Luteinizing Hormone-releasing Hormone (lh-rh); Related Peptides Patents (Class 930/130)
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Patent number: 7605121Abstract: A novel lyophilizate and method of preparation as well as the use of the lyophilizate to treat female infertility and for gonad protection. Cetrorelix is dissolved in acetic acid 30% v/v, the solution is transferred to water and freeze dried.Type: GrantFiled: January 24, 2005Date of Patent: October 20, 2009Assignee: AEterna Zentaris GmbHInventors: Jürgen Engel, Burkhard Wichert, Dieter Sauerbier, Gudrun Sauerbier, legal representative, Thomas Reissmann
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Patent number: 7402558Abstract: The invention provides a protocol leading to improved embryo implantation rates and/or decreased miscarriage rates in which hCG or LH, or a bio-analogue thereof, is administered during the follicular phase.Type: GrantFiled: September 12, 2002Date of Patent: July 22, 2008Assignee: Laboratoires SeronosaInventor: Yves Menezo
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Patent number: 7381556Abstract: Modified proteins are disclosed that maintain enzymatic and insecticidal activity while displaying reduced or eliminated allergenicity. Epitopes which bind to anti-patatin antibodies were identified, and removed via site directed mutagenesis. Tyrosines were observed to generally contribute to the allergenic properties of patatin proteins. Removal of glycosylation sites was observed to reduce or eliminate antibody binding. Permuteins are also disclosed which have a rearranged amino acid sequence while retaining enzymatic activity. Deallergenized proteins and permuteins can be used as insecticidal materials, as nutritional supplements, and as immunotherapeutic agents.Type: GrantFiled: June 28, 2007Date of Patent: June 3, 2008Assignee: Monsanto Technology LLCInventors: Murtaza F. Alibhai, James D. Astwood, Charles A. McWherter, Hugh A. Sampson
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Patent number: 7238511Abstract: Modified proteins are disclosed that maintain enzymatic and insecticidal activity while displaying reduced or eliminated allergenicity. Epitopes which bind to anti-patatin antibodies were identified, and removed via site directed mutagenesis. Tyrosines were observed to generally contribute to the allergenic properties of patatin proteins. Removal of glycosylation sites was observed to reduce or eliminate antibody binding. Permuteins are also disclosed which have a rearranged amino acid sequence while retaining enzymatic activity. Deallergenized proteins and permuteins can be used as insecticidal materials, as nutritional supplements, and as immunotherapeutic agents.Type: GrantFiled: September 7, 2005Date of Patent: July 3, 2007Assignee: Monsanto Technology LLCInventors: Murtaza F. Alibhai, James D. Astwood, Charles A. McWherter, Hugh A. Sampson
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Patent number: 7071165Abstract: Novel LHRH antagonist peptides, pharmaceutical compositions thereof, and methods of use thereof, are disclosed. The LHRH antagonist comprise a peptide compound, wherein a residue of the peptide compound corresponding to the amino acid at position 6 of natural mammalian LHRH comprises a hydrophilic N-acyl moiety, a dipolar moiety, a sulfonium moiety, a receptor-modifying moiety or a small polar moiety.Type: GrantFiled: April 5, 2002Date of Patent: July 4, 2006Assignee: Indiana University Research and Technology CorporationInventor: Roger W. Roeske
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Patent number: 6977242Abstract: The present invention relates to two novel Gonadotropin releasing hormones muGnRH I and muGnRH II of amino acid SEQ ID 1 as QHWSAWRLPG, and SEQ ID 2 QHWSWGILPG respectively, useful for induced breeding in fish both in combination and alone, by activating production of Gonadotropin, and a method of isolating the same from Indian Murrel brain, and further, a method of inducing breeding in fishes using the said novel gonadotropin releasing hormones.Type: GrantFiled: January 28, 2003Date of Patent: December 20, 2005Assignee: Council of Scientific and Industrial ResearchInventors: Abhijit Chatterjee, Partha Ray, Subrata Dasgupta, Samir Hattacharya, Santosh Pasha
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Patent number: 6884423Abstract: The invention includes antibiotic pharmaceutical compositions comprising eukaryotic histone H1 protein and methods of using eukaryotic histone H1 protein to kill or to inhibit the growth of microorganisms, including, but not limited to, human pathogenic bacteria. The invention further includes a eukaryotic histone H1-containing animal feed and methods of improving growth of an animal by supplying the feed to the animal. The invention still further includes a kit comprising a eukaryotic histone H1-containing antibiotic pharmaceutical composition and an instructional material which describes the use of the composition. In addition, the invention includes a vaccine comprising a eukaryotic histone H1 protein and a method of vaccinating an animal using the vaccine.Type: GrantFiled: August 9, 2000Date of Patent: April 26, 2005Assignees: Symbiotec GmbH, Philadelphia Health and Education CorporationInventors: Reiner Class, Michael Zeppezauer
