Containing Six-membered Hetero Ring Patents (Class 435/122)
  • Publication number: 20080248537
    Abstract: The present invention relates to biocatalytic asymmetric reduction for the preparation of 2-amino-[5-(1-hydroxy-2-hydroxy or halogen-ethyl)]-pyrazine derivatives of the formula wherein R is lower alkylcarbonyl or an amino protecting group and R1 is hydroxy or halogen. The compounds are key intermediates in the manufacture of a glucokinase activator.
    Type: Application
    Filed: April 3, 2008
    Publication date: October 9, 2008
    Inventors: Steven Paul Hanlon, Hans Iding, Ernst Kupfer, Roumen Nikolaev Radinov, Lianhe Shu, Ping Wang
  • Patent number: 7432089
    Abstract: The present invention relates to a DNA encoding a novel flavin adenine dinucleotide (FAD)-dependent D-erythronate 4-phosphate (EN4P) dehydrogenase originated from Sinorhizobium meliloti, which is involved in vitamin B6 biosynthesis, and a recombinant microorganism transformed with a vector having the DNA. It also relates to a process for production of vitamin B6 by using the recombinant microorganism. “Vitamin B6” as used in this invention includes pyridoxol (PN), pyridoxal and pyridoxamine. Vitamin B6 is a vitamin indispensable to human beings or other animals, and is used as a raw material of medicines or as feed additives.
    Type: Grant
    Filed: September 25, 2003
    Date of Patent: October 7, 2008
    Assignee: DSM IP Assets B.V.
    Inventors: Tatsuo Hoshino, Keiko Ichikawa, Masaaki Tazoe
  • Publication number: 20080193975
    Abstract: A D-aminotransferase can be modified so as to efficiently produce (2R,4R)-monatin having high sweetness intensity from 4-(indol-3-ylmethyl)-4-hydroxy-2-oxoglutaric acid by mutating the amino acid sequence of a wild-type D-aminotransferase represented in SEQ ID NO:4.
    Type: Application
    Filed: March 26, 2008
    Publication date: August 14, 2008
    Applicant: AJINOMOTO CO., INC.
    Inventors: Masakazu SUGIYAMA, Kunihiko WATANABE, Tasuki KASHIWAGI, Ei-ichiro SUZUKI
  • Patent number: 7371547
    Abstract: Disclosed is a mutant of a recombinant microorganism of the genus Sinorhizobium capable of producing vitamin B6 having a recombinant plasmid with pdxJ gene that acquired histidine requirement of glycine resistance, or its combination thereof.
    Type: Grant
    Filed: September 16, 2003
    Date of Patent: May 13, 2008
    Assignee: DSM IP Assets B.V.
    Inventors: Tatsuo Hoshino, Yoichiro Nagatani, Keiko Ichikawa, Masaaki Tazoe
  • Patent number: 7297800
    Abstract: The present invention relates to a process for producing efficiently glutamic acid derivatives (including salts thereof) such as monatin by converting a substituted ?-keto acid of formula (1) into a glutamic acid derivative of formula (2) in the presence of an enzyme catalyzing conversion of the same
    Type: Grant
    Filed: June 28, 2004
    Date of Patent: November 20, 2007
    Assignee: Ajinomoto Co., Inc.
    Inventors: Masakazu Sugiyama, Kunihiko Watanabe, Nao Funakoshi, Yusuke Amino, Shigeru Kawahara, Tadashi Takemoto
  • Patent number: 7241601
    Abstract: A process for the preparation of a compound of the formula by means of bioconversion with a microorganism culture of a compound of the formula
    Type: Grant
    Filed: March 20, 2003
    Date of Patent: July 10, 2007
    Assignee: Aventis Pharma SA
    Inventors: Robert Azerad, Jacques Biton, Isabelle Lacroix
  • Patent number: 7232908
    Abstract: The present invention relates to a process for the production of piperidine derivatives with microorganisms. This is carried out by incubating starting compounds in the presence of a microorganism under conditions effective to produce piperidine derivative products. Suitable microorganisms can be from any one of the genus of Stemphylium, Gliocladium, Bacillus, Botrytis, Cyathus, Rhizopus, Pycniodosphora, Pseudomonas, Helicostylum, Mucor, Gelasinospora, Rhodotorula, Candida, Mycobacterium, and Penicillium. In another aspect of the invention, starting compounds are incubated in the presence of Cunninghamella bainieria under conditions effective to produce piperidine derivative products.
