SUBSTITUTED 8 -PYRIDINYL-DIHYDROSPIRO- CYCLOALKYL -PYRIMIDO 1,2-a PYRIMIDIN-6-ONE AND 8 -PYRIMIDIN YL-DIHYDROSPIRO- CYCLOALKYL -PYRIMIDO 1,2-a PYRIMIDIN-6-ONE DERIVATIVES AND THEIR USE AGAINST NEUROGENERATIVE DISEASES
申请人:Sanofi-Aventis
公开号:EP1603915A1
公开(公告)日:2005-12-14
US7414030B2
申请人:——
公开号:US7414030B2
公开(公告)日:2008-08-19
[EN] SUBSTITUTED 8'-PYRIDINYL-DIHYDROSPIRO-[CYCLOALKYL]-PYRIMIDO [1,2-a] PYRIMIDIN-6-ONE AND 8'-PYRIMIDINYL-DIHYDROSPIRO-[CYCLOALKYL]-PYRIMIDO [1,2-a] PYRIMIDIN-6-ONE DERIVATIVES AND THEIR USE AGAINST NEUROGENERATIVE DISEASES<br/>[FR] DERIVES DE 8'-PYRIDINYL-DIHYDROSPIRO-(CYCLOALKYL)-PYRIMIDO (1,2-A) PYRIMIDIN-6-ONE ET DE 8'-PYRIMIDINYL-DIHYDROSPIRO-(CYCLOALKYL)-PYRIMIDO (1,2-A) PYRIMIDIN-6-ONE SUBSTITUES ET UTILISATION DE CES DERIVES CONTRE LES MALADIES NEURODEGENERATIVES
申请人:SANOFI SYNTHELABO
公开号:WO2004078760A1
公开(公告)日:2004-09-16
The invention relates to a dihydrospiro-[cycloalkyl]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, a carbonyl group, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; m represents 1 to 4 n represent 0 to 3 p represents 0 to 2 q represents 0 to 2, p+ q being inferior to 4. 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, such as Alzheimer disease.
The present invention discloses compounds of formulaes I, II, III, or IV, or a 5 racemate, enantiomer, regioisomer, salt, ester or prodrug thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.