The -c(=x)- Group, An Unsubstituted Benzene Ring And -nhh Bonded Directly To The Same Carbon Atom (e.g., Ampicillin, Etc.) Patents (Class 540/336)
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Patent number: 8975219Abstract: A fabric cleaning composition comprising from 1% to 20% by weight of the fabric cleaning composition of an oxygen-based bleaching source and a hueing agent, and wherein the neat composition has a pH between 2.5 and 5.5, and a method of using said fabric cleaning composition.Type: GrantFiled: May 16, 2012Date of Patent: March 10, 2015Assignee: The Procter & Gamble CompanyInventors: Margherita Scartozzi, Luca Sarcinelli, Sophie Anne Marguerite Goellner, Enza Ceccobelli, Leo Gagliardi
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Publication number: 20150050713Abstract: Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.Type: ApplicationFiled: July 25, 2014Publication date: February 19, 2015Inventors: Michael P. Malakhov, Fang Fang
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Publication number: 20140099696Abstract: Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.Type: ApplicationFiled: April 30, 2013Publication date: April 10, 2014Applicant: Ansun Biopharma, Inc.Inventors: Michael P. Malakhov, Fang Fang
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Publication number: 20120141590Abstract: Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.Type: ApplicationFiled: September 30, 2011Publication date: June 7, 2012Inventors: Michael Malakhov, Fang Fang
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Publication number: 20110282028Abstract: The invention provides a method of identifying an inhibitor of LtaS comprising: (a) providing bacteria which comprise a mutation in the mbl gene or homologue thereof; (b) culturing the bacteria of (a) in the presence of a test substance under conditions of low magnesium; (c) monitoring the growth of the bacteria; wherein growth or more rapid growth of the bacteria compared to growth in the absence of the test substance is indicative that the test substance is an inhibitor of LtaS.Type: ApplicationFiled: December 4, 2009Publication date: November 17, 2011Applicant: UNIVERSITY OF NEWCASTLE UPON TYNEInventors: Jeffery Errington, Kathrin Schirner
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Publication number: 20110269731Abstract: The present invention relates to a complex made up of at least one beta-lactam molecule covalently bonded to at least one hydrocarbon radical including at least 18 carbon atoms and containing at least one unit of 2-methyl-buta-2-ene, to nanoparticles of said complexes, and to a method for preparing same, said complex and/or said nanoparticles optionally being in the form of a lyophilisate. The present invention also relates to a pharmaceutical composition including at least said complex and/or said nanoparticles. The invention finally relates to said complex and/or to said nanoparticles for the treatment and/or prevention of bacterial infections, in particular caused by strains that are sensitive to beta-lactams.Type: ApplicationFiled: October 28, 2009Publication date: November 3, 2011Inventors: Patrick Couvreur, Didier Demaele, Fatima Zouhiri
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Publication number: 20080207583Abstract: A novel process for preparing a stable granulate, which comprises a mixture of amoxicillin trihydrate and amoxicillin sodium, by means of extrusion granulation of amoxicillin trihydrate with an aqueous solution of sodium hydroxide, sodium bicarbonate, sodium carbonate and mixture thereof or with an aqueous solution of sodium salt of (C1-8) organic acid as a sodium source to form a moist extruded mass, which is granulated through a sieve and dried the obtained granulate, is disclosed. Alternatively, a novel process for preparing a stable granulate comprising pure amoxicillin sodium may be obtained according to the above extrusion granulation process as well. In a further aspect the present invention relates to a novel stable granulate comprising the mixture of amoxicillin trihydrate and amoxicillin sodium or alternatively, to a novel stable granulate comprising pure amoxicillin sodium, whenever prepared according to the above described process.Type: ApplicationFiled: May 1, 2006Publication date: August 28, 2008Applicant: SANDOZ AGInventor: Franz Xaver Schwarz
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Patent number: 6949521Abstract: Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2?-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.Type: GrantFiled: May 4, 2001Date of Patent: September 27, 2005Assignees: The University of Georgia Research Foundation, Inc., Emory UniversityInventors: Chung K. Chu, Lakshmi P. Kotra, Konstantine Manouilov, Jinfa Du, Raymond Schinazi
