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Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators
专利权人:
Janssen Pharmaceutica; N.V.
发明人:
BISCHOFF, François,VELTER, Adriana,ROMBOUTS, Frederik,DE CLEYN, Michel,VAN BRANDT, Sven,GIJSEN, Henricus,ZAVATTARO, Chiara,VAN DEN KEYBUS, Frans
申请号:
ES14701007
公开号:
ES2612215T3
申请日:
2014.01.16
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of formula (I) ** Formula ** a tautomer or a stereoisomeric form thereof, wherein R1 is Ar1 or Ar2; R 2 is hydrogen, phenyl, C 3-7 cycloalkyl, 3,4,5,6-tetrahydropyranyl, 3,4,5,6-tetrahydrothiopyranyl, piperidinyl, or C 1-4 alkyl optionally substituted with one or more substituents each independently selected from the group that it consists of halo, hydroxyl, C1-4 alkyloxy and NR7R8; Z is methylene or 1,2-ethanediyl, in which methylene or 1,2-ethanediyl is optionally substituted with one or two C1-4 alkyl substituents; L is a covalent bond, 1,2-cyclopropanediyl, -C (>; = O) -C 1-6 alkanediyl, optionally substituted C 1-6 alkanediyl with one or more substituents selected from the group consisting of 3,4,5,6-tetrahydropyranyl , phenyl and C 1-4 alkyloxyC 1-4 alkyl, or C 1-6 alkanediyl in which two geminal hydrogen atoms are replaced by C 2-6 alkanediyl; Ar1 is a ring system selected from the group consisting of imidazolyl, 1,2,4-triazolyl, 1,3,4-triazolyl, pyrrolyl, furanyl, isoxazolyl, isothiazolyl, thienyl, thiazolyl, pyrrolidinyl, piperidinyl, pyrazolyl, 4, 5,6,7-tetrahydrobenzo [b] thienyl, 1,2-benzisoxazolyl, benzofuranyl, 2,3-dihydrobenzofuranyl, 1,3-dihydro-isobenzofuranyl, 5,6,7,8-tetrahydro-1,2,4- triazolo [4,3-a] pyridinyl, 4,5,6,7-tetrahydro-pyrazolo [1,5-a] pyridinyl, 1,2,4-triazolo [4,3-a] pyridinyl, pyrazolo- [1 , 5-a] pyridinyl, 3,4-dihydro-1-benzopyranyl, 1,2-benzothiazolyl, indazolyl, 1,2,3,4-tetrahydro-isoquinolinyl, 2,3-dihydro-benzo [b] thienyl, 1 , 3-dihydro-benzo [c] thienyl, 2-benzofuranyl, 3,4-dihydro-2-benzothiopyranyl, 3,4-dihydro-2- benzopyranyl and 1,2,3,4-tetrahydroquinolinyl; wherein said ring system is optionally substituted with one or more substituents each independently selected from the group consisting of halo, oxo, Ar3, R0, C1-4alkyl optionally substituted with one or more substituents each selected independently from the group consisting in halo, C 1-4 alkyloxy and C 3-7 cycloalkyl, and C 1-4 alkyloxy optionally substi
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