Patents Examined by Lester L. Lee
  • Patent number: 5047399
    Abstract: Novel hydrophobic psuedo-peptides of formula I ##STR1## wherein R.sub.1 is lower alkyl or -CH.sub.2 CONR.sub.6 R.sub.7 ; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently lower alkyl, cycloalkyl lower alkyl, aryl lower alkyl, heteroaryl lower alkyl, aryl lower alkoxy, substituted aryl lower alkyl, wherein the aryl portion is substituted with 1-3 substituents independently selected from lowr alkyl, hydroxyl, lower alkoxy and halogeno, substituted heteroaryl lower alkyl wherein the substituents on the heteroaryl portion are as defined for aryl lower alkyl, substituted cycloalkyl lower alkyl, wherein the substituents on the cycloalkyl portion are as defined for aryl lower alkyl, and substituted aryl lower alkoxy wherein the substituents are as defined for aryl lower alkyl;R.sub.6 and R.sub.7 are independently hydrogen or lower alkyl;X.sub.1, X.sub.2, X.sub.3, X.sub.4 and X.sub.5 are independently ##STR2## cis or trans --CR.sub.8 .dbd.CR.sub.9 --, --CHR.sub.8 CHR.sub.9 --, --CH.sub.2 NR.sub.
    Type: Grant
    Filed: July 13, 1988
    Date of Patent: September 10, 1991
    Assignee: Schering Corporation
    Inventors: Laura S. Lehman, Michael F. Czarniecki
  • Patent number: 5047502
    Abstract: Small cell lung carcinoma cells (SCLC) contain gastrin releasing peptide (GRP) receptors. The response of the cells to GRP is rapid growth. We have found a group of heptapeptides that act as GRP antagonists by blocking the binding of GRP to its receptor thereby inhibiting the growth of cells that are sensitive to the growth promoting acitivity of GRP.
    Type: Grant
    Filed: August 3, 1989
    Date of Patent: September 10, 1991
    Assignee: Merck and Co., Inc.
    Inventors: Allen I. Oliff, David C. Heimbrook, Mark W. Riemen, Victor M. Garsky
  • Patent number: 5047396
    Abstract: The present invention relates to an intravenous pharmaceutical composition comprising cyclosporin as active ingredient. The composition is composed ofa) 1 part by mass of one or more cyclosporins,b) 8 to 13 parts by mass of a monoester of a saturated hydroxylated fatty acid formed with polyethylene glycol or the mixture of said monoesters,c) 4 to 10 parts by mass of one or more intravenously administerable mono- or polivalent alcohols.The invention further relates to a process for preparing such composition.
    Type: Grant
    Filed: July 21, 1989
    Date of Patent: September 10, 1991
    Assignee: Biogal Gyogyszergyar
    Inventors: Erno Orban, Tibor Balogh, Lajos Ila, Gabor Ambrus, Antonia Jekkel, Sandor Elek, Eva Tomori, Istvan Elekes, Eva T. Sarudy, Imre Moravcsik, Lajos Siklosi
  • Patent number: 5047397
    Abstract: Compounds and compositions comprising synthetic analogs of Atrial Natriuretic Peptides are provided, together with methods for their production and use as natriuretics, diuretics and/or vasodilators, or as intermediates for or modulators of such useful compounds or of native Atrial Natriuretic Peptides.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: September 10, 1991
    Assignee: California Biotechnology Inc.
    Inventors: Robert M. Scarborough, John A. Lewicki, Lorin K. Johnson
  • Patent number: 5045531
    Abstract: A process for treating a wound in a host which comprises administering to the host having a wound at least one biologically active amphiphilic peptide. The peptide is an ion channel-forming peptide and is administered in an amount effective for treating a wound in a host.
    Type: Grant
    Filed: December 18, 1989
    Date of Patent: September 3, 1991
    Assignee: Magainin Sciences Inc.
    Inventors: Barry Berkowitz, Leonard S. Jacob
  • Patent number: 5045322
    Abstract: An antimicrobial superabsorbent composition of a cross-linked hydrophilic sodium salt form of a partially neutralized acrylic acid-based polymer gel having covalently bonded thereto a silane. The composition can be in the form of flakes, strips, powders, filaments, fibers, or films, and may be applied to a substrate in the form of a coating.
