Patents Examined by Robert T. Bond
  • Patent number: 5919926
    Abstract: Salinamides A and B are disclosed. These two bicyclic depsipeptides are produced by fermentation of a specific marine actinomycete, a Streptomyces sp, (CNB-091) in saltwater-based media. Salinamides A and B are useful as anti-biotic and anti-inflammatory agents.
    Type: Grant
    Filed: January 25, 1994
    Date of Patent: July 6, 1999
    Assignee: The Regents of the University of California
    Inventors: William H. Fenical, Robert S. Jacobs, Paul R. Jensen
  • Patent number: 5917033
    Abstract: The present invention pertains to a method for designing inhibitors of enzyme human immunodeficiency virus type 1 reverse transcriptase which comprises the steps of:(a) providing a three dimensional model of the receptor site in the prepolymerization complex of the p66 subunit of enzyme human immunodeficiency virus type 1 reverse transcriptase and a known nonnucleoside inhibitor;(b) locating the conserved residues in the p66 subunit which constitute the nonnucleoside inhibitor binding pocket; and(c) designing a new nonnucleoside inhibitor which possesses complementary structural features and binding forces to the residues in the p66 subunit nonnucleoside inhibitor binding pocket.
    Type: Grant
    Filed: October 31, 1995
    Date of Patent: June 29, 1999
    Assignee: University of Medicine & Dentistry of New Jersey
    Inventors: Mukund J. Modak, Prem N. S. Yadav, Janardan S. Yadav
  • Patent number: 5843941
    Abstract: Benzodiazepine derivatives represented by the structure below are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases foe which inhibition of the ras farnesyl:protein transferase as indicated.
    Type: Grant
    Filed: September 26, 1994
    Date of Patent: December 1, 1998
    Assignees: Genentech, Inc., Board of Regents University of Texas
    Inventors: James C. Marsters, Jr., Michael S. Brown, Craig W. Crowley, Joseph L. Goldstein, Guy L. James, Robert S. McDowell, David Oare, Thomas E. Rawson, Mark Reynolds, Todd C. Somers
  • Patent number: 5831094
    Abstract: The present invention relates to difluorostatone derivatives useful as antiviral agents.
    Type: Grant
    Filed: February 20, 1996
    Date of Patent: November 3, 1998
    Assignee: Merrell Pharamceuticals Inc.
    Inventors: Viviane Van Dorsselaer, Daniel Schirlin, Celine Tarnus
  • Patent number: 5801168
    Abstract: Antagonists at the NMDA receptor complex which are benz?b!azepines having a hydroxy, alkoxy or amino substituent at the 3-position and a 4-position alkenyl, alkynyl, aryl or heteroaryl substituent for treatment of stroke and/or other neurodegenerative disorders.
    Type: Grant
    Filed: February 3, 1997
    Date of Patent: September 1, 1998
    Assignee: Zeneca Limited
    Inventors: Marc Jerome Chapdelaine, Timothy W. Davenport, Laura E. Garcia-Davenport, Paul Francis Jackson, Jeffrey A. McKinney, Charles D. McLaren
  • Patent number: 5798381
    Abstract: Bistramide derivatives with virtually no toxic effects, of formula (I) wherein --R.sub.1, X, Y and R.sub.2 are a saturated or unsaturated hydrocarbonaceous chain having from 1 to 20 carbon atoms, substituted by at least one --OH group and/or a ketone function, including, if need be, at least one ring (a), the ring including one more unsaturations; --R.sub.3, R.sub.4 and R.sub.5 are the same or different and are selected from hydrogen, alkyl or alkoxy radicals having from 1 to 4 carbon atoms, a group --COOH, --OH, --NH or --NO.sub.2, or a halogen atom. The invention also concern bistramide derivatives of formula (I) such as ethers or esters and their isomers, excluding A, B and C bistramides. Said bistramides are useful especially as drugs having a cytostatic effect, in particular as antitumour or anti-parasitic drugs.
