Anti-malarial compounds
AssigneesThe Trustees of the University of Pennsylvania, Cellceutix Corporation
InventorsRichard W. Scott, Doron Greenbaum, Dahui Liu, Xiaodong Fan, Yongjiang Xu, Haizhong Tang, Ehab Khalil
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Abstract
The present invention provides tricyclic compounds, arylamide compounds, and other compounds, and compositions comprising the same, for treating malaria, and methods of treating malaria comprising administering such compounds to an animal.
Claims20
A compound of Formula I:
- wherein:
- X is N(R9), O, S, S(═O), or S(═O)2;
- R9 is H or C1-C8alkyl;
- R1 and R2 are H;
- R3 and R4 are, independently,
- wherein each W, Y, and Z are, independently, C or N;
- each R5 is, independently, H or C1-C8alkoxy;
- and
- each R6 is, independently, the free base or salt form of —(CH2)n—NH2, or —(CH2)n—NH—(CH2)n—NH2, or —(CH2)n—NH—C(═NH)NH2, where each n is, independently, 1 to 8;
- or a pharmaceutically acceptable salt thereof.
A compound of Formula I:
- wherein:
- X is NH or S;
- R1 and R2 are H;
- R3 and R4 are, independently,
- wherein each W, Y, and Z are, independently, C or N;
- each R5 is, independently, H or C1-C8alkoxy;
- and
- each R6 is, independently, heterocycle, or the free base or salt form of —(CH2)n—NH2, or —(CH2)n—NH—(CH2)n—NH2, or —(CH2)n—NH—C(═NH)NH2, where each n is, independently, 1 to 8;
- or a pharmaceutically acceptable salt thereof.
A compound of Formula I:
- wherein:
- X is N(R9), O, S, S(═O), or S(═O)2;
- R9 is H or C1-C8alkyl;
- R1 and R2 are H;
- R3 and R4 are, independently,
- wherein each W, Y, and Z are, independently, C or N;
- each R5 is, independently, H or C1-C8alkoxy;
- and
- each R6 is piperazinyl or the free base or salt form of —(CH2)n—NH2 where each n is, independently, 1 to 3.
A compound of Formula I:
- wherein:
- X is NH, O, or S;
- R1 and R2 are H;
- R3 and R4 are
- where each Z and Y are C, and each W is N;
- or each W, Y, and Z are C;
- each R5 is H, and each R6 is piperazinyl or the free base or salt form of —(CH2)n—NH2, where each n is, independently, 1 to 3.
A pharmaceutical composition comprising the compound
- or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
A method of treating malaria in an animal or killing or inhibiting the growth of a Plasmodium species comprising administering to the animal a therapeutically effective amount of a compound of Formula I or contacting the species with an effective amount of a compound of Formula I:
- wherein:
- X is N(R9), O, S, S(═O), or S(═O)2;
- R9 is H, C1-C8alkyl, C1-C8alkoxy, halo, OH, or CF3;
- R1 and R2 are, independently, H, C1-C8alkyl, C1-C8alkoxy, halo, OH, haloC1-C8alkyl, or CN;
- R3 and R4 are, independently,
- wherein each W, Y, and Z are, independently, C or N;
- each R5 and each R6 are, independently, H, C1-C8alkyl, C1-C8alkoxy, halo, OH, CF3, aromatic group, heterocycle, or the free base or salt form of —(CH2)n—NH2, —(CH2)n—NH—(CH2)n—NH2, or —(CH2)n—NH—C(═NH)NH2, where each n is, independently, 1 to 8;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.