Pyrimidone derivatives
AssigneeMitsubishi Chemical Corporation
InventorsKazutoshi Watanabe, Ryoichi Ando, Ken-ichi Saito, Rie Kawamoto, Aya Shoda
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Abstract
A pyrimidone derivative represented by the formula (I) or a salts thereof: wherein R1 represents an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group and the like; R2 represents a hydrogen atom, hydroxyl group, an alkyl group, an alkenyl group and the like, R3 represents a pyridyl group, and a medicament comprising said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as Alzheimer disease.
Claims14
A pyrimidone compound represented by formula (I) or a pharmaceutically acceptable salt thereof:
- wherein
- R1 represents a group represented by —N(R4)—W—R5 wherein
- R4 represents a hydrogen atom;
- R5 represents a C1–C18 alkyl group which may be substituted, a C3–C18 alkenyl group which may be substituted, a C3–C18 alkynyl group which may be substituted, a C3–C8 cycloalkyl group which may be substituted, or a C6–C14 aryl group which may be substituted, and
- symbol “W” represents a single bond, a carbonyl group, a sulfonyl group, NH or a nitrogen atom substituted with a C1–C18 alkyl group which may be substituted;
- R2 represents a hydrogen atom;
- and
- R3 represents a 4-pyridyl group which may be substituted.
A pyrimidone compound represented by formula (I) or a pharmaceutically acceptable salt thereof:
- wherein R1 represents a group represented by —N(R4)—W—R5 wherein
- R4 represents a hydrogen atom, a C1–C18 alkyl group which may be substituted, a C3–C18 alkenyl group which may be substituted, a C3–C18 alkynyl group which may be substituted, a C3–C8 cycloalkyl group which may be substituted, or a C6–C14 aryl group which may be substituted,
- R5 represents an alkyl group which may be substituted, said alkyl group being one of ethyl group, n-propyl group, isopropyl group, n-butyl group, isobutyl group, sec-butyl group, tert-butyl group, n-pentyl group, isopentyl group, neopentyl group, 1,1-dimethylpropyl group, n-hexyl group, isohexyl group, a linear or branched heptyl group, octyl group, nonyl group, decyl group, undecyl group, dodecyl group, tridecyl group, tetradecyl group, pentadecyl group or octadecyl group, a C3–C18 alkenyl group which may be substituted, a C3–C18 alkynyl group which may be substituted, a C3–C8 cycloalkyl group which may be substituted, or a C6–C14 aryl group which may be substituted, and
- symbol “W” represents a single bond, a carbonyl group, a sulfonyl group, NH or a nitrogen atom substituted with a C1–C18 alkyl group which may be substituted;
- R2 represents a hydrogen atom or a halogen atom;
- and
- R3 represents a 4-pyridyl group which may be substituted.
A pyrimidone compound which is selected from the group consisting of:
- 2-(N-phenylamino)-6-(4-pyridyl)pyrimidin-4-one,
- 2-(N,N-diethylamino)-6-(4-pyridyl)pyrimidin-4-one,
- 2-(N,N-dipropylamino)-6-(4-pyridyl)pyrimidin-4-one,
- 2-(N-benzylamino)-6-(4-pyridyl)pyrimidin-4-one,
- 2-(N-benzyl-N-methylamino)-6-(4-pyridyl)pyrimidin-4-one,
- 2-(N-(3-bromophenyl)amino)-6-(4-pyridyl)pyrimidin-4-one,
- 2-(N-(4-ethylphenyl)amino)-6-(4-pyridyl)pyrimidin-4-one,
- 2-(N-(3-methoxyphenyl)amino)-6-(4-pyridyl)pyrimidin-4-one,
- 2-(N-cyclohexylmethylamino)-6-(4-pyridyl)pyrimidin-4-one, and
- 2-(N-isobutyl-N-methylamino)-6-(4pyridyl)pyrimidin-4-one,
- or a pharmaceutically acceptable salt thereof.
A method for therapeutic treatment of Alzheimer disease, which comprises administering to a patient a therapeutically effective amount of a substance selected from a pyrimidone compound represented by formula (I) or a pharmaceutically acceptable salt thereof:
- wherein
- R1 represents a group represented by —N(R4)—W—R5 wherein
- R4 and R5 independently represent a hydrogen atom, a C1–C18 alkyl group which may be substituted, a C3–C18 alkenyl group which may be substituted, a C3–C18 alkynyl group which may be substituted, a C3–C8 cycloalkyl group which may be substituted, or a C6–C14 aryl group which may be substituted, and
- symbol “W” represents a single bond, a carbonyl group, a sulfonyl group, NH or a nitrogen atom substituted with a C1–C18 alkyl group which may be substituted;
- R2 represents a hydrogen atom or a halogen atom;
- and
- R3 represents a pyridyl group which may be substituted.
Dependencies are inferred from the claim text.