Preparing Heterocyclic Carbon Compound Having Only O, N, S, Se, Or Te As Ring Hetero Atoms Patents (Class 435/117)
  • Publication number: 20040014182
    Abstract: The present invention relates to a nucleotide sequence which encodes a benzaldehyde lyase and to its use in a process for stereoselectively preparing 2-hydroxyketone group-containing compounds.
    Type: Application
    Filed: January 2, 2003
    Publication date: January 22, 2004
    Inventors: Martina Pohl, Michael Muller, Ayhan Demir
  • Patent number: 6670157
    Abstract: The invention concerns methods for preparing pristinamycin IIB and methods for preparing modified pristinamycin IIB.
    Type: Grant
    Filed: August 9, 2000
    Date of Patent: December 30, 2003
    Assignee: Aventis Pharma S.A.
    Inventors: Veronique Blanc, Francis Blanche, Joel Crouzet, Nathalie Jacques, Patricia Lacroix, Denis Thibaut, Monique Zagorec, Laurent Debussche, Valerie De Crecy-Lagard
  • Patent number: 6660504
    Abstract: The present invention provides a process for preparing a phospholipid in an aqueous system in which hydrolysis is extremely controlled, and the synthetic yield is improved. A process for exchanging a base of a phospholipid as a raw material by subjecting the phospholipid to the action of phospholipase D in the presence of a receptor having a hydroxyl group, in which the reaction is carried out in an aqueous system, a phospholipid adsorbed on a carrier is used as a raw material phospholipid, and the receptor and the phospholipase D are used in free forms.
    Type: Grant
    Filed: January 11, 2002
    Date of Patent: December 9, 2003
    Assignee: Rinoru Oil Mills Co., Ltd.
    Inventors: Tsuneo Yamane, Yugo Iwasaki, Yukiko Mizumoto, Masaaki Kasai, Takahiro Okada
  • Patent number: 6638758
    Abstract: 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: Grant
    Filed: June 6, 2001
    Date of Patent: October 28, 2003
    Assignee: G.D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Mahima Trivedi, Rolando E. Gapud, John S. Ng, Alok K. Awasthi, Ping T. Wang
  • Patent number: 6635455
    Abstract: A process for producing pyrrole-2-carboxylic acid which comprises the steps of: allowing a microorganism that is derived from the genus Serratia, is capable of catalyzing decarboxylation of pyrrole-2-carboxylic acid, and is capable of catalyzing the synthesis of pyrrole-2-carboxylic acid from pyrrole in the presence of carbonate ion, or the microorganism optionally processed, to act on pyrrole; and recovering the pyrrole-2-carboxylic acid generated.
    Type: Grant
    Filed: July 5, 2001
    Date of Patent: October 21, 2003
    Assignee: Mitsubishi Rayon Co., Ltd.
    Inventor: Toru Nagasawa
  • Patent number: 6630330
    Abstract: Herein is disclosed a method of generating ascorbic acid from yeast. In one embodiment, the yeast is a Zygosaccharomyces spp. or a Kluyveromyces spp. growing in a medium comprising an ascorbic acid precursor. In a second embodiment the yeast is a recombinant yeast growing in a medium comprising an ascorbic acid precursor. Preferably the recombinant yeast is transformed with a coding region encoding an enzyme selected from L-galactose dehydrogenase (LGDH), L-galactono-1,4-lactone dehydrogenase (AGD), D-arabinose dehydrogenase (ARA), D-arabinono-1,4-lactone oxidase (ALO) or L-gulono-1,4-lactone oxidase (RGLO). The ascorbic acid precursor is preferably D-glucose, L-galactose, L-galactono-1,4-lactone, or L-gulono-1,4-lactone. In another preferred embodiment the ascorbic acid is accumulated in the medium at levels greater than background. Preferably, the yield of the conversion of the precursor to ascorbic acid is preferably at least about 35%.
    Type: Grant
    Filed: August 2, 2000
    Date of Patent: October 7, 2003
    Assignee: Biopolo S.C.a.R.L.
