Substituted...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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Details

C514S221000, C514S259100, C544S279000, C544S281000

Reexamination Certificate

active

10490135

ABSTRACT:
The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a hydroxyiminomethylene group, a dioxolan group, a nitrogen atom being optionally substituted; or a methylene group optionally substituted; or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring optionally substituted; R2 may represent a C1-6alkyl group optionally; a C3-6cycloalkyl group, a C1-4alkythio group, a C1-4alkoxy group, a C1-2perhalogenated alkyl group, a C1-3halogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; R3 and R4 represent, each independently, a hydrogen atom, a C1-6alkyl group, a hydroxy group, a C1-4alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C1-6alkyl group or a halogen atom; with the proviso that when R3 and R4 represent each a hydrogen atom then R5 is not a hydrogen atom. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β or GSK3β, and cdk5/p25, such as Alzheimer disease

REFERENCES:
patent: 6974819 (2005-12-01), Garcia et al.
patent: WO 98/16528 (1998-04-01), None
patent: WO 98/24780 (1998-06-01), None
patent: WO 99/65897 (1999-12-01), None
patent: WO 00/18758 (2000-04-01), None
patent: WO 01/42224 (2001-06-01), None
patent: WO 01/44246 (2001-06-01), None
Leclerc, et al. (“Indirubins Inhibit Glycogen Synthase Kinase-3β and CDK5/P25, Two Protein Kinases Involved in Abnormal Tau Phosphorylation in Alzheimer's Disease,” The Journal of Biological Chemistry, 276, No. 1, Jan. 2, 2001, pp. 251-260).
Bhat, et al. (“Glycogen Synthase Kinase 3: A Drug Target for CNS Therapies,” Journal of Neurochemistry, 2004, 89, 1313-1317).
Souillac, et al., Characterization of Delivery Systems, Differential Scanning Calorimetry, pp. 217-221 (in Encyclopedia of Controlled Drug Delivery, 1999, John Wiley & Sons, pp. 212-227).
Derivative (chemistry), retriieved from “http://en.wikipedia.org/wiki/Derivative-%28chemistry%29” on Aug. 10, 2006.
List of neurodegenerative diseases; from the University of California, Nov. 2006.
List of neurodegenerative diseases; from Wikipedia, Nov. 2006.
Harwood, PubMed abstract of Curr. Mol. Med., Aug. 2003; 3(5): 472-82.

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