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Patent number: 6863891Abstract: A novel lyophilizate and method of preparation as well as the use of the lyophilizate to treat female infertility and for gonad protection. Cetrorelix is dissolved in acetic acid 30% v/v, the solution is transferred to water and freeze dried.Type: GrantFiled: January 9, 2002Date of Patent: March 8, 2005Assignee: Zentaris AGInventors: Jürgen Engel, Burkhard Wichert, Dieter Sauerbier, Thomas Reissmann
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Patent number: 6716817Abstract: A method of treating female infertility using a novel cetrorelix acetate lyophilizate is disclosed.Type: GrantFiled: January 20, 1999Date of Patent: April 6, 2004Assignee: Zentaris AGInventors: Jürgen Engel, Burkhard Wichert, Dieter Eauerbiar, Thomas Reissman
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Patent number: 6455499Abstract: Methods of treating a subject having a disorder associated with LHRH activity are disclosed.Type: GrantFiled: February 23, 1999Date of Patent: September 24, 2002Assignee: Indiana University FoundationInventor: Roger W. Roeske
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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: 6303123Abstract: 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: June 7, 1995Date of Patent: October 16, 2001Assignee: Aphton CorporationInventors: Stephen Grimes, Robert Scibienski
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Patent number: 6210927Abstract: 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: June 30, 1997Date of Patent: April 3, 2001Assignee: University of Maryland Biotechnology InstituteInventors: Yonathan Zohar, Yoav Gothilf
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Patent number: 6153587Abstract: LH-RH analogues with excellent affinity for LH-RH receptors, of the formula A.sub.1 -A.sub.2 -W-A.sub.3 -A.sub.4 -SPL-A.sub.5 -A.sub.6 -Pro-Z(I) in which:-A.sub.1 is pGlu, AcSar or an aromatic D-amino acid;-A.sub.2 is a direct bond, His, DPhe, DpFPhe or DpClPhe;*W is an aromatic L- or D-amino acid;-A.sub.3 is Ala, Thr, Ser, DSer, Ser(OBzl) or MeSer;-A.sub.4 is Tyr, Phe, cPzACAla, L- or D-PicLys, L- or D-NicLys or L- or D-IprLys;*SPL is the spirolactam of formula: ##STR1## -A.sub.5 is an amino acid with a (C.sub.1 -C.sub.8)alkyl or (C.sub.3-C.sub.6)cycloalkyl side chain;-A.sub.6 is L- or D-(Arg, HArg, Lys, HLys, Orn, Cit, HCit or Aph), where L- or D-(Arg and HArg) can be substituted by one or two (C.sub.1 -C.sub.4)alkyl groups and L- or D-(Lys, HLys, Orn and Aph) can be substituted by an isopropyl, nicotinoyl or picolinoyl group; and*Z is GlyNH.sub.2, DAlaNH.sub.2, AzaGlyNH.sub.2 or --NHR.sub.1 where R.sub.1 is a (C.sub.1 -C.sub.Type: GrantFiled: May 24, 1999Date of Patent: November 28, 2000Assignee: Laboratoire THERAMEXInventors: Remi Delansorne, Jacques Paris
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Patent number: 6132720Abstract: 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: November 17, 1997Date of Patent: October 17, 2000Assignee: Aphton Corp.Inventors: Stephen Grimes, Robert Scibienski
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Patent number: 6106805Abstract: The invention relates to a diagnostic composition for improving the effectiveness of hysteroscopy, characterized in that it contains an LH-RH antagonist, in particular cetrorelix. The composition is envisaged for use prior to hysteroscopy and/or for preparation for surgery, specifically in a single dose of between 0.1 and 2 mg/kg.However, the composition can also be administered, for use prior to hysteroscopy and/or for preparation for surgery, in a multiple dose of between 0.01 and 0.5 mg/kg, preferably spread over 1-14 days. The composition is furthermore suitable for use in hysteroscopy in combination with the subsequent treatment of pathological conditions of the uterus such as myoma and endometrial hyperplasia.Type: GrantFiled: October 30, 1997Date of Patent: August 22, 2000Assignee: Asta Medica AktiengesellschaftInventors: Jurgen Engel, Klaus Diedrich, Ricardo Felberbaum
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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
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Patent number: 5883073Abstract: The invention is directed to a glycosylated or nonglycosylated protein which is composed of the amino acid sequence of a first .alpha. subunit common to the glycoprotein hormones linked covalently, optionally through a linker moiety, to the amino acid sequence of a second .alpha. subunit of said hormones, wherein said first and second .alpha. subunits consist of the native amino acid sequences or variants of said amino acid sequences. These proteins are useful as agonists or antagonists of glycoprotein hormone activity.Type: GrantFiled: April 3, 1997Date of Patent: March 16, 1999Assignee: Washington UniversityInventors: Irving Boime, David Ben-Menahem
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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
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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.
