Abstract: Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. In one embodiment, the compounds and compositions are thiazoles and thiadiazoles that inhibit the activity of protein tyrosine phosphatase 1B.

Abstract: Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. In one embodiment, the compounds and compositions are thiazoles and thiadiazoles that inhibit the activity of protein tyrosine phosphatase 1B.

Abstract: A system for analyzing a vast amount of data representative of chemical structure and activity information and concisely providing conclusions about structure-to-activity relationships. A computer may adaptively learn new substructure descriptors based on its analysis of the input data. The computer may then apply each substructure descriptor as a filter to establish new groups of molecules that match the descriptor. From each new group of molecules, the computer may in turn generate one or more additional new groups of molecules. A result of the analysis in an exemplary arrangement is a tree structure that reflects pharmacophoric information and efficiently establishes through lineage what effect on activity various chemical substructures are likely to have. The tree structure can then be applied as a multi-domain classifier, to help a chemist classify test compounds into structural subclasses.

Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

Abstract: Relatively small cyclic peptides that mimic the biological and/or chemical activity of larger cyclic peptide such as somatostatin, as well as synthetic methods therefor. In certain embodiments, cyclic peptides of the invention have structure: ##STR1## wherein R.sub.NP1 is H, an amine protecting group, or a solid support and R.sub.NP2 is H or an amine protecting group.

Abstract: The present invention discloses peptide aldehydes having a lactam group as part of the peptide backbone and having an original mimic group such as an amidinopiperidine or amidinophengyl tail. These compounds are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

Abstract: Relatively small cyclic peptides that mimic the biological and/or chemical activity of larger cyclic peptide such as somatostatin, as well as synthetic methods therefor. In certain embodiments, cyclic peptides of the invention have structure: ##STR1## wherein R.sub.NP1 is H, an amine protecting group, or a solid support and R.sub.NP2 is H or an amine protecting group.

Abstract: This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The compounds and their pharmaceutical compositions are useful for preventing thrombosis in mammals which are suspected of having a condition characterized by abnormal thrombosis.

Abstract: Peptides having the general sequence A-B-C-D-E-F-Z wherein A is Ala, B is pFPhe, C is, for example, Arg, D is Cha, E is, for example, hArg, F is, for example, Tyr, and Z is, for example NH.sub.2. The peptides are useful for promoting wound healing and arresting bleeding in a patient.

Abstract: 4-substituted cyclohexylamine derivatives which are thrombin catalytic site inhibitors and which are useful as anticoagulants. These compounds show selectivity for thrombin over other trypsin-like enzymes and have oral bioavailability.

Abstract: This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The compounds and their pharmaceutical compositions are useful for preventing thrombosis in mammals which are suspected of having a condition characterized by abnormal thrombosis.

Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease slates in mammals characterized by abnormal thrombosis.

Abstract: The radioligands are six amino acid peptides having iodinated tyrosine at amino acid position six, including Ala-pFPhe-hArg-Cha-hArg-Tyr(I)-NH.sub.2, which mimic the activated form of the thrombin receptor protein. Thrombin receptor radioligands of the present invention are useful for screening for thrombin receptor antagonists.

Abstract: A fibrinogen receptor antagonist of the formulaAc-Cys-Asn-Pro-(L-AMF)-Gly-Asp-Cys-OHorAc-Cys-Asn-(DiMeTzl)-(L-AMF)-Gly-Asp-Cys-OH.

Abstract: The present invention comprises fibrinogen receptor antagonist compounds, compositions containing them and methods for using them to inhibit fibrinogen binding to blood platelets. Compounds of the invention have the following formula ##STR1## wherein Z is ##STR2## X is COOH, CH.sub.2 SH or SH; R.sup.1 is Y--R.sup.3, wherein R.sup.3 is alkyl and Y is amino, pyridinyl, pyrimidinyl or piperidinyl;R.sup.2 is H, alkyl, aryl, or arylalkyl; andR.sup.4 is alkyl, heteroalkyl, aryl or heteroaryl, wherein the aryl or heteroaryl group can be mono- or bi-cyclic.

Abstract: A fibrinogen receptor antagonist of the formula ##STR1## wherein XX represents a synthetic alpha-amino acid containing a linear side chain and ZZ represents a sequence of 1, 2, 3 or 4 amino acids.

Abstract: Atrial natriuretic factor analogs containing N-alkylated amino acids and showing enhanced potency and increased metabolic stability. These analogs have natriuretic, diuretic and vasorelaxant activity, making them suitable for treating congestive heart failure and renal hypertension.

Abstract: The present invention relates to the use of peptide analogues as inhibitors of their respective naturally occurring peptides. The structure of the peptide analogues is exemplified by an internal region of the N-terminus of humoral hypercalcemic factor hHCF, and truncations thereof: hHCF(14-34)NH.sub.2, hHCF(13-34)NH.sub.2, hHCF(12-34)NH.sub.2, hHCF(11-23)NH.sub.2, hHCF(10-34)NH.sub.2, hHCF(9-34)NH.sub.2, hHCF(8-34)NH.sub.2 and various amino acid substitutions.