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US 10,292,976 B2Granted
Anti-malarial agent
AssigneeRiken
InventorsAkira Wada, Hiroki Hayase, Nobumoto Watanabe, Hiroyuki Osada, Takeshi Shimizu, Konstanty Wierzba
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Abstract
The present invention aims to prevent and/or treat malaria using an antimalarial drug comprising, as an active ingredient, a metal chelator represented by the following formula (I), (III), (IV), (V), (VI), or (VII), such as tris(2-pyridylmethyl)amine.
Claims6
A method of treating malaria, comprising administering a therapeutically effective amount(s) of one or more compounds selected from the group consisting of
- (a) the compounds of the following Formula (IX)
- in Formula (IX), R10 represents the following Formula (II-1)′,
- in Formula (II-1)′, any one of the Xs represents carbon (C) or nitrogen (N), and the other three Xs represent carbon (C),
- wherein, in Formula (II-1)′, and Formula (IX), each hydrogen (H) is optionally independently substituted with a halogen, C1-C10 alkyl, C1-C10 alkoxy, phenyl, hydroxyl (—OH), carboxyl (—COOH), amino (—NH2), benzamide (—NHCOC6H5), benzylamino (—NHCH2C6H5), tert-butylamide (—NHCO-tBu), neopentylamino (—NHCH2-tBu), —C(═O)OR, —S(═O)2OR, or —OP(═O)(OR)(OR′);
- R and R′ each independently represent hydrogen or C1-C10 alkyl;
- and further, each hydrogen (H) in the alkyl, alkoxy, phenyl, “—C6H5” of the benzamide, “—C6H5” of the benzylamino, “-tBu” of the tert-butylamide, and “—CH2—” and “-tBu” of the neopentylamino is optionally independently substituted with a halogen, hydroxyl, amino, —C(═O)OR, —S(═O)2OR, or —OP(═O)(OR)(OR′);
- and a hydrogen of an amino group may be substituted by C1-C10 alkyl,
- in Formula (II-1)′, C1-C10 alkyl which substitutes a halogen may contain nitrogen (N), and adjacent alkyls may bond to each other and form a ring, and
- (b) pharmaceutically acceptable salts and metal complexes thereof,
- to a subject suffering from malaria.
7 more elements
A method of treating malaria, comprising administering a therapeutically effective amount(s) of one or more compounds selected from the group consisting of
- (a) the compounds of the following Formula (X)
- wherein, in Formula (X), each hydrogen (H) is optionally independently substituted with a halogen, C1-C10 alkyl, C1-C10 alkoxy, phenyl, hydroxyl (—OH), carboxyl (—COOH), amino (—NH2), benzamide (—NHCOC6H5), benzylamino (—NHCH2C6H5), tert-butylamide (—NHCO-tBu), neopentylamino (—NHCH2-tBu), —C(═O)OR, —S(═O)2OR, or —OP(═O)(OR)(OR′);
- R and R′ each independently represent hydrogen or C1-C10 alkyl;
- and further, each hydrogen (H) in the alkyl, alkoxy, phenyl, “—C6H5” of the benzamide, “—C6H5” of the benzylamino, “-tBu” of the tert-butylamide, and “—CH2—” and “-tBu” of the neopentylamino is optionally independently substituted with a halogen, hydroxyl, amino, —C(═O)OR, —S(═O)2OR, or —OP(═O)(OR)(OR′), and
- (b) pharmaceutically acceptable salts and metal complexes thereof,
- to a subject suffering from malaria.
3 more elements
Dependencies are inferred from the claim text.