Abstract: The present invention relates to benzoxazinones of formula I: ##STR1## or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as an assay standard or reagent, and intermediates and processes for making the same.

Abstract: The present invention relates to benzoxazepinones of formula I: ##STR1## or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same and methods of using the same for treating viral infection or as an assay standard or reagent.

Abstract: Provided is a pharmaceutical composition comprising a tablet or capsule containing a pharmacologically effective amount of a pharmaceutical compound, or a pharmaceutically acceptable salt thereof, having an amidine-based group and an optional ester group, a pharmaceutically acceptable solid carrier, and a pharmaceutically acceptable acid in an amount to modify the pH of the composition to substantially that of the compound at pH of maximum stability.Such a composition is prepared by adding water during formulation manufacture and contacting the compound during formulation manufacture with a pharmaceutically acceptable acid having a pH in a saturated aqueous solution substantially that of the compound at pH of maximum stability.

Abstract: The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinthiones of formula I: ##STR1## or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.

Abstract: This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

Abstract: The present invention provides novel compounds, compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsy, irritable bowel syndrome, immune suppression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: ##STR1## wherein R.sup.1, R.sup.3, R.sup.4, R.sup.5, Z, Y, V, X, X', J, K, L, and M are as defined herein.

Abstract: The present invention relates to processes for the production of .alpha.-aryl-.beta.-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.

Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: ##STR1## and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.

Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric and neurological disorders are disclosed.

Abstract: The invention relates to a method of treating alcoholism and alcohol dependence in a mammal comprising administering to the mammal a therapeutically effective amount of a synergistic combination of: (i) at least one opioid antagonist, and (ii) at least one selective serotonin reuptake inhibitor. The invention also relates to compositions and kits containing the same.

Abstract: This invention relates to electrophilic dipeptide analogs conjugated to an N,N-disubstituted .alpha.-amino acid as inhibitors of trypsin-like serine protease enzymes.

Abstract: The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is a reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-ben zoxazin-2-one which is a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

Abstract: An apparatus for holding liquid, such as a microtiter plate, in which a plurality of wells are formed. Each of the wells have side walls that intersect in an edge that defines the boundary between adjacent wells. The edge boundary prevents liquid from collecting between the wells, thereby causing all of the liquid applied to the plate to enter one of the wells. The microtiter plate can be formed from a material having a reflectance and/or fluorescence that is optimized for the particular application in which the microtiter plate will be used. Microtiter plates for use in fluorescence measurement applications are made from material having low fluorescence, such as a liquid crystal polymer, while microtiter plates for use in luminescence measurements are made from material having a high reflectance. Microtiter plates for spectrophotometric applications are made with wells having clear bottoms and opaque walls.

Abstract: This invention provides novel radiopharmaceuticals that are radiolabeled cyclic compounds containing carbocyclic or heterocyclic ring systems which act as antagonists of the platelet glycoprotein IIb/IIIa complex; to methods of using said radiopharmaceuticals as imaging agents for the diagnosis of arterial and venous thrombi; to novel reagents for the preparation of said radiopharmaceuticals; and to kits comprising said reagents.

Abstract: The present invention relates generally to a novel method for preparation of substituted isoxazolin-5-yl acetic acid in high optical purity from a stereoisomeric mixture of an esterified substituted isoxazolin-5-yl acetate. The products are useful in the synthesis of compounds for pharmaceuticals, especially the treatment of thrombolytic disorders, and agricultural products.

Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(.dbd.NH)NH.sub.2, which are useful as inhibitors of factor Xa.

Abstract: The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.

Abstract: The present invention describes a method for the preparation of asymmetric N,N'-disubstituted cyclic ureas through the selective monodebenzylation of symmetric N,N'-disubstituted cyclic ureas using a dissolving metal reduction. The intermediates can be alkylated to give compounds which are useful as HIV protease inhibitors for the treatment of HIV infection.

Abstract: The present invention describes indazoles of cyclic ureas of formula I: ##STR1## wherein X is a linker group and Y may be acyclic or cyclic, which are useful as inhibitors of HIV protease, and pharmaceutical compositions and diagnostic kits comprising the same.