Somatostatin Or Derivatives Patents (Class 514/806)
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Patent number: 9937264Abstract: [Problem] To provide a glycosylated polypeptide having an affinity to somatostatin receptors, and, compared to somatostatins, having improved in-blood stability. [Solution] The glycosylated polypeptide is characterized by at least one amino acid in a somatostatin or an analog thereof being replaced with a glycosylated amino acid.Type: GrantFiled: July 8, 2016Date of Patent: April 10, 2018Assignee: GLYTECH, INC.Inventors: Hirofumi Ochiai, Taiji Shimoda, Kazuhiro Fukae, Masatoshi Maeda, Kazuyuki Ishii, Kenta Yoshida, Katsunari Tezuka, Keisuke Tazuru
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Patent number: 8435942Abstract: A method of formulating insulin compositions comprises preparing a carrier having a phosphatidylcholine component which entraps insulin, stabilizing insulin compositions at room temperatures.Type: GrantFiled: December 31, 2003Date of Patent: May 7, 2013Assignee: Transdermal Biotechnology, Inc.Inventors: Nicholas V. Perricone, Chim Potini
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Patent number: 8273711Abstract: The present invention relates to compositions and methods for transdermal drug delivery comprising formulating a phosphatidylcholine carrier composition containing the drug and applying the composition to the skin.Type: GrantFiled: February 10, 2011Date of Patent: September 25, 2012Assignee: Transdermal Biotechnology, Inc.Inventor: Nicholas V. Perricone
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Patent number: 7408024Abstract: The present invention is directed to a somatostatin antagonist according to formula (I): A1-cyclo {D-Cys-A2-D-Trp-A3-A4-Cys}-A5Y1, wherein A1 is an optionally substituted aromatic a-amino acid; A2 is an optionally substituted aromatic ?-amino acid; A3 is Dab, Dap, Lys or Om; A4 is ?-Hydroxyvaline, Ser, Hser, or Thr; A5 is an optionally substituted D- or L-aromatic amino acid; and Y1 is OH, NH2 or NHR1? where RI is (C1-6)alkyl; wherein each said optionally substituted aromatic amino acid is optionally substituted with one or more substituents each independently selected from the group consisting of halogen, NO2, OH, CN, (C1-6) alkyl, (C2-6) alkenyl, (C2-6) alkynyl, (C1-6)alkoxy, Bzl, O-Bzl, and NR9R10? wherein R9 ad R10 each is independently H, O, or (C1-6) alkyl; and wherein the amine nitrogen of each of amide peptide bond and the amino group of A1 of formula (I) is optionally substituted with a methyl group, provided that there is at least one said methyl group; or a pharmaceutically acceptable salt thereof,Type: GrantFiled: August 20, 2007Date of Patent: August 5, 2008Assignee: The Administrators of the Tulane Educational FundInventors: David H. Coy, William A. Murphy, Walajapet G. Rajeswaran
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Patent number: 7182956Abstract: A stable composition of a drug comprising a carrier having a phosphatidylcholine component which entraps the drug is applied to the skin for transdermal delivery of the drug.Type: GrantFiled: December 31, 2003Date of Patent: February 27, 2007Inventors: Nicholas V. Perricone, Chim Potini
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Patent number: 7109166Abstract: This invention is directed to a sustained release composition comprised of Compound (A) having the formula or a pharmaceutically acceptable salt thereof, and a copolymer comprised of poly-(I)-lactic-glycolic-tartaric acid wherein the amino group of Compound (A) is ionically bound to a carboxyl group of the copolymer and wherein further the composition may be made into a sustained release pharmaceutical composition with pharmaceutically acceptable carrier(s).Type: GrantFiled: August 16, 2000Date of Patent: September 19, 2006Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques, SASInventor: Jacques-Pierre Moreau
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Patent number: 7074761Abstract: The peptides and precursors thereof, inclusive salts thereof, of the present invention are useful as a pharmaceutical composition, for example as therapeutic or prophylactic agents for hormone-producing tumors, acromegaly, gigantism, dementia, gastric ulcer and the like, hormone secretion inhibitors, tumor growth inhibitors, neural activity or sleep modulators, etc. The DNAs coding for the peptides or precursors of the invention are useful as a pharmaceutical composition, for example as agents for the gene therapy or prevention of hormone-producing tumors, acromegaly, gigantism, dementia, gastric ulcer and the like, hormone secretion inhibitors, tumor growth inhibitors, neural activity or sleep modulators, etc. Furthermore, the DNAs coding for the peptides or precursors of the invention are useful as agents for the gene diagnosis of various diseases, for example, hormone-producing tumors, acromegaly, gigantism, dementia, gastric ulcer, etc.Type: GrantFiled: December 7, 1998Date of Patent: July 11, 2006Assignee: Takeda Chemical Ind., Ltd.Inventors: Shuji Hinuma, Shoji Fukusumi, Chieko Kitada
