Abstract: The present invention relates generally to methods for the preparation of unsymmetrically substituted cyclic ureas of the formulae ##STR1## which are useful as HIV protease inhibitors. The methods provided go through an isourea intermediate.

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 learning and cognition.The compounds of this invention are ##STR1## where Q is ##STR2## A and B are independently selected from H, R.sup.4, --OH and --OCOR.sup.4, orA and B together form .dbd.O, .dbd.S, .dbd.CH.sub.2, .dbd.CHR.sup.4, .dbd.C(R.sup.4), .dbd.NOH, .dbd.NOR.sup.4, 1,3-dioxane, 1,3-dioxolane, 1,3-dithiane or 1,3-dithiolane;R.sup.1 is 4-,3-, or 2-pyridyl, 2-fluoro-4-pyridyl or 3-fluoro-4-pyridyl;R.sup.3, R.sup.4 and R.sup.5 are herein defined;and physiologically suitable salts thereof.

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 provides improved synthetic processes for the preparation of hydroxy-protected cyclic urea compounds of Formula (IX), ##STR1## which are useful as intermediates for the preparation of cyclic urea human immunodeficiency virus (HIV) protease inhibitors, from N-protected aminoaldehydes. The processes of the present invention provide high yields, can be conducted on multikilogram scale, and eliminate the need for chromatographic purification of intermediates or final product.

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: 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: 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: The present invention relates to substituted 2, 5-diaryl-4-isothiazolin-3-ones, pharmaceutical preparations containing them, and their use in the treatment of, thrombosis and, especially inflammation.

Abstract: There are provided novel nitrogen-containing bicyclic compounds which are useful in the treatment of physiological or drug induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.

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: Processes for stabilizing active PAI-1 protein comprising combining active PAI-1 protein with an aqueous buffer having an ionic strength of at least about 5 millisiemens and a sugar selected from the group consisting of monosaccharides and disaccharides, and/or subjecting the active PAI-1 protein to lyophilization, are disclosed. Also described are compositions, including pharmaceutical compositions and kits, which include the stabilized active PAI-1 protein, and therapeutic processes employing the same in the treatment of fibrinolysis.

Abstract: (Benzimidazol-1'-ymethyl)phenylacetaldehydes as Topical Anti-inflammatories.

Abstract: (Indazol-1'-ymethyl)phenylacetaldehydes as Topical Anti-inflammatories.

Abstract: A method of separating active and inactive/latent forms of PAI-1 is disclosed comprising loading a sample containing a mixture of active and inactive/latent forms of PAI-1 to either an anion or cation exchange resin of 10-50 micron particle size and eluting active and inactive/latent forms of PAI-1 from the resin into separate fractions. Also disclosed is a method of extracting soluble E. coli-expressed recombinant PAI-1 from the lysed E. coli host cells in a buffered solution, wherein the ionic strength of the buffered solution is 8-25 millisiemens.

Abstract: Intermediates for the preparation of Peptides comprising C-terminal boronic acid derivatives of lysine, ornithine, and arginine, homoarginine and corresponding isothiouronium analogs thereof, are reversible inhibitors of trypsin-like serine proteases such as thrombin, plasma kallikrein and plasmin.

Abstract: This invention relates to substituted naphthofurans as anti-inflammatory and anti-allergic agents, pharmaceutical compositions containing them, processes for their preparation, and their use as anti-inflammatory and anti-allergic agents. The naphthofurans are of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 is CN or COOR.sup.9 ;R.sup.2 and R.sup.8 independently are H, C.sub.1 -C.sub.4 alkyl, COR.sup.9 or COR.sup.10 ;R.sup.3, R.sup.4, R.sup.6 and R.sup.7 are independently H, C.sub.1 -C.sub.4 alkyl, halogen, phenyl, CF.sub.3 or OR.sup.9 ;R.sup.5 is H, C.sub.1 -C.sub.4 alkyl, or COR.sup.9 ; andR.sup.9 and R.sup.10 are independently C.sub.1 -C.sub.4 alkyl, halogen or aryl.

Abstract: Peptides comprising C-terminal boronic acid derivatives of lysine, ornithine, and arginine, homoarginine and corresponding isothiouronium analogs thereof, are reversible inhibitors of trypsin-like serine proteases such as thrombin, plasma kallikrein and plasmin.

Abstract: There are disclosed pharmaceutical compositions containing polyoxoanions, methods of using them alone or in combination with other compounds, such as AZT and Poly-I:C for the treatment of retroviruses. Also disclosed are novel polyoxoanions.