首页> 外国专利> NEW PYRIMIDINE DERIVATIVES AND THEIR APPLICATION IN THERAPY, AND ALSO APPLICATION OF PYRIMIDINE DERIVATIVES IN THE PRODUCTION OF A MEDICINE FOR THE PREVENTION AND / OR TREATMENT OF ALZHEIMER'S DISEASE

NEW PYRIMIDINE DERIVATIVES AND THEIR APPLICATION IN THERAPY, AND ALSO APPLICATION OF PYRIMIDINE DERIVATIVES IN THE PRODUCTION OF A MEDICINE FOR THE PREVENTION AND / OR TREATMENT OF ALZHEIMER'S DISEASE

机译:新的嘧啶衍生物及其在治疗中的应用,以及嘧啶衍生物在生产用于预防和/或治疗老年痴呆症的药物中的应用

摘要

1. The use of the compounds of formula I:! ! where R1 is selected from hydrogen, halogen, cyano, NO2, C1-3 alkyl, C1-3 haloalkyl, ORa, SO2NRbRc, C0-2alkylC (O) NRbRc, C1-4alkylNRbRc, CH2ORh, SO2Ri, C (O) ORa, CH (OH ) Rj and C (O) Rj; ! R2 and R4 are independently selected from hydrogen, halogen, cyano, NO2, C1-4 alkyl, C1-3 haloalkyl, ORa, SO2NRbRc, C (O) NRbRc, CH2NRbRc, CH2ORh, SO2Ri, C (O) ORa and C (O) Rj ; or ! R1 and R2 together with the atoms to which they are attached are connected to form a 5- or 6-membered heterocyclic ring containing at least one N, O or S, moreover, any of the hydrogen atoms of the CH2 groups in the specified heterocyclic ring can be replaced by oxo , hydroxy or halogen, and any sulfur atom in said heterocyclic ring is optionally oxidized to —SO2—; ! R3 and R5 are independently selected from hydrogen, halo, cyano, C1-3 alkyl, C1-3 haloalkyl, and ORa; ! R6 is selected from CH3 and C6 alkyl, C6 alkenyl, C6 alkynyl and C6 haloalkyl; or ! R6 is a 6 membered heterocyclic ring containing one or more heteroatoms selected from N, O or S, which is optionally substituted with one or more C1-3 alkyl or C1-3 haloalkyl, which are optionally further substituted with one or more C1 -3 alkoxy; ! R7 is selected from hydrogen, C1-3 alkyl, cyano and C1-3 haloalkyl, where indicated! C1-3 alkyl or C1-3 haloalkyl is optionally substituted with one or more than one ORa; ! R8 and R9 are independently selected from hydrogen, cyano and halogen; ! Ra is selected from hydrogen, C1-3 alkyl and C1-3 haloalkyl, wherein said C1-3 alkyl or C1-3 haloalkyl is optionally substituted with one or more C1-3 alkoxy; ! Rb and Rc are independently selected from hydrogen, C1-6 alkyl, heterocyclyl, aryl, heteroaryl, and C1-6 haloalkyl, wherein said C1-6 alkyl, heterocyclyl, aryl, heteroaryl, or C1-6 gal
机译:1.式I化合物的用途:! !其中R1选自氢,卤素,氰基,NO2,C1-3烷基,C1-3卤代烷基,ORa,SO2NRbRc,C0-2烷基C(O)NRbRc,C1-4烷基NRbRc,CH2ORh,SO2Ri,C(O)ORa,CH (OH)Rj和C(O)Rj; ! R 2和R 4独立地选自氢,卤素,氰基,NO 2,C 1-4烷基,C 1-3卤代烷基,OR a,SO 2 NR b R c,C(O)NR b R c,CH 2 NR b R c,CH 2 ORh,SO 2 R 1,C(O)ORa和C(O )Rj;要么 ! R 1和R 2与它们所连接的原子一起连接形成5或6元杂环,该杂环含有至少一个N,O或S,并且还具有特定杂环中CH 2基团的任何氢原子环可以被氧代,羟基或卤素取代,并且所述杂环中的任何硫原子任选地被氧化为-SO 2-; ! R3和R5独立地选自氢,卤素,氰基,C1-3烷基,C1-3卤代烷基和ORa; ! R6选自CH3和C6烷基,C6烯基,C6炔基和C6卤代烷基;要么 ! R 6是含有一个或多个选自N,O或S的杂原子的6元杂环,其任选地被一个或多个C 1-3烷基或C 1-3卤代烷基取代,其任选地被一个或多个C 1-3取代烷氧基! R 7选自氢,C 1-3烷基,氰基和C 1-3卤代烷基,如果有说明! C1-3烷基或C1-3卤代烷基任选地被一个或多个一个ORa取代; ! R8和R9独立地选自氢,氰基和卤素; ! Ra选自氢,C 1-3烷基和C 1-3卤代烷基,其中所述C 1-3烷基或C 1-3卤代烷基任选地被一个或多个C 1-3烷氧基取代; ! Rb和Rc独立地选自氢,C1-6烷基,杂环基,芳基,杂芳基和C1-6卤代烷基,其中所述C1-6烷基,杂环基,芳基,杂芳基或C1-6gal

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