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
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-9745323-B2
Publication Date
2017-08-29
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 compounds expressed by formula (I), and also encompasses prodrugs of the compounds and pharmaceutically acceptable salts of the compounds. The structural definitions include R1 and R2 independently representing a hydrogen atom or a C1-6 hydrocarbon chain, R3 defined to include a ring Z formed from selected ring systems, and R4 as a hydrogen atom, a halogen atom, or a C1-6 alkyl group.
The subject matter further includes compounds expressed by formula (III), including cases where R7 and R8 independently are hydrogen, a halogen, or a linear or branched C1-6 alkyl group. This alternative structural framework is maintained with corresponding prodrug and pharmaceutically acceptable salt coverage, and the disclosed subject matter is also positioned as a pharmaceutical composition containing the compound, or its prodrug or pharmaceutically acceptable salt, as an active ingredient.
The document describes compounds according to the formula (I) framework in contexts including tau protein phosphorylation inhibition and anti-cancer cell growth inhibition across multiple cell lines. It also positions the compounds for neuropsychological disorders and malignant tumors, including Down’s syndrome, Alzheimer’s disease, and cancers including brain tumor and drug-resistant malignant tumors, with method of use described as administering the compound, prodrug, or pharmaceutically acceptable salt to a subject in need.
Claims Coverage
The claims cover two independent themes: chemical entities defined by formula (I), with prodrug and pharmaceutically acceptable salt coverage and alternative formula (III) matter, and therapeutic methods using those compounds. Across the independent claims, there are two main inventive feature groupings.
Compound expressed by formula (I) with prodrug and pharmaceutically acceptable salt coverage
A compound expressed by formula (I) or a prodrug of the compound or a pharmaceutically acceptable salt of the compound, wherein R1 and R2 independently represent a hydrogen atom or a C1-6 hydrocarbon chain; R3 represents a ring Z formed from one benzene ring, one heteroaromatic ring, an aromatic ring in which one or more benzene rings are condensed, a heteroaromatic ring in which one or more heteroaromatic rings are condensed, a mixed condensed polycyclic ring in which one or more benzene rings are condensed with one or more heteroaromatic rings, or a cyclic aliphatic, where the ring may have at least one substituent that is a hydrogen atom, a halogen atom, or a C1-6 alkyl group; and R4 represents a hydrogen atom, a halogen atom, or a C1-6 alkyl group.
Treatment method by administering formula (I) compound, prodrug, or pharmaceutically acceptable salt
A method for treating Down's syndrome, brain cancer, lung cancer, breast cancer, or Alzheimer's disease comprising administering a compound expressed by formula (I) or a prodrug of the compound or a pharmaceutically acceptable salt of the compound to a subject in need thereof, with the same formula (I) structural definitions for R1, R2, R3, and R4.
Overall, the claim coverage centers on formula-based compound definitions, including prodrug and pharmaceutically acceptable salt coverage and formula (III) variants, and on therapeutic use by administering those compounds to treat Down’s syndrome, specified cancers, and Alzheimer’s disease.
Stated Advantages
Intracerebral transferability.
Oral absorbability.
Inhibition of abnormal phosphorylation of tau and APP to reduce amyloid-β production is described.
Additional phosphoenzyme/receptor-tyrosine-kinase related effects are described for tumor treatment.
Documented Applications
Preventing, improving, inhibiting development of, and/or treating neuropsychological disorders, including Down’s syndrome and Alzheimer’s disease.
Preventing, improving, inhibiting development of, and/or treating malignant tumors, including a brain tumor and multiple named cancers.
Treatment by administering the compound family to a subject in need for Down’s syndrome, brain cancer, lung cancer, breast cancer, or Alzheimer’s disease.
Interested in licensing this patent?