公开(公告)号：US3728334A

公开(公告)日：1973-04-17

申请号：US3728334D

申请日：1971-03-03

Applicant: PFIZER

Inventor： BUTLER K ,  CARROLL R ,  HAMANAKA E

IPC: C07D499/00 ,  C07D499/72 ,  C07D499/74 ,  C07D99/16

CPC classification number: C07D499/00

Abstract: A NOVEL CLASS OF BROAD SPECTRUM ANTIBIOTICS DERIVED FROM 6-(1-CARBOXYCYCLOALKYLCARBOXAMIDO)PENICILLANIC ACIDS AND DERIVATIVES AND SALTS THEREOF.

公开(公告)号：US3770722A

公开(公告)日：1973-11-06

申请号：US3770722D

申请日：1971-10-04

Applicant: PFIZER

Inventor： BRIGHT G ,  HAMANAKA E

IPC: C07D499/00 ,  C07D499/64 ,  C07D99/16

CPC classification number: C07D499/00

Abstract: A NOVEL SERIES OF ANTIBACTERIAL AGENTS; NAMELY, 6-(A(ARYL SUBSTITUTED)ACYLAMINOACYLAMINO)PENICILLANIC ACIDS OF THE FORMULA

6-(Z-NH-CH2-CO-NH-),2-(HOOC-),3,3-DI(CH3-)PENAM

THE NON-TOXIC SALTS, ESTERS AND AMIDES THEREOF WHEREIN Z IS RR1CH-CO-; R IS PHENYL, SUBSTITUTED PHENYL OR THIENYL; R1 IS HYDROGEN OR COOH; AND INTERMEDIATES THEREFOR OF THE ABOVE FORMULA WHEREIN Z IS HYDROGEN.

公开(公告)号：US3748323A

公开(公告)日：1973-07-24

申请号：US3748323D

申请日：1971-07-09

Applicant: PFIZER

Inventor： HAMANAKA E

IPC: C07D499/00 ,  C07D499/60 ,  C07D99/16

CPC classification number: C07D499/00

Abstract: BROAD-SPECTRUM ANTIBACTERIAL AGENTS; NAMELY, 6-(SULFATO ACYLAMINO)PENICILLANIC ACIDS OF THE FORMULA:

6-(HO3S-O-C(-R1)(-R2)-CO-NH-),2-(R3-OOC-),3,3-DI(CH3-)-

PENAM

AND THE NON-TOXIC CATIONIC SALTS THEREOF WHEREIN R1 IS THIENYL, ALKYL, CYCLOALKYL, PHENYL OR SUBSTITUTED PHENYL WHEREIN THE SUBSTITUENTS IS LOWER ALKYL, LOWER ALKOXY, CHLORO, BROMO OR TRIFLUOROMETHYL; R2 IS HYDROGEN OR LOWER ALKYL; R1 AND R2 TOGETHER WITH THE CARBON ATOM TO WHICH THEY ARE ATTACHED REPRESENT CYCLOALKYL; R3 IS HYDROGEN AND ACYLOXY LOWER ALKYL WHEREIN THE ACYLOXY MOIETY IS LOWER ALKANOYLOXY, BENZOYLOXY OR SUBSTITUTED BENZOYLOXY WHEREIN THE SUBSTITUENT IS CHLORO, BROMO, FLUORO, LOWER ALKYL, LOWER ALKOXY OR TRIFLUOROMETHYL.

公开(公告)号：US3838153A

公开(公告)日：1974-09-24

申请号：US25385672

申请日：1972-05-16

Applicant: PFIZER

Inventor： HAMANAKA E ,  PATTON D

IPC: C07D499/70 ,  A61K31/43 ,  A61P31/04 ,  C07C275/16 ,  C07C279/28 ,  C07C335/34 ,  C07C335/38 ,  C07D233/42 ,  C07D233/44 ,  C07D233/46 ,  C07D499/00 ,  C07D499/04 ,  C07D499/10 ,  C07D499/64 ,  C07D499/68 ,  C07K5/02 ,  C07K7/02 ,  C07D99/16

CPC classification number: C07D499/00 ,  C07C275/16 ,  C07C279/28 ,  C07C335/34 ,  C07C335/38 ,  C07D233/42 ,  C07D233/44 ,  C07D233/46

Abstract: 2-(HOOC-),3,3-DI(H3C-),6-(R2-N(-R3)-C(=N-R4)-N(-R1)-CO-

(NH-A-CO)N-NH-CH(-AR)-CO-NH-)-PENAM
COMPOUNDS OF THE FOROULA
WHEREIN AR IS PHENYL, 4-HYDROXYPHENYL, 2-THIENYL OR 3THIENYL, A IS ALKENE OF 1 TO 4 CARBON ATOMS OR ALKYLIDENE OF 2 TO 4 CARBON ATOMS, N IS AN INTEGER OF 1 TO 3, R1, R2, R3 AND R4 CONSIDERED SEPARATELY ARE EACH HYDROGEN OR ALKYK OF 1 TO 4 CARBON ATOMS, R1 AND R4 CONSIDERED TOGETHER ARE ALKYLENE OF 2 TO 4 CARBON ATOMS, R2 AND R4 CONSIDERED TOGETHER ARE ALKYLENE OF 2 TO 4 CARBON ATOMS; AND R2 AND R3 CONSIDERED TOGETHER ARE ALKYLENE OF 4 TO 5 CARBON ATOMS AS BROAD SPECTRUM ANTIBIOTICS.

公开(公告)号：US3828025A

公开(公告)日：1974-08-06

申请号：US8701870

申请日：1970-11-04

Applicant: PFIZER

Inventor： HAMANAKA E

IPC: C07D499/00 ,  C07D499/44 ,  C07D99/16

CPC classification number: C07D499/00 ,  Y02P20/55 ,  Y10S514/937 ,  Y10S514/96 ,  Y10S514/962

Abstract: 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.

公开(公告)号：US3819600A

公开(公告)日：1974-06-25

申请号：US22181472

申请日：1972-01-28

Applicant: PFIZER

Inventor： HAMANAKA E

IPC: A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/72 ,  C07D99/16

CPC classification number: C07D499/00

Abstract: 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.