Containing D-amino Acid Patents (Class 930/21)
  • Patent number: 8303962
    Abstract: This invention provides novel antimicrobial peptides and formulations thereof. The peptides and/or formulations are effective to kill or to inhibit the growth and/or proliferation of various bacteria, yeast, and fungi.
    Type: Grant
    Filed: January 6, 2010
    Date of Patent: November 6, 2012
    Assignee: C3 Jian, Inc.
    Inventors: Randal H. Eckert, Chris Kaplan, Jian He, Daniel K. Yarbrough, Maxwell Anderson, Jee-Hyun Sim
  • Patent number: 7705119
    Abstract: Polypeptides, compositions, and methods for treating shock are described. A isolated polypeptide, Deltorphin-E, can be administered without concomitant fluid resuscitation, before, concurrently with, or after the onset of shock or the occurrence of an event that creates a risk of shock. Deltorphin-E can be administered in accordance with the method as part of a preconditioning strategy, which reduces the extent of ischemic injury. Deltorphin-E can be used in preparation for planned ischemia or in a prophylactic manner in anticipation of further ischemic events.
    Type: Grant
    Filed: June 6, 2007
    Date of Patent: April 27, 2010
    Assignee: University of Kentucky Research Foundation
    Inventors: Peter R. Oeltgen, Meera Govindaswami
  • Patent number: 7285534
    Abstract: This invention provides members of the corticiotropin-releasing hormone superfamily and peptide analogs thereof wherein the 38th amino acid from the N-terminus is D-Nle, i.e. [D-Nle38]-CRH peptide. The peptide analogs can be used to treat proliferative disorders of the skin such as melanoma.
    Type: Grant
    Filed: December 6, 2004
    Date of Patent: October 23, 2007
    Assignee: The Regents of the University of California
    Inventors: Edward Wei, Kurt Carlson
  • Patent number: 7189689
    Abstract: The present invention provides peptides and peptide analogues that mimic the structural and pharmacological properties of human ApoA-I. The peptides and peptide analogues are useful to treat a variety of disorders associated with dyslipidemia.
    Type: Grant
    Filed: March 15, 2002
    Date of Patent: March 13, 2007
    Inventors: Jean-Louis Dasseux, Renate Sekul, Klaus Büttner, Isabelle Cornut, Günther Metz, Jean Dufourcq
  • Patent number: 7147856
    Abstract: Methods are described for conjugating radioiodinated peptides or carbohydrate structures to proteins with improved yields and qualities of conjugates. In one method, specially designed radioiodinated bifunctional peptides containing nonmetabolizable amide bonds are coupled to antibodies. In a second method, radioiodinated nonmetabolizable bifunctional peptides, which also contain aminopolycarboxylates, are coupled to antibodies. In a third method, radioiodinated bifunctional aminopolycarboxylates are coupled to antibodies. In a fourth method, a hydrazide-appended antibody is coupled to a radioiodinated carbohydrate or a thiolated antibody is coupled to a hydrazide-appended and radioiodinated carbohydrate. In a fifth method a monoderivatized cyanuric chloride is used to conjugate thiolated antibody. Radioiodinated residualizing antibody conjugates made by these methods are particularly stable in vivo and are suitable for radioimmunodetection and radioimmunotherapy.
    Type: Grant
    Filed: April 11, 2003
    Date of Patent: December 12, 2006
    Assignee: Immunomedics, Inc.
    Inventor: Serengulam V. Govindan
  • Patent number: 6849600
    Abstract: This invention relates to peptide analogs of corticotropin-releasing hormone. Particularly, the invention provides analogs wherein the 38th amino acid from the N-terminus is D-Nle, i.e. [D-Nle38]-CRH peptide.
    Type: Grant
    Filed: March 25, 2002
    Date of Patent: February 1, 2005
    Assignee: The Regents of the University of California, Berkeley
    Inventors: Edward T. Wei, Kurt W. Carlson
  • Patent number: 6846803
    Abstract: The present invention relates to an antagonist of the ligand of the Corticotropin-Releasing Factor Receptor, type 2 (CRFR2) lacking the 8 to 10 N-terminal amino acids of native sauvagine. The present invention also relates to an antagonist of the ligand of the Corticotropin-Releasing Factor Receptor, type 2 (CRFR2) lacking the 11 N-terminal amino acids of native sauvagine, wherein the N-terminal amino acid of said antagonist is a charged amino acid. Furthermore, the present invention relates to a polynucleotide encoding the antagonist of the present invention, a vector comprising the polynucleotide of the present invention, and a host comprising the polynucleotide or the vector of the present invention. Also described are a method for producing the antagonist of the present invention, antibodies directed the antagonist of the present invention, as well as anti-idiotypic antibodies directed against the antibody of the present invention.
    Type: Grant
    Filed: July 23, 1999
    Date of Patent: January 25, 2005
    Assignee: Max Planck Gesellschaft zur Forderung der Wissenschaften E.V.
