Abstract: A chemically synthesized 15 amino acid peptide designated peptide 1-69, which has the sequence of amino acids numbers 308 to 322 (RIQRGPGRAFVTIGK) of the human immunodeficiency virus-1 (HIV-1) IIIB env-coded protein, was used to immunize animals. Peptide 1-69 elicited in immunized animals antibodies that block HIV proliferation and block HIV-induced cell fusion in cell culture.

Abstract: The present invention provides a process for the preparation of compounds of formula (V) below, and analogs thereof, which are useful as intermediates for the synthesis of HIV protease inhibitors, including cyclic ureas.

Abstract: The present invention relates to methods for the preparation of disubstituted cyclic ureas of the formula (IV): ##STR1## from linear diaminodiols. These cyclic urea compounds are useful as HIV protease inhibitor compounds for the treatment of HIV infection.

Abstract: This invention relates to 2-carbocyclic and 2-heterocyclic quinoline-4-carbocyclic acid compounds, and salts thereof, to pharmaceutical compositions comprising such compounds, and to methods of using such compounds for the treatment and/or prevention of organ transplantation rejection, graft versus host disease, and chronic inflammatory diseases, including but not limited to psoriasis and rheumatoid arthritis, in a mammal.

Abstract: This invention relates to novel compounds containing basic and acidic termini, 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 discloses processes for the preparation of substituted cyclic sulfamides which are useful as intermediates for the synthesis of cyclic sulfamide human immunodeficiency virus (HIV) protease inhibitors. Such substituted cyclic sulfamide intermediates contain a cyclic acetal-protected diol.

Abstract: The present invention provides compounds of Formula I, ##STR1## or a pharmaceutically acceptable salt forms thereof, which are inhibitors of acyl-Coenzyme A: cholesterol O-acyltransferase (ACAT), pharmaceutical compositions containing such compounds, processes for the preparation of such compounds, and the use of such compounds as antihypercholesterolemic and/or antiatherosclerotic agents.

Abstract: Oligonucleotides possessing at least one sulfamate or sulfamide internucleotides linkages. These compounds can be used as specific hybridization probes to detect complementary nucleic acid sequences.

Abstract: This invention relates to bis-naphthalimides, including 2,2'-[1,2-ethanediylbis[imino(1-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione] and 2,2'-[1,2-ethanediylbis[imino(2-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione], processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer in mammals.

Abstract: This invention relates to novel isoxazolines which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, 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: This invention relates to carbocyclic and heterocyclic fused-ring quinolinecarboxylic acid compounds, to pharmaceutical compositions comprising such compounds, and to methods of using such compounds for the treatment and/or prevention of organ transplantation rejection, graft versus host disease, autoimmune diseases, chronic inflammatory diseases, including but not limited to psoriasis and rheumatoid arthritis, and cancer in a mammal.

Abstract: Polycyclic cognition enhancers having the general formula (1a), (1b) or (1c) are provided: ##STR1## wherein: R.sub.1 is a heterocyclic aromatic moiety such as a 4-pyridyl, 2-pyridyl, 4-pyrimidyl, or pyrazinyl group;R.sub.2 and R.sub.3 are independently H, F, Cl, Br, NO.sub.2, CONH.sub.2, CON(R.sub.4)(R.sub.4 '), S(O).sub.m R.sub.4, CF.sub.3, or N(R.sub.4)(R.sub.4 ');R.sub.4 and R.sub.4 ' are independently H, alkyl having from 1 to 4 carbon atoms, CH.sub.2 Phe--W, or Phe--W;Phe is a phenyl group;R.sub.5 is --(CH.sub.2).sub.n --Y or --OCOR.sub.4 ;Y is H, OH, NH.sub.2, NHR.sub.4, N(R.sub.4)(R.sub.4 '), NHCOR.sub.4, NHCO.sub.2 R.sub.4, NHS(O).sub.2 R.sub.4, F, Cl, Br, OR.sub.4, S(O).sub.m R.sub.4, CO.sub.2 H, CO.sub.2 R.sub.4, CN, CON(R.sub.4)(R.sub.4 '), CONHR.sub.4, CONH.sub.2, COR.sub.4, Phe, Phe--W, --C.tbd.CCO.sub.2 R.sub.4, --CH.dbd.CHR.sub.4, --C.tbd.CR.sub.4, or a heterocyclic aromatic moiety such as a 4-pyridyl, 2-pyridyl, 4-pyrimidyl, or pyrazinyl group;W is F, Cl, Br, R.sub.4, OR.sub.4, NO.sub.2, NH.

Abstract: This invention relates to compounds, including 5-chloro-2-[2-[[(4-methylphenyl)sulfonyl]oxy]ethyl]-7-[2,4,6-trimethylphen yl)methoxy]anthra[1,9-cd]pyrazol-6(2H)-one and analogs thereof, which are useful as intermediates for the synthesis of anthrapyrazolone anticancer agents, including losoxantrone. This invention also relates to methods for the synthesis of anthrapyrazolone anticancer agents, including losoxantrone.

Abstract: The present invention is directed to immunoassay reagents including specific antibodies to quinoline carboxylic acids, such as brequinar; novel quinoline carboxylic acid haptens useful as standards in immunoassays or for conjugating to large molecular weight carriers as immunogens or conjugating to detectable fluorescent moieties as tracer compounds. The present invention also relates to immunoassays for detecting quinoline carboxylic acids in clinical samples, and finally to kits containing said reagents.

Abstract: This invention relates to unsymmetrical mono-3-nitro bis-naphthalimides of formula ##STR1## including (R,R)-2-{2-[2-((2-(1,3-dioxo-1H-benz[de]isoquinolin-2-(3H)-yl)-propylamino ))ethylamino]-1-methylethyl}-5-nitro-1H-benz[de]isoquinolin-1,3-(2H)-dione, processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer, particularly solid tumor carcinomas, in mammals.

Abstract: Disclosed are imidazoles linked to bicyclic heterocyclic groups, as inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT), processes for their preparation, pharmaceutical compositions, and their use as antihypercholesterolemics and/or antiatherosclerotics.

Abstract: This invention relates to unsymmetrical bis-imide compounds, and pharmaceutically acceptable salts thereof, of the formula (i): ##STR1## including (R,R)-1-[2-(acenaphthene-5,6-dicarboximido) propylamino]-2-[2-(3-nitronaphthalene-1,8-dicarboximido) propylamino]ethane, processes for the preparation of such compounds, pharmaceutical compositions containing such compounds, and methods of using such compounds to treat cancer, particularly solid tumor carcinomas, in mammals.

Abstract: Disclosed are cationic complexes of Tc-99m and ligands having the structure: ##STR1## wherein: R.sup.1 is hydrogen or is selected from the group consisting of C.sub.1 to C.sub.20 alkyl; C.sub.3 to C.sub.12 cycloalkyl; C.sub.7 to C.sub.24 aralkyl; C.sub.2 to C.sub.16 alkyl ethers, thioethers, ketones or esters; C.sub.7 to C.sub.27 aralkyl ethers;R.sup.2 is hydrogen or is a C.sub.1 to C.sub.4 lower alkyl radical selected from the group consisting of methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl and tert-butyl.

Abstract: This invention relates to bis-naphthalimides, including 2,2'-[1,2-ethanediylbis[imino(1-methy1-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione] and 2,2'-[1,2-ethanediylbis[imino(2-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione], processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer in mammals.

Abstract: Disclosed are imidazoles as inhibitors of acylCoA:cholesterol acyltransferase (ACAT), processes for their preparation, pharmaceutical compositions, and their use as antihypercholesterolemics and/or antiatherosclerotics.