Abstract: The invention relates to composition comprising a pharmaceutically effective amount of one or more functional vasoactive intestinal peptide (VIP) fragments, and the use of those compositions in the treatment of fibrosis, hypertension and other disorders.

Abstract: Method of obtaining and/or verifying a binder to prepro-Vasopressin (SEQ ID NO. 1) or fragments thereof of at least 6 amino acids in length, including Copeptin (SEQ ID NO. 2), comprising at least one of the steps of: a) generating the binder using a developer comprising an amino acid sequence of at least 6 amino acids in length contained in an amino acid sequence corresponding to the C-terminal part but lacking amino acid 164 of prepro-Vasopressin (SEQ ID NO. 1); b) determining whether the binder is capable of binding to an amino acid sequence of at least 4 amino acids in length contained in an amino acid sequence corresponding to the C-terminal part but lacking amino acid 164 of prepro-Vasopressin (SEQ ID NO. 1); c) selecting and optionally isolating the binder from a plurality of binders which is capable of binding to an amino acid sequence contained in an amino acid sequence corresponding to the C-terminal part but lacking amino acid 164 of prepro-Vasopressin (SEQ ID NO.

Abstract: The invention describes compositions of peptide analogs that are active in blood or cleavable in blood to release an active peptide. The peptide analogs have a general formula: A-(Cm)x-Peptide (SEQ ID NO: 76), wherein A is hydrophobic moiety or a metal binding moiety, e.g., a chemical group or moiety containing 1) an alkyl group having 6 to 36 carbon units, 2) a nitrilotriacetic acid group, 3) an imidodiacetic acid group, or 4) a moiety of formula (ZyHisw)p (SEQ ID NO: 50), wherein Z is any amino acid residue other than histidine, His is histidine, y is an integer from 0-6; w is an integer from 1-6; and p is an integer from 1-6; wherein if A has alkyl group with 6 to 36 carbon units x is greater than 0; and Cm is a cleavable moiety consisting of glycine or alanine or lysine or arginine or N-Arginine or N-lysine, wherein x is an integer between 0-6 and N may be any amino acid or none. The peptide analogs are complexed with polymeric carrier to provide enhanced half-life.

Abstract: The present invention provides a method for preparing atosiban acetate. The method comprises the following steps of: synthesizing to obtain linear atosiban; dissolving the linear atosiban in an acetonitrile aqueous solution, adjusting the pH value with ammonia water, adding H2O2 for oxidizing, filtering, purifying, and transferring salt to obtain the atosiban acetate. In the present invention, an appropriate route is provided, the linear atosiban is synthesized by adopting a solid phase method, and the atosiban is obtained by liquid phase oxidation. The method has the advantages of capabilities of solving the problem of insolubility of the linear atosiban, reducing the reaction size to the maximum extent and shortening reaction time, and being high in yield and easy to industrialize.

Abstract: The present invention relates to methods for the treatment of headache and headache disorders. The methods comprise administration of an oxytocin peptide for the treatment of primary and secondary headaches or trigeminal neuralgia.

Abstract: The present invention concerns a method of detecting the antifungal cyclic hexapeptides Pneumocandin B0 and/or Pneumocandin C0 specific fragment is/are detected using MS in negative mode.

Abstract: The invention provides methods for treating stroke and compositions for use in the same. The methods employ a chimeric peptide of an active peptide and an internalization peptide. The internalization peptide is a tat variant that promotes uptake of itself and a linked active peptide into a cell without substantial binding to N-type calcium channels. Use of the tat variant allows treating of stroke free of certain side effects associated with binding to N-type calcium channels. Tat variant peptides can also be linked to other active agent for use in treating other diseases.

Abstract: Peptide analogues of oxytocin are described together with methods of treating conditions ameliorated by modulating oxytocin receptor. The peptide analogues are seleno or telluro peptide analogues. Methods of synthesis of selenocysteine, tellurocysteine and oxytocin analogues are also described.

Abstract: The present invention provides methods for the therapy and prevention of problem drinking in alcohol-dependent and non-dependent subjects and those at risk of developing problem drinking behavior, and compositions of matter comprising oxytocin or an analog or derivative thereof or an agonist or partial agonist of an oxytocin receptor that are useful in preventing or treating problem drinking.

