Abstract: The present invention provides a novel process for making compounds of formula 2a or 2b or pharmaceutically acceptable salts thereof, ##STR1## wherein R.sub.1 is selected from the group consisting of phenyl and phenyl substituted with at least one group selected from NO.sub.2 and halogen;R.sub.2 is H;R.sub.3 is selected from the group consisting of C.sub.1-4 alkyl, phenyl, and benzyl; and,R.sub.4 is selected from the group consisting of H and halogen;which comprises the steps of:a) oxidizing a racemate of formula 2 or a salt thereof to form a dehydro-compound of formula 3, ##STR2## wherein R.sub.5 is selected from the group consisting of H, CH.sub.3, benzyl, C.sub.2-8 acyl Na, Li and K; and,b) asymmetrically hydrogenating a compound of formula 3 in the presence of a chiral phosphine catalyst to form a compound of formula 2a or 2b.

Abstract: This invention provides processes for the synthesis of platelet glycoprotein IIb/IIIa inhibitors and intermediate compounds useful in said processes.

Abstract: The present invention relates to substituted cyclic ureas and analogs thereof of formula (I): ##STR1## wherein, T is selected from: --N(R.sup.22)C(.dbd.Z)N(R.sup.23)--; --N(R.sup.22)C(.dbd.Z)C(.dbd.Z)N(R.sup.23)--; --N(R.sup.22)S(.dbd.Z')N(R.sup.23)--; --N(R.sup.22)S(.dbd.Z').sub.2 N(R.sup.23)--; or --N(R.sup.22)P(.dbd.O)(R.sup.24a)N(R.sup.23)--;Z is O, S, NR.sup.24 ; and,Z' is O or NR.sup.24 ;or pharmaceutically acceptable salt forms or prodrugs thereof, which are useful as retroviral protease inhibitors, and to pharmaceutical compositions comprising such compounds and methods of using the same for treating viral infection.

Abstract: This invention provides novel reagents for the preparation of radiopharmaceuticals useful as imaging agents for the diagnosis of cardiovascular disorders, infection, inflammation and cancer, diagnostic kits comprising said reagents and intermediate compounds useful for the preparation of said reagents. The reagents are comprised of stable hydrazone modified biologically active molecules that react with gamma emitting radioisotopes to form radiopharmaceuticals that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy.

Abstract: This invention provides novel radiopharmaceuticals which are useful as imaging agents for the diagnosis of cardiovascular disorders, infectious disease and cancer. The radiopharmaceuticals are comprised of phosphine or arsine ligated technetium-99m labeled hydrazino or diazino modified biologically active molecules that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy. This invention also provides methods for using the radiopharmaceuticals and kits comprising radiopharmaceutical precursors. The radiopharmaceuticals of this invention have the structure:?(Q).sub.d' L.sub.n --C.sub.h' !.sub.x --M.sub.t (A.sub.L1).sub.y (A.sub.L2).sub.z ;wherein the variables are as defined herein.

Abstract: Compounds of Formula I have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man, such as in Alzheimer's disease and other conditions involving learning and cognition, where subnormal levels of this neurochemical are found.The compounds of this invention can be described as shown in Formula I ##STR1## where Q is ##STR2## R.sup.1 is 4-, 3-, or 2-pyridyl, pyrimidyl, pyrazinyl, or fluoro-4-pyridyl;R.sup.2 and R.sup.3 are independently H, F, Cl, Br, NO.sub.2, OH, --R.sup.4, --O--R.sup.4, --CO.sub.2 R.sup.4, --COR.sup.4, --CONH.sub.2, --CONHR.sup.4, --CONR.sub.4 R.sup.4', --S(O).sub.m2 --R.sup.4, NH.sub.2, CF.sub.3, NHR.sup.4, NR.sup.4 R.sup.4' ;R.sup.4 and R.sup.4' are independently H, alkyl of 1 to 4 carbons, CH.sub.2 Phe-W or Phe-W;Phe is a phenyl group;R.sup.5 is --(CH.sub.2).sub.n --Y or --OCOR.sup.4 ;Y is H, OH, NH.sub.2, NHR.sup.4, NR.sup.4 R.sup.4', NHCOR.sup.4, NHCO.sub.2 R.sup.4, NHS(O).sub.2 R.sup.4 ; F, Cl, Br, OR.sup.

