Abstract: A regenerated collagen fiber is subjected to water-insolubilizing treatment with a monofunctional epoxy compound to produce a water-insolubilized regenerated collagen fiber which can substantially maintain the color and the high knot tenacity, inherent in the collagen. Where the monofunctional epoxy compound is an epihalohydrin, a regenerated collagen fiber can be treated with this epihalohydrin and a sulfur compound to produce a water-insolubilized regenerated collagen fiber which can be permanent-wave set. In addition, the water-insolubilized regenerated collagen fiber can be converted into a fiber which can be permanent-wave set, by introducing a disulfide linkage into carboxylic groups of the collagen, which remain unmodified by the insolubilizing treatment.

Abstract: Somatostain analogues comprising the amino acid sequence of the formula (I): -(D/L)Trp-Lys-X1-X2, wherein X1 is a substituted Thr, Ser, Tyr, Glu or Cys residue and X2 is an &agr;-amino acid having an aromatic residue on the C&agr; side chain, or an amino acid unit selected from Dab, Dpr, Dpm, His (Bzl)HyPro, thienyl-Ala, cyclohexyl-Ala and t.-butyl-Ala, the residue Lys of said sequence corresponding to the residue Lys9 of the native somatostatin-14, in free form, in salt form or complexed with a detectable element have interesting pharmacological properties.

Abstract: This invention relates to therapeutic reagents and peptides, including radiotherapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic agents. Specifically, the invention relates to cyclic peptide derivatives and analogs of somatostatin, and embodiments of such peptides radiolabeled with a radioisotope, as well as methods and kits for making, radiolabeling and using such peptides for radiodiagnostic and radiotherapeutic purposes. The invention specifically relates to cyclic peptide derivatives and analogues of somatostatin radiolabeled with technetium-99m and uses thereof as scintigraphic imaging agents. The invention also specifically relates to cyclic peptide derivatives and analogues of somatostatin radiolabeled with cytotoxic radioisotopes such as rhenium-186 (186Re) and rhenium-188 (188Re) for use as radiotherapeutic agents.

Abstract: Methods for increasing the growth rate of a human patient having partial growth hormone insensitivity syndrome, but not Laron syndrome, are described. One such method comprises administering an effective dose of growth hormone, preferably growth hormone with a native human sequence, with or without an N-terminal methionine, to the patient. The patient is characterized as having a height of less than about −2 standard deviations below normal for age and sex, a serum level of high-affinity growth hormone binding protein that is at least 2 standard deviations below normal levels, a serum level of IGF-I that is below normal mean levels, and a serum level of growth hormone that is at least normal. In another such method, the same patient population is treated with an effective amount of IGF-I, given alone or in combination with an amount of growth hormone that is effective in combination with the IGF-I.

Abstract: A cyclodextrin derivative, wherein at least 60 percent of the free hydroxy groups of said cyclodextrin are acylated with acyl groups where at least one of said acyl groups comprise a free carboxylic group.

Abstract: The present invention relates to a long-acting galenical formulation of GRF peptides, GRF and/or analogs thereof which comprises about 1 to about 100 mg of a GRF peptide, fragment or analog thereof pressed from about 1 to about 100 kg/mm2 in a tablet for parenteral administration, whereby these GRF peptides are released as the tablet is eroded.

Abstract: Compounds of formula I wherein M is a cation equivalent and A is Phe or Tyr, in free form or in salt form are useful as radiopharmaceuticals when complexed with a radionuclide.

Abstract: This invention relates to therapeutic reagents and peptides, including radiotherapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic agents. Specifically, the invention relates to cyclic peptide derivatives and analogs of somatostatin, and embodiments of such peptides radiolabeled with a radioisotope, as well as methods and kits for making, radiolabeling and using such peptides for radiodiagnostic and radiotherapeutic purposes. The invention specifically relates to cyclic peptide derivatives and analogues of somatostatin radiolabeled with technetium-99m and uses thereof as scintigraphic imaging agents. The invention also specifically relates to cyclic peptide derivatives and analogues of somatostatin radiolabeled with cytotoxic radioisotopes such as rhenium-186 (186Re) and rhenium-188 (188Re) for use as radiotherapeutic agents.

Abstract: 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 limited by 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.

Abstract: A pharmaceutical composition useful for killing or inhibiting multiplication of cancer cells. It is expected that the pharmaceutical composition will be useful in preventing, inhibiting, or modulating the hypersecretion of VIP, somatostatin, bombesin, Substance P, or a combination of VIP, somatostatin, bombesin, or Substance P. The composition may suitably comprise, consist of, or consist essentially of a therapeutically effective combination of peptide analogs of somatostatin, VIP, bombesin, and Substance P. Also provided is a method of treatment for humans or other animals suffering from cancer, the method comprising administering a therapeutically effective dose of the pharmaceutical composition so as to kill or inhibit the multiplication of cancer cells. The method of treatment may be particularly useful in the treatment of cancers of the colon and rectum.

