Nitrogen Or Oxygen Hetero Atom And At Least One Other Diverse Hetero Ring Atom In The Same Ring Patents (Class 435/120)
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Patent number: 6361979Abstract: The present invention relates to processes for the microbial oxidation of 2-methylquinoxaline to 2-quinoxalinecarboxylic acid which comprise contacting 2-methylquinoxaline with a microorganism, or a suitable mutant thereof, and incubating the resulting mixture under conditions sufficient to yield an amount of said 2-quinoxalinecarboxylic acid. The present processes optionally further comprise the isolation and purification of 2-quinoxalinecarboxylic acid.Type: GrantFiled: January 27, 2000Date of Patent: March 26, 2002Assignee: Pfizer Inc.Inventors: Michael P. Burns, James J. Cawley, John W. Wong
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Patent number: 6361982Abstract: DNA comprising a regulatory gene for clavulanic acid biosynthesis. DNA is no greater than 7 kb in length and has the configuration of restriction sites shown in FIG. 1 or a fragment thereof. Use of DNA in a method for producing clavulanic acid in a host.Type: GrantFiled: August 31, 1995Date of Patent: March 26, 2002Assignee: SmithKline Beecham p.l.c.Inventors: Nicola Jane Walters, Barry Barton, Alison Jane Earl
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Publication number: 20020015984Abstract: Improved purification methods for ansamitocins are disclosed.Type: ApplicationFiled: April 9, 2001Publication date: February 7, 2002Inventors: Mark Fulston, Anna L. Stefanska, Jan E. Thirkettle
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Publication number: 20010019837Abstract: The invention is a process for producing N-substituted glucamines, a process for oxidizing an N-substituted glucamine with an oxidizing microbe or extract thereof, and a process for oxidizing an N-substituted glucamine with an oxidizing microbe or extract thereof and reducing the oxidized N-substituted glucamine to an N-substituted-1-deoxynojirimycin. In addition, a one pot process for producing N-substituted-1-deoxynojirimycin from D-glucose is disclosed.Type: ApplicationFiled: April 14, 1999Publication date: September 6, 2001Inventors: ROY WALTER GRABNER, BRYAN HAYDEN LANDIS, PING TU WANG, MICHAEL LEE PRUNIER, MIKE G. SCAROS
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Patent number: 6277626Abstract: A method of separating enantiomeric lactam esters. The lactam esters are contacted with a biocatalyst, such as an enzyme or a microorganism, in a solution wherein only one enantiomer is selectively hydrolyzed to give the optically active isomer of the corresponding acid. The hydrolysis product is then separated from the unreacted lactam esters. The enzyme is then recycled for reuse in the next enzymatic resolution. The undesired isomer is also racemized and reused in the next enzymatic resolution.Type: GrantFiled: February 16, 1999Date of Patent: August 21, 2001Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mahima Trivedi, Rolando E. Gapud, John S. Ng, Alok K. Awasthi, Ping T. Wang
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Patent number: 6207428Abstract: A process for the isolation of clavulanic acid and pharmaceutically acceptable salts thereof, such as potassium clavulanate, from the aqueous fermentation broth of a clavulanic acid-producing microorganism comprises the microfiltration of the broth without prior treatment.Type: GrantFiled: October 8, 1999Date of Patent: March 27, 2001Assignee: Lek Pharmaceutical & Chemical Co. d.d.Inventor: Egidij Capuder
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Patent number: 6100052Abstract: A batch fermentation is carried out continuously or semicontinuously using strain of Streptomyces clavuligerus for the production of clavulanic acid. The fermentation process is carried out with strict control of the soluble phosphate in the medium both at the beginning and throughout the process.Type: GrantFiled: September 15, 1997Date of Patent: August 8, 2000Assignee: Antibioticos, S.A.Inventors: Carmelita Rodriguez Otero, Miguel Angel Moreno Valle, Manuel Jesus Lopez Nieto, Alfonso Juan Collados De La Vieja, Alejandro Vitaller Alba
