The Nitrogen Is In Same Side Chain As Ester Function Patents (Class 560/38)
  • Patent number: 6610710
    Abstract: Phenylalanine derivatives of the following formula and analogues thereof have an antagonistic activity to &agr;4&bgr;7 integrin and a selectivity toward &agr;4&bgr;1 integrin. They are used as therapeutic agents for various diseases to which &agr;4&bgr;7 integrin relates.
    Type: Grant
    Filed: June 28, 2002
    Date of Patent: August 26, 2003
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Chieko Ejima, Mitsuhiko Kojima, Eiji Nakanishi, Hiroyuki Izawa, Yuko Satake, Nobuyasu Suzuki, Manabu Suzuki, Masahiro Murata
  • Publication number: 20030158436
    Abstract: The present invention provides a commercially profitable process for producing a &bgr;-amino acid ester derivative
    Type: Application
    Filed: March 5, 2003
    Publication date: August 21, 2003
    Applicant: Kaneka Corporation
    Inventors: Akira Nishiyama, Kenji Inoue
  • Publication number: 20030109579
    Abstract: A novel class of dicarboxylic acid derivatives, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Application
    Filed: October 16, 2002
    Publication date: June 12, 2003
    Inventors: Per Sauerberg, Paul Stanley Bury, Lone Jeppesen, John Patrick Mogensen
  • Publication number: 20030109560
    Abstract: Novel compounds of general formula (I), the use of these compounds as medicaments, pharmaceuticaly compositions comprising the compounds and methods of treatment employing these compounds and compostiones. The present compounds may be useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). The compounds exert their effects by modulating the PPAR&ggr; response in a partial agonist manner.
    Type: Application
    Filed: July 29, 2002
    Publication date: June 12, 2003
    Inventors: Lone Jeppesen, Paul Stanley Bury, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg
  • Patent number: 6573399
    Abstract: The present invention provides a commercially profitable process for producing a &bgr;-amino acid ester derivative which comprises reacting an &agr;-amino acid ester derivative with a base and a dihalomethane, reacting the same with a lithium amide and an alkyllithium in succession, and treating the reaction product with an acid in an alcohol.
    Type: Grant
    Filed: February 21, 2001
    Date of Patent: June 3, 2003
    Assignee: Kaneka Corporation
    Inventors: Akira Nishiyama, Kenji Inoue
  • Publication number: 20030092746
    Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
    Type: Application
    Filed: May 21, 2001
    Publication date: May 15, 2003
    Inventors: William K. Hagmann, Stephen E. DeLaszlo, Theodore Kamenecka, Malcolm MacCoss
  • Publication number: 20030064976
    Abstract: The present invention provides certain alpha-amino acids and derivatives thereof, such as, but not limited to, esters, amides and salts. The present invention also provides a novel method for the synthesis of alpha-amino acids and derivatives thereof.
    Type: Application
    Filed: July 24, 2002
    Publication date: April 3, 2003
    Inventors: Sekar Alla, Seung-Yong Choi, Dale Dhanoa, Elso DiFranco, Galina Krokhina, Keqiang Li, Thiagarajan Balasubramanian, Wen-Chun Zhang
  • Patent number: 6541654
    Abstract: The invention includes selected novel optically active &agr;-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: April 1, 2003
    Assignee: Monsanto Company
    Inventor: John J. Talley
  • Patent number: 6518450
    Abstract: The present invention reveals a novel structure of guaiacoxypropanolamines shown in formula I: The composition comprising formula I acts as active intergant and pharmaceutical acceptable vehicle. The composition by perfect administration routes in the mammal when given potential &agr;/&bgr;-adrenergic blocking, is selective for emergency hypertension.
