Somatostatin; Related Peptides Patents (Class 930/160)
  • Patent number: 7074761
    Abstract: 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: Grant
    Filed: December 7, 1998
    Date of Patent: July 11, 2006
    Assignee: Takeda Chemical Ind., Ltd.
    Inventors: Shuji Hinuma, Shoji Fukusumi, Chieko Kitada
  • Patent number: 6579967
    Abstract: Analogs of SRIF which are selective for SSTR3 in contrast to the other cloned SRIF receptors. These analogs are useful in determining the tissue and cellular expression of the receptor SSTR3 and its biological role in the endocrine, exocrine and nervous system, as well as in regulating tumor growth. SRIF analog peptides, such as des-AA1,2,4,5,12,13[N&bgr;MeD-Agl8(2-naphthoyl) ]-SRIF and counterparts incorporating D-Cys3 and/or Tyr7, inhibit the binding of a universal SRIF radioligand to the cloned human receptor SSTR3, but they do not bind with significant affinity to human SSTR1, SSTR2, SSTR4 or SSTR5. By incorporating an iodinated tyrosine in position-2 or in position-11 in these SSTR3-selective SRIF analogs, a labeled compound useful in drug-screening methods is provided. Because the N-terminus accommodates bulky moieties without loss of selectivity, a cytotoxin or a complexing agent to accept a radioactive nuclide may be present at the N-terminus.
    Type: Grant
    Filed: June 29, 2000
    Date of Patent: June 17, 2003
    Assignee: The Salk Institute for Biological Studies
    Inventors: Jean E. F. Rivier, Jean Claude Reubi
  • Patent number: 6521599
    Abstract: 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: Grant
    Filed: October 10, 2001
    Date of Patent: February 18, 2003
    Assignee: Lipotec, S.A.
    Inventors: Berta Ponsati Obiols, Gemma Jodas Farres, Francisco Javier Clemente Rodriguez, Sergi Pavon Fernandez, Jordi Bacardit Cabado
  • Patent number: 6123916
    Abstract: The invention relates to a new pharmaceutical use of somatostatin peptides comprising on the terminal amino group a polyamino polycarboxylic group, in free form or in a pharmaceutically acceptable salt form, particularly in the manufacture of a medicament for treating disorders with an aetiology comprising or associated with excess of GH-secretion.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: September 26, 2000
    Assignee: Novartis AG
    Inventors: Eric Paul Krenning, Steven Willem Jan Lamberts
  • Patent number: 6001960
    Abstract: Relatively small cyclic peptides that mimic the biological and/or chemical activity of larger cyclic peptide such as somatostatin, as well as synthetic methods therefor. In certain embodiments, cyclic peptides of the invention have structure: ##STR1## wherein R.sub.NP1 is H, an amine protecting group, or a solid support and R.sub.NP2 is H or an amine protecting group.
    Type: Grant
    Filed: December 23, 1997
    Date of Patent: December 14, 1999
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Ralph F. Hirschmann, Rolando A. Spanevello, Ruth F. Nutt
  • Patent number: 5965694
    Abstract: Relatively small cyclic peptides that mimic the biological and/or chemical activity of larger cyclic peptide such as somatostatin, as well as synthetic methods therefor. In certain embodiments, cyclic peptides of the invention have structure: ##STR1## wherein R.sub.NP1 is H, an amine protecting group, or a solid support and R.sub.NP2 is H or an amine protecting group.
    Type: Grant
    Filed: November 16, 1994
    Date of Patent: October 12, 1999
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Ralph F. Hirschmann, Rolando A. Spanevello
  • Patent number: 5833942
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: November 10, 1998
    Assignee: Diatide, Inc.
    Inventors: Richard T. Dean, John Lister-James
  • Patent number: 5820845
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: October 13, 1998
    Assignee: Diatide, Inc.
    Inventors: Richard T. Dean, John Lister-James
  • Patent number: 5753618
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: May 19, 1998
    Assignee: Novartis Corporation
    Inventors: Thomas Cavanak, Alan Harris
  • Patent number: 5708135
    Abstract: A cyclic peptide analog of somatostatin wherein a disulfide bond links the N-terminus residue and the C-terminus residue.
    Type: Grant
    Filed: December 26, 1995
    Date of Patent: January 13, 1998
    Assignees: Biomeasure Incorporated, The Administrators of the Tulane Educational Fund
    Inventors: David H. Coy, John E. Taylor
  • Patent number: 5700905
    Abstract: Relatively small cyclic peptides that mimic the biological and/or chemical activity of larger cyclic peptide such as somatostatin, as well as synthetic methods therefor. In certain embodiments, cyclic peptides of the invention have structure: ##STR1## wherein R.sub.NP1 is H, an amine protecting group, or a solid support and R.sub.NP2 is H or an amine protecting group.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: December 23, 1997
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Ralph F. Hirschmann, Rolando A. Spanevello, Ruth F. Nutt
  • Patent number: 5633263
    Abstract: Linear peptide analogs of somatostatin having the formula: ##STR1## As an example, D-Phe-Phe-Phe-D-Trp-Lys-Thr-Phe-Thr is covered by the above formula (i.e., R.sub.1 is H, R.sub.2 is H, A.sup.1 is D-Phe, A.sup.2 is Phe, A.sup.3 is Phe, A.sup.6 is Thr, A.sup.7 is Phe, A.sup.8 is Thr, and R.sub.3 is NH.sub.2).
    Type: Grant
    Filed: August 15, 1994
    Date of Patent: May 27, 1997
    Assignee: The Administrators of the Tulane Educational Fund
    Inventors: David H. Coy, William A. Murphy
  • Patent number: 5556939
    Abstract: Technetium or rhenium radionuclide labelled chelate-hexapeptide complexes are useful for the selective detection or treatment of tumors with somatostatin receptors. In particular, compounds of formula: ##STR1## (wherein R, R.sup.1, R.sup.3 and A are as defined herein) incorporating an N3S2 chelate may be labelled with a radionuclide. The resulting complexes are useful as radioimaging agents or as radiopharmaceuticals for the treatment of certain tumors.
    Type: Grant
    Filed: October 13, 1994
    Date of Patent: September 17, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Richard J. Flanagan, Jean-Marc Dufour, Keith T. Hogan
  • Patent number: 5506339
    Abstract: A compound 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;each X.sub.1 and X.sub.2, independently, is H, F, Cl, Br, OH, CH.sub.3, or CF.sub.3, provided that at least one of X.sub.1 and X.sub.2 must be H;A.sub.3 is Phe or Tyr; andA.sub.4 is OH, NH.sub.2, or NH-R.sub.3 (wherein R.sub.3 is a saturated aliphatic C.sub.1-8 alkyl);or a pharmaceutically acceptable salt thereof. A therapeutic composition containing the compound of the present invention and a method of using the same are also described.
    Type: Grant
    Filed: February 21, 1992
    Date of Patent: April 9, 1996
    Assignee: The Administrators of the Tulane Educational Fund
    Inventors: David H. Coy, William A. Murphy
  • Patent number: 5439688
    Abstract: 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: Grant
    Filed: November 12, 1991
    Date of Patent: August 8, 1995
    Assignee: Debio Recherche Pharmaceutique S.A.
    Inventors: Piero Orsolini, Frederic Heimgartner