    Type: Grant
    Filed: March 4, 1996
    Date of Patent: August 25, 1998
    Assignee: Institut Francais de Recherche Scientifique pour le Development en Cooperation (Orstom)
    Inventors: Jean-Francois Biard, Dominique Cortadellas, Cecile Debitus, Dominique Laurent, Cristos Roussakis, Jean-Francois Verbist
  • Patent number: 5789587
    Abstract: There are disclosed certain novel compounds identified as heterocyclic-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such heterocyclic-fused lactams as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: November 6, 1996
    Date of Patent: August 4, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Michael H. Fisher, Helmut Mrozik, William R. Schoen, Thomas L. Shih, Matthew J. Wyvratt
  • Patent number: 5786350
    Abstract: Rifamycin antibiotic derivatives of formulae (I) and (Ia) bearing at the position 36 a substituent selected from (C.sub.1 -C.sub.8)alkyl, halo, hydroxy, (C.sub.1 -C.sub.4)acyloxy, (C.sub.1-C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkylamino, di(C.sub.1-C.sub.4)alkylamino and substituted 4-oxo-3-pyridinyl carbonyloxy of formula (1) obtained by reacting rifamycin with suitably substituted malonic acid. The compounds of the invention are antimicrobial agents mainly active against gram positive bacteria and fastidious gram negative bacteria showing the considerable antimicrobial activity against the rifamypicin resistant microbial strains.
    Type: Grant
    Filed: January 31, 1997
    Date of Patent: July 28, 1998
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Emilio Occelli, Sergio Lociuro, Romeo Ciabatti, Maurizio Denaro
  • Patent number: 5780623
    Abstract: Process to prepare .epsilon.-caprolactam starting from a liquid aqueous mixture containing an alcohol and 6-aminocaproic acid by cyclization of 6-aminocaproic acid in the aqueous mixture at an elevated temperature. The alcohol is separated from the starting aqueous mixture before performing the cyclization to such extent that the concentration of alcohol in the aqueous mixture during the cyclization is less than 1 wt. %. The advantages include reduced amounts of undesirable by-product.
    Type: Grant
    Filed: February 23, 1996
    Date of Patent: July 14, 1998
    Assignee: DSM N.V.
    Inventors: Rudolf P.M. Guit, Samuel L. Lane, Wim Buijs
  • Patent number: 5776929
    Abstract: A benzodiazepine derivative of the formula (I): ##STR1## wherein R.sub.1 is a bond, --CH.sub.2 --, --CH.sub.2 O--, --SCH.sub.2 -- or a group of the formula: ##STR2## R.sub.2 is a lower alkyl, --COOR.sub.5, --CONH(CH.sub.2).sub.n COOR.sub.5, --CONHSO.sub.2 R.sub.5, --SO.sub.2 NHCOR.sub.5, or an optionally substituted heterocyclic group (R.sub.5 is a hydrogen atom, lower alkyl or benzyl and n is an integer of 1 to 5); R.sub.3 is a bond, --CO-- or --CONH--; and R.sub.4 is an optionally substituted heterocyclic group, optionally substituted lower alkyl, optionally substituted lower cycloalkyl, optionally substituted aryl, or lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof, which has a high affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors, and is useful for treating diseases associated with gastrin receptors and/or CCK-B receptors without inducing the side effects associated with CCK-A receptors.
    Type: Grant
    Filed: June 25, 1996
    Date of Patent: July 7, 1998
    Assignee: Shionogi & Co., Ltd.
    Inventors: Sanji Hagishita, Susumu Kamata, Kaoru Seno, Nobuhiro Haga, Yasunobu Ishihara
  • Patent number: 5777105
    Abstract: Imidazolmethyloxy-substituted tricyclo-macrolide immunosuppressants are prepared by reacting a tricyclo-macrolide with an imidazolmethyl trichloroacetimidate in the presence of an acid. The invention further provides a crystalline salt of imidazolmethyloxy-substituted tricyclo-macrolide, as well as novel compounds useful in the process of the present invention.
    Type: Grant
    Filed: July 23, 1996
    Date of Patent: July 7, 1998
    Assignee: Merck & Co., Inc.
    Inventors: David J. Mathre, Richard F. Shuman, Paul Sohar, Zhiguo Song
  • Patent number: 5776936
    Abstract: There are disclosed 18-thiomarcfortine derivatives of the natural products marcfortine A, B and C, C-18 thioparaherquamide and derivatives thereof, novel N-1 marcfortines A, B, and C and derivatives thereof, novel N-1 paraherquamide and derivatives thereof usefull in the treatment and prevention of helninth and arthropod infections of animals and plants.Any inquiry concerning this communication or earlier communications from the examiner should be directed to Examiner Robert T. Bond whose telephone number is (703)308-4711. The examiner can normally be reached on Monday through Friday from 8:00 AM to 4:30 PM.
    Type: Grant
    Filed: May 19, 1994
    Date of Patent: July 7, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventors: Byung H. Lee, Stephen J. Nelson
  • Patent number: 5773428
    Abstract: Compounds of formula (I): ##STR1## as single stereoisomers or mixtures thereof and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as interstitial collagenases, and are useful in the treatment of mammals having disease states alleviated by the inhibition of such matrix metalloproteases, for example arthritic diseases or bone resorption diseases, such as osteoporosis.
    Type: Grant
    Filed: February 5, 1996
    Date of Patent: June 30, 1998
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Arlindo Lucas Castelhano, Teng Jiam Liak, Stephen Horne, Alexander Krantz, Zhengyu Yuan, Jian Jeffrey Chen, Paul David Cannon, Hal Van Wart
  • Patent number: 5770604
    Abstract: This invention provides novel aconitine compounds of the formula (I) or salt thereof ##STR1## wherein, R.sub.1 is a hydrogen atom or hydroxyl group; R.sub.2 is an acetyloxy group; R.sub.3 is an alkyl having 1-4 carbon atoms; and R.sub.4 is a hydrogen atom, a hydroxyl group, or an acetyloxy group; and antipyretic/analgesic/anti-inflammatory agents containing the compound as an active ingredient which are highly safe and exhibit a powerful analgsic effect and antipyretic/anti-inflammatory activities. The compound is usable alone in painful, pyretic and inflammatory illnesses but its concomitant use with morphine reinforces the analgesic effect of morphine and allows alleviation of morphine side effects through reduction in morphine dosage.
    Type: Grant
    Filed: October 6, 1995
    Date of Patent: June 23, 1998
    Assignee: Sanwa Shoyaku Kabushiki Kaisha
    Inventor: Mitsuo Murayama
  • Patent number: 5756728
    Abstract: An improved process for preparing 1,1'-?1,4-phenylenebis-(methylene)!-bis-1,4,8,11-tetraazacyclotetradecane comprising the selective functionalization of an acyclic tetraamine, and subsequent dimerization and hydrolyzation/tosylation to obtain a 1,4-phenylenebis-methylene bridged hexatosyl acyclic precursor in a first step, the cyclization of said precursor to obtain a hexatosyl cyclam dimer in a second step, and the detosylation of said cyclam dimer in a third step followed by basification to obtain the desired 1,1'-?1,4-phenylenebis-(methylene)!-bis-1,4,8,11-tetraazacyclotetradecane.
    Type: Grant
    Filed: December 30, 1996
    Date of Patent: May 26, 1998
    Assignee: Johnson Matthey Public Limited Company
    Inventors: David Xu, Prasad Kapa, Oljan Repic, Thomas J. Blacklock
  • Patent number: 5753677
    Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## which have excellent vasopressin antagonistic activities and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 19, 1998
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Hajime Komatsu, Michinori Tanaka, Shinya Kora, Michiaki Tominaga, Yoichi Yabuuchi
  • Patent number: 5750680
    Abstract: N-vinyllactam derivatives protected at the 3-position are provided and represented by the following formula (I). These are polymerized into homo- and copolymers for use in microlithography of semiconductor manufacture. The polymers are used as a photoresist material suitable for a deep UV process so that pictures of high sensitivity and high resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in pattern formation can be accomplished through the use of the photoresist of the invention.
    Type: Grant
    Filed: September 12, 1996
    Date of Patent: May 12, 1998
    Assignees: Hyundai Electronics Industries Co., Ltd., Korea Advanced Institute of Science & Technology
    Inventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
  • Patent number: 5750725
    Abstract: The present invention provides a class of compounds having the formula:Y--R--CH.sub.2 --CH.sub.2 --?O--CH.sub.2 --CH.sub.2 !.sub.n --R'--Y'wherein n is an integer from about 5 to about 200; R is carbamate, urea, or amide; R' is carbamate, urea, amide, or oxygen; Y is 4-phenylmalemimido or 3-phenylmaleimido; and Y' is 4-phenylmalemimido, 3-phenylmaleimido, methyl or hydrogen. The present invention also provides various hemoglobin compositions modified with the class of compounds of the present invention, processes for preparing these compositions, as well as pharmaceutical compositions comprising these compositions.
    Type: Grant
    Filed: September 26, 1996
    Date of Patent: May 12, 1998
    Assignee: Albert Einstein College of Medicine of Yeshiva University, a Division of Yeshiva
    Inventors: A. Seetharama Acharya, Belur N. Manjula, Paul K. Smith
  • Patent number: 5750700
    Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof;useful for treating disorders of the central nervous system.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: May 12, 1998
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Jan W. F. Wasley
  • Patent number: 5741904
    Abstract: A method of producing .epsilon.-caprolactam from cyclohexanone in the gaseous phase using MFI catalysts on whose surface symmetrically arranged OH groups are present.
    Type: Grant
    Filed: May 6, 1996
    Date of Patent: April 21, 1998
    Assignee: Degussa Aktiengesellschaft
    Inventors: Wolfgang Hoelderich, Joerg Roeseller, Dietrich Arntz