    Type: Grant
    Filed: December 20, 2000
    Date of Patent: February 11, 2003
    Assignee: National Science Council
    Inventor: Ing-Jun Chen
  • Publication number: 20030013881
    Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) 1
    Type: Application
    Filed: September 21, 2001
    Publication date: January 16, 2003
    Inventors: Roy Hom, Shumeye Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Fang
  • Publication number: 20030004360
    Abstract: Disclosed are intermediates and processes for preparing epoxides of the formula: 1
    Type: Application
    Filed: April 23, 2002
    Publication date: January 2, 2003
    Inventor: Michael R. Reeder
  • Publication number: 20020198400
    Abstract: A process for the synthesis of a compound of the formula 1
    Type: Application
    Filed: July 15, 2002
    Publication date: December 26, 2002
    Inventors: Ahmed F. Abdel-Magid, Judith H. Cohen, Cynthia A. Maryanoff, Frank John Villani, Hua M. Zhong
  • Publication number: 20020160961
    Abstract: Compositions comprising TRH and a compound of the general formula A—B—C—D(—E)p are used for treating the catabolic state of prolonged critical illness.
    Type: Application
    Filed: December 4, 2001
    Publication date: October 31, 2002
    Inventor: Michael Ankersen
  • Patent number: 6465684
    Abstract: A diastereomer complex obtained via a process for the separation of enantiomers is disclosed, wherein separation can be rapidly effected such that enantiomers are obtained with high e.e. values. The process permits the separation of mixtures of enantiomers in which more than one resolving agent is used, of which at least one resolving agent is optically active, and which yields a diastereomer complex containing at least two resolving agents in optically active form. The process provides for, inter alia, a diastereomer complex having at least three compounds of which at least two compounds are resolving agents in optically active form, and at least one compound is an enantiomer in optically active form. Also provided is a diastereomer complex having at least three compounds of which at least one compound is a resolving agent in optically active form, and at least two compounds which are enantiomers in optically active form.
    Type: Grant
    Filed: February 16, 2001
    Date of Patent: October 15, 2002
    Assignee: DSM N.V.
    Inventors: Ton R. Vries, Hans Wijnberg, Erik Van Echten, Lumbertus A. Hulshof, Quirinus B. Broxterman
  • Patent number: 6451854
    Abstract: The present invention relates to &agr;-amino acid phenyl ester derivatives having general formula (I) wherein R1 is (C1-3)alkyloxy; R2 is (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R3 is hydrogen, (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R4 is (C1-6)alkyl; R5 and R6 are independently (C1-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl or aralkyl, each of which may be optionally substituted with (C1-3)alkyloxy, (C1-3)alkyloxycarbonyl, cyano or NR7R8; R7 and R8 are independently (C1-6)alkyl; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these &agr;-amino acid phenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.
    Type: Grant
    Filed: January 18, 2001
    Date of Patent: September 17, 2002
    Assignee: Akzo Nobel N.V.
    Inventor: Niall Morton Hamilton
  • Patent number: 6433209
    Abstract: Methods for stereoselective substitution in which a (mono or un)-&agr;-substituted unprotected &bgr;-amino ester compound or salt thereof is reacted with an aliphatic electrophile in the presence of a base selected from alkyl lithium compounds, lithium hydride, lithium amide, lithium dialkyl amides and alkali hexamethyldisilylamines.
    Type: Grant
    Filed: January 26, 2000
    Date of Patent: August 13, 2002
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Sithamalli V. Chandramouli, Michael K. O'Brien, Tory H. Powner
  • Publication number: 20020107406
    Abstract: A novel calcium receptor active compound having the formula is provided:
    Type: Application
    Filed: January 17, 2002
    Publication date: August 8, 2002
    Applicant: NPS Pharmaceuticals, Inc.
