Patents Examined by Lester L. Lee
  • Patent number: 5061693
    Abstract: A fibrinogen receptor antagonist compound of the structure:A--B--C--Gly--Asp--D--E (I)wherein A, B, C, D and E are preferably defined as follows:A is L-asparagine, D-asparagine or acylated asparagineB is an L-or D-isomer of proline, thioproline, .beta.,.beta.-dimethylthioproline, or N-methylalanine;C is arginine;D is phenylalanine, tryptophan .alpha.-naphthylalanine, .beta.-napthlalanine, arginine or lysine; andE is OH.
    Type: Grant
    Filed: July 28, 1989
    Date of Patent: October 29, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Ruth F. Nutt, Stephen F. Brady, Daniel F. Veber
  • Patent number: 5061627
    Abstract: A process for isolating valuable bioactive substances such as the enzymes alkaline phosphates, hyaluronidase and chitinase from crustacea, mainly shrimp, by extracting said enzymes with a water soluble eluant and to treat the extracted brine in the following process steps; purifying by centrifugation or filtration, purification, extraction and removal of unwanted substances and isolation of the valuable substances.
    Type: Grant
    Filed: October 11, 1989
    Date of Patent: October 29, 1991
    Assignee: Norsk Hydro A.S.
    Inventors: Ragnar L. Olsen, Even Stenberg, Erling Sandsdalen, Karl A. Almas
  • Patent number: 5059588
    Abstract: A method of promoting and accelerating the healing of bones in animals utilizing an effective amount of a GHL-(Cu) pharmicuetical composition is disclosed. Also methods of inducing the formulation of granulation tissue in affected bones of animals using a GHL-(Cu) composition is disclosed.
    Type: Grant
    Filed: October 13, 1989
    Date of Patent: October 22, 1991
    Assignee: ProCyte Corporation, Incorporated
    Inventor: Loren R. Pickart
  • Patent number: 5057496
    Abstract: There are described new compounds of formula (1) ##STR1## wherein R.sup.1 represents an acyl group;X.sup.1 represents phenylalanine or p-methoxyphenylalanine bonded N-terminally to R.sup.1 and C-terminally to X.sup.2 ;X.sup.2 represents histidine or N-methylhistidine bonded N-terminally to X.sup.1 and C-terminally to the group --NH--;R.sup.2 represents a C.sub.4-6 cycloalkyl group;R.sup.3 represents a group CHR.sup.6 R.sup.7 (where R.sup.6 is a hydrogen atom or a hydroxyl group and R.sup.7 is a pyridinyl ring);X.sup.3 represents a C.sub.2-6 alkylene chain optionally substituted by one or more C.sub.1-4 alkyl groups;R.sup.4, and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a C.sub.1-4 alkyl group, or NR.sup.4 R.sup.5 may form a 5- or 6- membered polymethylenimine ring;and salts and solvates thereof.The new compounds have been found to exhibit activity as renin inhibitors, combining good duration of action with significant oral potency.
    Type: Grant
    Filed: December 6, 1988
    Date of Patent: October 15, 1991
    Assignee: Glaxo Group Limited
    Inventors: Peter C. Cherry, Michael W. Foxton, Barry E. Ayres, Andrew D. Searle
  • Patent number: 5057312
    Abstract: This nitrocellulose-free varnish contains at least one resin in a solvent system for varnishes, and is characterized in that the said resin is a copolymer containing units resulting from the copolymerization:(1) of 20 to 70% of at least one alkyl acrylate or methacrylate of general formula: ##STR1## in which: R' denotes a hydrogen atom or a methyl radical, andR denotes a saturated, linear or branched hydrocarbon chain containing from 1 to 6 carbon atoms, and(2) of 30 to 80% of at least one hydroxyalkyl acrylate or methacrylate of general formula: ##STR2## in which: R.sub.1 denotes a hydrogen atom or a methyl radical and R.sub.2 denotes a linear or branched hydrocarbon chain containing from 2 to 4 carbon atoms and 1 or 2 hydroxyl(s), it being understood that the said copolymer cannot contain more than 30% of units derived from the copolymerization of an alkyl acrylate and/or a hydroxyalkyl acrylate, the viscosity of the copolymer at a concentration of 28% in ethyl acetate at 25.degree. C. being higher than 0.
    Type: Grant
    Filed: June 17, 1988
    Date of Patent: October 15, 1991
    Assignee: L'Oreal
    Inventors: Bernard Langla, Jean Mondet, Christos Papantoniou
  • Patent number: 5055450
    Abstract: The invention concerns pharmaceutically useful trifluoromethyl ketone substituted di-, tri- and tetra-peptide derivatives of the formulae Ia, Ib, Ic set out hereinafter, and salts thereof, which are inhibitors of human leukocyte elastase. Also described herein are pharmaceutical compositions containing a peptide derivative and processes and intermediates for use in the manufacture of the peptide derivatives.
    Type: Grant
    Filed: March 13, 1990
    Date of Patent: October 8, 1991
    Assignee: ICI Americas Inc.