    Inventors: Joachim Spiess, Andreas Ruhmann
  • Patent number: 6841657
    Abstract: Inhibitors of HIV membrane fusion and a method of identifying drugs or agents which inhibit binding of the N-helix coiled-coil and the C helix of HIV gp41 envelope protein.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: January 11, 2005
    Assignee: Whitehead Institute for Biomedical Research
    Inventors: Debra M. Eckert, David C. Chan, Vladimir Malashkevich, Peter A. Carr, Peter S. Kim
  • Patent number: 6538106
    Abstract: Compositions and methods for treating infections, especially bacterial infections, are provided. Indolicidin peptide analogues containing at least two basic amino acids are prepared. The analogues are administered as modified peptides, preferably containing photo-oxidized solubilizer.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: March 25, 2003
    Assignee: Micrologix Biotech, Inc.
    Inventors: Janet R. Fraser, Michael H. P. West, Timothy J. Krieger, Robert Taylor, Douglas Erfle
  • Patent number: 6472369
    Abstract: The testing of tumor cells, including human tumors capable of metastases, in assays employing fibronectin-depleted substrates is described. Ex vivo induction of cells, including biopsied human cells, is performed with invasion-inducing agents. Additionally, anti-cancer chemotherapeutics are described. Specifically, chemotherapeutic agents which have anti-metastatic and anti-growth properties are described including non-peptide compositions of matter.
    Type: Grant
    Filed: August 13, 1999
    Date of Patent: October 29, 2002
    Assignee: The Regents of the University of Michigan
    Inventor: Donna Livant
  • Patent number: 6444645
    Abstract: The present invention relates to crosslink-stabilized analogs of indolicidin, which is a naturally occurring peptide having the amino acid sequence Ile-Leu-Pro-Trp-Lys-Trp-Pro-Trp-Trp-Pro-Trp-Arg-Arg-CONH2 (“Indol 1-13;” SEQ ID NO: 1). The crosslinked indolicidin (“X-indolicidin”) analogs of the invention include, for example, analogs such as Indol 1-13(W6,9), which has the structure Ile-Leu-Pro-Trp-Lys-Trp-Pro-Trp-Trp-Pro-Trp-Arg-Arg-CONH2 (SEQ ID NO: 3), and Indol 1-13/6,9C(C6,9), which has the structure Ile-Leu-Pro-Trp-Lys-Cys-Pro-Trp-Cys-Pro-Trp-Arg-Arg-CONH2 (SEQ ID NO: 4), where a crosslink formed between the first and last underlined amino acid residues. In addition, the invention provides nucleic acid molecules encoding the X-indolicidin analogs of the invention, particularly precursors of such analogs.
    Type: Grant
    Filed: June 18, 1998
    Date of Patent: September 3, 2002
    Assignee: The Regents of the University of California
    Inventors: Michael E. Selsted, Klara Ösapay
  • Patent number: 6355681
    Abstract: Process for treating psychosis such as schizophrenia using a glycine substitute or a precursor thereof to potentiate NMDA receptormediated neurotransmission.
    Type: Grant
    Filed: May 27, 1999
    Date of Patent: March 12, 2002
    Assignee: Glytech, Inc.
    Inventor: Daniel C. Javitt
  • Patent number: 6326463
    Abstract: Novel cyclic CRF agonist peptides have the amino acid sequence: (cyclo 30-33)Ac-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Glu-Ala-R32-R33-Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH2 wherein R32 is His, D-His or an equivalent &agr;-amino acid; R33 is Lys or Orn. The N-terminus may be extended by Tyr, D-Tyr or Ile. Lys may be substituted for Arg23, and its side chain connected by a lactam bridge to Glu20 to form a bicyclic peptide. Certain disclosed CRF agonists include: (cyclo 30-33)[Ac-Ser7, D-Phe12, Nle21,38, Glu30, Lys33]r/hCRF(7-41); (cyclo 30-33)[Ac-Ser7, D-Phe12, Nle21,38, Glu30, D-His32, Lys33]r/hCRF(7-41); (bicyclo 20-23, 30-33)[Ac-Ser7, D-Phe12, Nle21,38, Lys23,33, Glu30, D-His32]-r/hCRF(7-41); (cyclo 30-33)[Ac-Ser7, D-Phe12, Nle18,21, Glu30, D-Ala32, Lys33]&agr;-helicale CRF(7-41); and (cyclo 30-33)[Ac-Ser7, D-Phe12, Nle21,38, CML27,40, Glu30, Lys33]r/hCRF(7-41).
    Type: Grant
    Filed: November 29, 1999
    Date of Patent: December 4, 2001
    Assignee: The Salk Institute For Biological Studies
    Inventor: Jean E. F. Rivier
  • Patent number: 6323179
    Abstract: Specially designed non-mammalian GnRH analog decapeptides resistant to degradation by the placental enzyme, C-ase-1, or a post-proline peptidase, are disclosed. The GnRH analogs are further defined as analogs of Chicken II GnRH or Salmon GnRH. These non-mammalian analogs incorporate D-arginine, D-leucine, D-tBu-Serine or D-Trp at position 6 and ethylamide or aza-Gly-amide at position 10. The D-Arg (6)-Chicken II GnRH-ethylamide, D-Arg (6)-Chicken II GnRH-aza-Gly (10)-amide, the D-Arg (6)-Salmon GnRH ethylamide, and D-Arg (6)-Salmon GnRH-aza-Gly (10)-amide analogs are also provided, and demonstrate preferential binding to chorionic GnRH receptor that is greater relative to the biding of these analogs to pituitary GnRH receptor. These non-mammalian GnRH analogs may be used in pharmaceutical preparation, and specifically in various treatment methods as a contraceptive or post-coital contraceptive agent.
