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Fused pyrimidineone compounds as trpv3 modulators
专利权人:
GLENMARK PHARMACEUTICALS S.A.
发明人:
KATTIGE VIDYA G.,THOMAS ABRAHAM,KHAIRATKAR-JOSHI NEELIMA,LINGAM V.S. PRASADORAO,CHAUDHARI SACHIN SUNDARLAL
申请号:
NZ59577809
公开号:
NZ595778A
申请日:
2009.04.15
申请国别(地区):
NZ
年份:
2014
代理人:
摘要:
595778 Disclosed are 7-[2-aryl-vinyl]-6-(aryl)-[1,3]thiazolo[3,2-a]pyrimidin-5-one derivatives as represented by the general formula (I), wherein X is O, S or NRb Y is CR3 or N ring A is aryl, heterocyclyl or heteroaryl R1 and R3, are each independently selected from hydrogen, halogen, nitro, cyano, -COOH, substituted or unsubstituted alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, cycloalkenyl, aryl, heteroaryl, heterocyclic group, -NR4R5, -S(O)pNR4R5 and -S(O)pR4 or R1 and R3 together with the carbon atoms to which they were attached may form a 5 to 7 membered cyclic ring, which may be substituted or unsubstituted, saturated, unsaturated or partially saturated, which cyclic ring may optionally contain one or more heteroatoms selected from O, NRb and S R2 is aryl, heteroaryl, or heterocyclic group, each of which may be optionally mono- or polysubstituted with substituent(s) independently selected from the group consisting of halogen, hydroxyl, nitro, cyano, -COOH, -NR4R5, acyl, substituted or unsubstituted alkyl, alkenyl, alkoxy, cyanoalkoxy, haloalkyl, haloalkyloxy, cycloalkyl, cycloalkylalkyl, cycloalkylalkoxy, aryl, heterocyclic group and heteroaryl and wherein the remaining substituents are as defined herein. Representative compounds include 7-{ (E)-2-[2-(cyclopropylmethoxy)-3-methoxyphenyl]-1-ethenyl} -6-(4-trifluoromethoxy-phenyl)-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one, 7-[(E)-2-(2-hydroxy-3-methoxyphenyl)-1-ethenyl]-6-[4-(trifluoromethoxy)phenyl]-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one, 7-[(E)-2-{ (2,3-dihydroxy)phenyl} -1-ethenyl]-6-(4-trifluoromethoxy-phenyl)-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one and 7-{ (E)-2-[2-cyclopropylmethoxy-3-hydroxyphenyl]-1-ethenyl} -6-(4-trifluoromethoxyphenyl)-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one or a pharmaceutically acceptable salt thereof. Further disclosed is a pharmaceutical composition comprising a compound as defined above and a pharmaceutically acceptable carrier or diluent for the treatement of pain, acute pain, chro
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