公开(公告)号：US3804832A

公开(公告)日：1974-04-16

申请号：US13835371

申请日：1971-04-28

申请人： CIBA GEIGY CORP

发明人： BICKEL H ,  MUELLER J

IPC分类号： A61K20060101 ,  C07D20060101 ,  C07D501/36 ,  C07D99/24

CPC分类号： C07D501/36

摘要： COMPOUNDS OF THE FORMULA

2-(HOOC-),3-(R3-S-CH2-),7-(R1-OOC-CH(-R2)-CO-NH-)-2-CEPHEM

IN WHICH R1 REPRESENTS A LOWER ALKYL RESIDUE, AND R2 REPRESENTS HYDROGEN OR A LOWER ALKOXY-CARBONYL RESIDUE, AND IN WHICH R3 REPRESENTS A HETEROCYCLIC RESIDUE OF AROMATIC CHARACTER BOUND THROUGH A CARBON ATOMS THE THE SULPHUR ATOM, AND WHICH HETEROCYCLIC RESIDUE CONTAINS AT LEAST 2 NITROGEN ATOMS AND ALSO A FURTHER HETEROATOM WHICH IS SELECTED FROM THE GROUP CONSISTING OF NITROGEN, OXYGEN AND SULPHUR. THEY HAVE ANTIMICROBIAL ACTIVITY.

公开(公告)号：US3778432A

公开(公告)日：1973-12-11

申请号：US3778432D

申请日：1971-12-13

申请人： MERCK & CO INC

发明人： PINES S

IPC分类号： C07D499/00 ,  C07D499/10 ,  C07D501/04 ,  C07D99/24

CPC分类号： C07D499/00

摘要： PREPARATION OF 6-AMINO-6-METHOXY PENICILLINS AND 7AMINO-7-METHOXY-3-CEPHEM-4-CARBOXYLIC ACID AND ITS ESTERS WHICH ARE USEFUL AS INTERMEDIATES IN THE PRODUCTION OF THE ANTIBIOTICS 7-ACYLAMIDO-7-METHOXY-3-CEPHEM-4-CARBOXYLIC ACID AND ITS ESTERS AND SALTS. THE PRODUCTS ARE PREPARED BY REMOVAL OF THE SUBSTITUTED OXYCARBONYL GROUP FROM A 6(OR 7)-SUBSTITUTED OXYCARBONYLAMINO-6(OR 7)METHOXY COMPOUND BY REDUCTION EMPLOYING A CHEMICAL, CATALYTIC OR PHOTOCHEMICAL METHOD UNDER NON-ACIDIC CONDITIONS.

公开(公告)号：US3775410A

公开(公告)日：1973-11-27

申请号：US3775410D

申请日：1971-11-29

申请人： CHRISTENSEN B ,  FIRESTONE R

发明人： CHRISTENSEN B ,  FIRESTONE R

IPC分类号： C07D501/04 ,  C07D499/00 ,  C07D501/57 ,  C07D99/16 ,  C07D99/24

CPC分类号： C07D499/00

摘要： A PROCESS IS PROVIDED FOR PREPARING 7-ACYLAMINO-7METHOXYCEPHALOSPORINS WHICH COMPRISES METHYLATING A 7-ACYLAMINO-7-HYDROXYCEPHALOSPORIN. THE FINAL PRODUCTS HAVE ANTIBACTERIAL ACTIVITY.

