Compound and pharmaceutical composition for neuropsychological disorder or malignant tumor
Inventors
Hagiwara, Masatoshi • Onogi, Hiroshi • Kii, Isao • Hosoya, Takamitsu • Sumida, Yuto
Assignees
Tokyo Medical and Dental University NUC • KinoPharma Inc • Kyoto University NUC
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Publication Number
US-10017524-B2
Publication Date
2018-07-10
Expiration Date
Abstract
The present invention provides a compound and a pharmaceutical composition for neuropsychological disorders or malignant tumors, the use of the compound and the pharmaceutical composition, or a method for preventing, improving, inhibiting the development of, and/or treating neuropsychological disorders or malignant tumors with the use of the compound and the pharmaceutical composition. One or more embodiments disclose a compound expressed by the following general formula (I) or (II) or a pharmaceutically acceptable salt of the compound:
Core Innovation
The invention relates to a compound expressed by formula (II), or a prodrug of the compound, or a pharmaceutically acceptable salt of the compound. In the formula (II), X and Y each independently represent S or NH, and R5 and R6 are defined with specific allowable ring types and substituent types, with a proviso that the compound is not among the excluded embodiments.
R5 is defined such that Z and atoms marked with a and b form a ring selected from one benzene ring, one heteroaromatic ring, condensed aromatic ring systems, condensed heteroaromatic ring systems, mixed condensed polycyclic rings combining benzene and heteroaromatic rings, or a cyclic aliphatic ring. The ring may include at least one substituent that is a hydrogen atom, a halogen atom, or a C1-6 alkyl group, and R6 is limited to a hydrogen atom, a halogen atom, or a C1-6 alkyl group.
The invention further covers pharmaceutical composition contexts by claiming compositions that include the compound of formula (II), or its pharmaceutically acceptable salt, as an active ingredient. The same compound definition is used in methods for treating Down's syndrome and specific cancers, including brain cancer, lung cancer, and breast cancer, by administering the compound, or its prodrug or pharmaceutically acceptable salt, to a subject.
Claims Coverage
The independent claims include a compound claim and therapeutic method claims, with further claim language refining the compound definition and pharmaceutical composition scope. Across the independent claims, the inventive features center on the specified chemical formula (II) structural constraints and its use in treating Down's syndrome and certain cancers via administration.
Formula (II) compound, prodrug, or pharmaceutically acceptable salt
A compound expressed by formula (II), or a prodrug of the compound, or a pharmaceutically acceptable salt of the compound, wherein X and Y each independently represent S or NH; R5 includes Z and atoms marked with a and b forming a ring selected from one benzene ring, one heteroaromatic ring, condensed aromatic ring systems, condensed heteroaromatic ring systems, mixed condensed polycyclic rings combining benzene and heteroaromatic rings, and a cyclic aliphatic ring, with optional substituents being a hydrogen atom, a halogen atom, or a C1-6 alkyl group; R6 represents a hydrogen atom, a halogen atom, or a C1-6 alkyl group; with the proviso that the compound is not among the excluded embodiments.
Treating by administering formula (II) compound, prodrug, or salt
A method for treating Down's syndrome, brain cancer, lung cancer, or breast cancer, comprising administering a compound expressed by formula (II), or a prodrug of the compound, or a pharmaceutically acceptable salt of the compound, to a subject, with the same structural constraints on X, Y, R5, and R6 and the same exclusion proviso.
Treating by administering formula-specified compound
A method for treating Down's syndrome, brain cancer, lung cancer, or breast cancer, comprising administering a compound expressed by the formula referenced in the claim text, or a prodrug of the compound, or a pharmaceutically acceptable salt of the compound, to a subject.
The independent claims cover a defined compound, or prodrug or pharmaceutically acceptable salt, characterized by formula (II) structural constraints on X, Y, R5, and R6 with an exclusion proviso, and methods of treating Down's syndrome and specified cancers by administering that compound, or prodrug or salt, to a subject.
Stated Advantages
Inhibits abnormal tau phosphorylation.
Inhibits APP phosphorylation leading to reduced Aβ production.
Suppresses phosphoenzyme activity relevant to cancer targets, including the receptor tyrosine kinase/EGFR pathway.
Provides intracerebral transferability and oral absorbability.
Documented Applications
Methods for treating Down's syndrome and cancers including brain cancer, lung cancer, and breast cancer by administering the formula (II) compound, or its prodrug or pharmaceutically acceptable salt, to a subject.
Prevention and/or treatment of neuropsychological disorders, including Down's syndrome, Alzheimer's disease, and AD in Down's syndrome.
Prevention and/or treatment of malignant tumors, including drug-resistant tumors.
Pharmaceutical composition use as an active ingredient containing the compound, or pharmaceutically acceptable salt, for administering to treat the listed disorders and cancers.
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