The Nitrogen Is In Same Side Chain As Ester Function Patents (Class 560/38)
  • Patent number: 7253299
    Abstract: A process for purifying N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine which comprises subjecting N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine contaminated with impurities to crystallization from a solvent comprising a water-soluble non-protic organic solvent, thereby removing the impurities into the mother liquor and giving crystals of N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine, according to which N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine having a high quality can be obtained in a high yield and a high productivity and which is suitable for practice on an industrial scale.
    Type: Grant
    Filed: July 10, 2002
    Date of Patent: August 7, 2007
    Assignee: Kaneka Corporation
    Inventors: Yasuhiro Iida, Hajime Manabe, Yasuyoshi Ueda
  • Patent number: 7238830
    Abstract: The present invention provides N-alkylaspartyl dipeptideester compounds and salts thereof, such as N-[N-[3-(3-hydroxy-4-methoxyphenyl)-3-methylbutyl]-L-?-aspartyl]-L-phenylalanine 1-methyl ester, which provide high degrees of sweetness in comparison to conventional products, compositions and products containing the novel aspartyl dipeptide ester compounds and method of producing the novel aspartyl dipeptide ester compounds.
    Type: Grant
    Filed: March 16, 2001
    Date of Patent: July 3, 2007
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yusuke Amino, Kazuko Yuzawa, Tadashi Takemoto, Ryoichiro Nakamura
  • Patent number: 7202381
    Abstract: This invention is directed towards novel compounds as opioid receptor modulators, antagonists, and agonists useful for the treatment of opioid modulated disorders such as pain and gastrointestinal disorders.
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: April 10, 2007
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Henry J. Breslin, Wei He, Robert W. Kavash
  • Patent number: 7125442
    Abstract: A lightfast additive and an ink composition including the same include a benzophenone moiety for lightfastness and a moiety for wettability and the ability to stabilize a colorant, wherein the two moieties are covalently bonded. The lightfast additive may exhibit effective ultraviolet (UV) light absorption capacity, effective wettability, and an ability to stabilize a colorant. The ink composition utilizing the light fast additive thus has an improved lightfastness and long-term storage stability.
    Type: Grant
    Filed: May 24, 2004
    Date of Patent: October 24, 2006
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Kyung-hoon Lee, Seung-min Ryu, Yeon-kyoung Jung
  • Patent number: 7091373
    Abstract: There is provided a production method for producing a biarylalanine compound of formula (4): wherein R1 represents a amino protective group and R2 represents an amino protective group or a hydrogen atom, R3 is a carboxy protective group, or the like, and R4 is a substituted or unsubstituted aryl or heteroaryl group, characterized by reacting an aromatic amino acid of formula (1) wherein X is a halogen atom or a trifluoromethanesulfonyloxy group, and R1, R2 and R3 has the same meaning as defined above, with an organic boron compound of formula (2): wherein R4 has the same meaning as defined above, and Q1 and Q2 are the same or different and each is a hydroxy group, an alkoxy group having 1 to 4 carbon atom(s), in the presence of nickel catalyst and a base.
    Type: Grant
    Filed: March 4, 2003
    Date of Patent: August 15, 2006
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hiroshi Ueda, Isao Kurimoto
  • Patent number: 7071349
    Abstract: The present invention is to provide a purification method of obtaining N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine of high quality in good yield with high productivity, which is accordingly suited for commercial scale application. An impurity-contaminated N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine is crystallized from a mixed solvent of alcohol and water in a volume ratio of alcohol/water being 1 to 20 to remove a contaminating impurity into a mother liquor and give crystals of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.
    Type: Grant
    Filed: March 19, 2002
    Date of Patent: July 4, 2006
    Assignee: Kanaka Corporation
    Inventors: Akira Matsumoto, Michio Nomura, Yoshikazu Kogame, Yasuyoshi Ueda
  • Patent number: 7064231
    Abstract: The invention relates to stereoisomerically enriched diamines, to metal complexes comprising these diamines and also to their use in a process for asymmetrically reducing ketones using silanes, in particular polymethylhydrosiloxane, as reducing agents.
    Type: Grant
    Filed: August 19, 2003
    Date of Patent: June 20, 2006
    Assignee: Bayer Aktiengesellschaft
    Inventor: Jürgen Köcher
  • Patent number: 7034015
    Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: April 25, 2006
    Assignee: Leo Pharma A/S
    Inventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
  • Patent number: 7015348
    Abstract: To provide a producing method of an optically active ?-amino acid useful as intermediate for the production of medicines, agricultural chemicals and physiologically active substances, by means of a catalytic and asymmetric synthesis method of high performance and a high enantiomeric excess, without requiring additional procedures such as introduction and removal of protecting group and so on. A producing method of an optically active ?-amino acids which comprises subjecting an enamine to an asymmetric hydrogenation.
    Type: Grant
    Filed: July 29, 2003
    Date of Patent: March 21, 2006
    Assignee: Takasago International Corporation
    Inventors: Kazuhiko Matsumura, Xiaoyong Zhang, Takao Saito
  • Patent number: 7012071
    Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
    Type: Grant
    Filed: July 16, 2004
    Date of Patent: March 14, 2006
    Assignee: Wellstat Therapeutics Corporation
    Inventors: Shalini Sharma, Reid W. von Borstel
  • Patent number: 6946491
    Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
    Type: Grant
    Filed: October 14, 2003
    Date of Patent: September 20, 2005
    Assignee: Wellstat Therapeutics Corporation
    Inventors: Shalini Sharma, Reid W. von Borstel
  • Patent number: 6936719
    Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.
    Type: Grant
    Filed: December 18, 2003
    Date of Patent: August 30, 2005
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, R. Scott Rowland, Pooran Chand, Pravin L. Kotian, Yahya El-Kattan, Shri Niwas
  • Patent number: 6936636
    Abstract: Compounds of the formula: where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of reducing serum thyroxine levels and transiently increasing triglyceride levels.
    Type: Grant
    Filed: June 26, 2003
    Date of Patent: August 30, 2005
    Assignee: Allergan, Inc.
    Inventors: Santosh Sinha, Kwok Yin Tsang, Smita Bhat, Roshantha A. Chandraratna
  • Patent number: 6930200
    Abstract: Mono-substituted and di-substituted alpha-amino acids and derivatives thereof, substituted at the alpha positon with one (mono-) or two (di-) substituents (R2 and/or R3) as shown in Formula 1: N(R4R5)C(R2R3)CO(OR1).
    Type: Grant
    Filed: June 26, 2003
    Date of Patent: August 16, 2005
    Assignee: Pharmacore, Inc.
    Inventor: Adnan M. M. Mjalli
  • Patent number: 6921774
    Abstract: The invention provides novel compounds of the formula I below: wherein the meaning of each substituent is defined in the application. The compounds are useful as inhibitors of the glycine transporter and useful in the treatment of diseases responsive to the inhibition of the glycine transporter. The invention provides a pharmaceutical composition comprising a compound of Formula I as defined above and the use of compounds as above for the manufacture of medicaments for treatment of diseases responsive to ligands of the glycine transporter.
    Type: Grant
    Filed: January 17, 2003
    Date of Patent: July 26, 2005
    Assignee: H. Lundbeck A/S
    Inventors: Ejner Knud Moltzen, Paul Garrick Smith, Christian Krog-Jensen, Klaus Peter Bøgesø
  • Patent number: 6900344
    Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention also relates to dicarboxylic salicylamide delivery agent compounds for the delivery of active agents. Methods of administration are provided as well.
    Type: Grant
    Filed: March 21, 2001
    Date of Patent: May 31, 2005
    Assignee: Emisphere Technologies, Inc.
