Plural Fermentates Of Different Origin (e.g., Mixtures Of Antibiotics, Etc.) Patents (Class 424/114)
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Patent number: 4647457Abstract: .beta.-lactams of the formula ##STR1## wherein R.sup.1 signifies hydrogen or a group readily cleavable by hydrolysis, A signifies the group R.sup.2 --N.dbd.C(CH.sub.3)--CH.dbd.C< or O.dbd.C(CH.sub.3)--CH.sub.2 --C(R.sup.3)<, R.sup.2 signifies hydroxy, lower alkoxy or arylamino and R.sup.3 signifies arylthio, lower alkanoylthio, lower alkoxycarbonylhydrazino or a N-containing saturated heterocycle attached via a N-atom, and pharmaceutically acceptable salts thereof, are disclosed. The compounds and their salts exhibit .beta.-lactamase inhibiting activities against .beta.-lactamases from bacteria.Type: GrantFiled: March 2, 1984Date of Patent: March 3, 1987Assignee: Hoffmann-La Roche Inc.Inventor: Solange Adam-Molina
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Patent number: 4645671Abstract: Tetrazolyl derivatives of clavulanic acid are described, having the formula: ##STR1## wherein X is an optionally substituted tetrazolyl group attached via a nitrogen atom. These compounds are useful as antibiotics and .beta.-lactamase inhibitors.Type: GrantFiled: July 15, 1985Date of Patent: February 24, 1987Assignee: Beecham Group p.l.c.Inventor: John B. Harbridge
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Patent number: 4594246Abstract: This invention relates to penicillanic acid derviatives of the formula I ##STR1## in which X stands for chlorine, bromine or iodine, to pharmaceutically acceptable, non-toxic salts of the compounds of formula I, to pharmaceutically acceptable, easily hydrolyzable esters thereof, including salts of such esters, to pharmaceutical compositions containing the compounds of the invention and dosage units thereof, to methods for the preparation of the compounds of the invention, and to methods of using the said new compounds in the human and veterinary therapy.The 6.beta.-halopenicillanic acids of formula I are potent inhibitors of .beta.-lactamases from a variety of gram-positive and gram-negative bacteria, making the 6.beta.-halopenicillanic acids as well as their salts and easily hydrolyzable esters valuable in human and veterinary medicine.Type: GrantFiled: December 23, 1983Date of Patent: June 10, 1986Assignee: Leo Pharmaceutical ProductsInventor: Welf von Daehne
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Patent number: 4594247Abstract: Antibiotic compositions comprising a 1-oxa .beta.-lactam antibiotic compound of the formula ##STR1## or pharmaceutically acceptable salts thereof and either tobramycin, amikacin or piperacillin exhibit synergistic activity against multiple-antibiotic-resistant organisms. The 1-oxa compound can be used in conjunction with tobramycin, amikacin or piperacillin in a method of treating infections caused by resistant organisms.Type: GrantFiled: January 27, 1984Date of Patent: June 10, 1986Assignee: Eli Lilly and CompanyInventor: Gordon L. Brier
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Patent number: 4591459Abstract: beta-Lactamase inhibitors which are aminoacid esters of 6-alpha- and 6-beta-(hydroxymethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, said compositions useful in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoacyloxymethyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also useful in the treatment of bacterial infections; and intermediates therefor.Type: GrantFiled: December 3, 1984Date of Patent: May 27, 1986Assignee: Pfizer Inc.Inventor: Wayne E. Barth
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Patent number: 4590073Abstract: A series of novel derivatives of penicillanic acid 1,1-dioxide, having a disubstituted methyl group of the formula X--CH--Y at the 6-position, and the pharmaceutically-acceptable salts thereof and the pharmaceutically-acceptable esters thereof readily hydrolyzable in vivo, wherein X is hydroxy, acylated hydroxy or amino and Y is carboxy or esterified carboxy. The compounds of the invention are inhibitors of bacterial beta-lactamases, and they will protect certain beta-lactamase-susceptible beta-lactam antibiotics, e.g. ampicillin, against inactivation by beta-lactamases. Co-administration of a compound of the invention with a beta-lactam antibiotic such as ampicillin to a mammalian subject increases the effectiveness of the beta-lactam antibiotic against infections caused by beta-lactamase-producing bacteria.Type: GrantFiled: July 2, 1985Date of Patent: May 20, 1986Assignee: Pfizer Inc.Inventor: Wayne E. Barth