Abstract: The present invention relates to methods for the treatment or prevention of trigeminal nerve-associated pain, in particular chronic, acute and procedural-related pain. The methods comprise administration of analgesic agents to the trigeminal nerve system which results in analgesia to the facial or head region.

Abstract: The present invention relates to methods for the treatment of headache and headache disorders. The methods comprise administration of an oxytocin peptide for the treatment of primary and secondary headaches or trigeminal neuralgia.

Abstract: The present invention relates to oxytocin receptor agonist compounds, pharmaceutical compositions comprising the same, use of such compounds for the manufacture of a medicament for treatment of inter alia, abdominal pain, irritable bowel syndrome (IBS), autism, erectile dysfunction, female sexual dysfunction, labor induction and maintenance, lactation induction and maintenance, postpartum hemorrhage, Post Traumatic Stress Disorder (PTSD), pain, anxiety and other conditions, as well as to methods for the treatment of such conditions, wherein such compounds are administered.

Abstract: The present invention relates to the use of novel compounds for the manufacture of a medicament for treatment of, inter alia, conditions associated with critical care sepsis, septic shock, hepatorenal syndrome type I, hypertension induced by endstage venal disease, severe burns, thermal injury as well as to a method for treatment of the conditions by administering the compounds. The compounds used are represented by the general formula (1), as further defined in the specification.

Abstract: The present disclosure demonstrates the utility of ion pairing agents in the preparative scale of purification. More particularly, the disclosure relates to the usage of ion pairing agents in RP preparative linear chromatography enabling high purity of the desired end product. The disclosure shows that ion-pairing agents have dramatic effect on desired purity of polypeptides.

Abstract: The present invention relates to methods for the treatment of headache and headache disorders. The methods comprise administration of an oxytocin peptide for the treatment of primary and secondary headaches or trigeminal neuralgia.

Abstract: The present invention relates to methods for the treatment of headache and headache disorders. The methods comprise administration of an oxytocin peptide for the treatment of primary and secondary headaches or trigeminal neuralgia.

Abstract: The present invention relates to a novel and improved process for the preparation of 1-deamino-8-D-arginine vasopressin (Desmopressin) or its pharmaceutically acceptable salts thereof and also relates to an improved process for the purification of Desmopressin or its pharmaceutically acceptable salts. Further, the present invention also relates to pharmaceutical composition of Desmopressin or its pharmaceutically acceptable salts thereof.

Abstract: Stabilized radiopharmaceutical formulations are disclosed. Methods of making and using stabilized radiopharmaceutical formulations are also disclosed. The invention relates to stabilizers that improve the radiostability of radiotherapeutic and radiodiagnostic compounds and formulations containing them. In particular, it relates to stabilizers useful in the preparation and stabilization of targeted radiodiagnostic and radiotherapeutic compounds, and, in a preferred embodiment, to the preparation and stabilization of radiodiagnostic and radiotherapeutic compounds that are targeted to the Gastrin Releasing Peptide Receptor (GRP-Receptor).

Abstract: The present invention relates to methods for the treatment of headache and headache disorders. The methods comprise administration of an oxytocin peptide for the treatment of primary and secondary headaches or trigeminal neuralgia.

Abstract: The present invention provides a method for preparing a site-specific physiologically active polypeptide conjugate in a high yield by treating a physiologically active polypeptide with a non-peptidyl polymer in the presence of an alcohol at a specific pH, which can be desirably employed in the development of long acting formulations of various peptide drugs having high in-vivo activity and markedly prolonged in-blood half-life.

Abstract: substances and the nasal administration thereof, in particular as one of a liquid, as a suspension or solution, or a powder, to the nasal airway of a subject, in particular the posterior region of the nasal airway, and in particular the upper posterior region of the nasal airway, which includes the olfactory bulb, in particular in the treatment of neurological conditions and disorders.

