Merck + Co., Inc.

Lilly Industries, Inc.

Lilly, Sa

Maria I Fernandez

Richard L Monaghan

Sheldon B Zimmerman

Sagrario M Del Val

Otto D Hensens

David Edward Tupper

Terrence M Hotten

Kenneth E Wilson

James E Flor

Cheryl Deriso

Louis Chaiet

A pharmaceutical compound of the formula ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen, hydroxy, halo, nitro, amino, C.sub.2-5 acylamino, C.sub.1-4 alkyl, --CHO, --CH.sub.2 OH, --CH.sub.2 OC.sub.1-4 alkyl, --COOH, --COC.sub.1-3 alkyl, --CH(OH)C.sub.1-3 alkyl, C.sub.1-4 alkoxy, C.sub.2-4 alkenyloxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphinyl, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene bridge; provided that at least one of R.sup.2 and R.sup.3 is C.sub.1-4 alkoxy or C.sub.2-4 alkenyloxy; and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.2 --, and n is 1, 2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a C.sub.1-3 alkylene chain; and salts and esters thereof.

Organic compounds and their use as pharmaceuticals

Compounds of the following formula have pharmacutical properties: ##STR1## in which R.sup.1 and R.sup.2 independently are hydrogen, halo, nitro, amino, C.sub.2-5 acylamino, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene bridge, R.sup.3 is C.sub.1-4 alkyl or C.sub.2-4 alkenyl, and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.2 --, and n is 1, 2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a C.sub.1-3 alkylene chain; and salts thereof.

The process for the manufacture of the compound of the general structural formula ##STR1## which is a 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) synthase inhibitor and useful as an antihypercholesterolemic agent for the treatment of disease in which the inhibition of cholesterol biosynthesis would be useful, and which is an antifungal agent is disclosed.

Process for the manufacture of an antifungal antihypercholesterolemic .beta

Process for the preparation of difficidin and derivative antibacterial compounds of the formula: ##STR1## where R.sub.a and R.sub.b are members independently selected from the group consisting of hydrogen; alkali metal and alkaline earth metal cations; ammonium; and substituted ammonium; and R.sup.1 is hydrogen or hydroxy.

Process for the preparation of difficidin and derivative antibacterials

R-(Z)-4-amino-3-chloro-2-pentenedioic acid is a novel antibacterial and isolated from Streptomyces viridogenes MA5450, ATCC 39387.

R-(Z)-4-amino-3-chloro-2-pentenedioic acid, novel antibacterial agent

Difficidin and derivative antibacterial compounds of the formula: ##STR1## where R.sub.a and R.sub.b are members independently selected from the group consisting of hydrogen; alkali metal and alkaline earth metal cations; ammonium; and substituted ammonium; and R.sup.1 is hydrogen or hydroxy.

Growing community of inventors

Madrid, Spain

Maria I Fernandez