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Patent number: 4588527Abstract: 6-alpha/beta-[(C.sub.1 -C.sub.4)Alkoxyaminomethyl and benzyloxyaminomethyl]penicillanic acid 1,1-dioxides, pharmaceutically acceptable salts thereof and conventional esters thereof hydrolyzable under physiological conditions, all of which are useful in medicine as beta-lactamase inhibitors; intermediates and processes therefor; and a process for the conversion of the present compounds to 6-alpha- and 6-beta-(aminomethyl)penicillanic acid 1,1-dioxides and derivatives.Type: GrantFiled: December 3, 1984Date of Patent: May 13, 1986Assignee: Pfizer Inc.Inventors: Donald K. Pirie, Robert A. Volkmann, Edward F. Kleinman
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Patent number: 4562073Abstract: A penicillin derivative represented by the following formula ##STR1## wherein R.sub.1 is hydrogen or trialkylsilyl; R.sub.2 is hydrogen, trialkylsilyl or COOR.sub.2 ' wherein R.sub.2 ' is hydrogen, C.sub.1-18 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 or group for forming a pharmaceutically acceptable salt; and R.sub.3 has the same meaning as above R.sub.2 '.Type: GrantFiled: August 1, 1983Date of Patent: December 31, 1985Assignee: Taiho Pharmaceutical Company LimitedInventors: Ronald G. Micetich, Shigeru Yamabe, Motoaki Tanaka, Makoto Kajitani, Tomio Yamazaki, Naobumi Ishida
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Patent number: 4560550Abstract: A class of 6-alkylidene penem compounds of formula (II) have antibacterial and .beta.-lactamase inhibitory properties: ##STR1## where R.sup.1 and R.sup.2 represent hydrogen or optionally substituted hydrocarbon or heterocyclic, and R.sup.3 represents hydrogen or an organic group.Type: GrantFiled: April 23, 1984Date of Patent: December 24, 1985Assignee: Beecham Group p.l.c.Inventor: Neal F. Osborne
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Patent number: 4560552Abstract: A new antibacterially active agent has been isolated from Streptomyces clavuligerus. This new compound which is designated clavulanic acid has the formula (I): ##STR1## In addition to being a broad spectrum antibiotic of medium potency, clavulanic acid and its salts and esters have the ability to enhance the effectiveness of .beta. lactam antibiotics against many .beta.-lactamase producing bacteria.Type: GrantFiled: December 14, 1981Date of Patent: December 24, 1985Assignee: Beecham Group p.l.c.Inventors: Martin Cole, Thomas T. Howarth, Christopher Reading
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Patent number: 4557932Abstract: The present invention relates to a new compounded composition with synergistic properties, to dosage units thereof, and to the use of the said compounded composition and dosage units.The composition contains as active ingredients the amidinopenicillanic acid mecillinam or a pharmaceutically acceptable, non-toxic salt or pro-drug thereof in combination with another antibiotic compound of the formula ##STR1## or a pharmaceutically acceptable, non-toxic salt or pro-drug thereof, optionally together with pharmaceutically acceptable, non-toxic carriers and/or auxiliary agents.The new composition is valuable in the human and veterinary practice for the treatment of patients suffering from infectious diseases.Type: GrantFiled: December 29, 1982Date of Patent: December 10, 1985Assignee: Leo Pharmaceutical Products Ltd.Inventor: Leif Tybring
