Plural Fermentates Of Different Origin (e.g., Mixtures Of Antibiotics, Etc.) Patents (Class 424/114)
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Patent number: 4426377Abstract: This invention provides the compounds of the formula (II): ##STR1## and salts and esters thereof, wherein R.sub.1 is H and R.sub.3 is H or an aryl, aralkyl, lower alkyl or substituted lower alkyl group or R.sub.1 and R.sub.3 are joined so that the CHR.sub.1.NH.CO.R.sub.3 moiety forms a group of the sub-formula (a): ##STR2## wherein R.sub.4 is a hydrogen atom or a NH.CO.R.sub.5 group wherein R.sub.5 is a lower alkyl, lower alkoxy lower alkyl, aryl, aralkyl, aryloxyalkyl, lower alkoxy or aryloxy group.The compounds have .beta.-lactamase inhibitory and anti-bacterial properties.The invention also provides a process for their preparation, and pharmaceutical compositions containing them.Type: GrantFiled: April 11, 1980Date of Patent: January 17, 1984Assignee: Beecham Group LimitedInventor: Thomas T. Howarth
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Patent number: 4421760Abstract: The compound of the formula (VI): ##STR1## pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, are useful for their antibacterial activity and for their .beta.-lactamase inhibitory activity. They may be combined in a synergistically effective amount with a penicillin or cephalosporin for the treatment of bacterial infections in humans and animals.Type: GrantFiled: June 17, 1981Date of Patent: December 20, 1983Assignee: Beecham Group LimitedInventor: Stephen J. Box
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Patent number: 4414204Abstract: The invention relates to pharmaceutical preparations that contain an antibiotic and a muramylpeptide of the formula I or a salt thereof, to processes for their manufacture and to a method for increasing the antibiotic effectiveness of antibiotics. ##STR1## In the formula I, X represents carbonyl or carbonyloxy, R.sub.1 represents optionally substituted alkyl or aryl, R.sub.2, R.sub.3, R.sub.4 and R.sub.6 represent hydrogen or lower alkyl, R.sub.5 represents hydrogen, optionally substituted lower alkyl, cycloalkyl, aryl or nitrogen-containing heterocyclyl, or R.sub.4 and R.sub.5 together represent also C.sub.3 -C.sub.4 alkylene, R.sub.7 represents hydrogen or free, esterified or amidated carboxyl, one of the radicals A.sub.1 and A.sub.2 represents a radical of the formula II and the other of the radicals A.sub.1 and A.sub.2 represents optionally substituted or functionally modified hydroxy or amino.Type: GrantFiled: January 21, 1981Date of Patent: November 8, 1983Assignee: Ciba-Geigy CorporationInventors: Lajos Tarcsay, Gerhard Baschang, Albert Hartmann, Jaroslav Stanek
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Patent number: 4413000Abstract: The present invention provides the compounds of the formula (II): ##STR1## and salts and esters thereof wherein R.sup.3 is a hydrogen atom or is an organic bonded via a carbon atom to the carbapenem ring, n is zero or one, X is a saturated or unsaturated hydrocarbon radical optionally substituted by bromo or chloro, and R.sup.4 is a C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.1-10 aralkyl or aryl group, any of such groups R.sup.4 being optionally substituted. These compounds are useful as antibacterial agents.Type: GrantFiled: July 8, 1981Date of Patent: November 1, 1983Assignee: Beecham Group LimitedInventor: Alfred J. Eglington
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Patent number: 4409207Abstract: The compound of the formula (I): ##STR1## and salts and esters thereof may be used as a .beta.-lactamase inhibitor to enhance the effectiveness of penicillins or cephalosporins.Type: GrantFiled: May 11, 1981Date of Patent: October 11, 1983Assignee: Beecham Group LimitedInventor: Brian C. Gasson
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Patent number: 4407815Abstract: The present invention provides the compounds of the formula (II): ##STR1## and pharmaceutically acceptable salts and cleavable esters thereof wherein RCONH is an organic acylamino group and E is a carboxy group or pharmaceutically acceptable salt or ester thereof or is a cyano group. Their preparation is described as is their use in compositions containing them. Compounds wherein RCONH is replaced by an azido group are described as useful intermediates.Type: GrantFiled: February 10, 1981Date of Patent: October 4, 1983Assignee: Beecham Group LimitedInventors: Michael J. Pearson, Clive L. Branch
