Patents Examined by S. G. Marshall
  • Patent number: 5648461
    Abstract: Compounds and compositions comprising fragments and synthetic analogs of human thrombospondin are provided together with methods for their use as thrombospondin-like agents.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 15, 1997
    Assignees: W.R. Grace & Co.-Conn, The Medical College of Pennsylvania
    Inventors: Jacob Eval, Bruce King Hamilton, George Paul Tuszynski
  • Patent number: 5648336
    Abstract: The present invention pertains to modified bradykinin antagonist peptides of the formula X-A.sup.0 -B.sup.1 -C.sup.2 -D.sup.3 -E.sup.4 -F.sup.5 -G.sup.6 -H.sup.7 -J.sup.8 -K.sup.9, where at least one of F.sup.5, H.sup.7 and J.sup.8 is an indane substituted amino acids.
    Type: Grant
    Filed: November 18, 1994
    Date of Patent: July 15, 1997
    Assignee: University of Colorado
    Inventors: John M. Stewart, Lajos Gera, Eric T. Whalley
  • Patent number: 5648458
    Abstract: The peptide HITWDQLWNVMN (SEQ ID NO: 4) and related peptides and peptidomimetics bind to endothelial leukocyte adhesion molecule 1 and block the binding of leukocytes to this important receptor and so can be used to ameliorate the detrimental effects of certain disease conditions.
    Type: Grant
    Filed: February 16, 1995
    Date of Patent: July 15, 1997
    Assignee: Affymax Technologies N.V.
    Inventors: Steven E. Cwirla, Ronald W. Barrett, William J. Dower, Christine L. Martens
  • Patent number: 5643870
    Abstract: A cyclosporin of the formula ##STR1## wherein A is a residue of the formula ##STR2## wherein R is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy or C.sub.1-3 alkylthio; halo-substituted-C.sub.1-3 alkyl, -C.sub.1-3 alkoxy or -C.sub.1-3 alkylthio; hydroxy-substituted-C.sub.1-3 alkyl, -C.sub.2-3 alkoxy or -C.sub.2-3 alkylthio; or amino or mono- or di-(C.sub.1-2 alkyl)-amino,X is oxygen or sulphur,--x--y-- is --CH.dbd.CH-- (trans) or --CH.sub.2 --CH.sub.2 --,B is -.alpha.Abu-, -Val-, -Thr- or -Nva- andQ is -(D)Ala-; -(D)Ser-; -[O-(2-hydroxyethyl)(D)Ser]-; or -[O-acyl(D)Ser]- or -[O-(2-acyloxy ethyl)(D)Ser]-in which the acyl residue is physiologically hydrolysable and acceptable, are useful in the topical treatment of asthma.
    Type: Grant
    Filed: February 26, 1993
    Date of Patent: July 1, 1997
    Assignee: Sandoz Ltd.
    Inventors: Johann Jakob Boelsterli, Marcel Karl Eberle, Reto Naef, Trevor Glyn Payne
  • Patent number: 5643869
    Abstract: Pipecolic acid-containing peptolides wherein the peptidic backbone is of at least 9 .alpha.-amino acid residues joined together by peptide bonds, particularly the compounds of formula I ##STR1## wherein the substituents have various significances, are disclosed. They can be prepared by isolation or derivation from an appropriate microorganism strain such as S 42508/F (NRRL 15761).They have interesting pharmacological, e.g. antifungal, chemotherapeutic drug resistance reversing and to some extent immunosuppressant and antiinflammatory properties.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: July 1, 1997
    Assignee: Sandoz Ltd.
