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US 5,593,993 AGranted
Method for inhibition of HIV related viruses
AssigneeMedivir AB
InventorsJohn M. Morin, Jr., Robert J. Ternansky, Rolf Noreen, Tomas Lind
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Abstract
Treatment of AIDS, inhibition of the replication of HIV and related viruses thereof, and formulations using thiourea derivative compounds or salts thereof is disclosed. Also disclosed are novel thiourea derivative compounds.
Claims9
A method for inhibiting the replication of HIV which comprises contacting a compound of the formula below ##STR94## in which R.sub.1 is a cyclo(C.sub.3 -C.sub.8)alkyl, cyclo (C.sub.3 -C.sub.8) alkenyl;
- isothiazolyl, substituted isothiazolyl, tetrazolyl, substituted tetrazolyl, triazolyl, substituted triazolyl, pyridyl, substituted pyridyl, imidazolyl, substituted imidazolyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, benzoxazolyl, substituted benzoxazolyl, benzimidazolyl, substituted benzimidazolyl, thiazolyl, substituted thiazolyl, oxazolyl, substituted oxazolyl, benzothiazolyl, substituted benzothiazolyl, pyrazinyl, substituted pyrazinyl, pyridazinyl, substituted pyridazinyl, thiadiazolyl, substituted thiadiazolyl, benzotriazolyl, substituted benzotriazolyl, pyrrolyl, substituted pyrrolyl, indolyl, substituted indolyl, benzothienyl, substituted benzothienyl, thienyl, substituted thienyl, benzofuryl, substituted benzofuryl, furyl, substituted furyl, quinolinyl, substituted quinolinyl, isoquinolinyl, substituted isoquinolinyl, pyrazolyl, and substituted pyrazolyl;
- R.sub.2 is a group of the formula ##STR95## wherein R.sub.5 is R.sub.1 as defined above;
- or R.sub.5 is a group of the formula
- (R.sub.10)y--X--
- wherein
- y is 1 or 2;
- X is N, S, O and R.sub.10 is R.sub.1 as defined;
- or R.sub.10 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.2 -C.sub.6 alkynyl;
- or R.sub.5 is hydrogen, halo, cyano, carboxy, amino, thio, hydroxy, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 alkynyl, or C.sub.2 -C.sub.8 alkenoxy;
- R.sub.6, R.sub.7, R.sub.8, and R.sub.9 are independently C.sub.3 -C.sub.8 cycloalkyl, hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, halo, amino, nitro, cyano, C.sub.1 -C.sub.5 alkoxy, hydroxy, carboxy, hydroxymethyl, aminomethyl, carboxymethyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkanoyloxy, carbamoyl, or a halo substituted C.sub.1 -C.sub.6 alkyl;
- or two of which, along with the carbons to which they are attached, combine to form a stable, saturated or unsaturated, substituted or unsubstituted, 3 to 7 membered organic monocylic ring having 0 to 4 hetero atoms selected from S, O, or N;
- or R.sub.6 and R.sub.8, or R.sub.7 and R.sub.9, along with the carbon to which they are attached, form a stable, saturated or unsaturated, substituted or unsubstituted, 3 to 7 membered organic monocylic ring having 0 to 4 hetero atoms selected from S, O, or N;
- R.sub.3 and R.sub.4 are independently hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, amine, cyano, nitro, C.sub.1 -C.sub.5 alkoxy, carboxy, hydroxymethyl, aminomethyl, carboxymethyl, C.sub.1 -C.sub.4 alkythio, C.sub.1 -C.sub.4 alkanoyloxy, halo-substituted (C.sub.1 -C.sub.6) alkyl, or carbamoyl;
- or salts thereof, with HIV.
11 more elements
Dependencies are inferred from the claim text.