Abstract: The present invention relates to novel peptides which have hemoregulatory activities and can be used to inhibit the myelopoietic system of humans and animals.
Type:
Grant
Filed:
May 25, 1994
Date of Patent:
June 2, 1998
Assignee:
SmithKline Beecham Corporation
Inventors:
Pradip Kumar Bhatnagar, William Francis Huffman
Abstract: This invention discloses that certain fragments of a pulmonary surfactant protein exhibit unexpected surface activity. These protein fragments are useful in preparing formulations for the treatment of respiratory distress syndrome.
Abstract: Somatostatin peptides bearing at least one chelating group for a detectable element, said chelating group being linked to an amino group of said peptide, and said amino group having no significant binding affinity for somatostatin receptors, in free or salt form, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of somatostatin receptor positive tumors or for therapy.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
May 19, 1998
Assignee:
Novartis AG
Inventors:
Rainer Albert, Eric P. Krenning, Steven W. J. Lamberts, Janos Pless
Abstract: A compound of the formulaR.sup.1 --A.sup.2 --A.sup.1 -Asp-p-nitroanilidewherein:A.sup.1 is a residue of any of the naturally occurring .alpha.-amino acids or a homolog, analog or derivative of a natural .alpha.-amino acid;A.sup.2 is a residue of a lipophilic .alpha.-amino acid;R.sup.1 is alkylcarbonyl, phenalkylcarbonyl, alkoxycarbonyl, phenalkoxycarbonyl, alkylaminocarbonyl, phenalkylaminocarbonyl or R.sup.2 --A.sup.3 whereinA.sup.3 is a residue of a lipophilic .alpha.-amino acid; andR.sup.2 is alkylcarbonyl, alkoxycarbonyl or phenylalkoxycarbonyl, anda method of detecting inhibitors of interleukin 1.beta. converting enzyme (ICE) comprising evaluating a test compound's capacity to inhibit the ICE-induced hydrolysis of a compound of the formula I. The greater the ability of a test compound to inhibit such hydrolysis, the greater its expected activity in treating inflammation as well as diseases whose pathogenesis is induced or sustained by interleukin-1.beta..
Abstract: This invention pertains to cyclic polypeptides having gastrointestinal motor stimulating activity which may be represented by formula (1): ##STR1## including optically active isomeric forms and the pharmaceutically acceptable acid addition salts thereof, wherein groups A and D are linked to from a cyclic structure; and R.sub.1 is lower alkyl; R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is phenyl or substituted phenyl, wherein the phenyl group may be substituted with one or more substituents selected from the group consisting of halogen, hydroxy, and lower alkoxy; R.sub.5 is --OH or --NH.sub.2 ; A is selected from the group consisting of L-glutamic acid, L-aspartic acid, L-lysine, L-ornithine, and L-2,4-diaminobutyric acid; B is L-alanine or L-glutamine; C is L-arginine or D-arginine; D is selected from the group consisting of L-lysine, L-ornithine, L-2,4-diaminobutyric acid, L-glutamic acid, and L-aspartic acid; E is a direct bond between group D and group R.sub.
Type:
Grant
Filed:
May 16, 1996
Date of Patent:
March 31, 1998
Assignee:
Ohmeda Pharmaceutical Products Division Inc.
Inventors:
Ramalinga Dharanipragada, Mark J. Macielag, Jung Kim-Dettelback, James Florance
Abstract: Antagonists of neurokinin A which are derivatives of naturally occurring neurokinin A in which the amide bond connecting the two amino acids on the carboxy terminal end is modified are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which neurokinin A is implicated is also described.
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 12, 1995
Date of Patent:
March 17, 1998
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
Abstract: Cyclized integrin receptor antagonist compounds useful in modulating cell adhesion, including adhesion related to fibronectin, as well as leukocyte adhesion to endothelial cells, are disclosed. Methods for synthesizing, testing, formulating, and using the compounds as therapeutic agents are also disclosed.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
February 24, 1998
Assignee:
Tanabe Seiyaku Co., Ltd.
Inventors:
Thomas J. Lobl, Shiu-Lan Chiang, Pina M. Cardarelli
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 17, 1995
Date of Patent:
February 17, 1998
Assignee:
Eli Lilly and Company
Inventors:
Richard D. DiMarchi, Ronald N. Hermeling, James A. Hoffmann
Abstract: There are disclosed alpha-helix mimetics and methods relating to the same for imparting or stabilizing alpha-helicity to a peptide or protein. In one aspect, the alpha-helix mimetics contain six- or seven-membered rings covalently attached at the end or within the length of the peptide or protein. The alpha-helix mimetics render the resulting peptide or protein more stable with regard to thermal stability, as well as making the peptide or protein more resistant to proteolytic degredation. In addition, the alpha-helix mimetics may be used in standard peptide synthesis protocols.
Abstract: The invention relates to compounds which are antagonists of endothelin, to processes for their preparation, and to their use as pharmaceuticals. The compounds of the invention are Useful in the treatment of hypertension, pulmonary hypertension, Reynaud's disease, myocardial infarction, angina pectoris, acute renal failure, cerebral infarction, cerebral vasospasm, arteriosclerosis, asthma, endotoxin shock, endotoxin-induced multiple organ failure or disseminated intravascular coagulation, and/or cyclosporin-induced renal failure or hypertension.