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Patent number: 6914046Abstract: Compounds inhibiting the activation of the nuclear factor ?B (NF-?B) are used for the preparation of medications adapted for the treatment of malignant hemopathies and solid tumors, and for the prevention of the appearance or the treatment, of phenomena of resistance to cytotoxic molecules used in the scope of treatment of the above pathologies, appearing in patients treated with these molecules when the latter are adapted to activate NF-?B.Type: GrantFiled: November 24, 1999Date of Patent: July 5, 2005Assignee: Centre National de la Recherche ScientifiqueInventors: Francois Hirsch, Astrid Haeffner
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Patent number: 6867181Abstract: A method of spherifying a sustained release ionic conjugate which contains a free carboxyl group-containing polymer and a free amino group-containing drug which are ionically bonded to each other.Type: GrantFiled: January 26, 2000Date of Patent: March 15, 2005Assignees: Societe de Conseils de Recherches et d'Applications Scientifiques, S.A.S., Poly-Med, IncorporatedInventors: Shalaby Wahba Shalaby, Steven A. Jackson, Jacques-Pierre Moreau
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Patent number: 6630123Abstract: Administration of a radioisotopic compound by infusion over a period of time greater than two hours, preferably greater than twelve hours, greatly increases the maximum radioactivity that accumulates in the target cell. The efficacy of the administration of the radiolabeled compound can be increased about five times higher than prior bolus injection or short infusion methods. This method enhances the tumor to background ratio by increasing the actual radioligand accumulated inside the target cells. This technique works for any radiolabeled compound whose cellular uptake is limitedly a cellular process of either binding to a cellular receptor or to a transport protein. Once the radiolabeled compound is bound and internalized, the ability of an unlabeled compound to compete with the radioligand is markedly decreased. The primary factor governing residence time after internalization is the physical half-life of the radioisotope, not biologic half-life.Type: GrantFiled: September 18, 2000Date of Patent: October 7, 2003Assignee: Board of Supervisors of Louisiana State University and Agricultural and Mechanical CollegeInventors: Eugene A. Woltering, Gregory D. Espenan
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Patent number: 6521599Abstract: A stable pharmaceutical formulation for intravenous or intramuscular administration of Octreotide, which is characterized in that the vehicle for injection of the peptide or pharmaceutically acceptable salts thereof contains glycine in concentrations ranging from 10 to 60 mM and aqueous solution of hydrochloric acid in sufficient quantity to adjust the pH of the formulation to values between 3.0 and 4.2.Type: GrantFiled: October 10, 2001Date of Patent: February 18, 2003Assignee: Lipotec, S.A.Inventors: Berta Ponsati Obiols, Gemma Jodas Farres, Francisco Javier Clemente Rodriguez, Sergi Pavon Fernandez, Jordi Bacardit Cabado
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Patent number: 6319512Abstract: The present intention relates to an implant for the controlled release of at least one pharmaceutically active principle comprising a core containing at least one active principle and a sheath surrounding said core, wherein said sheath is composed of at least one polymeric film applied around said core. It also relates to a process for the preparation of such an implant, characterised by the production of a core containing at least one active principle, preparation of at least one polymeric film, application of the polymeric film(s) around said core by juxtaposition and/or superposition thereof, and sterilisation of the implant thus obtained.Type: GrantFiled: February 23, 2000Date of Patent: November 20, 2001Assignee: Debio Recherche Pharmaceutique SAInventors: Alexandra Rothen-Weinhold, Robert Gurny, Piero Orsolini, Frédéric Heimgartner
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Patent number: 6307013Abstract: Protein suspensions comprising soluble and insoluble components are purified via flocculation with anionic polymers, such as polyacrylamides, potato starch, or modified cellulose. The procedure improves the efficiency of solid/liquid separations and can minimize or eliminate the requirement for centrifugation and/or filtration in large scale biotechnological processes. The method is particularly well suited for the purification and clarification of protein suspensions containing soluble somatotropin monomer using polyacrylamide and polysaccharide flocculants.Type: GrantFiled: July 16, 1999Date of Patent: October 23, 2001Assignee: Monsanto Technology LLCInventor: Mark L. Chivers