    Inventors: Danilo Porro, Michael Sauer
  • Patent number: 6620599
    Abstract: The invention provides a process for the production of a biologically active phenolic compound (+) catechin from Taxus wallichiana tissue cultures, said process comprising the steps of (a) inoculating the of explants on a culture medium supplemented with combinations of auxins and cytokinins, (b) incubating the cultures under continuous light or dark conditions for 4-6 weeks for callus initiation followed by subculturing at 4-6 weeks intervals, (c) extracting the fresh pulverized calli with polar solvents at room temperature; (d) evaporating the solvent to obtain a residue; and (e) treating the residue with a chlorinated solvent and isolating (+) catechin compound by filtration.
    Type: Grant
    Filed: March 28, 2000
    Date of Patent: September 16, 2003
    Assignee: Council of Scientific and Industrial Research
    Inventors: Sunil Kumar Chattopadhyay, Suchitra Banerjee, Shipra Agarwal, Manish Kulshrestha, Ram Prakash Sharma, Vijay Kumar Mehta, Sushil Kumar
  • Patent number: 6610518
    Abstract: The following invention relates to a process for oxidizing alkyl groups attached directly or via a linker, to a sulfonamide moiety (II) by the use of cytochrome P450 enzymes, to give the corresponding alcohol or carboxylic acid (I). wherein R is an organic radical, X is a linker, Y is —C(CH3)2— or —CH(CH3)— and Z is —CH2OH or —COOH.
    Type: Grant
    Filed: May 29, 2001
    Date of Patent: August 26, 2003
    Assignees: Pfizer Inc., Pfizer Products Inc.
    Inventor: Michael Stephen Pacey
  • Publication number: 20030129712
    Abstract: A process for preparing enantiomer-enriched heterocyclic (R)- and (S)-cyanohydrins of the formula (I), 1
    Type: Application
    Filed: December 23, 2002
    Publication date: July 10, 2003
    Inventors: Peter Poechlauer, Wolfgang Skranc, Herbert Mayrhofer, Irma Wirth, Rudolf Neuhofer, Herfried Griengl, Martin Fechter
  • Publication number: 20030129713
    Abstract: Process for preparing enantiomer-enriched cyanohydrins in which an acetal or ketal of the formula (I) is reacted 1
    Type: Application
    Filed: December 23, 2002
    Publication date: July 10, 2003
    Inventors: Wolfgang Skranc, Peter Poechlauer, Irma Wirth, Rudolf Neuhofer, Herbert Mayrhofer
  • Publication number: 20030092140
    Abstract: Facile methods for preparing diketide and triketide thioesters are disclosed. The resulting thioesters may be used as intermediates in the synthesis of desired polyketides, and may contain functional groups which ultimately reside in side chains on the resulting polyketide and thus can be used further to manipulate the polyketide so as form derivatives. The polyketides produced may also be tailored by glycosylation, hydroxylation and the like. New polyketides and their derivatives and tailored forms are thereby produced.
    Type: Application
    Filed: August 8, 2002
    Publication date: May 15, 2003
    Inventors: Gary Ashley, Isaac C. Chan-Kai, Mark A. Burlingame
  • Publication number: 20030077767
    Abstract: Genes and proteins involved in the biosynthesis of benzodiazepines by microorganisms, including the genes and proteins forming the biosynthetic loci for the benzodiazepine anthramycin from Streptomyces refuineus subsp. thermotolerans. The genes and proteins allow direct manipulation of benzodiazepines and related chemical structures via chemical engineering of the enzymes involved in the biosynthesis of anthramycin.
    Type: Application
    Filed: June 11, 2002
    Publication date: April 24, 2003
    Inventors: Chris M. Farnet, Alfredo Staffa
  • Publication number: 20030073804
    Abstract: The invention is to provide polyhydroxyalkanoate of a novel structure enabling application to wider fields, and a producing method therefor. The invention also provides a biodegradable charge control agent having excellent charging characteristics, excellent dispersibility in the toner resin and improved spent property. The polyhydroxyalkanoate of the present invention is featured by including, in the polymer molecule, a units represented by the general formulas (1) and (2) and at least one of the units represented by the general formulas (3) to (6).
