Abstract: Peptides of the formulaAc-D-Nal(2)-D-Phe-D-Phe-Ser-X-D-Ser(Rha)-Leu-Arg-Pro-Yin which X represents Tyr or His and Y represents Gly-NH.sub.2, D-Ala-NH.sub.2, Azgly-NH.sub.2 or NH--C.sub.2 H.sub.5 are competitive antagonists of Gn-RH. They are used for the treatment of gonadotropin- and steroid-dependent diseases and are prepared by known methods of peptide chemistry.

Abstract: Disclosed herein are peptides of the formulaY--R.sup.1 --R.sup.2 --R.sup.3 --R.sup.4 --R.sup.5 --R.sup.6 --Zwherein R.sup.1 to R.sup.5 are designated amino acid residues; R.sup.6 is Phe, homoPhe or an amino acid residue derived from 2-amino-3-cyclohexylpropionic acid, 2-amino-3-(4-(lower alkoxy)phenyl) propionic acid or 2-amino-3-(4-halophenyl)propionic acid; Y is Phe, desamino-Phe, (lower alkanoyl)-Phe, p-haloPhe, Tyr, desamino-Tyr or (lower alkanoyl)-Tyr, or Y is the decapeptide radical W--Val--R.sup.7 --Ser--R.sup.8 --R.sup.9 --Thr--Glu--R.sup.10 --Ser--Phe wherein W is hydrogen or lower alkanoyl and R.sup.7 to R.sup.10 are designated amino acids residues, or Y is a fragment of the decapeptide radical wherein from one to nine of the amino acid residues (i.e. Val to Ser) may be deleted serially from the amino terminus of the decapeptide radical; and Z is hydroxy, amino, lower alkylamino or di(lower alkyl)amino.

Abstract: Esters or amides of a peptide, preferebly a dipeptide, consisting essentially of natural or synthetic L-amino acids with hydrophobic side chains were found to have specific cellular toxicities. Preferable amino acids of the peptide are leucine, phenylalanine valine, isoleucine, alanine, proline, glycine or aspartic acid beta methyl ester. Preferable dipeptides are L leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-Leucyl L-isoleucine, L-henylalanyl L-phenylalanine, L-valyl L-leucine, L-leucyl L-alanine, L-valyl L-valine, L-phenylalanyl L leucine, L prolyl L-leucine, L-leucyl L-valine, L-phenylalanyl L-valine, L glycyl L-leucine, L-leucyl L-glycine, glycyl L-phenylalanine and L-aspartyl beta methyl ester L-phenylalanine. Most preferable dipeptides are L-leucyl L-leucine, L-leucyl L-phenylalanine, L-valyl L-phenylalanine, L-phenylalanyl L-leucine, L-leucyl L-isoleucine L-phenylalanyl L-phenylalanine and L-valyl L-leucine.

Abstract: The invention relates to a process for the preparation of compounds of the formula I ##STR1## in which n is 1 or 2, R denotes hydrogen or an organic radical, R.sup.1 denotes an organic radical, R.sup.2 and R.sup.3 are identical or different and denote hydrogen or an organic radical, and R.sup.4 and R.sup.5, together with the atoms bearing them, form a monocyclic, bicyclic or tricyclic heterocyclic ring system having 5 to 15 carbon atoms, which process comprises reacting compounds of the formula II defined in the description with compounds of the formula IV defined in the description, in the presence of phosphinic anhydrides of the formula III, where appropriate eliminating radicals which have been introduced to protect other functional groups and, where appropriate, esterifying free carboxyl groups in a manner known per se.

Abstract: Biodegradable polyamides, useful as absorbable sutures and as controlled release binder materials, are prepared by condensing 4,4'-spirobibutyrolactone with a primary diamine, optionally in the presence of a nylon salt, leading to homopolymers containing lactam structural units, or to random copolymers.

Abstract: This invention relates to a novel polypeptide represented by the formula: ##STR1## (wherein Lys represents lysine, Trp tryptophan, Cys cystine, Phe phenylalanine, Arg arginine, Val valine, Tyr tyrosine, Gly glycine, Ile isoleucine and X a hydroxyl group or an amino group), its analogue and a method for preparing the same.The polypeptide exhibits strong affinity for lipolysaccharide, and is useful for removing endotoxin and as a therapeutic agent of bacterial infections.

Abstract: A treatment to alleviate the debilitating symptoms of motility disorders including the functional bowel diseases. Treatment of patients with analogs of GnRH significantly reduces or elmininates the symptoms of motility disorders, including bowel disease.

Abstract: The invention relates to a polypeptide of formula I:R.sup.1 -A.sup.1 -A.sup.2 -A.sup.3 -A.sup.3 -A.sup.4 -A.sup.5 -A.sup.6 -A.sup.7 -A.sup.9 -Qwherein each of the generic terms is disclosed in full in the specification and includes: R.sup.1 is (2-6C)alkanoyl or (1-4C)alkoxycarbonyl; A.sup.1 is a direct link to A.sup.2, or is Gly or Arg; A.sup.2 is a direct link to A.sup.3, or is Gly or Pro; A.sup.3 is a direct link to A.sup.4, or is Lys or Lys(Z); A.sup.4 is His or D-His; A.sup.5 is Trp or MeTrp; A.sup.6 is Ala or MeAla; A.sup.7 is Val or MeVal; A.sup.8 is Gly or Sar; A.sup.9 is His or MeHis; and Q is a group of the formula -A.sup.10.R.sup.2 in which A.sup.10 is Leu or D-Leu and R.sup.2 is hydroxy, amino, (1-3C)alkylamino or (1-3C)alkoxy; or Q is (1-6C)alkoxy or (1-10C)alkylamino; provided that when R.sup.1 is acetyl and -A.sup.4 -A.sup.5 -A.sup.6 -A.sup.7 -A.sup.8 -A.sup.9 -Q is -His-Trp-Ala-Val-Gly-His-Leu-NH.sub.2 then -A.sup.1 -A.sup.2 -A.sup.3 - is not a direct link to His.