Abstract: There is disclosed a composition containing a biologically active polypeptide selected from LHRH, an LHRH analog, somatostatin and a somatostatin analog, in a therapeutically effective amount, a membrane permeability enhancing agent, and a protease enzyme inhibitor enveloped within an enteric coating. The composition possesses enhanced bioavailability upon oral administration.

Abstract: The present invention relates to compounds, compositions containing them, and their use for treating medical disorders related to binding to human somatostatin receptor subtypes.

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.

Abstract: A method for the prevention of a patient's fibroproliferative vasculopathy following vascular injury or a vascular surgical operation. The method includes administering to the patient an agonist specific for at least one somatostatin (SST) receptor showing an increased expression in the patient's vascular wall subsequent to injury or operation, the administering being carried out for one to two weeks after the injury or surgical operation.

Abstract: The invention is directed to a method and food product for achieving at least one of the following: increasing muscle protein or reducing fat in an animal. The method comprises administering to the animal an effective amount of a composition comprising a gastrointestinal neuro-modulator antibody in order to neutralize the gastrointestinal neuro-modulator.

Abstract: This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to peptides, methods and kits for making such peptides, and methods for using such peptides to image sites in a mammalian body labeled with technetium-99m (Tc-99m) via a radiolabel-binding moiety covalently attached to a specific binding peptide via an amino acid side-chain of the peptide.

Abstract: The present invention provides a method for chemically removing a N-terminal methionine residue selectively, specifically and efficiently from a peptide or a salt thereof having an optionally oxidized methinine residue at its N-terminal. The method reacts a peptide or a salt thereof having an optionally oxidized methinine residue at its N-terminal with an .alpha.-diketone derivative, followed by hydrolysis.

Abstract: Novel peptides which are conformationally constrained backbone cyclized somatostatin analogs. Methods for synthesizing the somatostatin analogs and for producing libraries of the somatostatin analogs are also disclosed. Furthermore, pharmaceutical compositions comprising somatostatin analogs, and methods of using such compositions are disclosed.

Abstract: This invention relates to therapeutic reagents and peptides, including radiotherapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic agents. Specifically, the invention relates to cyclic peptide derivatives and analogs of somatostatin, and embodiments of such peptides radiolabeled with a radioisotope, as well as methods and kits for making, radiolabeling and using such peptides for radiodiagnostic and radiotherapeutic purposes. The invention specifically relates to cyclic peptide derivatives and analogues of somatostatin radiolabeled with technetium-99m and uses thereof as scintigraphic imaging agents. The invention also specifically relates to cyclic peptide derivatives and analogues of somatostatin radiolabeled with cytotoxic radioisotopes such as rhenium-186 (.sup.186 Re) and rhenium-188 (.sup.

Abstract: Disclosed are lanthionine peptides having the structure ##STR1## methods of their preparation and use as pharmacologically active agents.

Abstract: This invention relates to radiotherapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic and radiotherapeutic agents. Specifically, the invention relates to vasoactive intestinal peptide receptor binding peptides, derivatives and analogues of vasoactive intestinal peptide, and embodiments of such peptides radiolabeled with a radioisotope, as well as methods and kits for making, radiolabeling and using such peptides for radiodiagnostic and radiotherapeutic purposes. The invention specifically relates to vasoactive intestinal peptide receptor binding peptide derivatives and analogues of vasoactive intestinal peptide radiolabeled with technetium-99m and uses thereof as scintigraphic imaging agents. The invention also specifically relates to vasoactive intestinal peptide receptor binding peptide derivatives and analogues of vasoactive intestinal peptide radiolabeled with cytotoxic radioisotopes such as rhenium-186 (.sup.186 Re) and rhenium-188 (.

Abstract: The present invention relates to a method of decreasing body weight in a patient. The method includes the step of administering a therapeutically effective amount of a type-5 selective somatostatin agonist to the patient.

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.

Abstract: A cyclic peptide analog of somatostatin wherein a disulfide bond links the N-terminus residue and the C-terminus residue.

