Patents Examined by Floyd D. Higel
  • Kappa agonist compounds and pharmaceutical formulations thereof
    Patent number: 6391910
    Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formulae I, II, IIA, III, IIIA, IV and IVA have the structure: wherein R1, R2, R3, R4; and X, X4, X5, X7, X9; Y, Z and n are as described in the specification.
    Type: Grant
    Filed: January 6, 2000
    Date of Patent: May 21, 2002
    Assignee: Adolor Corporation
    Inventors: Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, An-Chih Chang, Deqi Guo
  • Method for the production of n,n?-carbonyldiazoles
    Patent number: 6392057
    Abstract: The invention relates to a process for the preparation of N,N′-carbonyldiazoles by reacting azoles with phosgene in a solvent, whereby the azole and the phosgene are metered into an aromatic solvent dried by incipient distillation in such a way that in the time in which 1 mol of azole is metered in, from 0.17 to 0.34 mol of phosgene is metered in simultaneously.
    Type: Grant
    Filed: January 17, 2001
    Date of Patent: May 21, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Johannes Scherer, Alexander Klausener, Robert Söllner
  • Triazole derivatives having antifungal activity
    Patent number: 6392082
    Abstract: Compounds of the following formula (I) and pharmaceutically acceptable esters and salts thereof: Ar is phenyl group which may optionally be substituted by from 1 to 3 substituents selected from the group consisting of halogen atoms and trifluoromethyl groups. Said compounds (and pharmaceutically acceptable esters and salts thereof) have excellent antifungal activity.
    Type: Grant
    Filed: July 18, 2001
    Date of Patent: May 21, 2002
    Assignee: Sankyo Company, Limited
    Inventors: Toshiyuki Konosu, Sadao Oida, Makoto Mori, Takuya Uchida
  • Sulfonamide inhibitors of aspartyl protease
    Patent number: 6392046
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: September 30, 1999
    Date of Patent: May 21, 2002
    Assignee: Vertex Pharmaceuticals, Inc.
    Inventors: Roger D. Tung, Mark A. Murcko, Govinda Rao Bhisetti
  • Hydronaphtho[2,3-c]furan derivatives and process for the preparation thereof
    Patent number: 6392059
    Abstract: Intermediates for the preparation of himbacine exhibiting muscarinic M2 receptor antagonism, which are hydronaphtho[2,3-c]furan derivatives represented by general formula (1) or intermediates for the preparation thereof: wherein R1 is lower alkyl or aralky; R2 is hydrogen, lower alkyl or aralkyl; R3 and R4 together represent oxygen or methylene, or alternatively R4 is hydroxyl, lower alkoxy, aralkyloxy or lower acyloxy, with R3 being hydrogen; R5 and R6 together represent oxygen, or alternatively R6 is hydroxyl, lower alkxy, aralkyloxy or lower acyloxy, with R5 being hydrogen; and either of the broken lines is a single bond and the other thereof is a double bond, or alternatively both are single bonds.
    Type: Grant
    Filed: June 7, 2001
    Date of Patent: May 21, 2002
    Assignees: Sagami Chemical Reasearch Center, Kyorin Pharmaceutical Co., Ltd.
    Inventors: Shiro Terashima, Masanori Takadoi, Akihiro Ishiwata, Tadashi Katoh
  • Pyrrolic compounds having a high herbicidal activity and their agronomic use
    Patent number: 6391827
    Abstract: The invention relates to pyrrolic compounds having formula The compounds having formula (I) have a high herbicidal activity and are used for controlling weeds in the agronomic field
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: May 21, 2002
    Assignee: Isagro Ricerca S.r.l.
    Inventors: Giovanni Meazza, Franco Bettarini, Paolo Castoro, Piero La Porta, Ernesto Signorini, Domenico Portoso
  • Cyclopentene compounds useful as antagonists of the motilin receptor
    Patent number: 6392040
    Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.
