Abstract: A novel industrial process for producing an anthelmintic depsipeptide derivative represented by structural formula (I), which is excellent in the yield etc.

Abstract: A compound of the formula ##STR1## is disclosed which is useful for the treatment of fungal infections and for the treatment of infections caused by Pneumocystis carinii.

Abstract: Peptides derived from the second type 1 repeat of human endothelial cell thrombospondin which bind to the gelatin-binding domain of fibronectin have been isolated and synthetically produced. The peptides can be used to bind to fibronectin or other related collagen-binding proteins to inhibit fibronectin-dependent cell adhesion to collagen matrices and to inhibit interactions with collagen of other proteins that share homologies with the gelatin-binding domain of fibronectin.

Abstract: A method for decreasing the effect of somatostatin. A peptide of formula I which is a pure somatostatin antagonist, methods for increasing the release of growth hormone, insulin and glucagon in mammals, and a method for the enhancement of growth in mammals are also described.

Abstract: The present invention provides glycopeptide antibiotic derivative compounds. These derivative compounds possess antibacterial activity aginst a wide variety of bacteria, including activity against vancomycin-resistant isolates. Methods of making and using these glycopeptide antibiotic derivative compounds are also provided.

Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin -1.beta. protease activity, the compounds having the structure of formula (1) as described in the specification.

Abstract: Pharmaceutical compositions of matter adapted for intravaginal administration comprise a biologically active polypeptide, an absorption promoter, such as an anionic and/or nonionic surfactant or a nonionic surfactant and an aliphatic carboxylic acid, optionally an animal and/or vegetable protein and a nontoxic pharmaceutically acceptable carrier or diluent therefor, in a formulation suitable for intravaginal administration. Preferred compositions comprise calcitonin as the biologically active polypeptide. Preferred absorption promoters are anionic surfactants, e.g., sodium lauryl sulfate, and the combination absorption promoter of a nonionic surfactant and a medium chain aliphatic carboxylic acid or its salt, e.g. polyoxyethylenealkylphenylether and a medium chain aliphatic carboxylic acid.

Abstract: Peptide reagents and compositions thereof which reduce blood clotting initiated by the ternary complex of tissue factor (TF), FVIIa and FXa. The peptides have the amino acid sequences Thr--Leu--Tyr--Tyr--Trp--Arg--Ala--Ser--Ser--Thr (SEQ. ID. NO: 3) and Ile--Ile--Thr--Tyr--Arg--Lys--Gly--Ser--Ser--Thr (SEQ. ID. NO: 2).

Abstract: A fibrinogen concentrate has a purity of 98% or higher and is free of viral contaminants and proteases. The fibrinogen concentrate is obtained by subjecting a solubilized plasma fraction containing fibrinogen to a viral inactivation chemical treatment using a solvent/detergent, subjecting the resulting viral-inactivated fraction to precipitation in a solution containing an amino acid at an acidic pH to obtain a supernatant, filtering the supernatant to obtain a purified fibrinogen concentrate, and recovering the purified fibrinogen concentrate.

Abstract: Lipodepsipeptides from Pseudomonas syringae pv. syringae were evaluated for antifungal activity. Specifically, the in vitro antifungal and fungicidal activities of three cyclic lipodepsinonapeptides syringomycin E, syringotoxin B, and syringostatin A against medically important isolates were evaluated using a standard broth microdilution susceptibility method. Erythrocyte toxicity was also evaluated. All three compounds showed broad antifungal activity and fungicidal action against most of the fungi tested.In addition, the present invention relates to a novel method for suppressing the immune system of mammals using cyclic lipodepsipeptides. The ability of cyclic lipodepsipeptides to suppress the immune system was evaluated in mitogen-induced lymphocytes. One cyclic lipodepsipeptide, syringomycin-E significantly inhibited mitogen--induced lymphocytes stimulation by pokeweed mitogen, phytohemagglutinin, and monoclonal antibodies to CD3.

Abstract: The present invention provides novel compounds, which comprise an obesity protein analog complexed with a divalent metal cation, pharmaceutical formulations thereof, and methods of using such compounds for treating obesity, and disorders associated with obesity such as diabetes, cardiovascular disease and cancer.

Abstract: Pharmaceutical compositions of matter adapted for intravaginal administration comprise a biologically active polypeptide, an absorption promoter, such as an anionic and/or nonionic surfactant or a nonionic surfactant and an aliphatic carboxylic acid, optionally an animal and/or vegetable protein and a nontoxic pharmaceutically acceptable carrier or diluent therefor, in a formulation suitable for intravaginal administration. Preferred compositions comprise calcitonin as the biologically active polypeptide. Preferred absorption promoters are anionic surfactants, e.g., sodium lauryl sulfate, and the combination absorption promoter of a nonionic surfactant and a medium chain aliphatic carboxylic acid or its salt, e.g. polyoxyethylenealkylphenylether and a medium chain aliphatic carboxylic acid.

Abstract: A method for detecting the performance reduction of an exhaust gas purification catalyst by examining the temperature of an exhaust gas flowing into the catalyst, necessary for the activation of the catalyst. This method enables accurate detection of the performance reduction of an exhaust gas purification catalyst without conducting a constant-speed vehicle operation for a long time.