    Inventors: Teruyuki Sakai, Atsuya Takami, Rika Nagao
  • Patent number: 6426364
    Abstract: Provided, among other things, is a compound of Formula I: wherein: Ar1 and Ar2 are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkoxy, cycloalkyl, cycloalkyloxy, heterocycloalkyl, heterocycloalkyloxy, alkanoyl, thioalkyl, aralkyl, aralkyloxy, aryloxyalkyl, aryloxyalkoxy, cycloalkyl-substituted alkyl, cycloalkyloxy-substituted alkyl, cycloalkyl-substituted alkoxy, cycloalkyloxy-substituted alkoxy, heterocycloalkyl-substituted alkyl, heterocycloalkyloxy-substituted alkyl, heterocycloalkyl-substituted alkoxy, heterocycloalkyloxy-substituted alkoxy, thioaryl, aralkylthio, thioarylalkyl, aralkylthioalkyl, halo, NO2, CF3, CN, OH, alkylenedioxy, SO2NRR′, NRR′, CO2R (where R and R′ are independently selected from the group consisting of H and alkyl), and a second aryl group, which may be substituted as above; R1 is selected from the group consisting of H and alkyl; R2 is selec
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: July 30, 2002
    Assignee: NPS Allelix Corp.
    Inventors: Ian Egle, Jennifer Frey, Methvin Isaac
  • Publication number: 20020099220
    Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.
    Type: Application
    Filed: October 19, 2001
    Publication date: July 25, 2002
    Applicant: NPS Pharmaceuticals, Inc.
    Inventors: Eric G. Del Mar, Robert M. Barmore, Derek Sheehan, Bradford C. Van Wagenen, James F. Callahan, Richard M. Keenan, Nikesh R. Kotecha, Maria Amparo Lago, Linda Sue Southall, Mervyn Thompson
  • Publication number: 20020099092
    Abstract: GABA-related pro-drugs of the formula (III) are provided that when administered to humans or other mammals provide an increased duration of active compound in the plasma compared to compounds of corresponding structure in which labile groups are not present.
    Type: Application
    Filed: August 1, 2001
    Publication date: July 25, 2002
    Inventors: David Clive Blakemore, Justin Stephen Bryans, Sophie Caroline Williams
  • Patent number: 6423866
    Abstract: Lower alkyl esters of 3-amino crotonates substituted by halogen in the C-4 position, e.g. ethyl 3-amino-4,4,4-trifluoro-crotonate, in which the amino group optionally may be substituted by one or two C1 to C3 alkyl groups or by one or two aryl groups, e.g. phenyl, are synthesized by thermolysis of ammonium salts of corresponding lower alkyl esters of acetoacetic acid substituted in the C-4 position by halogen, and removal of the resulting water of reaction. The water of reaction may be removed by an entraining agent, which preferably has a specific gravity heavier than that of the aqueous phase which forms in the reaction. This minimizes yield losses due to the ammonium salt becoming dissolved in the aqueous phase and results in especially high yields. Formation of the ammonium salt and thermolysis can be carried out simultaneously. Alternatively, it is possible to start from a molten ammonium salt of the halogencrotonate, e.g.
    Type: Grant
    Filed: May 8, 2000
    Date of Patent: July 23, 2002
    Assignee: SolvaytFlour und Derivate GmbH
    Inventors: Max Braun, Francine Jannssens, Werner Rudolph, Kerstin Eichholz
  • Publication number: 20020091142
    Abstract: Compounds of the formula I 1
    Type: Application
    Filed: March 9, 2001
    Publication date: July 11, 2002
    Inventors: Nigel Graham Cooke, Michael Lloyd Sabio
  • Publication number: 20020091102
    Abstract: SNACE derivatives as pharmacological active agents and pharmacological compositions containing these compounds, in particular for transdermal, oral, rectal and inhalational application, are described.
