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US 8,999,969 B2Granted
Anti-RSV compounds
AssigneeGilead Sciences, Inc.
InventorsRichard L. Mackman, David Sperandio, Hai Yang
Life of this patent
Estimating the term…
Abstract
The present invention relates to anti-RSV compounds of Formula (I) and methods for use of the compounds in the treatment and prevention of RSV infection.
Claims24
The present invention provides a compound of Formula I:
- wherein A is aryl or heteroaryl;
- R1 is selected from alkyl, alkoxy, haloalkyl, aryl, heteroaryl, heterocyclyl, and cycloalkyl, said heterocyclyl is optionally substituted by one to three substituents independently selected from the group consisting of halo, hydroxyl, haloalkyl, alkoxy, alkyl, alkoxy-alkyl-, hydroxyl-alkyl-, CN, and alkyl-NH—:
- said aryl or heteroaryl is optionally substituted by one to three substituents independently selected from the group consisting of halo, cyano, nitro, hydroxyl, alkyl, alkoxy, and alkyl-NH—, with the proviso that when A is aryl, R1 is not unsubstituted aryl;
- R2 is selected from hydrogen, alkyl, alkoxy, amino, alkyl-NH—, CN, alkyl-SO2—, and halo;
- R3 is selected from hydrogen, alkyl, heterocyclyl, heteroaryl, heteroaryl-alkyl- and cycloalkyl, wherein said alkyl is optionally substituted by one substituent selected from the group consisting of NH2—C(O)—, halo, hydroxyl, NH2—SO2—, alkoxy-alkyl-, heterocyclyl;
- aryl, heteroaryl, CN, and alkyl-NH—;
- R4 is selected from hydrogen, alkyl and haloalkyl;
- R3 and R4 taken together with the nitrogen atom to which they are attached optionally form a 3- to 7-membered ring;
- R5 is selected from hydrogen, alkyl, alkoxy, haloalkyl, and halo;
- or
- a pharmaceutically acceptable salt thereof.
8 more elements
A compound of Formula IA:
- wherein X, Y and Z are independently N or CH;
- R1 is selected from alkyl, alkoxy, haloalkyl, aryl, heteroaryl, and heterocyclyl, said heterocyclyl is optionally substituted by one to three substituents independently selected from the group consisting of halo, hydroxyl, haloalkyl, alkoxy, alkyl, alkoxy-alkyl-, and hydroxyl-alkyl-, said aryl is optionally substituted by one to two substituents independently selected from the group consisting of halo,
- cyano, nitro and hydroxyl, with the proviso that when X and Y are simultaneously CH, R1 is not unsubstituted aryl;
- R2 is selected from hydrogen, alkyl, alkoxy, and halo;
- R3 is hydrogen, alkyl, heterocyclyl, heteroaryl, heteroaryl-alkyl-, or cycloalkyl, said alkyl is optionally substituted by one substituent selected from the group consisting of NH2—C(O)—, halo, hydroxyl, NH2—SO2 alkoxy-alkyl-, and heterocyclyl;
- R4 is hydrogen, or alkyl;
- R3 and R4 taken together with the nitrogen atom to which they are attached optionally form a 3- to 7-membered ring;
- R5 is selected from hydrogen, alkyl, alkoxy, haloalkyl, and halo;
- or
- a pharmaceutically acceptable salt thereof.
7 more elements
A compound of Formula IB:
- wherein R1 is haloalkyl, or heterocyclyl, said heterocyclyl is optionally substituted by one to two substituents independently selected from the group consisting of halo, hydroxyl, alkoxy-alkyl-, alkyl, haloalkyl, and hydroxyl-alkyl-;
- R3 is selected from hydrogen, alkyl, heterocyclyl, heteroaryl, heteroaryl-alkyl-, and cycloalkyl, said alkyl is optionally substituted by one substituent selected from the group consisting of NH2—C(O)—, halo, and hydroxyl;
- R4 is hydrogen;
- and R5 is hydrogen, or halo;
- or a pharmaceutically acceptable salt thereof;
- or an optical isomer thereof, or a mixture of optical isomers.
3 more elements
Dependencies are inferred from the claim text.