Bradykinin; Kallidin; Related Peptides Patents (Class 530/314)
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Patent number: 5635593Abstract: A brandykinin antagonist of the formula:X(BKA).sub.nwherein BKA is the peptide chain of a bradykinin antagonist peptide, X is a linking group and n is a whole number greater than 1. The BKA substituents may be the same or different. Monomeric antagonists of the formula X(BKA) are also disclosed. Also disclosed are bradykinin antagonists of the formula:(Y)(X)(BKA)where X and BKA have the meanings indicated above and Y is the peptide chain of an antagonist or agonist for a non-bradykinin receptor.Type: GrantFiled: May 12, 1995Date of Patent: June 3, 1997Assignee: Cortech, Inc.Inventors: John C. Cheronis, James K. Blodgett, Eric T. Whalley, Shadrach R. Eubanks, Lisa G. Allen, Khe T. Nguyen
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Patent number: 5620958Abstract: A bradykinin antagonist of the formula:X(BKA).sub.nwherein BKA is the peptide chain of a bradykinin antagonist peptide, X is a linking group and n is a whole number greater than 1. The BKA substituents may be the same or different. Monomeric antagonists of the formula X(BKA) are also disclosed. Also disclosed are bradykinin antagonists of the formula:(Y)(X)(BKA)where X and BKA have the meanings indicated above and Y is the peptide chain of an antagonist or agonist for a non-bradykinin receptor.Type: GrantFiled: April 13, 1994Date of Patent: April 15, 1997Assignee: Coretech, Inc.Inventors: John C. Cheronis, James K. Blodgett, Eric T. Whalley, Shadrach R. Eubanks, Lisa G. Allen, Khe T. Nguyen
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Patent number: 5610140Abstract: The present invention provides a heterodimeric compound possessing bradykinin and neurokinin receptor antagonist activities useful in the treatment of asthma and other inflammatory diseases especially those involving the airway or pulmonary system. The present invention is also useful in the treatment of pain and inflammation.Type: GrantFiled: August 1, 1994Date of Patent: March 11, 1997Assignee: Cortech, Inc.Inventors: Val S. Goodfellow, Eric T. Whalley, Francine E. Wincott
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Patent number: 5610142Abstract: Novel compounds with as few as three natural amino acids that incorporate a substituted 4-keto-1,3,8-triazaspiro[4.5]decan-3-alkanoyl bridge in place of selected fragments of peptidic bradykinin receptor antagonists are pseudopeptides with potent bradykinin receptor antagonist actions. These pseudopeptides and their pharmaceutical compositions are of benefit in treating conditions and diseases of mammals, including humans, in which an excess of bradykinin or a related kinin is produced endogenously or is received exogenously, for example via insect bite.Type: GrantFiled: April 3, 1995Date of Patent: March 11, 1997Assignee: Scios Inc.Inventors: Babu J. Mavunkel, Zhijian Lu, Donald J. Kyle
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Patent number: 5597803Abstract: Peptides of the formula IZ-P-A-B-C-E-F-K-(D)Q-G-M-F'-I (I)and the physiologically tolerated salts thereof, are described.They have an excellent bradykinin-antagonistic action.They are obtained by reacting reacting a fragment with a C-terminal free carboxyl group or its activated derivative with a corresponding fragment with an N-terminal free amino group or assembling the peptide stepwise, where appropriate eliminating in the compound obtained in this way one or more protective groups introduced temporarily to protect other functionalities, and where appropriate converting the compounds of the formula I obtained in this way into the physiologically tolerated salt thereof.Type: GrantFiled: January 17, 1995Date of Patent: January 28, 1997Assignee: Hoechst AktiengesellschaftInventors: Gerhard Breipohl, Stephan Henke, Jochen Knolle, Bernward Scholkens, Hans-Georg Alpermann, Hermann Gerhards, Klaus Wirth
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Patent number: 5585355Abstract: The permeability of the blood-ocular barrier to therapeutic or diagnostic agents in the bloodstream of a host is increased by administering a permeabilizer peptide, preferably bradykinin or a bradykinin analogue, into the bloodstream of a host. The invention provides methods of treatment or diagnosis of ocular diseases by administration of a permeabilizer peptide, such as permeabilizer A-7, in combination with a therapeutic or diagnostic agent.Type: GrantFiled: September 12, 1994Date of Patent: December 17, 1996Assignee: Alkermes, Inc.Inventor: William F. Graney