    Type: Grant
    Filed: October 15, 1999
    Date of Patent: November 27, 2001
    Inventor: Theresa Siler-Khodr
  • Patent number: 6180604
    Abstract: Compositions and methods for treating infections, especially bacterial infections, are provided. Indolicidin peptide analogues containing at least two basic amino acids are prepared. The analogues are administered as modified peptides, preferably containing photo-oxidized solubilizer.
    Type: Grant
    Filed: August 20, 1997
    Date of Patent: January 30, 2001
    Assignee: Micrologix Biotech Inc.
    Inventors: Janet R. Fraser, Michael H. P. West, Timothy J. Krieger, Robert Taylor, Douglas Erfle
  • Patent number: 6103699
    Abstract: A peptide of the formula IX--A--D--Trp--Ywherein X is hydrogen, glycine, alanine, leucine, isoleucine, valine, N-valine, proline, tyrosine, phenylalanine, tryptophan, D-alanine, D-leucine, D-isoleucine, D-valine, D-N-valine, D-proline, D-tyrosine, D-phenylalanine, D-tryptophan, .gamma.-aminobutyric acid or .xi.-aminocaproic acid; A is D-gluptamic acid or D-iso-glutamic acid; and Y is glycine, alanine, leucine, isoleucine, valine, N-valine, proline, tyrosine, phenylalanine, tryptophan, D-alanine, D-leucine, D-isoleucine, D-valine, D-N-valine, D-proline, D-tyrosine, D-phenylalanine, D-tryptophn, .gamma.-aminobutyric acid, .xi.-aminocaproic acid, hydroxyl, or an amide group.
    Type: Grant
    Filed: February 26, 1998
    Date of Patent: August 15, 2000
    Assignee: Immunotech Developments Inc.
    Inventors: Vladislav I. Deigin, Andrei Marxovich Korotkov
  • Patent number: 6051685
    Abstract: A peptide derivative having analgesic activity represented by the following Formula I: ##STR1## wherein Q represents D-Arg or L-Arg; and X represents for example NR.sup.6 --CHR.sup.7 R.sup.8. Typical compounds include H.sub.2 NC(NH)-Tyr-D-Arg-Phe-NHCH.sub.2 CH.sub.2 COOH and H.sub.2 NC(NH)-Tyr-D-Arg-Phe-NHCH.sub.2 CH.sub.2 CONH.sub.2.
    Type: Grant
    Filed: September 2, 1998
    Date of Patent: April 18, 2000
    Assignee: Daiichi Pharmaceuticals Co., Ltd.
    Inventors: Shinobu Sakurada, Kimie Murayama, Masaharu Nakano, Kazuya Hongo, Satoko Takeshima, Nobuhiro Take
  • Patent number: 6001965
    Abstract: The testing of tumor cells, including human tumors capable of metastases, in assays employing fibronectin-depleted substrates is described. Ex vivo induction of cells, including biopsied human cells, is performed with invasion-inducing agents. Additionally, anti-cancer chemotherapeutics are described. Specifically, chemotherapeutic agents which have anti-metastatic and anti-growth properties are described.
    Type: Grant
    Filed: August 20, 1997
    Date of Patent: December 14, 1999
    Assignee: The Regents of the University of Michigan
    Inventor: Donna L. Livant
  • Patent number: 5990276
    Abstract: An inhibitor of the HCV NS3 protease. The inhibitor is a subsequence of a substrate of the NS3 protease or a subsequence of the NS4A cofactor. Another inhibitor of the present invention contains a subsequence of a substrate linked to a subsequences of the NS4A cofactor. In another embodiment the inhibitor is a bivalent inhibitor comprised of a subsequence, a mutated subsequence or a mutated full-length of a substrate of the NS3 protease linked to a subsequence, a mutated subsequence or a mutated full-length suquence of the HCV NS4A cofactor.
    Type: Grant
    Filed: May 9, 1997
    Date of Patent: November 23, 1999
    Assignee: Schering Corporation
    Inventors: Rumin Zhang, Philip W. Mui, Patricia C. Weber
  • Patent number: 5935932
    Abstract: The present invention provides bradykin antagonists containing pentafluorophenylalanine which are therapeutically useful. Moreover, the present invention provides methods to antagonize bradykinin receptors in a mammal in need of such antagonism, comprising administering a bradykinin antagonist containing pentafluorophenylalanine. Also provided are methods to treat inflammation in a mammal in need of such inhibition, comprising administering a bradykinin antagonist containing pentafluorophenylalanine. Lastly, a method to treat cancer in a mammal in need of such inhibition, comprising administering a bradykinin antagonist containing pentafluorophenylalanine.
