Abstract: Disclosed are a peptide represented by formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein M represents a mercaptoacyl group; P, Q, R, S, T, U, V, W, X, Y and Z each represent amino acid residues, wherein an amino acid side chain of Y is either a substituted saturated aliphatic hydrocarbon group having 1 to 15 carbon atoms or an unsubstituted saturated aliphatic hydrocarbon group having 4 to 15 carbon atoms other than (1S)-1-methylpropyl; (2) a method for producing the above-mentioned peptide or the salt thereof, which comprises subjecting a peptide represented by formula (II) or a salt thereof to an oxidation reaction:M-P-Cys-Q-R-S-T-Asp-U-Glu-Cys-Val-Tyr-V-Cys-His-W-X-Y-Ile-Z-OH(II)wherein M, P, Q, R, S, T, U, V, W, X, Y and Z are as diefined above; and (3) use of the above-mentioned peptide or the pharmaceutically acceptable salt thereof as an anti-endothelin agent.
Abstract: A medicament for prevention and remedy of diseases caused by the infection of viruses is disclosed, which is characterized by containing as an effective ingredient thereof a nonapeptide having the following amino acid configuration:pGlu-Ala-Lys-Ser-Gln-Gly-Gly-Ser-Asn or an ester and an amide at the carboxyl group of the C-terminal of the asparagine or a pharmacologically acceptable salt thereof.
Abstract: An enteric formulation for a proteinous drug which protects it from enzymatic degradation and promotes its uptake by the intestinal tract when administered orally, comprises either a solid mass of an intimate mixture of the drug, a nontoxic nonionic surfactant, and an enteric material, or a solid mass of an intimate mixture of the drug with the nonionic surfactant covered by a discrete enteric coating.
Abstract: Disclosed is a novel peptide having one of the formulae: ##STR1## (A and B are the amino acids: wherein if A is D- or L-Pro, B is Hat or Cit;if A is D-Pro, B is D-Arg, andif B is D- or L-Arg, A is Sat, Pip, Aze or Arg)Asn-A-L- (D-)Pro-Arg- (Gly)n (A is Set, Thr or Ala, n is 1 or 0)A-Ser-Pip-Arg (A is Pro-Asn-, Asn- or Pro-) ##STR2## (A is cyclopentylcarbonyl, Pro or pGlu; B is Gly or .beta.-Ala, W is a hydrogen atom or a group having the formula:or a peptide having the formula: ##STR3## wherein A and B have the same meanings as mentioned above, respectively pGlu-Asn-Ser-A-B-(Gly)n (A is Aze, D- or L-Pro, Pip or Sat, B is D- or L-Arg, Cit, Hat, Lys or Orn, n is 1 or 0) andPro- (Ash)m-Set-L- (D-)Pro-Arg- (Gly) n (m and n are independently 0 or 1)their functional derivatives, and pharmaceutically acceptable salts thereof.
Abstract: Methods and compositions for (a) improving and/or maintaining the health of skin, and (b) increasing subcutaneous fat in warm-blooded animals are disclosed. The methods utilize an effective amount of a composition comprising GHL--Cu or a derivative of GHL--Cu.
Abstract: Treatment and prophylaxis of endotoxin caused toxicity is disclosed. This is accomplished by administering a lipid into which the endotoxin of concern is associated, preferably together with a peptide which is not an apolipoprotein. Preferably, the two components are administered in the form of a reconstituted particle, although this is by no means required.
Type:
Grant
Filed:
August 12, 1992
Date of Patent:
September 6, 1994
Assignee:
The Rogosin Institute
Inventors:
Daniel M. Levine, Thomas S. Parker, Albert L. Rubin
Abstract: Peptide analog type-B CCK receptor ligands or pharmaceutically-acceptable salts thereof, which are useful for treating central nervous system disorders, substance abuse, gastrointestinal disorders, endocrine disorders, eating-related disorders and for the treatment of shock, respiratory and cardiocirculatory insufficiencies.
Type:
Grant
Filed:
January 29, 1993
Date of Patent:
August 23, 1994
Assignee:
Abbott Laboratories
Inventors:
Kazumi Shiosaki, Alex M. Nadzan, David S. Garvey, Youe-Kong Shue, Mark S. Brodie, Mark W. Holladay, John Y.-L. Chung, Michael D. Tufano, Paul D. May
Abstract: The present invention comprises fibrinogen receptor antagonist compounds, compositions containing them and methods for using them to inhibit fibrinogen binding to blood platelets. Compounds of the invention have the following formula ##STR1## wherein Z is ##STR2## X is COOH, CH.sub.2 SH or SH; R.sup.1 is Y--R.sup.3, wherein R.sup.3 is alkyl and Y is amino, pyridinyl, pyrimidinyl or piperidinyl;R.sup.2 is H, alkyl, aryl, or arylalkyl; andR.sup.4 is alkyl, heteroalkyl, aryl or heteroaryl, wherein the aryl or heteroaryl group can be mono- or bi-cyclic.
Abstract: A fibrinogen receptor antagonist of the formula ##STR1## wherein XX represents a synthetic alpha-amino acid containing a linear side chain and ZZ represents a sequence of 1, 2, 3 or 4 amino acids.
