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

A method of forming a photographic coupler (A) having the formula: comprising: (a) providing a coupler (B) having a coupling-off group represented by the formula: ##STR1## (b) reacting said coupling-off group of coupler (B) with phosgene to provide a chloroformate coupling-off group of coupler (B) (c) reacting said chloroformate coupling-off group of coupler (B) in the presence of a strong base selected from the group consisting of triethylamine, N,N-diisopropylethylamine, and tetramethylguanine...

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.

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 present compounds represented by the formula: ##STR1## (wherein R.sup.1 is a phenyl group, a halophenyl group or a cycloalkyl group having 3 to 8 carbon atoms, R.sup.2 is a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, R.sup.3 is a hydrogen atom, an alkyl group having 1 to 7 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms, an alkenyl group having 3 to 5 carbon atoms or a benzyl group, or R.sup.2 and R.sup.3 are bonded together to form a 5- to 7-membered heterocycle)...

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.

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.

o-Amidophenylmorpholine compounds having a halo, haloalkyl, lower alkylsulfonyl, halo-lower alkylsulfonyl, or lower alkyl substituent on the aromatic ring para to the morpholino nitrogen. The compounds are useful as herbicides.

A compound of the formula ##STR1## wherein n, X, R.sup.3, R.sup.4 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF.