Merck + Co., Inc.

Other

Robert A Zambias

Milton L Hammond

Michael N Chang

Norman P Jensen

James M Balkovec

John McDonald

Kathleen M Rupprecht

Charles G Caldwell

Ihor E Kopka

James Francis Dropinski

Frances A Bouffard

James V Heck

Kathryn L Thompson

Stanley H Wright

Cyclohexapeptidyl amine compounds are disclosed of the formula:

Cyclohexapeptidyl amine compounds

Certain bisamine compounds which have a cyclohexapeptidyl nucleus and which are found to have antibiotic activity with physical properties suitable for direct use in therapeutic compositions are described. A novel process for their preparation is also described.

Cyclohexapeptidyl bisamine compounds

Certain propanolamine compounds are described which have a cyclohexapeptidyl nucleus and which possess antibiotic activity with physical properties suitable for direct use in therapeutic compositions. A process for their preparation is also described.

Cyclohexapeptidyl propanolamine compounds

Certain propanolamine compounds which have a cyclohexapeptidyl nucleus and which are found to have extremely active antibiotic activity with physical properties suitable for direct use in therapeutic compositions are described. A novel process for their preparation is also described.

Novel amino acid conjugates of cyclohexa-peptidyl amines having the formula ##STR1## and having antifungal and antiparasital properties are described. The compounds exhibit less acute toxicity than the free amines.

Amino acid conjugates of cyclohexapeptidyl amines

Certain aminoalkyl substituted amides which have a cyclohexapeptidyl group and which are found to have antibiotic activity with physical properties suitable for use in therapeutic compositions are described.

Cyclohexapeptide with basic nitrogen containing alkylamide groups

Certain propionitrile compounds which have a cyclohexapeptidyl nucleus and which are found to have antibiotic activity with physical properties suitable for use in therapeutic compositions are described. A novel process for their preparation is also described. ##STR1##

Cyclohexapeptidyl hydroxypropionitrile compounds

Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or hydroxyl; R.sub.2 is hydrogen; hydroxyl or methyl, R.sub.3 is hydrogen or hydroxyl; R.sub.4 is C.sub.5 -C.sub.23 alkyl, C.sub.5 -C.sub.23 alkenyl, aryl or substituted aryl; R.sub.5 is --CH.sub.2 OH, --CH(CH.sub.3)OH, --CH(CH.sub.2 CONH.sub.2)OH; R.sub.6 is --CH.sub.2 OH or --CH(CH.sub.3)OH; R is --CH.sub.2 OH or --CH(CH.sub.3)OH; provided that when R.sub.4 is --(CH.sub.2).sub.8 CH(CH.sub.3)CH.sub.2 CH(CH.sub.3)C.sub.2 H.sub.5, R.sub.5 is --CH.sub.2 OH or --CH(CH.sub.3)OH. The compounds are useful as antimicrobial agents, especially as antifungal agents.

Cyclic hexapeptide compounds

Novel 7-Aroyl-4-Hydroxy-3-Methyl-Benzofurans of the following general formula (I) are disclosed: ##STR1##

Novel 7-aroyl-4-hydroxy-3-methyl-benzofurans as dual inhibitors of

Novel position-4 and/or position-6 substituted 5-hydroxy-2,3-dihydrobenzofuran and analogs of the following general structural formula (I) are disclosed: ##STR1## These compounds are found to be potent inhibitors of leukotriene biosynthesis.

6-substituted 5-hydroxy-2,3-dihydrobenzofurans as inhibitors of

Position-4 and/or position-6 substituted 5-hydroxy-2,3-dihydrobenzothiophenes and analogs of the following general structural formula (I) are disclosed: ##STR1## These compounds are found to be potent inhibitors of leukotriene biosynthesis.

Substituted 5-hydroxy-2,3-dihydrobenzothiophenes as inhibitors of

An anti-theft device for audio equipment which is accessible through an opening in a frame of an automotive vehicle, includes a rectangular sliding door movable in a vertical direction between a closed position in blocking relation to the opening and an open position permitting access to the audio equipment through the opening; a trackway which guides movement of the sliding door between the open and closed positions; a lead screw rotatably connected with the frame; a support nut connected with the sliding door for threadedly receiving the lead screw; a first gear fixedly mounted on the lead screw; a motor secured to the frame and having an output shaft with a second gear at the free end thereof, the second gear being in meshing engagement with the first gear; an actuation switch for selectively actuating the motor only when the ignition switch of the vehicle is on, to cause the sliding door to move along the trackway between the open and closed positions.

Anti-theft device for automobile audio equipment

Substituted cinnamyl-2,3-dihydrobenzofurans and analogs were prepared from the nucleophlic substitution of a cinnamylhalide with a 2,3-dihydrobenzofuran anion or an analog thereof. These compounds were found to be potent topical anti-inflammatory agents.

Substituted 2-(heteroaryl-2-propenyl)phenols useful as anti-inflammatory

Thiazole derivatives have been made, for example, by reacting a 2-aryl-2,2-dialkoxyethylamine with an appropriately substituted aryl acetyl halide followed by treating the resulting amide with diphosphoryl pentasulfide. The thiazole derivatives are found to be effective immunoregulants.

Substituted thiazoles as immunoregulants

Substituted 2-benzyl-mercapto-imidazoles and analogs were prepared from the nucleophlic substitution of an appropriately substituted benzoxyacetate with a 2-imidazole mercapto anion or an analog thereof. These compounds were found to be anti-inflammatory agents.

Growing community of inventors

Springfield, NJ, United States of America

Robert A Zambias