COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES

摘要

The present invention provides compounds of formula I:;;or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.

主权项

1. A compound of Formula I,or a pharmaceutical acceptable salt, tautomer or stereoisomer thereof, wherein
n is 0, 1, 2 or 3; p is 0, 1, 2 or 3; L is selected from the group consisting of *—(CHR3)1-3—, *—CHR3N(R2)—, *—CHR3O—, *—CHR3S—, *—CHR3S(O)—, *—CHR3N(R2)CHR3—, *—C(O)—, *—C(O)N(R2)—, *—C(O)N(R2)CHR3—, *—N(R2)—, *—N(R2)CHR3—, *—N(R2)C(O)—, *—N(R2)C(O)N(R2)—, *—N(R2)S(O)2—, wherein
* represents the point of attachment of L to the pyrazolo[1,5-a]pyridine fused ring depicted in Formula I;each R2 is independently selected from the group consisting of hydrogen, C1-6alkyl, haloC1-6alkyl, R—C0-4alkylene, and R—C0-4alkylene-C(O)—, wherein R is selected from the group consisting of hydroxyl, C1-4alkoxy, amino, C1-4alkylamino, C3-6cycloalkyl, C4-6heterocycloalkyl, and C5-6heteroaryl, wherein the C3-6cycloalkyl, C4-6heterocycloalkyl, and C5-6heteroaryl of R are each unsubstituted or substituted with 1-2 substituents independently selected from the group consisting of halo, amino, hydroxyl, C1-4alkyl, C1-4alkoxy, oxo, and C5-6heteroaryl; andeach R3 is independently selected from the group consisting of hydrogen and C1-4alkyl; Ring A is selected from the group consisting of C6-10aryl and C5-10heteroaryl; Ring C is selected from the group consisting of C6-10aryl, C5-10heteroaryl, C5-7cycloalkyl, C5-7heterocycloalkyl, and fused bicyclyl comprising a C5-6heterocycloalky fused to a phenyl; each R1 is independently selected from the group consisting of halo, cyano, amino, C1-4alkyl, C1-4alkoxyl, halo-C1-4alkyl, —C(O)NR7R8, —NHC(O)R11, phenyl, and C5-6heteroaryl; wherein
the phenyl and C5-6heteroaryl of R1 are each unsubstituted or substituted with 1-2 substituents independently selected from the group consisting of C1-4alkyl, amino, halo, and C1-4alkylamino;R7 and R8 are each independently selected from hydrogen, C1-4alkyl and haloC1-4alkyl;R11 is C1-6alkyl, unsubstituted or substituted with 1-2 substituents independently selected from the group consisting of amino, C3-6cycloalkyl and C4-6heterocycloalkyl; R17 is selected from the group consisting of cyano, halo, C1-4alkyl, halo-C1-4alkyl, oxo, C3-6cycloalkyl, and —SO2—C1-4alkyl.