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Patent number: 4406887Abstract: Bacteroides which are uniformly resistant to ceftazidime fail to grow when exposed to 2.beta.-chloromethyl-2.alpha.-methylpenam-3.alpha.-carboxylic acid (BL-P 2013), which itself is non-inhibitory, in combination with ceftazidime. Bacteroides infections are abated by treatment of the infected mammal with this combination of substances.Type: GrantFiled: October 13, 1981Date of Patent: September 27, 1983Assignee: Bristol-Myers CompanyInventors: Maxwell Gordon, I. Jacob Pachter
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Patent number: 4406889Abstract: Described are derivatives of pyranoses of the formula I, manufacturing processes and intermediates, and their use as medicaments. ##STR1## The pyranose moiety in the compounds of the formula I is derived especially from D-glucose, but alternatively from D-galactose or D-mannose.Characteristic of the compounds of the formula I is the lower alkyl or phenyl-lower alkyl radical R.sub.8, which carries an oxycarbonyl, mercaptocarbonyl or aminocarbonyl group, which is bonded to an aliphatic, cycloaliphaticaliphatic, cycloaliphatic or aromatic hydrocarbon radical R.sub.0, each of which is optionally substituted and which may be interrupted by oxycarbonyl, mercaptocarbonyl and/or iminocarbonyl and which, like the remaining radicals of the formula I, is defined in patent claim 1.Type: GrantFiled: February 10, 1981Date of Patent: September 27, 1983Assignee: Ciba-Geigy CorporationInventors: Albert Hartmann, Gerhard Baschang, Oskar Wacker, Jaroslav Stanek
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Patent number: 4405637Abstract: Compounds are described of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group; A.sub.1 is a hydrogen atom; and A.sub.2 is a group CR.sub.2 R.sub.3 R.sub.4 wherein R.sub.2 is a hydrogen atom or a hydroxyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.3 to form part of a C.sub.5-7 carboxylic ring or is a group of the formula CH(OH)R.sub.5 or CHX wherein R.sub.5 is a hydrogen atom or lower alkyl group and X is an oxygen atom or a CR.sub.6 R.sub.7 group where R.sub.6 is a hydrogen atom or a lower alkyl, phenyl, CN, CO.sub.2 R.sub.8 where R.sub.8 is a lower alkyl, phenyl or benzyl group and R.sub.7 is a hydrogen atom or a lower alkyl group or is joined to R.sub.6 to form part of a C.sub.5-7 carbocyclic ring. These compounds have been found to possess antibacterial properties. The preparation of these compounds is described.Type: GrantFiled: September 28, 1981Date of Patent: September 20, 1983Assignee: Beecham Group LimitedInventors: Kay H. Dickinson nee Berryman, Terence C. Smale, Robert Southgate
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Patent number: 4404218Abstract: An antibiotic SF-2103A substance or a salt thereof, and a process for the production thereof are described, and the process comprises cultivating an antibiotic SF-2103A substance-producing strain in a nutrient medium and recovering the desired substance from the culture broth.Type: GrantFiled: August 17, 1981Date of Patent: September 13, 1983Assignee: Meiji Seika Kaisha Ltd.Inventors: Tatsuo Ito, Takashi Shomura, Michio Kojima, Norio Ezaki, Masaji Sezaki, Tomizo Niwa
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Patent number: 4404189Abstract: A synergistic antimicrobial active ingredient for a pharmaceutical or veterinary composition comprises 5 to 50 percent by weight of a primycin component which consists of a primycin fermentation product of Thermonospora galeriensis and 95 to 50 percent by weight of at least one other component selected from the group which consists of doxycyline compounds and sisomicin compounds. The doxycycline compounds are selected from the group which consists of doxycycline, salts thereof with mineral acids, and doxycycline tryclate. The sisomicin compounds are selected from the group which consists of sisomicin, substituted sisomicins with substitution at the N atom by lower alkyl, hydroxyl lower alkyl, lower aminoalkyl and lower alkanoyl, and sisomicin acid salts.Type: GrantFiled: January 21, 1981Date of Patent: September 13, 1983Assignee: Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.Inventors: Gabor Kulcsar, Gyula Sebestyen, Agoston David, Tibor Zilahi