Abstract: The invention describes compositions of peptide analogs that are active in blood or cleavable in blood to release an active peptide. The peptide analogs have a general formula: A-(Cm)x-Peptide (SEQ ID NO: 76), wherein A is hydrophobic moiety or a metal binding moiety, e.g., a chemical group or moiety containing 1) an alkyl group having 6 to 36 carbon units, 2) a nitrilotriacetic acid group, 3) an imidodiacetic acid group, or 4) a moiety of formula (ZyHisw)p (SEQ ID NO: 50), wherein Z is any amino acid residue other than histidine, His is histidine, y is an integer from 0-6; w is an integer from 1-6; and p is an integer from 1-6; wherein if A has alkyl group with 6 to 36 carbon units x is greater than 0; and Cm is a cleavable moiety consisting of glycine or alanine or lysine or arginine or N-Arginine or N-lysine, wherein x is an integer between 0-6 and N may be any amino acid or none. The peptide analogs are complexed with polymeric carrier to provide enhanced half-life.

Abstract: The invention describes compositions of peptide analogs exemplified by peptides derived from vasopressin, terlipressin, and GLP1 and others that are active in blood or cleavable in blood to release an active peptide. The peptide analogs have a general formula: A-(Cm)x-Peptide, wherein A is a hydrophobic moiety or a metal binding moiety, and Cm is a cleavable moiety consisting of glycine or alanine or lysine or arginine or N-Arginine or N-lysine, wherein x is an integer between 0-6 and N may be any amino acid or none. A may be linked to Cm by a linker group. The peptide analogs are complexed with polymeric carrier to provide enhanced half-life.

Abstract: More efficient and/or economical methods for synthesizing heptapeptide alcohol analogs of oxytocin are provided along with novel intermediates which are useful in synthesizing such oxytocin analogs. Efficient and economical methods for synthesizing intermediates useful in synthesizing these oxytocin analogs are also provided.

Abstract: The use of copeptin as diagnostic marker for the determination of the release of vasopressin, especially in connection with disorders associated with non-physiological alterations of vasopressin release from the neurohypophysis, especially for detection and early detection, diagnosing and monitoring of the course of cardiovascular diseases, renal and pulmonary diseases as well as shock, including septic shock, sepsis and diseases/disorders of the central nervous system and neurodegenerative diseases.

Abstract: This invention relates to the use of a cyclic compound of formula (I) wherein A, B independently in each occurrence is alkane-i,j-diyl having k carbon atoms, i and independently j being less than or equal k and k being selected from 1 to 10, wherein said alkane-i,j-diyl (i) may comprise one or more double bonds; (ii) is optionally substituted; and/or (iii) comprises a cycle, wherein the total number of cycles being cyclic sugars in said compound is selected from 0 to 4 and is less than p·n+m); X,Y independently in each occurrence is a biocompatible functional group comprising at least one oxygen atom or two sulphur atoms; n, m independently of each other are selected from 0 to 20; p is selected from 1 to 10; n+m is equal or greater than 1; and p·(n+m) is selected from 3 to 30; wherein said compound is capable of forming a complex with a protonated primary and/or protonated secondary amino group and/or a protonated guanidinium group for the manufacture of a pharmaceutical or diagnostic composition further

Abstract: Good bioavailability of desmopressin can be obtained by means of an orodispersible pharmaceutical dosage form. Preferred dosage forms comprise desmopressin and an open matrix network which is an inert water-soluble or water-dispersible carrier material. Desmopressin formulated in this way is useful for voiding postponement, or the treatment or prevention of incontinence, primary noctural enuresis (PNE), nocturia or central diabetes insipidus. Peptides other than desmopressin can also be formulated in this way.

Abstract: The present invention provides a method of synthesizing an intramolecularly bridged polypeptide comprising at least one intramolecular bridge. The present invention further provides a method of synthesizing an intramolecularly bridged polypeptide comprising two intramolecular bridges, wherein the two intramolecular bridges form two overlapping ring, two rings in series, or two embedded rings. The present invention also provides methods for synthesizing lantibiotics, including Nisin A. Additionally, the invention provides intramolecularly bridged polypeptides synthesized by the methods disclosed herein and differentially protected orthogonal lanthionines.