    Type: Grant
    Filed: June 12, 1998
    Date of Patent: August 10, 1999
    Assignee: University Technology Corporation
    Inventors: John M. Stewart, Lajos Gera
  • Patent number: 5874227
    Abstract: Novel cyclic CRF antagonist peptides have the amino acid sequence: ##STR1## wherein Y is Ac, H, Ac-Thr or H-Thr; R.sub.30 is Glu or Cys; R.sub.32 is His or preferably a basic and/or aromatic D-amino acid such as D-His or D-Arg; R.sub.33 is Lys, Orn or Cys. The N-terminus may be extended by Leu or Asp-Leu. CML may be substituted for Leu.sup.27, and D-Tyr may be substituted for D-Phe to facilitate labelling. Lys may be substituted for Arg.sup.23, and its side chain connected by a lactam bridge to Glu.sup.20 to form a bicyclic peptide. Disclosed CRF antagonists include:(cyclo 30-33)?D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, Lys.sup.33 !r/hCRF(12-41),(cyclo 30-33)?Ac-Thr.sup.11, D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, Lys.sup.33 !r/hCRF(11-41),(cyclo 30-33)?D-Phe.sup.12, Nle.sup.21,38, Cys.sup.30,33 !r/hCRF(12-41),(bicyclo 20-23,30-33)?D-Phe.sup.12, Nle.sup.21,38, Lys.sup.23,33, Glu.sup.30 !-r/hCRF(12-41),(cyclo 30-33)?D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, D-His.sup.32, Lys.sup.
    Type: Grant
    Filed: November 10, 1995
    Date of Patent: February 23, 1999
    Assignee: The Salk Institute for Biological Studies
    Inventor: Jean E. F. Rivier
  • Patent number: 5844074
    Abstract: Novel cyclic CRF agonist peptides have the amino acid sequence: (cyclo 30-33)Ac-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu -Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-R.sub.30 -Ala-R.sub.32 -R.sub.33 -Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH.sub.2 wherein R.sub.30 is Glu or Cys; R.sub.32 is His or a D-amino acid such as D-His, D-Arg or similar; R.sub.33 is Lys, Orn or Cys. The N-terminus may be extended by Ser-Glu-Glu. Lys may be substituted for Arg.sup.23, and its side chain connected by a lactam bridge to Glu.sup.20 to form a bicyclic peptide. Certain disclosed CRF agonists include:(cyclo 30-33)?Ac-Pro.sup.4, D-Phe.sup.12, Nle.sup.21,38, D-His.sup.32, Glu.sup.30, Lys.sup.33 !r/hCRF(4-41),(cyclo 30-33)?Ac-Pro.sup.4, D-Phe.sup.12, Nle.sup.21,38, D-His.sup.32, Glu.sup.30, Orn.sup.33 !r/hCRF(4-41),(cyclo 30-33)?Ac-Pro.sup.4, D-Phe.sup.12, Nle.sup.21,38, Cys.sup.30,33, D-His.sup.32 !r/hCRF(4-41),(bicyclo 20-23,30-33)?Ac-Pro.sup.4, D-Phe.sup.12, Nle.sup.21,38, Lys.sup.23,33, Glu.sup.30, D-His.sup.
    Type: Grant
    Filed: December 19, 1995
    Date of Patent: December 1, 1998
    Assignee: The Salk Institute for Biological Studies
    Inventor: Jean E. F. Rivier
  • Patent number: 5824771
    Abstract: Novel cyclic CRF agonist peptides have the amino acid sequence: (cyclo 30-33)Ac-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu -Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-R.sub.30 -Ala-R.sub.32 -R.sub.33 -Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH.sub.2 wherein R.sub.30 is Glu or Cys; R.sub.32 is His, D-His or an equivalent .alpha.-amino acid; R.sub.33 is Lys, Orn or Cys. The N-terminus may be extended by Ser-Glu-Glu or shortened by up to three more residues. Lys may be substituted for Arg.sup.23, and its side chain connected by a lactam bridge to Glu.sup.20 to form a bicyclic peptide. Certain disclosed CRF agonists include:(cyclo 30-33)?Ac-Pro.sup.4, D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, D-His.sup.32, Lys.sup.33 !r/hCRF(4-41),(cyclo 30-33)?Ac-Ser.sup.7, D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, Lys.sup.33 !r/hCRF(7-41),(cyclo 30-33)?Ac-Ser.sup.7, D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, D-His.sup.32, Lys.sup.33 !r/hCRF(7-41),(bicyclo 20-23, 30-33)?Ac-Pro.sup.4, D-Phe.sup.12, Nle.sup.21,38, Lys.sup.