Abstract: This invention relates to diagnostic and radiodiagnostic agents, including radiolabeled scintigraphic imaging agents, and therapeutic and radiotherapeutic agents. The invention provides such agents and reagents for preparing such agents, and methods for producing and using such reagents. Specifically, the invention provides radiolabeled imaging agents and non-radioactively labeled imaging agents for imaging sites in a mammalian body and reagents for preparing these imaging agents. The invention also provides radiolabeled therapeutic agents, as well as non-radioactively labeled therapeutic agents, and reagents and methods for preparing these agents. The agents and reagents provided comprise a specific binding peptide, covalently linked to a metal ion-complexing moiety. Reagents, methods and kits for making such reagents, methods for labeling such reagents, and methods for using such labeled reagents are provided.

Abstract: The invention relates to radiotherapy with somatostatin-derived peptides labeled with medically useful metal ions. The invention in particular provides for methods and reagents for labeling somatostatin-derived peptides with perrhenate, in which a solution including somatostatin-derived peptide analogue containing at least one disulfide bond is provided, the solution is reacted with stannous ions and with a radioisotope, wherein the stannous ions are sufficient to substantially reduce the disulfide bonds of the peptide and the radioisotope, and the radiolabeled somatostatin-derived peptide analogue recovered. Also provided are methods for regional administration of radiolabeled somatostatin-derived peptides, methods for enhanced regional retention of radiolabeled somatostatin-derived peptides, methods for treatment of arthritis using radiolabeled somatostatin derived peptides, and methods for stabilizing radiolabeled somatostatin derived peptides.

Abstract: This invention relates to diagnostic and radiodiagnostic agents, including radiolabeled scintigraphic imaging agents, and therapeutic and radiotherapeutic agents. The invention provides such agents and reagents for preparing such agents, and methods for producing and using such reagents. Specifically, the invention provides radiolabeled imaging agents and non-radioactively labeled imaging agents for imaging sites in a mammalian body and reagents for preparing these imaging agents. The invention also provides radiolabeled therapeutic agents, as well as non-radioactively labeled therapeutic agents, and reagents and methods for preparing these agents. The agents and reagents provided comprise a specific binding peptide, covalently linked to a metal ion-complexing moiety. Reagents, methods and kits for making such reagents, methods for labeling such reagents, and methods for using such labeled reagents are provided.

Abstract: The present invention provides methods and kits for detecting cardiovascular disease in a living mammal, using a labeled form of a somatostatin analog. The methods and kits of the invention provide early detection of atherosclerotic plaque, in particular, unstable atherosclerotic plaque, thus allowing therapeutic intervention prior to acute and potentially fatal incidents of cardiovascular disease.

Abstract: This invention relates to diagnostic and radiodiagnostic agents, including radiolabeled scintigraphic imaging agents, and therapeutic and radiotherapeutic agents. The invention provides such agents and reagents for preparing such agents, and methods for producing and using such reagents. Specifically, the invention provides radiolabeled imaging agents and non-radioactively labeled imaging agents for imaging sites in a mammalian body and reagents for preparing these imaging agents. The invention also provides radiolabeled therapeutic agents, as well as non-radioactively labeled therapeutic agents, and reagents and methods for preparing these agents. The agents and reagents provided comprise a specific binding peptide, covalently linked to a metal ion-complexing moiety. Reagents, methods and kits for making such reagents, methods for labeling such reagents, and methods for using such labeled reagents are provided.

Abstract: This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to specific binding peptides, methods and kits for making such peptides, and methods for using such peptides labeled with technetium-99m via a radiolabel-binding moiety covalently linked to the peptide to image thrombus sites in a mammalian body.

Abstract: The present invention is directed to a method of using somatostatin or a somatostatin agonist to inhibit the proliferation of Helicobacter pylori (H. pylori), which comprises administering to a patient in need thereof an effective amount of said somatostatin or somatostatin agonist. Preferably, a somatostatin sub-type receptor 2 (SSTR-2) selective somatostatin agonist is administered in a method of this invention. The inhibition of H. pylori proliferation is useful in treating various gastroduodenal diseases such as peptic ulcers, gastric cancer and gastric lymphoma.

Abstract: This invention relates to diagnostic and radiodiagnostic agents, including radiolabeled scintigraphic imaging agents, and therapeutic and radiotherapeutic agents. The invention provides such agents and reagents for preparing such agents, and methods for producing and using such reagents. Specifically, the invention provides radiolabeled imaging agents and non-radioactively labeled imaging agents for imaging sites in a mammalian body and reagents for preparing these imaging agents. The invention also provides radiolabeled therapeutic agents, as well as non-radioactively labeled therapeutic agents, and reagents and methods for preparing these agents. The agents and reagents provided comprise a specific binding peptide, covalently linked to a metal ion-complexing moiety. Reagents, methods and kits for making such reagents, methods for labeling such reagents, and methods for using such labeled reagents are provided.