    Inventors: Joseph N. Bernadino, Doris C. O'Toole, William E. Bay
  • Patent number: 6875831
    Abstract: The invention pertains to a compound of formula (I), (II) or (III) wherein R1 and R2 are independently of each other hydrogen, C1-C18alkyl, C3-C18alkenyl, C3-C18alkinyl or phenyl which are unsubstituted or substituted by NO2, halogen, amino, hydroxy, cyano, carboxy, C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylamino or di(C1-C4alkyl)amino; A is a group capable of forming a stable free nitroxyl radical A*, which is bound via its oxygen atom to the carbon atom; Y is O, NR3 or CHR3—Xa, wherein Xa is O, S or NR3; R3 is hydrogen, C1-C18alkyl, C3-C18alkenyl, C3-C18alkinyl or phenyl which are unsubstituted or substituted by NO2, halogen, amino, hydroxy, cyano, carboxy, C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylamino or di(C1-C4alkyl)amino; Q1 is an organic or inorganic radical, derived from a compound having at least one functional group being capable of reacting with a hydroxy group; Q2 is an organic radical derived from a mono or polyfunctional alcohol, mono or polyfunctional aminoalcohol, mono or polyfunctional amine
    Type: Grant
    Filed: June 26, 2000
    Date of Patent: April 5, 2005
    Assignee: CIBA Specialty Chemicals Corp.
    Inventors: Andreas Kramer, Peter Nesvadba, Marie-Odile Zink, Wiebke Wunderlich
  • Patent number: 6855843
    Abstract: The present invention relates to a pharmaceutical composition comprising as an active ingredient a compound of formula (I), wherein Ring A is an aromatic or a heterocyclic ring; Q is a bond, carbonyl, lower alkylene, lower alkenylene, —O— -(lower alkylene)-, etc.; n is 0, 1 or 2; Z is oxygen or sulfur; W is oxygen, sulfur, —CH?CH—, —NH— or —N?CH—; R1, R2 and R3 are the same or different and are hydrogen, halogen, hydroxyl, a substituted or unsubstituted lower alkyl gorup, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, etc.; R4 is tetrazolyl, carboxyl group, amide or ester; R5 is hydrogen, nitro, amino, hydroxyl, lower alkanoyl, lower alkyl, etc.; R6 is selected from (a) a substituted or unsubstituted phenyl group, (b) a substituted or unsubstituted pyridyl group, (c) a substituted or unsubstituted thienyl group, (d) a substituted or unsubstituted benzofuranyl group, etc.; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 4, 2002
    Date of Patent: February 15, 2005
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Ila Sircar, Kristjan S. Gudmundsson, Richard Martin
  • Patent number: 6852876
    Abstract: The novel compound of the disclosure is 4-chloro-4-(4-ethoxy-phenyl)-2-(fluoren-9-ylidene-hydrazono)-but-3-enoic acid methyl ester (3F-19), and it alone or in combination with 4-(4-Ethoxy-phenyl)-2-(N?-fluoren-9-ylidene-hydrazino)-2-hydroxy-4-oxo-butyric acid methyl ester (OF-13), appears useful in humans as therapeutic means for the eradication of tumors from the human's colon.
    Type: Grant
    Filed: June 7, 2002
    Date of Patent: February 8, 2005
    Assignee: University of Central Florida
    Inventors: D. Howard Miles, Solodnikov Sergey Yurjevich, Lisovskaja Natalja Anatoljevna, Elena A. Goun
  • Patent number: 6849756
    Abstract: The invention includes selected novel optically active ?-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: February 14, 2003
    Date of Patent: February 1, 2005
    Assignee: Monsanto Company
    Inventor: John J. Talley
  • Patent number: 6838527
    Abstract: As an ?-iminoester derivative that is stable under normal conditions and a method of producing various ?-aminoester derivatives using them, a polymer-immobilized ?-iminoester derivative represented by the following general formula (1): wherein R1 represents an alkyl chain of 1 or more carbons, and R2 represents a hydrogen atom, halogen atom, or an alkyl group, aryl group or alkoxy group that may contain substituents, and a method of producing an ?-iminoester derivative using them are provided.
