Abstract: A compound of formula: 1

Abstract: This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel aryl-substituted pyrimidine compounds of Formula I: 1

Abstract: This invention relates aryl substituted thiazolidinones of Formula I: 1

Abstract: Novel compounds with as few as three natural amino acids that incorporate a substituted 4-keto-1,3,8-triazaspiro[4.5]decan-3-alkanoyl bridge in place of selected fragments of peptidic bradykinin receptor antagonists are pseudopeptides with potent bradykinin receptor antagonist actions. These pseudopeptides and their pharmaceutical compositions are of benefit in treating conditions and diseases of mammals, including humans, in which an excess of bradykinin or a related kinin is produced endogenously or is received exogenously, for example via insect bite.

Abstract: Pseudopeptide compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. All or a portion of the amino acids at postions 2 through 5 of the bradykinin sequence are replaced by 2-pyrrolidinyl and/or amino-alkanoic acid or related olefinic derivatives to reduce the peptidic nature of the compounds.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: Cyclic compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. Amino acid substitutions are made at postions 2 and 5 or 6 to facilitate the cyclization of the peptide through covalent bonding of the amino acid side chains.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: Pseudopeptide compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. Amino acids at at positions 2 through 5 are replaced by olefinic aminoalkenoyl groups to reduce the peptide nature of the compounds.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 invention relates to peptides of up to 10 amino acids that are synthesized by substituting at least one of the bradykinin amino acids found in positions 2, 3, 4 and 5 of the bradykinin peptide with a fatty acid amine. The modified bradykinin peptides produced confer increased resistance to enzymatic degradation and/or tissue specificity. The invention also relates to pharmaceutical preparations and processes of treatments using the modified bradykinin peptides.

Abstract: Pseudopeptide compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. Amino acids at postions 2 through 5 are replaced by olefinic aminoalkenoyl groups to reduce the peptidic nature of the compounds.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 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 present invention relates to a method of producing corticotropin-releasing factor (CRF) antagonist activity and thus provides a method of treating a wide range of stress-related disorders, including affective illnesses, such as depression and anxiety, as well as irritable bowel syndrome, anorexia nervosa, cardiovascular abnormalities and stress-induced immune suppression. The invention also relates to compounds (4-substituted thio-5-oxo-3-pyrazolines) and to pharmaceutical compositions suitable for use in such a method.

Abstract: The invention pertains to a method and pharmaceutical compositions for treating, preventing or reducing neurodegeneration associated with chronic central nervous system or hypoxic, ischemic and hypoglycemic injury to the central nervous system and for the treatment of anxiety through the use of 2-amino-.omega.-phosphonoalkanoic acids having a cycloalkyl group bridging adjacent carbons on the alkyl chain, their pharmaceutically acceptable salts and derivatives as neuroprotectants and anxiolytics.

Abstract: The invention pertains to novel, potent anticonvulsants, analgesics, cognition enhancers and neuroprotectants achieving their action through the antagonism of specific excitatory amino acid neurotransmitter receptors. In particular, the invention is directed to .omega.-[2-(phosphonoalkylenyl)-cycloalkyl]-2-aminoalkanoic acids having general formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl (C.sub.1 to C.sub.6), alkyl (C.sub.7 to C.sub.12), fatty acid chain (C.sub.13 to C.sub.24), aryl, aralkyl, hydroxyl; the stereoisomers being in their resolved or racemic form; n and m=0,1,2 or 3; z=0,1 or 2; the cycloalkyl ring being replaced with the cycloalkenyl ring; and the pharmaceutically acceptable salts and derivatives thereof.