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.

Abstract: Cyclic peptides of general formula (I), wherein the groups are as described in the disclosure, having inhibitory activity on growth hormone. The peptides of formula (I) have also anticancer activity.

Abstract: New LH-RH antagonists are disclosed, in particular peptidomimetics and peptides modified in a side chain, their salts with pharmaceutically acceptable acids and a process for preparing these LH-RH antagonists and their salts. The disclosed peptides represent analogues of the luteinising hormone releasing hormone (LH-RH). The disclosed compounds have a high antagonistic power and are free of undesirable side effects, in particular edematogenic effects.

Abstract: 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.

Abstract: This invention relates to therapeutic reagents and peptides, including radiotherapeutic reagents and peptides, and radiodiagnostic reagents and peptides. Specifically, the invention relates to cyclic peptide derivatives and analogs of somatostatin, and embodiments of such peptides radiolabeled with a radioisotope, as well as methods for using such peptides for radiodiagnostic and radiotherapeutic purposes.

Abstract: Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N.sup..alpha. (.omega.-functionalized)amino acids constructed to include a spacer and a terminal functional group. One or more of these N.sup..alpha. (.omega.-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

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 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.

Abstract: The invention features a novel recombinant polypeptide that transactivates the somatostatin promoter, the polypeptide being present in pancreatic duct cells and not present in pancreatic .alpha.-cells, the polypeptide being encoded by a gene which encodes a protein on the order of 31 kd.

Abstract: This invention relates to radiotherapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic and radiotherapeutic agents. Specifically, the invention relates to VIP receptor binding peptides, derivatives and analogues of VIP, and embodiments of such peptides radiolabeled with a radioisotope, as well as methods and kits for making, radiolabeling and using such peptides for radiodiagnostic and radiotherapeutic purposes. The invention specifically relates to VIP receptor binding peptide derivatives and analogues of VIP radiolabeled with technetium-99m and uses thereof as scintigraphic imaging agents. The invention also specifically relates to VIP receptor binding peptide derivatives and analogues of VIP radiolabeled with cytotoxic radioisotopes such as rhenium-186 (.sup.186 Re) and rhenium-188 (.sup.188 Re) for use as radiotherapeutic agents.

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.

Abstract: Antigenic molecules cause antibodies to be raised against at least some of the 91 to 102 region of a natural growth hormone when parenterally administered in vivo. The molecules can include portions of the 91 to 102 region, particularly the 94 to 98 region. The antibodies are believed to bind to growth hormone on administration and enhance its effect.

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.

Abstract: This invention relates to radiolabeled peptide compositions for radiopharmaceutical use and, more specifically, to radiolabeled peptides for diagnostic or therapeutic use having an unmodified carboxy terminal amino acid. The radiopharmaceutical composition may be used for targeting a selected biological site. The radiolabeled peptide is characterized by having its carboxy terminal amino acid in its carboxylic acid form and the peptide is coupled to a diagnostic or therapeutic radionuclide by a chelating agent. The radiopharmaceutical composition preferably comprises a radiolabeled peptide selected from the group consisting of somatostatin, an analog of somatostatin, a derivative of somatostatin and peptides capable of binding to the somatostatin receptor, where the peptide is coupled to a diagnostic or therapeutic radionuclide by a chelating agent has its carboxy terminal amino acid in its carboxylic acid form.

Abstract: Methods for increasing the growth rate of a human patient having partial growth hormone insensitivity syndrome, but not Laron syndrome, are described. One such method comprises administering an effective dose of growth hormone, preferably growth hormone with a native human sequence, with or without an N-terminal methionine, to the patient. The patient is characterized as having a height of less than about -2 standard deviations below normal for age and sex, a serum level of high-affinity growth hormone binding protein that is at least 2 standard deviations below normal levels, a serum level of IGF-I that is below normal mean levels, and a serum level of growth hormone that is at least normal. In another such method, the same patient population is treated with an effective amount of IGF-I, given alone or in combination with an amount of growth hormone that is effective in combination with the IGF-I.

Abstract: Light-emitting compounds of the formula: ##STR1## where R.sub.1 is a light-emitting moiety and R.sub.2 is a somatostatin-based peptide featuring a first amino acid sequence -Phe-Phe-Trp-Lys-Thr- or (SEQ ID NO:1) or -Phe-Phe-D-Trp-Lys-Thr-. The peptide is linked at a first amino acid position to (C-X), and the light-emitting compound exhibits substantial biological activity in the presence of a receptor having affinity for somatostatin-based peptides.

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.

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.

Abstract: Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor.