Patents Examined by A. M. Davenport
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Patent number: 5262519Abstract: The invention provides synthetic peptides which are extremely potent in stimulating the release of pituitary GH in animals, including humans and also resist enzymatic degradation in the body. Certain preferred peptides have the formula:(B)R.sub.1 -Ala-Asp-Ala-Ile-Phe-Thr-R.sub.8 -Ser-Tyr-Arg-Lys-Val-Leu-R.sub.15 -R.sub.16 - Leu-Ser-Ala-Arg-Lys-Leu-Leu-R.sub.24 -R.sub.25 -Ile-Nle-R.sub.28 -Arg-Y wherein R.sub.1 is Tyr, D-Tyr, Phe, D-Phe, His or D-His; B is H or N.sup..alpha. Me; R.sub.8 is Ala, Aib or Asn; R.sub.15 is Gly or Ala; R.sub.16 is Ala, Aib or Gln; R.sub.24 is Ala, Aib or Gln; R.sub.25 is Ala, Aib or Asp; R.sub.28 is Ser or Asn; Y is NHR with R being H or lower alkyl; provided that at least one of R.sub.8, R.sub.16, R.sub.24 and R.sub.25 is Ala or Aib.Type: GrantFiled: May 15, 1991Date of Patent: November 16, 1993Assignee: The Salk Institute for Biological StudiesInventors: Jean E. F. Rivier, Wylie W. Vale, Jr.
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Patent number: 5244883Abstract: The novel pseudo polypeptides of this invention are potent bombesin antagonists. There are provided processes for their production, pharmaceutical compositions comprising said polypeptides and their use as pharmaceutically active agents. More particularly the present invention provides pseudopeptides comprising a nonapeptide moiety of formula I:X-A.sup.1 -A.sup.2 -A.sup.3 -A.sup.4 -A.sup.5 -A.sup.6 -A.sup.7 -A.sup.8 -.sub.psi -A.sup.9 -Qwherein Q is NH.sub.2 or OQ.sup.1 where Q.sup.1 is hydrogen, C.sub.1-10 alkyl, phenyl or phenyl-C.sub.7-10 alkyl; X is hydrogen or a single bond linking to A.sup.2 the acyl residue of an organic acid, or a group of formula R.sup.1 CO-- wherein (1) R.sup.1 is hydrogen, C.sub.1-10 alkyl, phenyl or phenyl-C.sub.7-10 -alkyl; (2) R.sup.1 CO-- is (a) R.sup.2 N(R.sup.3)--CO-- wherein R.sup.2 is hydrogen, C.sub.1-10 alkyl, phenyl or C.sub.7-10 phenyl-C.sub.7-10 -alkyl, R.sup.3 is hydrogen or C.sub.1-10 alkyl; (b) R.sup.4 --O--CO-- wherein R.sup.4 is C.sub.Type: GrantFiled: November 29, 1990Date of Patent: September 14, 1993Assignee: The Administrators of the Tulane Educational FundInventors: Renzhi Cai, Andrew V. Schally
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Patent number: 5241053Abstract: Disclosed are (1) a fused protein comprising heat-labile enterotoxin B subunit and a protein heterologous to heat-labile enterotoxin, (2) a recombinant DNA containing a nucleotide sequence coding for the above fused protein, (3) a transformant harboring the above recombinant DNA, (4) a method for producing the fused protein which comprises cultivating the above transformant, producing and accumulating the above fused protein in a culture, and collecting the fused protein, and (5) a method for purifying a fused protein comprising a herpes simplex virus surface antigen and heat-labile enterotoxin B subunit, which comprises cultivating a transformant harboring a recombinant DNA containing a nucleotide sequence coding for the fused protein, producing an accumulating the fused protein in a culture, collecting the fused protein and subjecting the collected fused protein to purification processes comprising cationic exchange chromatography and gel permeation chromatography.Type: GrantFiled: September 5, 1990Date of Patent: August 31, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Yukio Fujisawa, Shuji Hinuma, Aki Mayumi, Tatsuo Yamamoto
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Patent number: 5236904Abstract: The present invention provides methods and compositions for inducing penile erections, sufficient for vaginal penetration, in a human male suffering from impotence. When the impotence is substantially only neurogenic, psycogenic or neurogenic and psychogenic, a method of the invention comprises (A) administering to the male by intracavernosal injection peptide N-terminal histidine C-terminal methionineamide and (B) sexually stimulating the male. When the impotence is caused by severe atherosclerosis, a method of the invention comprises (A) administering to the male by intracavernosal injection an amount of a physiologically acceptable composition comprising (1) a neuropeptide selected from the group consisting of human vasoactive intestinal peptide and peptide N-terminal histidine C-terminal methionineamide and (2) an alpha-adrenergic blocker, such as phentolamine or prazosin, and (B) sexually stimulating the male.Type: GrantFiled: September 18, 1989Date of Patent: August 17, 1993Assignee: Senetek, plcInventors: Thomas Gerstenberg, Jan Fahrenkrug, Bent Ottesen