    Type: Grant
    Filed: March 13, 2001
    Date of Patent: January 4, 2005
    Assignee: Japan Science and Technology Corporation
    Inventor: Shu Kobayashi
  • Patent number: 6812363
    Abstract: A process for preparing racemic mixtures containing nearly equal amounts of stereo isomers of compounds of formula (I), or their salts, by heating an enantiomerically enriched material with thionyl chloride. A required useful enantiomer may thereby be recovered from unwanted mother liquors that would otherwise be otherwise be discarded.
    Type: Grant
    Filed: October 15, 2002
    Date of Patent: November 2, 2004
    Assignee: USV Limited
    Inventors: Krishna K. Maheshwari, Rayaprolu Kodandarama Sarma, Shreerang Vidyadhar Joshi, Anup Ramkrishna Barde, Rajiv Pandurang Sutar, Prasad Vasudeo Ranade
  • Patent number: 6784311
    Abstract: Process for the preparation of 3-aminoalkanoic acid esters of the general formula: in which R is C1-6-alkyl and R1 is hydrogen, C1-6-alkyl or phenyl, or their salts, by catalytic hydrogenation of the corresponding 3-amino-2-alkenoic acid esters of the general formula: in which R and R1 have the above mentioned meanings. The hydrogenation is carried out in the presence of a strong acid and the salt of the 3-aminoalkanoic acid ester (I) and the strong acid formed is optionally converted into the free 3-aminoalkanoic acid ester (I) or into another salt in a manner known per se.
    Type: Grant
    Filed: August 21, 2002
    Date of Patent: August 31, 2004
    Assignee: Lonza AG
    Inventor: Rudolf Fuchs
  • Publication number: 20040147773
    Abstract: A process for purifying N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine which comprises subjecting N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine contaminated with impurities to crystallization from a solvent comprising a water-soluble non-protic organic solvent, thereby removing the impurities into the mother liquor and giving crystals of N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine, according to which N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine having a high quality can be obtained in a high yield and a high productivity and which is suitable for practice on an industrial scale.
    Type: Application
    Filed: May 20, 2003
    Publication date: July 29, 2004
    Inventors: Yasuhiro Iida, Hajime Manabe, Yasuyoshi Ueda
  • Publication number: 20040133012
    Abstract: The present invention is directed to novel themisone derivative compounds that have been modified to prevent the formation of the toxic metabolite, 2-phenyl-acrylamide. Compositions comprising such derivative compounds have activity as anesthetics and as neuroprotective agents.
    Type: Application
    Filed: October 15, 2003
    Publication date: July 8, 2004
    Inventor: Milton L. Brown
  • Publication number: 20040073057
    Abstract: A process for preparing racemic mixtures containing nearly equal amounts of stereo isomers of compounds of formula (I), or their salts, by heating an enantiomerically enriched material with thionyl chloride.
    Type: Application
    Filed: October 15, 2002
    Publication date: April 15, 2004
    Inventors: Krishna K. Maheshwari, Rayaprolu Kodandarama Sarma, Shreerang Vidyadhar Joshi, Anup Ramkrishna Barde, Rajiv Pandurang Sutar, Prasad Vasudeo Ranade
  • Publication number: 20040059149
    Abstract: Mono-substituted and di-substituted alpha-amino acids and derivatives thereof, substituted at the alpha positon with one (mono-) or two (di-) substituents (R2 and/or R3) as shown in Formula 1: N(R4R5)C(R2R3)CO(OR1).
    Type: Application
    Filed: June 26, 2003
    Publication date: March 25, 2004
    Inventor: Adnan M.M. Mjalli
  • Publication number: 20040044217
    Abstract: The present invention relates to a process for the preparation of halo-4-phenoxyquinolines.
    Type: Application
    Filed: June 30, 2003
    Publication date: March 4, 2004
    Inventors: Karl Leopold Krumel, Ruth Cezar Reed, Thomas A. Olmstead, Gary Alan Roth, Ian Robert King, Donald Neil Brattesani, Kent Douglas Campbell, John Davies
  • Patent number: 6699994
    Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.
