公开(公告)号：US4399131A

公开(公告)日：1983-08-16

申请号：US146780

申请日：1980-05-05

申请人： Walter Durckheimer ,  Eberhard Ehlers ,  Hubert Seliger ,  Elmar Schrinner

发明人： Walter Durckheimer ,  Eberhard Ehlers ,  Hubert Seliger ,  Elmar Schrinner

IPC分类号： A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61K31/675 ,  A61K31/695 ,  A61P31/04 ,  B23K1/18 ,  B23Q5/033 ,  C07D20060101 ,  C07D277/20 ,  C07D277/40 ,  C07D501/00 ,  C07D501/20 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46 ,  C07D501/59 ,  C07D501/60 ,  C07D519/06

CPC分类号： C07D501/20 ,  Y02P20/55

摘要： What are disclosed are cephem compounds of the formula ##STR1## in which R.sub.1 denotes hydrogen, an optionally substituted alkyl, acyl, arylsulfonyl or alkylsulfonyl group or an amino-protective group which is known from peptide chemistry, R.sub.2 denotes hydrogen or an optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, aralkyl, acyl, aryl, arylsulfonyl, alkylsulfonyl or heterocyclic group, R.sub.3 denotes hydrogen, an ester group or a cation, R.sub.4 denotes hydrogen, a lower alkoxy group or a group which can be converted to this, X denotes a SO group in the R or S configuration or a SO.sub.2 group and A denotes hydrogen, an optionally substituted alkoxy or alkenyloxy group, halogen or a group --CH.sub.2 Y, in which Y represents hydrogen, halogen or the radical of a nucleophilic compound, and in which the R.sub.2 O group is in the syn-position, which compounds are valuable chemotherapeutic agents having a very powerful antimicrobial action against Gram-positive and Gram-negative bacteria and an unexpectedly good action against penicillinase-forming Staphilococci.

摘要翻译： 公开的是头孢烯化合物，其中R 1表示氢，任选取代的烷基，酰基，芳基磺酰基或烷基磺酰基，或由肽化学已知的氨基保护基，R 2表示氢或任选取代的烷基 ，烯基，炔基，环烷基，芳烷基，酰基，芳基，芳基磺酰基，烷基磺酰基或杂环基，R3表示氢，酯基或阳离子，R4表示氢，低级烷氧基或可转化为的基团，X 表示R或S构型中的SO基团或SO 2基团，A表示氢，任选取代的烷氧基或烯氧基，卤素或基团-CH 2 Y，其中Y表示氢，卤素或亲核化合物的基团，以及 其中R2O基团处于顺式位置，哪些化合物是有价值的化学治疗剂，其对革兰氏阳性和革兰氏阴性细菌具有非常强大的抗微生物作用，并且出乎意料地良好 青霉素酶形成葡萄球菌的作用。