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: High-affinity response-selective C-terminal analogs of C5a anaphylatoxin are provided. Whereas natural C5a has considerable flexibility in the C-terminal region, the analogs of the invention possess a backbone conformation which is constrained at the C-terminus to a .beta.-turn. The stabilized .beta.-turn confers a marked increase in in potency of the analogs; the particular .beta.-turn motif further confers the capability to selectively elicit certain biological responses associated with C5a. Exemplary compounds of the invention are decapeptide analogs of the formula: A1-Ser-Phe-Lys-A2-A3-A4-A5-A6-A7, with the constrained .beta.-turn being localized in the region of A4-A7.

Abstract: A cyclic peptide includes a dicarboxylic amino acid. The cyclic peptide bears at least one tail for subsequent coupling on a solid support, on a high molecular weight compound, on a marker, or on one or more other similar or different cyclic peptides. The present invention is also related to the preparation process of the cyclic peptide and to a biomaterial which includes the cyclic peptide.

Abstract: An assay for screening snake venom for the presence or absence of platelet aggregation inhibitors (PAIs) based on specific receptor binding is described. Using this assay, the identification and characterization of PAIs in a wide range of snake venom samples was accomplished. The isolated and purified PAI from several of these active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K*-(G/Sar)-D wherein K* is a modified lysyl residue of the formulaR.sup.1.sub.2 N(CH.sub.2).sub.4 CHNHCO--wherein each R.sup.1 is independently H, alkyl(1-6C) or at most one R.sup.1 is R.sup.2 --C.dbd.NR.sup.3 wherein R.sup.2 is H, alkyl(1-6C), phenyl or benzyl, or is NR.sup.4.sub.2 in which each R.sup.4 is independently H or alkyl(1-6C) and R.sup.3 is H, alkyl(1-6C), phenyl or benzyl, or R.sup.2 --C.dbd.NR.sup.3 is a radical selected from the group consisting of: ##STR1## where m is an integer of 2-3, and each R.sup.

Abstract: Described are peptides and peptide mimetics that bind to and activate the thrombopoietin receptor. Such peptides and peptide mimetics are useful in methods for treating hematological disorders and particularly, thrombocytopenia resulting from chemotherapy, radiation therapy, or bone marrow transfusions as well as in diagnostic methods employing labeled peptides and peptide mimetics.

Abstract: Peptides having the formula:T-Gly-Val-D-Ile-Thr-Arg-Ile-U,V-Gly-D-Val-Ile-D-Thr-D-Arg-D-Ile-W,X-D-Arg-D-Ile-D-Arg-D-Thr-lle-D-Val-Y, andZ-Gly-Val-Ile-Thr-Arg-Ile-Uwherein T is absent or is selected from N-protecting group and a polypeptide of up to 12 amino acid residues optionally terminated with a N-protecting group; U is selected from Arg and Arg-NR.sup.1 R.sup.2 wherein R.sup.1 and R.sup.2 are independently selected from hydrogen and alkyl of one to four carbon atoms; V is absent or a N-protecting group; W is selected from D-Arg and D-Arg-NR.sup.1 R.sup.2 ; X is absent or a N-protecting group; Y is selected from Gly and Gly-NR.sup.1 R.sup.2 ; and Z is 1-12 amino acid residues optionally terminated with a N-protecting group wherein at least one of the amino acid residues is a D-amino acid residue inhibit angiogenesis and are useful in the treatment of disease states such as cancer, arthritis, macular degeneration and diabetic retinopathyin which angiogenesis plays a role.

Abstract: This invention relates to stable non-aqueous polar aprotic formulations of peptide compounds. These stable formulations comprise peptide in non- aqueous polar aprotic solvent. They may be stored at elevated temperatures for long periods of time and are especially useful in implantable delivery devices for long term delivery of drug.

Abstract: Methods and compositions are described for the treatment of intestinal disorders, and, more specifically, for improving motility in the colon in humans and animals. Compositions comprising neuropeptides are administered to humans and animals having symptoms of post-operative ileus.