    Type: Grant
    Filed: May 30, 1997
    Date of Patent: October 20, 1998
    Assignee: The Salk Institute for Biological Studies
    Inventor: Jean E. F. Rivier
  • Patent number: 5777073
    Abstract: Novel cyclic CRF antagonist peptides are created by shortening the N-terminus of a CRF family peptide by 8-11 residues and adding an acyl group. CML is preferably present in what would be the 27-position of the native CRF sequence, and D-Tyr may be incorporated at the N-terminus to facilitate labelling. The cyclizing bond is preferably created between the side chains of the residues in positions 30 and 33; but it may alternatively be created between the residues in either of positions 28 and 29 with those in positions 31 and 32 or with those in positions 32 and 33, respectively. The side chain of Lys in position 33 is preferably linked to the side chain of Glu in position 30 by a lactam bridge to form the cyclic peptide. Disclosed CRF antagonists include:(cyclo 30-33) ?Ac-Asp.sup.9, D-Phe.sup.12, Nle.sup.21,38, CML.sup.27,40, Glu.sup.30, Lys.sup.33 !r/hCRF(9-41),(cyclo 30-33) ?Ac-Asp.sup.9, D-Phe.sup.12, Nle.sup.21,38, CML.sup.27,37, Glu.sup.30, Lys.sup.33 !r/hCRF(9-41),(cyclo 30-33) ?Ac-Asp.sup.9, D-Phe.sup.
    Type: Grant
    Filed: May 30, 1997
    Date of Patent: July 7, 1998
    Assignee: The Salk Institute for Biological Studies
    Inventor: Jean E. F. Rivier
  • Patent number: 5723165
    Abstract: Aspartyldipeptide compounds of the formula (I)L-Asp-X-NH-C*R.sub.1 R.sub.2 (I)where R.sub.1 is alkyl or alkoxymethyl, R.sub.2 is phenyl, benzyl, cyclohexyl or cyclohexylmethyl, C* has an (S) configuration when R.sub.1 is alkyl and an (R) configuration when R.sub.1 is alkoxymethyl and X is a residue of a D-.alpha.-amino acid, a DL-.alpha.-amino acid or a residue of a cyclic or acyclic .alpha.,.alpha.-diallylamino acid and the bond between L-Asp and X is an .alpha.-bond; and their use as active ingredients in sweetener compositions.
    Type: Grant
    Filed: July 10, 1995
    Date of Patent: March 3, 1998
    Assignee: Ajinomoto Co., Inc.
    Inventors: Tadashi Takemoto, Yusuke Amino, Ryoichiro Nakamura
  • Patent number: 5698516
    Abstract: Vasopressin analogues of formula (I) ##STR1## wherein X is (S)-2-amino-2-methyl-butanoic acid (CaMeAbu) or Valine (Val), Y is Thienylalanine (Thi) or Methionine (Met), Z is D-Phenylalanine (D-Phe) or D-Thienylalanine (Thi) or D-Tyrosine (D-Tyr), are disclosed. Pharmaceutical preparations comprising a vasopressin analogue of the invention as active ingredient are disclosed and exemplified by oral preparations, nasal preparations, and intravenous preparations. The vasopressin analogues of the invention are intended for use as a medicament, specially an antidiuretic agent. The antidiuretic agent is preferably used for the treatment of diabetes insipidus or enuresis.
    Type: Grant
    Filed: December 18, 1995
    Date of Patent: December 16, 1997
    Assignee: Ferring B.V.
    Inventors: Anders Nilsson, H.ang.kan Olson, Christina Soderberg-Ahlm, Jerzy Trojnar
  • Patent number: 5663292
    Abstract: Improved CRF antagonist peptides have the formula: ##STR1## wherein R.sub.30 is Cys or Glu; R.sub.33 is Cys, Lys or Orn; provided that when R.sub.30 is Cys, R.sub.33 is Cys and when R.sub.30 is Glu, R.sub.33 is Lys or Orn. The N-terminus may be extended by Asp-Leu-Thr. Lys may be substituted for Arg.sup.23 and its side chain connected by a lactam bridge to Glu.sup.20 to form a dicyclic peptide. Specific CRF antagonists disclosed include (cyclo 30-33) [D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, Lys.sup.33 ]rCRF(12-41); (cyclo 30-33) [D-Phe.sup.12, Nle.sup.21,38, Glu.sup.30, Orn.sup.33 ]rCRF(12-41), (cyclo 30-33) [D-Phe.sup.12, Nle.sup.21,38, Cys.sup.30,33 ]rCRF (12-41) and (bicyclo 20-23,30-33) [D-Phe.sup.12, Nle.sup.21,38, Lys.sup.23,33, Glu.sup.30 ]-rCRF(12-41).
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: September 2, 1997
    Assignee: The Salk Institute for Biological Studies
    Inventor: Jean E. F. Rivier
  • Patent number: 5643877
    Abstract: Novel peptide hormones which influence the release of gonadotropins by the pituitary gland in fish are disclosed. Methods in which such peptides may be administered to fish to control their reproduction are also described. Furthermore, novel isolated cDNA encoding the precursor of the novel gonadotropin-releasing hormone is disclosed. The use of such cDNA in controlling the gonadal development and spawning of fish is also described.