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Patent number: 4401653Abstract: Described is a method of using a combination of rapamycin and picibanil for the treatment of transplantable carcinogenic tumors.Type: GrantFiled: March 9, 1981Date of Patent: August 30, 1983Assignee: Ayerst, McKenna & Harrison Inc.Inventor: Chee P. Eng
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Patent number: 4394375Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R is phenyl, 4-hydroxyphenyl, or a 5- or 6-membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C.sub.1-6 alkoxy;R.sup.1 represents hydrogen or C.sub.1-6 alkyl;R.sup.2 and R.sup.3 are the same or different and represent hydrogen, C.sub.1-6 alkyl, halogen, amino, hydroxy, or C.sub.1-6 alkoxy;X represents oxygen or sulphur; andA represents hydrogen, pyridyl, acetoxy, carbamoyloxy or a heterocyclicthio group;Their preparation and use is described.Type: GrantFiled: June 5, 1981Date of Patent: July 19, 1983Assignee: Beecham Group LimitedInventors: Peter H. Bentley, Kenneth D. Hardy, Peter H. Milner
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Patent number: 4388300Abstract: The compounds of the formula (II): ##STR1## wherein R.sub.3 and R.sub.4 are as defined in relation to formula (I) and R.sub.7 is a nitro, cyano, amino or aminomethyl group, are antibacterial agents and .beta.-lactamase inhibitors. Their use and a process for their preparation are described.Type: GrantFiled: December 10, 1980Date of Patent: June 14, 1983Assignee: Beecham Group LimitedInventor: John B. Harbridge
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Patent number: 4387051Abstract: The present invention provides the compounds of the formula (II): ##STR1## and pharmaceutically acceptable salts and esters thereof wherein R.sup.3 is a hydrogen atom, a group HO.sub.3 S-- or a group R.sup.5 CO wherein R.sup.5 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, aryl, aryl(C.sub.1-6)alkyl or aryloxy(C.sub.1-6)alkyl; and R.sup.4 is an organic group other than methyl bonded to the --CO--NH-- moiety via a carbon atom; with the proviso that when R.sup.3 is a hydrogen atom or a group R.sup.5 CO the stereochemical configuration at the .alpha.-carbon atom of the C-6 substituent is S, and with the further proviso that when R.sup.3 is a group HO.sub.3 S-- the hydrogen atoms at C-5 and C-6 are cis. Their use is described as are processes for their preparation. Compounds wherein the R.sup.4 CO-- moiety is replaced by a hydrogen atom are also prepared.Type: GrantFiled: October 28, 1980Date of Patent: June 7, 1983Assignee: Beecham Group LimitedInventors: David F. Corbett, Robert Southgate, Alfred J. Eglington
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Patent number: 4386070Abstract: Pharmaceutical compositions consisting of an antibiotic (cephalosporins, tetracyclines, kanamycin) associated with a heterocyclicic .beta.-ketoacid (nalidixic acid, oxolinic acid, cinoxacine, piromidic acid, pipemidic acid) are endowed with a marked synergism against Gram-positive and Gram-negative pathogens as well with a particularly relevant efficacy against antibiotic-resistant strains.Type: GrantFiled: February 27, 1981Date of Patent: May 31, 1983Assignee: Ausonia Farmaceutici S.R.L.Inventor: Leonardo De Vincentiis
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Patent number: 4382084Abstract: The compounds of the formula (II): ##STR1## and salts and esters theereof wherein R.sub.1 is an inert organic group of up to 14 carbon atoms and R.sub.2 is an inert organic group of up to 16 carbon atoms, the group NR.sub.1 R.sub.2 containing up to 22 carbon atoms, are antibacterial agents able to enhance the effectiveness of penicillins and cephalosporins against certain .beta.-lactamase producing bacteria.Type: GrantFiled: March 10, 1980Date of Patent: May 3, 1983Assignee: Beecham Group LimitedInventors: Roger J. Ponsford, Thomas T. Howarth
