Lutenizing Hormone Releasing Factor (lrf); Related Peptides Patents (Class 530/313)
-
Patent number: 5998368Abstract: There are provided novel compounds for the treatment of male impotence. The compounds are derived from vasoactive intestinal peptide (VIP) in which the natural amino acid sequence is modified by replacement of any of the 5, 17 and 19 amino acid residues by other natural or non-natural amino acids, and they bear at least one terminal lipophilic group.The modified VIP sequences are prepared by conventional peptide chain assembling methods.The novel compounds and compositions containing them are suitable for transdermal application for treating male impotence.Type: GrantFiled: July 21, 1997Date of Patent: December 7, 1999Assignees: Yeda Research and Development Co. Ltd., Ramot University Authority for Applied Research and Industrial Development Ltd.Inventors: Illana Gozes, Matityahu Fridkin
-
Patent number: 5990166Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: February 7, 1997Date of Patent: November 23, 1999Assignee: Emisphere Technologies, Inc.Inventors: Andrea Leone-Bay, Eric Wang, Donald J. Sarubbi, Harry Leipold
-
Patent number: 5985834Abstract: Described are LHRH-antagonistic and bombesin-antagonistic nona- and decapeptides suitable for use in the preparation of a drug for the treatment of AIDS and ARC as well as for use in the preparation of an immunostimulation drug.Type: GrantFiled: December 18, 1995Date of Patent: November 16, 1999Assignee: ASTA Medica AGInventors: Jurgen Engel, Bernhard Kutscher, Michael Bernd, Ulf Niemeyer
-
Patent number: 5981489Abstract: This invention relates to stable non-aqueous protic formulations of peptide compounds. These stable formulations comprise peptide in non-aqueous protic solvent. They may be stored at elevated temperatures for long periods of time and are especially useful in implantable delivery devices for long term delivery of drug.Type: GrantFiled: June 13, 1997Date of Patent: November 9, 1999Assignee: Alza CorporationInventors: Cynthia L. Stevenson, Sally A. Tao, Steven J. Prestrelski, James B. Eckenhoff, deceased, Jeremy C. Wright, John J. Leonard, Jr.
-
Patent number: 5972891Abstract: A sustained-release preparation which comprises a physiologically active peptide of general formula ##STR1## wherein X represents an acyl group; R.sub.1, R.sub.2 and R.sub.4 each represents an aromatic cyclic group;R.sub.3 represents a D-amino acid residue or a group of the formula ##STR2## wherein R.sub.3 ' is a heterocyclic group; R.sub.5 represents a group of the formula --(CH.sub.2).sub.n --R.sub.5 ' wherein n is 2 or 3, and R.sub.5 ' is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group;R.sub.6 represents a group of the formula --(CH.sub.2).sub.n --R.sub.6 ' wherein n is 2 or 3, and R.sub.6 ' is an amino group which may optionally be substituted;R.sub.7 represents a D-amino acid residue or an azaglycyl residue; andQ represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group.Type: GrantFiled: July 14, 1997Date of Patent: October 26, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigeru Kamei, Yasutaka Igari, Yasuaki Ogawa
-
Patent number: 5968895Abstract: Sustained delivery formulations comprising a water-insoluble complex of a peptide and a carrier macromolecule are disclosed. The formulations of the invention allow for loading of high concentrations of peptide in a small volume and for delivery of a pharmaceutically active peptide for prolonged periods, e.g., one month, after administration of the complex. The complexes of the invention can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. In a preferred embodiment, the peptide of the complex is an LHRH analogue, preferably an LHRH antagonist, and the carrier macromolecule is an anionic polymer, preferably carboxymethylcellulose. Methods of making the complexes of the invention, and methods of using LHRH-analogue-containing complexes to treat conditions treatable with an LHRH analogue, are also disclosed.Type: GrantFiled: December 11, 1996Date of Patent: October 19, 1999Assignee: Praecis Pharmaceuticals, Inc.Inventors: Malcolm L. Gefter, Nicholas Barker, Gary Musso, Christopher J. Molineaux
-
Patent number: 5939381Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: February 7, 1997Date of Patent: August 17, 1999Assignee: Emisphere Technologies, Inc.Inventors: Andrea Leone-Bay, Eric Wang, Donald J. Sarubbi, Harry Leipold
-
