Abstract: The invention relates to new comoounds having a cognition adjuvant action, to the use of ACE inhibitors as medicaments having a cognition adjuvant action, to agents containing them, and to the use thereof for the treatment and prophylaxis of cognitive dysfunctions.
Type:
Grant
Filed:
June 7, 1991
Date of Patent:
July 27, 1993
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Franz Hock, Josef Scholtholt, Hansjorg Urbach, Rainer Henning, Ulrich Lerch, Wolf-Ulrich Nickel, Wolfgang Ruger
Abstract: The invention relates to a method for the treatment of cardiac and of vascular hypertrophy and hyperplasia by administration of angiotensin converting enzyme inhibitors. Administration of compounds of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 are identical or different and each is hydrogen or an organic radical, and R.sup.4 and R.sup.5 form, together with the atoms carrying them, a mono-, bi- or tricyclic heterocyclic ring system, is preferred. The invention additionally relates to angiotensin converting enzyme inhibitors and to agents containing these for administration for the treatment of the abovementioned diseases.
Type:
Grant
Filed:
August 9, 1990
Date of Patent:
July 27, 1993
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Wolfgang Linz, Bernward Scholkens, Wolfgang Scholz, Gabriele Wiemer, Hansjorg Urbach, Rainer Henning, Volker Teetz
Abstract: Non-peptidyl compounds characterized generally as aminoalkylaminocarbonyl aminodiol derivatives of amino acids are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is independently selected from hydrido, methyl, ethyl, t-butyloxycarbonyl; and methoxymethylcarbonyl; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, phenethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.sub.7 is cyclohexylmethyl; wherein R.sub.8 is isobutyl; wherein each of R.sub.11 and R.sub.12 is hydrido; wherein m is zero or one and n is a number selected from zero through five; or a pharmaceutically-acceptable salt thereof; with the proviso that where m is zero, then R.sub.
Abstract: Congestive heart failure is treated by administration of a selective inhibitor of neutral endopeptidase and an angiotensin converting enzyme inhibitor. Captopril, fosinopril sodium, enalapril maleate and lisinopril are the preferred angiotensin converting enzyme inhibitors and the mercapto compounds of the formula ##STR1## are the preferred selective inhibitors of neutral endopeptidase.
Abstract: A novel hexapeptide is disclosed which has ligand binding specificity of the leukocyte response integrin expressed by human neutrophils and that has the following amino acid sequence ##STR1##
Type:
Grant
Filed:
April 9, 1992
Date of Patent:
July 6, 1993
Assignee:
Washington University
Inventors:
Hattie D. Gresham, Steven P. Adams, Eric J. Brown
Abstract: A biologically active peptide which includes the following structure:R.sub.1 -R.sub.1 -R.sub.1 -R.sub.4 -R.sub.1 -R.sub.1 -R.sub.2 -R.sub.1 -R.sub.1 -R.sub.1 -R.sub.1 -R.sub.1 -R.sub.1 -R.sub.1a -R.sub.1 -R.sub.1 -R.sub.3 -R.sub.2 R.sub.2 -R.sub.1aR.sub.1 and R.sub.1a are hydrophobic amino acids, R.sub.2 is a basic hydrophilic amino acid, R.sub.3 is a neutral hydrophilic amino acid, and R.sub.4 is hydrophobic or basic hydrophilic amino acid. Preferably, R.sub.1a is cysteine.Examples of peptides have the following structural formulae:(SEQ ID NO:1);(SEQ ID NO:2);(SEQ ID NO:3);(SEQ ID NO:4);(SEQ ID NO:5); and(SEQ ID NO:6).The peptide may be employed in a pharmaceutical composition.
Type:
Grant
Filed:
April 15, 1991
Date of Patent:
July 6, 1993
Assignee:
The Children's Hospital of Philadelphia
Inventors:
Michael Zasloff, W. Lee Maloy, U. Prasad Kari, Michael Brasseur
Abstract: Polypeptide useful for the preparation of antimalarial vaccines and of diagnostic kits for the detection of antisporozoite antibodies in clinical samples of malariated persons, constituted by: a synthetic peptide, which repeates the region I of P. falciparum and by a variable number of repetitive tetrapeptide units of CS protein of P. falciparum linked to each other by an amidic bond between the tail proline of I region and the head asparagine of the first tetrapeptide.
Type:
Grant
Filed:
December 4, 1991
Date of Patent:
July 6, 1993
Assignee:
Eniricerche S.p.A.
Inventors:
Adriano Bernardi, Fabio Bonelli, Antonello Pessi, Antonio S. Verdini
Abstract: The following oligopeptides containing -Asp-Gly- or -Asp-Ser- are synthesized:H-Asp-Gly-Lys-OHH-Ser-Asp-Gly-Lys-OHH-Asp-Ser-Asp-Gly-Lys-OHH-Ala-Asp-Ser-Asp-Gly-Lys-OHThe oligopeptides have antiallergic, vasodilating and immunoregulating activities and are very useful for treating allergic symptoms.
Abstract: A composition comprising a biologically active amphiphilic ion channel-forming peptide or ion channel forming protein and a toxic cation, such as a silver cation. Such compositions may be employed as pharmaceuticals, particularly for the treatment and prevention of eye infections.
Abstract: N-substituted amides which inhibit hydrolysis of elastin, are described, which compounds are tri-and di- fluoromethyl ketone amide and non-naturally occurring n-substituted amino acids derivatives.
