Abstract: Peptide medicaments, and antibody thereto, useful for treating or preventing diseases, particularly diseases involving an inflammatory response by a host organism against infection, that are preferably derived from the .beta. subunit, CD18, of the leukocyte integrins, and that have the property of either interfering with, or preventing undesirable leukocyte adhesion to biological materials, particular to endothelial cells, or that interfere with, or prevent the chemotaxis of leukocytes through the endothelial cell monolayer, consequently minimizing undesirable cell/tissue leukocyte binding and thus preventing or minimizing diseases resulting therefrom.

Abstract: Cell-free extracts from Pyrococcus furiosus were found to possess unusually high levels of proteolytic activity as measured by hydrolysis of azocasein; loss in activity was only 30% after incubation for 24 hours at 98.degree. C. and the half-life of proteolytic activity at that temperature was about 60 hours. Furthermore, cell-free extracts incubated at 98.degree. C. in 1% sodium dodecyl sulfate (SDS) for 24 hours yielded an SDS-resistant protease having a temperature optimum of at least 100.degree. C. The enzyme retained at least 40% of its activity when tested at 98.degree. C. by azocasein hydrolysis in the presence of 4M urea, 2M guanidinium chloride, 10 mM dithiothreitol or 150 mM .beta.-mercaptoethanol. The protease was found to have a pH optimum of 6.8 at 98.degree. C. and retained more than 45% of its activity at pH 9.3 and 82% of its activity at pH 4.5 in assays performed at those values.

Abstract: A high-absorbable transvaginal preparation having excellent absorbability of the active ingredient, which comprises a biologically active polypeptide and an absorption promoter comprising a polyoxyethylenealkylphenyl ether and one or more compounds selected from the group consisting of an N-acylamino acid, cholic acids, pectic acid, taurine, saccharin, glycyrrhizic acid, aspartame, or a salt thereof.

Abstract: This invention relates to peptide derivatives which are useful anticoagulant agents.

Abstract: New amino acid derivatives of the formulaR.sup.1 --Z--NR.sup.2 --CHR.sup.3 --CR.sup.4 --(CHR.sup.5).sub.a --CO--E--Q--Ywherein R.sup.1 to R.sup.5, a, Z, E, Q and Y have the meanings defined herein, and salts thereof inhibit the activity of human plasma renin.

Abstract: The invention relates to a method and apparatus for performing a multiple synthesis of peptides on a solid carrier. Active components are successively bonded to functional groups anchored on a carrier. The carrier planar functionalized porous material divided into compartments, into which the needed activated component is put. Common operations of the synthesis are carried out by all compartments of the carrier at the same time.

Abstract: Insulin precursors characterized by the amino acid sequence B(1-29)-X.sub.1 -X.sub.2 -Y.sub.2 -Y.sub.1 -A(1-21), wherein B(1-29) are the 29 first amino acid residues of the B chain of human insulin starting from the N-terminus, A(1-21) are the 21 amino acid residues of the A chain of human insulin, X.sub.1 represents a peptide bond or one or more arbitrary amino acid residues, X.sub.2 represents Glu or Asp, and Y.sub.1 and Y.sub.2 each represents Lys or Arg, the positions A6 and A11, A7 and B7 and A20 and B19, respectively, are connected through sulphur bridges, and, if desired, one or more of the amino acid residues of the chains B(1-29) and A(1-21) are substituted by another amino acid residue, are provided. The insulin precursors are prepared by culturing a yeast strain transformed with a replicable expression vehicle comprising a DNA sequence encoding an insulin precursor of the above formula in a suitable medium and isolating the insulin precursor thus formed from the culture medium.

Abstract: A process for the preparation of tripeptides of the general formula IU-A-B-C-OH Iin which U denotes hydrogen or a urethane protective group and A, B and C denote amino acids, by reaction of a compound of the general formula IIU'-B-OH IIin which U' is a urethane protective group which can be eliminated by hydrogenolysis, with a compound of the general formula IIIH-C-OR IIIin which R denotes alkyl, by the PPA method, elimination of U', and reacting the resulting compound of the formula IVH-B-C-OR IVwith a compound of the formula VU-A-OH Vin the presence of propylphosphonic anhydride, and finally eliminating R enzymatically.

Abstract: Oligopeptide compounds or oligopeptide analogue compounds of the formula A-B-D-E-G-J-L are ligands for the anaphylatoxin receptor and are useful in the treatment of inflammatory disease states. Also disclosed are anaphylatoxin receptor ligand compositions and a method for modulating anaphylatoxin activity.