Patent number: 5932547Abstract: This invention relates to stable non-aqueous polar aprotic formulations of peptide compounds. These stable formulations comprise peptide in non- aqueous polar aprotic solvent. They may be stored at elevated temperatures for long periods of time and are especially useful in implantable delivery devices for long term delivery of drug.Type: GrantFiled: June 13, 1997Date of Patent: August 3, 1999Assignee: ALZA CorporationInventors: Cynthia L. Stevenson, Steven J. Prestrelski
-
Patent number: 5925730Abstract: Peptides are provided which have improved duration of GnRH antagonistic properties. These antagonists may be used to regulate fertility and to treat steroid-dependent tumors and for other short-term and long-term treatment indications. These antagonists have a derivative of aminoPhe or its equivalent in the 5- and/or 6-positions. This derivative contains a carbamoyl group or a heterocycle including a urea in its side chain. Particularly effective decapeptides, which continue to exhibit very substantial suppression of LH secretion at 96 hours following injection, have the formulae: Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(hydroorotyl)-D-4Aph(acetyl)-Leu-Lys(isopr opyl)-Pro-D-Ala-NH.sub.2, and Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(hydroorotyl)-D-4Amf(Q.sub.2)-Leu-Lys(isop ropyl)-Pro-D-Ala-NH.sub.2, wherein Q.sub.2 is Cbm or MeCbm.Type: GrantFiled: April 11, 1997Date of Patent: July 20, 1999Assignee: Ferring BVInventors: Graeme Semple, Guangcheng Jiang
-
Patent number: 5908824Abstract: A nasally administrable composition having a physiologically active peptide dispersed homogeneously in and adsorbed homogeneously onto a unique carrier. The composition contains an effective amount of physiologically active peptide dispersed homogeneously in and adsorbed homogeneously onto a mucosa protecting and/or tissue repairing agent, e.g., gefarnate, aceglutamide aluminum, sucralfate, L-glutamine, sofalcone, teprenone, plaunotol, rebamipide, aldioxa, cetraxate or troxipide.Type: GrantFiled: October 16, 1996Date of Patent: June 1, 1999Assignee: Dott Research LaboratoryInventor: Akira Yanagawa
-
Patent number: 5897863Abstract: An analogue of lutenising hormone-releasing hormone (LHRH) having the amino acid sequence: pGlg-His-Trp-Ser-Tyr-X-Len-Arg-Pro-Gly-Y-Zwherein X represents Gly or a D-amino acid, Y represents one or more amino acid residues, which may be the same or different, and Z represents Cys or Tyr, such that the solution conformation of said analogue is substantially similar to that of native LHRH. The analogues may be used to prepare vaccines for reducing fertility in mammals.Type: GrantFiled: June 7, 1995Date of Patent: April 27, 1999Assignee: Proteus Molecular Design LimitedInventors: Barry Robson, Robert V. Fishleigh
-
Patent number: 5885966Abstract: The invention relates to a modified tandem LHRH-peptide vaccine preparation in which the amino acid glycine at position (6) of one or both LHRH decapeptides that constitute the tandem unit is substituted by a dextrorotatory amino acid that contains a side chain to whicha carrier compound can be coupled. In addition, the tandem LHRH-peptide can be brought into a tandem-dimer form which is also suitable for producing a vaccine that is effective against LHRH (luteinizing hormone releasing hormone) also referred to as GnRH (gonadotropin-releasing hormone), for immunological castration, to inhibit or affect reproductive functions or to affect behaviour in vertebrates in general and in domesticated animals and man in particular.Type: GrantFiled: December 5, 1997Date of Patent: March 23, 1999Assignee: DLO Instituut Voor Dierhouderij En DiergezondheidInventors: Robert Hans Meloen, Hendrica Berendina Oonk
-
Patent number: 5871886Abstract: A method of patterning a layer of reflective material, such as a layer of conductor metal, using a layer of antireflection coating material sandwiched between two layers of photoresist. A first layer of photoresist is formed on an integrated circuit wafer and provides a planar surface for subsequent layers of material. A layer of antireflection coating material is formed on the layer of first photoresist and a layer of second photoresist is formed on the layer of antireflection coating material. The layer of second photoresist is selectively exposed and developed. The layer of antireflection coating material is patterned using dry etching and the patterned layer of second photoresist as a mask. The layer of first photoresist is then patterned using dry etching and the patterned layer of antireflection coating material as a mask. The layer of reflecting material is then patterned using dry etching and the patterned layer of first photoresist as a mask. The patterned layer of first photoresist is then removed.Type: GrantFiled: December 12, 1996Date of Patent: February 16, 1999Assignee: Taiwan Semiconductor Manufacturing Company, Ltd.Inventors: Chen-Hua Yu, Syun-Ming Jang