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Patent number: 6066656Abstract: The present invention provides 2,5-diamino-3,4-disubstituted-1,6-diphenylhexane (DAD) isosteres comprising benzamide, sulfonamide and anthranilamide subunits, a pharmaceutical composition comprising such compounds, a method of using such compounds to treat retroviral, specifically HIV and more specifically HIV-1 and HIV-2, infections in mammals, particularly humans, a method of synthesizing asymmetric DAD isosteres comprising benzamide, sulfonamide and anthranilamide subunits, and a method of using such compounds to assay new compounds for antiretroviral activity.Type: GrantFiled: March 16, 1998Date of Patent: May 23, 2000Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Ramnarayan S. Randad, John W. Erickson
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Patent number: 6043058Abstract: Known cyclic depsipeptides which are PE 1022F substance and PF 1022H substance, as well as a novel cyclic depsipeptide, PF 1022G substance, are now prepared simultaneously by cultivating a fungal strain capable of producing PF 1022F substance, PF 1022G substance and PF 1022H substance represented by the known PE 1022 strain (deposited under FERM BP-2671) which is a kind of fungus belonging to asporous imperfect fungi (the order Agonomycetales) and is presumable to belong to the genus Xylaria or the genus Rosellinia in the family Xylariaceae.Type: GrantFiled: February 5, 1999Date of Patent: March 28, 2000Assignee: Maiji Seika Kaisha Ltd.Inventors: Makoto Ohyama, Masaaki Takahashi, Yoshiya Shigematsu, Osamu Sakanaka, Yashushi Murai, Katsuharau Iinuma
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Patent number: 5994346Abstract: Exochelins can be used to prevent damage to organs for transplant from the formation or presence of the .circle-solid.OH radical. In particular, the invention is directed to the administration of exochelins to the organ prior to or coincidental with removal from a donor, storage, implantation in a recipient or in conjunction with reestablishment of flow of body fluids to the organ.Type: GrantFiled: October 30, 1997Date of Patent: November 30, 1999Assignee: Regents of the University of CaliforniaInventors: Marcus A. Horwitz, Lawrence D. Horwitz
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Patent number: 5985628Abstract: A generator switch includes phase conductors each equipped with one disconnector and one vacuum switch having a horizontally disposed pole gap. At least one vacuum chamber is provided per phase. The disconnector is constructed as a linear-travel disconnector, and the vacuum chambers are disposed spatially one behind the other, are aligned with the disconnector, and are each accommodated in one tubular housing which surrounds all of the components of a phase as an outer encapsulation.Type: GrantFiled: January 21, 1998Date of Patent: November 16, 1999Assignee: ABB Patent GmbHInventors: Ahmed Sherif Adel, Walter Weber, Horst Plettner
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Patent number: 5985625Abstract: A process for the isolation of clavulanic acid pharmaceutically acceptable salts thereof, such as potassium clavulanate, from the aqueous fermentation broth of a clavulanic acid-producing microogranism comprises the microfiltration of the broth without prior treatment.Type: GrantFiled: July 10, 1998Date of Patent: November 16, 1999Assignee: Lek Pharmaceutical & Chemical Co. ddInventor: Egidij Capuder
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Patent number: 5968788Abstract: Disclosed is a method for producing folic acid, comprising incubating yeast having the ability to produce folic acid of 0.3 mg or more or incubating bacteria having the ability to produce folic acid of 1 mg or more per liter of the culture, thereby accumulating folic acid in the culture.Type: GrantFiled: August 26, 1996Date of Patent: October 19, 1999Assignee: Toray Industries, Inc.Inventors: Reiko Miyata, Tetsu Yonehara
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Patent number: 5945315Abstract: The present invention provides novel cryptophycin compounds having the following structure: ##STR1## The present invention also provides methods for producing cryptophycins from the Nostoc sp. of blue-green algae (cyanobacteria). Pharmaceutical compositions comprising novel cryptophycins are also provided by the present invention, as are methods for using cryptophycins to inhibit the proliferation of hyperproliferative cells. The present invention further provides methods for using cryptophycins to inhibit the proliferation of hyperproliferative cells with drug resistant phenotypes, and to treat pathological conditions, such as neoplasia.Type: GrantFiled: November 4, 1996Date of Patent: August 31, 1999Assignee: University of HawaiiInventors: Richard E. Moore, Gregory M. L. Patterson
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Patent number: 5945316Abstract: The present invention relates to a process for the preparation of lactic-acid-containing, optically active, cyclic depsipeptides having 18 ring atoms with the aid of fungal strains of the species Fusarium or enzymatic preparations isolated therefrom.Type: GrantFiled: March 20, 1997Date of Patent: August 31, 1999Assignee: Bayer AktiengesellschaftInventors: Peter Jeschke, Achim Harder, Norbert Mencke, Horst Kleinkauf, Rainer Zocher
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Patent number: 5914263Abstract: The invention relates to an enzymatic process for the stereoselective preparation of a hetero-bicyclic alcohol enantiomer, characterized in that a substantially pure enantiomer of the general formula ##STR1## wherein X is O, S, NH, N--(C.sub.1 -C.sub.4)alkyl or CH.sub.2 ; Y.sub.1, Y.sub.2 and Y.sub.3 are each independently hydrogen or substituents selected from halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl, nitro and cyano;the NO.sub.2 substituent is attached to the bicyclic ring system in the 5- or 7-position; andthe C*-atom has either the R or the S configuration;is prepared from its corresponding alcohol racemate by the following successive reaction steps:(1) stereoselective esterification,(2) separation of the alcohol from the ester produced,(3) hydrolysis of the ester to produce the corresponding alcohol enantiomer, and(4) conversion of the alcohol enantiomer into the starting racemate under basic conditions in order to allow its reuse.Type: GrantFiled: July 23, 1997Date of Patent: June 22, 1999Assignee: Duphar International Research B.V.Inventors: Nicolaas Buizer, Chris G. Kruse, Melle Van Der Laan, Georges Langrand, Gustaaf J.M. Van Scharrenburg, Maria C. Snoek
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Patent number: 5840682Abstract: The invention is directed to a compound of formula ##STR1## in which R represents a hydroxyl, alkyloxy, phenylalkyloxy or --NH--CH.sub.2 --COOH radical, R.sub.1 represents a hydrogen atom, an adamantylacetyl, adamantylcarbonyl, norbornylacetyl, norbornylphenoxycarbonyl, benzoyl, nicotinoyl, 4-phenylbenzoyl, 4-tert-butylbenzoyl or 2-pyrrolidinecarbonyl radical or a protective group for an amine functional group, R.sub.2 represents an Arg or Lys residue, R.sub.3 represents an Arg or Lys residue, R.sub.4 represents a Pro residue, m, n and p, which are the identical or different, represent a number equal to 0 or 1, R.sub.5 and R.sub.6 are identical and represent a hydroxyl or methoxy radical and R.sub.7 represents a hydrogen, chlorine, bromine or iodine atom or a nitro radical, or the compound wherein one or a number of peptide bonds between two amino acid residues are replaced by --CH.sub.2 --NH bonds or the peptide bond between the R.sub.2 and R.sub.3 amino acid residues is replaced by a CH.dbd.Type: GrantFiled: November 19, 1996Date of Patent: November 24, 1998Assignee: Rhone-Poulenc Rorer S.A.Inventors: Francois-Frederic Clerc, Marie-Christine Dubroeucq, Gerard Helynck, Jean Leboul, Jean-Paul Martin
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Patent number: 5837677Abstract: The invention is directed toward the use of desferri-Exochelins to destroy cancer cells or retard or eliminate the growth of those cancer cells.Type: GrantFiled: June 25, 1997Date of Patent: November 17, 1998Assignee: Keystone Biomedical, Inc.Inventors: Lawrence D. Horwitz, Kathryn B. Horwitz