    Type: Application
    Filed: April 29, 2002
    Publication date: April 17, 2003
    Inventors: Takeshi Imamura, Etsuko Sugawa, Tetsuya Yano, Takashi Kenmoku
  • Publication number: 20030073205
    Abstract: Recombinant Myxococcus host cells can be used to produce polyketides, including epothilone and epothilone analogs that can be purified from the fermentation broth and crystallized.
    Type: Application
    Filed: September 19, 2001
    Publication date: April 17, 2003
    Inventors: Robert L. Arslanian, Gary Ashley, Scott Frykman, Bryan Julien, Leonard Katz, Chaitan Khosla, Janice Lau, Peter J. Licari, Rika Regentin, Daniel Santi, Li Tang
  • Publication number: 20030054507
    Abstract: The present invention relates to a process for the preparation of the enantiomeric forms of 2-substituted 2-(2,5-dioxoimidazolidin-1-yl)acetic acid derivatives of the formula I, 1
    Type: Application
    Filed: July 12, 2002
    Publication date: March 20, 2003
    Inventor: Wolfgang Holla
  • Patent number: 6509177
    Abstract: A procedure for the preparation of pseudomonic acid A comprising submerged cultivation of a Pseudomonas bacterium strain capable of biosynthesis of the substantially pure pseudomonic acid A in aerated conditions via fermentation; and isolation of the desired compound is disclosed. In particular, the procedure of the present invention comprises cultivation of the Pseudomonas sp. bacterium strain No. 19/26 deposited under accession No. NCAIM(P)B 001235 in the National Collection of the Agricultural and Industrial Microorganisms, Budapest, Hungary, or its pseudomonic acid A-producing mutant or variant, on a medium at a temperature of between about 20° C. and 30° C. containing organic nitrogen and carbon sources and, optionally, mineral salts.
    Type: Grant
    Filed: February 3, 2000
    Date of Patent: January 21, 2003
    Assignee: Biogal Gyogyszergyar Rt.
    Inventors: Valeria Szell, Ildiko Lang, Istvan Barta, Aniko Tedges, Karoly Albrecht, Julianna Mozes Nee Suto, Istvan M. Szabo, Magdolna Petroczki, Janos Erdei, Eva Gulyas, Gabor Balogh
  • Publication number: 20020192773
    Abstract: The preparation of macrocyclic molecules from linear, synthetic thioester precursors is disclosed. An excised thioesterase domain isolated from either a PKS or NRPS multidomain system catalyzes the cyclization reaction. Thioester substrates also are described that are efficiently cyclized by the method of the present invention. Additionally, macrocyclic molecules, including macrolactones and macrolactams, that are prepared by the macrocyclization methods of the invention are described.
    Type: Application
    Filed: December 15, 2001
    Publication date: December 19, 2002
    Applicant: The President and Fellows of Harvard College
    Inventors: Christopher Thomas Walsh, John W. Trauger, Rahul Manu Kohli, Michael D. Burkart, Mohammed A. Maraheil, Henning Dieter Mootz, Dirk Schwarzer
  • Publication number: 20020187529
    Abstract: A method for the production of clavulanic acid by the fermentation of a clavulanic acid producing microorganism at a controlled level of at least 50 mg/l ammonia has been provided for.
    Type: Application
    Filed: July 9, 2002
    Publication date: December 12, 2002
    Inventors: Gesina Visser-Luirink, Wilhelmus Theodorus Antonius Maria De Laat, Jeroen Martijn Klop
  • Patent number: 6479621
    Abstract: Microorganisms capable of synthesizing novel polyhydroxyalkanoate having 3-hydroxythienylalkanoic acid as monomer unit, using thienylalkanoic acid as a stock are cultured on a culture medium containing thienylalkanoic acid, and the polyhydroxyalkanoate produced in the cultured cell is extracted and
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: November 12, 2002
    Assignee: Canon Kabushiki Kaisha
    Inventors: Tsutomu Honma, Tetsuya Yano, Shin Kobayashi, Takeshi Imamura, Takashi Kenmoku, Shinya Kozaki
  • Patent number: 6458568
    Abstract: A method for the continuous synthesis of baccatin-III is performed by means of the enzymatic acetylations of 10-deacetyl baccatin-III (10-DAB) in an enzyme reactor. This objective is accomplished by a method, for which an aqueous reaction batch is used, which contains a partially purified or a very pure acetyl transferase from a Taxus species and synthesis components, especially 10-DAB, acetyl compounds or optionally an acetyl coenzyme A, which can be regenerated, a protective colloid and optionally a buffer substance in solution. The solution is separated by a semipermeable membrane from an organic solvent, which serves as extraction agent for baccatin-III, the reaction batch being regenerated at regular intervals in an aqueous buffer system and the solvent continuously being exchanged. By conducting the reaction, the product can be removed continuously from the reaction batch for the partial synthesis of taxol and taxoter. By the above method, achievable yields are increased significantly.