    Type: Grant
    Filed: April 23, 2002
    Date of Patent: March 2, 2004
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, R. Scott Rowland, Pooran Chand, Pravin L. Kotian, Yahya El-Kattan, Shri Niwas
  • Patent number: 6699463
    Abstract: Compounds of Formula I Each R is independently linear or branched C1 to C8 alkyl, or linear or branched C1 to C8 alkoxy or one R is H and the other R is linear or branched C1 to C8 alkyl, or linear or branched C1 to C8 alkoxy; R1 is selected from the group consisting of COCH3, CO2R3, CONH2, CONH(R4)2, CN, COX(CH2)n-N—(R2)(R4)(R3), and the quaternized salt form of the formula COX(CH2)n-N—(R2)(R4)(R3)+Y−; X is O or NH; n is an integer of 1 to 5; Y is an anion; and R2, R3 and R4 are independently linear or branched C1 to C20. Hair care formulations and other compounds containing compounds of Formula I, and methods for protecting hair and substrates such as polymers, textiles, fabrics, leathers and paints using the compounds herein.
    Type: Grant
    Filed: April 10, 2002
    Date of Patent: March 2, 2004
    Assignee: EM Industries
    Inventor: Ratan K. Chaudhuri
  • Publication number: 20040037778
    Abstract: Iodinated and/or brominated derivatives of aromatic dihydroxy monomers are prepared and polymerized to form radio-opaque polymers. The monomers may also be copolymerized with other dihydroxy monomers. The iodinated and brominated aromatic dihydroxy monomers can be employed as radio-opacifying, biocompatible non-toxic additives for other polymeric biomaterials. Radio-opaque medical implants and drug delivery devices for implantation prepared from the polymers of the present invention are also disclosed.
    Type: Application
    Filed: November 5, 2002
    Publication date: February 26, 2004
    Inventors: Joachim B. Kohn, Durgadas Bolikal, Sanyog M. Pendharkar
  • Publication number: 20040024229
    Abstract: There is provided a production method for producing a biarylalanine compound of formula (4): 1
    Type: Application
    Filed: March 4, 2003
    Publication date: February 5, 2004
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Hiroshi Ueda, Isao Kurimoto
  • Publication number: 20040014969
    Abstract: The invention relates to compound of formula (I): 1
    Type: Application
    Filed: March 14, 2003
    Publication date: January 22, 2004
    Inventors: Carole Descamps-Francois, Said Yous, Daniel Lesieur, Gerald Guillaumet, Marie-Claude Viaud, Herve Da Costa, Caroline Bennejean, Philippe Delagranes, Pierre Renard
  • Publication number: 20040010148
    Abstract: A compound of Formula (IA) or Formula (IB) 1
    Type: Application
    Filed: May 28, 2003
    Publication date: January 15, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Thomas Martin Kirrane, Daniel Kuzmich, John Robert Proudfoot, Hossein Razavi, David Thomson
  • Patent number: 6677360
    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. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.
    Type: Grant
    Filed: April 6, 2001
    Date of Patent: January 13, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
  • Patent number: 6673543
    Abstract: The invention provides solid support synthetic methods for producing combinatorial libraries of modulators of LXRs. The combinatorial libraries thus produced are useful both as diagnostic indicators of LXR&agr; function and as pharmacologically active agents. The combinatorial libraries find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.
    Type: Grant
    Filed: April 4, 2001
    Date of Patent: January 6, 2004
    Assignees: Tularik, Inc., Sumitomo Pharmaceuticals Co., Ltd.
    Inventors: Julio Medina, Naonori Imazaki
  • Patent number: 6667314
    Abstract: The present invention provides compounds of the formula: wherein R1 is C3-6 cycloalkyl optionally substituted by one or more fluorine atoms, or C1-6 alkyl optionally substituted by one or more fluorine atoms, or C3-6 cycloalkylmethyl optionally ring-substituted by one or more fluorine atoms; and R2 is phenyl optionally substituted by one or more fluorine atoms, to pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such compounds.
    Type: Grant
    Filed: May 25, 2001
    Date of Patent: December 23, 2003
    Assignee: Pfizer, Inc.