    Inventors: Philip D. Edwards, John A. Schwartz, Mark M. Stein, Diane A. Trainor, Richard A. Wildonger
  • Patent number: 5055299
    Abstract: A mono-layer liquid phase type water-based insecticidal aerosol comprises (A) a base liquid for aerosol containing at least one specific pyrethroidal compound, a specific organic solvent and a buffer solution, which base liquid has a pH of from 7.0 to 9.0 and (B) dimethyl ether as a propellant. The aerosol according to the present invention has a long-term storage stability, as well as an excellent insecticidal activity and causes no degradiation of the container.
    Type: Grant
    Filed: December 8, 1988
    Date of Patent: October 8, 1991
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Kazunobu Dohara, Tadahiro Matsunaga, Motomitsu Shiraishi, Goro Shinjo
  • Patent number: 5055451
    Abstract: Thiol protease inhibitors are disclosed having the formula: ##STR1## or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, wherein:n is 0 or 1;m is 0, 1 or 2;X is H or an N-protecting group;each Y is independently an optionally protected .alpha.-amino acid residue;R is an optionally protected .alpha.-amino acid side chain that is H or CH.sub.3 or that is bonded to the .alpha.-carbon atom to which it is attached by a methylene, methine or phenyl radical; andR' is optionally substituted aryl.
    Type: Grant
    Filed: December 7, 1987
    Date of Patent: October 8, 1991
    Assignee: Syntex Inc.
    Inventors: Alexander Krantz, Heinz W. Pauls, Roger A. Smith, Robin W. Spencer
  • Patent number: 5055591
    Abstract: The invention relates to a process for the preparation of compounds of the formula I ##STR1## in which n is 1 or 2, R denotes hydrogen or an organic radical, R.sup.1 denotes an organic radical, R.sup.2 and R.sup.3 are identical or different and denote hydrogen or an organic radical, and R.sup.4 and R.sup.5, together with the atoms bearing them, form a monocyclic, bicyclic or tricyclic heterocyclic ring system having 3 to 15 carbon atoms, which process comprises reacting compounds of the formula II defined in the description with compounds of the formula III defined in the description, in the presence of alkanephosphonic anhydrides, where appropriate eliminating radicals which have been introduced to protect other functional groups and, where appropriate, esterifying free carboxyl groups in a manner known per se.
    Type: Grant
    Filed: March 23, 1988
    Date of Patent: October 8, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hansjorg Urbach, Rainer Henning, Hans Wissmann, Volker Teetz
  • Patent number: 5053520
    Abstract: Novel polyamino acid based coupling agents are disclosed. These reagents are useful for conjugating proteins (e.g. antibodies to enzymes) for use in diagnostic assays.
    Type: Grant
    Filed: October 1, 1989
    Date of Patent: October 1, 1991
    Assignee: Abbott Laboratories
    Inventors: Christopher Bieniarz, Christopher J. Welch, Grady Barnes
  • Patent number: 5053333
    Abstract: There is disclosed a protease having the following enzymatic properties in view of:(a) function and substrate specificity,(b) optimum pH,(f) activation, and(g) inhibition;(a) the protease can hydrolyze, in particular, a peptide bond on the C-terminal side of Y of a peptide X--Y--, in which X is Arg, Lys or Pro optionally having a peptide bond on the N-terminal side, Y is Arg and -- indicates a peptide bond;(b) the protease has an optimum pH of about 7.0 in Tris hydrochloride buffer;(f) the protease is activated with calcium chloride or a surfactant; and(g) the protease is inhibited with p-amidinophenylmethanesulfonyl fluoride, p-chloromercuribenzoic acid, a metal chelater, tetraacetic acid or a heavy metal.
    Type: Grant
    Filed: January 26, 1989
    Date of Patent: October 1, 1991
    Assignee: M & D Research Co., Ltd.
    Inventor: Hiroaki Yamamoto
  • Patent number: 5053392
    Abstract: Disclosed are novel amino acid derivatives of the formula: ##STR1## wherein X is H, amidino or ##STR2## Y is H, amino or ##STR3## Z is ##STR4## OR.sub.1 or a naturally occurring L-amino acid, bounded to the carbon atom at the .alpha.-amino position;R is alkyl, aryl or aralkyl;R.sub.1 and R.sub.2 are independently H, alkyl, aryl, aralkyl or allyl;m is 1 through 5;n is 0 through 4; andpharmaceutically acceptable salts thereof, that inhibit platelet aggregation and thrombus formation in mammalian blood.
    Type: Grant
    Filed: December 1, 1989
    Date of Patent: October 1, 1991
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Scott I. Klein, Bruce F. Molino
  • Patent number: 5051405
    Abstract: Disclosed are novel peptides and pseudopeptides and pharmaceutical compositions thereof containing certain amino acids and pharmaceutical compositions thereof that inhibit platelet aggregation and thrombus formation in mammalian blood.