-
Patent number: 5863900Abstract: The present invention provides novel LHRH antagonists and complexes between these antagonists and VB12. The present invention is particularly useful for the oral administration of LHRH antagonists. The antagonists of the invention are selected from the group consisting of ANTIDE-1, ANTIDE-2 and ANTIDE-3.Type: GrantFiled: January 16, 1996Date of Patent: January 26, 1999Assignee: Biotech Australia Pty., Ltd.Inventor: Gregory John Russell-Jones
-
Patent number: 5847066Abstract: A peptide which is a variant of the human growth hormone-releasing factor. The peptide, containing 23-28 amino acid residues, differs from its native counterpart at least at positions 8, 9, 16, 18, 24, 25, 27, and 28, and is potent in stimulating the release of growth hormone.Type: GrantFiled: April 12, 1996Date of Patent: December 8, 1998Assignee: The Administrators of the Tulane Educational FundInventors: David H. Coy, William Murphy
-
Patent number: 5846934Abstract: A method for decreasing the effect of somatostatin. A peptide of formula I which is a pure somatostatin antagonist, methods for increasing the release of growth hormone, insulin and glucagon in mammals, and a method for the enhancement of growth in mammals are also described.Type: GrantFiled: February 19, 1997Date of Patent: December 8, 1998Assignee: American Cyanamid CompanyInventors: Roy Tyson Bass, Brian Lee Buckwalter, John Richard Hadcock, Bomi Pilloo Patel, John Francis Chiarello
-
Patent number: 5824646Abstract: Pharmaceutical compositions of matter adapted for intravaginal administration comprise a biologically active polypeptide, an absorption promoter, such as an anionic and/or nonionic surfactant or a nonionic surfactant and an aliphatic carboxylic acid, optionally an animal and/or vegetable protein and a nontoxic pharmaceutically acceptable carrier or diluent therefor, in a formulation suitable for intravaginal administration. Preferred compositions comprise calcitonin as the biologically active polypeptide. Preferred absorption promoters are anionic surfactants, e.g., sodium lauryl sulfate, and the combination absorption promoter of a nonionic surfactant and a medium chain aliphatic carboxylic acid or its salt, e.g. polyoxyethylenealkylphenylether and a medium chain aliphatic carboxylic acid.Type: GrantFiled: November 17, 1997Date of Patent: October 20, 1998Assignee: Teikoku Seiyaku Co., Ltd.Inventors: Takeru Fujii, Seiichi Sako, Shigeyuki Takama, Toru Hibi, Akiya Yamada
-
Patent number: 5817753Abstract: Endogenous and exogenous proteins, and fragments thereof, are chemically modified outside the body of an animal so that when injected into the animal they produce more antibodies against the unmodified protein than would injection of the unmodified protein or fragment alone. The chemical modification may be accomplished by attaching the proteins or fragments to carriers such as, for example, bacterial toxoids. The chemical modification can also be accomplished by polymerization of protein fragments. Proteins which can be modified include Follicle Stimulating Hormone and Human Chorionic Gonadotropin. The modified polypeptides may be administered to animals for the purpose of contraception, abortion or treatment of hormone-related disease states and disease disorders, treatment of hormone-associated carcinomas, and to boost the animals resistance to exogenous proteins, for example viral proteins.Type: GrantFiled: October 6, 1992Date of Patent: October 6, 1998Assignee: The Ohio State University Research FoundationInventor: Vernon C. Stevens
-
Patent number: 5811512Abstract: Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor.Type: GrantFiled: January 19, 1996Date of Patent: September 22, 1998Assignee: The Trustees of the University of PennsylvaniaInventors: Ralph F. Hirschmann, Paul Sprengeler, Wenqing Yao
-
Patent number: 5807983Abstract: Betides having at least one betidamino acid are provided which have GnRH antagonistic properties. These antagonists may be used to regulate fertility and to treat steroid-dependent tumors, such as prostatic and mammary tumors. One particularly effective betide, which is an analog of the decapeptide GnRH that is highly soluble in water at physiologic pH, has the formula: Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-Aph(acetyl)-D-Aph(acetyl)-Leu-D/L-Agl(methyl,i sopropyl .beta.-alanyl)-Pro-D-Ala-NH.sub.2, and another has the formula Ac-D-2Nal-D-Cpa-D-3Pal-D/L-Agl(For)-Aph(Ac)-D-Aph(Ac)-Leu-ILys-Pro-D-Ala-N H.sub.2.Type: GrantFiled: February 8, 1996Date of Patent: September 15, 1998Assignee: The Salk Institute for Biological StudiesInventors: Guangcheng Jiang, Jean E. F. Rivier
-
Patent number: 5783562Abstract: A method is provided for the design and synthesis of Leuteinizing Hormone Releasing Hormone (LHRH) antagonists having exact amino acid sequences and containing 5-100 amino acids. This method can be used to produce peptides useful in treating disorders of the reproductive endocrine system, including endometriosis, precocious puberty, prostate cancer and breast cancer. Additionally, peptides produced by this method can be used as contraceptives for either males or females. Peptides produced by this method can further be employed in the diagnosis and treatment of infertility.Type: GrantFiled: May 23, 1995Date of Patent: July 21, 1998Assignee: Asta Medica AktiengesellschaftInventor: Xiao Shaobo
-
Patent number: 5767082Abstract: Synthetic nona- and decapeptide LHRH antagonist analogs are disclosed, having a sterically hindered guanidino-substituted arginyl or homoarginyl residue at position 8, with no arginyl substituent at position 6.Type: GrantFiled: June 2, 1993Date of Patent: June 16, 1998Assignee: Syntex (U.S.A.) Inc.Inventors: John J. Nestor, Jr., Brian H. Vickery
-
Patent number: 5763404Abstract: Antide is the decapeptide, N-Ac-D-2-Nal,D-pClPhe, D-3-Pal, Ser,NicLys, D-NicLys, Leu, ILys, Pro, D-Ala,NH.sub.2 which is an antagonist of luteinizing hormone releasing hormone (LHRH). This decapeptide, like others of the present invention, has high antiovulatory activity (AOA) and releases negligible histamine. Antide is scheduled for scale-up, safety testing and evaluation in the experimental primate and in clinical medicine. Numerous other peptides having structures related to Antide were prepared and tested. These peptides had variations primarily in positions 5, 6, 7, and 8. Of these, N-Ac-D-2-Nal, D-pClPhe,D-3-Pal,Ser,PicLys,cis-DPzACAla,Leu,ILys,Pro,D-Ala-NH.sub.2 was one of the most potent and had higher antiovulatory activity than Antide, i.e. 73%/0.25 ug and 100%/0.5 ug vs. 36%/0.5 ug and 100%/1.0 ug. Antide showed significant, (p<0.001) duration of action, when injected at a dose of 10 ug, 44 hours before 50 ng of the agonist, ?D-3-Qal.sup.6 !-LHRH.Type: GrantFiled: June 6, 1995Date of Patent: June 9, 1998Inventors: Karl A. Folkers, Cyril Y. Bowers, Anders Ljungqvist, Pui-Fun Louisa Tang, Minoru Kubota, Dong-Mei Feng
-
Patent number: 5760000Abstract: The invention provides a method for treating liver cancer in a mammal comprising administering to the mammal an inhibitory effective amount of at least one GnRH-related compound. Pharmaceutical preparations useful for the treatment of liver cancer comprising an inhibitory effective amount of at least one GnRH-related compound and a pharmaceutically acceptable carrier are also provided. A further aspect of the invention provides a method for diagnosing liver cancer by determining the presence of receptors for GnRH on a biological sample.Type: GrantFiled: May 13, 1994Date of Patent: June 2, 1998Assignee: University Technologies International,Inc.Inventor: Hamid R. Habibi
-
Patent number: 5744450Abstract: Peptides which include unnatural amino acids and which either promote or inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such peptides that are GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads and may be used to treat steroid-dependent tumors. The agonists can be used for control of reproduction processes, to treat precocious puberty, endometriosis, and the like. The peptides are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions.Type: GrantFiled: June 2, 1995Date of Patent: April 28, 1998Assignee: The Salk Institute for Biological StudiesInventors: Carl A. Hoeger, Jean E. F. Rivier, Paula Guess Theobald, John S. Porter, Catherine L. Rivier, Wylie Walker Vale, Jr.