Abstract: This invention relates generally to cyclic polypeptides comprising a thioether linkage and methods for their preparation. More particularly, this invention relates to halogenated polypeptides having at least one haloalanine-like amino acid, and methods for their preparation which involve converting the hydroxyl group (i.e., --OH) of a serine-like amino acid to a halo group (i.e., --X where X is Cl, Br, or I) with the aid of a phosphorus-based halogenation reagent such as a triphenylphosphine dihalide (i.e., (C.sub.6 H.sub.5).sub.3 PX.sub.2, wherein X is Cl, Br, or I), a triphenylphosphite dihalide (i.e., (C.sub.6 H.sub.5 O).sub.3 PX.sub.2, wherein X is Cl, Br, or I), or a mixture of triphenylphosphine or triphenylphosphite with a halohydrocarbon (i.e., "halo-conversion").

Abstract: This invention provides a method of suppressing the cytotoxic activity of mammalian Natural Killer (NK) cells.The method of this invention comprises administering to an individual in need of treatment a polypeptide comprising the amino acid sequence corresponding to dynorphin A or a dynorphin A analog, including amidated analogs, in an amount sufficient to suppress the cytotoxic activity of NK cells. This invention is particularly useful for those individuals undergoing gene therapy who are to be infected with a viral or viroid vector containing a therapeutic gene. This invention is also useful to aid recipients of transplanted tissue and for individuals suffering from autoimmune diseases.

Abstract: Disclosed are (1) a polypeptide represented by formula (I), or a pharmaceutically acceptable amide, ester or salt thereof:His-Ser-Asp-Gly-Ile-Phe-Thr-Asp-Ser-Tyr-Ser-Arg-Tyr-Arg-Lys-Gln-NH-CHX-CO-A la-Val-Lys-Lys-Tyr-Y SEQ ID NO:13 (I)wherein X is hydrogen atom; or a lower alkyl group which may be substituted with a member selected from the group consisting of hydroxy group, substituted or unsubstituted amino group, carboxyl group, carbamoyl group, and substituted or unsubstituted aromatic group; and Y is one of amino acids or peptides consisting of 1 to 16 amino acid residues counted from the N-terminal side of Leu-Ala-Ala-Val-Leu-Gly-Lys-Arg-Tyr-Lys-Gln-Arg-Val-Lys-Asn-Lys SEQ ID NO:20, and (2) a pharmaceutical composition comprising a polypeptide represented by formula (I), or a pharmaceutically acceptable amide, ester or salt thereof, which has remarkable c-AMP activity and is useful as a nerve activating agent.

Abstract: Streptogramine derivatives of general formula (I) below, wherein the radical R.sub.1 is a methyl or ethyl radical, the radical R.sub.2 is a bromine or chlorine atom, or is an alkenyl radical with 3 to 5 carbon atoms when R.sub.3 and R.sub.4 are methyl, and one of R.sub.3 and R.sub.4 is a hydrogen atom or a methyl radical and the other is a methyl radical are disclosed. The streptogramine derivatives of general formula (I) have particularly useful antibacterial properties, and may be used in combination with a pristinamycin II derivative.

Abstract: Disclosed are peptides and peptide mimetics that bind selectins, including endothelial leukocyte adhesion molecule 1 (ELAM-1). Such peptides and peptide mimetics are useful in methods for blocking adhesion of leukocytes to the selectins for the purpose of inhibiting inflammation as well as in diagnostic methods employing labeled peptides and peptide mimetics that bind selectins for the purpose of determining the site of inflammation in mammals which inflammation is mediated by the presence of one or more selectins.

Abstract: Antide is the decapeptide, N-Ac-D-2-Nal,D-pClPhe, D-3-Pal, Ser,NicLys, D-NicLys, Leu, ILys, Pro, D-Ala,NH.sub.2 which is an antagonist of luteinizing hormone releasing hormone (LHRH). This decapeptide, like others of the present invention, has high antiovulatory activity (AOA) and releases negligible histamine. Antide is scheduled for scale-up, safety testing and evaluation in the experimental primate and in clinical medicine. Numerous other peptides having structures related to Antide were prepared and tested. These peptides had variations primarily in positions 5, 6, 7, and 8. Of these, N-Ac-D-2-Nal, D-pClPhe,D-3-Pal,Ser,PicLys,cis-DPzACAla,Leu,ILys,Pro,D-Ala-NH.sub.2 was one of the most potent and had higher antiovulatory activity than Antide, i.e. 73%/0.25 ug and 100%/0.5 ug vs. 36%/0.5 ug and 100%/1.0 ug. Antide showed significant, (p<0.001) duration of action, when injected at a dose of 10 ug, 44 hours before 50 ng of the agonist, ?D-3-Qal.sup.6 !-LHRH.

Abstract: The subject invention involves anti-inflammatory compounds having the following structure: ##STR1## wherein: a) --X is cyclic alkyl, having from 4 to 15 carbon atoms; branched alkyl, having from 6 to 15 carbon atoms; or aryl having from 6 to 15 carbon atoms;(b) n is an integer from 0 to 2;(c) --V-- is --OC(O)--, --N(Q)C(O)--, --N(Q)C(S)--, --C(O)--, --SO2-- or --P(O)(OH)--;(d) --Q is hydrogen; or straight or branched chain alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 1 to 6 carbon atoms; or --Q and --X are covalently linked forming a cyclic moiety which includes the nitrogen to which --Q is bonded and from 5 to 20 carbon atoms;(e) Z is --O-- or --NH--; when V is --OC(O)--, --Z-- is --NH--;(f) --R1 is a hydrophobic moiety;(g) --R2 is a hydrophobic moiety;(h) --R3 is --(CH2)m--A--NH2 or --(CH2)m--A--B--C(NH2).dbd.