    Type: Grant
    Filed: August 11, 2003
    Date of Patent: June 19, 2007
    Assignee: AMR Technology, Inc.
    Inventors: Peter C. Michels, Eric L. Zirbes
  • Patent number: 7052885
    Abstract: A process for preparing enantiomer-enriched heterocyclic (R)- and (S)-cyanohydrins of the formula (I), where R1, R2, R3, R4 independently of one another are H, an unsubstituted or substituted C1–C24-alkyl, alkenyl or alkynyl radical, where one or more carbon atoms in the chain can be replaced by an oxygen atom, a nitrogen atom, a sulfur atom, an SO or an SO2 group, an unsubstituted or substituted aryl or heteroaryl radical or heterocyclic radical or halogen, hydroxyl, NR5R6, acetyl, oxo, C1–C6-carbalkoxy, C1–C6-carbalkoxyamino, COOR7, cyano, amide, benzoylamino or NO2, R5 and R6 are H, C1–C6-alkyl radical, phenyl radical, benzyl radical or COOR7, or together form a C2–C8-alkylene or heteroalkylene radical, R7 is H or C1–C6-alkyl, n is 0, 1, 2 or 3, X, Y and Z can be an unsubstituted or substituted carbon atom or a radical selected from the group consisting of N, O, S or NR5R6, where R5 and R6 are as defined above, SO or SO2, and at least one of the radicals X, Y and Z is not a carbon atom, where the compo
    Type: Grant
    Filed: December 23, 2002
    Date of Patent: May 30, 2006
    Assignee: DSM Fine Chemicals Austria NFG GmbH & Co KG
    Inventors: Peter Poechlauer, Wolfgang Skranc, Herbert Mayrhofer, Irma Wirth, Rudolf Neuhofer, Herfried Griengl, Martin Fechter
  • Patent number: 6946269
    Abstract: The invention relates to lower-alkyl esters of 3-(3,4-dihalophenyl)-2,6-dioxopiperidine-3-propionic acid derivatives, and to processes for preparing the same.
    Type: Grant
    Filed: December 4, 2003
    Date of Patent: September 20, 2005
    Assignee: Sanofi-Aventis
    Inventors: Bertrand Castro, Jean-Robert Dormoy, Alain Rabion
  • Patent number: 6919199
    Abstract: The present invention provides methods of using a microbe containing a polypeptide that degrades, preferably detoxifies, a compound that is present in the environment. Preferably, the polypeptide is a hydrolase and the compound is at least one s-triazine. The present invention also provides a microbe containing a polypeptide that degrades, preferably detoxifies, a compound that is present in the environment.
    Type: Grant
    Filed: December 10, 2002
    Date of Patent: July 19, 2005
    Assignee: Regents of the University of Minnesota
    Inventor: Hugh McTavish
  • Patent number: 6780635
    Abstract: The present invention provides a process for preparation of optically active azabicyclo heptanone derivates using lactamases that will react with racemic lactam of formula (I) to give a single enanotiomer of lactam (III) and the corresponding ring opened compound of formula (IV) in an enantiomerically pure form.
    Type: Grant
    Filed: December 27, 2001
    Date of Patent: August 24, 2004
    Assignee: Council of Scientific and Industrial Research
    Inventors: Rohini Ramesh Joshi, Asmita Ashutosh Prabhune, Ramesh Anna Joshi, Mukund Keshav Gurjar
  • Patent number: 6780634
    Abstract: A biotechnological method is described for preparing compounds of the general formulas wherein R1 is acyl or acyloxy and R2 is a hydrogen atom or C1-10 alkyl, comprising the conversion of a lactam of the general formula by means of a hydrolase in the presence of a nucleophile and in the presence of a base in a constant pH range.
    Type: Grant
    Filed: April 17, 2001
    Date of Patent: August 24, 2004
    Assignee: Lonza AG
    Inventors: Christine Bernegger-Egli, Frank Brux, Jean Paul Roduit, Oleg Werbitzky, Yves Guggisberg
  • Patent number: 6770463
    Abstract: There is provided a process for the preparation of a chiral insecticidal and acaricidal compound of formula I. Also provided are intermediate compounds useful in the process of the present invention.
    Type: Grant
    Filed: August 2, 2001
    Date of Patent: August 3, 2004
    Assignee: BASF Aktiengesellschaft
    Inventors: John Francis Chiarello, Brian Lee Buckwalter, Timothy Claude Barden
  • Publication number: 20040086983
    Abstract: An objective of the present invention is to provide a method of producing hydroxylated heterocyclic compounds and hydroxylated aromatic carboxylic acids by bioengineering technique, and modified enzymes which can be used for this method. A method of producing hydroxylated heterocyclic compounds or hydroxylated aromatic carboxylic acids comprises reacting an aromatic ring dioxygenase with heterocyclic compounds or aromatic carboxylic acids to hydroxylate these compounds. An enzyme according to the present invention is an aromatic ring dioxygenase comprising an &agr;-subunit consisting of the amino acid sequence of SEQ ID NO: 2, which is modified according to the &agr;-subunit of the biphenyl dioxygenase derived from the strain Burkholderia cepacia LB400, a &bgr;-subunit consisting of the amino acid sequence of SEQ ID NO: 4, and a ferredoxin consisting of the amino acid sequence of SEQ ID NO: 6, and a ferredoxin reductase consisting of the amino acid sequence of SEQ ID NO: 8.
    Type: Application
    Filed: September 13, 2001
    Publication date: May 6, 2004
    Inventors: Norihiko Misawa, Kazutoshi Shindo, Hiroshi Okazaki, Kensuke Furukawa, Sueharu Horinouchi
  • Publication number: 20040029237
    Abstract: A process for the preparation of N-substituted 4-hydroxypiperidine, wherein an oxygen atom is inserted regioselectively into the corresponding N-substituted piperidine, by using as a biocatalyst a bacterium degrading alkanes or alicyclic hydrocarbons, or a prokaryotic host-organism having the gene(s) necessary for the hydroxylation derived from the said bacterium, or an enzyme having hydroxylation activity derived therefrom. The bacterium may be selected from species from, for example, the genera Sphingomonas and Pseudomonas, that are capable of degrading n-alkanes having 4 to 20 carbon atoms.
    Type: Application
    Filed: August 21, 2003
    Publication date: February 12, 2004
    Inventors: Zhi Li, Dongliang Chang, Bernard Witholt
  • Patent number: 6689587
    Abstract: The present invention relates to polynucleotides corresponding to the nadC gene and which encode the nicotinate nucleotide pyrophosphorylase protein, methods of producing nicotinic acid or nicotinic acid derivatives, and methods of screening for polynucleotides which encode proteins having nicotinate nucleotide pyrophosphorylase activity.
    Type: Grant
    Filed: February 22, 2001
    Date of Patent: February 10, 2004
    Assignee: Degussa AG
    Inventors: Christine Bastuck, Brigitte Bathe, Nicole Dusch, Bettina Moeckel, Georg Thierbach
  • Patent number: 6686182
    Abstract: The invention relates to lower-alkyl esters of 3-(3,4-dihalophenyl)-2,6-dioxopiperidine-3-propionic acid derivatives, and to processes for preparing the same.
    Type: Grant
    Filed: June 19, 2002
    Date of Patent: February 3, 2004
    Assignee: Sanofi-Synthelabo
    Inventors: Bertrand Castro, Jean-Robert Dormoy, Alain Rabion
  • Patent number: 6673582
    Abstract: The present invention provides methods of using a microbe containing a polypeptide that degrades, preferably detoxifies, a compound that is present in the environment. Preferably, the polypeptide is a hydrolase and the compound is at least one s-triazine. The present invention also provides a microbe containing a polypeptide that degrades, preferably detoxifies, a compound that is present in the environment.
    Type: Grant
    Filed: January 25, 2001
    Date of Patent: January 6, 2004
    Assignee: Regents of the University of Minnesota
    Inventor: Hugh McTavish
  • Publication number: 20030232405
    Abstract: Methods of producing fluorescence from fluorogenic substrates reactive with a peroxidase enzyme are disclosed. Use of the methods in assays for peroxidase enzymes, peroxidase-labeled analytes are provided. Fluorogenic compounds, compositions and kits for reaction with peroxidase enzymes are described. Two modes of producing fluorescent compounds are described.
    Type: Application
    Filed: June 6, 2002
    Publication date: December 18, 2003
    Inventors: Hashem Akhavan-Tafti, Renuka de Silva, Mark Sandison, Richard Handley
  • Publication number: 20030186395
    Abstract: The present invention relates to a process for the systhesis of optically enriched dextro- and laevo-rotatory isomers of rose oxide from racemic citronellol. The invention particularly relates to the preparation of optically enriched (−)-(2 S, 4 R)-rose oxide and its isomer (+)-(2 R, 4 S)-rose oxide torn racemic citronellol.
    Type: Application
    Filed: March 29, 2002
    Publication date: October 2, 2003
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Shubhash Chandra Taneja, Vijay Kumar Sethi, Surrinder Koul, Samar Singh Andotra, Ghulam Nabi Qazi
  • Publication number: 20030165968
    Abstract: Recombinant microbial strains are provided that express nitrilase enzyme and are useful as biocatalysts for the hydrolysis of nitrile-containing substrates. The recombinant cells are transformed with a foreign gene isolated from Acidovorax facilis 72W encoding a thermostable nitrilase enzyme that catalyzes the hydrolysis of nitrile-containing substrates to carboxylic acids under mild reaction conditions. The nucleotide sequence of the nitrilase gene and the deduced amino acid sequence encoded by the nitrilase gene are provided.
    Type: Application
    Filed: February 27, 2003
    Publication date: September 4, 2003
    Inventors: Sarita Chauhan, Robert Dicosimo, Robert D. Fallon, John E. Gavagan, Mark S. Payne
  • Patent number: 6613907
    Abstract: The present invention relates to the production of a product compound having a structure according to Formulae IA and/or IB: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, and alkoxy. This process involves incubating a starting compound having a structure according to Formulae IIA and/or IIB: wherein R3 is —CH3 and R1, R2, A, B, and D are defined above In the presence of a microorganism under conditions effective to produce the product compound.
    Type: Grant
    Filed: January 4, 2001
    Date of Patent: September 2, 2003
    Assignee: AMR Technology, Inc.
    Inventors: Peter C. Michels, Eric L. Zirbes
  • Publication number: 20030130521
    Abstract: It is an objective to produce intermediates of optically active beta-3 adrenaline receptor agonists from readily available raw materials in a safe, efficient and industrially advantageous manner. A substituted acetylpyridine derivative represented by the general formula (9) is reduced by enantioselective reduction to produce an optically active hydroxyethylpyridine derivative represented by the general formula (10) (wherein * represents an asymmetric carbon atom), and it is further derivatized to an intermediate of an optically active beta-3 adrenaline receptor agonist, such as an optically active dihydroxyethylpyridine derivative represented by the general formula (14) or an optically active oxirane derivative represented by the general formula (16).
    Type: Application
    Filed: November 27, 2002
    Publication date: July 10, 2003
    Applicant: KANEKA CORPORATION
    Inventors: Susumu Amano, Naoaki Taoka, Masaru Mitsuda, Kenji Inoue
  • Publication number: 20030096335
    Abstract: The invention relates to a process halogenation, which comprises halogenating a chemical compound in the presence of a halogenase, where the halogenase is
    Type: Application
    Filed: April 5, 2002
    Publication date: May 22, 2003
    Inventors: Stefan Pelzer, Petra Huber, Roderich Suessmuth, Juergen Recktenwald, Dorothee Heckmann, Wolfgang Wohlleben
  • Patent number: 6558931
    Abstract: The invention concerns a method for preparing Fexofenadine from Terfenadine by a bioconversion process using Absidia corymbifera LCP 63-1800 or Stepromyces platensis NRRL 2364 strain.
    Type: Grant
    Filed: October 31, 2000
    Date of Patent: May 6, 2003
    Assignee: Aventis Pharma S.A.
    Inventors: Robert Azerad, Jacques Biton, Isabelle Lacroix
  • Patent number: 6489147
    Abstract: A gene which contains the nucleotide sequence shown in SEQ ID NO:1 from nucleotide 671 to nucleotide 6295 or a nucleotide sequence which can be obtained therefrom by substitution, insertion or deletion of up to 30%, preferably up to 10%, particularly preferably up to 20%, especially preferably up to 5%, of the nucleotides, and whose gene product has the enzymatic activity of an adenylate cyclase, and its use.
    Type: Grant
    Filed: June 21, 1999
    Date of Patent: December 3, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Regula Altmann-Jöhl, Peter Philippsen, Henning Althöfer, Harald Seulberger
  • Publication number: 20020161027
    Abstract: The present invention relates to a novel antifungal antibacterial compound 2-methylheptylisonicotinate of formula 1 below obtained from natural sources and to a process for the isolation thereof.
    Type: Application
    Filed: December 20, 2001
    Publication date: October 31, 2002
    Applicant: Council of Scientific and Industrial Research
    Inventors: Gojendra Nath Bordoloi, Babita Kumari, Nabibjyoti Bordoloi, Monoj Kanti Roy, Tarun Chandra Bora
  • 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: 6444450
    Abstract: A process for large-scale, low cost, batch or continuous production of polyphenols using enzyme-mediated reactions and methods for recycling non-consumed reactants.
    Type: Grant
    Filed: January 28, 1998
    Date of Patent: September 3, 2002
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: Joseph A. Akkara, Madhu S. R. Ayyagari, David L. Kaplan
  • Publication number: 20020115132
    Abstract: A method for producing carbon dioxide in a high concentration suitable for direct usage or more facile further purification wherein microbial growth and fermentation of one or more carbonaceous materials are carried out with the use of defined high concentration oxidant fluid which is provided to a fermentation broth to provide oxygen in a defined limited amount.
    Type: Application
    Filed: April 3, 2002
    Publication date: August 22, 2002
    Inventors: Chris Ka Kee Ho, Dan Grunwald
  • Patent number: 6416979
    Abstract: The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are independently H, C2-C6 acyl or halo-substituted benzoyl; and R3 is —C(O)O—C1-C6 alkyl, C(O)OH, CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R2 is acetyl and R3 is methoxycarbonyl, R1 is not H; and that when R3 is CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, R1 and R2 are H. The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like. The present invention further relates to a process for producing the compounds of the formula (I).
    Type: Grant
    Filed: September 8, 2000
    Date of Patent: July 9, 2002
    Assignee: Pfizer Inc.
    Inventors: Hideo Hirai, Katsuomi Ichikawa, Nakao Kojima, Hiroyuki Nishida, Kunio Satake, Nobuji Yoshikawa
  • Patent number: 6410265
    Abstract: This invention relates to the isolation of a novel putative efflux gene from Pseudomonas mendocina. The putative efflux gene is useful for probing an organism's efflux system to gain an understanding of the mechanisms of solvent tolerance. The invention further provides a Pseudomonas mendocina strain deficient in this gene. This strain is unable to grow in the presence of chloramphenicol and, compared to the wildtype strain, grows slowly in the presence of high concentrations of PHBA.
    Type: Grant
    Filed: October 30, 1998
    Date of Patent: June 25, 2002
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Kevin Keqin Chen
  • Patent number: 6387667
    Abstract: A process for producing cytidine diphosphate choline is provided. The process comprises carrying out an enzymatic reaction using microorganisms having the enzyme activities of cytidine-5′-triphosphate synthetase (pyrG), cholinephosphate cytidylyltransferase (CCT) and choline kinase (CKI) and a microorganism capable of producing uridine-5′-triphosphate from orotic acid as the enzyme sources, and orotic acid and choline and/or phosphorylcholine as the substrates; allowing cytidine diphosphate choline to accumulate in the reaction mixture; and recovering cytidine diphosphate choline from said reaction mixture.
    Type: Grant
    Filed: January 28, 1993
    Date of Patent: May 14, 2002
    Assignee: Kyowa Hakko Kogyo, Co., Ltd.
    Inventors: Akihiko Maruyama, Tatsuro Fujio, Sadao Teshiba
  • Publication number: 20020045225
    Abstract: The present invention relates to processes for the microbial oxidation of bicyclic heteroaromatic compounds which comprise contacting these compounds with a microorganism, or a suitable mutant thereof, and incubating the resulting mixture under conditions sufficient to yield an amount of their respective carboxylic acids. The present processes optionally further comprise the isolation and purification of the product carboxylic acids.
    Type: Application
    Filed: August 8, 2001
    Publication date: April 18, 2002
    Inventors: James J. Cawley, John W. Wong
  • Patent number: 6361979
    Abstract: 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: Grant
    Filed: January 27, 2000
    Date of Patent: March 26, 2002
    Assignee: Pfizer Inc.
    Inventors: Michael P. Burns, James J. Cawley, John W. Wong
  • 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
  • Patent number: 6284522
    Abstract: An isolated and purified DNA molecule, and an isolated and purified protein, that are involved in the degradation of s-triazine compounds (e.g., atrazine) are provided. A method for the purification of this protein is also provided.
    Type: Grant
    Filed: October 23, 1995
    Date of Patent: September 4, 2001
    Assignee: Regents of the University of Minnesota
    Inventors: Lawrence P. Wackett, Michael J. Sadowsky, Mervyn L. de Souza
  • Patent number: 6268183
    Abstract: The invention discloses a two-step process for recovery of thuringiensin, comprising adsorbing the thuringiensin from fermentation broth by calcium silicate, and dissociating the thuringiensin by dibasic sodium phosphate. The resulting thuringiensin can be further purified by using semi-preparative HPLC and electrodialysis to remove the excess salts from the recovered thuringiensin solution.
    Type: Grant
    Filed: June 2, 2000
    Date of Patent: July 31, 2001
    Assignee: National Science Council
    Inventors: Yew-Min Tzeng, Bing-Lan Liu, Shyuan-Shuenn Huang, Cheng-Ming Liu, Hung-Yieng Tsun
  • Publication number: 20010008768
    Abstract: A process for large-scale, low cost, batch or continuous production of polyphenols using enzyme-mediated reactions and methods for recycling non-consumed reactants.
    Type: Application
    Filed: January 28, 1998
    Publication date: July 19, 2001
    Inventors: JOSEPH A. AKKARA, MADHU S. R. AYYAGARI, DAVID L. KAPLAN
  • Patent number: 6248571
    Abstract: A process for the preparation of dihydroxypyrimidine derivatives of the general formula: in which R1 and R2 are identical or different and are a hydrogen atom, aryl group, or a C1-C4-alkyl group or an aryl group, starting from a compound of the general formula: in which R2 has the meaning mentioned above and R3 is —CN or COOR4, in which R4 is a C1-C4-alkyl group.
    Type: Grant
    Filed: February 25, 1998
    Date of Patent: June 19, 2001
    Assignee: Lonza AG
    Inventors: Beat Schmidt, Andreas Kiener, John McGarrity
  • 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: 6143541
    Abstract: This invention provides DNA fragments for efficiently preparing a protein having asymmetric hydrolase activity for 4-substituted 1,4-dihydropyridine derivatives, transformants obtained by using such a DNA fragment, and a process for preparing the aforesaid enzyme. Specifically, an isolated gene derived from the chromosome of Streptomyces viridosporus and encoding a protein having asymmetric hydrolase activity for 4-substituted 1,4-dihydropyridine derivatives, plasmids having the aforesaid gene integrated thereinto, transformants obtained by using such a plasmid, and a process for preparing the aforesaid enzyme by using such a transformant are disclosed. A process for the enzymatic conversion of 4-substituted 1,4-dihydropyridine derivatives by using the aforesaid enzyme is also disclosed.
    Type: Grant
    Filed: January 30, 1998
    Date of Patent: November 7, 2000
    Assignee: Mercian Corporation
    Inventors: Akira Arisawa, Motoko Matsufuji, Takurou Tsuruta, Kazuyuki Dobashi, Takashi Nakashima, Kunio Isshiki, Takeo Yoshioka
  • Patent number: 6121025
    Abstract: The present invention relates to a process for producing optically active 3-quinuclidinol or derivatives, wherein a racemic 3-quinuclidinol ester represented by the general formula (I): ##STR1## wherein R represents a straight-chain or branched alkyl group, and (H.sup.+) represents that said ester may be in the form of a salt formed with a mineral acid or an organic acid, is reacted with a microorganism belonging to the genus Aspergillus, Rhizopus, Candida or Pseudomonas having the ability to asymmetrically hydrolyze said ester linkage, a culture of said microorganism, a treated material from said microorganism, an enzyme produced by said microorganism, or an enzyme derived from swine or cattle.According to the present invention, there is provided a process for easily producing optically active 3-quinuclidinol derivatives which are important synthetic intermediates for pharmaceutical preparations etc.
    Type: Grant
    Filed: May 5, 1999
    Date of Patent: September 19, 2000
    Assignee: Mitsubishi Rayon Co., Ltd.
    Inventors: Eiji Sato, Kanehiko Enomoto
  • Patent number: 6037166
    Abstract: The invention relates to a process for preparing a substituted (6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidine compound of the formula (+)-I ##STR1## wherein: R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen, halo, C.sub.1 -C.sub.6 alkyl, amino, --OCH.sub.3, --OCF.sub.3 and CF.sub.3, and the dotted line represents an optional double bond; comprising:enzymatically catalyzing the acylation of a compound of the formula (.+-.)-II ##STR2## wherein the variables are as defined above, and hydrolysing the product to obtain (+)-I.
    Type: Grant
    Filed: June 15, 1998
    Date of Patent: March 14, 2000
    Assignee: Schering Corporation
    Inventors: William Brian Morgan, Jinchu Liu
  • 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: 5986095
    Abstract: A process is described for preparing a compound of the formula or the S-enantiomer thereof,wherein:R is alkyl, aryl, cycloalkyl, aralkyl, or cycloalkylalkyl,R.sup.1 is halogen;R.sup.2 is halogen, alkyl, cycloalkyl, aryl or ##STR1## wherein the process comprises treating the associated racemic alcohol with an acylatingagent ##STR2## (wherein L is a leaving group) and an enzyme or microorganism capable of enantioselective acylation. This process may also be used to isolate the unreacted R- or S-alcohol. The acylated product may be enantioselectively hydrolyzed with a lipase or lipase-supplying microorganism to the S- or R-alcohol. Compounds prepared by this invention are useful antipsychotic agents or useful intermediates therefor.