-
Patent number: 5698522Abstract: The present invention provides a class of decapeptide compounds which are potent antagonists of LHRH activity and which have the structure A.sup.1 -D.sup.2 -E.sup.3 -G.sup.4 -J.sup.5 -L.sup.6 -M.sup.7 -Q.sup.8 -R.sup.9 -T.sup.10. The compounds of the percent invention are characterized by having an .OMEGA.-amino-functionalized side chain on the D-aminoacyl residue at position 6. The .OMEGA.-amino group of this side chain is further derivatized by the attachment of an extending group which likewise has a terminal amino group which is capped by an acyl group.Type: GrantFiled: June 1, 1995Date of Patent: December 16, 1997Assignee: Abbott LaboratoriesInventors: Fortuna Haviv, Timothy D. Fitzpatrick, Rolf E. Swenson, Charles J. Nichols, Nicholas A. Mort, Jonathan Greer
-
Patent number: 5688506Abstract: Immunogenic compositions capable of generating an immune response in mammals against GnRH are disclosed. The immunogenic compositions are effective in methods of treating gonadotropin and gonadal steroid hormone dependent diseases and immunological contraception of mammals.Type: GrantFiled: January 27, 1994Date of Patent: November 18, 1997Assignee: Aphton Corp.Inventors: Stephen Grimes, Robert Scibienski
-
Patent number: 5656727Abstract: LHRH analogs and congeners with high water solubility have been synthesized. These new analogs had 0%-100% antiovulatory activity at a 0.5 .mu.g dosage and 0%-80% at 0.25 .mu.g. The ED.sub.50 for histamine release was 30.5 .mu.g/ml->300 .mu.g/ml.Type: GrantFiled: April 28, 1995Date of Patent: August 12, 1997Assignees: The Administrators of the Tulane Educational Fund, Board of Regents, The University of Texas SystemInventors: Cyril Y. Bowers, Karl A. Folkers, Anna Janecka
-
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
-
Patent number: 5631229Abstract: Certain toxic compounds (T) such as, for example, compounds based upon diphtheria toxin, ricin toxin, pseudomonas exotoxin, .alpha.-amanitin, pokeweed antiviral protein (PAP), ribosome inhibiting proteins, especially the ribosome inhibiting proteins of barley, wheat, corn, rye, gelonin and abrin, as well as certain cytotoxic chemicals such as, for example, melphalan and daunomycin can be conjugated to certain analogs of gonadotropin-releasing hormone to form a class of compounds which, when injected into an animal, destroy the gonadotrophs of the animal's anterior pituitary gland. Hence such compounds may be used to sterilize such animals and/or to treat certain sex hormone related diseases.Type: GrantFiled: July 7, 1993Date of Patent: May 20, 1997Assignee: Colorado State University Research FoundationInventors: Torrance M. Nett, Leonard M. Glode
-
Patent number: 5618513Abstract: A method for radiolabelling peptides using polyaminocarboxylate ligands having suitable protecting groups such that they can be added to peptides by standard solid phase or solution phase peptide synthetic chemistry and can be deproteced using standard cleavage/deprotection reagents and produce the peptide/chelate conjugate as a high purity mono-addition product is provided. The cleaved and deprotected ligand-peptide molecules can then be labeled with lanthanide or actinide radionuclides. The protected polyaminocarboxylate ligands form mono-anhydrides or mono-active esters under solid phase or solution phase conditions and permit only the desired monoaddition chelate-peptide conjugate to be formed.Type: GrantFiled: June 7, 1995Date of Patent: April 8, 1997Assignee: Mallinckrodt Medical, Inc.Inventor: Ananthachari Srinivasan
-
