公开(公告)号：US3883569A

公开(公告)日：1975-05-13

申请号：US20898571

申请日：1971-12-16

申请人： GLAXO LAB LTD

发明人： PHILLIPPS GORDON HANLEY ,  NEWALL CHRISTOPHER EARLE ,  COOK MARTIN CHRISTOPHER

IPC分类号： A61K20060101 ,  C07C20060101 ,  C07C169/32

CPC分类号： C07J5/00

摘要： Steroids of the 5 Alpha -pregnane series possessing a 3 Alpha hydroxy group, a 10-hydrogen atom or methyl group, an 11-oxo group, a 17 Alpha -hydrogen atom, a 20-oxo group, and a group of the formula -XR at the 21-position wherein -XR represents -OCOR, -OCOOR, -CCOSR or -OCONHR and R represents (a) a solubilising group containing a basic nitrogen atom, (b) a nitrobenzyl group (c) a lower alkyl group (when X is not -OCO-) or (d) a halogenoalkyl group. The steroids possess anaesthetic properties.

摘要翻译： 具有3α-羟基，10-氢原子或甲基，11-氧代基，17α-氢原子，20-氧代基和式 - 基团的5α-孕烷系的类固醇 -XR为21位，其中-XR表示-OCOR，-OCOOR，-CCOSR或-OCONHR，R表示（a）含有碱性氮原子的增溶基团，（b）硝基苄基（c）低级烷基 （当X不为-OCO-）或（d）卤代烷基时。

公开(公告)号：US3926957A

公开(公告)日：1975-12-16

申请号：US46678074

申请日：1974-05-03

申请人： GLAXO LAB LTD

发明人： GREGSON MICHAEL ,  COOK MARTIN CHRISTOPHER ,  GREGORY GORDON IAN

IPC分类号： C07C259/02 ,  C07D307/54 ,  C07D333/24 ,  C07D499/70 ,  C07D499/44

CPC分类号： C07D307/54 ,  C07C259/02 ,  C07D333/24

摘要： WHERE R is a hydrogen atom or an organic group and Ra is a hydrogen atom or an acyl group. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to Beta -lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.

The invention provides novel antibiotic compounds which are 6 Beta -acylamidopenam-3-carboxylic acids and non-toxic derivatives thereof, characterized in that the acylamido group has the structure