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Patent number: 6414141Abstract: Applicants have developed a process for purifying an ampicillin pro-drug ester, e.g., bacampicillin, or an acid addition salt thereof of formula I. The process comprises a step wherein a crude solution of the pro-drug ester is subjected to an evaporation which is controlled by the evaporation rate of the organic solvent such that a continuous operation is accomplished for the crystallization of the desired purified pro-drug ester or salt thereof. Said crystallization is preferably preceded by an aqueous phase extraction and/or an organic phase extraction, both preferably also being performed continuously.Type: GrantFiled: January 26, 1999Date of Patent: July 2, 2002Assignee: AstraZeneca ABInventors: Hans-Jürgen Federsel, Erik Könberg
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Patent number: 6013647Abstract: This invention relates to new benzoxazinedione derivatives corresponding to the formula I: ##STR1## wherein R.sup.1 =H or carboxyalkyl, R.sup.2 =H, alkyl or phenyl, and R.sup.3 represents different acid groups derived from amino acids, dipeptides and hydrazones or conjugates thereof with active ingredients, e.g. antibiotics. The compounds may be present as free acids, in the form of their salts or as readily cleavable esters. The compounds according to the invention constitute heterocyclically protected catechol derivatives and are effective as siderophores against gram-negative bacterial strains, particularly against Pseudomonads and strains of E. coli and Salmonella. In the form of their conjugates with active ingredients, e.g. antibiotics (as "siderophore-antibiotic conjugates"), they can transport the latter into bacterial cells and can improve or extend the antibacterial effect thereof, sometimes even in relation to bacterial strains which are resistant to other .beta.-lactams.Type: GrantFiled: March 5, 1998Date of Patent: January 11, 2000Assignee: Gruenenthal GmbHInventors: Lothar Heinisch, Steffen Wittmann, Ute Moellmann, Rolf Reissbrodt
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Patent number: 5607671Abstract: The invention concerns medical use, a medical method and a pharmaceutical preparation. The invention allows the action of .beta.-lactam antibiotics to be targeted and their side effects to be reduced by inactivation of part of the antibiotic in a desired section of the digestive tract distal to the stomach by administering, separately from or simultaneously with antibiotic, and enzyme, such as .beta.-lactamase, which breaks down said antibiotic.Type: GrantFiled: September 14, 1994Date of Patent: March 4, 1997Inventor: Pekka U. Heino
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Patent number: 5599987Abstract: An integrated process for producing cyclohexanone oxime, a caprolactam precursor, is provided wherein isopropanol is utilized to generate the hydrogen peroxide oxidizing agent. The acetone produced as a co-product is recycled back to the secondary alcohol by hydrogenation. Ammoximation of cyclohexanone is performed in the presence of water and an alcohol other than isopropanol such as methanol or t-butyl alcohol.Type: GrantFiled: March 31, 1995Date of Patent: February 4, 1997Assignee: Arco Chemical Technology, L.P.Inventors: Guy L. Crocco, John C. Jubin, Jr., John G. Zajacek
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Patent number: 5451701Abstract: An integrated process for producing cyclohexanone oxime, a caprolactam precursor, is provided wherein a secondary alcohol is utilized to generate the hydrogen peroxide oxidizing agent and as a reaction medium for ammoximation. The ketone produced as a co-product is recycled back to the secondary alcohol by hydrogenation.Type: GrantFiled: June 27, 1994Date of Patent: September 19, 1995Assignee: Arco Chemical Technology, L.P.Inventors: John G. Zajacek, John C. Jubin, Guy L. Crocco
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Patent number: 5304643Abstract: .epsilon.-Caprolactam is prepared by subjecting cyclohexanone oxime in a gas phase to a catalytic reaction using zeolite catalysts in the presence of water and at least one compound selected from alcohols and ether compounds.Type: GrantFiled: November 25, 1992Date of Patent: April 19, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Hiroshi Kajikuri, Masaru Kitamura, Yasuhiko Higashio
