
基本信息:
- 专利标题: NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
- 专利标题(中):磷酸二酯酶类型10A的新型抑制剂化合物
- 申请号:US13660524 申请日:2012-10-25
- 公开(公告)号:US20130116241A1 公开(公告)日:2013-05-09
- 发明人: Hervé Geneste , Michael Ochse , Karla Drescher , Sean Turner , Berthold Behl , Loic Laplanche , Jürgen Dinges , Clarissa Jakob , Lawrence Black
- 申请人: Abbott GmbH & Co. KG , AbbVie Inc.
- 申请人地址: US IL North Chicago DE Wiesbaden
- 专利权人: AbbVie Inc.,Abbott GmbH & Co. KG
- 当前专利权人: AbbVie Inc.,Abbott GmbH & Co. KG
- 当前专利权人地址: US IL North Chicago DE Wiesbaden
- 主分类号: C07D495/04
- IPC分类号: C07D495/04 ; C07D471/04 ; C07D417/14
摘要:
The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. wherein Q is O or S, X1 is N or CH, X2 is N or C—R7; X3 is O, S—X4═C(R8)—, where C(R8) is bound to the carbon atom which carries R2, or —X5═C(R9)—, where X5 is bound to the carbon atom which carries R2; X4 is N or C—R9; X5 is N; Het is selected from optionally substituted phenyl, monocyclic hetaryl and fused bicyclic hetaryl; R1 is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkylsulfanyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkoxy, the moiety Y1-Cyc1; R2 is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkoxy, C2-C4-alkenyloxy, etc; A represents one of the following groups A1, A2, A3, A4 or A5: where * indicates the points of attachment to Het and to the nitrogen atom, respectively; and where R3 to R9, R3e, R3f, A′, Y1 and Cyc1 are defined in the claims.
摘要(中):
本发明涉及式I的新型化合物,其是10A型磷酸二酯酶的抑制剂及其用于制备药物的用途,因此其适用于治疗或控制选自神经障碍和精神疾病的医学病症,用于改善 与这些疾病相关的症状并降低这种疾病的风险。 其中Q为O或S,X1为N或CH,X2为N或C-R7; X3为O,S-X4 = C(R8) - ,其中C(R8)与携带R2的碳原子结合,或-X5 = C(R9) - ,其中X5与携带R2的碳原子结合 ; X4是N或C-R9; X5是N; Het选自任选取代的苯基,单环杂芳基和稠合双环杂芳基; R1特别选自氢,卤素,OH,C 1 -C 4 - 烷基,三甲基甲硅烷基,C 1 -C 4烷基硫烷基,C 1 -C 4 - 烷氧基-C 1 -C 4烷基,C 1 -C 4 - 烷氧基,C 1 -C 4烷氧基 - C1-C4-烷氧基,Y1-Cyc1部分; R2选自氢,卤素,OH,C 1 -C 4 - 烷基,三甲基甲硅烷基,C 1 -C 4 - 烷氧基-C 1 -C 4 - 烷基,C 1 -C 4 - 烷氧基,C 1 -C 4 - 烷氧基-C 1 -C 4烷氧基, C2-C4-烯氧基等; A代表以下组A1,A2,A3,A4或A5:其中*表示分别与Het和氮原子相连的点; 并且在权利要求中定义R3至R9,R3e,R3f,A',Y1和Cyc1。
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D495/00 | 杂环化合物,在稠环系中至少有1个杂环具有硫原子作为仅有的杂环原子 |
--------C07D495/02 | .在稠环系中含有两个杂环 |
----------C07D495/04 | ..邻位稠合系 |