Pyrazole Compound
OwnerTetsuya Tsukamoto, Takeshi Yamamoto +5inventors
InventorsTetsuya Tsukamoto, Takeshi Yamamoto, Ryosuke Tokunoh, Tomohiro Kawamoto, Masahiro Okura, Masakumi Kori, Katsuhito Murase
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Abstract
The present invention provides a pyrazole compound represented by the formula (I): wherein ring A0 is a pyrazole ring optionally further having 1 or 2 substituents; Ra is a substituted carbamoyl group; and Rb is an optionally substituted acylamino group, or a salt thereof or a prodrug thereof, which is useful as an agent for the prophylaxis or treatment of GSK-3β related pathology or disease, and a GSK-3β inhibitor including same.
Claims33
A compound represented by the formula
- wherein
- ring A0 is a pyrazole ring optionally further having 1 or 2 substituents;
- Ra is a substituted carbamoyl group;
- and
- Rb is an optionally substituted acylamino group] or a salt thereof, excluding the following compounds;
- 1) N-methyl-2,5-dimethyl-4-{2-[4-(4-nitrophenoxy)phenyl]acetylamino}-2H-pyrazole-3-carboxamide,
- 2) N-methyl-4-{2-[4-(4-chlorophenoxy)phenyl]acetylamino}-2,5-dimethyl-2H-pyrazole-3-carboxamide,
- 3) N-(9-methyl-4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-3-yl)-4-acetylamino-2,5-dimethyl-2H-pyrazole-3-carboxamide,
- 4) N-phenyl-4-benzoylamino-2-ethyl-5-methyl-2H-pyrazole-3-carboxamide,
- 5) N-phenyl-2-ethyl-5-methyl-4-(2-nitrobenzoylamino)-2H-pyrazole-3-carboxamide,
- 6) N-(4-chlorophenyl)-2-ethyl-5-methyl-4-(4-nitrobenzoylamino)-2H-pyrazole-3-carboxamide,
- 7) N-phenyl-2-ethyl-5-methyl-4-(4-methylbenzoylamino)-2H-pyrazole-3-carboxamide,
- 8) N-methyl-N-(2-phenyl-2H-pyrazol-3-yl)-4-acetylamino-2-ethyl-5-methyl-2H-pyrazole-3-carboxamide,
- 9) N-methyl-N-(5-methyl-2-phenyl-2H-pyrazol-3-yl)-4-acetylamino-2-ethyl-5-methyl-2H-pyrazole-3-carboxamide,
- 10) N-methyl-N-(2-methyl-2H-pyrazol-3-yl)-4-acetylamino-2-ethyl-5-methyl-2H-pyrazole-3-carboxamide,
- 11) N-(2,5-dimethyl-2H-pyrazol-3-yl)-N-methyl-4-acetylamino-2-ethyl-5-methyl-2H-pyrazole-3-carboxamide,
- 12) N-(4-tert-butylbenzyl)-4-acetylamino-2,5-dimethyl-2H-pyrazole-3-carboxamide,
- 13) N-(4-tert-butylbenzyl)-4-(2-chloroacetylamino)-2,5-dimethyl-2H-pyrazole-3-carboxamide,
- 14) N-(4-tert-butylbenzyl)-4-benzoylamino-2,5-dimethyl-2H-pyrazole-3-carboxamide,
- 15) N,N-dimethyl-4-methanesulfonylamino-1-methyl-5-[1-methyl-2,5-dioxo-4-(1-phenylpropylamino)-2,5-dihydro-1H-pyrrol-3-ylamino]-1H-pyrazole-3-carboxamide,
- 16) N,N-dimethyl-5-[2,5-dioxo-4-(1-phenylpropylamino)-2,5-dihydro-1H-pyrrol-3-ylamino]-4-methanesulfonylamino-1-methyl-1H-pyrazole-3-carboxamide,
- 17) N,N-dimethyl-5-(4-chloro-1-methyl-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-ylamino)-4-methanesulfonylamino-1-methyl-1H-pyrazole-3-carboxamide,
- 18) N,N-dimethyl-5-(4-chloromethyl-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-ylamino)-4-methanesulfonylamino-1-methyl-1H-pyrazole-3-carboxamide.
A GSK-3β inhibitor comprising a compound represented by the formula:
- wherein
- ring A0 is a pyrazole ring optionally further having 1 or 2 substituents;
- Ra is substituted carbamoyl;
- and
- Rb is optionally substituted acylamino,
- or a salt thereof or a prodrug thereof.
A method of inhibiting GSK-3β comprising administering a compound represented by the formula:
- wherein
- ring A0 is a pyrazole ring optionally further having 1 or 2 substituents;
- Ra is substituted carbamoyl;
- and
- Rb is optionally substituted acylamino,
- or a salt thereof or a prodrug thereof to a subject.
A method of promoting neural stem cell differentiation comprising administering a compound represented by the formula:
- wherein
- ring A0 is a pyrazole ring optionally further having 1 or 2 substituents;
- Ra is substituted carbamoyl;
- and
- Rb is optionally substituted acylamino,
- or a salt thereof or a prodrug thereof to a subject.
A method of preventing or treating a neurodegenerative disease or diabetes comprising administering a compound represented by the formula:
- wherein
- ring A0 is a pyrazole ring optionally further having 1 or 2 substituents;
- Ra is substituted carbamoyl;
- and
- Rb is optionally substituted acylamino,
- or a salt thereof or a prodrug thereof to a subject.
A method of lowering blood glucose comprising administering a compound represented by the formula:
- wherein
- ring A0 is a pyrazole ring optionally further having 1 or 2 substituents;
- Ra is substituted carbamoyl;
- and
- Rb is optionally substituted acylamino,
- or a salt thereof or a prodrug thereof to a subject.
29-32. (canceled)
Dependencies are inferred from the claim text.