Patents Examined by Lester L. Lee
  • Patent number: 5449662
    Abstract: Compounds with natriuretic, diuretic and/or vasodilation activity which enhance the function of an endogenous ANP are provided. These compounds are capable of both binding to the clearance receptors for ANP and of inhibition of endopeptidase 24.11, an enzyme believed responsible for ANP clearance.
    Type: Grant
    Filed: February 20, 1992
    Date of Patent: September 12, 1995
    Assignee: Scios Nova Inc.
    Inventor: Robert M. Scarborough
  • Patent number: 5446026
    Abstract: The present invention is directed to Cholic, Chenodeoxycholic and deoxycholic acid derivatives of a peptide having the sequence: Pro-Arg-Thr-Asn-Thr-Gly-Ser-Gly-Thr-Pro-amide and use thereof in inducing analgesia.
    Type: Grant
    Filed: February 19, 1993
    Date of Patent: August 29, 1995
    Assignee: Advanced Peptides & Biotechnology Sciences
    Inventors: Michael R. Ruff, Joanna M. Hill, Lawrence D. Kwart, Candace B. Pert
  • Patent number: 5428016
    Abstract: An antimicrobial peptide containing at least the following amino acid sequence, or a derivative thereof, an antimicrobial agent containing said antimicrobial peptide or a derivative thereof as active components at a concentration of at least 1 .mu.M, an antimicrobial composition containing said antimicrobial peptide or a derivative thereof, and a method for processing products which uses the antimicrobial agent containing at least said antimicrobial peptide or a derivative thereof:A--X--A(where, A is an arginine residue or a lysine residue; and X is an amino acid sequence comprising at least from three to nine arbitrary amino acid residues other than cysteine residues.
    Type: Grant
    Filed: March 13, 1992
    Date of Patent: June 27, 1995
    Assignee: Morinaga Milk Industry Co., Ltd.
    Inventors: Mamoru Tomita, Kozo Kawase, Mitsunori Takase, Wayne R. Bellamy, Koji Yamauchi, Hiroyuki Wakabayashi, Yukio Tokita
  • Patent number: 5411943
    Abstract: A method for treating liver cancer in a mammalian subject. The method includes administering to the subject a composition which contains a therapeutically effective amount of an octapeptide of the following formula: ##STR1## wherein, A.sub.1 is D-.beta.-Nal or D-Phe; A.sub.2 is Phe, pentafluro-Phe, or p-substituted X-Phe where X is a halogen, NH.sub.2, NO.sub.2, OH, or C.sub.1-3 alkyl; A.sub.3 is Thr, Ser, Phe, Val, .varies.-aminobutyric acid, or Ile; A.sub.4 is Thr, .beta.-Nal, or Trp; and Y is NH.sub.2 or OH; or a pharmaceutically acceptable salt or complex thereof.
    Type: Grant
    Filed: February 25, 1992
    Date of Patent: May 2, 1995
    Assignee: Biomeasure, Inc.
    Inventor: Arthur E. Bogden
  • Patent number: 5409898
    Abstract: The invention is directed to compositions and methods for treating an infection caused by an organism susceptible to a .beta.-lactam antibiotic comprising two or more active agents. In one embodiment, the composition comprises: (1) a .beta.-lactam antibiotic and (2) a cationic oligopeptide. In another embodiment, the invention is also directed to a composition comprising: (1) a .beta.-lactam antibiotic which inhibits the growth of Enterobacteriaceae bacteria and (2) at least one membrane active substance. Further, the invention is also directed to improved methods for screening potential bactericidal compositions in vitro wherein components of an active complement cascade are included.
    Type: Grant
    Filed: April 26, 1994
    Date of Patent: April 25, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: Richard C. Darveau, James J. Blake, Wesley J. Cosand
  • Patent number: 5405831
    Abstract: Use of amylin, or variants of amylin, as well as amylin agonists, for the treatment of bone disorders, in particular osteoporosis, Paget's disease, and malignant deposits in bone, bone loss of malignancy or endocrine disorders or autoimmune arthritides or immobility and disuse, and in other conditions where a hypocalcaemic effect is of benefit. Functional peptide fragments of amylin, or a variant of amylin or amylin fragment, are provided as well as a soluble amylin, amylin fragments, or variants thereof, or a lyophilized product, or an oral formulation for use alone, or in combination with other agents, including insulin (or insulin-stimulating agents, including but not limited to the sulfonylureas) and estrogens, for the treatment of disorders of bone or calcium balance.