    Type: Grant
    Filed: March 9, 2001
    Date of Patent: May 21, 2002
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Robert H. Chen, Min A. Xiang
  • Intermediates for the preparation of N-[2-(carboxymethoxy) ethyl]-N-(carboxymethyl) glycine
    Patent number: 6392095
    Abstract: Compounds represented by the formula wherein R and R1 independently represent H, —CH2CN or —CH2CO2X, with the proviso that R and R1 can not be both H or —CH2CO2X; and X represents hydrogen, an alkali metal or alkaline earth metal are disclosed. These compounds are useful as intermediate compounds in the preparation of N-[2-(carboxymethoxy)ethyl]-N-(carboxy-methyl)glycine. These intermediates can be formed by contacting 3-morpholinone with glycolonitrile under alkaline conditions to form an aminonitrile which can be hydrolyzed and contacted with additional glycolonitrile to form the nitrile intermediate which can be converted to N-[2-(carboxymethoxy)ethyl]-N-(carboxymethyl)glycine via hydrolysis.
    Type: Grant
    Filed: March 30, 2001
    Date of Patent: May 21, 2002
    Assignee: The Dow Chemical Company
    Inventors: Phillip S. Athey, David A. Wilson
  • Process for producing salts of cyanobenzylamines
    Patent number: 6392083
    Abstract: A process for producing a salt of a cyanobenzylamine comprising reacting a cyanobenzylamine with an acid. A salt of a cyanobenzylamine can industrially easily be produced and the resulting salt of a cyanobenzylamine has a high bulk density.
    Type: Grant
    Filed: June 7, 2001
    Date of Patent: May 21, 2002
    Assignee: Showa Denko K.K.
    Inventors: Isao Yamagami, Hiroshi Yasuda, Masatoshi Murakami, Toru Yoshida
  • Protein tyrosine phosphatase-inhibiting compounds
    Patent number: 6388076
    Abstract: Y—X—C(R′)═C(R″)COOR′″  (A1) The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryoic cells, whole animals and human beings. R′ and R″ are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl.
    Type: Grant
    Filed: August 24, 2000
    Date of Patent: May 14, 2002
    Assignee: Ontogen Corporation
    Inventors: Adnan Mjalli, Sepehr Sarshar, Xiaodong Cao, Farid Bakir
  • Preparation method of arbutin intermediates
    Patent number: 6388103
    Abstract: The invention is related to a preparation method of arbutin intermediate (chemical formula I). It is characterized by the glycosylation of hydroquinone or mono-protectected hydroquinone (chemical formula II) with pentaacetyl-&bgr;-D-glucose (chemical formula III) in the presence of Lewis acid and base as catalysts. where Ac is acetyl group, R is hydrogen, alkyl or cycloalkyl group with 1 to 10 carbon, or aliphatic or aromatic acyl group with 1 to 10 carbon.
    Type: Grant
    Filed: April 20, 2001
    Date of Patent: May 14, 2002
    Assignees: Korea Research Institute of Chemical Technology, Biolano Co., Ltd.
    Inventors: Yeon Soo Lee, Bum Tae Kim, Yong Ki Min, No Kyun Park, Ki Ho Kim, Jae Seob Lee, See Wha Jeoung, Ki Soo Kim
  • 2,4,4-trisubstituted-1,3-dioxolane antifungals
    Patent number: 6387906
    Abstract: The present invention concerns novel compounds of formula a N-oxide form, a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, wherein n is zero, 1, 2 or 3; X is N or CH; each R1 independently is halo, nitro, cyano, amino, hydroxy, C1-4alkyl, C1-4alkyloxy or trifluoromethyl; R2 is hydrogen; C3-7alkenyl; C3-7alkynyl, aryl; C3-7cycloalkyl; optionally substituted C1-6alkyl R3 and R4 each independently are hydrogen, C1-6alkyl, C3-7cycloalkyl or aryl; or R3 and R4 taken together form a bivalent radical —R3—R4— of formula: wherein R5a, R5b, R5c, R5d each independently are hydrogen, C1-6alkyl or aryl; and aryl is optionally substituted phenyl; as antifungals; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: January 7, 2000
    Date of Patent: May 14, 2002
    Inventors: Lieven Meerpoel, Jan Heeres, Frank Christopher Odds, Hugo Florent Adolf Vanden Bossche, Louis Jozef Elisabeth Van der Veken
  • Vancoresmycin, a process for its production and its use as a pharmaceutical
    Patent number: 6387943
    Abstract: The present invention relates to a compound named Vancoresmycin which is obtainable by cultivation of the microorganism HIL-006734 (DSM 12216), and to its pharmaceutically acceptable salts. The present invention further relates to a process for the production of Vancoresmycin, to the microorganism HIL-006734 (DSM 12216), to the use of Vancoresmycin and its pharmaceutically acceptable salts as pharmaceuticals, and in particular to their use as antibiotics, and to pharmaceutical compositions comprising Vancoresmycin or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 9, 1999
    Date of Patent: May 14, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Nirogi Venkata Satya Ramakrishna, Ravi Gajanan Bhat, Eyyammadichiyil Sankaranarayanan Sreekumar, Erra Koteswara Satya Vijayakumar, Shantilal Dayaram Naker, Uttara Vinayak Oak, Rajendra Prakash Tanpure, Cordula Hopmann, Michael Kurz, Joachim Wink, Gerhard Seibert, Dominique Le Beller, Jozsef Aszodi
  • Process for the preparation of 1,2,3,9-tetrahydro-9-methyl-3-{(2-methyl-1H-imidazol-1-yl)methyl}-4H-carbazol-4-one
    Patent number: 6388091
    Abstract: Pure -1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carbazol-4-one or a pharmaceutically acceptable salt thereof is prepared in a high yield by a simple process which reacts 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one with a 2-methylimidazole derivative in an organic solvent or in a mixture of an organic solvent and water in the presence of a halosilane compound.
