The present invention relates particularly to novel heterocycle based nitrogen-sulfur ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.

The invention concerns novel renin-inhibitory peptides which contain novel amino acids having an .alpha.-heteroatom attached to the backbone of the amino acid. ##STR1## These novel amino acids are positioned at the P.sub.2 position of the peptide. These are useful for treating renin-associated hypertension, hyperaldosteronism, and congestive heart failure. Processes for preparing the peptides, compositions containing them and methods of using them are included. Novel intermediates are also discl...

A compound of the formula ##STR1## wherein R.sup.1, R.sup.2 R.sup.3, R.sup.4 R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and Ar are as defined above, useful in the treatment of a condition seiected from the group consisting of arthritis, cancer, tisuue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis and other disease characterized by matrix metalloproteinase activity, as well as AIDS, sepsis, septic shock and other diseases involving the production of TNF.

A method of preparing intermediates for making 1-substituted, 2-substituted 1H-imidazo[4,5-c]quinolin-4-amines is disclosed.

The present invention provides a matrix metalloproteinase inhibiting compound having structure (VIII) or a salt, an enantiomer, a diastereomer, a racemate, or a tautomer thereof. In other embodiments, the present invention provides a method of changing the conformation of a matrix metalloproteinase, a method of inhibiting a matrix metal metalloproteinase, and a method of treating osteoarthritis. ##STR1##

The present invention relates to alkyne containing metalloproteinase inhibitors of the formula ##STR1## wherein n, X, and R.sup.1 -R.sup.9 are as defined in the specification, and to pharmaceutical compositions and methods of treatment thereof.

Methods of preparing 1-substituted, 2-substituted 1H-imidazo [4-5c]-quinolin-4-amines are disclosed. The compounds function as antiviral agents, they induce the biosynthesis of various cytokines including interferon, and they inhibit tumor formation in animal models.

The invention relates to compounds of formula ##STR1## in which R.sub.1 to R.sub.9, R.sub.16 and R.sub.17 are as defined in claim 1. These compounds are pharmacologically active.

The disclosure relates to new 2-(substituted anilino)-methylmorpholine derivatives which possess sedative activity, to processes for the manufacture of the said morpholine derivatives, and to pharmaceutical compositions containing them. Typical of the morpholine derivatives disclosed is 2-(3-methoxyanilino)methylmorpholine.

Amide and ester derivatives of 2-[N-(morpholinoalkyl)aminosulfonyl]-6-nitrobenzoic acids are disclosed to have activity in increasing the sensitivity of hypoxic tumor cells to therapeutic radiation. Also disclosed are methods of preparing such compounds and pharmaceutical compositions including such compounds.