Phosphono substituted acylpenicillins
    52.
    发明授权
    Phosphono substituted acylpenicillins 失效
    磷酸二氢卟吩

    公开(公告)号:US3828025A

    公开(公告)日:1974-08-06

    申请号:US8701870

    申请日:1970-11-04

    申请人: PFIZER

    发明人: HAMANAKA E

    摘要: BROAD SPECTRUM ANTIBACTERIAL AGENTS; NAMELY, A-(PHOSPHONOALKYL) AND A-(W-PHOSPHONOCYCLOALKYL)PENICILLINS OF THE FORMULA

    2-(R3OOC-),3,3-DI(H3C-),6-(R5-O-P(=O)(-O-R4)-(CH2)N-C(-R1)

    (-R2)-CO-NH-)-PENAM

    AND THE NON-TOXIC CATIONIC SALTS THEREOF WHEREIN R1 IS HYDROGEN, LOWER ALKYL, PHENYL AND SUBSTITUTED PHENYL WHEREIN THE SUBSTITUENT IS LOWER ALKYL, LOWER ALKOXY, CHLORO, BROMO, FLUORO AND TRIFLUOROMETHYL; R2 IS HYDROGEN; R1 AND R2 TOGETHER WITH THE CARBON ATOM TO WHICH THEY ARE ATTACHED ARE ALICYCLIC OF FROM 3 TO 7 CARBON ATOMS; R3 IS HYDROGEN AND ACYLOXY LOWER ALKYL WHEREIN THE ACYLOXY MOIETY IS LOWER ALKANOYLOXY, BENZOYLOXY AND SUBSTITUTED BENZOYLOXY WHEREIN THE SUBSTITUENT IS CHLORO, BROMO, FLUORO, LOWER ALKYL, LOWER ALKOXY AND TRIFLUOROMETHYL; N IS 0 OR AN INTEGER FROM 1 TO 8; EACH OF R4 AND R5 IS HYDROGEN, LOWER ALKYL, SUBSTITUTED LOWER ALKYL WHEREIN THE SUBSTITUENT IS LOWER ALKOXY AND FLUORO; PHENYL AND SUBSTITUTED PHENYL WHEREIN THE SUBSTITUENT IS CHLORO, BROMO, FLUORO, LOWER ALKYL, LOWER ALKOXY AND TRIFLUOROMETHYL.

    Derivatives of 6-amino penicillanic acid
    53.
    发明授权
    Derivatives of 6-amino penicillanic acid 失效
    6-氨基茴香酸的衍生物

    公开(公告)号:US3821198A

    公开(公告)日:1974-06-28

    申请号:US24984072

    申请日:1972-05-03

    申请人: SQUIBB & SONS INC

    发明人: LEE B RYU D PANSY F

    CPC分类号: C07D499/00

    摘要: WHEREIN Z is hydrogen, lower alkyl on a salt forming ion and X is aryl, substituted aryl, lower alkyl, cyclohexadienyl, cycloalkyl or saturated or unsaturated N-, O- or S-containing heterocyclic rings. These compounds are useful as antibacterial agents.
    New penicillin and cephalosporin derivatives and methods for preparing the same are provided, said derivatives having the structures

    Alpha-carboxamido acyl derivatives of penicillin
    55.
    发明授权
    Alpha-carboxamido acyl derivatives of penicillin 失效
    派尼林的阿尔法 - 卡博酰胺类衍生物

    公开(公告)号:US3819600A

    公开(公告)日:1974-06-25

    申请号:US22181472

    申请日:1972-01-28

    申请人: PFIZER

    发明人: HAMANAKA E

    CPC分类号: C07D499/00

    摘要: PENICILLINS OF THE FORMULA

    2-(R2-OOC-),3,3-DI(CH3-),6-(PHENYL-CH(-CO-NH-Z-R1)-CO-

    NH-)PENAM

    WHEREIN R1 IS ALKYL OR SUBSTITUTED ALKYL WHEREIN SAID ALKYL CNTAINS FROM 1 TO 4 CARBONATOMS AND SAID SUBSTITUENTS IS CARBOXY, CARBAMYL, CYANO, CHLORO, BROMO OR ALKOXY OR ALKYLTHIO CONTAINING 1 TO 3 CARBON ATOMS; Z IS -0-

    -CO-,

    OR SO2 2 2; R2 IS HYDROGEN OR 1-ALKANOYLOXYALKYL WHEREIN SAID ALKANOYL CONTAINS 2 TO 5 CARBONATOMS AND SAID ALKY CONTAINS FROM 1 TO 4 CARBON ATOMS; AND THE PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, WHEREIN SAID PENCILLIN IS AN ACID AS BROAD SPECTRUM ANTIBIOTICS.

    Process for producing 6-amino-penicillanic acid
    56.
    发明授权
    Process for producing 6-amino-penicillanic acid 失效
    生产6-氨基 - 丙酸的方法

    公开(公告)号:US3809699A

    公开(公告)日:1974-05-07

    申请号:US9890770

    申请日:1970-12-16

    申请人: UNIV OSAKA

    发明人: ISHIMARU T

    CPC分类号: C07D499/00

    摘要: 6-AMINOPENCILLANIC ACID IS PREPARED, WITH ADVANTAGE IN INDUSTRIAL VIEWPOINT, BY (A) REACTING 6-ACYLAMINOPENICILLANIC ACID OR A SALT THEREOF WITH A HALOGENATED COMPOUND SUCH AS TRIHALIDE OF PHOSPHORUS, TETRAHALIDE OF SILICON, PHOSPHOROUS PENTAHALIDE, PHOSGENE OR THIOPHOSGENE, IN THE PRESENCE OF AN ACID-BINDING REAGENT FOR THE PURPOSE OF TO PROTECT THE CARBOXYL GROUP OF THE 6-ACYLAMIDOPENICILLANIC ACID BY FORMING A MIXED ACID ANHYDRIDE, (B) CONVERTING THE RESULTANT MIXED ACID ANHYDRIDE INTO THE CORRESPONDING IMINO HALIDE BY REACTING IT WITH AN AMINO HALIDEFORMING REAGENT SUCH AS PHOSPHOROUS OXYCHLORIDE, PHOSPHORUS PENTACHLORIDE, PHOSPHORUS TRIBROMIDE, PHOSGENE, OXALYL CHLORIDE OR PROTOCATECHYL PHOSPHOROUS TRICHLORIDE TO FORM THE CORRESPONDING IMINO HALIDE, (C) CONVERTING THE RESULTANT IMINO HALIDE INTO THE CORRESPONDING IMINOETHER BY REACTING IT WITH AN ALCOHOL AND FINALLY (D) HYDROLYZING THE IMINO ETHER AND REMOVING THE PROTECTED GROUP OF THE CARBOXYL GROUP TO FORM 6-AMINOPENCILLANIC ACID.

    Acylthioacetyl penicillins
    60.
    发明授权
    Acylthioacetyl penicillins 失效
    ACYLTHIOACETYL PENICILLINS

    公开(公告)号:US3767645A

    公开(公告)日:1973-10-23

    申请号:US3767645D

    申请日:1971-09-14

    申请人: SQUIBB & SONS INC

    发明人: TREUNER U BREUER H

    CPC分类号: C07D499/00

    摘要: ACYLTHIOACETYLPENICILINS OF THE GENERAL FORMULA

    6-(R2-CO-S-CH(-R1)-CO-NH-),2-(R-OOC-),3,3-DI(CH3-)PENAM

    WHEREIN R IS HYDROGEN, LOWER ALKYL, ARALKYL, TRI(LOWER ALKYL) SILYL, A SALT FORMING ION OR THE GROUP

    -CH2-OOC-R3

    R1 IS HYDROGEN, LOWER ALKYL, CYCLOALKYL, ARALKYL, ARYL OR CERTAIN HETEROCYCLIC GROUPS; R2 IS LOWER ALKYL, CYCLOALKYL, ARYL OF CERTAIN HETEROCYCLIC GROUPS; AND R3 IS LOWER ALKYL, ARYL OR ARALKYL, ARE USEFUL AS ANTIBACTERIAL AGENTS.