    Inventors: Manoussos Perros, David Anthony Price, Blanda Luzia Christa Stammen, Anthony Wood
  • Publication number: 20030220497
    Abstract: O-medium alkyl esters of diflunisal and related compounds are disclosed having anti-platelet activity, hydroxy radical scavenging properties, enhanced hepatic clearance and low ulcerogenic potential. These compounds have general formula (I) wherein n equals 3-13.
    Type: Application
    Filed: December 27, 2002
    Publication date: November 27, 2003
    Applicant: The University of Queensland
    Inventors: Daniel Yung-Yu Hung, Michael Stephen Roberts
  • Publication number: 20030220350
    Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.
    Type: Application
    Filed: August 30, 2002
    Publication date: November 27, 2003
    Inventors: Jesper Lau, Peter Madsen, Christian Sams, Carsten Behrens, Josef Vagner, Inge Thoger Christensen, Behrend Frederik Lundt, Ulla Grove Sidelmann, Henning Thogersen, Anthony L. Ling, Michael Bruno Plewe, Larry Kenneth Truesdale, Anker Steen Jogensen, Janos Tibor Kodra, Shenghua Shi
  • Publication number: 20030216466
    Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of GABA analogs following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.
    Type: Application
    Filed: May 13, 2003
    Publication date: November 20, 2003
    Inventors: Randall A. Scheuerman, Mark A. Gallop, Kenneth C. Cundy, Ronald W. Barrett
  • Patent number: 6649784
    Abstract: Aspartyl dipeptide ester derivatives, such as a N-[N-[3-(3,4-dihydroxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester, or salts thereof, having a high degree of sweetness compared to conventional sweeteners. These derivatives are excellent in sweetening potency and may be used as sweetener components in products such as foods and drinks. They may also be used as low calorie sweeteners and in methods of sweetening products. Foods and drinks comprising these derivatives as well as methods for their production.
    Type: Grant
    Filed: April 1, 2002
    Date of Patent: November 18, 2003
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yusuke Amino, Tadashi Takemoto, Kazuko Yuzawa, Ryoichiro Nakamura
  • Publication number: 20030203902
    Abstract: This invention describes the new, nonsteroidal gestagens of general formula I 1
    Type: Application
    Filed: February 5, 2003
    Publication date: October 30, 2003
    Applicant: SCHERING AKTIENGESELLSCHAFT
    Inventors: Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
  • Publication number: 20030203898
    Abstract: The invention relates to novel diphenylmethane derivatives, processes for their preparation and their use in medicaments, in particular for the indications of arteriosclerosis and hypercholesterolaemia.
    Type: Application
    Filed: March 11, 2003
    Publication date: October 30, 2003
    Inventors: Helmut Haning, Gunter Schmidt, Josef Pernerstorfer, Hilmar Bischoff, Carsten Schmeck, Verena Vohringen, Michael Woltering, Axel Kretschmer, Christiane Faeste
  • Patent number: 6639094
    Abstract: A process for producing &agr;-amino-dihalogenated methyl ketone derivatives by reacting an N-protected &agr;-amino acid ester with a dihalomethyl lithium is provided. This process is suitable for the production on an industrial scale and by this process, &agr;-amino-dihalogenated methyl ketone derivatives and &bgr;-amino-&agr;-hydroxycarboxylic acid derivatives can be obtained efficiently and economically advantageously.
    Type: Grant
    Filed: September 12, 1999
    Date of Patent: October 28, 2003
    Assignee: Ajinomoto Co., Inc.
