公开(公告)号：US3647788A

公开(公告)日：1972-03-07

申请号：US3647788D

申请日：1969-06-13

申请人： GLAXO LAB LTD

发明人： CLARK JOHN COLIN ,  COWLEY BRIAN RICHARD ,  GREGORY GORDON IAN ,  KENNEDY JAMES ,  LONG ALAN GIBSON

IPC分类号： A47J43/07 ,  A61K31/545 ,  C07D501/36 ,  C07D99/24

CPC分类号： C07D501/36 ,  A61K31/545 ,  Y10S514/96 ,  Y10S514/962

摘要： 7-ACYLAMIDO CEPHALOSPORANIC ACIDS AND NON-TOXIC SALTS THEREOF HAVING A THIOETHER GROUP AT THE 3-POSITION, THE ACYL GROUP IN THE 7-SUBSTITUENT BEING OF THE ALIPHATIC, HETEROCYCLIC ARALIPHATIC CONTAINING 1 TO 2 HETERO ATOMS, ARALIPHATIC OR CYCLOALIPHATIC SERIES, AN ARALIPHATIC ACYL GROUP HAVING AN ATOMIC WEIGHT SUM OF AT LEAST 120 WHEN THE ARYL MOIETY THEREOF IS A CARBOXYLIC AROMATIC GROUP. SUCH COMPOUNDS ARE ANITBIOTICS MORE RESISTANT TO METABOLIC PROSSESS REDUCING ANTIBIOTIC ACTIVITY THAN ARE CEPHALOSPORINS POSSESSING A 3-ACETOXYMETHYL GROUP AND CERTAIN OF THEM SHOW SIGNIFICANT ABSORPTION AFTER ORAL ADMINISTRATION.

公开(公告)号：US3665003A

公开(公告)日：1972-05-23

申请号：US3665003D

申请日：1968-08-13

申请人： GLAXO LAB LTD

发明人： KENNEDY JAMES ,  LONG ALAN GIBSON ,  UNDERWOOD WILLIAM G E

IPC分类号： A61K31/545 ,  B21C37/26 ,  C07D409/04 ,  C07D409/12 ,  C07D501/04 ,  C07D501/24 ,  C07D501/26 ,  C07D501/32 ,  C07D99/24

CPC分类号： C07D409/04 ,  A61K31/545 ,  C07D409/12 ,  C07D501/26 ,  C07D501/32

摘要： 7 Beta -Acylamidoceph-3-em-4-carboxylic acids having an etherified 3-hydroxymethyl group, physiologically acceptable base or acid addition salts thereof and intermediates for the preparation of the acids and salts.

公开(公告)号：US3479350A

公开(公告)日：1969-11-18

申请号：US3479350D

申请日：1966-12-05

申请人： GLAXO LAB LTD

发明人： EARDLEY STEPHEN ,  GREGORY GORDON IAN ,  LAZENBY JOHN KEVIN ,  LONG ALAN GIBSON

IPC分类号： A61K31/545 ,  C07D501/46 ,  A61K21/00

CPC分类号： C07D501/46 ,  A61K31/545

公开(公告)号：US3668203A

公开(公告)日：1972-06-06

申请号：US3668203D

申请日：1969-06-13

申请人： GLAXO LAB LTD

发明人： CLARK JOHN COLIN ,  KENNEDY JAMES ,  LONG ALAN GIBSON

IPC分类号： A61K31/545 ,  C07D501/36 ,  G01G21/04 ,  C07D99/24

CPC分类号： C07D501/36 ,  A61K31/545 ,  Y10S514/96 ,  Y10S514/962

摘要： 7 Beta -ACYLAMIDOCEPH-3-EM-4-CARBOXYLIC ACIDS HAVING A THIOETHERIFIED METHYL GROUP AT THE 3-POSITION AND PHYSIOLOGICALLY ACCEPTABLE DERIVATIVES THEREOF. The compounds have utility as antibiotics and show significant absorption after oral administration.

摘要翻译： 7β-ACYLAMIDOCEPH-3-EM-4-羧酸在三位和生理上可接受的衍生物中具有三环族甲基。 该化合物具有作为抗生素的效用，并且在口服给药后显示出显着的吸收。

公开(公告)号：US3546219A

公开(公告)日：1970-12-08

申请号：US3546219D

申请日：1968-03-14

申请人： GLAXO LAB LTD

发明人： LONG ALAN GIBSON ,  WILSON EDWARD MCKENZIE ,  GRAHAM WILLIAM

IPC分类号： A61K31/545 ,  C07D501/38 ,  C07D501/44 ,  C08G75/00 ,  C07D99/24

CPC分类号： A61K31/545 ,  C07D501/44 ,  C08G75/00

公开(公告)号：US3900487A

公开(公告)日：1975-08-19

申请号：US16787471

申请日：1971-07-30

申请人： GLAXO LAB LTD

发明人： UNDERWOOD WILLIAM GEORGE ELPHI ,  LONG ALAN GIBSON

IPC分类号： A61K31/425 ,  C07D20060101 ,  C07D495/04 ,  C07D513/04 ,  C07D99/10

CPC分类号： C07D501/08 ,  Y02P20/55

摘要： Novel semisynthetic thiazolidine derivatives of formula

WHERE R1 is the residue of an acyl group R1CO- containing 1-21 carbon atoms are provided by reduction of the corresponding Delta 3-thiazoline, the thiazolidine derivatives being of use in the production of cephalosporins, penicillins and related Beta lactam antibiotics. The preparation and use of such thiazolines and thiazolidines in N-protected forms are also described. The Delta 3-thiazoline starting materials may be obtained from penicillins without changing the configuration of the Beta lactam structure desired in the final product.

公开(公告)号：US3658799A

公开(公告)日：1972-04-25

申请号：US3658799D

申请日：1968-08-13

申请人： GLAXO LAB LTD

发明人： EARDLEY STEPHEN ,  KENNEDY JAMES ,  LONG ALAN GIBSON

IPC分类号： A61K31/545 ,  C07D501/04 ,  C07D501/24 ,  C07D501/26 ,  C07D501/38 ,  E05D15/10 ,  C07D99/24

CPC分类号： C07D501/04 ,  A61K31/545 ,  C07D501/18 ,  C07D501/24 ,  C07D501/26 ,  C07D501/38 ,  Y02P20/55

摘要： 7B-AMINO- AND ACYLAMIDOCEPH-3-EM-4-CARBOXYLIC ACIDS HAVING AT THE 3-POSITION A HALO-, FORMYLOXY-, ISOTHIOCYANATO- OR HALOACETOXYMETHYL GROUP AND SALTS AND ESTERS THEREOF. THESE COMPOUNDS ARE USEFUL AS STARTING COMPOUNDS FOR PREPARING 7B-ACYLAMIDOCEPH-3-EM-4-CARBOXYLIC ACIDS HAVING A GROUP AT THE 3-POSITION, OTHER THAN 3-ACETOXYMETHYL, BY REACTION WITH A NUCLEOPHILE. THE COMPOUNDS PREPARED HAVE MODIFIED ANTIBIOTIC ACTIVITY.

公开(公告)号：US3573294A

公开(公告)日：1971-03-30

申请号：US3573294D

申请日：1968-03-14

申请人： GLAXO LAB LTD

发明人： LONG ALAN GIBSON ,  WILSON EDWARD MCKENZIE ,  GRAHAM WILLIAM

IPC分类号： C07D501/26 ,  C07D99/24

CPC分类号： C07D501/26

摘要： THE INVENTION RELATES TO ANTIBIOTICS WHICH ARE COMPOUNDS OF THE FORMULA

2-(HOOC-),3-(CH3-COO-CH2-),7-(AR-CO-CO-NH-)-2-CEPHEM

IN WHICH AR REPRESENTS AN AROMATIC GROUP HAVING AN ATOMIC WEIGHT SUM OF AT LEAST 78 AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS AND A-CARBONYL DERIVATIVES.