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Patent number: 5814495Abstract: The present invention is directed to a process for producing melanins, their precursors and their analoges, hereinafter referred to generically as melanins. According to the invention, melanins are produced in amounts greater than about 3.3 grams wet weight per liter of growth medium. The enhanced production of melanin can be achieved by manipulating the constituents of the growth medium, and/or attenuating fermentations conditions, and/or by genetically engineering microorganisms to produce melanins, and/or mutating the microorganisms.Type: GrantFiled: March 14, 1995Date of Patent: September 29, 1998Assignee: Biosource Technologies, Inc.Inventors: Guy della-Cioppa, Stephen J. Garger, Jr., Genadie G. Sverlow, Thomas H. Turpen, Laurence K. Grill, Miles R. Chedekal
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Patent number: 5801023Abstract: This invention provides compounds of the following chemical formula or their pharmaceutically-acceptable salts: ##STR1## wherein R is hydrogen or chloro. Also, the present invention provides a process for the production of the compound of formula I, which comprises cultivating a microorganism having the identifying characteristics of Aspergillus fischeri var. thermomutatis ATCC 18618 or the like, and then isolating the compound of formula I from the fermentation broth. The pyrrolobenzoxazine compounds of formula I of this invention have broad antiparasitic activity, and thus are useful as antiparasitic agents, especially as anthelmintics.Type: GrantFiled: November 29, 1996Date of Patent: September 1, 1998Assignee: Pfizer Inc.Inventors: Yasuhiro Kojima, Yuji Yamauchi, Nakao Kojima, Bernard F. Bishop
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Patent number: 5780274Abstract: A process for the isolation of clavulanic acid and pharmaceutically acceptable salts thereof, such as potassium clavulanate, from the aqueous fermentation broth of a clavulanic acid-producing microorganism comprises the microfiltration of the broth without prior treatment. Additional steps may include an optional ultrafiltration of the microfiltration filtrate, concentration of the filtrate, direct extraction of the concentrated filtrate with a water-immiscible organic solvent, washing, drying, and concentration of the organic solvent, and isolation of the clavulanic acid or a pharmaceutically acceptable salt from the organic solvent.Type: GrantFiled: April 10, 1996Date of Patent: July 14, 1998Assignee: Lek Pharmaceutical and Chemical Company D.D.Inventor: Egidij Capuder
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Patent number: 5753471Abstract: A process for the biotechnological preparation of alcohols, aldehydes and carboxylic acids by oxidation of compounds of the formula R.sup.1 --C(CH.sub.3).dbd.CR.sup.2 R.sup.3, where R.sup.1, R.sup.2 and R.sup.3 have the meanings indicated in the description, with the aid of microorganisms is described.Type: GrantFiled: December 28, 1995Date of Patent: May 19, 1998Assignee: BASF AktiengesellschaftInventors: Uwe Pressler, Friedhelm Balkenhohl, Bernhard Hauer, Wolfgang Ladner, Ursula Schnell, Horst Ralf Staudenmaier
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Patent number: 5747303Abstract: The invention is directed to a novel compound of formula ##STR1## in which R is a hydroxyl, alkyloxy, phenylalkyloxy or --NH--CH.sub.2 --COOH radical, R' and R" are identical and are each a hydroxy or methoxy radical and R'" represents a hydrogen, bromine, chlorine or iodine atom or a nitro radical. The invention is also directed to the salts of said compounds and their use.Type: GrantFiled: November 19, 1996Date of Patent: May 5, 1998Assignee: Rhone-Poulenc Rorer S.A.Inventors: Jean-Jacques Debernard, Catherine Dubertret, Gerard Helynck, Jean Leboul, Jean-Paul Martin
