公开(公告)号：US3917830A

公开(公告)日：1975-11-04

申请号：US26313372

申请日：1972-06-15

申请人： GLAXO LAB LTD

发明人： PEARCE DEREK ROGER ,  DAVIS BENJAMIN ,  PEARCE DEREK ROGER ,  CONNOR PAUL

IPC分类号： A61K31/57 ,  A61K38/00 ,  A61K17/00

CPC分类号： B82Y5/00 ,  A61K31/57

摘要： A composition for use by injection as an anaesthetic comprising 3 Alpha -hydroxy 5 Alpha - pregnane - 11,20 dione in solution in an inert organic liquid medium. The composition may be in the form of a solution which also contains water, a non-aqueous solution or an emulsion or microemulsion. The emulsions and microemulsions are preferably of the oil-in-water type. Water-miscible substances which may be used as or in the liquid medium include polyhydroxy alcohols and water-soluble esters and amides. Other substances which may be used as the liquid medium include oils, long chain alcohols and esters, and fatty acid esters.

摘要翻译： 用于作为麻醉剂注射使用的组合物，其在惰性有机液体培养基中在溶液中包含3α-羟基5α-孕烷-11,20二酮。 组合物可以是还含有水，非水溶液或乳液或微乳液的溶液的形式。 乳液和微乳液优选为水包油型。

公开(公告)号：US3915992A

公开(公告)日：1975-10-28

申请号：US22181072

申请日：1972-01-28

申请人： GLAXO LAB LTD

发明人： BAXTER-SMALLWOOD JOHN CHRISTOP ,  COOKSEY ALBERT ROY ,  TOWNSON LEWIS WALTON ,  WALKER DEREK

IPC分类号： C07D333/24 ,  C07C63/54

CPC分类号： C07D333/24

摘要： A process for the preparation of esters of DL-2-amino-2arylacetic acids in which a 2-arylacetic acid ester is nitrosated and then, without separation of the individual nitrosation products, reduced to yield the desired DL-2-amino-2-arylacetic acid ester. 2-Amino-2-arylacetic acids, and more particularly D-2-amino-2phenylacetic acid, are valuable intermediates in the synthesis of anti-biotics of the penicillin and cephalosporin types. The present invention provides a relatively cheap, high yield process for the preparation of esters of DL-2-amino-2-arylacetic acids and also, by a modification, for the preparation of the acids themselves. The process is described and exemplified.

摘要翻译： 制备其中将2-芳基乙酸酯亚硝化然后不分离各个亚硝基化产物的DL-2-氨基-2-芳基乙酸的酯的方法减少，得到所需的DL-2-氨基 - 2-芳基乙酸酯。

公开(公告)号：US3887551A

公开(公告)日：1975-06-03

申请号：US22053772

申请日：1972-01-24

申请人： GLAXO LAB LTD

发明人： CRISP HAROLD ALFRED ,  OUGHTON JOHN FRANCIS ,  SHARP CHRISTOPHER JOHN ,  WILKINSON PETER ALFRED

IPC分类号： C07D501/46 ,  C07D99/24

CPC分类号： C07D501/46

摘要： The invention is concerned with two novel crystalline forms of the antibiotic cephaloridine which are relatively non-hygroscopic compared with previously known forms of cephaloridine and hence possess important advantages in handling and formulation. The novel crystalline forms are characterised in particular by X-ray crystallographic data set out in detail in the following disclosure.

摘要翻译： 本发明涉及两种新型的抗生素头孢哌啶的结晶形式，与先前已知的头孢噻吩形式相比，它们相对不吸湿，因此在处理和制剂方面具有重要的优点。 新颖的结晶形式特别表现在以下公开内容中详细列出的X射线晶体学数据。

公开(公告)号：US3880713A

公开(公告)日：1975-04-29

申请号：US46773374

申请日：1974-05-07

申请人： GLAXO LAB LTD

发明人： FLEMING IAN DUNLOP ,  TURNER MICHAEL KEITH ,  NAPIER EUNICE JEAN

IPC分类号： C07D501/18 ,  C12N9/80 ,  C12P35/02 ,  C12D9/00

CPC分类号： C12P35/02 ,  C12N9/80 ,  Y10S435/847

摘要： A process for the N-deacylation of a 7 Beta -phenoxyacetamido cephalosporin which comprises subjecting the cephalosporin to the action of an amidohydrolase enzyme which is derived from a bacterial source, e.g. Erwinia aroideae, which is free from cells and deleterious enzymes, which is stabilised in solution by the presence of ferrous ions and which is effective to cause optimal N-deacylation at a pH of from 3.5 to 6.5.

摘要翻译： 一种7β-苯氧基乙酰氨基头孢菌素N-脱酰基的方法，其包括使头孢菌素起源于源自细菌来源的酰胺水解酶的作用。 没有细胞和有害酶的欧文氏菌（Erwinia aroideae），其通过亚铁离子的存在而在溶液中稳定，并且在3.5至6.5的pH下有效地引起最佳的N-脱酰基化。

公开(公告)号：US3853860A

公开(公告)日：1974-12-10

申请号：US16787071

申请日：1971-07-30

申请人： GLAXO LAB LTD

发明人： WEIR N

IPC分类号： C07D501/04 ,  C07D501/14 ,  C07D501/20 ,  C07D501/24 ,  C07F9/6561 ,  C07D99/24 ,  C07D99/16

CPC分类号： C07D501/04 ,  C07F9/65613

摘要： A new group of cephalosporin compounds characterized by possessing as 3-position substituent a phosphoranylidene ethyl group. The new compounds can be used as intermediates in the production of cephalosporin antibiotics characterized by possessing an ethyl or substituted ethyl group as 3-position substituent.

摘要翻译： 一组新的头孢菌素化合物，其特征在于具有3-位取代基亚正膦基乙基。 新化合物可用作生产头孢菌素抗生素的中间体，其特征在于具有乙基或取代的乙基作为3-位取代基。

公开(公告)号：US3846416A

公开(公告)日：1974-11-05

申请号：US21318871

申请日：1971-12-28

申请人： GLAXO LAB LTD

发明人： ELPHINSTONE W ,  KENNEDY J ,  LONG A

IPC分类号： C07D501/32 ,  C07D99/24

CPC分类号： C07D501/32

摘要： 7 Beta -Acylamidoceph-3-em-4-carboxylic acids having an etherified hydroxymethyl group at the 3-position and physiologically acceptable derivatives thereof. The compounds have utility as antibiotics and show absorption after oral administration.

摘要翻译： 7位在3-位具有醚化羟甲基的β-酰胺基头孢-3-烯-4-羧酸及其生理上可接受的衍生物。 该化合物具有作为抗生素的作用，并且在口服给药后显示吸收。

公开(公告)号：US3833572A

公开(公告)日：1974-09-03

申请号：US21985872

申请日：1972-01-21

申请人： GLAXO LAB LTD

发明人： CLARK J ,  ELKS J

IPC分类号： A61K31/545 ,  C07D501/04 ,  C07D501/14 ,  C07D501/24 ,  C07D99/24

CPC分类号： C07D501/04

摘要： A PROCESS FOR PREPARING CEPHALOSPORIN COMPOUNDS HAVING A SUBSTITUTED METHYL GROUP AT THE 3-POSITION WHICH COMPRISES REACTING A CORRESPONDING CEPHALOSPORIN COMPOUND HAVING A DIFFERENT SUBSTITUTED METHYL GROUP AT THE 3-POSITION WITH AN ONIUM SALT CORRESPONDING TO THE MEDIA, THE ANION OF THE ONIUM SALT CORRESPONDING TO THE DESIRED METHYL SUBSTITUENT.

公开(公告)号：US3828080A

公开(公告)日：1974-08-06

申请号：US21957472

申请日：1972-01-20

申请人： GLAXO LAB LTD

发明人： PHILLIPPS G ,  MAY P

IPC分类号： C07J3/00 ,  C07C169/52

CPC分类号： C07J3/00

摘要： THE SPECIFICATION DESCRIBES NEW ANDROSTANE COMPOUNDS HAVING ANTI-INFLAMMATORY ACTIVITY. THE NEW ANDROSTANCES DESCRIBED IN THE SPECIFICATION HAVE AN ESTERFIELD 17B-CARBOXYLICC ACID GROUPING WHEREIN THE ALCOHOL RESIDUE COMPRISES EITHER AT LEAST ONE HALOGEN ATOM OR A LOWER ALKOXYBY EITHER AT LEAST ONE HALOGEN ATOM OR A LOWER ALKOXYCARBONYL GROUP OR A (C2-4) LOWER ALKYL GROUP SUBSTITUTED BY A LOWER ACYLOXY GROUP. THE 17A-GROUPING OF THESE ANDROSTANCES IS AN ESTERIFIED HYDROXY GROUP COMPRISING A FORMLY, C2-4 ALKANOYL OR BENZOYL GROUP.

公开(公告)号：US3822297A

公开(公告)日：1974-07-02

申请号：US30524572

申请日：1972-11-10

申请人： GLAXO LAB LTD

发明人： PHILLIPPS G ,  STEPHENSON L

IPC分类号： C07J7/00 ,  A61K20060101 ,  A61K31/57 ,  C07C20060101 ,  C07J20060101 ,  C07J1/00 ,  C07J41/00 ,  C07C167/00 ,  C07C169/00

CPC分类号： C07J75/00 ,  Y10S514/816

摘要： THE INVENTIOON PROVIDES A NEW ANAESTHETIC SUBSTANCE, NAMELY, 3A-HYDROXY-19-NOR-5A-PREGNANE-11,20-DONE, AND A METHOD FOR ITS MANUFACTURE WHEREBY (A) 19 - NOR 5A-PREGNANE-3,11,20-TRIONE IS REDUCED, E.G. USING AN IRIDIUM CATA YST REDUCTION SYSTEM OR (B) 3A-HYDROXY -19NOR-5-APREGNANE-16-ONE-11,20-DIONE IS HYDROGENATED. THE INVENTION ALSO INCLUDES PHARMACEUTICAL COMPOSITIONS CONTAINING THE NEW COMPOUND AND A METHOD OF INDUCING ANAESTHESIA BY ADMINISTRATION OF THE NEW COMPOUND.

公开(公告)号：US3819622A

公开(公告)日：1974-06-25

申请号：US27219972

申请日：1972-07-17

申请人： GLAXO LAB LTD

发明人： COWLEY B ,  WETHERILL L ,  WHITE W ,  GRAHAM W ,  HUMBER D

IPC分类号： A61K31/545 ,  C07D501/10 ,  C07D99/24

CPC分类号： C07D501/10 ,  A61K31/545

摘要： THE INVENTION RELATES TO A PROCESS FOR THE PREPARATION OF 7B-ACYLAMIDO-3-METHYLCEPH-3-EM-4-CARBOXYLIC ACID ESTERS FROM 6B-ACYLAMIDO-PENICILLANIC ACID 1-OXIDE ESTERS IN THE PRESENCE OF AN ACID CATALYST IN ADVANTAGEOUS YIELDS BY CAREFUL SELECTION OF THE SOLVENT USED IN THE REACTION, THE ACID CATALYST AND THE TEMPERATIVE AND DURATION OF THE REACTION.