公开(公告)号：DK147513C

公开(公告)日：1985-03-18

申请号：DK168778

申请日：1978-04-18

Applicant: GLAXO LAB LTD

Inventor： GREGSON MICHAEL

IPC: C07D501/26 ,  A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07C68/02 ,  C07C68/06 ,  C07D20060101 ,  C07D501/00 ,  C07D501/20 ,  C07D501/34 ,  C07D501/60

Abstract: Cephalosporin derivatives of the formula: in which R denotes lower alkyl and R denotes hydrogen or lower alkyl. In contrast to the free carboxylic acids, these novel esters are very well absorbed by the gastrointestinal tract and then hydrolyse rapidly to give corresponding carboxylic acids having a broad spectrum antibiotic action. They are prepared by esterification of the carboxyl group in the 4-position, by N-acylation of the 7-aminocephemcarboxylic acid ester or by carbamoylation of the hydroxymethyl group in the 3-position.

公开(公告)号：AU521098B2

公开(公告)日：1982-03-18

申请号：AU3518778

申请日：1978-04-18

Applicant: GLAXO LAB LTD

Inventor： GREGSON MICHAEL

IPC: C07D501/26 ,  A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07C68/02 ,  C07C68/06 ,  C07D20060101 ,  C07D501/00 ,  C07D501/20 ,  C07D501/34 ,  C07D501/60

Abstract: Cephalosporin derivatives of the formula: in which R denotes lower alkyl and R denotes hydrogen or lower alkyl. In contrast to the free carboxylic acids, these novel esters are very well absorbed by the gastrointestinal tract and then hydrolyse rapidly to give corresponding carboxylic acids having a broad spectrum antibiotic action. They are prepared by esterification of the carboxyl group in the 4-position, by N-acylation of the 7-aminocephemcarboxylic acid ester or by carbamoylation of the hydroxymethyl group in the 3-position.

公开(公告)号：AU514236B2

公开(公告)日：1981-01-29

申请号：AU2228877

申请日：1977-02-15

Applicant: GLAXO LAB LTD

Inventor： GREGSON MICHAEL ,  SYKES RICHARD BROOK

IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07B57/00 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/20 ,  C07D501/30 ,  C07D501/34 ,  C07D501/60

Abstract: The invention provides novel antibiotic cefuroxime esters of the formula (wherein R1 is a primary or secondary alkyl group containing 1 to 4 carbon atoms and R2 is a primary or secondary alkyl group containing 1 to 6 carbon atoms provided that at least one of the groups R1 and R2 is methyl). These compounds are useful as orally administrable broad spectrum antibiotics.

公开(公告)号：CA1056373A

公开(公告)日：1979-06-12

申请号：CA215228

申请日：1974-12-04

Applicant: GLAXO LAB LTD

Inventor： GREGORY GORDON I ,  GREGSON MICHAEL ,  WEBB GODFREY B

IPC: C07D307/46 ,  C07D307/54 ,  C07D333/22 ,  C07D333/24 ,  C07D499/00 ,  C07D499/44 ,  C07D499/46 ,  C07D501/20 ,  C07D501/30 ,  C07D501/36 ,  C07D501/42 ,  C07D501/57

Abstract: Novel antibiotic compounds which are 7.beta.-acrylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof wherein the acrylamido group has the structure wherein A is aryl group and B is a substituted or unsubstituted lower alkyl, lower alkenyl or lower alkynyl group; or an aryl, cycloalkyl or cycloalkenyl group. These compounds possess antibacterial activity against gram-positive and gram-negative organisms coupled with stability to .beta.-lactamases. The invention further relates to the administration of the compounds.

公开(公告)号：DE2816873A1

公开(公告)日：1978-11-02

申请号：DE2816873

申请日：1978-04-18

Applicant: GLAXO LAB LTD

Inventor： GREGSON MICHAEL

IPC: C07D501/26 ,  A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07C68/02 ,  C07C68/06 ,  C07D20060101 ,  C07D501/00 ,  C07D501/20 ,  C07D501/34 ,  C07D501/60

Abstract: Cephalosporin derivatives of the formula: in which R denotes lower alkyl and R denotes hydrogen or lower alkyl. In contrast to the free carboxylic acids, these novel esters are very well absorbed by the gastrointestinal tract and then hydrolyse rapidly to give corresponding carboxylic acids having a broad spectrum antibiotic action. They are prepared by esterification of the carboxyl group in the 4-position, by N-acylation of the 7-aminocephemcarboxylic acid ester or by carbamoylation of the hydroxymethyl group in the 3-position.

公开(公告)号：DE2706413A1

公开(公告)日：1977-08-18

申请号：DE2706413

申请日：1977-02-15

Applicant: GLAXO LAB LTD

Inventor： GREGSON MICHAEL ,  SYKES RICHARD BROOK

IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07B57/00 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/20 ,  C07D501/30 ,  C07D501/34 ,  C07D501/60

Abstract: The invention provides novel antibiotic cefuroxime esters of the formula (wherein R1 is a primary or secondary alkyl group containing 1 to 4 carbon atoms and R2 is a primary or secondary alkyl group containing 1 to 6 carbon atoms provided that at least one of the groups R1 and R2 is methyl). These compounds are useful as orally administrable broad spectrum antibiotics.

公开(公告)号：DE2457358A1

公开(公告)日：1975-06-12

申请号：DE2457358

申请日：1974-12-04

Applicant: GLAXO LAB LTD

Inventor： GREGORY GORDON IAN ,  GREGSON MICHAEL ,  WEBB GODFREY BASIL

IPC: C07D307/46 ,  C07D307/54 ,  C07D333/22 ,  C07D333/24 ,  C07D499/00 ,  C07D499/44 ,  C07D499/46 ,  C07D501/20 ,  C07D501/30 ,  C07D501/36 ,  C07D501/42 ,  C07D501/57 ,  C07D501/34 ,  C07D499/76

Abstract: Novel antibiotic compounds which are 7 beta -acrylamidoceph-3-em-4-carboxylic acids, and 6 beta -acrylamidopenam-3-carboxylic acids and non-toxic derivatives thereof wherein the acrylamido group has the structure wherein A is aryl group and B is a substituted or unsubstituted lower alkyl, lower alkenyl or lower alkynyl group; or an aryl, cycloalkyl or cycloalkenyl group. These compounds possess antibacterial activity against gram-positive and gram-negative organisms coupled with stability to beta -lactamases. The invention further relates to the administration of the compounds.

公开(公告)号：AU3845072A

公开(公告)日：1973-08-02

申请号：AU3845072

申请日：1972-01-28

Applicant: GLAXO LAB LTD

Inventor： GREGSON MICHAEL ,  COOK MARTIN CHRISTOPHER ,  GREGORY GORDON IAN

IPC: C07C259/02 ,  C07D307/54 ,  C07D333/24 ,  C07D499/64 ,  C07D501/20 ,  C07D501/24 ,  C07D501/38 ,  C07D99/16 ,  A61K21/00 ,  C07C119/00 ,  C07C121/02 ,  C07D99/24