Type:
Grant
Filed:
September 21, 1992
Date of Patent:
August 16, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Ruth F. Nutt, Stephen F. Brady, Daniel F. Veber, Mark E. Duggan
Abstract: A novel peptide, polydiscamide A, has been isolated from a marine sponge. This compound, and its derivatives, are useful as antibacterial agents.
Type:
Grant
Filed:
February 7, 1992
Date of Patent:
August 9, 1994
Assignee:
Harbor Branch Oceanographic Institution, Inc.
Inventors:
Nanda K. Gulavita, Sarath P. Gunasekera, Shirley A. Pomponi, Ross E. Longley, Peter J. McCarthy
Abstract: The subject invention relates to a peptide having the amino acid sequence Glu-Ile-Cys-Thr-Glu-Met-Glu-Lys-Glu-Gly-Lys-Ile-Ser-Lys-Ile-Gly-Pro or portions thereof. This peptide is derived from, or based upon, a region of a relatively conserved epitope of HIV-1 reverse transcriptase. The peptide may be utilized in the treatment of patients having human immunodeficiency virus or in the prevention of infection of those individuals who have been exposed to the disease, yet have not become sero-positive. The preparation containing the peptide may be administered either subcutaneously, intramuscularly or intravenously.
Type:
Grant
Filed:
March 9, 1990
Date of Patent:
August 9, 1994
Assignee:
The United States of America as represented by the Department of Health and Human Services
Inventors:
Jay A. Berzofsky, Anne Hosmalin, Mario S. Clerici, Ronald N. Germain, Gene Shearer, Bernard Moss, Charles D. Pendleton
Abstract: Described are the use of hexopyranose compounds of the formula I ##STR1## for the prophylaxis and treatment of virus infections, and novel pharmaceutical preparations especially suitable for the use in accordance with the invention.The substituents in formula I have the meanings given in the claims.
Abstract: Compounds of the formula I ##STR1## in which X denotes a hydrogen atom, a group which irreversibly masks the terminal amino group, or a protecting group which is conventional in peptide chemistry, such as, for example, Boc-, Z- or Fmoc-,A and B may be identical or different and denote an alpha- beta- or gamma-amino acid which comprises 2 to 15 carbon atoms and up to 4 nitrogen atoms, 2 sulfur atoms and 6 oxygen atoms and whose side chain may be substituted, and B, if appropriate, denotes a dipeptide formed from these amino acids,C denotes arginine, Lysine, tyrosine, phenylalanine or tryptophane, and their homologs,R.sub.1 and R.sub.2 are identical or different and denote a hydrogen atom or an alkyl radical having up to 4 carbon atoms,R.sub.3 to R.sub.8 are identical or different and denote hydrogen, an alkyl radical, an alkoxy radical or a halogen radical,Y denotes oxygen, andAn.sup.- denotes an anion, and their water-soluble salts, and a process for their preparation are described.
Abstract: Synthetic polypeptides corresponding to the B lymphocyte CR2 receptor binding site present on a CR2 ligand are disclosed together with polypeptide aggregates, compositions, anti-polypeptide antibodies and methods of preparing and using the polypeptides and antibodies.
Type:
Grant
Filed:
September 8, 1989
Date of Patent:
July 19, 1994
Assignee:
California Institute of Biological Research
Abstract: A process of preparation of collagen containing in major proportion insoluble collagen is disclosed, including rinsing and washing the collagenic tissue, acidifying the ground material pH value 1 to 4 to get a collagenic paste which is diluted in a diluting solution to get the collagen gel having a concentration in collagen lower than about 2.5 by weight expressed in dry collagen, and performing a shearing stirring at high speed producing ultrasonic effect to get a substantially homogeneous collagenic gel. The collagen has improved mechanical resistance and thermal stability.
Abstract: Disclosed are novel peptide and pseudopeptide derivatives and pharmaceutical compositions thereof that inhibit platelet aggregation and thrombus formation in mammalian blood.
Type:
Grant
Filed:
October 15, 1992
Date of Patent:
July 12, 1994
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Abstract: Human Neuropeptide Y (NPY) has the formula: H-Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu-Asp-Ala-Pro- Ala-Glu-Asp-Met-Ala-Arg-Tyr-Tyr-Ser-Ala-Leu-Arg-His-Tyr-Ile-Asn-Leu-Ile- Thr-Arg-Gln-Arg -Tyr-NH.sub.2. Porcine and rat NPY have the same sequence except for Leu instead of Met in the 17-position. Porcine PYY is homologous having 11 different residues. NPY analogs and N-terminally-shortened fragments, e.g. NPY(18-36), which contain one or more specific D-isomer substitutions for the naturally occurring residues (as well as pharmaceutically acceptable salts thereof), dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals, including humans, to substantially lower blood pressure over an extended period of time or to counteract hypertension.
Type:
Grant
Filed:
May 12, 1992
Date of Patent:
July 12, 1994
Assignees:
The Salk Institute for Biological Studies, The Regents of the University of California
Inventors:
Jaroslav H. Boublik, Jean E. F. Rivier, Marvin R. Brown, Neal A. Scott