    Type: Grant
    Filed: August 6, 1990
    Date of Patent: September 3, 1991
    Assignee: Dow Corning Corporation
    Inventors: Lynne M. B. Blank, Thomas D. Boyce, William C. White
  • Patent number: 5045465
    Abstract: A fermentation process and improved aqueous nutrient medium are used for the production of urease-free creatinine iminohydrolase from an aerobic soil microorganism. In the process, an inoculum culture of the microorganism is transferred into a production medium to generate microorganisms in which creatinine iminohydrolase production has been induced, said nutrient medium containing a source of ammonia and after the ammonia is substantially exhausted, incrementally adding a solution of creatinine, controlling the pH by addition of .alpha.-ketoglutaric acid, and extracting urease-free creatinine iminohydrolase. An improved aqueous nutrient medium for use as the production medium is disclosed.
    Type: Grant
    Filed: August 14, 1989
    Date of Patent: September 3, 1991
    Assignee: Eastman Kodak Company
    Inventor: Jefferson C. Lievense
  • Patent number: 5045530
    Abstract: A pharmaceutical preparation is disclosed which is made up of a micelle or a vesicle each consisting of a cationic tenside with a monovalent ion and a hydrophobic cyclic or linear peptide, dispersed in a solvent whose pH value lies between pH 7-pH 8, the critical micellization concentration (cmc) lying in the range of 1.0.10.sup.-7 to 7.0.10.sup.-5 mol/liter. The preparations disclosed have in particular the advantage that by the increasing of the hydrophobicity of the alkyl or aryl chain or the radical at the N.sup.+ tenside both the membrane permeability is increased and furthermore the pharmaceutical active substance, in particular linear and cyclic tyrocidines (A-J), can be transferred actively into the cytosol. They thus act on the transciption level. In addition, linear and cyclic tyrocidines in particular have antiviral effects.
    Type: Grant
    Filed: April 27, 1989
    Date of Patent: September 3, 1991
    Assignee: Medici Chem.-Pharm. Fabrik Putter GmbH
    Inventor: Henrich H. Paradies
  • Patent number: 5043163
    Abstract: The present invention relates to a multi-component pesticidal composition against anthropoda containing as active ingredient pyrethroides and phosphate esters and optionally piperonyl butoxide and excipients comprising as pyrethroid component 0.1 to 40 percent by weight of cypermethrin related to the total weight comprising out of the 8 possible isomers 40 to 100 percent by weight of 1RcisS and/or 1RtransS stereoisomer and as a second component at least one phosphoric acid, thiophosphoric acid or dithiophosphate being toxic on arthropoda at a ratio of 1:1-99 related to the amount of cypermethrin.
    Type: Grant
    Filed: August 9, 1990
    Date of Patent: August 27, 1991
    Assignee: Chinoin Gyogyszer- es Vegyeszeti Termekek Gyara Rt.
    Inventors: Laszlo Pap, Eva Somfai, Andras Szego, Istvan Szekely, Lajos Nagy, Gyorgy Hidasi, Sandor Zoltan, Andrea Toth, Bela Bertok, Sandor Botar, Antal Gajary, Agnes Hegedus, Aniko Deak
  • Patent number: 5043322
    Abstract: Synthetic peptides which stimulate the release of pituitary GH in animals, including humans, and are more resistant to enzymatic degradation in the body than hGRF having the sequence: (B)R.sub.1 -R.sub.2 R.sub.3 -Ala-Ile-Phe-Thr-R.sub.8 -Ser-R.sub.10 -Arg-R.sub.12 R.sub.13 -Leu-R.sub.15 -Gln-Leu-R.sub.18 -Ala-Arg-R.sub.21 -R.sub.22 -Leu-R.sub.24 -R.sub.25 -Ile-R.sub.27 -R.sub.28 -R.sub.29 -Gln-Gln-Gly-Glu-R.sub.34 -Asn-Gln-Glu-R.sub.38 R.sub.39 -R.sub.40 -Arg-R.sub.42 -R.sub.43 -R.sub.44 wherein R.sub.1 is Tyr, D-Tyr, Met, D-Met, Phe, D-Phe, pCl-Phe, Leu, His or D-His; B is H, C.sup.a Me, N.sup.1 Me, desamino, Ac or For; R.sub.2 is Ala, D-Ala, NMA or D-NMA; R.sub.3 is Asp or D-Asp; R.sub.8 is Ser, Asn, Lys, Arg, Asp or Gln; R.sub.10 is Tyr, D-Tyr or Phe; R.sub.12 is Arg or Lys; R.sub.13 is Ile, Val, Leu or Ala; R.sub.15 is Gly, Ala or .beta.-Ala; R.sub.18 is Ser or Tyr; R.sub.21 is Lys, D-Lys, Arg or D-Arg; R.sub.22 is Leu, Ile, Ala or Val; R.sub.24 is Gln or His; R.sub.