Patent number: 5580957Abstract: Peptides which include unnatural amino acids and which either promote or inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such peptides that are GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads and may be used to treat steroid-dependent tumors. The agonists can be used for control of reproduction processes, to treat precocious puberty, endometriosis, and the like. The peptides are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions.Type: GrantFiled: March 18, 1994Date of Patent: December 3, 1996Assignee: The Salk Institute for Biological StudiesInventors: Carl A. Hoeger, Jean E. F. Rivier, Paula G. Theobald, John S. Porter
-
Patent number: 5573767Abstract: Method for improving the organoleptic qualities of the meat from uncastrated male domestic animals, vaccines which are usable in this method, new peptide, in particular, for producing these vaccines and vaccination kit relating thereto.The method for improving the organoleptic qualities, especially the smell, taste and tenderness, of the meat from uncastrated male domestic animals comprises, shortly before slaughter of the animal in question, abolition of the action of the androgenic and non-androgenic steroids by active or passive anti-LHRH immunoneutralization, while the advantages linked to the male character of the animal are maintained virtually up to slaughter. The vaccines comprise, as a peptide, natural LHRH or a peptide of formula Trp - Ser - Tyr - Gly - Leu - Arg - Pro - Gly - NH.sub.2, coupled to an immunogenic carrier protein.Type: GrantFiled: November 17, 1994Date of Patent: November 12, 1996Assignee: Societe AnonymeInventors: Raymond Dufour, Claude Roulet, Claire Chouvet, Michel B. Bonneau
-
Patent number: 5565574Abstract: Methods of making unnatural amino acids are provided which unnatural amino acids can be incorporated into peptides which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. These unnatural amino acids are useful in the synthesis of peptides and have the formula (a): ##STR1## where W is (CH.sub.2).sub.n or ##STR2## n is an integer from 1 to 6; j=1, 2 or 3, and preferably, Y is N--CN, X is NH and R.sub.2 is alkyl, modified alkyl, alkenyl, alkynyl, aryl or methyl pyridyl. Disclosed are peptides that are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions.Type: GrantFiled: August 11, 1994Date of Patent: October 15, 1996Assignee: The Salk Institute for Biological StudiesInventors: Carl A. Hoeger, Jean E. F. Rivier, John S. Porter
-
Patent number: 5556836Abstract: Use of 7-amino-L-glycero-L-gulo-2,6-anhydro-7-desoxy-heptonic acid and 2-benzoxycarbonylamino-0.sup.1 -methyl-2-desoxy-.beta.-glucopyranuronic acid, their derivatives and the enantiomorphous compounds for incorporation and for manufacture in pharmacologically active peptide hormones.Type: GrantFiled: November 1, 1994Date of Patent: September 17, 1996Assignee: Asta Medica AktiengesellschaftInventors: Erich G. Roedern, Horst Kessler, Bernhard Kutscher, Michael Bernd, Thomas Klenner
-
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
-
Patent number: 5527777Abstract: The invention concerns LHRH antagonists of the general formula (I),X-X.sub.1 -X.sub.2 -X.sub.3 -L-Ser-L-Tyr-X.sub.6 -L-Leu-X.sub.8 -L-Pro-X.sub.10 (I)The invention concerns LHRH antagonists of the general formula (I), in which X is an acyl group, X.sub.1 is a D-Nal, X.sub.2 is D-(4-Cl)-Phe, X.sub.3 is D-(3)-Pal, X.sub.6 is D-Cit or D-Neu, X.sub.8 is L-Arg or L-Neu, at least one of the groups X.sub.6 and X.sub.8 being a Neu, and X.sub.10 is D-Ala-NH.sub.2, Neu being a group of formula (II), (IV), (IX) or (X), wherein W is one of the group (a)-(d). The invention includes drugs containing a compound of formula (I), plus the usual auxiliaries and carriers. These drugs are suitable for use in cases of carcinoma of the prostate and in endometriosis, as well as for fertility control.Type: GrantFiled: May 4, 1994Date of Patent: June 18, 1996Assignee: Schering AktiengesellschaftInventors: Paul Thamm, Alessandro Lobbia, Thomas Brumby, Johann Mulzer, Fridtjog Schroder, Ursula Habenicht