    Type: Grant
    Filed: January 6, 1992
    Date of Patent: November 16, 1999
    Assignee: E.R. Squibb & Sons, Inc.
    Inventors: Ronald L. Hanson, Ramesh N. Patel, Laszlo J. Szarka
  • Patent number: 5976563
    Abstract: The invention is related to a novel strain(s) of Bacillus thuringiensis in which essentially all of the pesticidal activity of said strain is in the supernatant of a fermentation of said strain. The strain produces a substance which has activity against an insect pest(s) of the order Coleoptera and which enhances the pesticidal activity of a Bacillus related pesticide. The invention further relates to pesticidal compositions comprising the substance and a pesticidal carrier, or the substance and a Bacillus related pesticide, a chemical pesticide and/or a virus with pesticidal properties as well as methods of using the pesticidal compositions to control a pest.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: November 2, 1999
    Assignee: Abbott Laboratories
    Inventors: Chi-Li Liu, Anita M. MacMullan, Patricia Ann Lufburrow, Robert L. Starnes, Denise C. Manker
  • 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
  • Patent number: 5922589
    Abstract: A process for the preparation of five-membered or six-membered ring lactams from aliphatic .alpha., .omega.-dinitriles has been developed. In the process an aliphatic .alpha.,.omega.-dinitrile is first converted to an ammonium salt of an .omega.-nitrilecarboxylic acid in aqueous solution using a catalyst having an aliphatic nitrilase (EC 3.5.5.7) activity, or a combination of nitrile hydratase (EC 4.2.1.84) and amidase (EC 3.5.1.4) activities. The ammonium salt of the .omega.-nitrilecarboxylic acid is then converted directly to the corresponding lactam by hydrogenation in aqueous solution, without isolation of the intermediate .omega.-nitrilecarboxylic acid or .omega.-aminocarboxylic acid. When the aliphatic .alpha.,.omega.-dinitrile is also unsymmetrically substituted at the .alpha.-carbon atom, the nitrilase produces the .omega.-nitrilecarboxylic acid ammonium salt resulting from hydrolysis of the .omega.
    Type: Grant
    Filed: July 1, 1998
    Date of Patent: July 13, 1999
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Robert Di Cosimo, Robert Donald Fallon, John Edward Gavagan, Frank Edward Herkes
  • Patent number: 5908954
    Abstract: A process for the preparation of five-membered or six-membered ring lactams from aliphatic .alpha.,.omega.-dinitriles has been developed. In the process an aliphatic .alpha.,.omega.-dinitrile is first converted to an ammonium salt of an .omega.-nitrile-carboxylic acid in aqueous solution using a catalyst having an aliphatic nitrilase (EC 3.5.5.7) activity, or a combination of nitrile hydratase (EC 4.2.1.84) and arnidase (EC 3.5.1.4) activities. The ammonium salt of the .omega.-nitrilecarboxylic acid is then converted directly to the corresponding lactam by hydrogenation in aqueous solution, without isolation of the intermediate .omega.-nitrilecarboxylic acid or .omega.-aminocarboxylic acid. When the aliphatic .alpha.,.omega.-dinitrile is also unsymmetrically substituted at the .alpha.-carbon atom, the nitrilase produces the .omega.-nitrilecarboxylic acid ammonium salt resulting from hydrolysis of the .omega.
    Type: Grant
    Filed: July 1, 1998
    Date of Patent: June 1, 1999
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Robert Di Cosimo, Robert Donald Fallon, John Edward Gavagan, Frank Edward Herkes