    Type: Grant
    Filed: December 5, 1994
    Date of Patent: July 1, 1997
    Assignees: University of Maryland Biotechnology Institute, University of Victoria Innovation and Development Corporation
    Inventors: Yonathan Zohar, Nancy M. Sherwood, Jean Rivier, Jim Powell, Yoav Gothilf
  • Patent number: 5633230
    Abstract: Described herein are anti-cytomegalovirus peptides. In a preferred embodiment, the peptide is acetyl-[D-Arg].sub.9 -NH.sub.2. The use of these peptides, either per se or in combination with other anti-CMV compounds, is disclosed as an effective method for controlling CMV infection.
    Type: Grant
    Filed: October 31, 1994
    Date of Patent: May 27, 1997
    Assignee: Allelix Biopharmaceuticals, Inc.
    Inventors: Michael Twist, deceased, Martin Sumner-Smith
  • Patent number: 5510458
    Abstract: Disclosed are improved CRF peptide antagonists such as those having the formula: Y-D-Phe-Xaa.sub.13 -Leu-Leu-Arg-Xaa.sub.17 -Xaa.sub.18 -Leu-Xaa.sub.20 -Nle-Xaa.sub.22 -Xaa.sub.23 -Xaa.sub.24 -Xaa.sub.25 -Xaa.sub.26 -Leu-Xaa.sub.28 -Xaa.sub.29 -Gln-Xaa.sub.31 -Xaa.sub.32 -Xaa.sub.33 -Xaa.sub.34 -Arg-Xaa.sub.36 -Xaa.sub.37 -Nle-Xaa.sub.39 -Xaa.sub.40 -Xaa.sub.41 -NH.sub.2 wherein Y is Ac or hydrogen; Xaa.sub.13 is His, Tyr or Glu; Xaa.sub.17 is CML, Glu, Asn or Lys; Xaa.sub.18 is Val, Nle or Met; Xaa.sub.20 is Glu, D-Glu, Aib or D-Ala; Xaa.sub.22 is Ala, Aib, Thr, Asp or Glu; Xaa.sub.23 is Arg, Orn, Har or Lys; Xaa.sub.24 is Ala or Aib; Xaa.sub.25 is Asp or Glu; Xaa.sub.26 is Gln, Asn or Lys; Xaa.sub.28 is Ala or Aib; Xaa.sub.29 is Gln, Aib or Glu, Xaa.sub.31 is Ala or Aib; Xaa.sub.32 is His, Aib, Gly, Tyr or Ala; Xaa.sub.33 is Ser, Aib, Asn, Leu, Thr or Ala; Xaa.sub.34 is Asn or Aib; Xaa.sub.36 is Lys, Orn, Arg, Har or Leu; Xaa.sub.37 is Leu or Tyr; Xaa.sub.39 is Glu, Aib or Asp; Xaa.sub.
    Type: Grant
    Filed: December 14, 1993
    Date of Patent: April 23, 1996
    Assignee: The Salk Institute For Biological Studies
    Inventors: Wayne D. Kornreich, Jean F. Hernandez, Jean E. Rivier, Catherine L. Rivier, Wylie W. Vale, Jr.
  • Patent number: 5487898
    Abstract: Pharmaceutical compositions for the sublingual or buccal administration of therapeutic agents which are normally degraded upon oral administration comprise such a therapeutic agent, a solvent, optionally a cosolvent and/or hydrogel, and an oral mucosal membrane transport enhancing agent which is selected from the group consisting of essential and volatile oils and inorganic and organic acids.
    Type: Grant
    Filed: February 7, 1994
    Date of Patent: January 30, 1996
    Assignee: Abbott Laboratories
    Inventors: Mou-Ying F. Lu, Thomas L. Reiland
  • Patent number: 5441935
    Abstract: A 75-85 Kd glycopolypeptide, capable of acting as a receptor for polypeptide of the bombesin type, is isolated from the surface of Swiss 3T3 cells. Certain antagonists and antibodies to the glycopolypeptide are described, the antagonists being of quite different structure to bombesin e.g. .differential.D-Pro.sup.2 [-spantide, .differential.D-Phe.sup.5 [-spantide and position 5 variants thereof. The antagonists and antibodies are of interest medically in that they are able to influence cell proliferation that occurs under the influence of the bombesin-like polypeptides.
    Type: Grant
    Filed: September 3, 1992
    Date of Patent: August 15, 1995
    Assignee: Imperial Cancer Research Technology Ltd.
    Inventors: Enrique Rozengurt, Ian Zachary, Penella Woll
  • Patent number: 5439688
    Abstract: A pharmaceutical composition is prepared in the form of microparticles or of an implant comprising a biodegradable polymer selected from poly-1,4-butylene succinate, poly-2,3-butylene succinate, poly-1,4-butylene fumarate and poly-2,3-butylene succinate, incorporating as the active substance the pamoate, tannate, stearate or palmitate of a natural or of a synthetic peptide comprising 3 to 45 amino acids, such as LH-RH, somatostatin, GH-RH or calcitonin, or one of their synthetic analogues or homologues. The preparation comprises dry blending the ingredients in the form of powders, pre-compressing and preheating the mixture and then extruding the pre-compressed and pre-heated mixture. The product resulting from the extrusion step can then be comminuted and finally sieved.
    Type: Grant
    Filed: November 12, 1991
    Date of Patent: August 8, 1995
    Assignee: Debio Recherche Pharmaceutique S.A.