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Patent number: 6221958Abstract: Disclosed is a sustained release pharmaceutical composition. The composition includes a polyester containing a free COOH group ionically conjugated with a bioactive polypeptide comprising at least one effective ionogenic amine, wherein at least 50% by weight of the polypeptide present in the composition is ionically conjugated to the polyester.Type: GrantFiled: January 26, 1999Date of Patent: April 24, 2001Assignees: Societe de Conseils de Recherches et d'Applications Scientifiques, SAS, Poly-Med IncorporatedInventors: Shalaby Wahba Shalaby, Steven A. Jackson, Jacques-Pierre Moreau
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Patent number: 6171856Abstract: The present invention relates to methods and compositions for the treatment of diabetes involving free radicals. In particular, the present invention is directed to the treatment or prophylactic intervention of diabetes. The present invention demonstrates that MnSOD can play a protective role against cytokine killing, and provides strategies for engineering cell lines as islet surrogates for transplantation therapy of diabetes mellitus. Further, the present invention shows that &bgr;-cell destruction and dysfunction in adipogenic diabetes is mediated via fatty acids. Methods and compositions for ameliorating this disorder are provided herein.Type: GrantFiled: July 30, 1998Date of Patent: January 9, 2001Assignees: Board of Regents, The University of Texas System, Betagene, IncInventors: Anice Thigpen, Hans-Ewald Hohmeier, Christopher B. Newgard, Roger H. Unger, Michio Shimabukuro, Guoxun Chen, Christopher J. Rhodes, Sigrun R. H{umlaut over (u)}gl, Sharon Cousin
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Patent number: 6087337Abstract: A method of treating a mammal suffering from benign or malignant proliferative skin disease, e.g., melanoma or malignant skin metastases of melanoma, by topically administering to the mammal at the site of said diseased skin an effective amount of a somatostatin analog containing six or more amino acids.Type: GrantFiled: July 9, 1993Date of Patent: July 11, 2000Assignee: Biomeasure Inc.Inventors: Arthur E. Bogden, Jacques-Pierre Moreau
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Patent number: 6034175Abstract: This invention relates to novel salts composed of a cation derived from a peptide containing at least one basic group and an anion derived from a carboxy-terminated polyester, processes for the manufacture of such salts, and the use of such salts in the manufacture of extended release pharmaceutical compositions. The salts of the invention possess a variety of properties which are useful in the formulation of extended release pharmaceutical compositions, whether the salts are in pure form or are in admixture with either an excess of the peptide in its free, unbound form or an excess of the free polyester.Type: GrantFiled: January 22, 1999Date of Patent: March 7, 2000Assignee: Zeneca LimitedInventor: Francis Gowland Hutchinson
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Patent number: 5976569Abstract: Compositions useful in the delivery of active agents are provided. These delivery compositions include (a) an active agent; and either (b)(1) a carrier of (i) at least one amino acid and (ii) at least one diketopiperazine or (b)(2) at least one mono-N-substituted, di-N-substituted, or unsubstituted diketopiperazine. Methods for preparing these compositions and administering these compositions are also provided.Type: GrantFiled: April 29, 1997Date of Patent: November 2, 1999Assignee: Emisphere Technologies, Inc.Inventor: Sam J. Milstein
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Patent number: 5889110Abstract: This invention relates to novel salts composed of a cation derived from a peptide containing at least one basic group and an anion derived from a carboxy-terminated polyester, processes for the manufacture of such salts, and the use of such salts in the manufacture of extended release pharmaceutical compositions. The salts of the invention possess a variety of properties which are useful in the formulation of extended release pharmaceutical compositions, whether the salts are in pure form or are in admixture with either an excess of the peptide in its free, unbound form or an excess of the free polyester.Type: GrantFiled: June 7, 1995Date of Patent: March 30, 1999Assignee: Zeneca LimitedInventor: Francis Gowland Hutchinson
