Abstract: The present invention provides novel 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 palsey, irritable bowl syndrome, immune supression, 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: wherein R1, R3, R5, Q, Z, Y, V, X and X′ are as defined herein.

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 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: 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 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: 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.

Abstract: There are provided nitrogen-containing bicyclic compounds, pharmaceutical compositions containing these compounds and methods of using these compounds to treat physiological or drug-induced psychosis or diskinesia in a mammal.

Abstract: This invention relates to novel compounds and derivatives thereof containing a trioxepane protected diol in addition to a hydrazone, hydrazine, amine, or cyclic urea moiety; methods for the preparation of said compounds; and the use of said compounds in processes to prepare human immunodeficiency virus (HIV) protease inhibitors which effectively inhibit HIV. The novel compounds provided by this invention have the formulae: ##STR1## wherein the substituents are as defined herein.

Abstract: Cognitive defeciencies or neurological dysfunction in mammals are treated with .alpha.,.alpha.-disubstituted aromatic or heteroaromatic compounds. The compounds have the formula: ##STR1## or a salt thereof wherein X and Y are taken together to form a saturated or unsaturated carbocyclic or heterocyclic first ring and the shown carbon in said ring is .alpha. to at least one additional aromatic ring or heteroaromatic ring fused to the first ring;one of Het.sup.1 or Het.sup.2 is 2, 3, or 4-pyridyl or 2, 4, or 5-pyrimidinyl and the other is selected from(a) 2, 3, or 4-pyridyl,(b) 2, 4, or 5-pyrimidinyl,(c) 2-pyrazinyl,(d) 3, or 4-pyridazinyl,(e) 3, or 4-pyrazolyl,(f) 2, or 3-tetrahydrofuranyl, and(g) 3-thienyl.

Abstract: Radiopharmaceuticals consisting essentially of a lipophilic, charge neutral radionuclide complex of a diaminedithiol ligand having 1-4 ester groups of the formula --A--COOR where A is a straight or branched chain alkylene of 0-10 carbon atoms and R is an alkyl group of 1-10 carbon atoms are useful in radioimaging brain perfusion in primates. Ester-substituted diaminedithiols in sterile, pharmaceutically acceptable form, and kits of the diaminedithiols and sterile, non-pyrogenic reducing agents for reducing preselected radionuclides are also provided. Technetium-99m is a preferred radionuclide.

Abstract: There are provided novel 1,4 Diamine 2,3 Dihydroxybutanes useful as antiviral agents, pharmaceutical compositions containing them and processes for preparing such compounds.

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: 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: Anticancer compounds of formula I: ##STR1## and pharmaceutically acceptable salts thereof, wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected H, CH.sub.3, NH.sub.2, NO.sub.2, and CN;R.sup.9 and R.sup.10 are H or alkyl or halo, X.sup.1 and Y.sup.1 or X.sup.2 and Y.sup.2, when present, join together to form, independently, a six membered 1N heterocycle substituted with 1-2 R.sup.3 ; or the 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 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 disclosed.

Abstract: Compounds of the following formula have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man involving learning and cognition, where subnormal levels of this neurochemical are found ##STR1## wherein R.sup.1 is 4-,3-, or 2-pyridyl, 2-fluoro-4-pyridyl or 3-fluoro-4-pyridyl;R.sup.2 is alkyl of 1 to 10 carbons, cycloalkyl of 3 to 8 carbons, 2-,3-, or 4-pyridyl, Phe or Phe-W;Phe is a phenyl group;W is F, Cl, Br, R.sup.4, --OH, --OR.sup.4, --NO.sub.2, --NH.sub.2, --NHR.sup.4, --NR4R.sup.4, --CN, --S(O)m --R.sup.4 ;R.sup.3 is H, F, Cl, Br, --CN, --OH, --NO.sub.2, --NH.sub.2, --CF.sub.3, --NHR.sup.4, --NR.sup.4 R.sup.4, R.sup.4, --OR.sup.4, --S(O).sub.m --R.sup.4R.sup.4 is alkyl of 1 to 4 carbons, CH.sub.2 Phe-- or Phe--;R.sup.5 is --(CH.sub.2).sub.n --Y or --OCOR.sup.4 ;Y is NH.sub.2, --NHR.sup.4, --NR.sup.4 R.sup.4, --NHCOR.sup.4, --NHCO.sub.2 R.sup.4, F, Cl, Br, OR.sup.4, --S(O).sub.m R.sup.4, --CO.sub.2 H, --CO.sub.2 R.sup.