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Patent number: 4556559Abstract: A new antibacterially active agent has been isolated from Streptomyces clvuligerus. This new compound which is designated clavulanic acid has the formula (I): ##STR1## In addition to being a broad spectrum antibiotic of medium potency, clavulanic acid and its salts and esters have the ability to enhance the effectiveness of .beta.-lactam antibiotics against many .beta.-lactamase producing bacteria.Type: GrantFiled: July 13, 1978Date of Patent: December 3, 1985Assignee: Beecham Group p.l.c.Inventors: Martin Cole, Thomas T. Howarth, Christopher Reading
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Patent number: 4554160Abstract: The invention relates to a new series of penicillin esters and salts thereof, to methods of their preparation and to intermediates in the production of the esters of the general formula ##STR1## in which R.sub.1 and R.sub.2 represent an alkyl radical having from 1 to 6 carbon atoms, a cycloalkyl or cycloalkylalkyl radical the cycloalkyl part having from 3 to 10 carbon atoms, or R.sub.1 and R.sub.2 together with the nitrogen atom represent a heterocyclic ring with from 4 to 8 carbon atoms; R.sub.3 represents radicals known from natural, biosynthetic, and semisynthetic penicillins; and pharmaceutically acceptable salts thereof.The new compounds are efficiently absorbed from the gastrointestinal tract and after the absorption they are rapidly transformed into the corresponding free penicillins and amidinopenicillanic acids, whereby a broad-spectrum infection can be combated.Type: GrantFiled: March 3, 1975Date of Patent: November 19, 1985Assignee: Lovens Kemiske Fabrik ProduktionsaktieselskabInventor: Wagn O. Godtfredsen
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Patent number: 4552763Abstract: Antibiotic compositions comprising a 1-oxa .beta.-lactam antibiotic compound of the formula ##STR1## or pharmaceutically acceptable salts thereof and either tobramycin, amikacin or piperacillin exhibit synergistic activity against multiple-antibiotic-resistant organisms. The 1-oxa compound can be used in conjunction with tobramycin, amikacin or piperacillin in a method of treating infections caused by resistant organisms.Type: GrantFiled: January 27, 1984Date of Patent: November 12, 1985Assignee: Eli Lilly and CompanyInventor: Gordon L. Brier
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Patent number: 4548815Abstract: The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R is an inert ogranic group of up to 18 carbon atoms and are able to inhibit the action of various bacterial .beta.-lactamases. Thus when a compound of the formula (II) or its salt or ester is used together with a penicillin or cephalosporin, the effectiveness of that penicillin or cephalosporin can be considerably enhanced. These novel synergysts can be prepared by etherification of an ester of clavulanic acid followed if desired by deesterification. The novel synergysts also possess antibacterial activity.Type: GrantFiled: October 3, 1983Date of Patent: October 22, 1985Assignee: Beecham Group p.l.c.Inventors: Roger J. Ponsford, Thomas T. Howarth
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Patent number: 4544549Abstract: Tetrazolyl derivatives of clavulanic acid are described, having the formula: ##STR1## wherein X is an optionally substituted tetrazolyl group attached via a nitrogen atom. These compounds are useful as antibiotics and .beta.-lactamase inhibitors.Type: GrantFiled: December 27, 1982Date of Patent: October 1, 1985Assignee: Beecham Group p.l.c.Inventor: John B. Harbridge
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Patent number: 4539202Abstract: The compounds of the formula (II): ##STR1## or pharmaceutically acceptable salts or esters thereof wherein A is a hydrogen atom or an esterifying radical; X is an alkyl group of 1-12 carbon atoms optionally substituted by a hydroxy, amino, acylamino of C.sub.1-6 alkoxy group, which substituents are not on the carbon atom adjacent to the nitrogen atom; or a C.sub.5-7 cycloalkyl group; or a phenylalkyl group wherein the carbon atom content of the alkyl part is 1-6 and the phenyl part is optionally substituted with a fluorine, bromine, chlorine, C.sub.1-6 alkyl, or C.sub.1-6 alkoxy; with the proviso that when X represents an optionally substituted phenylalkyl group and A represents C.sub.1-3 alkyl, then the --CO.sub.2 A group is attached to the alkyl part of the phenylalkyl group; have been found to be .beta.-lactamase inhibitors and antibacterial agents. Their preparation and use is described.Type: GrantFiled: March 24, 1983Date of Patent: September 3, 1985Assignee: Beecham Group p.l.c.Inventors: Brian P. Clarke, John B. Harbridge, Irene Stirling