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Patent number: 5871711Abstract: This invention relates to therapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic agents. Specifically, the invention relates to peptide derivatives and analogs of somatostatin, and embodiments of such peptides labeled with technetium-99m (Tc-99m), as well as methods and kits for making, radiolabeling and using such peptides to image sites in a mammalian body. The invention also relates to peptide derivatives and analogues of somatostatin labeled with rhenium-186 (.sup.186 Re) and rhenium-188 (.sup.188 Re), and methods and kits for making, radiolabeling and using such peptides therapeutically in a mammalian body.Type: GrantFiled: January 13, 1995Date of Patent: February 16, 1999Assignee: Diatide, Inc.Inventors: Richard T. Dean, John Lister-James
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Patent number: 5863985Abstract: Disclosed is a sustained release pharmaceutical composition. The composition includes a polyester containing a free COOH group ionically conjugated with a bioactive polypeptide comprising at least one effective ionogenic amine, wherein at least 50% by weight of the polypeptide present in the composition is ionically conjugated to the polyester.Type: GrantFiled: June 2, 1997Date of Patent: January 26, 1999Assignee: Kinerton LimitedInventors: Shalaby W. Shalaby, Steven A. Jackson, Jacques-Pierre Moreau
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Patent number: 5843401Abstract: This invention relates to therapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic agents. Specifically, the invention relates to peptide derivatives and analogs of somatostatin, and embodiments of such peptides labeled with technetium-99m (Tc-99m), as well as methods and kits for making, radiolabeling and using such peptides to image sites in a mammalian body. The invention also relates to peptide derivatives and analogues of somatostatin labeled with rhemium-186 (.sup.186 Re) and rhenium-188 (.sup.188 Re), and methods and kits for making, radiolabeling and using such peptides therapeutically in a mammalian body.Type: GrantFiled: June 6, 1995Date of Patent: December 1, 1998Assignee: Diatide, Inc.Inventors: Richard T. Dean, John Lister-James
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Patent number: 5833942Abstract: This invention relates to therapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic agents. Specifically, the invention relates to peptide derivatives and analogs of somatostatin, and embodiments of such peptides labeled with technetium-99m (Tc-99m), as well as methods and kits for making, radiolabeling and using such peptides to image sites in a mammalian body. The invention also relates to peptide derivatives and analogues of somatostatin labeled with rhemium-186 (.sup.186 Re) and rhenium-188 (.sup.188 Re), and methods and kits for making, radiolabeling and using such peptides therapeutically in a mammalian body.Type: GrantFiled: June 6, 1995Date of Patent: November 10, 1998Assignee: Diatide, Inc.Inventors: Richard T. Dean, John Lister-James
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Patent number: 5820845Abstract: This invention relates to therapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic agents. Specifically, the invention relates to peptide derivatives and analogs of somatostatin, and embodiments of such peptides labeled with technetium-99m (Tc-99m), as well as methods and kits for making, radiolabeling and using such peptides to image sites in a mammalian body. The invention also relates to peptide derivatives and analogues of somatostatin labeled with rhemium-186 (.sup.186 Re) and rhenium-188 (.sup.188 Re), and methods and kits for making, radiolabeling and using such peptides therapeutically in a mammalian body.Type: GrantFiled: June 6, 1995Date of Patent: October 13, 1998Assignee: Diatide, Inc.Inventors: Richard T. Dean, John Lister-James
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Patent number: 5817624Abstract: The present invention is directed to a pharmaceutical formulation of a therapeutic polypeptide together with a permeation-enhancing mixture of sodium 3-nitrobenzoate and an oil to provide enhanced absorption of the polypeptide through the wall of the gastrointestinal tract, and particularly of the colon, after oral administration.Type: GrantFiled: June 5, 1995Date of Patent: October 6, 1998Assignee: Alza CorporationInventors: Heechung Yang, Robert E. Myrback, Deborah A. Fox, Vu Anh Nguyen
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Patent number: 5753618Abstract: The invention provides a pharmaceutical composition containing a somatostatin analogue, and its use in the treatment of breast cancer. The pharmaceutical composition preferably contains lactic acid in addition to the somatostatin analogue and is better tolerated when administered by injection.Type: GrantFiled: June 6, 1995Date of Patent: May 19, 1998Assignee: Novartis CorporationInventors: Thomas Cavanak, Alan Harris
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Patent number: 5693338Abstract: Compositions useful in the delivery of active agents are provided. These delivery compositions include (a) an active agent; and either (b)(1) a carrier of (i) at least one amino acid and (ii) at least one diketopiperazine or (b)(2) at least one mono-N-substituted, di-N-substituted, or unsubstituted diketopiperazine. Methods for preparing these compositions and administering these compositions are also provided.Type: GrantFiled: September 29, 1994Date of Patent: December 2, 1997Assignee: Emisphere Technologies, Inc.Inventor: Sam J. Milstein
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Patent number: 5672659Abstract: A composition including a polyester containing one or more free COOH groups ionically conjugated with a bioactive polypeptide comprising at least one effective ionogenic amine, wherein the polyester contains a member selected from the group of L-lactic acid, D-lactic acid, DL-lactic acid, .epsilon.-caprolactone, p-dioxanone, .epsilon.-caprolic acid, alkylene oxalate, cycloalkylene oxalate, alkylene succinate, .beta.-hydroxybutyrate, substituted or unsubstituted trimethylene carbonate, 1,5-dioxopan-2-one, 1,4-dioxepan-2-one, glycolide, glycolic acid, L-lactide, D-lactide, DL-lactide, meso-lactide, and any optically active isomers, racemates or copolymers thereof, and at least 50%, by weight, of the polypeptide present in the composition is ionically conjugated to said polyester.Type: GrantFiled: June 29, 1995Date of Patent: September 30, 1997Assignee: Kinerton LimitedInventors: Shalaby W. Shalaby, Steven A. Jackson, Jacques-Pierre Moreau
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Patent number: 5500224Abstract: A pharmaceutical composition in the form of a colloidal suspension of nanocapsules, comprising an oily phase consisting essentially of an oil containing dissolved therein a surfactant and suspended therein a plurality of nanocapsules having a diameter of less than 500 nanometers, said nanocapsules encapsulating an aqueous phase consisting essentially of a solution or a suspension of a therapeutically active substance, a surfactant and optionally ethanol; a process for preparing the said composition is also described. The walls of said nanocapsules are formed from a poly(alkyl 2-cyanoacrylate) wherein the alkyl radical has 1 to 6 carbon atoms. This composition is particularly suitable for oral administration of polypeptides and polysaccharides.Type: GrantFiled: January 10, 1994Date of Patent: March 19, 1996Assignee: U C B S.A.Inventors: Henri Vranckx, Martine Demoustier, Michel Deleers
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Patent number: 5468726Abstract: The administration of Somatostatin and growth hormone releasing factor at useful dosage levels alleviates the symptoms of various neuropsychiatric disorders.Growth hormone and neuropsychiatric responses to the administration of growth hormone releasing factor to mammals indicate its usefulness as an antemortem marker for senile dementia of the Alzheimer's type.Type: GrantFiled: February 23, 1990Date of Patent: November 21, 1995Assignee: Ares Holding 89 N.V.Inventor: Ramon Cacabelos
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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: 5389664Abstract: Alleviation of stomach ulcers in swine which are being administered exogenous somatotropin, by administering to the swine a benzimidazole compound selected from heterocyclylalkyl(sulfinyl or thio)benzimidazoles and [benzimidazolyl(sulfinyl or thio)alkyl]anilines.Type: GrantFiled: April 5, 1994Date of Patent: February 14, 1995Assignee: Monsanto CompanyInventors: Clifton A. Baile, Frances C. Buonomo, Carol L. McLaughlin, Billy D. Vineyard
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Patent number: 5244882Abstract: An analog of porcine growth hormone, is disclosed which retains the diabetogenic, insulin-sparing and lipolytic properties of porcine growth hormone while being capable of improving growth in mammals.Type: GrantFiled: July 28, 1992Date of Patent: September 14, 1993Assignees: Amgen, Inc., SmithKline Beecham CorporationInventor: Lawrence M. Souza
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Patent number: 5225205Abstract: A method for preparing a pharmaceutical composition in the form of microparticles, the composition thus obtained and its use for preparing injectable suspensions.Type: GrantFiled: February 18, 1992Date of Patent: July 6, 1993Assignee: Debiopharm S.A.Inventor: Piero Orsolini
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Patent number: 5015626Abstract: Muscle quality of pigs normally susceptible to porcine stress syndrome is improved by administering to the pigs in conjunction with their daily feed ration, a small amount of porcine somatotropin.Type: GrantFiled: August 2, 1989Date of Patent: May 14, 1991Assignee: Iowa State University Research Foundation, Inc.Inventors: Lauren L. Christian, Lindy F. Miller
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Patent number: 5008244Abstract: Somatotropin is administered to food producing animals in the finishing stage of growth to increase fertility by increasing embryonic survival and litter size during the reproductive stage of growth.Type: GrantFiled: May 15, 1989Date of Patent: April 16, 1991Assignee: Pitman-Moore, Inc.Inventors: Lindy F. Miller, Peter J. Thomford
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Patent number: 4966889Abstract: The treatment of certain inflammatory articular diseases, e.g., rheumatoid arthritis, is carried out via the use of injectable compositions containing somatostatin.Type: GrantFiled: November 3, 1987Date of Patent: October 30, 1990Assignee: Industria Farmaceutica Serono SpAInventors: Marco M. Cerinic, Simone Marabini
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Patent number: 4904642Abstract: An octapeptide of the formula: ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl), or R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H; A.sub.3 is CH.sub.2 -A.sub.6 (where A.sub.6 is pentafluorophenyl, naphthyl, pyridyl, or phenyl); A.sub.4 is o- m- or p-substituted X-Phe (where X is a halogen, H, NO.sub.2, OH, NH.sub.2, or C.sub.1-3 alkyl), pentafluoro-Phe, or .beta.-Nal; A.sub.5 is Thr, Ser, Phe, Val, .alpha.-aminobutyric acid, or Ile, provided that when A.sub.3 is phenyl, A.sub.1 is H, and A.sub.2 is H, A.sub.5 cannot be Val; and A.sub.7 is Thr, Trp, or .beta.-Nal; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 17, 1989Date of Patent: February 27, 1990Assignee: The Administrators of the Tulane Educational FundInventors: David H. Coy, William A. Murphy, Mark L. Heiman
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Patent number: 4857505Abstract: The invention relates to compositions comprising adducts of activated polysaccharides with biologically active growth hormones, somatomedins, growth factors and biologically active fragments. The invention also relates to a method for increasing and maintaining increased levels of these biologically active molecules in the blood of treated animals for extended periods of time, increasing weight gains in animals, and increasing milk production of lactating animals by the administration of a composition of the invention.Type: GrantFiled: March 9, 1987Date of Patent: August 15, 1989Assignee: American Cyanamid CompanyInventor: Volker D. Arendt
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Patent number: 4853371Abstract: An octapeptide of the formula: ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl, R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H; A.sub.3 is CH.sub.2 -A.sub.6 (where A.sub.6 is pentafluorophenyl, naphthyl, pyridyl, or phenyl); A.sub.4 is o- m- or p-substituted X-Phe (where X is a halogen, H, NO.sub.2, OH, NH.sub.2, or C.sub.1-3 alkyl), pentafluoro-Phe, or .alpha.-Nal; A.sub.5 is Thr, Ser, Phe, Val, .alpha.-aminobutyric acid, or Ile, provided that when A.sub.3 is phenyl, A.sub.1 is H, and A.sub.2 is H, A.sub.5 cannot be Val; and A.sub.7 is Thr, Trp, or .beta.-Nal; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 22, 1988Date of Patent: August 1, 1989Assignee: The Administrators of the Tulane Educational FundInventors: David H. Coy, William A. Murphy, Mark L. Heiman
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Patent number: 4816438Abstract: Anglerfish somatostatin-28 has the formula: ##STR1## Anglerfish somatostation-28 is insulin-selective when administered in vivo and is useful for the treatment of insulinoma. The 14-residue C-terminal peptide may also be used.Type: GrantFiled: April 1, 1987Date of Patent: March 28, 1989Assignee: The Salk Institute for Biological StudiesInventors: Joachim Spiess, Bryan D. Noe
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Patent number: 4798821Abstract: Process and compositions for lowering blood pressure in diabetic by employing a cyclopeptide compound is described.Type: GrantFiled: March 2, 1987Date of Patent: January 17, 1989Assignee: Merck & Co., Inc.Inventor: John F. Hartmann
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Patent number: 4748153Abstract: Compounds having somatostatin-like activity have been found to be useful as local anti-inflammatory agents in the treatment of such conditions as, for example, psoriasis, eczema, seborrhea, and other localized inflammatory and allergic conditions. Particularly useful are cyclic and bridged somatostatin analogs.Type: GrantFiled: September 2, 1987Date of Patent: May 31, 1988Assignee: Merck & Co., Inc.Inventors: Evan R. Morgan, Daniel F. Veber, Sanford L. Steelman