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Patent number: 5227368Abstract: This invention provides a purified endotoxin-induced thrombosis factor, preferably an endotoxin-induced thrombosis factor characterized by an apparent molecular weight between about 50,000 and 65,000 daltons, more specifically about 55,000 daltons, on reduced and nonreduced SDS-polyacrylamide gels, by maximal recovery on elution from such gels at 52,000 to 58,000 daltons, by the ability to migrate as a single band on such gels, by the ability to precipitate in ammonium sulfate at saturations from 40% to 70%, by the ability to precipitate in polyethylene glycol at concentrations above 15%, by high hydrophobicity, by the ability to bind weakly to a hydroxylapatite column and to a lentil lectin column, by the ability to bind tightly to a hydrophobic interaction resin and smear off with ethylene glycol, and by the ability to bind tightly to a reverse-phase column and elute more effectively with isopropranol than with acetonitrile, by the ability to bind to an anion exchange resin over a pH range from 5 to 10, byType: GrantFiled: February 28, 1990Date of Patent: July 13, 1993Assignee: The Trustees of Columbia University in the City of New YorkInventors: Herwig Gerlach, David Stern
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Patent number: 5223485Abstract: Oligopeptide compounds or oligopeptide analogue compounds of the formula A-B-D-E-G-J-L-M-Q-T are ligands for the anaphylatoxin receptor and are useful in the treatment of inflammatory disease states. Also disclosed are anaphylatoxin receptor ligand compositions and a method for modulating anaphylatoxin activity.Type: GrantFiled: June 19, 1991Date of Patent: June 29, 1993Assignee: Abbott LaboratoriesInventors: Megumi Kawai, Yat S. Or, Paul E. Wiedeman, Jay R. Luly, Mikel P. Moyer
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Patent number: 5223487Abstract: 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.Type: GrantFiled: January 23, 1992Date of Patent: June 29, 1993Assignee: Hitachi Chemical Co., Ltd.Inventors: Keiichi Noguchi, Noriya Ohta, Daisuke Irie, Katsurou Matsuo, Kouhei Hirano, Asako Tokunaga, Fumio Ishikawa
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Patent number: 5219988Abstract: 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: GrantFiled: February 21, 1990Date of Patent: June 15, 1993Assignees: Eniricerche S.p.A., Sclavo S.p.A.Inventors: Laura Gazerro, Massimo Pinori, Antonio S. Verdini
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Patent number: 5218089Abstract: 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: GrantFiled: November 26, 1991Date of Patent: June 8, 1993Assignee: Sclavo S.p.A.Inventors: Sabina Mariotti, Alessandro Sisto, Luciano Nencioni, Luigi Villa, Antonio S. Verdini
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Patent number: 5216124Abstract: The present invention provides substituted cyclic tetrapeptide compounds of Formula I: ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, which are useful for treating pain in animals, pharmaceutical compositions which comprises a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: May 21, 1991Date of Patent: June 1, 1993Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Karen B. Peterson, Nizal S. Chandrakumar, Henry I. Mosberg
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Patent number: 5214030Abstract: A method of treating erectile dysfunctions in mammals and men, by administering to the mammal or man a pharmaceutical composition comprising a therapeutically effective amount of a calcitonin gene-related peptide.Type: GrantFiled: October 18, 1991Date of Patent: May 25, 1993Inventor: Georg Stief
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Patent number: 5214130Abstract: New immunosuppressive cyclosporin analogs are disclosed consisting of [dehydro-Ala].sup.8 cyclosporins and derived therefrom cyclosporins having a sulfur containing amino acid at position-8.Type: GrantFiled: August 12, 1991Date of Patent: May 25, 1993Assignee: Merck & Co., Inc.Inventors: Arthur A. Patchett, David Taub, Robert T. Goegelman
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Patent number: 5206221Abstract: An alkyl ester of dipeptide consisting essentially of natural or synthetic L-amino acids with hydrophobic side chains. Preferable amino acids are leucine, phenylalanine valine, isoleucine, alanine, proline, glycine or aspartic acid beta methyl ester. Preferable dipeptides are L leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-leucyl L-isoleucine, L-phenylalanyl L-phenylalanine, L-valyl L-leucine, L-leucyl L-alanine, L-leucine, L-leucyl L-valine, L-phenylalanyl L-valine, L glycyl L-leucine, L-leucyl L-glycine or L-aspartyl beta methyl ester L-phenylalaine. Most preferable dipeptides are L-leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-phenylalanyl L-leucine, L-leucyl L-isoleucine, L-phenylalanyl L-phenylalanine and L-valyl L-leucine.The alkyl ester of the dipeptide is most preferably a methyl ester and may also be an ethyl ester or alkyl of up to about four carbon atoms such as propyl, isopropyl, butyl or isobutyl.Type: GrantFiled: January 18, 1991Date of Patent: April 27, 1993Assignee: Board of Regents, The University of Texas SystemInventors: Peter E. Lipsky, Dwain L. Thiele