-
Patent number: 5527882Abstract: The present invention relates to one or more polypeptides having useful biological activity in a mammal, which comprise:a polypeptide related to bradykinin of four to ten amino acid residues wherein one or more specific amino acids in the polypeptide chain are replaced with achiral N-benzylglycine. These polypeptide analogues have useful potent agonist or antagonist pharmacological properties depending upon the structure. A preferred polypeptide is (N-benzylglycine.sup.7)-bradykinin.Type: GrantFiled: November 7, 1994Date of Patent: June 18, 1996Assignee: The Regents of the University of CaliforniaInventors: Alexander R. Mitchell, Janis D. Young
-
Patent number: 5516887Abstract: A luteinizing hormone releasing hormone antagonist peptide is provided which effectively decreases plasma levels of estrogens and androgens. The peptide exhibits increased levels of potency while at the same time minimizing histamine releasing properties, vascular permeability (or edematogenic effects), hypotension, poor water solubility an inadequate duration of action associated with luteinizing hormone releasing hormone antagonist peptides of the past.Type: GrantFiled: January 17, 1994Date of Patent: May 14, 1996Assignee: Romano DeghenghiInventor: Romano Deghenghi
-
Patent number: 5516759Abstract: Peptides possessing LHRH antagonistic activity, and useful for the controlling the release of LHRH in mammals are decapeptide analogues of LHRH having a lactam group at the N-terminus of the formula ##STR1## where n is 1, 2, or 3 and R.sup.1 is selected from the group consisting of hydrogen, benzyl, 4-chlorobenzyl, 2-methylnaphth-1-yl, 1-methylnaphth-2-yl, and quinolin-3-ylmethyl.Type: GrantFiled: December 8, 1994Date of Patent: May 14, 1996Assignee: TAP Holdings Inc.Inventors: Rolf E. Swenson, Fortuna Haviv, Nicholas A. Mort
-
Patent number: 5510460Abstract: A process for the solid phase synthesis of peptides containing an aza-amino acid, for example the decapeptide goserelin, which comprises:(i) assembling all the amino acids of the peptide except the C-terminal aza-amino acid by conventional solid phase synthesis;(ii) cleaving the peptide from the support with hydrazine or a substituted hydrazine; and(iii) reacting the hydrazide thus released with a cyanate ion.Type: GrantFiled: May 26, 1995Date of Patent: April 23, 1996Assignee: Zeneca LimitedInventor: Christopher F. Hayward
-
Patent number: 5508383Abstract: A class of cyclic peptides are effective inhibitors of LHRH and are useful in the treatment of disease conditions which are mediated by sex hormones including prostate cancer, endometriosis, uterine fibroids, and precocious puberty.Type: GrantFiled: March 9, 1994Date of Patent: April 16, 1996Assignee: Tap Holdings Inc.Inventors: Daryl R. Sauer, Fortuna Haviv
-
Patent number: 5503989Abstract: Methods of preparing a peptide having a C-terminal amide group from peptides having a C-terminal carboxyl group are provided.Type: GrantFiled: August 10, 1992Date of Patent: April 2, 1996Assignee: Amylin Pharmaceuticals, Inc.Inventors: Jeffrey A. Bibbs, Laura S. Lehman De Gaeta, Howard Jones
-
Patent number: 5502035Abstract: Decapaptide and undecapaptides substituted on the N-terminal nitrogen atom by acyl groups which include furo-2-yl, isonicotinyl, nicotinyl, 2-, 3-, and 4-quinolinecarbonyl, shikimyl, dihydroshikimyl, and tetrahydrofur-2-oyl are potent antagonists of LHRH and are useful for suppressing the levels of sex hormones in mammals.Type: GrantFiled: July 27, 1994Date of Patent: March 26, 1996Assignee: Tap Holdings Inc.Inventors: Fortuna Haviv, Timothy D. Fitzpatrick, Rolf E. Swenson, Charles J. Nichols, Nicholas A. Mort
