首页> 外国专利> SUBSTITUTED PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEURODEGENERATIVE OR NEUROLOGICAL DISORDERS OF THE CENTRAL NERVOUS SYSTEM

SUBSTITUTED PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEURODEGENERATIVE OR NEUROLOGICAL DISORDERS OF THE CENTRAL NERVOUS SYSTEM

机译:取代的嘧啶衍生物,其制备及其在中枢神经系统神经退行性疾病或神经疾病中的应用

摘要

The present invention relates to novel derivatives of a series of substitutedpyrimidines of formula (I); wherein W is O, CH2, CH2CH2, OCH2, CH2CH2CH2, or abond; R1 is a hydroxyC1-6alkyloxyC1-6alkylamino, diC1-6alkylamino (wherein thealkyl groups may be the same or different), aminoC1-6alkylamino, morpholino,piperidino, piperazino, piperazinoamino, homopiperazino, homopiperidino,homomorpholino, benzoxazino, indolino, 1,2,3,4-tetrahydroquinolino,benzylamino or anilino wherein C or N atoms may be substituted with one ormore substituents; R2 is selected from the group consisting of H; halogen; N3;OR; SR; C1-6alkyl; C6-10aryl; C6-10arylC1-6alkyl; C6-10heteroaryl; NR7R8;N=C(R11)N(R6)2; aziridino; azetidino; pyrrolidino; piperidino;hydroxypiperidino; heptamethyleneimino; piperazino; N-substituted piperazino;homopiperazino; N-substituted homopiperazino; morpholino; homomorpholine;thiomorpholino; and R12C(O)C1-6alkyl; C-substituted piperidino; X is a C6-10aryl ring or a C6-10 heteroaryl ring optionally substituted with one or moresuitable substituents for an aryl ring; R is H, C1-6alkyl, C3-8cycloalkyl, C6-10aryl or C6-10arylC1-6alkyl; provided that when -W-X is benzyl, R1 is notpiperidine; and when R1 is a hydroxyalkyloxyalkylamino, R2 is not aheterocyclic ring; and to pharmaceutical compositions which contain them, tomethods for their preparation and to their use in therapy, particularly in thetreatment of neurodegenerative or other neurological disorders of the centraland peripheral systems.
机译:本发明涉及一系列取代的新衍生物式(I)的嘧啶;其中W是O,CH2,CH2CH2,OCH2,CH2CH2CH2或键; R1是羟基C1-6烷氧基C1-6烷基氨基,二C1-6烷基氨基(其中烷基可以相同或不同),氨基C1-6烷基氨基,吗啉代,哌啶子基,哌嗪子基,哌嗪子基氨基,高哌嗪子基,高哌啶子基,同吗啉代,苯并恶嗪,吲哚诺,1,2,3,4-四氢喹啉,其中C或N原子可被一个或多个取代的苄氨基或苯胺基更多取代基; R2选自由H组成的组;卤素; N3;要么; SR; C 1-6烷基; C6-10芳基; C6-10芳基C1-6烷基; C6-10杂芳基; NR7R8;N = C(R11)N(R6)2;阿齐利迪诺阿塞季迪诺吡咯烷哌啶子基羟基哌啶子七亚甲基亚氨基;胡椒N-取代的哌嗪子;同哌嗪N-取代的高哌嗪子;吗啉代同吗啉硫吗啉代; R 12 C(O)C 1-6烷基; C-取代的哌啶子基; X是C6-任选被一个或多个取代的10芳基环或C6-10杂芳基环芳基环的合适取代基; R为H,C 1-6烷基,C 3-8环烷基,C 6-10芳基或C6-10芳基C1-6烷基;前提是-W-X为苄基时,R1不是哌啶;当R1为羟烷基氧基烷基氨基时,R2不为杂环以及含有它们的药物组合物,以制备方法及其在治疗中的用途,尤其是在中枢神经退行性疾病或其他神经系统疾病的治疗和外围系统。

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