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1.发明授权Process to prepare 7-substituted cephalosporins or 6-substituted penicillins 失效制备7-取代头孢菌素或6-取代青霉素的方法
公开(公告)号：US4447602A
公开(公告)日：1984-05-08
申请号：US803332
申请日：1977-06-03
IPC分类号： C07D499/00 , C07D499/21 , C07D501/57 , C07D501/04 , C07D499/04
CPC分类号： C07D499/00
摘要： A process is provided which yields derivatives of cephalosporins and penicillins. The process starts with 7-acylaminocephalosporin, or 6-acylaminopenicillin, then the latter compounds are treated with an organolithium compound, followed with t-butyl-hypochlorite. Finally, a defined reagent is added yielding a side chain on the carbon adjacent to the amino-nitrogen. Novel intermediate compounds are also described. The end compounds prepared are active against both gram-positive and gram-negative bacteria.
摘要翻译： 提供了产生头孢菌素和青霉素衍生物的方法。 该过程从7-酰基氨基头孢菌素或6-酰基氨基青霉素开始，然后后者化合物用有机锂化合物处理，然后用叔丁基次氯酸盐处理。 最后，加入定义的试剂，在邻近氨基氮的碳上产生侧链。 还描述了新的中间体化合物。 所制备的最终化合物对革兰氏阳性菌和革兰氏阴性细菌均有活性。
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公开(公告)号：US4343937A
公开(公告)日：1982-08-10
申请号：US145160
申请日：1980-04-30
IPC分类号： C07D501/18
CPC分类号： C07D501/18 , C07D501/57 , Y02P20/582
摘要： Process and intermediate products useful in the preparation of cephalosporin compounds having a substituent at the 7-position in place of hydrogen are provided. The new cephalosporin compounds are active against various gram-negative and gram-positive organisms.
摘要翻译： 提供了可用于制备在7-位具有取代基而不是氢的头孢菌素化合物的方法和中间产物。 新的头孢菌素化合物对各种革兰氏阴性和革兰氏阳性菌有活性。
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公开(公告)号：US4219462A
公开(公告)日：1980-08-26
申请号：US492812
申请日：1974-07-29
IPC分类号： C07D277/06 , C07D499/00 , C07D499/42
CPC分类号： C07D499/00 , C07D277/06
摘要： New 6-methyl penicillins and the corresponding 6-aminopenicillanic acid compounds and processes for the preparation of these penicillins are provided. The new penicillins are antibiotics which are active against various gram-negative and gram-positive pathogens.
摘要翻译： 提供新的6-甲基青霉素和相应的6-氨基青霉烷酸化合物以及这些青霉素的制备方法。 新青霉素是抗各种革兰氏阴性和革兰氏阳性病原体的抗生素。
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公开(公告)号：US4014873A
公开(公告)日：1977-03-29
申请号：US528109
申请日：1974-11-29
IPC分类号： C07D501/04
CPC分类号： C07D501/04 , C07D501/28
摘要： New 7-diacylimido cephalosporins are produced by reacting 7-acylamido cephalosporins with an acylating agent in the presence of a silyl reagent. The 7-diacylimido cephalosporins are cleaved to produce cephalosporins containing a different acylamido moiety. Thus, the aminoadipoyl group of cephalosporins produced by fermentation is replaced by a different acyl group by the process of the present invention. The cephalosporins produced are antibiotics having enhanced activity against gram-negative and gram-positive pathogens.
摘要翻译： 新的7-二酰基亚氨基头孢菌素是通过7-酰基酰氨基头孢菌素与酰化剂在甲硅烷基试剂存在下反应生成的。 裂解7-二酰基亚氨基头孢菌素以产生含有不同酰基酰氨基部分的头孢菌素。 因此，通过本发明的方法，通过发酵产生的头孢菌素的氨基己二酰基被不同的酰基所取代。 产生的头孢菌素是对革兰氏阴性和革兰氏阳性病原体具有增强活性的抗生素。
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公开(公告)号：US4775669A
公开(公告)日：1988-10-04
申请号：US83938
申请日：1987-07-31
IPC分类号： C07D205/08 , C07D477/10 , C07D498/04 , C07F7/18 , C07F9/568 , C07D487/04 , A61K31/40
CPC分类号： C07D205/08 , C07D477/10 , C07F7/186 , C07F9/5683
摘要： Disclosed are 1-carba-2-penem-3-carboxylic acids of the following structure: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, aryl, and aralkyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmacetical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
摘要翻译： 公开了以下结构的1-咔二-2-青霉烯-3-羧酸：其中R 1，R 2和R 3特别独立地选自氢，烷基，芳基和芳烷基。 这些化合物及其药学上可接受的盐，酯和酰胺衍生物可用作抗生素。 还公开了制备这种化合物的方法，包含这些化合物的药物组合物和治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。
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公开(公告)号：US4154845A
公开(公告)日：1979-05-15
申请号：US831465
申请日：1977-09-08
IPC分类号： C07C57/38 , C07C57/72 , C07D499/44
摘要： Novel 6-methoxy and 6-thioalkyl-6-acylamido-penicillanic acids and their non-toxic pharmaceutically-acceptable salts, esters and amides which are useful as antibiotics. The products are prepared by treating an ester of 6-substituted-6-aminopenicillanic acid with an acylating agent followed by removal of the ester group. Also disclosed are novel intermediates.