    Type: Grant
    Filed: July 27, 1993
    Date of Patent: April 11, 1995
    Assignee: Amylin Pharmaceuticals, Inc.
    Inventor: Iain MacIntyre
  • Patent number: 5401722
    Abstract: New peptide analogues of the formula IR.sup.1 --Z--NR.sup.2 --CHR.sup.3 --CR.sup.4 --(CH.sub.2).sub.o --(CR.sup.5).sub.t --(CH.sub.2).sub.v --CE--C.sub.w H.sub.2w --R.sup.6 Iin which R.sup.1 to R.sup.6 Z, E, o, t and w have the meanings described herein, and the salts thereof, inhibit the activity of human plasma renin.
    Type: Grant
    Filed: February 15, 1991
    Date of Patent: March 28, 1995
    Inventors: Horst Juraszyk, Peter Raddatz, Johannes Sombroek, Claus J. Schmitges, Klaus-Otto Minck
  • Patent number: 5397771
    Abstract: A pharmaceutical preparation for application of an effective amount of one or more biologically active substance(s) to a mucosal membrane of a mammal comprising an n-glycofurol represented by the formula I: ##STR1## wherein n is 1 to 4 in an amount from: 0.1-30% preferably 0.1-20% most preferably 1-15% in water, or in vegetable oil or n-ethylene glycol(s) represented by formula II:H(OCH.sub.2 CH.sub.2).sub.p OHwherein p is 2 to 8, or in a mixture thereof. Nasal administration of the preparation produces a high plasma concentration of the pharmaceutically active substance(s) nearly as rapid as by i.v. administration.
    Type: Grant
    Filed: September 10, 1993
    Date of Patent: March 14, 1995
    Assignee: Bechgaard International Research and Development A/S
    Inventors: Erik Bechgaard, Sveinbjorn Gizurarson, Rolf K. Hjortkjaer
  • Patent number: 5393869
    Abstract: Disclosed are peptides and salts thereof represented by general formul ##STR1## wherein R.sub.1 represents Ser or Aib; R.sub.2 represents Met or a naturally occurring hydrophobic amino acid; R.sub.3 represents Leu, Ser, Lys or an aromatic amino acid; R.sub.4 represents Gly or a D-.alpha.-amino acid; R.sub.5 represents Lys or Leu; R.sub.6 represents Met or a naturally occurring hydrophobic amino acid; R.sub.7 represents Glu or a basic amino acid; R.sub.8 represents Val or basic amino acid; R.sub.9 represents Trp or 2-(1,3-dithiolane-2-yl)Trp; R.sub.10 represents Arg or His; R.sub.11 represents Lys or His; R.sub.12 represents Lys, Gln or Leu; and R.sub.13 represents Phe or Phe-NH.sub.2 ; except that simultaneously R.sub.1 consists of Ser, R.sub.2 consists of Met, R.sub.3 consists of Leu, R.sub.4 consists of Gly, D-Ala or D-Pro, R.sub.5 consists of Lys, R.sub.6 consists of Met, R.sub.7 consists of Glu, R.sub.8 consists of Val, R.sub.9 consists of Trp, R.sub.10 consists of Arg, R.sub.11 consists of Lys and R.sub.
    Type: Grant
    Filed: September 25, 1991
    Date of Patent: February 28, 1995
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shizue Nakagawa, Tsunehiko Fukuda, Masahiro Kawase, Iwao Yamazaki
  • Patent number: 5387746
    Abstract: A novel hydrophobic surfactant-associated protein mixture, i.e., a SAP-6 proteins, has been isolated from pulmonary animal tissue. A small, novel pulmonary hydrophobic surfactant-associated SAP-6-Val protein having a molecular weight of about 6,000 daltons as determined by SDS-PAGE and about 3,500-4,000 daltons as determined by tricine-SDS-PAGE has been further isolated from the SAP-6 protein mixture. The amino acid residue compositions of the SAP-6-Val protein for human and bovine have been determined and disclosed. When a SAP-6-Val protein is combined with phospholipids, it enhances the surfactant-like activity of the phospholipids in lungs of animals and, therefore, uniquely imparts to the mixture significant pulmonary biophysical activity. Such a mixture results in enhanced adsorption of the phospholipids with properties similar to that of natural pulmonary surfactant material.