Abstract: This invention relates to (2-quinoxalinyloxy)phenoxypropanoic acids, related derivatives thereof, enantiomeric and diastereomeric forms thereof, mixtures of enantiomeric diastereomeric forms thereof, and pharmaceutically acceptable salt forms thereof, pharmaceutical compositions containing them, processes for their preparation, and methods of using them to treat cancer, particularly solid tumors, in mammals.

Abstract: Tris(isonitrile) copper(I) sulfate complexes and their use in synthetic methods for making radionuclide isonitrile coordination complexes such as ?.sup.99m Tc(1-isocyano-2-methoxy-2-methylpropane).sub.6 !.sup.+. The coordination complexes are useful as radiopharmaceutical imaging agents.

Abstract: This invention relates to compounds and methods for use in determining renal function by means of scintigraphic urography. More specifically, this invention relates to radionuclide complexes of ester-substituted diaminethiols, radiopharmaceutical compositions comprising said complexes, kits for the preparation of said compositions, and a method of using said compositions for examining renal function. Compounds of this invention have the formula: ##STR1## wherein the various groups are as defined herein.

Abstract: The present invention provides a novel process for making compounds of formula 2a or 2b or pharmaceutically acceptable salts thereof, ##STR1## wherein R1 is selected from the group consisting of phenyl and phenyl substituted with at least one group selected from NO.sub.2 and halogen;R.sub.2 is H;R.sub.3 is selected from the group consisting of C.sub.1-4 alkyl, phenyl, and benzyl; and,R.sub.4 is selected from the group consisting of H and halogen;which comprises the steps of:a) oxidizing a racemate of formula 2 or a salt thereof to form a dehydro-compound of formula 3, ##STR2## wherein R.sub.5 is selected from the group consisting of H, CH.sub.3, benzyl, C.sub.2-8 acyl Na, Li and K; and,b) asymmetrically hydrogenating a compound of formula 3 in the presence of a chiral phosphine catalyst to form a compound of formula 2a or 2b.

Abstract: This invention relates to a method of treating human immunodeficiency virus (HIV) infection in a mammal comprising administering to the mammal a therapeutically effective amount of a combination of: (i) at least one cyclic HIV protease inhibitor and (ii) at least one HIV reverse transcriptase inhibitor.

Abstract: The present invention provides methods of testing the cardiotoxicity of compounds and kits useful for the same.

Abstract: Compounds of Formula I have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful as chemical intermediates and as pharmacological agents in the treatment of diseases of man, such as in Alzheimer's Disease and other conditions involving learning and cognition, where subnormal levels of this neurochemical are found.

Abstract: Compounds of Formula (I) have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man where subnormal levels of this neurochemical are found, such as in Alzheimer's disease, and other conditions involving learning and cognition.

Abstract: Anticancer compounds of formula I: ##STR1## and pharmaceutically acceptable salts thereof, wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.9 and R.sup.10 are independently selected from the group H, C.sub.1 -C.sub.4 alkyl, OR.sup.4, N(R.sup.4).sub.2, NO.sub.2, CN, F, Cl, Br, I, Ph, and CF.sub.3, and NHC(O)R.sup.4 ;R.sup.4 is independently selected from the group H, C.sub.1 -C.sub.4 alkyl, Ph, and CH.sub.2 Ph;X.sup.1 and Y.sup.1, and X.sup.2 and Y.sup.2 when present, join together to form:a benzene ring substituted with 1-4 R.sup.3 ;a five membered heterocycle having 1-2N, NH, O or S atoms and substituted with 1-2 R.sup.3 ;a six membered heterocycle having 1-2N and substituted with 1-2 R.sup.3 ; orthe group: ##STR2## wherein one of W or Z is C.dbd.O and the other is C.dbd.O, NH, S or O; or when X.sup.2 and Y.sup.2 are present and not joined together and when R.sup.2 is in the 4-position, then X.sup.2 and R.sup.2 may join together to form an ethylene bridge;are addressed.