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Patent number: 5558987Abstract: A method of treating a patient having a panic disorder, the patient having an elevated CCK peptide plasma level, by lowering the plasma CCK peptide level of the patient. A further method provides a diagnosis of panic disorder in a patient by detecting if that patient's plasma contains elevated CCK peptide levels. A further method determines the efficacy of the drug for the treatment of panic disorder by detecting the ability of the drug to lower elevated CCK peptide levels in a model for panic disorder. Additionally, a method of dosing a patient having elevated CCK peptide levels with an antipanic disorder drug is characterized by administering the drug to a patient and monitoring the lowering of the elevated plasma CCK peptide levels of the patient.Type: GrantFiled: November 18, 1994Date of Patent: September 24, 1996Assignee: University of South FloridaInventors: Thomas N. Thomas, David V. Sheehan, Janet D. Talbot
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Patent number: 5552383Abstract: Pseudopeptide compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. All or a portion of the amino acids at postions 2 through 5 of the bradykinin sequence are replaced by 2-pyrrolidinyl and/or amino-alkanoic acid or related olefinic derivatives to reduce the peptidic nature of the compounds.The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.Type: GrantFiled: September 9, 1993Date of Patent: September 3, 1996Assignee: Scios Nova Inc.Inventors: Donald J. Kyle, Babu J. Mavunkel
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Patent number: 5552520Abstract: Peptide derivatives containing one or more substituents separately linked by an amide, amino or sulfonamide bond to an amino group on either the N-terminal end or side chain of a biologically active peptide moiety. The peptide derivatives have relatively enhanced biological activity when compared to the corresponding peptide alone.Type: GrantFiled: August 9, 1994Date of Patent: September 3, 1996Assignee: Biomeasure, Inc.Inventors: Sun H. Kim, Susan R. Keyes, Sylviane Moreau, Zheng X. Dong, John Taylor
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Patent number: 5543496Abstract: Cyclic compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. Amino acid substitutions are made at postions 2 and 5 or 6 to facilitate the cyclization of the peptide through covalent bonding of the amino acid side chains.The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.Type: GrantFiled: July 25, 1994Date of Patent: August 6, 1996Assignee: Scios Nova Inc.Inventors: Donald J. Kyle, Sarvajit Chakravarty
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Patent number: 5541286Abstract: Pseudopeptide compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. Amino acids at at positions 2 through 5 are replaced by olefinic aminoalkenoyl groups to reduce the peptide nature of the compounds.The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.Type: GrantFiled: July 28, 1994Date of Patent: July 30, 1996Assignee: Scios Nova Inc.Inventor: Donald J. Kyle
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Patent number: 5521158Abstract: The invention relates to peptides of up to 10 amino acids that are synthesized by substituting at least one of the bradykinin amino acids found in positions 2, 3, 4 and 5 of the bradykinin peptide with a fatty acid amine. The modified bradykinin peptides produced confer increased resistance to enzymatic degradation and/or tissue specificity. The invention also relates to pharmaceutical preparations and processes of treatments using the modified bradykinin peptides.Type: GrantFiled: October 8, 1992Date of Patent: May 28, 1996Assignee: Scios Nova Inc.Inventors: Donald J. Kyle, Babu J. Mavunkel
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Patent number: 5506206Abstract: Polypeptides called receptor mediated permeabilizers (RMP) increase the permeability of the blood-brain barrier to molecules such as therapeutic agents or diagnostic agents. These receptor mediated permeabilizers are more efficacious than bradykinin in causing the blood-brain barrier to become more permeable. The permeabilizer A-7 or conformational analogues can be intravenously co-administered to a host together with molecules whose desired destination is the cerebrospinal fluid compartment of the brain. The permeabilizer A-7 or conformational analogues allow these molecules to penetrate the blood-brain barrier and arrive at this destination.Type: GrantFiled: September 13, 1993Date of Patent: April 9, 1996Assignee: Alkermes, Inc.Inventors: John W. Kozarich, Gary F. Musso, Bernard Malfroy-Camine