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Patent number: 5733755Abstract: A method for manufacturing S-3-(4'-tert-butyl)-phenyl-2-methyl propylamines having the structure I ##STR1## where NR.sub.1 R.sub.Type: GrantFiled: November 5, 1996Date of Patent: March 31, 1998Assignee: Industrie Chimiche Capparo S.p.A.Inventors: Vitomir Sunjic, Maja Majeric, Zdenko Hamersak, Amir Avdagic
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Patent number: 5721209Abstract: Exochelins can be used to prevent damage to living tissue from the formation or presence of the (.cndot.OH) radical. In particular, the invention is directed to the administration of exochelins to infarcted myocardium prior to or coincidental with reperfusion to prevent damage to myocardium from iron mediated free radical formation. Also presented is the chemical structure of exochelins and modified exochelins as well as other applications of these materials in the treatment and diagnosis of disease in mammals.Type: GrantFiled: February 3, 1995Date of Patent: February 24, 1998Assignee: The Regents of the University of CaliforniaInventors: Lawrence D. Horwitz, Marcus A. Horwitz, Bradford W. Gibson, Joseph Reeve
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Patent number: 5661014Abstract: Enantiomeric glutarimides such as aminoglutethimide and rogletimide are prepared by cyclisation of a corresponding ester-nitrile which is a good substrate for biotransformation with an enantiospecific esterase.Type: GrantFiled: May 30, 1995Date of Patent: August 26, 1997Assignee: Chiroscience LimitedInventors: Christopher Thomas Evans, Raymond McCague, Stephen John Clifford Taylor
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Patent number: 5656464Abstract: The present invention relates to a process for the preparation of lactic-acid-containing, optically active, cyclic depsipeptides having 18 ring atoms with the aid of fungal strains of the species Fusarium or enzymatic preparations isolated therefrom.Type: GrantFiled: February 17, 1995Date of Patent: August 12, 1997Assignee: Bayer AktiengesellschaftInventors: Peter Jeschke, Achim Harder, Norbert Mencke, Horst Kleinkauf, Rainer Zocher
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Patent number: 5618707Abstract: A stereoselective reduction of compound II to compound of formula I ##STR1## which comprises adding ketone substrate II to a culture broth of the Zygosaccharomyces bailii ATCC 38924, incubating the resulting mixture, and isolating a hydroxy compound of formula I, is described. The resulting compound of formula I is useful as an intermediate in the preparation of 1-(4-fluorophenyl)-3(R)-[3(S)-hydroxy-3-(4-fluorophenyl)propyl]-4(S)-(4-hy droxyphenyl)-2-azetidinone which is a serum cholesterol lowering agent. Also described is a stereoselective reduction of a compound of formula IV to compound of formula III ##STR2## using Schizosaccharomyces octosporus ATCC 2479.Type: GrantFiled: January 4, 1996Date of Patent: April 8, 1997Assignee: Schering CorporationInventors: Michael J. Homann, Edward Previte
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Patent number: 5593871Abstract: This invention relates to the enantioselective biologically-catalyzed hydrolysis of certain racemic nitriles to the corresponding R- or S-amides, chemically or biologically-catalyzed hydrolysis of the amides to the corresponding R- or S-acids in a batch process or in a continuous process that employs racemization and recycling of enantiomeric nitrile intermediates, the racemic nitriles being selected from the group, A--C(R.sup.1)(R.sup.2)CN, wherein A, R.sup.1 and R.sup.2 are as defined in the text, as well as certain biological materials employed to catalyze the process.Type: GrantFiled: February 15, 1995Date of Patent: January 14, 1997Assignee: E. I. Du Pont de Nemours and CompanyInventors: David L. Anton, Robert D. Fallon, Barry Stieglitz, Vincent G. Witterholt
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Patent number: 5591614Abstract: This invention concerns a process for enzymatically preparing a compound of formula (1) ##STR1## from the compound of formula (2) ##STR2## by way of a microorganism or an acellular preparation derived from this microorganism. The microorganism and acellular preparation oxidizes the 2-3 bond of the macrolactones' D-proline into dehydroproline.Type: GrantFiled: April 5, 1995Date of Patent: January 7, 1997Assignee: Rhone-Poulenc Rorer, S.A.Inventors: Francis Blanche, Denis Thibaut