公开(公告)号：US3766175A

公开(公告)日：1973-10-16

申请号：US3766175D

申请日：1971-05-11

申请人： R & L MOLECULAR RESEARCH LTD

发明人： LEMIEUX R ,  RAAP R

IPC分类号： C07D209/48 ,  C07D249/04 ,  C07D501/36 ,  C07D99/24

CPC分类号： C07D209/48 ,  C07D249/04

摘要： 7-(O-AMINOMETHYLPHENYLACETAMIDO)-3-(1 - METHYL-5TETRAZOLYTHIO) METHYL) CEPH-3-EM-4-CARBOXYLIC ACID, 7-(ODIAZOLYTHIO) METHYL)-CEPH-3-EM-4-CARBOXYLIC ACID AND 7(O-AMINOMETHYLPHENYLACETAMIDO)-3-(S-(1,2,3 - TRAZOLE-5YL)-THIOMETHYL)-CEPH-3-EM-4-CARBOXYLIC ACID AND THEIR NONTOXIC, PHARMACEUTICALLY ACCEPTABLE SALTS ARE VALUABLE AS ANTIBACTERIAL AGENTS, AS NUTRITIONAL SUPPLEMENTS IN ANIMAL FEED AND AS THERAPEUTIC AGENTS IN POULTRY AND ANIMALS, INCLUDING MAN, AND ARE ESPECIALLY USEFUL IN THE TREATMENT OF INFECTIOUS DISEASES CAUSED BY MANY GRAMPOSITIVE AND GRAM-NEGATIVE BACTERIA. 7-(O-AMINOMETHYLPHENYLACETAMIDO)-3-(1 - METHYL-5-TETRAZOLYLTHIO)METHYL) CEPH-3-EM-4-CARBOXYLIC ACID IS PREPARED, FOR EXAMPLE, BY TREATMENT AT 0*C. WITH TRIFLUOROACETIC ACID OF THE CORRESPONDING COMPOUND IN WHICH THE FREE AMINO GROUP IS PROTECTED WITH A TERT-BUTOXYCARBONYL GROUP.

公开(公告)号：US3759905A

公开(公告)日：1973-09-18

申请号：US3759905D

申请日：1971-10-14

申请人： R & L MOLECULAR RESEARCH LTD

发明人： LEMIEUX R ,  GORDON CHIN C

IPC分类号： A23K20/195 ,  C07C271/16 ,  C07D309/12 ,  C07D501/20 ,  C07D99/24

CPC分类号： C07C247/00 ,  C07C271/16 ,  C07D309/12

摘要： 7-(0-, M- AND P-(2''AMINOETHOXY)PHENYLACETAMIDO)-3(SUBSTITUTED METHYL)-CEPH-3-EM-4-CARBOXYLATES, WHEREIN THE SUBSTITUENT ON THE "3-METHYL" GROUP IS HYDROGEN, ACETOXY, PYRIDINIUM, PICOLINIUM, LUTIDINIUM, 5-METHYL-1, 3,4-THIADIAZOL-2-YLTHIO, 1-METHYL-5-TETRAZOLYLTHIO OR 3METHYL- 1,2,4-THIADIAZOL-5-YLTHIO AND THEIR ZWITTERIONS, BETAINES AND NONTOXIC, PHARAMCEUTICALLY ACCEPTABLE ACID ADDITION AND CATIONIC SALTS ARE VALUABLE AS ANTIBACTERIAL AGENTS AND AS THERPEUTIC AGENTS IN POLUTRY AND ANIMALS, INCLUDING MAN, AND ARE ESPECIALLY USEFUL IN THE TREATMENT OF INFECTIOUS DISEASES CAUSED BY MANY GRAM-POSITIVE AND GRAM-NEGATIVE BACTERIA. 7-(P-2''AMINOETHOXY)-PHENYLACETAMIDO)-3-(PYRIDINIUMMETHYL)CEPH-3-EM-4 -CARBOXYLATE IS PREPARED, FOR EXAMPLE, BY TREATMENT AT 0*C. WITH TRIFLUOROACETIC ACID OF THE CORRESPONDING COMPOUND IN WHICH THE FREE AMINO GROUP IS PROTECTED WITH A TERT.BUTOXYCARBONYL GROUP.