摘要翻译： 新的6-甲氧基和6-硫烷基-6-酰氨基 - 青霉烷酸及其无毒的药学上可接受的盐，酯和酰胺，其可用作抗生素。 通过用酰化剂处理6-取代-6-氨基青霉烷酸的酯，然后除去酯基来制备产物。 还公开了新型中间体。
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7.发明授权7-(Substituted methyl)-3-(substituted thio)-cephalosporins, derivatives and pharmaceutical compositions containing them 失效7-（取代的甲基）-3-（取代的硫代） - 头孢菌素，含有它们的衍生物和药物组合物
公开(公告)号：US4150156A
公开(公告)日：1979-04-17
申请号：US903455
申请日：1978-05-08
IPC分类号： C07D501/00 , A61K31/545
CPC分类号： C07D501/00
摘要： Disclosed are antibiotic 3-(substituted thio)-7-(substituted methyl) cephalosporins, derivatives and analogues thereof; wherein the methyl substituent is, inter alia, hydroxyl, ketonic oxygen, imino nitrogen, amino or mercapto. Also disclosed are processes for the preparation of such compounds and their pharmaceutically acceptable salt, ester and amide derivatives; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
摘要翻译： 公开了抗生素3-（取代的硫代）-7-（取代的甲基）头孢菌素，其衍生物和类似物; 其中甲基取代基尤其是羟基，酮氧，亚氨基氮，氨基或巯基。 还公开了制备这些化合物及其药学上可接受的盐，酯和酰胺衍生物的方法; 包含这些化合物的药物组合物; 和治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。
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公开(公告)号：US4107432A
公开(公告)日：1978-08-15
申请号：US790793
申请日：1977-04-25
IPC分类号： C07D501/20 , C07D501/32 , C07D501/34
CPC分类号： C07D501/20 , C07D501/28
摘要： New 7-diacylimido cephalosporins are produced by reacting 7-acylamido cephalosporins with an acylating agent in the presence of a silyl reagent. The 7-diacylimido cephalosporins are cleaved to produce cephalosporins containing a different acylamido moiety. Thus, the aminoadipoyl group of cephalosporins produced by fermentation is replaced by a different acyl group by the process of the present invention. The cephalosporins produced are antibiotics having enhanced activity against gram-negative and gram-positive pathogens.
摘要翻译： 新的7-二酰基亚氨基头孢菌素是通过7-酰基酰氨基头孢菌素与酰化剂在甲硅烷基试剂存在下反应生成的。 裂解7-二酰基亚氨基头孢菌素以产生含有不同酰基酰氨基部分的头孢菌素。 因此，通过本发明的方法，通过发酵产生的头孢菌素的氨基己二酰基被不同的酰基所取代。 产生的头孢菌素是对革兰氏阴性和革兰氏阳性病原体具有增强活性的抗生素。
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公开(公告)号：US4035359A
公开(公告)日：1977-07-12
申请号：US599266
申请日：1975-07-25
IPC分类号： C07C57/38 , C07C57/72 , C07D499/00 , C07D499/58 , C07D499/46
CPC分类号： C07D499/00 , C07C57/38 , C07C57/72
摘要： Novel 6-methoxy and 6-thioalkyl-6-acylamido-penicillanic acids and their non-toxic pharmaceutically-acceptable salts, esters and amides which are useful as antibiotics. The products are prepared by treating an ester of 6-substituted-6-aminopenicillanic acid with an acylating agent followed by removal of the ester group. Also disclosed are novel intermediates.
摘要翻译： 新的6-甲氧基和6-硫烷基-6-酰氨基 - 青霉烷酸及其无毒的药学上可接受的盐，酯和酰胺，其可用作抗生素。 通过用酰化剂处理6-取代-6-氨基青霉烷酸的酯，然后除去酯基来制备产物。 还公开了新型中间体。
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10.发明授权
公开(公告)号：US4873324A
公开(公告)日：1989-10-10
申请号：US307135
申请日：1989-02-06
IPC分类号： C07D205/08 , C07D498/04 , C07F7/18
CPC分类号： C07F7/186 , C07D205/08 , Y02P20/55
摘要： Compounds are disclosed of the structural formula: ##STR1## wherein R.sup.2 is independently selected from hydrogen, linear or branched C.sub.1 -C.sub.3 alkyl, which can be substituted with fluoro, hydroxy, or protected hydroxy, R.sup.3 is hydrogen or a protecting group, X is sulfur or selenium, Q is hydroxymethyl, carboxy or C.sub.1 -C.sub.4 alkoxycarbonyl, and R.sup.1 is C.sub.1 -C.sub.4 alkyl, C.sub.6 -C.sub.10 aryl, or pyridyl which can be substituted with C.sub.1 -C.sub.4 alkyl, alkoxy and nitro; such compound are useful for selectively obtaining 1-.beta.-methylcarbapenem intermediates.
摘要翻译： 公开了以下结构式的化合物：其中R 2独立地选自氢，直链或支链C 1 -C 3烷基，其可以被氟，羟基或保护的羟基取代，R 3是氢或保护基，X是 硫或硒，Q是羟甲基，羧基或C 1 -C 4烷氧基羰基，R 1是可被C 1 -C 4烷基，烷氧基和硝基取代的C 1 -C 4烷基，C 6 -C 10芳基或吡啶基; 这种化合物可用于选择性地获得1-β-甲基碳青霉烯中间体。
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