Abstract: Targeting substance-diagnostic/therapeutic agent conjugates joined by stabilized Schiff base or hydrazone linkages are disclosed. In addition, slow release carrier-drug pharmaceuticals are described. The diagnostic and therapeutic conjugates and pharmaceuticals of the present invention provide certain advantages relating to in vivo administration, including controlled release of the active agent at a target site.

Abstract: A substrate comprises a porous polymeric material having a porosity of at least 75% and comprising pores having a diameter within the range 1 to 100 .mu.m and being interconnected by a plurality of holes, and a gel or material adapted in use to form a gel which gel or pre-gel materials is contained and retained within the pores of the polymeric material and is adapted in use to interact with a reactive species and can be made by depositing and retaining the gel or a material adapted in use to form the gel within the pores of the porous polymeric material. The high porosity of the porous polymeric material in combination with the retention of the gel within the pores permit high loading capacities, particularly in the area of peptide synthesis to be achieved. The substrate can be employed in chemical synthesis, chromatography techniques, ion exchange and separation techniques.

Abstract: Disclosed are DC115A compounds represented by the following general formula: ##STR1## wherein R represents ethyl, propyl or 1-propenyl, and which have antibacterial and anti-tumor activity. DC115A compounds are produced by culturing a microorganism belonging to the genus Streptomyces.

Abstract: A peptide optionally in isosteric form wherein a methylene group in the backbone chain is disubstituted, one or both substituents being fluorine and/or chlorine, in free form or in pharmaceutically acceptable salt form, such as a compound of formula I ##STR1## wherein the substituents have various significances, or an isosteric form thereof,is useful as an enzyme inhibitor. In particular, as a renin inhibitor, it is useful in the prophylaxis or treatment of hypertension and congestive heart failure.It is prepared by a process comprising the step of coupling two corresponding peptide residues optionally in isosteric form, or precursors thereof, and if required appropriately converting any resultant compound in precursor form.

Abstract: A mono-layer liquid phase type water-based insecticidal aerosol comprises a base liquid for aerosol containing at least one specific pyrethroidal compound, a specific organic solvent and a specific buffer solution, which base liquid has a pH of from 7.0 to 11.0, and dimethyl ether as a propellant. The aerosol according to the present invention has a long-term storage stability as well as an excellent insecticidal activity and causes no degradation of the container.

Abstract: Peptides which inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. These peptides may be used to treat steroid-dependent tumors, such as prostatic and mammary tumors. The peptides include cyclic, bicyclic and tricyclic analogs of the decapeptide GnRH, and preferably there are at least two covalent bonds between the residues in the 4- and 10-positions, the residues in the 5- and 8-positions and the residues in the 1- and 3-positions, respectively. Examples of such bonds include a disulfide linkage between Cys residues, an amide linkage between a side chain amino group and a side chain carboyxl group, a dicarba linkage between side-chain alkyl groups, and a carba linkage between a side-chain alkyl group and a side-chain sulfhydryl group.

Abstract: The oject of this invention are de-mannosylated teicoplanin derivatives which can be obtained in good yield by microbiological transformation with cultures of Nocardia orientalis NRRL 2450 or Streptomyces candiodus NRRL 3218.

Abstract: A combination therapy for treatment of selected sex steroid dependent cancers in susceptible warm-blooded animals comprising administering to such animals whose hormone output of their testes or ovaries, respectively, is blocked a therapeutically effective amount of an antiandrogen and/or an antiestrogen and/or at least one inhibitor of sex steroid biosynthesis or pharmaceutical compositions thereof wherein the selected sex steroid dependent cancer are, for example, testicular cancer, ovarian cancer, renal cancer or uterine cancer is disclosed.

Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism and diseases caused by retroviruses including HTLV-I and -III. Processes for preparing the peptides, novel intermediates useful in the preparation thereof, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, congestive heart failure, or hyperaldosteronism.

Abstract: The invention relates to the use of .kappa.-caseinoglycopeptide or CGP, in particular from cow's ewe's, goat's or human milk, for the manufacture of a composition, in particular a medicament, for the prevention and/or the treatment of thrombi.A medicament of this kind can advantageously be presented in lyophilised form intended for injection, after being dissolved in a compatible solvent, or in the form of nanoparticles enclosed in capsules.Application to the prevention and the treatment of thrombi.

Abstract: A renin inhibiting compound having an aminodiol functional group is useful for treating hypertension, congestive heart failure and glaucoma and inhibits retroviral protease.

Abstract: Methods and compositions for the treatment of non-IgE-mediated inflammatory disease conditions utilizing the peptide Asp-Ser-Asp-Pro-Arg, or derivative thereof are disclosed.