公开(公告)号：US3741963A

公开(公告)日：1973-06-26

申请号：US3741963D

申请日：1971-07-28

申请人： SQUIBB & SONS INC

发明人： DURSCH F ,  KOCY O

IPC分类号： C07D501/04 ,  A61K20060101 ,  A61K31/545 ,  C07D20060101 ,  C07D501/22 ,  C07D501/60 ,  C07F20060101 ,  C07D99/24

CPC分类号： C07D501/22

摘要： N-CARBOSY DERIVATIVES OF CEPHRADINE AND OF CEPHALEXIN ARE PROVIDED WHICH ARE READILY WATER SOLUBLE AND ARE USEFUL AS ANTIBIOTICS WHICH MAY BE ADMINISTERED PARENTERALLY.

公开(公告)号：US3739002A

公开(公告)日：1973-06-12

申请号：US3739002D

申请日：1969-12-17

申请人： LILLY CO ELI

发明人： HAYES H ,  HUFF G

IPC分类号： C07D501/04 ,  C07C20060101 ,  C07D20060101 ,  C07D501/12 ,  C07D501/18 ,  C07D501/28 ,  C07D501/50 ,  C12P35/06 ,  C07D99/24

CPC分类号： C07D501/12

摘要： ACYLATION OF THE SIDE-CHAIN AMINO GROUP OF CEPHALOSPORIN C WITH A HALO LOWER ALKANOYL GROUP LEADS TO A SOLVENT-SOLUBLE PRODUCT WHICH CAN BE EFFICIENTLY EXTRACTED FROM THE AQUEOUS FERMENTATION BROTH BY USE OF AN ORGANIC SOLVENT.

公开(公告)号：US3708479A

公开(公告)日：1973-01-02

申请号：US3708479D

申请日：1970-10-26

申请人： SQUIBB & SONS INC

发明人： WELCH A ,  DOLFINI J ,  GIARRUSSO F

IPC分类号： C07D499/00 ,  C07D501/20 ,  C07D99/24

CPC分类号： C07D499/00

摘要： New acyloxymethyl esters of Alpha ureidocyclohexadienylalkylene-cephalosporins of the general formula

ARE EFFECTIVE AS ANTIBACTERIAL AGENTS AND SHOW PROLONGED ACTION AS WELL AS OTHER IMPROVED RESULTS.

摘要翻译： 新型的α-环脲基环己二烯基亚烷基 - 头孢菌素的新型酰氧基甲基酯作为抗菌药物有效并显示出广泛的作用，作为其他改进的结果。

公开(公告)号：US3701775A

公开(公告)日：1972-10-31

申请号：US3701775D

申请日：1970-11-25

申请人： SMITH KLINE FRENCH LAB

发明人： BERGES DAVID A ,  DUNN GEORGE L ,  HOOVER JOHN R E

IPC分类号： A61K20060101 ,  C07C20060101 ,  C07D20060101 ,  C07D501/20 ,  C07D501/32 ,  C07D99/24

CPC分类号： C07D501/20 ,  Y02P20/55

摘要： ESTERS OF MANDELAMIDOCEPHALOSPORANIC ACIDS HAVING ANTIBACTERIAL ACTIVITY ARE PREPARED BY CONDENSING THE MANDELAMIDOCEPHALOSPORIN WITH A CARBOXYLIC ACID. PREFERRED COMPOUNDS INCLUDE THOSE WHERE THE CARBOXYLIC ACID IS AN AMINO ACID.

公开(公告)号：US3681328A

公开(公告)日：1972-08-01

申请号：US3681328D

申请日：1967-06-27

申请人： FUJISAWA PHARMACEUTICAL CO

发明人： KURITA MASARU ,  SAITO YOSHIHISA ,  TERAJI TSUTOMU

IPC分类号： C07D499/00 ,  C07D501/34 ,  C07D99/24

CPC分类号： C07D499/00

摘要： THE DISCLOSURE TEACHES NOVEL 3- AND/OR 4-SUBSTITUTED SYDNONE DERIVATIVES OF 7-AMINOCEPHALOSPORANIC ACIDS WHICH ARE USEFUL AS AN ANTIBACTERIAL AGENT IN THE TREATMENT OF THE INFECTIOUS DISEASES BY GRAM-NEGATIVE AND GRAM-POSITIVE ORGANISMS.