    Type: Grant
    Filed: May 13, 1999
    Date of Patent: October 1, 2002
    Assignee: Institut fuer Bioanalytik, Umwelt-Toxikologie und Biotechnologie Halle GmbH
    Inventors: Konrad Glund, Matthias Hoffmann, Wolfram Weckwerth, Rainer Zocher
  • Patent number: 6451587
    Abstract: The present invention relates to microbial processes for carrying out the asymmetric reduction of a ketone to an alcohol, which comprises: contacting the ketone with a microorganism, or an enzyme reduction system capable of accomplishing the subject reduction comprising an enzyme derived from said microorganism and a co-factor for said enzyme, and incubating the resulting mixture under conditions sufficient to yield more of the desired (R)-enantiomer of the corresponding alcohol than the undesired (S)-enantiomer. The chiral (R)-enantiomer can be used in the synthesis of certain &bgr;-adrenergic receptor agonists.
    Type: Grant
    Filed: June 2, 2000
    Date of Patent: September 17, 2002
    Assignee: Pfizer Inc.
    Inventors: Michael P. Burns, John W. Wong
  • Patent number: 6440708
    Abstract: A method for the production of clavulanic acid by the fermentation of a clavulanic acid producing microorganism at a controlled level of at least 50 mg/l ammonia has been provided for. Under the application of these reaction conditions surprisingly high production levels of clavulanic acid have been obtained.
    Type: Grant
    Filed: September 27, 1999
    Date of Patent: August 27, 2002
    Assignee: DSM N.V.
    Inventors: Gesina Visser-Luirink, Wilhelmus Theodorus Antonius De Laat, Jeroen Martijn Klop
  • Patent number: 6436395
    Abstract: Disclosed is a method for controlling phytopathogenic fungi using pure strains of Rosellinia subiculata ATCC 74386 and fungus ATCC 74387. Further, methods of producing a sordarin compound are disclosed. The method includes cultivating each strain separately in a nutrient medium containing assimilable sources of carbon and nitrogen and recovering the compound. A sordarin compound of formula I is also disclosed. Also an antifungal composition containing a sordarin compound is also disclosed.
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: August 20, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Gerald F. Bills, Anne W. Dombrowski, Wendy S. Horn, Richard K. Jansson, Mark Rattray, Dennis Schmatz, Robert E. Schwartz
  • Patent number: 6416762
    Abstract: The present invention provides structure-based combinatorial libraries of compounds containing the functional group minima of picornaviruses including poliovirus and rhinovirus. The libraries can be used to screen for therapeutical antiviral compounds, e.g., anti-picornaviral capsid-binding compounds.
    Type: Grant
    Filed: December 11, 1998
    Date of Patent: July 9, 2002
    Assignee: President and Fellows of Harvard College
    Inventors: Diane M. Joseph-McCarthy, Lyle D. Isaacs, George M. Whitesides, Martin Karplus, James M. Hogle, James Li-wen Cheh
  • Publication number: 20020048796
    Abstract: The present invention relates to a process for preparing optically pure (S)-3-hydroxy-&ggr;-butyrolactone expressed by the following Formula 1 and more particularly, to a process that enables preparing optically pure (S)-3-hydroxy-&ggr;-butyrolactone economically in large quantities, by:
    Type: Application
    Filed: September 6, 2001
    Publication date: April 25, 2002
    Applicant: Samsung Fine Chemicals Co., Ltd.
