Abstract: A penicillin derivative represented by the following formula ##STR1## wherein R.sub.1 and R.sub.2 are each the same or different and represent hydrogen, C.sub.1-18 alkyl, mononitro-substituted benzyl or group for forming a pharmaceutically acceptable salt and R.sub.3 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkoxymethyl, C.sub.3-8 alkylcarbonyloxymethyl, C.sub.4-9 alkylcarbonyloxyethyl, (C.sub.5-7 cycloalkyl)carbonyloxymethyl, C.sub.9-14 benzylcarbonyloxyalkyl, C.sub.3-8 alkoxycarbonylmethyl, C.sub.4-9 alkoxycarbonylethyl, phthalidyl, crotonolacton-4-yl, .gamma.-butyrolacton-4-yl, halogenated C.sub.1-6 alkyl substituted with 1 to 3 halogen atoms, C.sub.1-6 alkoxy- or nitro-substituted or unsubstituted benzyl, benzhydryl, tetrahydropyranyl, dimethylaminoethyl, dimethylchlorosilyl, trichlorosilyl, (5-substituted C.sub.1-6 alkyl or phenyl or unsubstituted-2-oxo-1,3-dioxoden-4-yl)methyl, C.sub.8-13 benzoyloxyalkyl and group for forming a pharmaceutically acceptable salt.
Type:
Grant
Filed:
June 6, 1983
Date of Patent:
July 16, 1985
Assignee:
Taiho Pharmaceutical Company, Limited
Inventors:
Ronald G. Micetich, Shigeru Yamabe, Tomio Yamazaki, Naobumi Ishida, Takeshi Ishizawa
Abstract: There is presented a method, in the form of a dosage formulation, for transforming substantially orally inactive .beta.-lactam antibiotics or their pharmaceutically acceptable salts or the esters, ethers, or hydrates of said antibiotics or their salts into orally active compounds by combination of the chosen .beta.-lactam antibiotic with an enhancer comprising an aliphatic, preferably a C.sub.2 to C.sub.18, straight- or branched-chain, saturated or unsaturated, fatty acid or an aliphatic, preferably a C.sub.2 to C.sub.12, straight- or branched-chain, saturated or unsaturated, fatty acid mono-, di- or triglyceride or mixtures thereof, partial or total esters of propylene glycol, polyethylene glycol and carbohydrates of C.sub.2 to C.sub.12 fatty acids, as well as the pharmaceutically acceptable esters and ethers of said glycerides. The antibiotic and enhancer mixture may be administered orally as a solid dosage form with the .beta.
Type:
Grant
Filed:
October 15, 1982
Date of Patent:
June 25, 1985
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Charanjit Behl, George Beskid, Navnit Shah, Jacques Tossounian, Joel Unowsky
Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R represents an alkyl or aralkyl group, substituted on an alkyl carbon atom other than that adjacent to --NH-- group, with one or more functional groups selected from halogen, non-aromatic heterocyclyl linked through carbon, aromatic heterocyclyl, nitro, oxo, --OR.sup.1, SR.sup.1 --P(O)R.sup.2 R.sup.3, --NR.sup.4 R.sup.5, .dbd.NR.sup.6, or a sulphur linked organic radical, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are various organic radicals.Processes for the preparation of these compounds and pharmaceutical compositions containing them are also disclosed.
Type:
Grant
Filed:
July 20, 1983
Date of Patent:
June 18, 1985
Assignee:
Beecham Group p.1.c.
Inventors:
Irene Stirling, Gordon Bruton, Stephen H. Calvert, Brian P. Clarke
Abstract: There are presented .beta.-lactams of the formula ##STR1## wherein R.sup.1 is cyano or a group of the formula R.sup.4 --CO-- or R.sup.5 --A--CO--, R.sup.2 is hydrogen, lower alkyl or halogen, R.sup.3 is hydrogen or a group readily cleavable by hydrolysis, n is the number 0, 1 or 2, R.sup.4 is hydrogen, hydroxy, lower alkoxy, lower alkyl, aryl or a group of the formula ##STR2## R.sup.5 is halogen, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, aryl, aryloxy, arylthio, arylsulphinyl, arylsulphonyl or di-(loweralkoxy)phoshinyl, R.sup.6 and R.sup.7 are lower alkyl and A is lower alkylene,and pharmaceutically acceptable salts of carboxylic acids of formula I with bases.The compounds exhibit pronounced .beta.-lactamase-inhibiting properties.
Abstract: There is disclosed the antibacterial 5R,6S,8R-6-(1-hydroxyethyl)-2-(2-carbamoyloxyethylthio)-penem-3-carboxylic acid, its pharmaceutically acceptable salts and metabolizable esters as well as compositions containing them and methods for their use, preferably the sodium salt for parenteral administration.
Type:
Grant
Filed:
April 4, 1983
Date of Patent:
March 12, 1985
Assignee:
Schering Corporation
Inventors:
Stuart W. McCombie, Ashit K. Ganguly, Viyyoor M. Girijavallabhan
Abstract: The present invention provides a method for inhibiting the synthesis and release of toxins from bacteria which comprises contacting the bacteria with an antitoxic prostaglandin.