Antiprotozoal Compounds

摘要

The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by administration of the compound, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis and malaria, the method comprising administering to a mammal, including a human, in need of such treatment a compound of formula I as described above.

主权项

1. A compound of the formula (I):or the pharmaceutically acceptable salt(s) thereof, wherein:
X1 is a group of the general formula: wherein R5, R6 and R7 are independently defined as H, C1-C6 alkyl, C3-C7-cycloalkyl, un(substituted) aryl, or heteroaryl; or R5 and R6, taken together with the N—C═N group to which they are attached form a 5-10 member cyclic or bicyclic ring, optionally substituted with up to two additional heteroatoms selected from the group consisting of N, O or S (including, for example, the cyclic or bicyclic rings dihydro-imidazole and benzimidazole) and optionally substituted with H, C1-C6 alkyl or cycloalkyl groups, (un)substituted aryl or heteroaryl rings, or oxygen, e.g., sulfoxide or sulfone); or R6 and R7, taken together with the nitrogen atom to which they are attached form a 5-10 member cyclic or bicyclic ring, optionally substituted with up to two additional heteroatoms selected from the group consisting of N, O or S (including, for example, the cyclic or bicyclic rings azetidine, pyrrolidine, piperidine, azepine, piperazine, morpholine, thiomorpholine) and optionally substituted with H, C1-C6 alkyl or cycloalkyl groups, aryl or heteroaryl rings, or oxygen, e.g., sulfoxide or sulfone); X2 is H, Cl, or F; R1 and R2 are independently hydrogen or methyl; R3 is hydrogen; and n is zero, one or two.