ARIGON JEROME,JEROME ARIGON,BROLLO MAURICE,MAURICE BROLLO,COMBET ROMAIN,ROMAIN COMBET,DURAND FLORENCE,FLORENCE DURAND,EL AHMAD YOUSSEF,YOUSSEF EL AHMAD,LABROSSE JEAN ROBERT,JEAN ROBERT LABROSSE,LETALL
申请号：
FR1061197
公开号：
FR2969613A1
申请日:
2010.12.23
申请国别(地区):
FR
年份:
2012
代理人:
摘要：
Tetrahydro-pyrimido{1,2-a}pyrimidin-6-one compounds (I) and their racemic forms, enantiomers, diastereoisomers, and addition salts with mineral and organic acids or bases are new. Tetrahydro-pyrimido{1,2-a}pyrimidin-6-one compounds of formula (I) and their racemic forms, enantiomers, diastereoisomers, and addition salts with mineral and organic acids or bases are new. p : 0 or 1； q : 1 or 2, provided that if p is 0 then q is 2, and if p is 1 then q is 1； R1 : 1-7C alkyl, 1-7C alkenyl or 1-7C alkynyl, 1-7C cycloalkyl or 1-7C heterocycloalkyl group (all optionally substituted by one or more halo, R7, -S(O) x-R7, -SO 2NR5R7, -CN, -OR5, -NR5R6, -NR5-COR7, -NR5-CO 2-R7, -NR5-SO 2-R7, -NHCONR5R6, -COR7, -CO 2R5 or CONR5R6)； x : 0-2； either R2 : H, alkyl group or cycloalkyl group； and R3 : alkyl, cycloalkyl or phenyl optionally substituted by halo or OR5, or -NR5R6； or CR2R3 : 3-10 membered cyclic group (optionally one or more other heteroatoms comprising O, S or NR5), which group is optionally substituted by one or more halo, oxo, R5, -OR5 or -NR5R6； R4 : H, alkyl, halo or CN； R5, R6 : H, alkyl, cycloalkyl or heterocycloalkyl； R7 : alkyl, cycloalkyl or heterocycloalkyl, where the alkyl, cycloalkyl, or heterocycloalkyl in R5, R6 and R7 is optionally substituted by one or more halo, -OR8 or -NR8R9； and R8, R9 : H, alkyl, cycloalkyl or heterocycloalkyl. Independent claims are included for: (1) the preparation of (I)； and (2) intermediates comprising 6-hydroxy-3H-pyrimidin-4-one compound of formula (D), 6-chloro-3H-pyrimidin-4-one compound of formula (E), 6-morpholin-4-yl-3H-pyrimidin-4-one compound of formula (F) and 6-chloro-3H-pyrimidin-4-one compound of formula (J). [Image] [Image] ACTIVITY : Cytostatic； Vasotropic； Antiinflammatory； Metabolic； Antiallergic； Antiasthmatic； Anticoagulant； Thrombolytic； Neuroprotective； Ophthalmological； Antipsoriatic； Antiarthritic； Antirheumatic； Antidiabetic； Muscular-Gen. MECHANISM OF ACTION : Vps34 inhibitor. The ability of (I) to inhi