Type:
Grant
Filed:
April 16, 1991
Date of Patent:
June 22, 1993
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: Polyaspartic acid having a weight average molecular weight of 1000 to 5000 is produced by hydrolysis of anhydropolyaspartic acid. Anhydropolyaspartic acid is produced by condensation polymerization of L-aspartic acid. Greater than 80% conversion is achievable utilizing "temperature vs time" profiles.
Type:
Grant
Filed:
February 22, 1991
Date of Patent:
June 22, 1993
Assignee:
Donlar Corporation
Inventors:
Larry P. Koskan, Kim C. Low, Abdul R. Y. Meah, Anne M. Atencio
Abstract: Peptides which exhibit improved broad spectrum antimicrobial activity are designed and synthesized based on the peptide sequences of magainin or PGS peptides. The modified peptide analogues are synthesized by replacing low helical potential amino acid residues with high helical potential residues and modifying the two termini in order to enhance the amphiphilic structures as well as to prolong antimicrobial activity by lowering their susceptibility to protease degradation. For example, low propensity residues within a strategic region of magainin II, e.g. Ser.sup.8, Gly.sup.13 and Gly.sup.18 are modified with Ala which is known to have high propensity. Amidation of Ser.sup.23, and acylation of Gly.sup.1 with acetyl or beta-alanyl and substitution of Gly.sup.1 with beta-alanine are carried out in order to lower the susceptibility to exopeptidase action.
Type:
Grant
Filed:
December 6, 1988
Date of Patent:
June 22, 1993
Assignee:
The United States of America as represented by the Department of Health and Human Services
Inventors:
Hao-Chia Chen, Judith H. Brown, John L. Morell, Charng-Ming Huang
Abstract: The invention is a process of manufacture, and a product manufactured by that process. The process comprises various steps. The steps include charging aspartic acid particles into a process unit and heating those particles to approximately 400.degree.-480.degree. F. As the aspartic acid particles are heated, vacuum is applied to that unit. Water is removed from the aspartic acid to form polyanhydroaspartic acid.
Abstract: The present invention provides methods for treating mammalian diseases and conditions characterized by myelin destruction. The present invention provides methods for inducing myelin formation by myelin forming cells expressing reovirus type 3 receptors comprising administering to such cells an effective amount of a compound bindable with the reovirus type 3 receptor. The compounds for use in the method of the invention preferably comprise antibodies and peptides, more preferably synthetic peptides.
Type:
Grant
Filed:
June 21, 1990
Date of Patent:
June 15, 1993
Assignee:
Trustees of the University of Pennsylvania
Inventors:
Jeffrey A. Cohen, Mark I. Greene, William V. Williams
Abstract: This invention relates to new gem-diamino derivatives of general formula (I) ##STR1## where R is the side chain of an amino acid, of which any functional groups are suitably protected, andX is an acyl group chosen from the group consisting of 2-nitrobenzoyl, 4-chloro-butyryl, acetoacetyl, 4-bromo-butyryl, (2-nitrophenoxy)-acetyl and 2-methyl-2-(2'-nitro-phenoxy)propionyl, of use in introducing gem-diamino residues into retro-inverso peptides. The invention further relates to a method for the synthesis of retro-inverso peptides in which the gem-diamino residue or residues are introduced using the new compound (I).
Type:
Grant
Filed:
February 21, 1990
Date of Patent:
June 15, 1993
Assignees:
Eniricerche S.p.A., Sclavo S.p.A.
Inventors:
Laura Gazerro, Massimo Pinori, Antonio S. Verdini
Abstract: New analogues of thymopentin (TP5) and of its tetrapeptide fragment (TP5.sup.1-4) containing two non-contiguous retro-inverted bonds in the peptide chain are described which are of the general formula (I) ##STR1## where R is hydrogen or an acyl radical, and R.sup.1 is an --OR.sup.2 group or an ##STR2## group where R.sup.2 is a hydrogen atom or a hydrocarbon radical, and R.sup.3 is a hydrogen atom or a hydroxyl group, and the corresponding pharmaceutically acceptable salts of acid or basic addition, possess immunomodulating activity.
Type:
Grant
Filed:
November 26, 1991
Date of Patent:
June 8, 1993
Assignee:
Sclavo S.p.A.
Inventors:
Sabina Mariotti, Alessandro Sisto, Luciano Nencioni, Luigi Villa, Antonio S. Verdini
Abstract: A method of treating cancer in a human patient, the method involving administering to the patient a cancer cell inhibiting amount of an analog of a naturally occurring biologically active peptide or a fragment thereof, the peptide being one of mammalian gastrin-releasing peptide, neuromedin B, neuromedin C, amphibian bombesin, or litorin.
Type:
Grant
Filed:
May 9, 1990
Date of Patent:
June 8, 1993
Assignee:
Biomeasure, Inc.
Inventors:
Arthur E. Bogden, Jacques-Pierre Moreau
Abstract: Disclosed is a novel polypeptide useful as a leader or trailer peptide moiety in recombinant DNA protein production techniques involving fused protein methodology The polypeptide comprises an amphiphilic helix designed at the DNA level to have hydrophilic charged amino acid residues on one side of the barrel of the helix and nonpolar amino acid residues on the other side of the barrel of the helix. When DNA encoding the helix is attached to a gene encoding a protein of interest, high level expression is achieved and inclusion bodies are spontaneously formed. The inclusion bodies may be collected and purified easily by altering the ionic strength and/or pH of media used to dissolve the inclusion bodies. After purification, the fused protein is cleaved to separate the amphiphilic helix from the product.
Type:
Grant
Filed:
March 25, 1992
Date of Patent:
June 1, 1993
Assignee:
Creative BioMolecules, Inc.
Inventors:
Peter C. Keck, Charles M. Cohen, James S. Huston, Richard J. Ridge