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Patent number: 5559017Abstract: A novel process comprises reducing a benzazepine or benzothiazepine at the 3-position in d-cis configuration by treatment with reductase-supplying microorganisms or enzymes derived therefrom. The process can be catalyzed in a single stage by growing microbial cultures or in a two-stage fermentation/transformation by resting cell-suspensions. The enzymes derived from the microorganisms can be used in free state or immobilized form. The microorganisms and enzymes catalyzes the specific reduction with 90 to 99% conversion efficiency to 99% or greater optical purity of the desired enantiomer.Type: GrantFiled: November 19, 1990Date of Patent: September 24, 1996Assignee: E. R. Squibb & Sons, Inc.Inventors: Ramesh N. Patel, Laszlo J. Szarka, Richard H. Mueller
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Patent number: 5484708Abstract: The invention concerns a method for the colorimetric determination of an analyte by means of enzymatic oxidation with a PQQ-dependent dehydrogenase in the presence of an electron acceptor from the group of the electron-rich aromatic nitroso compounds by enzymatic reduction of the nitroso compound to an imino compound and detection of the imino compound by color formation. In addition the invention concerns a corresponding agent containing a PQQ-dependent dehydrogenase, an electon-rich aromatic nitroso compound as well as, if desired, a detection reagent for imino compounds. The invention in addition concerns novel nitrosoamino compounds which form colored quinone diimines on reduction as well as their use for the colorimetric enzymatic determination of an analyte.Type: GrantFiled: April 8, 1994Date of Patent: January 16, 1996Assignee: Boehringer Mannheim GmbHInventors: Joachim Hoenes, Volker Unkrig
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Patent number: 5290682Abstract: Compounds which are useful as substrates for enzymes are disclosed. An enzyme-controlled process is provided for generating a colored species from an initially substantially colorless material as a result of enzymatic attack. The process can be exploited to provide an enzyme-amplified diagnostic assay method to detect an analyte of interest present in a test sample.Type: GrantFiled: May 31, 1991Date of Patent: March 1, 1994Assignee: Polaroid CorporationInventors: Frank A. Meneghini, Paul S. Palumbo
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Patent number: 5236832Abstract: A microbiological process for the oxidation of methyl groups in aromatic 5- or 6-member ring heterocycles to the corresponding carboxylic acid. The heterocycle serves as the substrate and exhibits no substituent on the carbon atoms adjacent to the methyl groups to be oxidized. The reaction of the heterocycle takes place by means of microorganisms of the genus Pseudomonas utilizing toluene, xylene, or cymene. The enzymes of the microorganisms been previously induced.Type: GrantFiled: October 30, 1991Date of Patent: August 17, 1993Assignee: Lonza, Ltd.Inventor: Andreas Kiener
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Patent number: 5217884Abstract: A process using microorganisms which contain genes, which form an active xylene monooxygenase, which form no effective, chromosomally or plasmid-coded alcohol hydrogenase, and which are, thus, capable of hydroxylating methyl groups on aromatic 5- or 6-atom heterocycles to the corresponding hydroxymethyl derivatives, for the production of hydroxymethylated 5- or 6-atom heterocycles.Type: GrantFiled: September 23, 1991Date of Patent: June 8, 1993Assignee: Lonza Ltd.Inventors: Thomas Zimmermann, Andreas Kiener, Shigeaki Harayama
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Patent number: 5215900Abstract: Fermentation of the microorganism Streptomyces sp. (MA6804), ATTC No. 55095, in the presence of the HIV reverse transcriptase inhibitor ##STR1## yields a 5-(1-hydroxy)ethyl analog which is useful in the prevention or treatment of infection by HIV and the treatment of AIDS.Type: GrantFiled: June 7, 1991Date of Patent: June 1, 1993Assignee: Merck & Co., Inc.Inventors: Shieh-Shung T. Chen, George Doss