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Patent number: 4728638Abstract: Somatostatine derivatives of the general formula ##STR1## wherein either (a)A is ##STR2## W is -CO-N(A.sub.4) or -N(A.sub.5)-CO- and Y.sub.1 and Y.sub.2 are H or together a bondor (b)A is H, alkyl, phenylalkyl or RCO andY.sub.1 and Y.sub.2 are acyl groups as defined in claim 1,A', B, C, D, E, F, A.sub.1, A.sub.2, A.sub.3, A.sub.4, A.sub.5, R and Z having the meanings recited in claim 1, have pharmacological, in particular GH-, gastric- and pancreatic secretion inhibiting activity.Type: GrantFiled: January 7, 1986Date of Patent: March 1, 1988Assignee: Sandoz Ltd.Inventors: Wilfried Bauer, Janos Pless, Rene Huguenin
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Patent number: 4703034Abstract: There is disclosed a series of novel cyclic tetrapeptides related to somatostatin. The compounds have surprisingly been found to have the activity of increasing blood glucose when administered. The compounds are prepared using the solid phase or mixed anhydride synthesis methods and compositions and methods utilizing the novel compounds are also disclosed.Type: GrantFiled: April 28, 1986Date of Patent: October 27, 1987Assignee: Merck & Co., Inc.Inventors: Roger Freidinger, Ruth F. Nutt, Terry A. Lyle, Richard Saperstein
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Patent number: 4670419Abstract: A pharmaceutical composition containing a hydrophilic drug which is poorly absorbable through the gastrointestinal tract, and cyclodextrin, increases the absorbability of the drug into the mammalian body when administered by a non-oral or non-injection route.Type: GrantFiled: July 8, 1985Date of Patent: June 2, 1987Assignee: Takeda Chemical Industries, Ltd.Inventors: Yoshiaki Uda, Shin-ichiro Hirai, Takatsuka Yashiki
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Patent number: 4670418Abstract: Somatostatin in the form of a peridural, intraspinal or intraventricular injection and/or infusion can be used as an analgesic or anesthetic.Type: GrantFiled: March 8, 1985Date of Patent: June 2, 1987Assignee: CuraMED Pharma GmbHInventors: Joachim Chrubasik, Sigrun Chrubasik
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Patent number: 4663435Abstract: Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a bridged grouping which replaces eight of the ring amino acids of somatostatin. The bridged cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of selectively inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These bridged cyclic hexapeptides are prepared by the solid phase method.Type: GrantFiled: June 24, 1985Date of Patent: May 5, 1987Assignee: Merck & Co., Inc.Inventor: Stephen F. Brady
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Patent number: 4621073Abstract: The invention relates to cyclic hexapeptides of the general formula III ##STR1## in which X represents the radical of an L-aminoacid of the general formula IIIa ##STR2## in which A and B are identical or different and denote alkyl having 1 to 3 carbon atoms, or A and B together represent a saturated, unsaturated or aromatic monocyclic or bicyclic structure having 3 to 6 carbon atoms, n denotes 0 or 1, and Y represents an aliphatic or aromatic L-aminoacid the side chain of which can be hydroxylated, and their salts with physiologically tolerated acids, and to a process for their preparation and their use and their intermediates.Type: GrantFiled: January 31, 1984Date of Patent: November 4, 1986Assignee: Hoechst AktiengesellschaftInventors: Axel Friedrich, Wolfgang Konig, Volker Teetz, Rolf Geiger, Jurgen K. Sandow
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Patent number: 4612302Abstract: A method of increasing the clearance of particles from the blood stream of a vertebrate, which comprises administering to a vertebrate having a surplus of particles in the blood stream of the vertebrate an amount of a somatostatin analogue sufficient to increase phagocytosis in the vertebrate is disclosed along with a method treating vascular lesions or deterioration of biological membranes comprising the step of administering to a human or other mammal suspected of having one or more vascular lesions or of having deterioration of a biological membrane in the liver of said human or mammal an amount of a somatostatin analogue sufficient to reduce the number or severity of said lesions or to prevent further deterioration or reduce the extent of deterioration of said membrane.Type: GrantFiled: November 14, 1983Date of Patent: September 16, 1986Assignee: Brigham and Women's HospitalInventors: Sandor Szabo, Klaus W. Usadel, Horst Kessler