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Heterocyclic derivative as a microsomal prostaglandin E synthase inhibitor (mPGES)
专利权人:
Nippon Shinyaku Co.; Ltd.
发明人:
OTSU, Hironori
申请号:
ES12823510
公开号:
ES2561105T3
申请日:
2012.08.17
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A heterocyclic derivative represented by the general formula [1]: ** Formula ** or its tautomer or a pharmaceutically acceptable salt thereof, wherein ring A is a group represented by the general formulas [2], [3] or [ 4]: ** Formula ** wherein X1 is NH, N-alkyl or O; A1 is hydrogen or alkyl; A2 is i) hydrogen; ii) halogen; iii) alkyl optionally substituted with one to three groups selected from the group consisting of halogen, amino, monolakylamino, dialkylamino, carbamoyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, a saturated cyclic aminocarbonyl, alkoxy, alkoxyalkoxy and alkylcarbonyloxy; iv) cycloalkyl optionally substituted with alkyl optionally substituted with one to three halogens; v) alkoxy; vi) a saturated heterocycle group optionally substituted with alkyl, alkyloxycarbonyl, alkylcarbonyl or oxo; vii) alkylthio; viii) alkylsulfonyl; ix) alkylsulfinyl; x) a group represented by the general formula [5]: ** Formula ** wherein R3 and R4 are the same or different group selected from: a) hydrogen; b) alkyl optionally substituted with a group selected from the group consisting of monoalkylamino, dialkylamino, a saturated cyclic amino optionally substituted with alkyl, a saturated heterocycle group optionally substituted with alkyl, alkoxy, hydroxycarbonyl, hydroxyl, alkyloxycarbonyl, and alkylthio, oc) cycloalkyl ; or xi) a saturated cyclic amino optionally substituted with alkyl, amino, monoalkylamino, dialkylamino, alkoxy or hydroxy; R1 is phenyl, benzyl, naphthyl, cycloalkyl, cycloalkylmethyl, heteroaryl, heteroarylmethyl, 1,2,3,4-tetrahydronaphthalen-5-yl, 1,2,3,4-tetrahydronaphthalen-6-yl, 2,3-dihydro- 1H-inden-4-yl, 2,3-dihydro-1H-inden-5-yl, 1,2-dihydrocyclobutabencen-3-yl, 1,2-dihydrocyclobutabencen-4-yl or alkyl, wherein said phenyl, benzyl , cycloalkyl, cycloalkylmethyl, heteroaryl, and heteroarylmethyl is optionally substituted with one to three groups selected from the group consisting of i) halogen, ii) alkyl optionally substituted with one to t
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