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Patent number: 4536393Abstract: 6-alpha- and 6-beta-(Aminomethyl)penicillanic acid, 1,1-dioxide esters which are hydrolyzable under physiological conditions, particularly those wherein the ester radical is 1H-isobenzofuran-3-on-1-yl or (5-methyl-1,3-dioxol-2-on-4-yl)methyl, and an improved process and intermediates used in their synthesis.Type: GrantFiled: February 6, 1984Date of Patent: August 20, 1985Assignee: Pfizer Inc.Inventor: Wayne E. Barth
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Patent number: 4534968Abstract: A synergistic combination is produced which comprises a synergistically effective amount of clavulanic acid or a pharmaceutically acceptable salt thereof and an antibacterially effective amount of a compound of the formula (II): ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1 is hydrogen, hydroxyl or acetoxyl, R.sup.2 is methyl and R.sup.3 is CO.R.sup.4 wherein R.sup.4 is phenyl, isobutyl, furyl, thienyl or NHCH.sub.3 or R.sup.2 is joined to R.sup.3 so that NR.sup.2 R.sup.3 is an imidazolin-2-on-1-yl.Type: GrantFiled: June 26, 1980Date of Patent: August 13, 1985Assignee: Beecham Group LimitedInventor: John P. Clayton
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Patent number: 4533542Abstract: The instant invention is a pharmaceutical composition suitable for storage in plastic containers which comprises a pharmaceutical compound in powder form coated with a surfactant. A second aspect of the invention is a method for making the composition. This method encompasses applying a solution of a surfactant to the surface of a pharmaceutical compound in powder form and then drying the composition.Type: GrantFiled: August 22, 1983Date of Patent: August 6, 1985Assignee: Eli Lilly and CompanyInventors: Harry C. Buddenbaum, Robert L. Robison
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Patent number: 4529591Abstract: Synergistic anti-bacterial compositions comprising (A) D-.alpha.-[(imidazolidin-2-on-1-yl)-carbonylamino]-benzylpenicillin or D-.alpha.-[(3-methylsulphonyl-imidazolidin-2-on-1-yl)-carbonylamino]-benzy lpenicillin, and (B) 3-(2,6-dichlorophenyl)-5-methyl-4-isoxazolylpenicillin, 3-(2-chloro-6-fluo rophenyl)-5-methyl-4-isoxazolylpenicillin, 3-(2-chlorophenyl)-5-methyl-4-isoxazolylpenicillin, 3-phenyl-5-methyl-4-isoxazolylpenicillin, or 2,6-dimethoxyphenylpenicillin, or salts thereof. They can be used to fight infection, as additives to animal feeds to promote growth, and as a preservative for polymers.Type: GrantFiled: March 1, 1982Date of Patent: July 16, 1985Assignee: Bayer AktiengesellschaftInventor: Karl G. Metzger
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Patent number: 4529592Abstract: 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: GrantFiled: June 6, 1983Date of Patent: July 16, 1985Assignee: Taiho Pharmaceutical Company, LimitedInventors: Ronald G. Micetich, Shigeru Yamabe, Tomio Yamazaki, Naobumi Ishida, Takeshi Ishizawa
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Patent number: 4526783Abstract: A new antibacterially active agent has been isolated from Streptomyces clavuligerus. This new compound which is designated clavulanic acid has the formula (I): ##STR1## In addition to being a broad spectrum antibiotic of medium potency, clavulanic acid and its salts and esters have the ability to enhance the effectiveness of .beta.-lactam antibiotics against many .beta.-lactamase producing bacteria.Type: GrantFiled: June 9, 1981Date of Patent: July 2, 1985Assignee: Beecham Group p.l.c.Inventors: Martin Cole, Thomas T. Howarth, Christopher Reading