    Type: Grant
    Filed: November 12, 1992
    Date of Patent: February 7, 1995
    Assignee: Scios Nova Inc.
    Inventor: Jeffrey A. Whitsett
  • Patent number: 5384309
    Abstract: The invention in its broad aspects relates to peptide derivatives which are useful as inhibitors platelet function mediated by the GP llbllla receptor and for the prevention of thrombus formation. The compounds of this invention are shown by the following Formula I: ##STR1## and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: July 17, 1989
    Date of Patent: January 24, 1995
    Assignee: Genentech, Inc.
    Inventors: Peter L. Barker, John P. Burnier, Eugene D. Thorsett
  • Patent number: 5382569
    Abstract: Novel antagonists of endothelin are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, metabolic, endocrinological, neurological disorders, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, Raynaud's disease, percutaneous transluminal coronary angioplasty or restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, ischemic bowel disease, and diabetes.
    Type: Grant
    Filed: December 21, 1992
    Date of Patent: January 17, 1995
    Assignee: Warner-Lambert Company
    Inventors: Wayne L. Cody, Patricia DePue, Annette M. Doherty, John X. He, Michael D. Taylor
  • Patent number: 5382655
    Abstract: A process is disclosed for the solution chromatographic purification of cyclosporin A from a starting mixture containing one or more of cyclosporin A, B, C, other cyclosporin components that are more polar or more apolar than cyclosporin A, and other like contaminants, by heating the starting mixture or an evaporation residue thereof to a temperature from about 80.degree. C. to about 115.degree. C., melting the heated starting mixture, and carrying out solution chromatography of the melted material, suitably first in a 48:50:2 mixture of chloroform, dichloromethane, and ethanol, and then in a mixture of like proportions, of the solvents chloroform, ethylacetate, and ethanol.
    Type: Grant
    Filed: May 25, 1993
    Date of Patent: January 17, 1995
    Assignee: Biogal Gyogyszerarugyar RT
    Inventors: Tibor Szanya, Laszlo Hanak, Gyongyi Strbka, Edit Nagy, Istvan Melczer, Gyorgy Deak, Berta Mako, Anita Karczub, Janos Balint, Ferenc Radnai, Erno Karacxony, Csaba Hajdufi, Vilmos Keri, Gyula Marton, Judit Dencs, Janos Kelemen
  • Patent number: 5378803
    Abstract: Azole-fused peptides useful as Substance P antagonists and analgesics, for example ##STR1## wherein ##STR2## represents ##STR3## wherein X is O, S or NH and * is D, or as intermediates therefor are prepared by azole and peptide forming methods.
    Type: Grant
    Filed: July 10, 1992
    Date of Patent: January 3, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: Barry A. Morgan, Thomas D. Gordon, Philip E. Hansen, Jasbir Singh
  • Patent number: 5378691
    Abstract: New amino acid derivatives of the formula IR.sup.1 --C.sub.p H.sub.2p --(NH).sub.y --CO--NH--CHR.sup.2 --CO--Z--C.sub.m H.sub.2m --CO--NH--CHR.sup.3 --CR.sup.4 --(CHR.sup.5).sub.n --CO--E--Q--Y Iin which R.sup.1 to R.sup.5, p, y, Z, m, n, E, Q and Y have the meanings defined herein, and the salts thereof, inhibit the activity of human plasma renin.
    Type: Grant
    Filed: August 15, 1994
    Date of Patent: January 3, 1995
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Peter Raddatz, Joachim Gante, Johannes Sombroek, Claus J. Schmitges, Klaus-Otto Minck
  • Patent number: 5378689
    Abstract: Compounds of formula (I): ##STR1## [in which: R.sup.1 is heterocyclic group having 5 or 6 ring atoms, or --NR.sup.7 R.sup.8, where R.sup.7 is alkyl and R.sup.8 is optionally substituted phenyl, optionally substituted phenylalkyl or cycloalkyl; R.sup.2 is optionally substituted phenyl or naphthyl; R.sup.3 is thiazolyl; R.sup.4 is cyclohexyl or isopropyl; R.sup.5 is alkyl; and R.sup.6 is alkyl] and salts thereof have renin-inhibitory and, hence, hypotensive activities and are of value in the diagnosis and treatment of hypertension induced by failures in the renin-angiotensin system. They may be prepared by reacting together appropriate amino acids or derivatives thereof.