Abstract: The invention relates to a method of diagnosing and treating individuals with diabetes or at risk to develop diabetes mellitus. In particular, gastric emptying determinations are used to assess risk. Risk or early symptoms associated with subsequent development of diabetes mellitus may be controlled or alleviated by delaying gastric emptying. Delay orThe Government may have certain rights in the invention pursuant to grant No. 2-S07-RR07187-11.

Abstract: A method is disclosed for producing an anabolic state in a mammal by co-administration by subcutaneous injection of a combination of effective amounts of IGF-I and an IGF binding protein in a defined molar ratio in the absence of growth hormone so as to produce a greater anabolic response in the mammal than that achieved using IGF-I alone in an amount equal to that used for IGF-I in the combination. Preferably, the IGF-I is native-sequence, mature human IGF-I, the binding protein is IGFBP-3, and the mammal is human or a non-human animal of economic importance such as a cow or pig.

Abstract: A novel dipeptide isostere is the biotransformed product after incubation with a culture of Streptomyces. It inhibits HIV protease, and is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: The present invention relates to DTrp-Phe containing tripeptides and pharmaceuticals, which possess tachykinin antagonism activity as well as processes of making such peptides.

Abstract: Admixture of insulin and a hydroxypyridone being: (1) a 3-hydroxypyrid-4-one in which the hydrogen atom attached to the nitrogen atom is replaced by an aliphatic acyl group, by an aliphatic hydrocarbon group, or by an aliphatic hydrocarbon group substituted by one or more substituents selected from aliphatic acyl, alkoxy, cycloalkoxy, aliphatic amide, aliphatic ester, halogen and hydroxy groups and, optionally, in which one or more of the hydrogen atoms attached to ring carbon atoms are replaced by an aliphatic acyl, alkoxy, cycloalkoxy, aliphatic amide, aliphatic ester, halogen or hydroxy group, by an aliphatic hydrocarbon group, or by an aliphatic hydrocarbon group substituted by an alkoxy, cycloalkoxy, aliphatic ester, halogen or hydroxy group, or a salt thereof.

Abstract: The present invention relates to compounds of the general formula I ##STR1## in which A denotes a radical from the group comprising S, SO, SO.sub.2, O, CO, CS or a direct bond,B denotes the radical of an amino acid andD denotes a CH.sub.2 group or a radical --NR.sup.7 --, where R.sup.7 can be hydrogen or a (C.sub.1 -C.sub.4)alkyl radical;and in which R.sup.1 to R.sup.4 are defined as indicated in the description, to a process for the preparation thereof, to agents containing these, and to the use thereof.

Abstract: This invention relates to solid phase peptide synthesis.Solid phase peptide synthesis is accomplished on polyacrylic resins (such as those described in EP 0 079 812 and EP 0 081 408 which correspond to U.S. Pat. Nos. 4,436,874 and 4,439,545 respectively) by a method which includes in the coupling protocol steps of washing the resin in water and/or aqueous solution(s).

Abstract: The present invention provides substituted cyclic pentapeptide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable slats, esters and amides thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract: Peptides comprising the tripeptide sequence of arginine-tyrosine-aspartic acid, linked from amino- to carboxy-terminus, are inhibitors of fibrinogen binding, platelet aggregation, glycoprotein IIb-IIIa binding and related aberrant and normal physiological conditions.

Abstract: Methods for making peptides of a suitable length for solid phase synthesis, which peptides include in their sequence a pair of residues of a different character which have acylated side chains and a residue which has an N-alkylated side chain. A peptide intermediate is constructed on the resin using commercially available starting materials. The N-terminus can be acylated by removing the .alpha.-amino protecting group and acylating under standard conditions. First primary amino protecting groups included in those residues to be acylated are removed, and acylation is effected, preferably by using a carboxypyridine or a similar heterocyclic acylating agent. Following such side chain acylation, a second protecting group included in the residue to be N-alkylated is removed, and the N-alkylation reaction is carried out while the peptide remains on the resin using a borohydride and an appropriate aldehyde or ketone.

Abstract: Described is a purified osteogenic factor that when delivered to bone in association with a physiologically acceptable delivery vehicle is capable of inducing new bone growth at the bone surface. The osteogenic factor is water soluble, and is characterized physically by a molecular weight of about 2.5 kD when measured by gel filtration under dissociating conditions and an isoelectric point in the pH range from about 4.6 to 7.2. Use of the purified factor in treating bone defects is described. Also described is a method for obtaining the purified factor from mammalian bone.