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Patent number: 4525352Abstract: A new antibacterially active agent has been isolated from Streptomyces clavuligerus. This new compound which is designated clavulanic acid has the formula (I): ##STR1## In addition to being a broad spectrum antibiotic of medium potency, clavulanic acid and its salts and esters have the ability to enhance the effectiveness of .beta. lactam antibotics against many .beta.-lactamase producing bacteria.Type: GrantFiled: December 3, 1981Date of Patent: June 25, 1985Assignee: Beecham Group p.l.c.Inventors: Martin Cole, Thomas T. Howarth, Christopher Reading
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Patent number: 4525353Abstract: A new antibacterially active agent has been isolated from Streptomyces clavuligerus. This new compound which is designated clavulanic acid has the formula (I): ##STR1## In addition to being a broad spectrum antibiotic of medium potency, clavulanic acid and its salts and esters have the ability to enhance the effectiveness of .beta.-lactam antibiotics against many .beta.-lactamase producing bacteria.Type: GrantFiled: February 26, 1982Date of Patent: June 25, 1985Assignee: Beecham Group p.l.c.Inventors: Martin Cole, Thomas T. Howarth, Christopher Reading
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Patent number: 4510134Abstract: There is provided a method for controlling nematodes in warm-blooded animals by orally administering thereto a nematocidally effective amount of a new antibiotic or mixture of antibiotics produced in a microbiological fermentation under controlled conditions using a newly discovered strain of Actinomadura yumaense and mutants thereof.There is also provided a method for controlling nematodes in soil by applying to said soil a nematocidally effective amount of the above-mentioned antibiotic or antibiotic mixture.Type: GrantFiled: May 7, 1982Date of Patent: April 9, 1985Assignee: American Cyanamid Co.Inventor: Irwin B. Wood
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Patent number: 4505894Abstract: Compounds of the formula ##STR1## wherein X is S, SO or SO.sub.2 and R is an inert hydrocarbon of up to 20 carbon atoms which will not lead to rapid degradation of the above compound unsubstituted or substituted and A is a group such and CO.sub.2 A represents a carboxylic acid group or a salt or ester thereof, are useful for their antibacterial activity and for their .beta.-lactamase inhibitory activity.Type: GrantFiled: August 30, 1982Date of Patent: March 19, 1985Assignee: Beecham Group LimitedInventor: Roger J. Ponsford
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Patent number: 4503040Abstract: Beta-lactamase inhibitors which are aminoacid esters of 6-alpha- and 6-beta-(hydroxymethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, said compositions useful in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoacyloxymethyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also useful in the treatment of bacterial infections; and intermediates therefor.Type: GrantFiled: February 27, 1984Date of Patent: March 5, 1985Assignee: Pfizer Inc.Inventor: Wayne E. Barth
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Patent number: 4501732Abstract: This invention relates to new synergistic antimicrobial compositions containing primycin, doxycycline and sisomicin.Type: GrantFiled: June 18, 1982Date of Patent: February 26, 1985Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.Inventors: Gabor Kulcsar, Gyula Sebestyen, Agoston David, Tibor Zilahi
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Patent number: 4486411Abstract: 6-Beta-sulfonyloxypenicillanic acid derivatives are novel beta-lactamase inhibitors, useful in combination with standard beta-lactam antibiotics against bacterial strains otherwise resistant to said beta-lactam antibiotics by dint of their production of beta-lactamases.Type: GrantFiled: July 1, 1981Date of Patent: December 4, 1984Assignee: Pfizer Inc.Inventor: Ernest S. Hamanaka
