公开(公告)号：US4465831A

公开(公告)日：1984-08-14

申请号：US332326

申请日：1981-12-18

申请人： Piero Bellani ,  Goffredo Bolis ,  Giampietro Broccali ,  Roberto Giani ,  Mario Pinza

发明人： Piero Bellani ,  Goffredo Bolis ,  Giampietro Broccali ,  Roberto Giani ,  Mario Pinza

IPC分类号： C07D501/28 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D319/06 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36

CPC分类号： C07D319/06

摘要： There is described a new class of ketohydroxyimino derivatives of cephalosporins of the formula ##STR1## wherein: R is an alkyl radical having from 2 to 4 carbon atoms, a phenyl, or a 5-membered heterocyclic radical which may be substituted, containing nitrogen, oxygen and/or sulphur;R.sup.1 is an acetoxy, carbamoyloxy or S-heterocyclic group, which may be substituted, and the heterocyclic ring is a 5- or 6-membered ring containing one or more nitrogen atoms, alone or combined with sulphur;R.sup.2 is hydrogen, alkyl or acetyl.The present compounds have an interesting broad-spectrum antibacterial activity.

摘要翻译： 描述了一类新的头孢菌素的酮类羟基亚氨基衍生物，其结构式为：其中：R是具有2至4个碳原子的烷基，可被取代的苯基或5元杂环基，含有氮， 氧和/或硫; R1是可以被取代的乙酰氧基，氨基甲酰氧基或S-杂环基，杂环是含有一个或多个单独或与硫结合的氮原子的5-或6-元环; R2是氢，烷基或乙酰基。 本发明化合物具有有趣的广谱抗菌活性。

公开(公告)号：US4329285A

公开(公告)日：1982-05-11

申请号：US221365

申请日：1980-12-29

申请人： Goffredo Bolis ,  Roberto Giani ,  Mario Pinza ,  Giorgio Pifferi ,  Giampietro Broccali

发明人： Goffredo Bolis ,  Roberto Giani ,  Mario Pinza ,  Giorgio Pifferi ,  Giampietro Broccali

IPC分类号： C07D333/24 ,  C07D499/00 ,  C07D499/44 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70

CPC分类号： C07C243/00 ,  C07D333/24 ,  C07D499/00

摘要： Formyl derivatives of hydrazinopenicillins of the formula ##STR1## wherein R is thienyl or phenyl, R' is hydrogen, formyl or alkyl containing from 1 to 3 carbon atoms and R" is hydrogen or formyl, provided that at least one of R' and R" is a formyl group, the carbon atom with the asterisk indicating a center of asymmetry of the molecule, and pharmaceutically acceptable salts and esters thereof, as mixture or as separated epimers. These compounds have antibacterial activity against Gram-negative and Gram-positive bacteria and are prepared by a process wherein the corresponding hydrazinopenicillin is reacted under anhydrous conditions with acetoformic anhydride to give the desired compounds.

摘要翻译： 其中R是噻吩基或苯基，R'是氢，甲酰基或含有1至3个碳原子的烷基，R“是氢或甲酰基，其中R'和R'中至少有一个是式 R“是甲酰基，具有星号的碳原子表示分子的不对称中心，以及其药学上可接受的盐和酯，作为混合物或分离的差向异构体。 这些化合物对革兰氏阴性和革兰氏阳性菌具有抗菌活性，并通过其中相应的肼青霉素在无水条件下与乙酰甲酸酐反应得到所需化合物的方法制备。