Patents Examined by Delbert R. Phillips
  • Patent number: 4826815
    Abstract: The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; Or.sub.10 wherein R.sub.10 is hydrogen or loweralkyl; NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are independently selected from hydrogen and loweralkyl; or R.sub.13 --CO--B wherein B is NH, O, CH.sub.2, HNCH.sub.2 and R.sub.13 is loweralkyl, alkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, aminoalkyl, N-protected aminoalkyl, hydroxylated dialkylamino, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic, carboxyalkyl, or lower alkyl carboxyalkyl esters; W is N or CH: U,V may be the following combinations H,OH; OH,H; H,H; or when taken together as O represents a carbonyl with the provisos that if U,V.dbd.H,OH, then W=CH, and if U,V.dbd.O then W.dbd.N; R.sub.1 , R.sub.3 and R.sub.5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R.sub.2, R.sub.4, R.sub.7, R.sub.8 and R.sub.
    Type: Grant
    Filed: January 9, 1987
    Date of Patent: May 2, 1989
    Assignee: Abbott Laboratories
    Inventors: Jay R. Luly, Joseph Dellaria, Anthony K. L. Fung, Dale J. Kempf, Jacob J. Plattner, Saul H. Rosenberg, Hing L. Sham
  • Patent number: 4826813
    Abstract: Vasopressin antagonists which have a 4'-methyl-.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid group have vasopressin antagonist activity without substantial agonist activity. A species of the invention is [1-(4'-methyl-.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-8-arginine]vasopressin.
    Type: Grant
    Filed: May 21, 1987
    Date of Patent: May 2, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: William F. Huffman, Nelson C. F. Yim
  • Patent number: 4826814
    Abstract: There are provided tripeptide compounds represented by the following formula ##STR1## wherein R.sub.1 represents a C.sub.1-10 alkyl group, a C.sub.4-7 cycloalkyl or C.sub.
    Type: Grant
    Filed: May 5, 1987
    Date of Patent: May 2, 1989
    Assignee: Dainippon Pharmaceutical Co., Ltd.
    Inventors: Tadahiro Sawayama, Masatoshi Tsukamoto, Takashi Sasagawa, Kazuya Nishimura, Kanoo Hosoki, Kunihiko Takeyama
  • Patent number: 4824994
    Abstract: A method for the production of N-carbobenzoxy-.alpha.-L-aspartyl-L-phenylalanine methyl ester characterized by the reaction of L-phenylalanine methyl ester with fine N-carbobenzoxy-L-aspartic anhydride crystals, is disclosed.
    Type: Grant
    Filed: September 14, 1984
    Date of Patent: April 25, 1989
    Assignee: Ajinomoto Co., Inc.
    Inventors: Satoji Takahashi, Katsumi Sugiyama
  • Patent number: 4822606
    Abstract: Novel peptides having immunosuppressive or immunoregulatory activity are disclosed.
    Type: Grant
    Filed: April 7, 1986
    Date of Patent: April 18, 1989
    Assignee: Duke University
    Inventors: Ralph D. Snyderman, George J. Cianciolo
  • Patent number: 4822774
    Abstract: A peptide is novel and useful for the bronchodilative activity and the hypotensive activity, having the following structure:His-Ser-Asp-Ala-Val-Phe-Thr-Asp-Asn-Tyr-Thr-Arg-Leu-Arg-Lys-Gln-X-Ala-Val-L ys -Lys-Tyr-Leu-Asn-Ser-Ile-Leu-Asn-Gly-Y(wherein X is Met or Leu; and Y is OH, Lys-OH, Arg-OH, Lys-Arg-OH, or Lys-NH.sub.2 when X is Met, or Y is Lys-NH.sub.2, Lys-OH, or Lys-Arg-OH when X is Leu).
    Type: Grant
    Filed: April 5, 1988
    Date of Patent: April 18, 1989
    Assignee: Eisai Co., Ltd.
    Inventors: Osamu Ito, Shinro Tachibana
  • Patent number: 4822776
    Abstract: A mediator substance exhibiting inhibitory effect upon anabolic enzyme activity in mammals, is prepared by a method comprising gathering a sample of macrophage cells from a mammal, incubating a portion of the macrophage cells with a stimulating mateThis invention was made in the course of a grant from the National Institutes of Health.
    Type: Grant
    Filed: October 29, 1985
    Date of Patent: April 18, 1989
    Assignee: The Rockefeller University
    Inventors: Anthony Cerami, Masanobu Kawakami
  • Patent number: 4822818
    Abstract: New bicyclic compounds, inclusive of salts thereof, of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents hydrogen, hydroxyl or lower alkoxy, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is hydrogen, lower alkyl, amino-lower-alkyl or acylamino-lower-alkyl, R.sup.5 is hydrogen, lower alkyl or aralkyl which may be substituted, R.sup.6 is hydroxyl, lower alkoxy, amino or lower alkylamino, and m and n each means 1 or 2, have inhibitory activities of angiotensin converting enzyme and bradykinin decomposing enzyme, and are useful as antihypertensive agents.