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Patent number: 4889929Abstract: Process for the preparation of 1'-ethoxy carbonyloxy ethyl esters of penicillins, wherein a compound of the formula ##STR1## in which A is phenyl, phenoxy or 4-hydroxyphenyl, B is hydrogen, an amino group or a protected amino group and Z is hydrogen or a cation selected from the group of alkali metal, tri (lower alkyl ) ammonium and tetra (lower alkyl) ammonium, is reacted with 1-bromoethyl ethyl carbonate in an organic solvent and when B is a protected amino group the protecting group is split off to yield a primary amino group.There are also provided novel compounds of the formula ##STR2## in which Ph is phenyl and R is CH.sub.3 -- or C.sub.2 H.sub.5 --.Type: GrantFiled: March 26, 1987Date of Patent: December 26, 1989Assignee: Astra Lakemedel AktiebolagInventors: Jacob Vaya, David Ladkani, Clara Schoenberger, Joseph Kaspi, Gad Salemnick, Haim Yellin, Stephan Cherkez
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Patent number: 4882325Abstract: Crystalline 1,1-dioxopenicillanoyloxymethyl 6-(D-.alpha.-amino-.alpha.-phenylacetamido)penicillanate napsylate. The product may be prepared by reacting 1,1-dioxopenicillanoyloxymethyl 6-(D-.alpha.-amino-.alpha.-phenylacetamido)penicillanate or a salt thereof with 2-naphthalenesulfonic acid or salt thereof.Type: GrantFiled: October 21, 1988Date of Patent: November 21, 1989Assignee: Leo Pharmaceutical Products Ltd. A/SInventors: Wagn O. Godtfredsen, Welf von Daehne
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Patent number: 4866170Abstract: A stable trihydrate of (2S, 5R, 6R)-6-{(2R)-2-[(2R)-2-amino-3-(N-methylcarbamoyl)propionamido]-2-(p-hydrox yphenyl)acetamido}-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-c arboxylic acid and process for preparing the same are disclosed.Type: GrantFiled: September 18, 1987Date of Patent: September 12, 1989Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Susumu Ohshiro, Masaru Senuma, Mitsuyoshi Wagatsuma
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Patent number: 4840944Abstract: The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R.sub.1 stands for a phenyl, 4-hydroxyphenyl, 1,4-cyclohexadienyl or a 3-thienyl group; R.sub.2 represents a primary amino or a carboxy group; R.sub.3 is a hydrogen atom, or a lower alkyl, aryl or aralkyl radical, and A stands for a radical of a .beta.-lactamase inhibitor containing a .beta.-lactam ring as well as a carboxy group, A being connected via the carboxy group.The present invention provides new compounds useful in the treatment of bacterial infections. The new compounds are in particular strongly active against .beta.-lactamase producing bacteria.Type: GrantFiled: January 24, 1980Date of Patent: June 20, 1989Assignee: Leo Pharmaceutical Products Ltd.Inventors: Wagn O. Godtfredsen, Welf von Daehne
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Patent number: 4831025Abstract: The present invention relates to a crystalline hydrate of a salt of the antimicrobial agent 1,1-dioxopenicillanoyloxymethyl 6-(D-.alpha.-amino-.alpha.-phenylacetamido)penicillanate with p-toluenesulfonic acid, more particularly the mono- and dihydrate.The hydrates are easily obtained in a crystalline state devoid of organic solvent residues, they show good stability on storage, they are effectively absorbed and hydrolyzed in vivo, and they are thus specifically suitable for medical treatment of patients, in particular for oral administration.Type: GrantFiled: March 13, 1987Date of Patent: May 16, 1989Assignee: Leo Pharmaceutical Products Ltd.Inventors: Wagn O. Godtfredsen, Welf von Daehne
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Patent number: 4820857Abstract: The novel compound .alpha.-bromodiethylcarbonate, novel methods for the preparation thereof, its use in the preparation of 1-ethoxycarbonyloxyethyl esters of penicillins and cephalosporins, and improvements in the method for preparing such esters.Type: GrantFiled: April 13, 1988Date of Patent: April 11, 1989Assignee: Astra Lakemedel AktiebolagInventors: Derek R. Palmer, Robert G. Tyson
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Patent number: 4626532Abstract: A new process for the stabilization of bacampicillin hydrochloride against degradation by humidity characterized by the incorporation of between 3 to 9% by weight of straight-chain alkanes, alkenes, fatty acids, alcohols, and esters of fatty acids and alcohols with molecular weights between 144 and 350, which may be carried out in one step together with wetmassing for granulation.Type: GrantFiled: October 29, 1985Date of Patent: December 2, 1986Assignee: Astra Lakemedel AktieboagInventors: Ulf A. Kjellberg, Per G. H. Nyqvist, Jan U. Stenhede, Lars B. Stenmark