    Type: Application
    Filed: October 30, 2001
    Publication date: July 11, 2002
    Inventor: Dimitrios Tsikas
  • Patent number: 6417368
    Abstract: The invention provides a resin-immobilized imine represented by the following formula: P—Q—N—═CH—R   I [in the formula, P represents the principal chain of a resin polymer; Q represents a substituted or unsubstituted hydrocarbon side chain or a substituted or unsubstituted hydrocarbon side chain with a heteroatom interposed therein; R represents a substituted or unsubstituted hydrocarbon group or heterocyclic group] and a resin-immobilized &bgr;-aminocarbonyl compound of the following formula: which can be released as &bgr;-aminocarbonyl compound from the solid phase; and the invention also provide a resin-immobilized amine of the following formula: —P—Q1—O—Q2—NH2   III [Q1 and Q2 independently represent a hydrocarbon chain such as arylene, alkylenearylene or arylenealkylene], which is essential for solid state synthesis; and the invention has enabled the solid state synthesis of &bgr;-am
    Type: Grant
    Filed: November 8, 2000
    Date of Patent: July 9, 2002
    Assignee: Japan Science and Technology Corporation
    Inventors: Shu Kobayashi, Yoji Aoki
  • Publication number: 20020087026
    Abstract: The invention relates to a method for preparing an ester, by admixing a compound having the structure I: 1
    Type: Application
    Filed: February 6, 2002
    Publication date: July 4, 2002
    Applicant: Emory University
    Inventors: Dennis C. Liotta, Hariharan Venkatesan, Laura Captain, Michael V. Voronkov, James P. Snyder, Marcus A. Schestopol
  • Publication number: 20020082440
    Abstract: This invention relates to a method of preparing a compound type where at least one of R′ or R″ is a carboxyl group (I) by treating a compound of formula (II) with a Group I(a) or Group II(a) metal halide, with an aprotic dipolar amide-based solvent and water.
    Type: Application
    Filed: November 8, 2001
    Publication date: June 27, 2002
    Applicant: SmithKline Beecham Corporation
    Inventors: Kevin Webb, Wilford Mendelson, Jianhao Chen
  • Patent number: 6399809
    Abstract: Process for the preparation of amino acid derivatives of the general formula I where R1-R4 are as defined herein, from the corresponding malonic acid monoester amides of the general formula II  by Hofmann degradation using a hypohalite in an aqueously basic medium, which comprises carrying out the reaction in the presence of an alcohol or amine and using the hypohalite in amounts of from 1.0 to 1.5 equivalents and the base in amounts of from 0.8 to 4.0 equivalents per mole of starting material II.
    Type: Grant
    Filed: April 21, 2000
    Date of Patent: June 4, 2002
    Assignee: Degussa AG
    Inventors: Wolfgang Kleemiss, Marcel Feld
  • Patent number: 6384220
    Abstract: Para-aryl or heteroaryl substituted phenyl amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.
    Type: Grant
    Filed: May 1, 2001
    Date of Patent: May 7, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Wendy Lea Corbett, Nancy-Ellen Haynes, Ramakanth Sarabu
  • Publication number: 20020049332
    Abstract: The invention includes selected novel optically active &agr;-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.
    Type: Application
    Filed: October 11, 2001
    Publication date: April 25, 2002
    Inventor: John J. Talley
  • Patent number: 6369194
    Abstract: The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.
    Type: Grant
    Filed: November 9, 1998
    Date of Patent: April 9, 2002
    Assignee: Yale University
    Inventor: Harry H. Wasserman
  • Patent number: 6355618
    Abstract: The present invention is directed to novel dipeptide thereof, represented by the general Formula I: where R1-R3, X and Y are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: March 12, 2002
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Eckard Weber, Yan Wang, Gordon B. Mills, Douglas R. Green
  • Patent number: 6353111
    Abstract: 2,3-Di-substituted trans olefinic N-heteroaromatic or urido propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
    Type: Grant
    Filed: December 1, 2000
    Date of Patent: March 5, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Wendy Lea Corbett, Ramakanth Sarabu, Achyutharao Sidduri
  • Patent number: 6348614
    Abstract: Novel aminobutyric acids derivatives and methods for protecting crops against fungal diseases by applying to the crops or their locus a composition containing an effective amount of said derivatives.
    Type: Grant
    Filed: June 25, 1999
    Date of Patent: February 19, 2002
    Assignee: Agrogene Ltd.
    Inventors: Yogal Cohen, Moshe Korat
  • Publication number: 20020016461
    Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases.