    Inventors: Piero Orsolini, Frederic Heimgartner
  • Patent number: 5262521
    Abstract: A novel atrial peptide-degrading enzyme (ADE) is provided in isolated, purified form. The enzyme has a molecular weight of approximately 160,000 Daltons as measured by gel filtration chromatography, and is effective to cleave atrial peptides such as APII, APIII and ANF. Also provided are novel compounds useful as inhibitors of the enzyme and thus useful as blood pressure lowering agents, pharmaceutical compositions containing the inhibitors, and methods of using the inhibitors.
    Type: Grant
    Filed: June 7, 1991
    Date of Patent: November 16, 1993
    Assignee: SRI International
    Inventors: Ronald G. Almquist, Lawrence Toll
  • Patent number: 5252718
    Abstract: Antagonists to basic fibroblast growth factor, a 146 amino acid residue polypeptide, are produced. These antagonists are generally between 10 and 45 residues in length and are characterized by their ability to interact with the FGF receptor and/or inhibit and therefore modulate endothelial and other cell growth in vitro and also in vivo. These antagonists includes the sequence of bovine basic FGF(106-115), namely Tyr-Arg-Ser-Arg-Lys-Tyr-Ser-Ser-Trp-Tyr or a sequence having equivalent residues substituted therein. These peptides are also antagonistic to acidic FGF and other members of the family of FGF peptides. They are effective to combat FGF-promoted mitosis in melanomas and the like.
    Type: Grant
    Filed: April 27, 1992
    Date of Patent: October 12, 1993
    Assignee: The Salk Institute for Biological Studies
    Inventors: J. Andrew Baird, Nicholas C. Ling
  • Patent number: 5250517
    Abstract: Compounds which are amino acid derivatives and have the formula ##STR1## in which R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl or imidazol-4-yl, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, and A is defined as herein are useful as renin inhibitors.
    Type: Grant
    Filed: May 4, 1992
    Date of Patent: October 5, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Quirico Branca, Albrecht Edenhofer, Eva-Maria Gutknecht, Werner Neidhart, Henri Ramuz, Wolfgang Wostl
  • Patent number: 5248667
    Abstract: Peptides previously disclosed as useful for preventing HIV from binding to cell binding sites have now been shown to have thymoleptic qualities and to be useful for tretment of psoriasis in patients who lack antibodies against HIV.
    Type: Grant
    Filed: July 18, 1991
    Date of Patent: September 28, 1993
    Assignee: The United States of America as represented by the Secretary of the Department of Health & Human Services
    Inventors: Peter Bridge, Frederick K. Goodwin
  • Patent number: 5245009
    Abstract: Disclosed are improved CRF peptide antagonists such as those having the formula: Y-D-Phe-R.sub.13 -Leu-Leu-Arg-R.sub.17 -R.sub.18 -Leu-R.sub.20 -Nle-R.sub.22 -R.sub.23 -R.sub.24 -R.sub.25 -R.sub.26 -Leu-R.sub.28 -R.sub.29 -Gln-R.sub.31 -R.sub.32 -R.sub.33 -R.sub.34 -Arg-R.sub.36 -R.sub.37 -Nle-R.sub.39 -R.sub.40 -R.sub.41 -NH.sub.2 wherein Y is Ac or hydrogen; R.sub.13 is His, Tyr or Glu; R.sub.17 is Cys, Glu, Asn or Lys; R.sub.18 is Val, Nle or Met; R.sub.20 is D-Cys, Glu, D-Glu, Aib or D-Ala; R.sub.22 is Ala, Aib, Thr, Asp or Glu; R.sub.23 is Arg, Orn, Har or Lys; R.sub.24 is Ala or Aib; R.sub.25 is Asp or Glu; R.sub.26 is Gln, Asn or Lys; R.sub.28 is Ala or Aib; R.sub.29 is Gln, Aib or Glu, R.sub.31 is Ala or Aib; R.sub.32 is His, Aib, Gly, Tyr or Ala; R.sub.33 is Ser, Aib, Asn, Leu, Thr or Ala; R.sub.34 is Asn or Aib; R.sub.36 is Lys, Orn, Arg, Har or Leu; R.sub.37 is Leu or Try; R.sub.39 is Glu, Aib or Asp; R.sub.40 is Ile, Aib, Thr, Glu, Ala, Val, Leu, Nle, Phe, Nva, Gly or Gln; and R.sub.
    Type: Grant
    Filed: June 14, 1991
    Date of Patent: September 14, 1993
    Assignee: The Salk Institute for Biological Studies
    Inventors: Wayne D. Kornreich, Jean-Francois Hernandez, Jean E. F. Rivier, Catherine L. Rivier, Wylie W. Vale, Jr.
  • Patent number: 5235036
    Abstract: Analogs of CRF, which are based upon hCRF, oCRF and alpha-helical CRF, are disclosed that can be administered to achieve a substantial elevation of ACTH, .beta.-endorphin, .beta.-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone levels. Analogs include those having the formula: Y-R.sub.1 -R.sub.2 -R.sub.3 -R.sub.4 -R.sub.5 -Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-R.sub.20 -R.sub.21 -R.sub.22 -R.sub.23 -R.sub.24 -R.sub.25 -Gln-Leu-Ala-Gln-Gln-Ala-R.sub.32 -Ser-Asn-Arg-Lys-Leu-R.sub.38 -R.sub.39 -Ile-R.sub.41 -NH.sub.2, wherein Y is an acyl group having 7 or fewer carbon atoms or hydrogen; R.sub.1 is Ser or desR.sub.1 ; R.sub.2 is Glu, Gln or desR.sub.2 ; R.sub.3 is Glu or desR.sub.3 ; R.sub.4 is Pro or desR.sub.4 ; R.sub.5 is Pro or desR.sub.5 ; R.sub.20 is Ala or Glu; R.sub.21 is Met or Nle; R.sub.22 is Ala or Thr; R.sub.23 is Arg or Lys; R.sub.24 is D-Ala or Ala; R.sub.25 is Glu or Asp; R.sub.32 is D-His or His; R.sub.38 is Met, Nle or Leu; R.sub.
    Type: Grant
    Filed: May 31, 1991
    Date of Patent: August 10, 1993
    Assignee: The Salk Institute for Biological Studies
    Inventors: Wayne D. Kornreich, Jean-Francois Hernandez, Jean E. F. Rivier, Wylie W. Vale, Jr.
  • Patent number: 5232912
    Abstract: This invention relates to peptide derivatives which are useful anticoagulant agents.
    Type: Grant
    Filed: October 30, 1992
    Date of Patent: August 3, 1993
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: John L. Krstenansky
  • Patent number: 5212154
    Abstract: Preparation for preventing or combating complications in diabetes, characterized in that it comprises:(a) insulin or a salt or complex thereof, and(b) a peptide of the general formula I:H-L-Met(X)-L-Glu-L-His-L-Phe-D-Lys-L-Phe-Yor a salt or a N-acyl derivative thereof, whereinMet(X) represents the amino acid radical Met, Met(O) or Met(O.sub.2),Y represents the group Gly-Z or Z, andZ represents the hydroxyl group, an esterified hydroxyl group or a substituted or unsubstituted amino group.
    Type: Grant
    Filed: May 19, 1992
    Date of Patent: May 18, 1993
    Assignee: Akzo N.V.
    Inventor: Robby Huisman
  • Patent number: 5190922
    Abstract: Oligopeptide compounds or oligopeptide analogue compounds of the formula A-B-D-E-G-J-L 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: Grant
    Filed: June 4, 1991
    Date of Patent: March 2, 1993
    Assignee: Abbott Laboratories
    Inventors: Jay R. Luly, Megumi Kawai, Paul E. Wiedeman
  • Patent number: 5187156
    Abstract: The present invention relates to DTrp-Phe containing tripeptides and pharmaceuticals, which possess tachykinin antagonism activity as well as processes of making such peptides.
    Type: Grant
    Filed: March 2, 1989
    Date of Patent: February 16, 1993
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masaaki Matsuo, Daijiro Hagiwara, Hiroshi Miyake
  • Patent number: 5128447
    Abstract: A synthetic peptide corresponding to the following formula:X--Asp--Y--DTrp--Val--DTrp--Z--K--NH.sub.2where:X=H, Arg, DArg, Lys, DLys, Thr, DThrY=Tyr, Trp, DTrp, Ser, MetZ=Trp, DTrpK=Arg, Phe, DTrp, Tyr, Metand pharmaceutically acceptable salts thereof with organic and inorganic acids as competitive antagonists against neurokinin A (NK-2 receptor).
    Type: Grant
    Filed: May 24, 1990
    Date of Patent: July 7, 1992
    Assignee: A. Menarini Industrie Farmaceutiche Riunite S.r.l.
    Inventors: Paolo Rovero, Vittorio Pestellini, Carlo A. Maggi, Riccardo Patacchini, Paolo Santicioli, Sandro Giuliani, Alberto Meli
  • Patent number: 5109111
    Abstract: Several known members of the corticotropin releasing factor (CRF) family have been synthesized and tested, including human and rat CRF which have the formula: H-Ser-Glu-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His- Leu-Leu-Arg-Glu-Val-Leu-Glu-Met-Ala-Arg-Ala-Glu-Gln- Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Arg-Lys-Leu-Met-Glu- Ile-Ile-NH.sub.2. Peptides are herein disclosed that are potent competitive antagonists of CRF in mammals. One which has been found to be particularly potent is: H-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle-Ala- Arg-Ala-Glu-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn- Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH.sub.2. One that has shown particularly prolonged duration of potency is: H-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle-Ala- Arg-Ala-Glu-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn- Arg-Lys-CML-Nle-Glu-Ile-Ile-NH.sub.2.
    Type: Grant
    Filed: March 23, 1990
    Date of Patent: April 28, 1992
    Assignee: The Salk Institute for Biological Studies
    Inventors: Jean E. F. Rivier, Wylie W. Vale, Jr., Catherine L. Rivier, Jean-Francois Hernandez