    Type: Grant
    Filed: July 22, 1988
    Date of Patent: August 27, 1991
    Assignee: The Salk Institute for Biological Studies
    Inventors: Jean E. F. Rivier, Catherine L. Rivier, Wylie W. Vale, Jr.
  • Patent number: 5043321
    Abstract: A method for alleviating stress induced immunosuppression is accomplished by application of low doses of ANF[1-28] or other ANF analogs having intact N-terminal sequences. Atrial natriuretic factors (ANFs) with intact N-terminal sequences are shown to be effective inhibitors of CRF 41-stimulated ACTH secretion when the ANFs are present in low concentrations. ANF[1-28] significantly inhibited ACTH release stimulated by 1-5 nM CRF. At the most effective concentration of 100 pM, ACTH release was inhibited by 40.1% (p<0.001). This effect was manifested after three hours, but not after only one half or one hour of incubation. Conversely, ANF[5-28], at concentrations of 10 to 10,000 pM, had no effect on ACTH secretion after one half, one, or three hours. ANF[1-11] weakly inhibited ACTH secretion at concentrations of 100 pM and 1000 pM. Again, three hours of incubation was required to manifest these effects.
    Type: Grant
    Filed: July 11, 1988
    Date of Patent: August 27, 1991
    Assignees: Center for Innovative Technology, University of Virginia
    Inventor: Alex J. Baertschi
  • Patent number: 5043422
    Abstract: A peptide having anti-HIV activity consists of an amino acid chain represented by Asn-Phe-Pro-Leu-Ile-Ile-Lys-Asn-Leu-Lys-Ile-Glu-Asp-Ser-Asp-Thr-Tyr-Ile-Cy s-Glu-Val-Glu-Asp-Gln-Lys-Glu. The Cys underlined in the above amino acid chain may be replaced by Phe, Ser, Cys.sup.Acm or Cys.sup.Bzl.
    Type: Grant
    Filed: July 2, 1990
    Date of Patent: August 27, 1991
    Inventors: Kohji Ohki, Kazuyoshi Ikuta, Kazutaka Ohmura, Shiro Kato
  • Patent number: 5041423
    Abstract: New antibiotics of the mureidomycin group have the formula ##STR1##wherein X represents the group ##STR2##and wherein R represents hydrogen, an alkyl group having from 1 to 10 carbon atoms, an alkenyl group having from 2 to 7 carbon atoms, an alkynyl group having from 3 to 7 carbon atoms, an aryl group having from 6 to 10 carbon atoms, an aralkyl group having from 7 to 10 carbon atoms, or one of the said aryl or aralkyl groups substituted with at least one substituent selected from halogen and alkyl groups having from 1 to 5 carbon atoms. The compound in which X represents 8-hydroxy-1,2,3,4-tetrahydroisoquinolin-3-yl is named mureidomycin E and the compound in which X represents 6-hydroxy-1,2,3,4-tetrahydroisoquinolin-3-yl is named mureidomycin F. This group of compounds and their pharmaceutically acceptable esters and salts are useful as antibiotics for the treatment of bacterial infections.
    Type: Grant
    Filed: November 17, 1988
    Date of Patent: August 20, 1991
    Assignee: Sankyo Company, Limited
    Inventors: Tatsuo Haneishi, Masatoshi Inukai, Keiko Shimizu, Fujio Isono, Yoshiharu Sakaida, Takeshi Kinoshita
  • Patent number: 5039663
    Abstract: Novel compounds, called mureidomycins A, B, C and D, may be prepared by cultivation of a suitable microorganism of the genus Streptomyces, especially Streptomyces flavidovirens SANK 60486 (FERM P-8636, FERM BP-1347). These represent a wholly new class of antibiotics, which are valuable in the treatment of infections caused by a variety of bacteria, notably of the genus Pseudomonas.