    Type: Grant
    Filed: July 28, 1993
    Date of Patent: January 3, 1995
    Assignee: Sankyo Company, Limited
    Inventors: Yasuhiro Morisawa, Mitsuru Kataoka, Yuichiro Yabe, Hiroyuki Koike, Hidekuni Takahagi, Yasuteru Iijima, Tatsuo Kokubu, Kunio Hiwada
  • Patent number: 5378690
    Abstract: Oligopeptides of formula (I): ##STR1## where R.sup.1 -R.sup.5 are various organic groups, and A represents a group of formula --NH-- or --(CH.sub.2).sub.n --, in which n represents an integer of from 1 to 3, have renin-inhibitory activity and are particularly suitable for oral administration. They may be prepared by condensing their component amino acids or lower oligopeptides using conventional peptide synthesis reactions.
    Type: Grant
    Filed: July 30, 1993
    Date of Patent: January 3, 1995
    Assignee: Sankyo Company, Limited
    Inventors: Yasuhiro Morisawa, Mitsuru Kataoka, Yuichiro Yabe, Yasuteru Iijima, Hidekuni Takahagi, Hiroyuki Koike, Tatsuo Kokubu, Kunio Hiwada
  • Patent number: 5378807
    Abstract: A method is disclosed for significantly diminishing the rate of degradation of naturally-produced .gamma.-PGA in a .gamma.-PGA-producing cell culture. Also, a method is disclosed for significantly decreasing the water solubility coefficient of naturally-produced .gamma.-PGA by forming derivatives of .gamma.-PGA. In addition, a polymer solution is disclosed which includes a polysaccharide component and a .gamma.-PGA component.
    Type: Grant
    Filed: February 7, 1992
    Date of Patent: January 3, 1995
    Assignee: University of Massachusetts at Lowell
    Inventors: Richard A. Gross, Stephen P. McCarthy, Devang T. Shah
  • Patent number: 5376638
    Abstract: Methods for treating conditions associated with elevated, inappropriate or undesired renin activity are disclosed which comprise administration of an effective amount of any amylin antagonist alone or in conjunction with other anti-hypertensive agents. Methods for screening for and/or evaluating anti-renin amylin antagonists are also described.
    Type: Grant
    Filed: September 1, 1992
    Date of Patent: December 27, 1994
    Assignee: Amylin Pharmaceuticals, Inc.
    Inventors: Andrew A. Young, Timothy J. Rink
  • Patent number: 5376369
    Abstract: This invention is directed to an adjuvant composition in the form of an emulsion which is comprised of an emulsion-forming amount of a non-toxic tetra-polyol or of a POP-POE block polymer and an immunopotentiating amount of a muramyldipeptide of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, where R and R.sub.1 are each independently H or acyl of 1 to 22 carbon atoms, R.sub.2 is optionally substituted alkyl or optionally substituted aryl, R.sub.3 is H, alkyl, or aryl, R.sub.4 is H or lower alkyl, X is L-alanyl, L-.alpha.-aminobutyryl, L-arginyl, L-asparginyl, L-aspartyl, L-cysteinyl, L-glutaminyl, L-glutamyl, glycyl, L-histidyl, L-hydroxyprolyl, L-isoleucyl, L-leucyl, L-lysyl, L-methionyl, L-ornithinyl, L-phenylalanyl, L-prolyl, L-seryl, L-threonyl, L-tyrosyl, L-tryptophanyl, or L-valyl, and Y is D-glutamine, D-isoglutamine or D-isoasparagine. This invention is also directed to a vaccine containing an antigen and an adjuvant composition of the invention.
    Type: Grant
    Filed: February 8, 1990
    Date of Patent: December 27, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Anthony C. Allison, Noelene E. Byars, Cherng-Chyi Fu, Deborah M. Lidgate, Philip L. Felgner, Linda C. Foster, William A. Lee