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Patent number: 5204446Abstract: A peptide having immunoreactivity with an antibody specific to a hepatitis B virus, containing one of the following amino acid sequences:(1) Asp-Cys-Val-Phe-Lys-Asp-Trp-Glu-Glu-Leu-Gly-Glu-Glu-Ile-Arg-Leu-Lys-Val-Ph e-Val-Leu-Gly-Gly-Cys,(2) Asp-Cys-Val-Phe-Lys-Asp-Trp-Glu-Glu-Leu-Gly-Glu-Glu-Ile-Arg-Leu-Met-Ile-Ph e-Val-Leu-Gly-Gly-Cys or(3) Asp-Cys-Leu-Phe-Lys-Asp-Trp-Glu-Glu-Leu-Gly-Glu-Glu-Ile-Arg-Leu-Lys-Val-Ph e-Val-Leu-Gly-Gly-Cys.Type: GrantFiled: April 2, 1990Date of Patent: April 20, 1993Assignee: Olympus Optical Co., Ltd.Inventors: Toshiaki Kumazawa, Masatoshi Osanai
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Patent number: 5202310Abstract: A cyclosporine metabolite having a molecular weight determined by mass spectrometry of about 1205 and having the following properties: (a) being immunologically distinct from cyclosporine metabolites OL-1, OL-17 and OL-8; (b) being more polar than OL-1 or OL-17 and less polar than OL-8 when eluated from a gradient high performance liquid chromatography; (c) being extractable from bile of test animals which have been administered cyclosporine A; and (d) being substantially free of other cyclosporine metabolites and cyclosporine A, and a physiologically acceptable salt or stereoisomer thereof.Type: GrantFiled: June 6, 1990Date of Patent: April 13, 1993Inventors: Gary A. Levy, Pui Y. Wong
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Patent number: 5202417Abstract: Disclosed is a novel polypeptide whose N-terminus is EAQ and which is composed of 60 amino acids. The polypeptide is produced from human breast cancer cell MCF7, or human gastric cancer cell MKN-45 or KATO-III, which polypeptide has a isoelectric point of 4.Type: GrantFiled: August 21, 1989Date of Patent: April 13, 1993Assignee: Takeda Chemical Industries, Ltd.Inventor: Kyozo Hayashi
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Patent number: 5200397Abstract: Compounds and compositions comprising fragments and synthetic analogs of human thrombospondin are provided together with methods for their use as thrombospondin-like agents.Type: GrantFiled: January 31, 1991Date of Patent: April 6, 1993Assignees: W. R. Grace & Co.-Conn., The Medical College of PennsylvaniaInventors: Alan H. Deutch, George P. Tuszynski
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Patent number: 5200504Abstract: The invention contemplates a metallopeptide and a method for producing the metallopeptide. The metallopeptide comprises a polypeptide bonded to a metal cation at two coordinating amino acid residues that are aqueous solvent-accessible, said metallopeptide having a secondary structure stabilized by said bonded metal cation.Type: GrantFiled: October 2, 1990Date of Patent: April 6, 1993Assignee: The Scripps Research InstituteInventor: Reza M. Ghadiri
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Patent number: 5200394Abstract: The invention synergimicin derivatives having the general formula: Z--X--R, in which Z is a type A or type B synergimycin radical linked by its reactive carbonyl position, through a branch X, where X is .dbd.N-- or .dbd.N--O--, to a substituted R, where R is a hydrogen atom, an alkyl group, an alkyl-COOH group, an -alkyl-(.alpha.NH.sub.2)COOH group (I), group (II), group (III) or a group (IV), where n is a function of the number of --NH.sub.2 groups present on the coupling protein. Also described are the salts, esters and possibly addition products of pharmaceutically acceptable acids. The invention also concerns a process for preparing these substances, and their use.Type: GrantFiled: June 22, 1990Date of Patent: April 6, 1993Inventors: Mario Di Giambattista, Andre Pecher, Carlo Cocito
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Patent number: 5198424Abstract: Peptides derived from three regions of the lectin binding region of GMP-140 have been found to selectively interact with "selectins", including GMP-140, ELAM-1, and lymphocyte homing receptor. The peptides can be as short as eight to thirteen amino acids in length and are easily prepared and modified by standard techniques. Critical elements of the counter-receptor or ligand on the neutrophils which binds GMP-140 are also identified. The peptides are useful as diagnostics andThe U.S. Government has rights in this invention by virtues of grants from the National Heart, Lung and Blood Institute.Type: GrantFiled: April 7, 1992Date of Patent: March 30, 1993Assignee: Board of Regents of the University of OklahomaInventor: Rodger P. McEver