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Patent number: 5213973Abstract: A microbiological process for oxidation of methyl groups in aromatic 5- or 6-ring heterocycles to the corresponding carboxylic acid. The reaction of the heterocycle takes place by microorganisms of the genus Pseudomonas, which utilize toluene, xylene or cymene. An inducer, the aromatic heterocycle, as the substrate, and a carbon source and energy source are fed in and, after the maximal product concentration is reached, the product is separated.Type: GrantFiled: July 3, 1991Date of Patent: May 25, 1993Assignee: Lonza Ltd.Inventor: Frans Hoeks
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Patent number: 5206157Abstract: N-substituted dialkanolamine may be converted to N-substituted-2-morpholone by the action of Gluconobacter oxydan ATCC #621 or Gluconobacter roseus IAM 1841.Type: GrantFiled: September 28, 1988Date of Patent: April 27, 1993Assignee: Texaco Inc.Inventor: Kechia J. Chou
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Patent number: 5204248Abstract: Disclosed is a process for preparing 2-halogeno-3-hydroxy-3-phenylpropionic acid ester compounds represented by the formula (I): ##STR1## wherein Ring A is a phenyl group which may be substituted, R.sup.1 is an ester residue, and X is a halogen atom, which comprises permitting an enzyme having the ability of stereoselectively reducing oxo group to hydroxy group to act on 2-halogeno-3-oxo-3-phenylpropionic acid ester compounds represented by the formula (II): ##STR2## wherein Ring A, R.sup.1 and X have the same meanings as defined above.Type: GrantFiled: March 22, 1991Date of Patent: April 20, 1993Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takeji Shibatani, Takuo Nishida, Hiroaki Matsumae
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Patent number: 5192668Abstract: A dipeptide isostere is the biotransformed product after incubation with a culture of Streptomyces. It inhibits HIV protease, and is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: February 27, 1992Date of Patent: March 9, 1993Assignee: Merck & Co., Inc.Inventors: Laszlo R. Treiber, Lawrence F. Colwell, Jr., Byron H. Arison, Georgette Dezeny, Russell B. Lingham, Wayne J. Thompson, Suresh K. Balani
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Patent number: 5188950Abstract: Novel dipeptide isosteres are the biotransformed products after incubation with rat liver slices. They inhibit HIV protease, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts (when appropriate), pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: February 27, 1992Date of Patent: February 23, 1993Assignee: Merck & Co., Inc.Inventors: Suresh K. Balani, Harri G. Ramjit, Steven M. Pitzenberger, Michael S. Schwartz, Anthony Y. H. Lu
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Patent number: 5169769Abstract: Incubation of ##STR1## with a preparation from mammalian organ yields as biotransformation products the 6-hydroxymethyl and 5-(1-hydroxy)ethyl anologs. These products are useful in the prevention or treatment of infection by HIV and the treatment of AIDS.Type: GrantFiled: June 7, 1991Date of Patent: December 8, 1992Assignee: Merck & Co., Inc.Inventors: Suresh K. Balani, Byron H. Arison, Harri G. Ramjit, Anthony D. Theoharides, Laura R. Kauffman
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Patent number: 5135858Abstract: An improved biological conversion of a nitrile such as acrylonitrile or a cyanopyridine into the corresponding carboxylic acid such as acrylic acid or a nicotinic acid by the action upon the nitrile of a nitrilase enzyme, in which the improvement resides in the use as the source of the enzyme of a microorganism of Rhodococcus, such as Rh. rhodochrous J-1, FERM BP-1478, which is cultured in the presence of a lactam compound.Type: GrantFiled: February 22, 1991Date of Patent: August 4, 1992Assignees: Hideaki Yamada, Nitto Kagaku Kogyo Kabushiki KaishaInventors: Hideaki Yamada, Toru Nagasawa, Tetsuji Nakamura