    Type: Grant
    Filed: October 4, 1988
    Date of Patent: August 13, 1991
    Assignee: Sankyo Company Limited
    Inventors: Tatsuo Haneishi, Masatoshi Inukai, Keiko Shimizu, Fujio Isono, Yoshiharu Sakaida, Takeshi Kinoshita
  • Patent number: 5039660
    Abstract: A bioerodible pellet capable of administering an even and continuous dose of a peptide over a period of up to a year, when subcutaneously implanted, is provided. The bioerodible implant is a partially-fused pellet, which pellet has a peptide drug homogeneously-bound in a matrix of a melted and recrystallized, nonpolymer carrier. Preferably, the nonpolymer carrier is a steroid and in particular is cholesterol or a cholesterol derivative. In one embodiment, the peptide drug is growth hormone-releasing hormone. A method for making the bioerodible pellet also is provided.
    Type: Grant
    Filed: March 2, 1988
    Date of Patent: August 13, 1991
    Assignee: Endocon, Inc.
    Inventors: Robert J. Leonard, S. Mitchell Harman
  • Patent number: 5039440
    Abstract: A traction fluid comprising at least one compound selected from diesters or monoesters represented by general formulas ##STR1## wherein: A is an ester linkage ##STR2## n.sub.1 and n.sub.2 are independently integers having a value of from 0 to 5 inclusive;R.sub.1 is hydrogen or a C.sub.1 -C.sub.8 alkyl; andR.sub.2 is a C.sub.1 to C.sub.3 alkyl group.
    Type: Grant
    Filed: March 31, 1988
    Date of Patent: August 13, 1991
    Assignee: Toa Nenryo Kogyo, K.K.
    Inventors: Narihiko Yoshimura, Hirotaka Tomizawa
  • Patent number: 5039664
    Abstract: Peptides of the formula: ##STR1## which comprise novel elements replacing the Phe(8)-His(9) sequence in renin-inhibitory peptides based on substrate analogy, which inhibit the substrate-cleaving action of renin and have improved bioavailability; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension or congestive heart failure or of establishing renin as a causative factor in these problems which employ the novel peptides.
    Type: Grant
    Filed: March 8, 1989
    Date of Patent: August 13, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Arthur A. Patchett, William H. Parsons, William J. Greenlee, Prasun K. Chakravarty
  • Patent number: 5039662
    Abstract: The invention discloses an acylated pentapeptide that inhibits metastasis activity of malignant cells.
    Type: Grant
    Filed: May 10, 1989
    Date of Patent: August 13, 1991
    Assignee: Monsanto
    Inventor: Charles S. Schasteen
  • Patent number: 5037957
    Abstract: New compounds which are cysteine proteinase inhibitors of the formulaB - A - CwhereinB=Pro-Arg-Leu-Val-Gly-, Arg-Leu-Val-Gly-, Leu-Val-Gly-, or Val-Gly-, or zero; the N-terminal amino acid optionally having a protective group,A=a reactive group capable of specifically reacting with free-SH groups,C=-Gly-Pro-Met-Asp-Ala; -Gly-Pro-Met-Asp; -Gly-Pro-Met; or -Gly-Pro, or zero;with the proviso that B and C are not both zero.
    Type: Grant
    Filed: December 11, 1989
    Date of Patent: August 6, 1991
    Inventors: Anders Grubb, Magnus Abrahamson, Jerzy Trojnar
  • Patent number: 5037804
    Abstract: The present invention relates to an agent for preventing and treating thrombocytopenia which comprises, an an active ingredient, a muramyldipeptide derivative of the formula: ##STR1## wherein X represents an amino acid residue selected from L-alanine, L-serine and L-valine, Y represents ##STR2## wherein R.sub.1 represents a carboxyl group, n represents an integer of 1 to 6, A represents a saturated aliphatic hydrocarbon group having 7 to 29 carbon atoms which may have branched chains, and Acyl represents an acyl group having 2 to 6 carbon atoms, and the agent exhibits excellent preventing and treating effects on thrombocytopenia when administered orally or parenterally.
    Type: Grant
    Filed: June 8, 1989
    Date of Patent: August 6, 1991
    Assignee: Daiichi Seiyaku Co., Ltd.
    Inventors: Toshiro Nakayasu, Ken Masuo, Teruo Takayanagi, Atsuo Inoue, Eiro Tsubura, Toru Masaoka