    Type: Grant
    Filed: October 10, 1989
    Date of Patent: September 24, 1991
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Scott I. Klein, Bruce F. Molino, Mark Czekaj, Charles J. Gardner
  • Patent number: 5051400
    Abstract: Vasopressin derivatives having V.sub.1 antagonist activity which alleviate the symptoms of motion sickness. More specifically, the vasopressin V.sub.1 antagonists of this invention are employed to prevent nausea and emesis associated with motion. The antagonists may also be employed for preventing nausea and emesis due to other etiologies.
    Type: Grant
    Filed: June 28, 1990
    Date of Patent: September 24, 1991
    Assignee: SmithKline Beecham Corporation
    Inventors: Lewis B. Kinter, Randall L. Kohl
  • Patent number: 5051403
    Abstract: A method of reducing neuronal damage related to an ischemic condition in a human patient, such as stroke-induced damage, by administration of a binding/inhibitory omega-conotoxin peptide.
    Type: Grant
    Filed: November 22, 1989
    Date of Patent: September 24, 1991
    Assignee: Neurex Corporation
    Inventors: George P. Miljanich, Robert S. Bitner, Stephen S. Bowersox, James A. Fox, Karen L. Valentino, Donald H. Yamashiro
  • Patent number: 5049182
    Abstract: Microcapsule formulations are combined with emulsions or particle dispersions in a single-package formulation which is storage-stable and provides substantially the full efficacy of each of the two forms as if applied individually. The single-package formulation is suspension having two dispersed phases--the first being an active species encapsulated in a shell of inert polymeric diffusion-limiting material (i.e., a microcapsule), and the second being an active species in water-insoluble form with no diffusion-limiting barrier at its surface. An appropriate suspension system is included to prevent the dispersed phases from agglomerating within themselves and with each other. The invention is useful in combining two different active ingredients as well as in combining immediate-delivery and delayed-delivery forms of the same active ingredient.
    Type: Grant
    Filed: February 3, 1989
    Date of Patent: September 17, 1991
    Assignee: ICI Americas Inc.
    Inventors: Herbert B. Scher, Marius Rodson, Jose L. Calvo, Miguel Gimeno
  • Patent number: 5049382
    Abstract: A coating composition contains an effective amount of between 5 and 70 percent by weight of metalized tubules which are or which encapsulate a composition known to have an antifouling effect or known to possess antimicrobial, herbicidal algaicidal or pesticidal (biocidal) properties. When the coating composition is applied to a surface to be protected, a toxic surface environment is formed. The tubules can be used alone or the tubules can contain in the hollow core a secondary or co-biocidal agent or mixtures of these agents. When desired, the metal coating layer metalizing the tubule can be a non-biocidal metal. In those cases, protection is provided by the biocidal agent carried in the core.
    Type: Grant
    Filed: April 14, 1989
    Date of Patent: September 17, 1991
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: Ronald R. Price, Robert F. Brady, Jr.
  • Patent number: 5049506
    Abstract: Glutamine-containing peptides, a process for the preparation thereof, and the use thereof Peptides of the structureH-A.sub.1 -A.sub.2 -A.sub.3 -A.sub.4 -Gln-A.sub.6 -Lys-Val-A.sub.9 -A.sub.10 -NH.sub.2 (I)in which A.sub.1 =Val, LeuA.sub.2 =Gly, SerA.sub.3 =Pro, HypA.sub.4 =Gly, SerA.sub.6 =Gly, SerA.sub.9 =Leu, Ile andA.sub.10 =Gly, Ala,and the salts thereof, and a process for the preparation thereof, are described. These peptides act as substrates of blood coagulation factor XIII and can be used for the quantification of this enzyme and for detecting reactions in which activated blood coagulation factor XIII is produced, consumed or inhibited.
    Type: Grant
    Filed: October 27, 1988
    Date of Patent: September 17, 1991
    Assignee: Behringwerke Aktiengesellschaft
    Inventor: Werner Stuber
  • Patent number: 5049548
    Abstract: Renin-inhibitory di-, tri-, and tetrapeptides of the formula I:A-B-E-G-T-Jin whichA is heterocyclic, substituted heterocyclic etc;B is --N(A.sup.1)CH[(CH.sub.2).sub.2 R.sup.3 ]CO--,E is absent or is --N(A.sup.2)CH[(CH.sub.2).sub.2 R.sup.4 ]CO--;G is ##STR1## and J is --Y--(CH.sub.2).sub.x [CH(R.sup.5)].sub.y --(CH.sub.2).sub.z --R.sup.10and pharmaceutically acceptable salts thereof are disclosed. These compounds inhibit renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these problems which employ these novel peptides.
    Type: Grant
    Filed: March 3, 1989
    Date of Patent: September 17, 1991
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, Jan ten Broeke
  • Patent number: 5049378
    Abstract: Methods of treating diseases in swine are disclosed using porcine interferon alpha and/or gamma.
    Type: Grant
    Filed: April 24, 1989
    Date of Patent: September 17, 1991
    Assignee: Ciba-Geigy Canada Ltd.
    Inventor: Manuel Campos