菌剂是非常有效的。

3. 发明授权

US5185330A Penam derivatives and salts thereof, and antibacterial agent comprising the same 失效
标题翻译： PENAM衍生物及其盐，以及包含其的抗菌剂
公开(公告)号：US5185330A
公开(公告)日：1993-02-09
申请号：US540697
申请日：1990-06-20
申请人： Hirokazu Ochiai , Yasuo Watanabe , Yoshiharu Murotani , Hirohiko Fukuda , Osamu Yoshino , Shinzaburo Minami , Toshio Hayashi , Kaishu Momonoi
发明人： Hirokazu Ochiai , Yasuo Watanabe , Yoshiharu Murotani , Hirohiko Fukuda , Osamu Yoshino , Shinzaburo Minami , Toshio Hayashi , Kaishu Momonoi
IPC分类号： C07D499/00 , C07D499/21 , C07D499/87 , C07D519/06
CPC分类号： C07D499/00 , Y02P20/55
摘要： A penam derivative represented by the following general formula or a salt thereof: ##STR1## wherein R.sup.1 represents a hydrogen atom, an amino-protecting group or an acyl group; R.sup.2 represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a lower alkoxy group, a lower alkylthio group or a formamido group; R.sup.4 represents a protected or unprotected carboxy group or a craboxylato group; R represents a group of the formula, --NHR.sup.5 or --NR.sup.5 R.sup.6 (in which R.sup.5 and R.sup.6, which may be the same or different, represent protected or unprotected hydroxyl groups, cyano groups, sulfo groups, or unsubstituted or substituted lower alkyl, aryl, acyl, carbamoyl, sulfamoyl, lower alkylsulfonyl or heterocyclic groups) or a group of the formula, --N.dbd.CR.sup.7 R.sup.8 (in which R.sup.7 and R.sup.8, which may be the same or different, represent hydrogen atoms or protected or unprotected carboxyl groups, cyano groups or unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl, aryl, amino, acyl, acyloxy, carbamoyl, carbamoyloxy, sulfamoyl, lower alkylthio, ureido or heterocyclic groups, or R.sup.7 and R.sup.8 may form a cycloalkene or a heterocyclic ring with the carbon atom to which R.sup.7 and R.sup.8 are attached); and n represents 1 or 2. The above penam derivative or its salt is very effective as antibacterial agents.
摘要翻译：由以下通式表示的penam衍生物或其盐：其中R 1表示氢原子，氨基保护基或酰基; R2表示氢原子或低级烷基; R3表示氢原子，低级烷氧基，低级烷硫基或甲酰氨基; R4表示保护或未保护的羧基或酰胺基; R表示式-NHR 5或-NR 5 R 6基团（其中R 5和R 6可以相同或不同，表示保护或未被保护的羟基，氰基，磺基或未取代或取代的低级烷基，芳基，酰基，氨基甲酰基，氨磺酰基，低级烷基磺酰基或杂环基）或下式基团-N = CR7R8（其中R7和R8可以相同或不同，表示氢原子或被保护或未被保护的羧基，氰基或未取代或取代的低级烷基，低级烯基，低级炔基，芳基，氨基，酰基，酰氧基，氨基甲酰基，氨基甲酰氧基，氨磺酰基，低级烷硫基，脲基或杂环基，或者R7和R8可以与碳形成环烯或杂环 R7和R8所连接的原子）; 并且n表示1或2.上述阳am衍生物或其盐作为抗菌剂是非常有效的。