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Patent number: 4379781Abstract: Macrolide antibiotics tylosin, spiromycin, cleandomycin, magnamycin, and leucomycin in combination with aminoglycoside antibiotics tobramycin, apramycin, nebramycin 5, gentamicin and neomycin form synergistic compositions which inhibit the growth of mycoplasma in mammalian tissue cultures. Tylosin-apramycin compositions enhance the feed efficiency and weight gain in post weaned pigs and are useful in the control of Pasturella hemolytica an infectious organism in cattle.Type: GrantFiled: March 9, 1981Date of Patent: April 12, 1983Assignee: Eli Lilly and CompanyInventors: Robert N. Hull, Robert S. Gordee
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Patent number: 4374144Abstract: The present invention relates to the preparation of compounds of the formula: ##STR1## wherein CO.sub.2 R.sub.1 is a free, salted or esterified carboxyl group, n is 0 or 1, and R.sub.2 is hydrogen or an acyl group or a group of the sub-formula (a):R.sub.3 O.sub.3 S (a)wherein R.sub.3 is a salting ion or a methyl or ethyl group, with the proviso that when R.sub.2 is a group of the formula (a), the compound has cis stereochemistry about the .alpha.-lactam ring; which have been found to possess antibacterial and .alpha.-lactamase inhibitory activity.Type: GrantFiled: November 3, 1980Date of Patent: February 15, 1983Assignee: Beecham Group LimitedInventor: David F. Corbett
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Patent number: 4372946Abstract: Compounds of the formula (I): ##STR1## and salts and esters thereof, wherein R.sub.1 is a hydrogen atom or a lower alkyl, aryl or aralkyl group, R.sub.2 and R.sub.3 are independently hydrogen, aryl, aralkyl, lower alkyl or substituted lower alkyl, or R.sub.3 is joined to R.sub.1 to form a 4-, 5-, or 6- membered ring or is joined to R.sub.2 to form a 5- or 6- membered ring with the proviso that when R.sub.2 is hydrogen, R.sub.1 is not hydrogen and R.sub.1 and R.sub.3 are not joined to form a group of the sub-formula (a) wherein R.sub.4 is a hydrogen atom or a NH.CO.R.sub.5 group wherein R.sub.5 is a lower alkyl, lower alkoxy lower alkyl, aryl, aralkyl, aryloxyalkyl; lower alkoxy or aryloxy group have .beta.-lactamase inhibitory and anti-bacterial properties.Type: GrantFiled: July 9, 1980Date of Patent: February 8, 1983Assignee: Beecham Group LimitedInventors: Thomas T. Howarth, Eric Hunt
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Patent number: 4364957Abstract: 6-Acylaminopenicillanoyloxymethyl esters and 1-(6-acylaminopenicillanoyloxy)ethyl esters of 2-beta-acetoxymethyl-2-alpha-methyl-(5R)penam-3-alpha-carboxylic acid 1,1-dioxide are useful as antibacterial agents. The 6-aminopenicillanoyloxymethyl ester, the 1-(6-aminopenicillanoyloxy)ethyl ester and certain other mono-substituted methyl and ethyl esters of 2-beta-acetoxymethyl-2-alpha-methyl-(5R)penam-3-alpha-carboxylic acid 1,1-dioxide are useful intermediates to the aforesaid antibacterial agents.Type: GrantFiled: February 20, 1981Date of Patent: December 21, 1982Assignee: Pfizer Inc.Inventor: Wayne E. Barth
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Patent number: 4356174Abstract: Beta-lactamase inhibiting 2-beta-substituted-2-alpha-methyl-(5R)penam-3-alpha-carboxylic acid 1,1-dioxides and esters thereof, wherein the 2-beta-substituent is cyano, acetyl, alkoxycarbonyl, omegahydroxyalkoxycarbonyl, carbalkoxymethoxycarbonyl or dialkylaminocarbonyl; intermediates therefor wherein the 2-beta-substituent is carboxy, chlorocarbonyl or aminocarbonyl; methods for their preparation and use as beta-lactamase inhibitors.Type: GrantFiled: September 14, 1981Date of Patent: October 26, 1982Assignee: Pfizer Inc.Inventor: Wayne E. Barth