    Type: Grant
    Filed: October 19, 1981
    Date of Patent: April 18, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yoshikazu Oka, Kohei Nishikawa, Akio Miyake
  • Patent number: 4820804
    Abstract: New hypocalcaemic peptides are disclosed of the formula ##STR1## wherein X represents H for the replacement of the N alpha amino group or acyl groups for the acylation of the N alpha amino group, the N-alpha amino group. The acyl groups are carboxylic acids especially formic, acetic, propionic, buteric, valeric, hexanoic, heptanoic, octanoic, and nonanoic acids or their respective isomers, L-lactic acid and the half amides of malonic, succinic, glutaric and adipic acids. Y is L-valine, glycine, L-methionine, L-alanine, L-leucine or L-isoleucine.
    Type: Grant
    Filed: April 21, 1987
    Date of Patent: April 11, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Ronald C. Orlowski, Jay K. Seyler, James E. Geever, Everett Flanigan
  • Patent number: 4820729
    Abstract: Compounds of the formula ##STR1## wherein R and R.sub.9 are independently hydroxy or lower alkoxy,R.sub.1 and R.sub.2 are hydrogen or lower alkyl, aryl-lower alkyl having from 7 to 12 carbon atoms, or heterocyclic-lower alkyl having from 6 to 12 carbon atoms,R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are hygrogen or lower alkyl,R.sub.6 is cycloalkly having from 3 to 20 carbon atoms, aryl or aryl-lower alkyl, and the aryl group contains from 6 to 10 carbon atoms, and their pharmaceutically acceptable, nontoxic acid addition salts and where R or R.sub.9 or both are hydroxy, their pharmaceutically acceptable, nontoxic basic salts possess antihypertensive activity.
    Type: Grant
    Filed: March 30, 1981
    Date of Patent: April 11, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Raymond D. Youssefyeh, Jerry W. Skiles, John T. Suh, Howard Jones
  • Patent number: 4820691
    Abstract: Compounds of the formula ##STR1## are disclosed. These compounds interevene in the conversion of angiotensin to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.
    Type: Grant
    Filed: June 24, 1987
    Date of Patent: April 11, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Dinesh V. Patel
  • Patent number: 4818748
    Abstract: Anti-hypertensive compounds of the formula ##STR1## in which A represents hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.7 -C.sub.14 -aralkyl, phenylsulphonyl, tolylsulphonyl or C.sub.1 -C.sub.8 -alkylsulfphonyl, or represents an aminoprotective group,B represents a direct bond, or represents sarcosyl, or represents a group of the formula ##STR2## D represents a direct bond, or represents a group of the formula ##STR3## wherein X represents methylene, ethylene or sulphur,E, G, J, K, L and M independently have the same meanings as B,R.sup.1 is an optionally substituted phenyl radical, andQ is a hydroxy, alkoxy or amino group, or a physiologically acceptable salt thereof.
    Type: Grant
    Filed: March 6, 1987
    Date of Patent: April 4, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Bender, Rolf Henning, Andreas Knorr, Johannes-Peter Stasch
  • Patent number: 4816439
    Abstract: Human growth hormone is used for the treatment of individuals who are intoxicated with poisonous substances of the type which is degraded in the liver by microsomal enzymes, such as hexobarbiturates or alcohol.
    Type: Grant
    Filed: March 27, 1987
    Date of Patent: March 28, 1989
    Assignee: Nordiske Gentofte A/S
    Inventor: Karin D. Jorgensen
  • Patent number: 4816568
    Abstract: Growth hormones are admixed with various stabilizers to provide for the decreased formation of insolubles and preservation of the soluble bioactivity of the growth hormone in aqueous environments. Examples of such stabilizers include certain polyols, amino acids, polymers of amino acids having a charged side group at physiological PH, and choline salts.
    Type: Grant
    Filed: May 16, 1986
    Date of Patent: March 28, 1989
    Assignee: International Minerals & Chemical Corp.
    Inventors: Edwin J. Hamilton, Jr., Bruce D. Burleigh
  • Patent number: 4816441
    Abstract: Peptides of the formula R.sup.1 -His-Asp-Glu-Ala-R wherein R.sup.1 is Ala-Gln, and R is a polypeptide residue with up to 50 amino acid residues, and wherein one, more or all of the amino acid residues in R.sup.1 and/or R independently may be omitted, can be used to augment cell mediated cytotoxicity and thereby to treat cancers and viral infections. These peptides may be prepared by proteolytic digestion of Staphylococcus aureus protein A, as well as by protein synthesis, recombinant DNA methods or any other methods known in the art.
    Type: Grant
    Filed: November 14, 1986
    Date of Patent: March 28, 1989
    Assignee: Novo Industri A/S
    Inventors: Jesper Zeuthen, Lars Thim, Niels P. H. Moller
  • Patent number: 4816562
    Abstract: Novel compounds represented by the following general formula (1) and salts thereof: ##STR1## wherein n represents an integer of 3 to 4, R.sup.1 represents ##STR2## or --SO.sub.2 R.sup.2, and R.sup.2 represents optionally branched lower alkyl group having 1 to 6 carbon atoms, phenyl group, benzyl group or tolyl group, which are useful as substrate for use in the measurement of biological components; a substrate for use in the measurement of biological component which comprises said novel compound or salt thereof; and a method for measuring biological component which comprises using said substrate.
    Type: Grant
    Filed: November 21, 1986
    Date of Patent: March 28, 1989
    Assignee: Nitto Boseki Co., Ltd.
    Inventors: Takeshi Nagasawa, Yoshio Nakamura, Kenji Tani, Katsumasa Kuroiwa
  • Patent number: 4816443
    Abstract: Novel peptides having potent natriuretic activity are disclosed with the following amino acid sequence: ##STR1## wherein Z is H, acetyl, Boc or Ser-Leu, E is Phe, NMP, OMT, ChA, F is Gly or DAl, G is Ala or Gly, H is Arg or DAr, Pro, Lys or Dly, I is Ile, Met, MeO, MO.sub.2, Leu, Nle, or Val, J is Aib, .alpha.MG or .alpha.MA, K is Arg or Lys, L is Ile or Val, M is Aib, Gly, Ala or DAl, N is Ala, NMA, Pro, Phe or NMP, O is Gln, DGl, Ala or DAl, P is Ser, His, Arg or Lys, Q is Gly, Pro, Ala or Dal, R is Leu, Phe or ChA, S is Gly, Ala or Dal, Arg or DAr, T is Asn DAs, Ala or Dal, U is Ser, DSe, Ala or DAl, V is Phe, DPh, Ala or DAl, Y is -OH or -NH.sub.2 and n is 0 or 1. Also included are the lower alkyl esters and the physiologically acceptable metal salts and acid addition salts of the foregoing peptides. Unless indicated otherwise all optically active amino acids have the L-configuration.
    Type: Grant
    Filed: May 19, 1987
    Date of Patent: March 28, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Stephen F. Brady, Ruth F. Nutt
  • Patent number: 4816561
    Abstract: Novel biologically active polypeptides, including a new class of transforming growth factor (TGF) polypeptides, which exhibit cell growth promoting properties are disclosed, as well as a process for isolating the TGF polypeptides from both human and murine cell lines in homogeneous form. Also disclosed are antigenic oligopeptides derived from the TGF polypeptides and antibodies raised therefrom which have application in the detection and treatment of malignancies and oligipeptides which have the ability to bind with cellular growth factor receptors and thus to interfere with transformation of certain cell lines into a cancerous state. Compositions and methods based on the disclosed peptides for detection and treatment of cancer and other proliferative diseases and for cell or tissue growth associated treatment, e.g., wound healing, ulcer therapy and bone loss are also described.
    Type: Grant
    Filed: September 17, 1985
    Date of Patent: March 28, 1989
    Inventor: George J. Todaro
  • Patent number: 4816559
    Abstract: The iron-containing biologically active peptide TAN-866 produced by microorganisms belonging to the genus Pseudomonas and its iron free compounds have antibacterial activity mainly against gram-negative bacteria. These peptides can be used as a therepeutic agent for bacterial infections in mammals, domestic fowl, etc., caused by Pseudomonas aeruginosa. Further, TAN-866 and its deacyl compounds are also promising as the starting materials and intermediates for the synthesis of novel products.
    Type: Grant
    Filed: July 8, 1987
    Date of Patent: March 28, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Setsuo Harada, Hideo Ono, Nozomi Katayama
  • Patent number: 4816560
    Abstract: New partially retro-inverted tuftsin analogues of general formula I ##STR1## wherein R represents the side-chain of the amino acids threonine, methionine or leucineR.sup.1 represents the side-chain of the amino acids lysine or arginineR.sup.2 is hydrogen or a metabolically labile acyl group,all the asymmetric carbon atoms are either of the S- or R-configuration, or, alternatively, the first, third, and fourth asymmetric carbons, starting from the N-terminal residue, are of the S-configuration while the second one is of the R- or (R,S)-configuration, and the corresponding pharmacologically acceptable salts, esters and amides. The new compounds which share the same pharmacological properties of tuftsin, are much more stable toward the enzymatic degradation than the parent molecule.
    Type: Grant
    Filed: July 16, 1987
    Date of Patent: March 28, 1989
    Assignees: Eniricerche S.p.A., Sclavo S.p.A.
    Inventors: Antonio S. Verdini, Fabio Bonelli, Antonello Pessi, Franco Cardinali, Diana Boraschi, Stefano Censini, Romano Di Trapani