Abstract: The present invention is comprised of culturing a microorganism having ability to produce K01-B0171-B substance and/or K01-B0171-C substance in a medium, accumulating K01-B0171-B substance and/or K01-B0171-C substance in a culture fluid and isolating K01-B0171-B substance and/or, K01-B0171-C substance from the culture fluid. The obtained K01-B0171-B substance, K01-B0171-C substance or a composition of these substances is expected to be useful as a medicament of antituberculous agent.

Abstract: The invention relates to colloidal aqueous solutions of complexes between a charged peptide and a bilayer-forming galactolipid. The colloidal solutions can be used as a drug delivery system for the charged peptide in the treatment of infections, in wound healing and in other diseases.

Abstract: A sustained-release drug composition consisting essentially of microparticles of hyaluronic acid having a high molecular weight or an inorganic salt thereof and a protein or peptide drug encased in said microparticles, wherein the average size of said microparticles ranges from 0.1 to 40 ?m.

Abstract: Analogs of 1-desamino-8-D-arginyl vasopressin having the formula: wherein, X and Y are amino acids as defined herein, useful as an anti-diuretic or as an inhibitor of metastasis and cancer cell migration.

Abstract: The present invention relates to an improved method for the treatment of hypovolaemia or hypotension associated with therapeutic paracentesis, which method is characterised by the use of a peptide according to general formulae (I) or a salt thereof, wherin Asn, Cys, Gln, Gly, Phe and Pro represent the amino acid residues asparigine, cysteine, glutamine, glycine, phenylalanine and proline respectively; Phe(X) represents a phenylalanine residue optionally substituted at the 4-position of the aromatic ring by a group selected from methyl, ethyl, hydroxy and methoxy; Y represents a group —(CH2)a—NH-Q, where a is 2–5 and Q is H or C(?NH)NH2; and R represents a chain of between two and for ?alpha-amino acid residues, at least one of which is glycine, as the active agent. The invention also provides uses of the peptide and pharmaceutical compositions.

Abstract: The present invention relates to use of peptide to which G-protein coupled receptor protein recognizes as a ligand. Since the ligand polypeptide of the present invention has a stimulating action on oxytocin secretion, it is useful as a drug for ameliorating, preserving or treating various diseases related to oxytocin secretion such as uterine inertia, atonic hemorrhage, placental expulsion, subinvolution and the like.

Abstract: An object of the present invention is to provide a protein useful as a sphingomyelin detecting probe, which specifically recognizes sphingomyelin and has low cytotoxicity. The present invention provides a protein which has an amino acid sequence having, as the amino acid sequence from the 1st to the 48th amino acid, the amino acid sequence from the 1st to the 48th amino acid in Lysenin 1, and as the amino acid sequence from the 49th to the 298th amino acid, the amino acid sequence from the 51st to the 300th amino acid in Lysenin 3; and a protein which is obtained by deleting N terminal and/or C terminal from earthworm toxins Lysenin 1 or 3, and which specifically recognizes sphingomyelin.

Abstract: The present invention provides domain 1 ?2GPI polypeptides, polynucleotides encoding these polypeptides, mimetics of these polypeptides, and methods using domain 1 ?2GPI polypeptides and mimetics. Domain 1 of ?2GPI has been shown to bind to anti-cardiolipin (?2GPI-dependent antiphospholipid) antibodies, which are associated with several pathologies, such as thrombosis and fetal loss. The domain 1 ?2GPI polypeptides may be used to detect ?2GPI-dependent antiphospholipid antibodies in a sample. The invention further provides methods of inducing tolerance using these domain 1 ?2GPI polypeptides.

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

Abstract: A method for normalising abnormally elevated ACTH release in mammals, such as humans, which method comprises the administration of an effective, non-toxic amount of a compound which regulates the biological activity of the arginine vasopressin V1b receptor (the AVP V1b receptor); a compound and composition for use in such method.

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

Abstract: Substances having oxytocin activity can be used for the preparation of a pharmaceutical composition for the curative or prophylactic treatment of wounds, such as chronic wounds. The wound healing effect can be strengthened or prolonged by combining oxytocin with estrogen.

