Abstract: CRF receptor antagonists are disclosed. Such receptor antagonists are thiadiazole-, pyrimidine-, triazine-, and triazole-containing compounds substituted with both a C3-C14 monocyclic or fused, homoaryl or heteroaryl group and a substituted amine group. The CFR receptor antagonists have utility in the treatment of a variety of disorders, including disorders associated with the hypersecretion of CRF.

Abstract: Novel compounds having activity against trypsin are disclosed. Specifically, novel peptide aldehyde analogues that have substantial potency and specificity as inhibitors of mammalian pancreatic trypsin are presented. The compounds are useful in the prevention and treatment of the tissue damage or destruction associated with pancreatitis.

Abstract: a-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions, diagnostic compositions and pharmaceutical compositions, which are useful for preventing or treating in a mammal a pathological condition characterized by thrombosis are described.a-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions and diagnostic compositions, which are useful for in vivo imaging of thrombi in a mammal are also described.Methods of preventing or treating in a mammal a pathological condition characterized by thrombosis and methods of in vivo imaging of thrombi in a mammal are also disclosed.

Abstract: .alpha.-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions, diagnostic compositions and pharmaceutical compositions, which are useful for preventing or treating in a mammal a pathological condition characterized by thrombosis are described..alpha.-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions and diagnostic compositions, which are useful for in vivo imaging of thrombi in a mammal are also described.Methods of preventing or treating in a mammal a pathological condition characterized by thrombosis and methods of in vivo imaging of thrombi in a mammal are also disclosed.

Abstract: The present invention is directed to N-sulfonyl arginine alpha-keto-amide derivatives, their pharmaceutically acceptable salts and compositions thereof which are useful as antithrombotic agents in mammals and also the use of these compounds as antithrombotic agents. Also, disclosed are methods of using these inhibitors in their various embodiments as therapeutic agents for disease states characterized by disorders of the blood coagulation process. Further disclosed are compounds useful as intermediates in the preparation of these compounds.

Abstract: Novel compounds having activity against trypsin are disclosed. Specifically, novel peptide aldehyde analogues that have substantial potency and specificity as inhibitors of mammalian pancreatic trypsin are presented. The compounds are useful in the prevention and treatment of the tissue damage or destruction associated with pancreatitis.

Abstract: This invention provides solution-phase methods for the synthesis of peptidyl argininals and to novel reagents useful therein.

Abstract: This invention relates to peptide aldehyde analogs that inhibit the thrombin or Factor Xa. The compounds are thought useful for preventing or treating conditions in mammal characterized by abnormal thrombosis.

Abstract: Asp-Pro-Arg alpha-keto-amide derivatives, and their pharmaceutically acceptable salts and compositions, for use as antithrombotic agents in mammals are disclosed. The method of use of these inhibitor compounds for treatment or prevention of conditions of abnormal thrombus formation in mammals is also disclosed. Further disclosed are alpha-hydroxy amide compounds used as intermediates in the preparation of the keto-amide compounds.

Abstract: Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.

Abstract: Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.

Abstract: A chimeric amino acid analogue is provided suitable for incorporating into peptides which compound is represented by Formula 1: ##STR1## where P.sub.1 is preferably an amine protecting agent, and P.sub.2 and P.sub.3 are preferably amine or guanidine protecting agents. X can be OH, halide, or preferably an activating group suitable for conjugating the compound of Formula 1 to a peptide by conventional means, and m and n are 0-1 and 0-2 respectively.Peptides containing the chimeric amino acid analog are provided and include a platelet-aggregation inhibitor represented byAaa.sub.1 -CPdl-Gly-Asp-Aaa.sub.2where Aaa.sub.1 is Gly or H, Cpdl is the compound of Formula 1 which has been deprotected and Aaa.sub.2 is a hydrophobic amino acid preferably Val.

Abstract: This invention relates to a support for oligonucleotide synthesis and more particularly to a necleoside-linker/polymer support composite having the general formulaP'--S'wherein P' is a polymer support which bears oxirane, aziridine or episulfide groups or which contains good leaving groups for nucleophilic displacement; and S' is a nucleoside-linker having the general formulaW--(CH.sub.2).sub.a --X--(CH.sub.2).sub.b --Y--(CH.sub.2).sub.c --Zwherein W and Z each independently comprise a nucleophile; X and Y which, independently may or may not be present, comprise groups of high hydrophilicity; and a, b, c are integers from 0 to 9, wherein a plus b plus c exceeds 6.