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Patent number: 4478822Abstract: This invention relates to a unique drug delivery system for delivering drugs to a body cavity. The drug delivery system comprises a medicament and a polymer such that the drug delivery system is a liquid at room temperature but forms a semi-solid or gel at the body temperature in the body cavity.Type: GrantFiled: May 16, 1983Date of Patent: October 23, 1984Assignee: Merck & Co., Inc.Inventors: John L. Haslam, Takeru Higuchi, Arthur R. Mlodozeniec
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Patent number: 4474751Abstract: This invention describes the application of selected polymers as novel drug delivery systems which use the body temperature and pH to induce a liquid to gel transition of the polymer which contains a drug or therapeutic agent therein. The goal of such a delivery system is to achieve a greater degree of bioavailability or sustained concentration of a drug.Type: GrantFiled: May 16, 1983Date of Patent: October 2, 1984Assignee: Merck & Co., Inc.Inventors: John L. Haslam, Takeru Higuchi, Arthur R. Mlodozeniec
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Patent number: 4474753Abstract: This invention relates to a unique drug delivery system for application to the skin which drug delivery system is a liquid at room temperature, but when administered topically to the skin becomes a semi-solid or gel when warmed by the body.Type: GrantFiled: May 16, 1983Date of Patent: October 2, 1984Assignee: Merck & Co., Inc.Inventors: John L. Haslam, Takeru Higuchi, Arthur R. Mlodozeniec
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Patent number: 4474752Abstract: Present invention provides a unique drug delivery device for delivering drug by injection into a body. The drug delivery system comprises the drug and polymer which is a liquid at room temperature and a semi-solid or gel at the body temperature.Type: GrantFiled: May 16, 1983Date of Patent: October 2, 1984Assignee: Merck & Co., Inc.Inventors: John L. Haslam, Takeru Higuchi, Arthur R. Mlodozeniec
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Patent number: 4473548Abstract: A method of immunizing cats against shedding of Toxoplasma oocysts is described wherein cats are given a primary Toxoplasma infection, preferably by feeding of tissue cysts, and are chemoprophylactically treated to suppress oocyst shedding as a result of the primary infection. thus, the treated cats are given immunity to oocyst shedding without the necessity of initial shedding. The treating agent is preferably monensin given with the cats' daily ration at a level of at least about 200 mg. monensin per kg. of cat food. Other useful treating agents include salinomycin or a combination of orally administered sulfadiazine and pyrimethamine.Type: GrantFiled: July 30, 1982Date of Patent: September 25, 1984Assignee: The Kansas University Endowment AssociationInventors: Jacob K. Frenkel, Donald D. Smith
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Patent number: 4468380Abstract: The present invention is directed to novel anticoccidial compositions and methods of employing the same to control coccidiosis in poultry. These compositions comprise a polyether antibiotic and a second component which is a selected carbanilide.Type: GrantFiled: May 6, 1981Date of Patent: August 28, 1984Assignee: Eli Lilly and CompanyInventors: George O. P. O'Doherty, Albert J. Clinton
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Patent number: 4452778Abstract: Antibiotic compositions comprising a 1-oxa .beta.-lactam antibiotic compound of the formula ##STR1## or pharmaceutically acceptable salts thereof and either tobramycin, amikacin or piperacillin exhibit synergistic activity against multiple-antibiotic-resistant organisms. The 1-oxa compound can be used in conjunction with tobramycin, amikacin or piperacillin in a method of treating infections caused by resistant organisms.Type: GrantFiled: December 21, 1981Date of Patent: June 5, 1984Assignee: Eli Lilly and CompanyInventor: Gordon L. Brier
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Patent number: 4448769Abstract: A 1,1-dioxopenicillanic acid ester represented by formula (I) ##STR1## wherein R represents a methyl or phenyl group. The ester of formula (I) may be prepared by reacting 1,1-dioxopenicillanic acid or its salt with a compound represented by formula (III) ##STR2## wherein R is as defined above, and X represents a halogen atom, or by oxidizing a compound of formula (V) ##STR3## wherein R is as defined above. The ester of the formula (I) is useful as a .beta.-lactamase inhibitor and may be used in association with a .beta.-lactam antibiotic.Type: GrantFiled: July 8, 1982Date of Patent: May 15, 1984Assignee: Kanebo Ltd.Inventors: Shoji Ikeda, Fumio Sakamoto, Goro Tsukamoto, Shigeru Yamabe
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Patent number: 4444771Abstract: A compound of formula (I) or a salt thereof: ##STR1## wherein R.sup.1 is an amino group, an azido group, or an acylamino group as found in antibacterially active penicillins or cephalosporins;R.sup.2 is a hydrogen atom or a C.sub.1-4 alkyl group;R.sup.3 is a hydrogen atom, or a C.sub.1-4 alkyl group optionally substituted by a carboxyl, carboxylic ester, hydroxy, C.sub.1-4 alkyloxy, acyloxy or heterocyclylthio group; andR.sup.4 is hydrogen or a readily removable carboxyl protecting group.The compounds wherein R.sup.1 is an acylamino group are found in known antibacterially active penicillins and cephalosporins and wherein R.sup.4 is a hydrogen, a pharmaceutically acceptable salting ion or an in vivo hydrolyzable ester forming radical may be formulated in pharmaceutical compositions.Processes for the preparation of the compound (I) are also described.Type: GrantFiled: September 4, 1981Date of Patent: April 24, 1984Assignee: Beecham Group LimitedInventors: Michael J. Pearson, Clive L. Branch
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Patent number: 4444783Abstract: The compounds of the formulaes (IV), (V) and (VI): ##STR1## and salts and esters thereof where X is a bromine or chlorine atom, and n is 0 or 1; are antibacterial agents. Their preparation and use is described.Type: GrantFiled: October 1, 1981Date of Patent: April 24, 1984Assignee: Beecham Group LimitedInventor: Alfred J. Eglington
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Patent number: 4444754Abstract: The compounds of the formula (I): ##STR1## and esters thereof wherein R.sub.1 is a lower alkyl group or a phenyl group and R.sub.2 is a hydrogen atom or R.sub.2 together with R.sub.1 represents the residue of a fused benzene ring are .beta.-lactamase inhibitors and anti-bacterial agents. Their preparation and use is described.Type: GrantFiled: March 10, 1981Date of Patent: April 24, 1984Assignee: Beecham Group LimitedInventors: Irene Stirling, Brian P. Clarke
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Patent number: 4440751Abstract: The novel antibiotic complex designated hazymicin consisting of eight components, is produced by a novel strain of Micromonospora herein designated Micromonospora echinospora var. challisensis SCC 1411. Also disclosed are the structures of the two components namely, Component 5 and Component 6.Type: GrantFiled: October 6, 1980Date of Patent: April 3, 1984Assignee: Schering CorporationInventors: Jay A. Waitz, Joseph A. Marquez, Mahesh G. Patel, Ann C. Horan
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Patent number: 4438036Abstract: The present invention provides a process for inversion of the absolute stereochemistry at the .alpha.-carbon atom of a C-6 substituent of a bicyclic carbapenem antibiotic via a phosphorus - azodicarboxylate mediated reaction. Novel azides, amines and formates are described as useful intermediates and as antibacterial agents.Type: GrantFiled: October 13, 1981Date of Patent: March 20, 1984Assignee: Beecham Group LimitedInventors: David F. Corbett, Robert Southgate, Steven Coulton
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Patent number: 4438101Abstract: The compounds of the formula (II): ##STR1## and salts and esters thereof 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: September 22, 1978Date of Patent: March 20, 1984Assignee: Beecham Group LimitedInventors: Roger J. Ponsford, Thomas T. Howarth
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Patent number: 4432970Abstract: 6-beta-Halopenicillanic acid 1,1-dioxides, physiologically acceptable salts thereof and esters thereof readily hydrolyzable; pharmaceutical compositions containing a 6-beta-halopenicillanic acid 1,1-dioxide, a physiologically acceptable salt thereof or an ester thereof readily hydrolyzable; and a method for enhancing the effectiveness of a beta-lactam antibiotic, using a 6-beta-halopenicillanic acid 1,1-dioxide, a physiologically acceptable salt thereof or an ester thereof readily hydrolyzable.Type: GrantFiled: December 9, 1980Date of Patent: February 21, 1984Assignee: Pfizer Inc.Inventor: Michael S. Kellogg
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Patent number: 4428936Abstract: An antibacterial composition for medical use comprising a cephalosporin or a pharmaceutically acceptable salt thereof and a .beta.-lactamase-inhibiting compound having a .beta.-lactam ring. The composition exhibits synergistic effect which is much greater than the sum of antibacterial effects of each component used alone.Type: GrantFiled: September 16, 1980Date of Patent: January 31, 1984Assignee: 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: 4428935Abstract: A compound of the formula ##STR1## is a prodrug of 4,4-dioxopenicillanic acid, wherein R is hydrogen or methyl; R.sub.1, R.sub.2 and R.sub.3 (a) when taken individually are each alkyl containing one to four carbon atoms, or (b) when taken together with the nitrogen to which they are attached form a five- or six-membered saturated monocyclic moiety, an eight-membered saturated bicyclic moiety or a five- or six-membered aromatic cyclic moiety annulated with zero, one or two fused benzene rings, with the proviso that any R.sub.1, R.sub.2 or R.sub.3 not part of a cyclic moiety is alkyl containing one to four carbon atoms; and X.sup.- is a pharmaceutically-acceptable anion. The prodrug can be included with a beta-lactam antibiotic in a pharmaceutical composition which can be employed in the treatment of infection in mammals. The above-described compounds hydrolyze in vivo to 4,4-dioxopenicillanic acid.Type: GrantFiled: May 24, 1982Date of Patent: January 31, 1984Assignee: Pfizer Inc.Inventor: Robert F. Myers
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Patent number: 4428937Abstract: 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 15, 1980Date of Patent: January 31, 1984Assignee: Beecham Group LimitedInventor: Thomas T. Howarth
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Patent number: 4428961Abstract: The present invention provides a compound of formula (I): ##STR1## wherein R.sup.1 is a group such that COOR.sup.1 is a carboxyic acid group or a salt or ester thereof;R.sup.3 is hydrogen or an organic radical;n is zero or 1;R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 -C.sub.3 alkyl;X is C.sub.1 -C.sub.6 alkylene optionally substituted by hydroxy or a carboxylic acid group or a salt or ester thereof;Y is an amino, or substituted amino, wherein the substituent is carboxylic acyl, C.sub.1 -C.sub.6 alkyl or a group .dbd.C(R.sup.14)NR.sup.15 R.sup.16 wherein R.sup.15 and or C.sub.1 -C.sub.6 alkyl and R.sup.14 is hydrogen or C.sub.1 -C.sub.6 alkyl, or a group --NR.sup.A R.sup.B wherein R.sup.A and R.sup.B are independently hydrogen or C.sub.1 -C.sub.6 alkyl.Type: GrantFiled: January 23, 1981Date of Patent: January 31, 1984Assignee: Beecham Group LimitedInventors: Robert Southgate, Terence C. Smale, Roger J. Ponsford
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Patent number: 4426390Abstract: A compound of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom, --OH or --OSO.sub.3 H, and R.sub.2 represents a hydrogen atom or an unsubstituted or substituted benzyl group; and a salt thereof; processes for production thereof by fermentation; and uses thereof as antimicrobial agents.Type: GrantFiled: September 29, 1981Date of Patent: January 17, 1984Assignee: Sanraku-Ocean Co., Ltd.Inventors: Mitsuyasu Okabe, Takeo Yoshioka, Yasuo Fukagawa, Rokuro Okamoto, Kageaki Kouno, Tomoyuki Ishikura