    Inventors: Michael Morris Dreyfuss, Gerhard Emmer, Maximilian Grassberger, Klaus Ruedi, Hans Tscherter
  • Patent number: 5643872
    Abstract: This invention relates to compounds of the formula: ##STR1## wherein: A' is absent, Asn, Gln, Ala or Abu;A is absent or a D- or L-amino acid chosen from Arg, HArg, (Me.sub.2)Arg, (Et.sub.2)Arg, Abu, Ala, Gly, His, Lys, or an .alpha.-R' substituted derivative thereof, Dtc, Tpr and Pro;B is a D- or L-amino acid chosen from Arg, HArg, NArg, (Me.sub.2)Arg, (Et.sub.2)Arg and Lys or an .alpha.-R' substituted derivative thereof;Q is absent or a D or L amino acid chosen from Tyr, (Alk)Tyr, Phe, (4'W)Phe, HPhe, Phg, Pro, Trp, His, Ser, (Alk)Ser, Thr, (Alk)Thr, (Alk)Cys, (Alk)Pen, Ala, Val, Nva, Met, Leu, Ile, Nle and Nal, or an .alpha.-R' substituted derivative thereof;M is absent or Gly or a D- or L-amino acid chosen from Glu, Phe, Pro, Lys and Ser or, provided n is 1, B-Gly-Glu-Q;W is halogen or Alk;R' is Alk or PhCH.sub.2 ; ##STR2## wherein Z.sub.1 and Z.sub.2 are linked via a covalent bond between L.sup.1 and L.sup.2 ; or Z.sub.1 and Z.sub.
    Type: Grant
    Filed: August 26, 1994
    Date of Patent: July 1, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: Fadia El-Fehail Ali, James Martin Samanen
  • Patent number: 5643873
    Abstract: Disclosed are peptides and peptide mimetics that bind selectins, including endothelial leukocyte adhesion molecule 1 (ELAM-1). Such peptides and peptide mimetics are useful in methods for blocking adhesion of leukocytes to the selectins for the purpose of inhibiting inflammation as well as in diagnostic methods employing labeled peptides and peptide mimetics that bind selectins for the purpose of determining the site of inflammation in mammals which inflammation is mediated by the presence of one or more selectins.
    Type: Grant
    Filed: May 11, 1994
    Date of Patent: July 1, 1997
    Assignee: Affymax Technologies N.V.
    Inventors: Ronald W. Barrett, Steven E. Cwirla, William J. Dower, Kerry J. Koller, Jung Lee, Christine L. Martens, Beatrice Ruhland-Fritsch
  • Patent number: 5637568
    Abstract: A composition designed for the sustained and controlled release of medicamentous peptide substances having the formula (I):Ac-D-Nal-D-pClPhe-R.sup.3 -Ser-Tyr-D-Cit-Leu-Arg-Pro-D-Ala-NH.sub.2wherein R.sup.3 is D-Pal or D-Trp. The composition is obtained in the form of microspheres of a biodegradable polymeric material incorporating a water-insoluble salt of the peptide of formula (I).
    Type: Grant
    Filed: March 16, 1994
    Date of Patent: June 10, 1997
    Assignee: Asta Medica Ag
    Inventors: Piero Orsolini, Frederic Heimgartner
  • Patent number: 5631222
    Abstract: Disclosed is a peptide compound represented by the following formula (I):R.sup.1 -R.sup.2 -R.sup.3 -R.sup.4 -R.sup.5 -R.sup.6 -R.sup.7 -R.sup.8 -R.sup.9 -R.sup.10 -R.sup.11 -R.sup.12 -Phe-R.sup.14 -R.sup.15 -R.sup.16 -R.sup.17 -R.sup.18 -Ile-R.sup.20 -Z SEQ. ID NO. 64, (I)wherein R.sup.1-12, R.sup.14-18, and R.sup.20 are as defined in the specification.
    Type: Grant
    Filed: February 10, 1995
    Date of Patent: May 20, 1997
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Kenji Shibata, Toshiyuki Suzawa, Motoo Yamasaki, Takeo Tanaka, Eiji Tsukuda, Koji Yamada, Tetsuji Ohno
  • Patent number: 5631230
    Abstract: Analogues of cholecystokinin-8, which are receptor selective, vary from the normal hormone by alteration of at least one of the two, three or six position amino acids of the natural sequence.