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Patent number: 4350703Abstract: Compounds are described of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group; A.sub.1 is a hydrogen atom; and A.sub.2 is a group CR.sub.2 R.sub.3 R.sub.4 wherein R.sub.2 is a hydrogen atom or a hydroxyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.3 to form part of a C.sub.5-7 carboxylic ring or is a group of the formula CH(OH)R.sub.5 or CHX wherein R.sub.5 is a hydrogen atom or lower alkyl group and X is an oxygen atom or a CR.sub.6 R.sub.7 group where R.sub.6 is a hydrogen atom or a lower alkyl, phenyl, CN, CO.sub.2 R.sub.8 where R.sub.8 is a lower alkyl, phenyl or benzyl group and R.sub.7 is a hydrogen atom or a lower alkyl group or is joined to R.sub.6 to form part of a C.sub.5-7 carbocyclic ring. These compounds have been found to possess antibacterial properties. The preparation of these compounds is described.Type: GrantFiled: January 5, 1981Date of Patent: September 21, 1982Assignee: Beecham Group LimitedInventors: Kay H. Dickinson, Terence C. Smale, Robert Southgate
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Patent number: 4342749Abstract: Compounds of the formula (II): ##STR1## wherein X is sulphur or oxygen and R is hydrogen or alkyl of 1 to 3 carbon atoms, are useful for their antibacterial, .beta.-lactamase inhibitory activity and synergistic activity when combined with a penicillin or cephalosporin.Type: GrantFiled: July 14, 1980Date of Patent: August 3, 1982Assignee: Beecham Group LimitedInventor: John B. Harbridge
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Patent number: 4341766Abstract: Method and compositions for deactivating bacterial hydrolytic enzymes which attack .beta.-lactam antibiotics.Type: GrantFiled: June 27, 1980Date of Patent: July 27, 1982Assignee: Harvard CollegeInventors: Jed F. Fisher, Jeremy R. Knowles
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Patent number: 4330529Abstract: The present invention relates to an antibacterial composition comprising a phosphonic acid derivative of the formula: ##STR1## wherein R is lower alkanoyl andn is an integer of 2 to 5 or its saltand an antibiotic selected from a B-lactam antibiotic, aminoglycoside antibiotic and their salts.Type: GrantFiled: September 29, 1980Date of Patent: May 18, 1982Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroshi Imanaka, Minoru Nishida
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Patent number: 4325937Abstract: An improved microbial insecticide composition, and methods for the production and utilization thereof, are disclosed. The disclosed composition comprises a microbial insect pathogen of viral, bacterial, or fungal origin which is susceptible to sunlight-induced inactivation embedded in a coacervate microbead which is comprised of a nucleic acid, typically RNA, and a proteinaceous material, whereby the microbead structure itself effectively shields the agent from sunlight-induced inactivation. The microbead is typically stabilized by chemical crosslinking.Type: GrantFiled: March 5, 1981Date of Patent: April 20, 1982Assignee: Battelle Development CorporationInventors: Kemet D. Spence, Robert E. Andrews
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Patent number: 4324783Abstract: An antibacterial composition for medical use comprising 6-[D(-)-.alpha.-(4-ethyl-2,3-dioxo-1-piperazinylcarbonylamino)phenylacetam ido]penicillanic acid or a pharmaceutically acceptable salt thereof and a .beta.-lactamase-inhibiting penicillin or cephalosporin. The composition exhibits synergistic effect which is much greater than the sum of antibacterial effects of each component used alone.Type: GrantFiled: January 17, 1980Date of Patent: April 13, 1982Assignee: Toyama Chemical Co., Ltd.Inventors: Isamu Saikawa, Takashi Yasuda, Masaru Tai, Yutaka Takashita, Hiroshi Sakai, Michiko Mae, Masahiro Takahata, Susumu Mitsuhashi
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Patent number: 4318916Abstract: A novel antibiotic substance and derivatives thereof, having strong antibiotic activity and .beta.-lactamase inhibiting effect and a method for producing the same by aerobic cultivation of Streptomyces A 271.Type: GrantFiled: March 2, 1978Date of Patent: March 9, 1982Assignee: Sanraku-Ocean Co., Ltd.Inventors: Kazuhiko Okamura, Shoji Hirata, Yasushi Okumura, Yasuo Fukagawa, Yasutaka Shimauchi, Tomoyuki Ishikura, Kageaki Kouno, Joseph Lein