    Inventors: Young Mi Park, Jongpil Chun, Yik-Haeng Cho, Kyoung Rok Roh, Hosung Yu, Dae II Hwang
  • Patent number: 6376221
    Abstract: There is disclosed an improved poppy straw of a stably reproducing Papaver somniferum for the extraction of thebaine and/or oripavine, the threshed straw having thebaine and oripavine constituting about 50% by weight or greater of the alkaloid combination consisting of morphine, codeine, thebaine and oripavine.
    Type: Grant
    Filed: August 31, 1999
    Date of Patent: April 23, 2002
    Assignee: Tasmanian Alkaloids Pty. Ltd.
    Inventors: Anthony John Fist, Christopher James Byrne, Wayne Lyle Gerlach
  • Patent number: 6361978
    Abstract: The present invention provides processes for making biotin from desthiobiotin by either contacting desthiobiotin with an enzyme reaction mixture containing bioB gene product and nifU gene product and/or nifS gene product and isolating the biotin or cultivating a microorganism transformed with DNA encoding the bioB gene product, nifU gene product and nifS gene product and isolating the biotin.
    Type: Grant
    Filed: April 24, 1997
    Date of Patent: March 26, 2002
    Assignee: Roche Vitamins, Inc.
    Inventors: Tatsuo Hoshino, Akira Asakura, Tatsuya Kiyasu, Yoshie Nagahashi
  • Publication number: 20020031810
    Abstract: Nucleotide sequences from coryneform bacteria coding for the lipA gene and a process for fermentative preparation of amino acids by attenuation of the lipA gene.
    Type: Application
    Filed: August 29, 2001
    Publication date: March 14, 2002
    Applicant: DEGUSSA AG
    Inventors: Bettina Moeckel, Walter Pfefferle, Michael Buchholz
  • Patent number: 6352839
    Abstract: The invention provides a method for preparing streptogramins using genetically-modified microorganisms to influence the biosynthesis of at least one of the precursors of the group B streptogramins. Cultures of the genetically-modified microorganisms are supplemented with a least one precursor that is different from the streptogramin precursor whose biosynthesis is altered and the streptogramins produced are recovered.
    Type: Grant
    Filed: March 20, 1997
    Date of Patent: March 5, 2002
    Assignee: Aventis Pharma S.A.
    Inventors: Véronique Blanc, Denis Thibaut, Nathalie Bamas-Jacques, Francis Blanche, Joël Crouzet, Jean-Claude Barriere, Laurent Debussche, Alain Famechon, Jean-Marc Paris, Gilles Dutruc-Rosset
  • Publication number: 20020025565
    Abstract: Disclosed is a method for optically resolving a racemic &agr;-substituted heterocyclic carboxylic acid (&agr;-HCCA) by taking advantage of enantioselectivity of enzymes. &agr;-HCCA is reacted with alcohol to give a racemic &agr;-HCCA ester, which is then reacted with an enzyme with enantioselectivity, whereby either R-form or S-form of the racemate is hydrolyzed. Extraction with an organic solvent can obtain enantiomers of the &agr;-HCCA ester. The extracted enantiomeric &agr;-HCCA ester is converted to enantiomeric &agr;-HCCA by catalytic hydrogenation in an organic solution or by enzymatic hydrolysis in an aqueous solution. Thus, a racemic mixture of &agr;-HCCA can be optically resolved with high optical purity at high yields as well as at low cost.
    Type: Application
    Filed: May 31, 2001
    Publication date: February 28, 2002
    Inventors: Ki-Nam Uhm, Sang-Chul Lim, Jong-Ho Lim
  • Patent number: 6348337
    Abstract: A process useful for the preparation of intermediates in synthesis or semi-synthesis of paclitaxel analogs wherein a starting taxane such as 10-deacetylbaccatin III is deacetylated at the C-4 position using a microorganism or an enzyme derived therefrom to provide 4-deacetyltaxanes, such as 4,10-dideacetylbaccatin III.
    Type: Grant
    Filed: August 17, 2000
    Date of Patent: February 19, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ronald L. Hanson, Ramesh N. Patel
  • Publication number: 20020012977
    Abstract: The following invention relates to a process for oxidizing alkyl groups attached directly or via a linker, to a sulfonamide moiety (II) by the use of cytochrome P450 enzymes, to give the corresponding alcohol or carboxylic acid (I).
