基本信息:
- 专利标题: PYRROLIDINE DERIVATIVES AS NK3 ANTAGONISTS
- 专利标题(中):吡咯啉衍生物作为NK3拮抗剂
- 申请号:PCT/EP2012/050034 申请日:2012-01-03
- 公开(公告)号:WO2012093109A1 公开(公告)日:2012-07-12
- 发明人: KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter
- 申请人: F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter
- 申请人地址: Grenzacherstrasse 124 CH-4070 Basel CH
- 专利权人: F. HOFFMANN-LA ROCHE AG,KNUST, Henner,NETTEKOVEN, Matthias,RATNI, Hasane,VIFIAN, Walter
- 当前专利权人: F. HOFFMANN-LA ROCHE AG,KNUST, Henner,NETTEKOVEN, Matthias,RATNI, Hasane,VIFIAN, Walter
- 当前专利权人地址: Grenzacherstrasse 124 CH-4070 Basel CH
- 代理机构: POPPE, Regina
- 优先权: EP11150352.0 20110107
- 主分类号: C07D401/06
- IPC分类号: C07D401/06 ; C07D401/14 ; C07D403/06 ; C07D413/10 ; A61K31/4025 ; A61P25/00
摘要:
The invention relates to compounds of formula (I) wherein R 1 is (A), or is phenyl, pyridinyl or pyridazinyl, wherein phenyl, pyridinyl and pyridazinyl may optionally be substituted by cyano, lower alkyl, halogen-substituted phenyl, lower alkyl-substituted [1,2,4]oxadiazol-3-yl or by 2-oxo-piperidin-1-yl; X is NR or O; R is C(O)-lower alkyl, -C(O)-cycloalkyl substituted by lower alkyl, cycloalkyl or is phenyl, pyridinyl or pyridazinyl, wherein phenyl, pyridinyl and pyridazinyl may optionally be substituted by lower alkyl, lower alkoxy, cyano, -C(O)-lower alkyl, halogen or lower alkyl substituted by halogen; R 2 is hydrogen or lower alkyl; R 3 is hydrogen, halogen, cyano, lower alkyl or lower alkyl substituted by halogen; R 4 is hydrogen or lower alkyl; wherein R 2 and R 4 are not simultaneously hydrogen or lower alkyl; R 5 is lower alkyl; R 6 halogen, hydroxy, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S(O) 2 -lower alkyl or cyano; or to a pharmaceutically suitable acid addition salt thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要(中):
本发明涉及式(I)化合物,其中R 1为(A),或为苯基,吡啶基或哒嗪基,其中苯基,吡啶基和哒嗪基可任选被氰基,低级烷基,卤素取代的苯基,低级烷基取代 [1,2,4]恶二唑-3-基或2-氧代 - 哌啶-1-基; X是NR或O; R是C(O) - 低级烷基,被低级烷基,环烷基或苯基,吡啶基或哒嗪基取代的-C(O) - 环烷基,其中苯基,吡啶基和哒嗪基可以任选地被低级烷基,低级烷氧基,氰基, -C(O) - 低级烷基,卤素或被卤素取代的低级烷基; R2是氢或低级烷基; R3是氢,卤素,氰基,被卤素取代的低级烷基或低级烷基; R4是氢或低级烷基; 其中R2和R4不同时为氢或低级烷基; R5是低级烷基; R 6卤素,羟基,低级烷基,低级烷氧基,被卤素取代的低级烷基,S(O)2 - 低级烷基或氰基; 或其药学上合适的酸加成盐。 已经发现,本发明化合物是用于治疗抑郁症,疼痛,精神病,帕金森病,精神分裂症,焦虑和注意缺陷多动障碍(ADHD)的高潜力NK-3受体拮抗剂。
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D401/00 | 杂环化合物,含有两个或更多个杂环,以氮原子作为仅有的杂环原子,至少有1个环是仅含有1个氮原子的六元环 |
--------C07D401/02 | .含有两个杂环 |
----------C07D401/06 | ..被仅含脂族碳原子的碳链连接的 |