Abstract: A composition for permucosal administration characterized by containing Antago-3 or a physiologically acceptable salt thereof, and a sucrose fatty acid ester. With the composition for permucosal administration of the invention there is provided a long-term stable preparation having the high permucosal absorption of physiologically active peptide Antago-3 without irritation.

Abstract: Heptapeptide analogues or pharmaceutically acceptable salts thereof consist of a hexapeptide moiety S and a C-terminal .beta.-aminoalcohol residue Z bound to the moiety S by an amide bond, wherein the .beta.-aminoalcohol Z is --NR--CH(Q)--CH.sub.2 OH, Q is (CH.sub.2).sub.n --NH--A is H or --C(.dbd.NH)NH.sub.2, and R is CH.sub.3 or C.sub.2 H.sub.5, and the moiety S wherein H is a D-aromatic .alpha.-aminoacid and Y is an aliphatic .alpha.-aminoacid and have oxytocin antagonist activity. Also disclosed is: a method of their synthesis; pharmaceutical compositions containing these analogues; the synthesis of such compositions; a method of control of uterine contractions.

Abstract: Fatty acid derivatives of disulfide-containing compounds (for example, disulfide-containing peptides or proteins) comprising fatty acid-conjugated products with a disulfide linkage are employed for delivery of the compounds to mammalian cells. This modification markedly increases the absorption of the compounds by mammalian cells relative to the rate of absorption of the unconjugated compounds, as well as prolonging blood and tissue retention of the compounds. Moreover, the disulfide linkage in the conjugate is quite labile in vivo and thus facilitates intracellular or extracellular release of the intact compounds from the fatty acid moieties.

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

Abstract: A process for preparing and purifying cyclic peptides having disulfide moieties in a two step processing operation including reverse phase chromatography which simplifies synthesis and reduces production costs, yet produces high, quality yield. The improved process is particularly useful for the preparation of vasopressin and oxytocin and their respective derivatives and analogs.

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: A solid pharmaceutical composition for oral administration of small and medium size peptides, particularly vasopressin, oxytocin, and their analogues, comprises said peptide, an enteric coat and a pharmaceutically acceptable carrier containing a buffering agent buffering at a pH of from 2 to 6, preferably at about pH 5. A method of manufacture of single doses of said peptide comprises mixing of the ingredients, forming the resulting mixture into spheres smaller than 2 mm, coating the spheres with an enteric coat which is readily soluble in gastric juice of pH 5.0 or higher but not at substantially lower pH, and filling the coated spheres in capsules or incorporating them into tablets, degradable in the stomach. Also disclosed is a method for oral administration to a patient of said single dose.

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 is in the field of the chemistry of targeting anticancer anthracycline derivatives. More particularly, it concerns doxorubicin (DOX) or its daunosamine modified derivatives (DM-DOX) linked covalently to analogs of peptide hormones such as LH-RH, bombesin and somatostatin. These covalent conjugates are targeted to various tumors bearing receptors for the peptide hormone analogs. The compounds of this invention are represented by General Formula Q.sup.14 --O--R--P wherein Q has the general formula ##STR1## wherein: Q.sup.14 signifies a Q moiety with a side chain at the 14 position, R-- is H or --C(O)--(CH.sub.2).sub.n --C(O)-- and n=0-7, R' is NH.sub.2 or an aromatic, saturated or partially saturated 5 or 6 membered heterocyclic compounds having at least one ring nitrogen and optionally having a butadiene moiety bonded to adjacent carbon atoms of said ring to form a bicyclic system; P is H or a peptide moiety, suitably an LHRH, somatostatin or bombesin analogs. Nevertheless where R' is NH.sub.

Abstract: A pharmaceutical composition is provided which comprises vasopressin and an adrenergic agent in combination with a pharmaceutically acceptable carrier. The pharmaceutical composition is effective to increase arterial blood pressure so as to enhance arterial blood flow to the brain and heart when administered to a patient suffering from cardiac arrest. A method of treating a patient in cardiac arrest is also provided, which method comprises the administration of the pharmaceutical composition during the administration of CPR.