    Type: Application
    Filed: May 29, 2001
    Publication date: January 31, 2002
    Inventor: Michael Stephen Pacey
  • Publication number: 20020006644
    Abstract: Disclosed is a method for preparing an R- or S-forms of &agr;-substituted heterocyclic carboxylic acid (&agr;-HCCA) and a counter enantiomeric form of &agr;-substituted heterocyclic carboxylic acid ester thereto by use of an enzyme. A racemic &agr;-HCCA is reacted with alcohol to give a racemic &agr;-HCCA ester, which is then brought into contact with an enzyme with enantioselectivity, whereby either R-form or S-form of the racemate is hydrolyzed. Extraction with an organic solvent can obtain enantiomers of the &agr;-HCCA ester. Thus, a certain enantiomeric form of &agr;-HCCA and a counter enantiomeric form of &agr;-HCCA ester thereto, respectively can be prepared with high optical purity at high yields as well as at low cost.
    Type: Application
    Filed: May 30, 2001
    Publication date: January 17, 2002
    Inventors: Ki-Nam Uhm, Sang-Chul Lim, Jong-Ho Lim
  • Publication number: 20010039041
    Abstract: The active component of the pharmaceutical composition of the present invention is a compound which has been isolated from the controlled aerobic fermentation of a marine microorganism, Agrobacterium sp. PH-103.
    Type: Application
    Filed: January 8, 2001
    Publication date: November 8, 2001
    Applicant: Pharma Mar, S.a.
    Inventors: Glynn T. Faircloth, Francisco Romero Millan, Librada Maria Canedo Fernandez, Cristina Accbal Sarabia
  • Patent number: 6297403
    Abstract: A process for the preparation of vinyl, alkynyl, aryl or heteroaryl aldehydes or vinyl, alkynyl, aryl or heteraoryl ketones includes reacting vinyl-, alkynyl-, aryl- and heteroarylmethyl and -methylene compounds with the aid of a mediator and an oxidant, wherein the mediator is selected from the group of the aliphatic, heterocyclic or aromatic NO, or NOH containing compounds.
    Type: Grant
    Filed: January 5, 2000
    Date of Patent: October 2, 2001
    Assignee: Consortium für elektrochemische Industrie GmbH
    Inventors: Elke Fritz-Langhals, Johannes Freudenreich
  • Patent number: 6287827
    Abstract: Fermentation of Nocardia sp. ATCC-202099 in the presence of a halogen- or hydroxy-substituted tryptophan precursor yields a novel corresponding halogen- or hydroxy-substituted nocathiacin compound which has broad spectrum antibiotic activity against Gram-positive bacteria and has in vivo efficacy in animals.
    Type: Grant
    Filed: May 1, 2000
    Date of Patent: September 11, 2001
    Assignee: Bristol-Myers Squibb Company
    Inventors: Wenying Li, John E. Leet, Kin S. Lam
  • Patent number: 6277626
    Abstract: 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: Grant
    Filed: February 16, 1999
    Date of Patent: August 21, 2001
    Assignee: G.D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Mahima Trivedi, Rolando E. Gapud, John S. Ng, Alok K. Awasthi, Ping T. Wang
  • Patent number: 6261813
    Abstract: A method for derivatizing a compound having a hydroxyl group by back to back acylation is provided. The compound is acylated with a bifunctional acyl donor in the presence of a hydrolase to form an activated acyl ester or carbonate. Preferably the bifunctional acylating donor is a di(vinyl) ester or carbonate. The activated acyl ester or carbonate is then used to acylate a nucleophile in the presence of a lipase. The method of the invention provides regioselective enzymatic acylation of the base compound.
    Type: Grant
    Filed: November 23, 1998
    Date of Patent: July 17, 2001
    Assignee: Albany Molecular Research, Inc.
    Inventors: Yuri L. Khmelnitsky, Cheryl L. Budde, John M. Arnold, Joseph O. Rich, Sharon S. Chen, Alexander Ya. Usyatinsky, Douglas S. Clark, Jonathan S. Dordick
  • Patent number: 6239111
    Abstract: The present invention discloses the use, in the manufacture of a preventive and therapeutic drug of a brain disease, of a compound represented by formula (1): CH2═CH—CH2—S(O)n—R  (1) [wherein R represents a hydrogen atom, an alkyl group, an alkenyl group, a substituted alkyl group, a substituted alkenyl group, an alkylthio group, an alkenylthio group, a phenyl group, a substituted phenyl group, a heterocyclic group, or a group derived from an amino acid or an oligopeptide by deletion of one hydrogen atom, and which group may have a protective group; and n is 0, 1, or 2], a glycoside thereof, or a salt of the compound or the glycoside. The drug of the present invention for ameliorating brain diseases, inhibiting reduction of brain neurons and promoting branching of neurites, is useful for the prevention and treatment of brain diseases such as dementia in association with degeneration and sloughing of brain neurons.
    Type: Grant
    Filed: January 26, 1998
    Date of Patent: May 29, 2001
    Assignee: Wakunaga Pharmaceutical Co., Ltd.
    Inventors: Toru Moriguchi, Hiromichi Matsuura, Hiroshi Saito
  • Patent number: 6207444
    Abstract: This invention relates to crystalline pharmaceutically acceptable salts of an alpha 1a adrenergic receptor antagonist, Compound A, which are useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts and pharmaceutical compositions of Compound A are also disclosed. This invention further relates to a process for obtaining enantiomerically pure intermediate useful for the synthesis of end product alpha 1a adrenergic receptor antagonists. The end product compounds are useful for the treatment of benign prostatic hyperplasia and for relaxing lower urinary tract tissue. The invention also relates to a process for preparing a class of dihydropyrimidinone compounds of which Compound A is a member, wherein the process involves deprotonating a dihydropyrimidinone compound and then coupling the deprotonated derivative with a primary amine.
    Type: Grant
    Filed: July 24, 1998
    Date of Patent: March 27, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Daniel R. Sidler, Michel Chartrain, Norihiro Ikemoto, Gerald F. Bills, Christopher Roberge, Colleen S. Taylor
  • Patent number: 6162622
    Abstract: An enzymatic hydroxylation method for the preparation of compounds useful as intermediates in the preparation of taxanes such as 6-.alpha.-hydroxy-7-deoxypaclitaxel, wherein one or more C-6 hydrogen-bearing taxanes are contacted with an enzyme or microorganism capable of hydroxylating said C-6 carbon to give C-6 hydroxyl-bearing taxane.
    Type: Grant
    Filed: January 14, 1999
    Date of Patent: December 19, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ronald L. Hanson, Ramesh N. Patel
  • Patent number: 6136572
    Abstract: Disclosed are isolated DNAs encoding a kynurenine aminotransferase selected from the group consisting of:(a) isolated DNA sequences which encode rat KAT;(b) an isolated DNA sequence which hybridizes to isolated DNA sequences of (a) above and which encodes a mammalian KAT enzyme; and(c) an isolated DNA sequence differing from the isolated DNA sequences of (a) and (b) above in codon sequence due to the degeneracy of the genetic code, and which encodes a KAT enzyme.Vectors and host cells containing the same, oligonucleotide probes for identifying kynurenine aminotransferase, and isolated and purified kynurenine aminotransferase are also disclosed.
    Type: Grant
    Filed: April 1, 1997
    Date of Patent: October 24, 2000
    Assignees: University of Maryland at Baltimore, Pharmacia & Upjohn S.P.A.
    Inventors: Luca Benatti, Jerome Breton, Carmela Speciale, Etsuo Okuno, Robert Schwarcz, Monica Mosca
  • Patent number: 6087137
    Abstract: A process for preparing a compound of Formula (3) in which R.sup.2 is --H; ##STR1## which comprises the steps: i) conversion of a compound of Formula (1) into a compound of Formula (2) using a dioxygenase enzyme; ##STR2## ii) conversion of the compound of Formula (2) into a compound of Formula (3) wherein is --COR; andiii) conversion of the compound of Formula (3) in which R.sup.2 is --COR into a compound of Formula (3) in which R.sup.2 is --H;wherein R.sup.2, a, b, c, d, Z, m and X are as defined in claim 1.Also claimed are individual steps of the process and new compounds of Formula (2).
    Type: Grant
    Filed: November 21, 1997
    Date of Patent: July 11, 2000
    Assignee: Zeneca Limited
    Inventors: Andrew John Blacker, Derek Raymond Boyd, Howard Dalton, Nigel Bowers
  • Patent number: 6071712
    Abstract: An enzymatic process for hydrolyzing the 7-position acyl ester of certain cephalosporin compounds to the corresponding alcohol is disclosed.
    Type: Grant
    Filed: September 18, 1997
    Date of Patent: June 6, 2000
    Assignee: SmithKline Beecham Corporation
    Inventors: Vedanthadesikan Renganathan, Martin Brenner
  • Patent number: 6043058
    Abstract: 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: Grant
    Filed: February 5, 1999
    Date of Patent: March 28, 2000
    Assignee: Maiji Seika Kaisha Ltd.
    Inventors: Makoto Ohyama, Masaaki Takahashi, Yoshiya Shigematsu, Osamu Sakanaka, Yashushi Murai, Katsuharau Iinuma
  • Patent number: 6015808
    Abstract: Pharmaceutical compositions with heretofore unknown and enhanced physical, chemical, and biological properties are prepared by combining known biologically active parent compounds with oxo thia azabicyclo compounds, such as lactam and .beta.-lactam compounds, capable of rapidly transporting the parent compounds in undegraded form to their target sites of action. A process for combining the parent compound with .beta.-lactam compounds consists of dissolving the parent compound in a polar solvent, adding a .beta.-lactam compound, incubating the resulting mixture, followed by drying, and subjecting the remaining solid material to solvent washing or extraction to further purify the new pharmaceutical composition. The new pharmaceutical composition possesses the biological and therapeutic activity of the parent compound and the barrier penetrating characteristics of the .beta.
    Type: Grant
    Filed: August 22, 1995
    Date of Patent: January 18, 2000
    Inventors: Mandayam Jeersannidhi Thirumalachar, Mandayam Jeersannidhi Narasimhan, Jr.
  • Patent number: 6013493
    Abstract: Taxol is produced from taxol-producing micro-organisms. Methods of obtain the taxol-producing microorganisms are described. Radioactive labelled taxol products and methods for use of the radioactive labelled taxol and for the treatment of leukemia and cancer cells are described.
    Type: Grant
    Filed: November 26, 1997
    Date of Patent: January 11, 2000
    Assignee: The Research and Development Institute at Montana State University
    Inventors: Andrea Stierle, Donald Stierle, Gary Strobel
  • Patent number: 6007812
    Abstract: An imperfect fungus such as a microorganism belonging to the genus Curvularia in a culture medium containing nutrients utilizable for normal microorganisms and isolating MK7634 substance of a molecular formula: C.sub.8 H.sub.15 N.sub.3 O.sub.4 from the culture by, for example, solvent extraction, ion exchange resin technique or gel filtration chromatography. The MK7634 substance can be used as an active ingredient of drugs. In particular, the MK7634 substance is a novel anthelmintic substance and expected to be used as an active ingredient of anthelmintics.
    Type: Grant
    Filed: May 12, 1997
    Date of Patent: December 28, 1999
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Mina Kanda, Noriko Chiba, Shigenori Kumazawa, Masayuki Takagi, Kenzo Harimaya, Tadaaki Okada
  • Patent number: 5989876
    Abstract: Colorant precursors, which are present in the cells of plants belonging to the genus Medicago, such as alfalfa, can react with quinones so as to yield colorants which can be used in dyeing compositions for textiles or hair.
    Type: Grant
    Filed: December 10, 1997
    Date of Patent: November 23, 1999
    Assignee: L'Oreal
    Inventors: Beatrice Belcour-Castro, Georges Hussler, Anne Bonnet
  • Patent number: 5968788
    Abstract: 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: Grant
    Filed: August 26, 1996
    Date of Patent: October 19, 1999
    Assignee: Toray Industries, Inc.
    Inventors: Reiko Miyata, Tetsu Yonehara