-
Patent number: 5492893Abstract: Certain toxic compounds (T) such as, for example, compounds based upon diphtheria toxin, ricin toxin, pseudomonas exotoxin, .alpha.-amanitin, pokeweed antiviral protein (PAP), ribosome inhibiting proteins, especially the ribosome inhibiting proteins of barley, wheat, corn, rye, gelonin and abrin, as well as certain cytotoxic chemicals such as, for example, melphalan and daunomycin can be conjugated to certain analogs of gonadotropin-releasing hormone to form a class of compounds which, when injected into an animal, destroy the gonadotrophs of the animal's anterior pituitary gland. Hence such compounds may be used to sterilize such animals and/or to treat certain sex hormone related diseases.Type: GrantFiled: July 20, 1993Date of Patent: February 20, 1996Assignee: Colorado State University Research FoundationInventors: Torrance M. Nett, Leonard M. Glode
-
Patent number: 5491217Abstract: A class of potent LHRH decapeptide antagonists possess N-alkylated aminoacyl residues where the side-chain portion of the residue is a 4-(substimtedamino)phenylalanyl, 4-(substituted-amino)cyclohexylalanyl, or .OMEGA.-(substitutedamino)alkyl group, and additionally the aminoacyl residues at position 5 are N-alkylated on the nitrogen atom of the peptide backbone.Type: GrantFiled: July 28, 1994Date of Patent: February 13, 1996Assignee: TAP Holding Inc.Inventors: Fortuna Haviv, Jonathan Greer, Rolf E. Swenson, Daryl R. Sauer
-
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
-
Patent number: 5488036Abstract: Certain toxic compounds (T) such as, for example, compounds based upon diphtheria toxin, ricin toxin, pseudomonas exotoxin, .alpha.-amanitin, pokeweed antiviral protein (PAP), ribosome inhibiting proteins, especially the ribosome inhibiting proteins of barley, wheat, corn, rye, gelonin and abrin, as well as certain cytotoxic chemicals such as, for example, melphalan and daunomycin can be conjugated to certain analogs of gonadotropin-releasing hormone to form a class of compounds which, when injected into an animal, destroy the gonadotrophs of the animal's anterior pituitary gland. Hence such compounds may be used to sterilize such animals and/or to treat certain sex hormone related diseases.Type: GrantFiled: July 20, 1993Date of Patent: January 30, 1996Assignee: Colorado State University Research FoundationInventors: Torrance M. Nett, Leonard M. Glode
-
Patent number: 5484592Abstract: A peptide suitable for a vaccine effective against Luteinizing Hormone Releasing Hormone (LHRH) is disclosed. The peptide has an LHRH tandem structure, i.e., a peptide comprising at least 2 LHRH sequences in tandem. The invention further provides vaccines and medicinal preparations including the composition and a method of immunizing a mammal against LHRH.Type: GrantFiled: November 8, 1993Date of Patent: January 16, 1996Assignee: Stitching Centraal Diergeneeskundig InstituutInventors: Robert H. Meloen, Cornelis J. G. Wensing
-
Patent number: 5480969Abstract: LHRH antagonists similar to antide and congeners with higher water solubility have been synthesized by substitutions in positions 1, 5 or 6 with hydrophilic residues. These peptides have antiovulatory activity with minimal histamine releasing effect.Type: GrantFiled: September 15, 1992Date of Patent: January 2, 1996Assignees: The Administrators of the Tulane Educational Fund, Board of Regents, The University of Texas SystemInventors: Cyril Y. Bowers, Karl A. Folkers, Anders Ljungqvist, Dong-Mei Feng, Anna Janceka