Containing D-amino Acid Patents (Class 930/21)
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Patent number: 8303962Abstract: 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: GrantFiled: January 6, 2010Date of Patent: November 6, 2012Assignee: C3 Jian, Inc.Inventors: Randal H. Eckert, Chris Kaplan, Jian He, Daniel K. Yarbrough, Maxwell Anderson, Jee-Hyun Sim
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Patent number: 7705119Abstract: 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: GrantFiled: June 6, 2007Date of Patent: April 27, 2010Assignee: University of Kentucky Research FoundationInventors: Peter R. Oeltgen, Meera Govindaswami
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Patent number: 7285534Abstract: 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: GrantFiled: December 6, 2004Date of Patent: October 23, 2007Assignee: The Regents of the University of CaliforniaInventors: Edward Wei, Kurt Carlson
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Patent number: 7189689Abstract: 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: GrantFiled: March 15, 2002Date of Patent: March 13, 2007Inventors: Jean-Louis Dasseux, Renate Sekul, Klaus Büttner, Isabelle Cornut, Günther Metz, Jean Dufourcq
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Patent number: 7147856Abstract: 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: GrantFiled: April 11, 2003Date of Patent: December 12, 2006Assignee: Immunomedics, Inc.Inventor: Serengulam V. Govindan
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Patent number: 6849600Abstract: 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: GrantFiled: March 25, 2002Date of Patent: February 1, 2005Assignee: The Regents of the University of California, BerkeleyInventors: Edward T. Wei, Kurt W. Carlson
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Patent number: 6846803Abstract: 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: GrantFiled: July 23, 1999Date of Patent: January 25, 2005Assignee: Max Planck Gesellschaft zur Forderung der Wissenschaften E.V.Inventors: Joachim Spiess, Andreas Ruhmann
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Patent number: 6841657Abstract: 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: GrantFiled: December 21, 2000Date of Patent: January 11, 2005Assignee: Whitehead Institute for Biomedical ResearchInventors: Debra M. Eckert, David C. Chan, Vladimir Malashkevich, Peter A. Carr, Peter S. Kim
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Patent number: 6538106Abstract: 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: GrantFiled: September 22, 2000Date of Patent: March 25, 2003Assignee: Micrologix Biotech, Inc.Inventors: Janet R. Fraser, Michael H. P. West, Timothy J. Krieger, Robert Taylor, Douglas Erfle
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Patent number: 6472369Abstract: 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: GrantFiled: August 13, 1999Date of Patent: October 29, 2002Assignee: The Regents of the University of MichiganInventor: Donna Livant
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Patent number: 6444645Abstract: 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: GrantFiled: June 18, 1998Date of Patent: September 3, 2002Assignee: The Regents of the University of CaliforniaInventors: Michael E. Selsted, Klara Ösapay
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Patent number: 6355681Abstract: Process for treating psychosis such as schizophrenia using a glycine substitute or a precursor thereof to potentiate NMDA receptormediated neurotransmission.Type: GrantFiled: May 27, 1999Date of Patent: March 12, 2002Assignee: Glytech, Inc.Inventor: Daniel C. Javitt
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Patent number: 6326463Abstract: 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: GrantFiled: November 29, 1999Date of Patent: December 4, 2001Assignee: The Salk Institute For Biological StudiesInventor: Jean E. F. Rivier
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Patent number: 6323179Abstract: 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: GrantFiled: October 15, 1999Date of Patent: November 27, 2001Inventor: Theresa Siler-Khodr
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Patent number: 6180604Abstract: 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: GrantFiled: August 20, 1997Date of Patent: January 30, 2001Assignee: Micrologix Biotech Inc.Inventors: Janet R. Fraser, Michael H. P. West, Timothy J. Krieger, Robert Taylor, Douglas Erfle
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Patent number: 6103699Abstract: 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: GrantFiled: February 26, 1998Date of Patent: August 15, 2000Assignee: Immunotech Developments Inc.Inventors: Vladislav I. Deigin, Andrei Marxovich Korotkov
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Patent number: 6051685Abstract: 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: GrantFiled: September 2, 1998Date of Patent: April 18, 2000Assignee: Daiichi Pharmaceuticals Co., Ltd.Inventors: Shinobu Sakurada, Kimie Murayama, Masaharu Nakano, Kazuya Hongo, Satoko Takeshima, Nobuhiro Take
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Patent number: 6001965Abstract: 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: GrantFiled: August 20, 1997Date of Patent: December 14, 1999Assignee: The Regents of the University of MichiganInventor: Donna L. Livant
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Patent number: 5990276Abstract: 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: GrantFiled: May 9, 1997Date of Patent: November 23, 1999Assignee: Schering CorporationInventors: Rumin Zhang, Philip W. Mui, Patricia C. Weber
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Patent number: 5935932Abstract: 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: GrantFiled: June 12, 1998Date of Patent: August 10, 1999Assignee: University Technology CorporationInventors: John M. Stewart, Lajos Gera
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Patent number: 5874227Abstract: 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: GrantFiled: November 10, 1995Date of Patent: February 23, 1999Assignee: The Salk Institute for Biological StudiesInventor: Jean E. F. Rivier
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Patent number: 5844074Abstract: 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: GrantFiled: December 19, 1995Date of Patent: December 1, 1998Assignee: The Salk Institute for Biological StudiesInventor: Jean E. F. Rivier
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Patent number: 5824771Abstract: 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: GrantFiled: May 30, 1997Date of Patent: October 20, 1998Assignee: The Salk Institute for Biological StudiesInventor: Jean E. F. Rivier
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Patent number: 5777073Abstract: 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: GrantFiled: May 30, 1997Date of Patent: July 7, 1998Assignee: The Salk Institute for Biological StudiesInventor: Jean E. F. Rivier
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Patent number: 5723165Abstract: 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: GrantFiled: July 10, 1995Date of Patent: March 3, 1998Assignee: Ajinomoto Co., Inc.Inventors: Tadashi Takemoto, Yusuke Amino, Ryoichiro Nakamura
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Patent number: 5698516Abstract: 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: GrantFiled: December 18, 1995Date of Patent: December 16, 1997Assignee: Ferring B.V.Inventors: Anders Nilsson, H.ang.kan Olson, Christina Soderberg-Ahlm, Jerzy Trojnar
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Patent number: 5663292Abstract: 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: GrantFiled: December 12, 1994Date of Patent: September 2, 1997Assignee: The Salk Institute for Biological StudiesInventor: Jean E. F. Rivier
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Patent number: 5643877Abstract: 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: GrantFiled: December 5, 1994Date of Patent: July 1, 1997Assignees: University of Maryland Biotechnology Institute, University of Victoria Innovation and Development CorporationInventors: Yonathan Zohar, Nancy M. Sherwood, Jean Rivier, Jim Powell, Yoav Gothilf
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Patent number: 5633230Abstract: 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: GrantFiled: October 31, 1994Date of Patent: May 27, 1997Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Michael Twist, deceased, Martin Sumner-Smith
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Patent number: 5510458Abstract: 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: GrantFiled: December 14, 1993Date of Patent: April 23, 1996Assignee: The Salk Institute For Biological StudiesInventors: Wayne D. Kornreich, Jean F. Hernandez, Jean E. Rivier, Catherine L. Rivier, Wylie W. Vale, Jr.
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Patent number: 5487898Abstract: 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: GrantFiled: February 7, 1994Date of Patent: January 30, 1996Assignee: Abbott LaboratoriesInventors: Mou-Ying F. Lu, Thomas L. Reiland
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Patent number: 5441935Abstract: 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: GrantFiled: September 3, 1992Date of Patent: August 15, 1995Assignee: Imperial Cancer Research Technology Ltd.Inventors: Enrique Rozengurt, Ian Zachary, Penella Woll
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Patent number: 5439688Abstract: 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: GrantFiled: November 12, 1991Date of Patent: August 8, 1995Assignee: Debio Recherche Pharmaceutique S.A.Inventors: Piero Orsolini, Frederic Heimgartner
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Patent number: 5262521Abstract: 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: GrantFiled: June 7, 1991Date of Patent: November 16, 1993Assignee: SRI InternationalInventors: Ronald G. Almquist, Lawrence Toll
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Patent number: 5252718Abstract: 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: GrantFiled: April 27, 1992Date of Patent: October 12, 1993Assignee: The Salk Institute for Biological StudiesInventors: J. Andrew Baird, Nicholas C. Ling
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Patent number: 5250517Abstract: 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: GrantFiled: May 4, 1992Date of Patent: October 5, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Quirico Branca, Albrecht Edenhofer, Eva-Maria Gutknecht, Werner Neidhart, Henri Ramuz, Wolfgang Wostl
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Patent number: 5248667Abstract: 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: GrantFiled: July 18, 1991Date of Patent: September 28, 1993Assignee: The United States of America as represented by the Secretary of the Department of Health & Human ServicesInventors: Peter Bridge, Frederick K. Goodwin
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Patent number: 5245009Abstract: 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: GrantFiled: June 14, 1991Date of Patent: September 14, 1993Assignee: The Salk Institute for Biological StudiesInventors: Wayne D. Kornreich, Jean-Francois Hernandez, Jean E. F. Rivier, Catherine L. Rivier, Wylie W. Vale, Jr.
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Patent number: 5235036Abstract: 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: GrantFiled: May 31, 1991Date of Patent: August 10, 1993Assignee: The Salk Institute for Biological StudiesInventors: Wayne D. Kornreich, Jean-Francois Hernandez, Jean E. F. Rivier, Wylie W. Vale, Jr.
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Patent number: 5232912Abstract: This invention relates to peptide derivatives which are useful anticoagulant agents.Type: GrantFiled: October 30, 1992Date of Patent: August 3, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: John L. Krstenansky
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Patent number: 5212154Abstract: 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: GrantFiled: May 19, 1992Date of Patent: May 18, 1993Assignee: Akzo N.V.Inventor: Robby Huisman
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Patent number: 5190922Abstract: 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: GrantFiled: June 4, 1991Date of Patent: March 2, 1993Assignee: Abbott LaboratoriesInventors: Jay R. Luly, Megumi Kawai, Paul E. Wiedeman
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Patent number: 5187156Abstract: 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: GrantFiled: March 2, 1989Date of Patent: February 16, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Daijiro Hagiwara, Hiroshi Miyake
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Patent number: 5128447Abstract: 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: GrantFiled: May 24, 1990Date of Patent: July 7, 1992Assignee: A. Menarini Industrie Farmaceutiche Riunite S.r.l.Inventors: Paolo Rovero, Vittorio Pestellini, Carlo A. Maggi, Riccardo Patacchini, Paolo Santicioli, Sandro Giuliani, Alberto Meli
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Patent number: 5109111Abstract: 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: GrantFiled: March 23, 1990Date of Patent: April 28, 1992Assignee: The Salk Institute for Biological StudiesInventors: Jean E. F. Rivier, Wylie W. Vale, Jr., Catherine L. Rivier, Jean-Francois Hernandez