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Patent number: 4301149Abstract: A dry unit-dose pharmaceutical composition suitable for oral administration which composition comprises 20 mg to 1500 mg of amoxycillin trihydrate, 20 mg to 500 mg of potassium clavulanate and a pharmaceutically acceptable carrier with the proviso that the weight ratio of amoxycillin trihydrate to potassium clavulanate is from 6:1 to 1:1; has favored storage properties. Such compositions are presented in enclosed containers which they also contain a desiccant.Type: GrantFiled: January 25, 1980Date of Patent: November 17, 1981Assignee: Beecham Group LimitedInventor: Patrick J. Crowley
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Patent number: 4297345Abstract: The compounds of the formula: ##STR1## and salts and esters thereof are useful agents for the treatment of bacterial infections either alone or in combination with a penicillin or cephalosporin derivative. The preceding compounds may be prepared by the hydrogenation of a compound of the formula: ##STR2## wherein R is a hydrogen atom or an acyl group or a salt or ester thereof.Type: GrantFiled: October 22, 1979Date of Patent: October 27, 1981Assignee: Beecham Group LimitedInventor: Thomas T. Howarth
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Patent number: 4287181Abstract: 6.beta.-Hydroxyalkylpenicillanic acids and derivatives thereof as useful enhancers of the effectiveness of several .beta.-lactam antibiotics against many .beta.-lactamase producing bacteria, and 6.beta.-substituted penicillanic acid benzyl ester derivatives as useful intermediates leading to said agents which enhance the effectiveness of .beta.-lactam antibiotics.Type: GrantFiled: October 22, 1979Date of Patent: September 1, 1981Assignee: Pfizer Inc.Inventor: Michael S. Kellogg
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Patent number: 4283388Abstract: Antibiotic compositions comprising tylosin and apramycin are effective in the treatment and control of colibacillosis in weanling pigs, and demonstrate greater effectiveness than apramycin alone or tylosin alone.Type: GrantFiled: December 26, 1979Date of Patent: August 11, 1981Assignee: Eli Lilly and CompanyInventor: Earl E. Ose
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Patent number: 4278686Abstract: The present invention provides antibiotic compounds of the formula: ##STR1## and salts and cleavable esters thereof wherein X is a SCH.sub.2 CH.sub.2 NH.sub.2 or YNH-COCH.sub.3 group where Y is a SCH.sub.2 CH.sub.2, trans --SO--CH.dbd.-- or cis or trans --S--CH.dbd.CH-- group and R is a lower alkyl, aryl, aralkyl, lower alkenyl, or substituted lower alkyl.Type: GrantFiled: April 27, 1979Date of Patent: July 14, 1981Assignee: Beecham Group LimitedInventors: David F. Corbett, Alfred J. Eglington
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Patent number: 4276285Abstract: Penicillanic acid 1,1-dioxide, pharmaceutically-acceptable salts thereof, and esters thereof readily hydrolyzable in vivo, enhance the antibacterial effectiveness of 7-(D-2-[4-ethylpiperazin-2,3-dione-1-carboxamido]-2-[4-hydroxyphenyl]aceta mido)-3-([1-methyl-5-tetrazolyl]thiomethyl)-3-desacetoxymethylcephalosporan ic acid, and salts thereof, against many beta-lactamase producing bacteria.Type: GrantFiled: March 5, 1979Date of Patent: June 30, 1981Assignee: Pfizer Inc.Inventor: Wayne E. Barth
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Patent number: 4268503Abstract: This invention relates to an antibacterial composition comprising a phosphonic acid and an antibiotic.Type: GrantFiled: August 14, 1979Date of Patent: May 19, 1981Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroshi Imanaka, Minoru Nishida
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Patent number: 4265882Abstract: Biologically active sulfur analogs of 6-aminopenicillanic acid having a nucleophile substituted in the 6-position are made by reacting a sulfenyl chloride with esters of diazopenicillanic acid. Biologically active sulfur analogs of 7-aminocephalosporanic acid having a nucleophile substituted in the 7-position are analogously made by reacting a sulfenyl chloride with esters of 7-diazocephalosporanic acid. Deacetoxycephalosporins can be formed from the corresponding analog of 6-aminopenicillanic acid and derivations thereof, by sulfoxide rearrangement of the thiazolidine ring of penicillins to the dihydrothiazine ring of cephalosporins. These nucleophile substituted sulfur analogs of penicillins and cephalosporins are new antibacterial agents and display antibacterial activity against a variety of microorganisms.Type: GrantFiled: October 3, 1977Date of Patent: May 5, 1981Assignee: Massachusetts Institute of TechnologyInventors: John C. Sheehan, Thomas J. Commons