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Patent number: 5444048Abstract: Pseudopeptide compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. Amino acids at postions 2 through 5 are replaced by olefinic aminoalkenoyl groups to reduce the peptidic nature of the compounds.The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.Type: GrantFiled: September 9, 1993Date of Patent: August 22, 1995Assignee: Scios Nova, Inc.Inventor: Donald J. Kyle
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Patent number: 5434132Abstract: Oligopeptides have been found that antagonist cell proliferation stimulated not only by bombesin-like peptides but also other neuropeptides e.g. vasopressin and bradykinin. These oligopeptides block a broad family of mitogenic neuropeptides that bind to receptors that use the inositol signalling pathway and one such receptor has been identified. These oligopeptides are of particular interest in relation to small cell lung cancer.Type: GrantFiled: November 2, 1993Date of Patent: July 18, 1995Assignee: Imperial Cancer Research Technology, Ltd.Inventors: Enrique Rozengurt, Penella Woll
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Patent number: 5416191Abstract: A bradykinin antagonist of the formulaX(BKA).sub.nwherein BKA is the peptide chain of a bradykinin antagonist peptide, X is a linking group and n is a whole number greater than 1. The BKA substituents may be the same or different. Monomeric antagonists of the formula X(BKA) are also disclosed.Type: GrantFiled: January 8, 1993Date of Patent: May 16, 1995Assignee: Cortech, Inc.Inventors: John C. Cheronis, Eric T. Whalley, Khe T. Nguyen, Shadrach R. Eubanks, Lisa G. Allen
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Patent number: 5409899Abstract: Compound of formula:G-Arg-Pro-Hyp-Gly-Thia-Ser-Tic-Oic-Arg-OHwhere G, Arg, Pro, Hyp, Gly, Thia, Ser, Tic and Oic are defined in the description.Medicinal products.Type: GrantFiled: January 13, 1993Date of Patent: April 25, 1995Assignee: Adir et CompagnieInventors: Jean-Luc Fauchere, Christophe Thurieau, Emmanuel Canet
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Patent number: 5385889Abstract: The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with a D-configuration hydroxyproline ether or thioether converts bradykinin agonists into bradykinin antagonists. The invention further includes the intermediate compounds and additional modifications at other positions within the novel 7-position modified bradykinin antagonists which increase enzyme resistance, antagonist potency, and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.Type: GrantFiled: December 16, 1993Date of Patent: January 31, 1995Assignee: Scios Nova Inc.Inventors: Donald J. Kyle, Roger N. Hiner
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Patent number: 5369015Abstract: Disclosed is a method for producing an angiotensin converting enzyme inhibitor composition from natural materials, which composition is of use as an antihypertensive drug or diet. The method comprises heating a meat in water at a temperature not lower than 50.degree. C. to extract water-soluble protein and hydrolyzing the residue predominantly composed of water-insoluble protein with a protease.Type: GrantFiled: October 14, 1992Date of Patent: November 29, 1994Assignee: Nippon Gohsei Kagaku Kogyo Kabushiki KaishaInventors: Masaaki Yoshikawa, Keiichi Yokoyama, Masayasu Hasegawa, Ryouichi Yasumoto, Hiroyuki Fujita
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Patent number: 5304632Abstract: The invention relates to a peptide, characterized in that it corresponds to the following sequence of amino acids:Xaa.sub.1 Pro Xaa.sub.2 Pro Xaa.sub.3 Xaa.sub.4 Phe Tyr Gly Leu Metin which a.sub.n with n equal to 1, 2, 3 or 4 represents any amino acid, and in particular in that the peptide is ranakinin having the following formula:Lys Pro Asn Pro Glu Arg Phe Tyr Gly Leu MetThe invention also relates to the use of this peptide in pharmacological applications.Type: GrantFiled: September 3, 1991Date of Patent: April 19, 1994Assignees: Creighton University, Centre National de la Recherche ScientifiqueInventors: Hubert Vaudry, J. Michael Conlon
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Patent number: 5268164Abstract: Polypeptides called receptor mediated permeabilizers (RMP) increase the permeability of the blood-brain barrier to molecules such as therapeutic agents or diagnostic agents. These receptor mediated permeabilizers are more efficacious than bradykinin in causing the blood-brain barrier to become more permeable. The permeabilizer A-7 or conformational analogues can be intravenously co-administered to a host together with molecules whose desired destination is the cerebrospinal fluid compartment of the brain. The permeabilizer A-7 or conformational analogues allow these molecules to penetrate the blood-brain barrier and arrive at this destination.Type: GrantFiled: April 23, 1991Date of Patent: December 7, 1993Assignee: Alkermes, Inc.Inventors: John W. Kozarich, Gary F. Musso, Bernard Malfroy-Camine
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Patent number: 5162497Abstract: A bradykinin analog which contains nine or ten amino acid residues and at least one [CH.sub.2 NH] pseudopeptide bond, the analog being useful as an antagonist or agonist of the naturally occuring bradykinin.Type: GrantFiled: December 9, 1988Date of Patent: November 10, 1992Assignee: The Administrators of the Tulane Educational FundInventors: David H. Coy, Jacques-Pierre Moreau, John E. Taylor, Sun H. Kim
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Patent number: 4923963Abstract: The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with an aliphatic, cyclic or aromatic amino acid of the D-configuration converts bradykinin agonists into a bradykinin antagonist. The invention further includes additional modifications at other positions within the novel 7-position modified bradykinin antagonists including C-terminal and N-terminal extensions and replacement of arginine in the one and nine positions which increase enzyme resistance, antagonist potency and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of the mannal and human body in which an excess of bradykinin or related kinins are produced or injected as by bites into the body.Type: GrantFiled: September 2, 1987Date of Patent: May 8, 1990Assignee: Nova Technology Limited PartnershipInventors: John M. Stewart, Raymond J. Vavrek
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Patent number: 4801613Abstract: The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with an aromatic amino acid or the D-configuration converts bradykinin agonists into a bradykinin antagonist. The invention further includes additional modifications at other positions within the novel 7-position modified bradykinin antagonists which increase enzyme resistance, antagonist potency and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of the mammal and human body in which an excess of bradykinin or related kinins are produced or injected as by bites into the body.Type: GrantFiled: June 17, 1987Date of Patent: January 31, 1989Assignee: Nova Technology Limited PartnershipInventors: John M. Stewart, Raymond J. Vavrek
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Patent number: 4728725Abstract: Retro-inverted peptides, analogues of Bradykinin Potentiator Pentapeptide (BPP.sub.5a), definable by the general formula (I) ##STR1## useful as antihypertensives and diagnostics.Type: GrantFiled: December 20, 1985Date of Patent: March 1, 1988Assignees: Enichem, S.p.A., Eniricerche, S.p.A.Inventors: Alessandro Sisto, Antonio S. Verdini, Antonino Virdia
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Patent number: 4713367Abstract: New partially retro-inverso peptides of the following general formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and represent, each independently, the side chain of the aminoacid residues present in the naturally occuring peptides, X is --S--Ph or --O--CH.sub.2 --Ph and Z is a hydroxy, alkoxy or amino group, are described as well as a suitable method for their preparation. The new compounds are useful as antihypertensive agents.Type: GrantFiled: January 22, 1986Date of Patent: December 15, 1987Assignee: Enichem S.p.A.Inventors: Alessandro Sisto, Antonio S. Verdini, Antonino Virdia
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Patent number: 4693993Abstract: The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with an aromatic amino acid or the D-configuration converts bradykinin agonists into a bradykinin antagonist. The invention further includes additional modifications at other positions within the novel 7-position modified bradykinin antagonists which increase enzyme resistance, antagonist potency and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of the mammal and human body in which an excess of bradykinin or related kinins are produced or injected as by bites into the body.Type: GrantFiled: June 13, 1985Date of Patent: September 15, 1987Inventors: John M. Stewart, Raymond J. Vavrek