Abstract: The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with a D-configuration hydroxyproline ether or thioether converts bradykinin agonists into bradykinin antagonists. The invention further includes the intermediate compounds and additional modifications at other positions within the novel 7-position modified bradykinin antagonists which increase enzyme resistance, antagonist potency, and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.

Abstract: The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with an isoquinoline derivative which converts bradykinin agonists into bradykinin antagonists. The invention further includes the novel 7-position modified bradykinin antagonists which increase enzyme resistance, antagonist potency, and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected as by insect bites.

Abstract: This invention provides a claycy and sticky substance as a new biomaterial that cannot be found in the current medical field, which is bioresorbable, shows tackiness, plasticity and shape holding ability at a temperature of approximately from 30 to 40° C. and can give unrestricted shapes at body temperature or more by increasing its fluidity. This clayey and sticky substance comprises a copolymer of two or more bioresorbable monomers, preferably any one of copolymers of p-dioxanone with D-lactic acid, L-lactic acid, D,L-lactic acid, trimethylene carbonate and &egr;-caprolactone, or a mixture of two or more of these copolymers. This clayey and sticky or clayey substance is suited for a hemostatic material, an adhesive material for tissues, a prosthetic material for tissue reconstruction use, a carrier of drug delivery system, a plugging material, an accretion-preventing material and a scaffold material for tissue engineering use.

Abstract: The substitution of the L-Pro at the 7-position with D-Phe or D-Tic and substitution of the L-Phe at the 8-position with hydroxyproline ethers and thioethers of the peptide hormone bradykinin and other additional substituted analogs of bradykinin converts bradykinin agonists into bradykinin antagonists. The invention further includes additional modifications at other positions within the novel 7- and 8-position modified bradykinin antagonists, which increase enzyme resistance, antagonist potency, and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected as by insect bites.

Abstract: Peptide derivatives which are antagonists of neurokinin A. The derivatives have a modified peptide bond having a reduced amide and a fluorinated alkyl attached to the nitrogen atom of the modified peptide bond. For example, Asp-Ser-Phe-Val-Gly-Leu&PSgr;[CH2N(CH2CF3)]Leu(NH2).

Abstract: The subject invention involves compounds having the structure: wherein the C.sub..alpha. --N.sub..beta. and C.sub.5 -C.sub.6 bonds are independently single or double bonds, R1 is selected from alkyl, aryl, and heterocycle; R2-R13 are independently selected from hydrogen and other substituents; and pharmaceutically-acceptable salts thereof. The subject invention also involves pharmaceutical compositions containing such compounds, and methods for treating or preventing diseases and disorders using such compounds.

Abstract: A controlled release pharmaceutical composition includes a biocompatible polymeric material, preferably polyethylene-vinyl acetate or poly(lactic-glucolic acid), having incorporated therein a soluble receptor capable of binding to its ligand and thus affecting the ligand's function. The soluble receptor is preferably the soluble form of TNF.alpha. receptor. Such compositions are for use in the treatment of disorders in which neutralization of the deleterious effects of TNF.alpha. is required.

Abstract: Novel pseudopeptide analogs of the insect kinin neuropeptide family which possess biological activity mimicking that of the naturally occurring neuropeptides are disclosed. By substituting a sterically hindered amino acid which is compatible with a turn conformation, for the Xaa.sup.2 amino acid of the insect kinin C-terminal pentapeptide (i.e. Ser, Pro, or Ala), analogs are produced which exhibit resistance to degradation by angiotensin converting enzyme (ACE) while still retaining biological activity. The analogs may be used for insect control by disrupting the diuretic and/or myotropic activity in insects.

Abstract: Peptides of the formula IA-B-C-E-F-K-P-G-M-F'-I (I),wherein the terms A, B, C, E, F, K, P, G, M, F', and I are defined in the specification, have bradykinin antagonist action. Their therapeutic utility includes all pathological states which are mediated, caused or supported by bradykinin and bradykinin-related peptides.

Abstract: The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with a D-configuration hydroxyproline ether or thioether converts bradykinin agonists into bradykinin antagonists. The invention further includes the intermediate compounds and additional modifications at other positions within the novel 7-position modified bradykinin antagonists which increase enzyme resistance, antagonist potency, and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.

Abstract: A bradykinin analog which contains nine or ten amino acid residues and at least one [CH.sub.2 NH] pseudopeptide bond, the analog being useful as an antagonist or agonist of the naturally occuring bradykinin.

Abstract: The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with an aliphatic, cyclic or aromatic amino acid of the D-configuration converts bradykinin agonists into a bradykinin antagonist. The invention further includes additional modifications at other positions within the novel 7-position modified bradykinin antagonists including C-terminal and N-terminal extensions and replacement of arginine in the one and nine positions which increase enzyme resistance, antagonist potency and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of the mannal and human body in which an excess of bradykinin or related kinins are produced or injected as by bites into the body.