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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
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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: 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
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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
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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: 5470947Abstract: 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 26, 1989Date of Patent: November 28, 1995Assignees: Board of Regents, The University of Texas System, The Administrators of the Tulane Educational FundInventors: Karl A. Folkers, Anders Ljungqvist, Dong-Mei Feng, Minoru Kubota, Pui-Fun L. Tang, Cyril Y. Bowers
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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: 5403586Abstract: This invention relates to the preparation of novel fusion proteins which comprise an analogue of LHRH and TraTp or an analogue of TraTp. The fusion proteins of the invention are useful as components of vaccines for the inhibition or control of reproductive functions in vertebrate hosts. The invention also relates to polynucleotide molecules encoding the fusion proteins, to transformant hosts expressing the fusion proteins and to methods of inhibiting or controlling reproductive function in vertebrate hosts using the fusion proteins or vaccines of the invention.Type: GrantFiled: June 25, 1991Date of Patent: April 4, 1995Assignee: Biotechnology Australia Ptl Ltd.Inventors: Gregory J. Russell-Jones, Andrew G. Stewart, Con G. Tsonis
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Patent number: 5389613Abstract: A novel method of treating prostate adenocarcinoma, prostate benign hypertrophia, endometriosis, dysmenorrhea, hirsuitism, hormono-dependant mammary tumors, treatment and prevention of precocious puberty, induction of a retardation of the appearance of puberty and treatment of acne of mammals comprising administering to warm-blooded animals an effective amount of a peptide of the formulaP Glu-His-Trp-Ser-Tyr-X-Y-Arg-Pro-Z (I)wherein (a) Z is Gly--NH.sub.2, Y is Leu and X is Gly, (b) Z is Gly--NH.sub.2, Y is Leu, X is DN Leu, DN Val, D Abu (.alpha.-aminobutyric acid), D Phe, D Ser, D Thr, D Met, D Pgl, D Lys, Leu, Ile, Nle, Val, N Val, Met, Phe, D Leu, D Arg, D Ser (tbu), D Thr (tbu), D Cys (tbu), D Asp (O tbu), D Glu (Otbu), D Orn (boc), D Lys (boc), D Trp, Trp, 2-methyl Ala, D Tyr, D Met .epsilon.-lauryl D Lys, .epsilon.Type: GrantFiled: February 18, 1993Date of Patent: February 14, 1995Assignees: Roussel Uclaf, Shering CorporationInventors: Fernand Labrie, Jean-Pierre Raynaud
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Patent number: 5171835Abstract: Disclosed herein are analogues of the luteinizing hormone-releasing hormone (LH-RH), which are potent antagonists of LH-RH. These peptides inhibit the release of gonadotropins from the pituitary in mammals, including humans and possess antitumor activity.Formula I represents peptides which are within the scope of this invention:X--R.sup.1 --R.sup.2 --R.sup.3 --Ser--R.sup.5 --R.sup.6 (AY.sub.2)--Leu--Arg--Pro--D--Ala--NH.sub.2 Iand the pharmaceutically acceptable salts thereof, whereinR.sup.1 is D-Phe, D-Phe(4Cl), D-Nal(1) or D-Nal(2),R.sup.2 is D-Phe or D-Phe(4HI),R.sup.3 is D-Trp, D-Phe, D-Phe(4HI), D-Nal(1), D-Nal(2) or D-Pal(3),R.sup.5 is Tyr or Arg,R.sup.6 is D-Lys or D-Orn,HI is fluoro, chloro or bromoX is a lower alkanoyl group of 2-5 carbon atoms,A is a diaminoacyl residue having the formula ##STR1## where m is 0 or 1,n is 0 or 1,Y is Y.sup.1 or Y.sup.2, whereinY.sup.Type: GrantFiled: January 30, 1991Date of Patent: December 15, 1992Assignee: The Administrators of the Tulane Educational FundInventors: Tamas Janaky, Atilla Juhasz, Andrew V. Schally