    Type: Application
    Filed: April 6, 2001
    Publication date: February 7, 2002
    Inventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Harter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jorg Keldenich, Ulf Brueggemeier, Klemens Lustig
  • Patent number: 6316656
    Abstract: The invention includes selected novel optically active &agr;-ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.
    Type: Grant
    Filed: July 5, 2000
    Date of Patent: November 13, 2001
    Assignee: Monsanto Company
    Inventor: John J. Talley
  • Patent number: 6306911
    Abstract: This invention relates to a series of substituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules that bind to neutral sphingomyelinase and inhibit its activity.
    Type: Grant
    Filed: February 7, 2000
    Date of Patent: October 23, 2001
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Michael P. Wachter, Praful Lalan
  • Publication number: 20010029300
    Abstract: A process for the synthesis of a compound of the formula 1
    Type: Application
    Filed: May 15, 2001
    Publication date: October 11, 2001
    Inventors: Ahmed F. Abdel-Magid, Judith H. Cohen, Cynthia A. Maryanoff, Frank John Villani, Hua M. Zhong
  • Patent number: 6291478
    Abstract: The present application relates to novel compounds belonging to the benzylaminodiacetamide family which have good anti-irritant and soothing properties. The invention also relates to their use in a composition comprising a physiologically acceptable medium, in particular in order to prevent and/or treat certain cutaneous disorders and more particularly in order to treat sensitive skins.
    Type: Grant
    Filed: March 13, 2000
    Date of Patent: September 18, 2001
    Assignee: L'Oreal
    Inventors: Jean-Baptiste Galey, Maria Dalko
  • Publication number: 20010008947
    Abstract: Use in the prevention and/or in the treatment of neurodegenerative diseases of 2-amino-4-phenyl-4-oxo-butyric acid derivatives which act as kynureninase enzyme inhibitors and/or kynurenine-3-hydroxylase enzyme inhibitors.
    Type: Application
    Filed: October 14, 1997
    Publication date: July 19, 2001
    Inventors: MARIO VARASI, ANTONIO GIORDANI, CARMELA SPECIALE, MASSIMO CINI, ALBERTO BIANCHETTI
  • Patent number: 6235929
    Abstract: A novel class of tripeptide &agr;-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula M1—AA—AA—AA—CO—NR3R4.
    Type: Grant
    Filed: December 27, 1996
    Date of Patent: May 22, 2001
    Assignee: Georgia Tech Research Corporation
    Inventor: James C Powers
  • Patent number: 6235927
    Abstract: A diastereomer complex obtained via a process for the separation of enantiomers is disclosed, wherein separation can be rapidly effected such that enantiomers are obtained with high e.e. values. The process pets the separation of mixtures of enantiomers in which more than one resolving agent is used, of which at least one resolving agent is optically active, and which yields a diastereomer complex containing at least two resolving agents in optically active form. The process provides for, inter alia, a diastereomer complex having at least three compounds of which at least two compounds are resolving agents in optically active form, and at least one compound is an onantiomer in optically active form. Also provided is a diastereomer complex having at least three compounds of which at lea one compound is a resolving agent in optically active form, and at least two compounds which are enantiomers in optically active form.
    Type: Grant
    Filed: October 22, 1997
    Date of Patent: May 22, 2001
    Assignee: DSM N.V.
    Inventors: Ton R. Vries, Hans Wijnberg, Erik Van Echten, Lumbertus A. Hulshof, Quirinus B. Broxterman
  • Patent number: 6207710
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis.
    Type: Grant
    Filed: September 30, 1998
    Date of Patent: March 27, 2001
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Thomas C. Britton, James J. Droste, Beverly K. Folmer, George W. Huffman, Varghese John, Lee H. Latimer, Thomas E. Mabry, Jeffrey S. Nissen, Warren J. Porter, Jon K. Reel, Eugene D. Thorsett, Jay S. Tung, Jing Wu
  • Patent number: 6201023
    Abstract: A method for protecting a crop against plant-parasitic nematode attack by inducing local and systemic resistance of the crop comprising the application of a composition containing an effective amount of &bgr;-amino butyric acid or derivatives thereof to the crop or its locus.