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Patent number: 4263280Abstract: The invention relates to new synergistic mixtures which contain, as active components, the antibiotic cefsulodin sodium and a second known antibiotic selected from the group comprising the .beta.-lactamase inhibitors, penicillins, cephalosporins or aminoglycosides, pharmaceutical preparations containing said mixtures and a process for their manufacture, and to the use of these preparations for combating infections.Type: GrantFiled: April 9, 1979Date of Patent: April 21, 1981Assignee: Ciba-Geigy CorporationInventors: Friedrich Kradolfer, Otokar Zak
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Patent number: 4263314Abstract: The present invention provides the antibacterial agents of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is a carboxylic acid group or a salt thereof or is a group of the formula CO.sub.2 R.sub.1.sup.1 wherein R.sub.1.sup.1 is a group such that CO.sub.2 R.sub.1.sup.1 is an ester group, R.sub.2 is a hydrogen atom or a lower alkyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a phenyl group or a phenyl group substituted by one or two groups selected from fluorine, chlorine, OR.sub.5, NH.CO.R.sub.5, NH.CO.sub.2 R.sub.5 or CO.sub.2 R.sub.5 where R.sub.5 is a lower alkyl or benzyl group.A process for their preparation and their use in pharmaceutical compositions is also described.Type: GrantFiled: January 19, 1979Date of Patent: April 21, 1981Assignee: Beecham Group LimitedInventors: Roger J. Ponsford, Robert Southgate, Patricia M. Roberts
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Patent number: 4261977Abstract: A novel antibiotic designated herein MM 17880 may be obtained from the cultivation of strains of Streptomyces olivaceus and related organisms. In addition to being potent antibacterial agents, MM 17880 and its salts inhibit .beta.-lactamase obtained from many organisms so that it shows a synergistic antibacterical effect when combined with .beta.-lactam antibiotics.Type: GrantFiled: August 29, 1978Date of Patent: April 14, 1981Assignee: Beecham Group LimitedInventors: Stephen J. Box, John D. Hood
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Patent number: 4260598Abstract: 6-Aminopenicillanic acid 1,1-dioxide, esters thereof readily hydrolyzable in vivo, and the pharmaceutically-acceptable salts of these compounds, are useful for enhancing the effectiveness of certain .beta.-lactam antibiotics against certain .beta.-lactamase producing bacteria. Derivatives of 6-aminopenicillanic acid 1,1-dioxide protected by a conventional carboxy protecting group are useful intermediates to 6-aminopenicillanic acid 1,1-dioxide and esters thereof readily hydrolyzable in vivo.Type: GrantFiled: October 22, 1979Date of Patent: April 7, 1981Assignee: Pfizer Inc.Inventor: Wayne E. Barth
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Patent number: 4256733Abstract: 2.beta.-Acetoxymethyl-2.alpha.-methyl-(5R)penam-3.alpha.-carboxylic acid 1,1-dioxide, pharmaceutically-acceptable salts thereof and esters thereof readily hydrolyzable in vivo; pharmaceutical compositions containing 2.beta.-acetoxymethyl-2.alpha.-methyl-(5R)penam-3.alpha.-carboxylic acid 1,1-dioxide or salt or ester thereof; and method of enhancing the effectiveness of a .beta.-lactam antibiotic using 2.beta.-acetoxymethyl-2.alpha.-methyl-(5R)penam-3.alpha.-carboxylic acid 1,1-dioxide or salt or ester thereof.Type: GrantFiled: September 26, 1979Date of Patent: March 17, 1981Assignee: Pfizer Inc.Inventor: Wayne E. Barth
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Patent number: 4241050Abstract: (3S, 5R)-Penam-3-carboxylic acid 1,1-dioxide, optionally having a methyl group at the 2-position, and esters thereof readily hydrolyzable in vivo, are useful for enhancing the effectiveness of several beta-lactam antibiotics against many beta-lactamase producing bacteria.Type: GrantFiled: September 1, 1978Date of Patent: December 23, 1980Assignee: Pfizer Inc.Inventor: Wayne E. Barth
