Benzothiazole compounds and their pharmaceutical use

摘要

The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I.;

主权项

1. A compound, or a pharmaceutically acceptable salt thereof, of formula Ia:wherein:
R1 is R1a or R1b; R5 is R5a or R5b; R1a is: a) halo; or b) H; R1b is cyano; R2 is (C1-C6)alkyl; R3 is —O(C1-C6)alkyl; R3′ is H; R4 is: R5a is: a) H, (C1-C6)alkyl, (C1-C6)haloalkyl, (C3-C7)carbocycle, single ring heterocycle, —C(═O)—R11, —C(═O)—O—R11, —(C1-C6)alkyl-R11, or —O—R11,
wherein each R11 is independently H, (C1-C6)alkyl, (C1-C6)haloalkyl, (C3-C7)carbocycle, or single ring heterocycle,and wherein single ring heterocycle is optionally substituted with 1 to 3 Z11 groups; or b) —N(R9)R10 or —C(═O)—N(R9)R10,
wherein each R9 is independently H or (C1-C6)alkyl,and wherein each R10 is independently H, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C6-C20)aryl, single ring heterocycle, —(C1-C6)alkyl-R11, or C(═O)—R11, and wherein each R11 is independently H, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C6-C20)aryl, or single ring heterocycle; R5b is: a) -(C2-C6)alkynyl-(C3-C7)carbocycle; or b) —NReRf; each Z11 is Z10; each Z10 is independently halo, —O(C1-C6)alkyl, —SO2(C1-C6)alkyl, or (C1-C6)alkyl; each Re is independently (C1-C6)alkyl; each Rf is independently —(C1-C6)alkyl-Z6; each Z6 is independently —NRaRa or —C(O)NRcRd; each Ra is independently (C1-C6)alkyl; and Rc and Rd are each independently (C1-C6)alkyl; wherein each single ring heterocycle has 1 to 6 carbon atoms and 1 to 3 heteroatoms selected from the group consisting of oxygen, nitrogen and sulfur.