    Inventors: Tomoyuki Onishi, Takashi Nakano, Naoko Hirose, Takayoshi Torii, Masakazu Nakazawa, Kunisuke Izawa
  • Publication number: 20030198607
    Abstract: Compounds of Formula I 1
    Type: Application
    Filed: April 10, 2002
    Publication date: October 23, 2003
    Applicant: EM Industries
    Inventor: Ratan K. Chaudhuri
  • Publication number: 20030191118
    Abstract: The present invention relates to a pharmaceutical composition comprising as an active ingredient a compound of formula (I), wherein Ring A is an aromatic or a heterocyclic ring; Q is a bond, carbonyl, lower alkylene, lower alkenylene, —O— -(lower alkylene)-, etc.; n is 0, 1 or 2; Z is oxygen or sulfur; W is oxygen, sulfur, —CH═CH—, —NH— or —N═CH—; R1, R2 and R3 are the same or different and are hydrogen, halogen, hydroxyl, a substituted or unsubstituted lower alkyl gorup, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, etc.; R4 is tetrazolyl, carboxyl group, amide or ester; R5 is hydrogen, nitro, amino, hydroxyl, lower alkanoyl, lower alkyl, etc.; R6 is selected from (a) a substituted or unsubstituted phenyl group, (b) a substituted or unsubstituted pyridyl group, (c) a substituted or unsubstituted thienyl group, (d) a substituted or unsubstituted benzofuranyl group, etc.
    Type: Application
    Filed: November 4, 2002
    Publication date: October 9, 2003
    Applicant: Tanabe Seiyaku Co., Ltd.
    Inventors: Ila Sircar, Kristjan S. Gudmundsson, Richard Martin
  • Patent number: 6620813
    Abstract: In accordance with the present invention, there are provided novel chemical entities which have multiple utilities, e.g., as prodrugs of NSAIDs; as dual inhibitors of cyclooxygenase (COX) and 5-lipoxygenase (5-LO); as anticancer agents (through promoting apoptosis and/or inhibiting the matrix metalloproteinases (MMPs)), and the like. Invention compounds comprise a non-steroidal anti-inflammatory agent (NSAID), covalently linked to a hydroxamate. Invention compounds are useful for a variety of applications, such as, for example, treating inflammation and inflammation-related conditions; reducing the side effects associated with administration of anti-inflammatory agents; promoting apoptosis; inhibiting matrix metalloproteinases; and the like.
    Type: Grant
    Filed: June 21, 2002
    Date of Patent: September 16, 2003
    Assignee: Medinox, Inc.
    Inventors: Tingmin Wang, Ching-San Lai
  • Publication number: 20030162991
    Abstract: The present invention is to provide a purification method of obtaining N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine of high quality in good yield with high productivity, which is accordingly suited for commercial scale application.
    Type: Application
    Filed: April 8, 2003
    Publication date: August 28, 2003
    Inventors: Akira Matsumoto, Michio Nomura, Yoshikazu Kogame, Yasuyoshi Ueda
  • Patent number: 6610855
    Abstract: A process for the synthesis of a compound of the formula wherein R1 is aryl, heteroaryl, substituted aryl or substituted heteroaryl and R2 is hydrogen, alkyl or aralkyl, or salt thereof.
    Type: Grant
    Filed: July 15, 2002
    Date of Patent: August 26, 2003
    Assignee: McNeil Pharmaceutical, Inc.
    Inventors: Ahmed F. Abdel-Magid, Judith H. Cohen, Cynthia A. Maryanoff, Frank John Villani, Jr., Hua M. Zhong
  • Patent number: RE38796
    Abstract: Compounds formed by reacting a protected amino acid with an alkali metal enolate of an alkyl acetate are reacted with a halogenating agent for halogenation of the 2-position, or a protected amino acid is reacted with an alkali metal enolate of an alkyl halogenoacetate, to form a 4-amino-3-oxo-2-halogenobutanoic acid ester derivative, and hydrolysis and decarboxylation are conducted to produce a 3-amino-2-oxo-1-halogenopropane derivative or its salt. The present method is a useful process for producing a 3-amino-2-oxo-1-halogenopropane derivatives which can easily be converted to a 3-amino-1,2-epoxypropane.
    Type: Grant
    Filed: June 16, 2000
    Date of Patent: September 13, 2005
    Assignee: Ajinomoto Co.,Inc.
    Inventors: Yutaka Honda, Satoshi Katayama, Kunisuke Izawa, Masakazu Nakazawa, Takayuki Suzuki, Naoko Kanno