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Patent number: 4235882Abstract: It has been found that an antibiotic can be obtained by the fermentation of certain strains of Streptomyces olivaceus and related organisms and when pure this antibiotic is an extremely potent inhibitor of many .beta.-lactamases. This antibiotic which we designate MM 4550A may be obtained in substantially pure form by the chromatographic purification of the crude antibacterial complex obtained from the culture medium.Type: GrantFiled: September 20, 1976Date of Patent: November 25, 1980Assignee: Beecham Group LimitedInventors: Martin Cole, John D. Hood, Dennis Butterworth
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Patent number: 4234596Abstract: Isomeric forms of 3-(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-en e-2-carboxylic acid (I) ##STR1## are disclosed; also disclosed is a process for their total synthesis; such isomers individually, and as mixtures, are useful as antibiotics.Type: GrantFiled: March 5, 1979Date of Patent: November 18, 1980Assignee: Merck & Co., Inc.Inventors: Burton G. Christensen, David B. R. Johnston, Susan M. Schmitt
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Patent number: 4232005Abstract: The compounds of the formula: ##STR1## and salts and esters thereof are useful agents for the treatment of bacterial infections either alone or in combination with a penicillin or cephalosporin derivative.The preceding compounds may be prepared by the hydrogenation of a compound of the formula: ##STR2## wherein R is a hydrogen atom or an acyl group or a salt or ester thereof.Type: GrantFiled: December 5, 1977Date of Patent: November 4, 1980Assignee: Beecham Group LimitedInventor: Thomas T. Howarth
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Patent number: 4225585Abstract: Fungicidal compositions for agricultural and horticultural use are provided which contain as an active ingredient thereof the antibiotics angustmycin A or angustmycin C. They exhibit excellent protective effects against attack by plant disease fungi or bacteria, have no phytotoxicity and cause no pollution in the environment. A method for protecting plants by the use thereof is also provided.Type: GrantFiled: May 23, 1978Date of Patent: September 30, 1980Assignee: Ajinomoto Company, IncorporatedInventors: Takao Kida, Zuisho Terahara, Toshiro Shida, Hiroshi Mizuno, Yoshiyuki Takahara, Yoshiteru Hirose
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Patent number: 4221781Abstract: An antibacterial synergistic composition consisting essentially of a mixture of a penicillin or cephalosporin derivative of the formula ##STR1## and a penicillin of the formula ##STR2## preferably in association with a pharmaceutical carrier.Type: GrantFiled: February 7, 1978Date of Patent: September 9, 1980Assignee: Astra Lakemedel AktiebolagInventors: Peter Bamberg, Bertil A. Ekstrom, Ulf E. Forsgren, Berndt O. H. Sjoberg
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Patent number: 4215128Abstract: This invention provides the compounds of the formula (II): ##STR1## and salts and esters thereof, wherein R.sub.1 is H and R.sub.3 is H or an aryl, aralkyl, lower alkyl or substituted lower alkyl group or R.sub.1 and R.sub.3 are joined so that the CHR.sub.1.NH.CO.R.sub.3 moiety forms a group of the sub-formula (a): ##STR2## wherein R.sub.4 is a hydrogen atom or a NH.CO.R.sub.5 group wherein R.sub.5 is a lower alkyl, lower alkoxy lower alkyl, aryl, aralkyl, aryloxyalkyl, lower alkoxy or aryloxy group.The compounds have .beta.-lactamase inhibitory and anti-bacterial properties.The invention also provides a process for their preparation, and pharmaceutical compositions containing them.Type: GrantFiled: September 14, 1978Date of Patent: July 29, 1980Assignee: Beecham Group LimitedInventor: Thomas T. Howarth
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Patent number: 4210662Abstract: Compounds of the formula ##STR1## and salts thereof are useful both for their antibacterial activity and as synergists in combination with penicillins and cephalosporins.Type: GrantFiled: May 25, 1977Date of Patent: July 1, 1980Assignee: Beecham Group LimitedInventors: Alfred J. Eglington, Thomas T. Howarth, David F. Corbett