Abstract: Porous polymer monoliths are made thermally responsive by functionalizing/grafting the pores with thermally responsive polymers and copolymers. Depending on the reaction conditions employed, the grafted polymer can either completely block flow through micrometer-sized pores in the monoliths or control the flow rate through the monoliths. The grafted monoliths are useful as thermal gates, thermal valves, and for isocratic hydrophobic interaction chromatography of proteins.

Abstract: The invention relates to a method of examining inorganic materials which are treated with organosilicon compounds, wherein the sample material is pyrolyzed within a few seconds and the pyrolysis products are analyzed on-line by gas chromatography on a PLOT column (porous layer open tubular column).

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: Methods for making preparations of homogenous peptides are disclosed. In these methods, reversible alterations of the physicochemical properties of the peptides are exploited. In preferred embodiments, the methods include the following sequential steps: (1) exhaustive capping is carried out during solid-phase synthesis of a desired peptide; (2) a cleavable linker is attached to the peptide, (3) a polymer is added to the peptide either by condensation with preformed polymer or by in situ polymerization such that the linker is interposed between the polymer moiety and the peptide moiety of the resultant adduct; alternatively, steps (2) and (3) can be conducted simultaneously by attaching a combination polymer/linker to the peptide; (4) the polymer-peptide adduct is cleaved from the resin; (5) the polymer-peptide adduct is purified from undesired, nonadducted peptides; and (6) the polymer-peptide adduct is cleaved at the linker, and the desired peptide is purified from the polymer.

Abstract: The present invention provides a novel internal standard for amino acid sequencing which contains a peptide consisting of unnatural amino acid residues, such as ornithine, norvaline, norleucine and .alpha.-aminobutyric acid, that is capable of being sequenced simultaneously with an unknown peptide or protein without interfering with the analysis. The internal standard peptide has an amino acid sequence containing at least two different unnatural amino acid residues having retention times distinct from the corresponding retention times for natural amino acid residues. Information derived from the sequencing of the internal standard allows determination of repetitive yield, lag, N-terminal blockage and discrimination between blank cycles caused by missed injection and blank cycles caused by faulty delivery of chemicals during the sequencer reactions.

Abstract: Disclosed are a peptide derivative, which may be protected, containing a fluorescent group whose fluorescence is quenched with a quenching group in its molecule, the quenching group and a phosphoric acid group existing between said fluorescent group and said quenching group, in its molecule, a method for measuring protein phosphatase activity using the same as a substrate, and a reagent therefor.

Abstract: The present invention provides novel peptides derived from portions of the sequence of amino acids 42-48 of P-selectin. The invention also provides pharmaceutical compositions comprising the peptides of the invention, and diagnostic and therapeutic methods utilizing the peptides and pharmaceutical compositions of the invention.

Abstract: Methods and compositions for the treatment of non-Ige-mediated inflammatory response or disease conditions are described.

Abstract: The invention relates to a highly selective chemical sensor comprising an acoustic wave transducer and a sensitive layer of so-called "molecular fingerprint" material. This is a macroporous crosslinked material having cavities whose steric and functional configuration is specifically suited to capturing molecular and/or ionic species.

Abstract: Monocyte chemotactic peptide-1 or a functional derivative thereof is useful in inducing cervical ripening, for example for; (A) induction of labor at term, (B) induction of labor in connection with a pathological pregnancy, (C) induction of labor in connection with intrauterine fetal death, (D) induction of abortion, (E) induction of pretern labor, (F) induction of cervical ripening of a non-pregnant female or pregnant female to assist for surgical or diagnostic procedure, and (G) induction of cervical ripening for female to be treated by in vitro fertilisation.

Abstract: This invention relates to the antibiotic feglymycin, as well as processes for its preparation and use.

Abstract: A method of preventing progression of neuropathic pain is disclosed. The method includes administering to a subject an N-type voltage-sensitive calcium channel blocking compound which is characterized by its ability to (a) inhibit electrically stimulated contraction of the guinea pig ileum, and (b) bind selectively to omega conopeptide MVIIA binding sites present in neuronal tissue. Also disclosed are formulations effective to stabilize omega conotoxin peptide preparations at elevated temperatures. Novel omega conopeptides also form part of the invention.