Abstract: The DNA encoding the cell surface receptor for thrombin has been cloned and sequenced. The availability of this DNA permits the recombinant production of thrombin receptor which can be produced at cell surfaces and is useful in assay systems both for the detection of thrombin and for the evaluation of candidate thrombin agonists and antagonists. Further, the elucidation of the structure of the thrombin receptor permits the design of agonist and antagonist compounds which are useful diagnostically and therapeutically. The availability of the thrombin receptor also permits production of antibodies specifically immunoreactive with the receptor per se or with specific regions thereof which are also useful diagnostically or therapeutically.
Type:
Grant
Filed:
November 7, 1991
Date of Patent:
November 18, 1997
Assignee:
COR Therapeutics, Inc.
Inventors:
Shaun R. Coughlin, Robert M. Scarborough
Abstract: A polypeptide for use as an interferon receptor-binding peptide, said polypeptide selected from the group of peptides having an amino acid sequence substantially of the formulae; CYS-LEU-LYS-ASP-ARG-HIS-ASP; ASP-GLU-SER-LEU-LEU-GLU-LYS-PHE-TYR-THR-GLU-LEU-TYR-GLN-LEU-ASN-ASP; ASN-GLU-THR-ILE-VAL-GLU-ASN-LEU-LEU-ALA-ASN-VAL-TYR-HIS-GLN-ILE-ASN-HIS; TYR-LEU-THR-GLU-LYS-LYS-TYR-SER-PRO-CYS-ALA; TYR-PHE-GLN-ARG-ILE-THR-LEU-TYR-LEU-THR-GLU-LYS-LYS-TYR-SER-PRO-CYS-ALA; TYR-PHE-GLN-ARG-ILE-THR-LEU-TYR; and GLU-LEU-TYR-GLN-GLN-LEU-ASN-ASP. The polypeptides are useful for delivering a pharmaceutically active drug to a cell.
Abstract: The present invention describes polypeptides and anti-peptide antibodies capable of inhibiting serine protease enzymatic activity. In particular, polypeptides and anti-peptide antibodies derived from the blood coagulation serine proteases Factor VIIa, Factor IXa, Factor Xa, Factor XIa, thrombin and plasma kallikrein are described that are capable of inhibiting coagulation. The polypeptide and antibody are useful in methods and systems for inhibiting serine proteases, and particularly for inhibiting blood coagulation processes mediated by serine proteases in vitro or in a human patient.
Abstract: Opioid peptides including those of the formula ##STR1## in which A.sub.1 is the identifying group of an amino acid selected from 3,4-dihydroxyphenylalanine, 3,4-dimethoxyphenylalanine, azatyrosine, and 2,6-dimethyltyrosine; A.sub.2 is the identifying group of an amino acid selected from D-Ala and D-Arg; A.sub.3 is H, or the identifying group of an amino acid selected from of 3,4-dihydroxyphenylalanine and 3,4-dimethoxyphenylalanine, A.sub.4 is H, cyclohexylmethyl, the identifying group of an amino acid selected from 3,4-dihydroxyphenylalanine, 3,4-dimethoxyphenylalanine, Phe, and substituted Phe with its benzene ring substituted by halogen, NO.sub.2, OH, or CH.sub.3 ; A.sub.5 is the identifying group of a D- or L-amino acid selected from Leu, Nle, Lys, Met and Met(O), or is deleted together with R.sub.4 --CH attached thereto; each R.sub.1 and R.sub.2 is --H, --C(NH.sub.2).dbd.NH, or C.sub.1-12 alkyl; R.sub.3 is ##STR2## R.sub.4 is ##STR3## and R.sub.5 is --(CH.sub.2).sub.
Type:
Grant
Filed:
December 8, 1994
Date of Patent:
September 2, 1997
Assignee:
Biomeasure Inc.
Inventors:
Jacques-Pierre Moreau, Sun Hyuk Kim, John E. Taylor
Abstract: Novel peptides of the formula A.sub.1 -A.sub.2 -Ala-Trp-DPhe-A.sub.5 are disclosed which promote the release of growth hormone when administered to animals. These peptides can be used therapeutically.
Type:
Grant
Filed:
August 22, 1991
Date of Patent:
September 2, 1997
Assignee:
Administrators of the Tulane Educational Fund
Abstract: An N-terminal substituted peptide or protein having the formula: ##STR1## X is a biologically active amphiphilic ion channel-forming peptide or protein. T is a lipophilic moiety, and preferably, T is: ##STR2## wherein R is a hydrocarbon (alkyl or aromatic or alkylaromatic) having at least 2 and no more than 10 carbon atoms. T is preferably an octanoyl group. W is T or hydrogen. The N-terminal substituted peptides and proteins have improved biological activity against target cells, viruses, and vitally-infected cells.
Abstract: Methods of use of compounds and compositions comprising fragments and synthetic analogs of human thrombospondin are provided for promoting or inhibiting thrombospondin-like activity.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
August 5, 1997
Assignees:
W. R. Grace & Co.-Conn., The Medical College of Pennsylvania
Inventors:
Jacob Eyal, Bruce King Hamilton, George Paul Tuszynski
Abstract: Amnestic novel peptides are disclosed. A topographical map or surface which includes binding sites for peptides having amnestic procedures and the use of such surface to identify and synthesize such peptides is also disclosed.