4. 发明授权

US4717767A 7-amino-3-(pyrazinylmethyl) or (pyridazinylmethyl)-cephalosporins 失效
标题翻译： 7-氨基-3-（吡嗪基甲基）或（哒嗪基甲基） - 头孢菌素
公开(公告)号：US4717767A
公开(公告)日：1988-01-05
申请号：US860317
申请日：1986-07-22
申请人： Hiroshi Sadaki , Hiroyuki Imaizumi , Takashi Nagai , Kenji Takeda , Isao Myokan , Takihiro Inaba , Yasuo Watanabe , Yoshikazu Fukuoka , Shinzaburo Minami , Isamu Saikawa
发明人： Hiroshi Sadaki , Hiroyuki Imaizumi , Takashi Nagai , Kenji Takeda , Isao Myokan , Takihiro Inaba , Yasuo Watanabe , Yoshikazu Fukuoka , Shinzaburo Minami , Isamu Saikawa
IPC分类号： C07D241/18 , C07D405/04 , C07D501/18 , C07D501/46
CPC分类号： C07D405/04 , C07D241/18 , Y02P20/55
摘要： This invention relates to a 7-amino-3-(pyrazinylmethyl)- or (pyridazinylmethyl)-cephalosporins of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl-protecting group; R.sup.2 represents a group of the formula: ##STR2## in which R.sup.6 represents a hydrogen atom, a C.sub.1-5 alkyl group or a di-C.sub.1-5 alkylamino group; R.sup.13 represents a C.sub.1-5 alkyl group; and R.sup.28 represents an amino group.
摘要翻译：本发明涉及下式的7-氨基-3-（吡嗪基甲基） - 或（哒嗪基甲基） - 头孢菌素，其中R 1表示氢原子或羧基保护基; R 2表示下式的基团：其中R 6表示氢原子，C 1-5烷基或二-C 1-5烷基氨基; R13表示C1-5烷基; R28表示氨基。

5. 发明授权

US4698352A 4-oxo-1,4-dihydronicotinic acid derivatives, salts thereof, and antibacterial agents containing the same 失效
标题翻译： 4-氧代-1,4-二氢烟酸衍生物，其盐和含有它们的抗菌剂
公开(公告)号：US4698352A
公开(公告)日：1987-10-06
申请号：US546165
申请日：1983-10-27
申请人： Hirokazu Narita , Yoshinori Konishi , Jun Nitta , Shunjiro Misumi , Hideyoshi Nagaki , Isao Kitayama , Yoriko Nagai , Yasuo Watanabe , Nobuyuki Matsubara , Shinzaburo Minami , Isamu Saikawa
发明人： Hirokazu Narita , Yoshinori Konishi , Jun Nitta , Shunjiro Misumi , Hideyoshi Nagaki , Isao Kitayama , Yoriko Nagai , Yasuo Watanabe , Nobuyuki Matsubara , Shinzaburo Minami , Isamu Saikawa
IPC分类号： C07D213/63 , C07D209/20 , C07D211/90 , C07D213/55 , C07D213/80 , C07D215/14 , C07D215/38 , C07D215/40 , C07D249/08 , C07D307/81 , C07D317/66 , C07D333/24 , C07D333/28 , C07D333/60 , C07D401/04 , C07D405/04 , C07D409/04 , C07D409/12 , C07D417/04 , C07D521/00 , A61K31/455 , C07D401/02 , C07D405/02
CPC分类号： C07D213/80 , C07D209/20 , C07D211/90 , C07D213/55 , C07D215/14 , C07D215/38 , C07D215/40 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/81 , C07D317/66 , C07D333/24 , C07D333/28 , C07D333/60 , C07D401/04 , C07D405/04 , C07D409/04 , C07D409/12 , C07D417/04 , Y02P20/55
摘要： This invention relates to a novel 4-oxo-1,4-dihydronicotinic acid derivative ##STR1## or a salt thereof, wherein R.sup.1 is hydrogen or carboxyl-protecting group;R.sup.2 is substituted phenyl and naphthyl, or a substituted or unsubstituted heterocyclic group; andR.sup.3 is haloalkyl, aminoalkyl, or substituted or unsubstituted alkenyl, phenylalkenyl, naphthylalkenyl, phenylalkyl, naphthylalkyl, phenylalkynyl, naphthylalkynyl, heterocyclic alkyl, heterocyclic alkenyl, phenyl, naphthyl, cycloalkyl, cycloalkenyl, carboxylic acyl, iminoalkyl, heterocyclic or bridged hydrocarbon, which has a broad antibacterial spectrum and a low toxicity, and are useful for treatment of diseases of human beings and animals, to a process for producing the same and to an antibacterial agent containing the same.
摘要翻译：本发明涉及一种新的4-氧代-1,4-二氢烟酸衍生物或其盐，其中R 1是氢或羧基保护基; R2是取代的苯基和萘基，或取代或未取代的杂环基团; 苯基，萘基烷基，苯基炔基，萘基炔基，杂环烷基，杂环烯基，苯基，萘基，环烷基，环烯基，羧酰基，亚氨基烷基，杂环或桥连烃，其中R 3为卤代烷基，氨基烷基或取代或未取代的链烯基具有广泛的抗菌谱和低毒性，并且可用于治疗人和动物的疾病，其制备方法和含有它们的抗菌剂。

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