    Type: Grant
    Filed: July 25, 1994
    Date of Patent: May 20, 1997
    Assignee: Arizona Technology Development Corporation
    Inventors: Sunan Fang, Victor Hruby
  • Patent number: 5624900
    Abstract: Peptides having high binding activity for human interleukin-1 and represented by the following formulaH-X.sup.1 -Cys-A-B-A-B-A-Ser-X.sup.2 -Ywherein each A represents an amino acid residue selected from the group consisting of Val, Leu, Ile and Nle, independent of any other selection for A; B represents an amino acid residue selected from the group consisting of Arg, Lys, Gln, His and Ser, independent of any other selection for B; X.sup.1 and X.sup.2 each is a single bond or a peptide segment comprising 1-10 amino acid residues selected from Gly, Ala, Val, Arg, Asn, Ser, Phe, Pro, Leu, Glu, Asp, Lys, Thr, His, Tyr, Nle and Ile and Y represents a hydroxyl group or an amino group; and their salts.
    Type: Grant
    Filed: May 9, 1994
    Date of Patent: April 29, 1997
    Assignee: Kuraray Co., Ltd.
    Inventors: Tatsuo Suda, Etsuko Abe, Masao Tanihara, Chie Fujiwara
  • Patent number: 5623050
    Abstract: Disclosed are (1) a polypeptide represented by formula (I), or a pharmaceutically acceptable amide, ester or salt thereof:His-Ser-Asp-Gly-Ile-Phe-Thr-Asp-Ser-Tyr-Ser-Arg-Tyr-Arg-Lys-Gln-NH-CHX-CO-A la-Val-Lys-Lys-Tyr-Y SEQ ID NO: 13 (I)wherein X is hydrogen atom; or a lower alkyl group which may be substituted with a member selected from the group consisting of hydroxy group, substituted or unsubstituted amino group, carboxyl group, carbamoyl group, and substituted or unsubstituted aromatic group; and Y is one of amino acids or peptides consisting of 1 to 16 amino acid residues counted from the N-terminal side of Leu-Ala-Ala-Val-Leu-Gly-Lys-Arg-Tyr-Lys-Gln-Arg-Val-Lys-Asn-Lys SEQ ID NO: 20, and (2) a pharmaceutical composition comprising a polypeptide represented by formula (I), or a pharmaceutically acceptable amide, ester or salt thereof, which has remarkable c-AMP activity and is useful as a nerve activating agent.
    Type: Grant
    Filed: August 18, 1992
    Date of Patent: April 22, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Chieko Kitada, Takuya Watanabe
  • Patent number: 5620959
    Abstract: The present invention provides polypeptides of the formula XX.sup.1 TrpX.sup.2 X.sup.3 X.sup.4 X.sup.5 X.sup.6 X.sup.7 NH.sub.2, methods of treatment using the polypeptides, pharmaceutical compositions comprising such polypeptides, and processes for their preparation. The polypeptides possess antagonist properties against bombesin and bombesin-like peptides and are useful in the treatment of malignant disease. M, X, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, X.sup.6, and X.sup.7 are as defined in the specification.
    Type: Grant
    Filed: November 23, 1994
    Date of Patent: April 15, 1997
    Assignee: Glaxo Wellcome Inc.
    Inventors: Johann J. Leban, Frederick C. Kull
  • Patent number: 5620955
    Abstract: Bombesin is an amphibian peptide that has a structure closely related to that of several mammalian peptides, including Gastrin Releasing Peptide (GRP) and Neuromedins B and C. Bombesin, GRP and related peptides exert their in vivo effects by binding to specific receptors present on cells of the gastrointestinal tract, the central nervous system, and tumors. The invention relates to novel bombesin derivatives which act as bombesin receptor antagonists by blocking the binding of bombesin, GRP or related peptides to cellular receptors. By blocking the binding of bombesin, GRP and related peptides to cellular receptors on cancer cells, these antagonists inhibit the growth of tumor cells that respond to the growth-promoting action of bombesin. These antagonists are expected to block the binding of bombesin, GRP or related peptides to similar receptors on cells in the gastrointestinal tract or the central nervous system.
    Type: Grant
    Filed: December 17, 1993
    Date of Patent: April 15, 1997
    Assignee: Peptide Technologies Corporation
    Inventors: Martha Knight, Kazuyuki Takahashi, Bhaskar Chandrasekhar
  • Patent number: 5614497
    Abstract: A peptide represented by the formula: ##STR1## wherein R.sub.1 represents an oil-soluble group; R.sub.2 and R.sub.5 represent a hydrogen atom or a lower alkyl group; R.sub.3 represents an aliphatic group which may have O or S; R.sub.4 represents a heterocyclic-substituted lower alkyl group; R.sub.6 represents a hydrogen atom, a lower alkyl group or an aromatic cyclic group; X represents a group having an aromatic ring; n represents an integer of 0 or more and m represents an integer of 2 or more, or a salt thereof exhibits a marked endothelin receptor-antagonistic action, and the peptide [I] is pharmaceutically useful as a therapeutic agent for hypertension, cardiovascular disease and renal disease, for instance.
    Type: Grant
    Filed: December 17, 1992
    Date of Patent: March 25, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Chieko Kitada, Tetsuya Ohtaki, Masahiko Fujino
  • Patent number: 5612453
    Abstract: The invention relates to preparation of selected peptides of the HIV gag protein and derivatives thereof which comprise the peptide sequence NPGLLETSEGCRQ, and which inhibit HIV.
    Type: Grant
    Filed: December 13, 1994
    Date of Patent: March 18, 1997
    Assignee: Chiron Behring GmbH & Co.
    Inventors: Matthias Niedrig, Susanne Modrow, Hans Wolf
  • Patent number: 5594104
    Abstract: The present invention provides anti-obesity proteins, which when administered to a patient regulate fat tissue. Accordingly, such agents allow patients to overcome their obesity handicap and live normal lives with much reduced risk for type II diabetes, cardiovascular disease and cancer.
    Type: Grant
    Filed: February 6, 1995
    Date of Patent: January 14, 1997
    Assignee: Eli Lilly and Company
    Inventors: Margret B. Basinski, Richard D. DiMarchi, David B. Flora, William F. Heath, Jr., James A. Hoffmann, Brigitte E. Schoner, James E. Shields, David L. Smiley
  • Patent number: 5594101
    Abstract: The present invention provides anti-obesity proteins, which when administered to a patient regulate fat tissue. Accordingly, such agents allow patients to overcome their obesity handicap and live normal lives with much reduced risk for type II diabetes, cardiovascular disease and cancer.
    Type: Grant
    Filed: March 3, 1995
    Date of Patent: January 14, 1997
    Assignee: Eli Lilly and Company
    Inventors: Gerald W. Becker, John E. Hale, Warren C. MacKellar
  • Patent number: 5593966
    Abstract: Peptide derivatives with inhibitory activity on the enzyme systems involved in the oxidative burst of human phagocytic cells comprise six and seven amino acid peptide sequences from human cytochrome b.sub.558. The derivatives may be used in medicaments for the treatment of inflammatory diseases.
    Type: Grant
    Filed: May 24, 1990
    Date of Patent: January 14, 1997
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Harry L. Malech, Daniel Rotrosen
  • Patent number: 5591719
    Abstract: A method for treating acute or chronic inflammatory or autoimmune disorders using polypeptides with fibronectin or related activity is provided. The method involves (administering an amount of) one or more polypeptides corresponding to isolated amino acid residue sequences of the 33 kD carboxy terminal heparin-binding region located on the A chain of fibronectin to effectively suppress inflammation and impairment of tissue function in a patient.
    Type: Grant
    Filed: December 10, 1992
    Date of Patent: January 7, 1997
    Assignees: Regents of the University of Minnesota, The United States of America as represented by the Secretary of Health and Human Services
    Inventors: Leo T. Furcht, James B. McCarthy, Sharon M. Wahl, Janice B. Allen