    Type: Grant
    Filed: June 10, 1997
    Date of Patent: March 13, 2001
    Assignee: Agrogene Ltd.
    Inventors: Yuji Oka, Yitzhak Spiegel, Yigal Cohen
  • Patent number: 6191306
    Abstract: Disclosed is a process for the preparation of cyclopropylglycine by a 5-step process wherein cyclopropanecarboxaldehyde is reacted with an &agr;-aminoalkylaromatic compound to obtain an imine which is reacted with a cyanide to produce an aminonitrile compound; the aminonitrile compound is hydrolyzed to the corresponding aminocarboxylic acid and finally the arylalkyl residue is removed from the amino group by hydrogenolysis.
    Type: Grant
    Filed: August 3, 1999
    Date of Patent: February 20, 2001
    Assignee: Eastman Chemical Company
    Inventors: Daniel John Bayston, Jonathan Luke William Griffin, Arne Gruman, Mario Eugenio Cosimino Polywka, Ronald Michael Scott
  • Patent number: 6172239
    Abstract: The invention relates to compounds of the formula The compounds have agreat affinity for the neurotensin receptors.
    Type: Grant
    Filed: August 16, 1999
    Date of Patent: January 9, 2001
    Assignee: Sanofi
    Inventors: Bernard Labeeuw, Danielle Gully, Francis JeanJean, Jean-Charles Molimard, Robert Boigegrain
  • Patent number: 6172256
    Abstract: The present invention is directed to a method for the preparation of a chiral &bgr;-amino ester of the formula wherein R is lower alkyl; and X and Y are the same or different Cl, Br or I.
    Type: Grant
    Filed: March 3, 1999
    Date of Patent: January 9, 2001
    Assignee: G.D. Searle & Co.
    Inventors: James W. Malecha, Thomas P. Fraher
  • Patent number: 6166081
    Abstract: A pharmaceutical composition for treatment of Parkinson's disease comprising a compound of levodopa dissolved in a non-degradative solvent which allows transdermal administrtion of levodopa. The compound of levodopa is an alkyl-ester of levodopa and the solvent is a formulation comprising a substantially non-aqueous solvent, a transdermal enhancer and a detergent. The alkyl-ester of levodopa is preferably levodopa-ethyl-ester (LDEE).
    Type: Grant
    Filed: April 7, 1999
    Date of Patent: December 26, 2000
    Inventors: Moshe Kushnir, Eliahu Heldman
  • Patent number: 6153650
    Abstract: Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.
    Type: Grant
    Filed: March 1, 1999
    Date of Patent: November 28, 2000
    Assignee: Warner-Lambert Company
    Inventors: Justin Stephen Bryans, David Christopher Horwell, Clare Octavia Kneen, Andrew John Thorpe, David Juergen Wustrow
  • Patent number: 6153591
    Abstract: The present invention is directed to novel dipeptides represented by the general Formula I: ##STR1## where R.sub.1 -R.sub.2 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
    Type: Grant
    Filed: March 16, 1999
    Date of Patent: November 28, 2000
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, John Drewe, Yan Wang, Eckard Weber
  • Patent number: RE37795
    Abstract: A method for preparing diphenol compounds, which method includes the steps of coupling a hydroxyphenyl carboxylic acid with a L-tyrosine ester in a water-miscible organic reaction solvent containing a carbodiimide capable of forming a water-soluble urea by-product, thereby forming a diphenol reaction product; and combining the reaction mixture with an amount of water effective to precipitate the diphenol as a water-immiscible organic phase, so that a water-immiscible organic phase is formed containing the diphenol reaction product. New diphenol monomers and polymers polymerized therefrom are also discussed.
    Type: Grant
    Filed: July 21, 1999
    Date of Patent: July 16, 2002
    Inventors: Joachim B. Kohn, Stephen Brocchini, Arthur L. Schwartz