    Type: Grant
    Filed: November 20, 2001
    Date of Patent: May 14, 2002
    Assignee: Hanmi Pharm. Co., Ltd.
    Inventors: Kwang-Ok Lee, Hee-Seock Kim, Young-Jin Ham, Maeng-Sup Kim, Han-Kyeng Kim, Cheol-Kyeung Kim, Kum-Sin Jung, Hoe-Chul Lee, Ki-Eun Kim, Gwan-Sun Lee
  • Tetrazolyl-phenyl acetamide glucokinase activators
    Patent number: 6388088
    Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: May 14, 2002
    Assignee: Hoffman-La Roche Inc.
    Inventor: Achyutharao Sidduri
  • Indole-containing quaternary ammonium compounds
    Patent number: 6388095
    Abstract: Compounds and pharmaceutical compositions containing such compounds and possessing anti-tussive activity, and a method of administering the same to warm-blooded animals, including humans.
    Type: Grant
    Filed: June 9, 1999
    Date of Patent: May 14, 2002
    Assignee: Cardiome Pharma Corp.
    Inventors: Gregory N. Beatch, Lewis S. L. Choi, Clive P. Page, Bertrand M. C. Plouvier, Yuzhong Liu
  • Methods of providing and using compounds having activity as inhibitors of cytochrome P450RAI
    Patent number: 6387892
    Abstract: Novel compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification, and certain previously known compounds have been discovered to act as inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids. The compound can also be used in co-treatment with retinoids.
    Type: Grant
    Filed: June 7, 2001
    Date of Patent: May 14, 2002
    Assignee: Allergan Sales, Inc.
    Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
  • Epothilone derivatives and their use as antitumor agents
    Patent number: 6387927
    Abstract: The invention relates to anti-tumour-effective compounds of formula (I), wherein the radicals have the meanings given in the description.
    Type: Grant
    Filed: June 1, 2001
    Date of Patent: May 14, 2002
    Assignee: Novatis AG
    Inventors: Karl-Heinz Altmann, Guido Bold, Giorgio Caravatti, Andreas Flörsheimer
  • Method for producing monohalogenated 2-oxo-1,3-dioxolanes
    Patent number: 6384239
    Abstract: The invention relates to a process for the preparation of monohalogenated 2-oxo-1,3-dioxolanes of the general formula C3H3XO3  (I) in which X is Cl or Br, characterized in that the monohalogenation is carried out starting from ethylene carbonate with sulfuryl dihalides under UV irradiation and in the absence of solvents.
    Type: Grant
    Filed: May 3, 2001
    Date of Patent: May 7, 2002
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Bernhard Seifert, Sylvia Becker
  • Meadowfoam based sorbitan esters
    Patent number: 6384248
    Abstract: The present invention deals with novel emulsifiers. The compounds are esters made by the reaction of sorbitol and meadowfoam acids. The introduction of the unsaturated highly stable meadowfoam acid portion of the molecule into the compounds of the present invention results in improved emulsification efficiency, improved oxidative stability and improved liquidity of the esters.
    Type: Grant
    Filed: August 17, 2000
    Date of Patent: May 7, 2002
    Assignee: Fan Tech LTD
    Inventor: Anthony J. O'Lenick, Jr.