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Patent number: 5130252Abstract: A method for resolving racemic mixtures of compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof that includes the steps of reacting the OR.sub.3 group of either compound with an esterifying agent in the case where R.sub.3 is H or a lower alkyl group; sujecting the compound to the action of an esterase capable of preferentially hydrolyzing either the (+) or (-) enantiomeric form of the compound; and separating the unhydrolyzed compound from the hydrolyzed compound.Type: GrantFiled: May 14, 1990Date of Patent: July 14, 1992Assignee: Synthetech, Inc.Inventors: Charles R. Eck, Paul C. Ahrens, Rae M. Saltzstein
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Patent number: 5122461Abstract: The invention relates to a novel method for preparing pyrocatecholic compounds from monophenolic compounds using catalysis by monophenol monooxygenase in an aqueous solution containing metal ions. The metal ions form complexes with the pyrocatecholic products. This method increases the yield of pyrocatecholic products. In particular, the method of the instant invention can be used to increase the yield of L-DOPA, a drug used in the treatment of Parkinson's disease.Type: GrantFiled: November 19, 1990Date of Patent: June 16, 1992Assignee: Industrial Technology Research InstituteInventors: Kuang-Pin Hsiung, Feng-Tsun Lee, Chung-Long Hsieh
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Patent number: 5104798Abstract: A microbiological process for the oxidation of methyl groups in aromatic 5- or 6-member ring heterocycles to the corresponding carboxylic acid. The heterocycle serves as the substrate and exhibits no substituent on the carbon atoms adjacent to the methyl groups to be oxidized. The reaction of the heterocycle takes place by means of microorganisms of the genus Pseudomonas utilizing toluene, xylene, or cymene. The enzymes of the microorganisms have been previously induced.Type: GrantFiled: February 5, 1991Date of Patent: April 14, 1992Assignee: Lonza Ltd.Inventor: Andreas Kiener
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Patent number: 5026642Abstract: In a process for the reduction of ketones, the keto compounds are enantioselectively reduced to give secondary alcohols by means of microorganisms. Keto compounds of the formulaR.sup.3 NH--CHR.sup.1 --CO--CH.sub.2 --COOR.sup.2in which R.sup.1, R.sup.2 and R.sup.3 have the meanings defined herein are used as starting compounds.Type: GrantFiled: July 22, 1988Date of Patent: June 25, 1991Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Hans-Eckart Radunz, Harry Schwartz, Martin Heinrich
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Patent number: 5006466Abstract: Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No. 53527, while the analog of Formula II is produced by chemical synthesis.Type: GrantFiled: October 26, 1989Date of Patent: April 9, 1991Assignee: Merck & Co., Inc.Inventors: Yiu-kuen T. Lam, Otto D. Hensens, Raymond S. Chang, Cheryl D. Schwartz, Deborah L. Zink
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Patent number: 4960698Abstract: L-654,040 of the structure: ##STR1## is a novel antibacterial and isolated from the novel organism Streptoverticillium synroense, strain MA6011, deposited at the ATCC.Type: GrantFiled: May 9, 1989Date of Patent: October 2, 1990Assignee: Merck & Co., Inc.Inventors: Sara A. Currie, Thomas W. Miller, Eugene L. Dulaney, James P. Springer, Mary E. Valiant, Sagrario M. del Val, Sheldon B. Zimmerman
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Patent number: 4946835Abstract: A novel dioxa-diazacyclohexadecenetetrone isolated from the fermentation of a cyanobacterium (Nostoc sp.) is described. The compound is a new antifungal agent with a specificity generally toward filamentous fungi but also effective against Cryptococcus sp.Type: GrantFiled: July 15, 1988Date of Patent: August 7, 1990Assignee: Merck & Co., Inc.Inventors: Charles F. Hirsch, Jerrold M. Liesch, Michael J. Salvatore, Robert E. Schwartz, David F. Sesin