公开(公告)号：EP0813065A2

公开(公告)日：1997-12-17

申请号：EP97109078.2

申请日：1997-06-05

申请人： F. HOFFMANN-LA ROCHE AG

发明人： Civelli, Olivier ,  Martin, James Richard ,  Monsma, Frederick ,  Moreau, Jean-Luc ,  Nothacker, Hans-Peter ,  Reinscheid, Rainer

IPC分类号： G01N33/566 ,  A61K38/10

CPC分类号： G01N33/9486 ,  G01N2500/00

摘要： The present invention relates to a method of screening for a therapeutically useful compound which comprises testing an LC132 receptor agonist in a screening assay for psychiatric and/or neurological disorders. More particularly, the screening method is based on contacting an LC132 receptor with an agent suspected of being an agonist of the LC132 receptor function, followed by the detection of the binding and/or the agonist activity of the compound and then testing of an agent with LC132 agonist activity in an antiepileptic, anticonvulsant or anxiolytic screening assay.

摘要翻译： 本发明涉及筛选治疗有用的化合物的方法，其包括在精神和/或神经障碍的筛选测定中检测LC132受体激动剂。 更具体地说，筛选方法是基于将LC132受体与疑似是LC132受体功能的激动剂的试剂接触，随后检测化合物的结合和/或激动剂活性，然后用 抗癫痫药，抗惊厥药或抗焦虑药筛选试验中LC132激动剂活性。

公开(公告)号：EP0856514B1

公开(公告)日：2001-06-13

申请号：EP98100970.7

申请日：1998-01-21

申请人： F. HOFFMANN-LA ROCHE AG

发明人： Adam, Geo ,  Cesura, Andrea ,  Galley, Guido ,  Jenck, François ,  Monsma, Frederick ,  Röver, Stephan ,  Wichmann, Jürgen

IPC分类号： C07D471/10 ,  A61K31/44

CPC分类号： C07D471/10

公开(公告)号：EP0856514A1

公开(公告)日：1998-08-05

申请号：EP98100970.7

申请日：1998-01-21

申请人： F. HOFFMANN-LA ROCHE AG

发明人： Adam, Geo ,  Cesura, Andrea ,  Galley, Guido ,  Jenck, François ,  Monsma, Frederick ,  Röver, Stephan ,  Wichmann, Jürgen

IPC分类号： C07D471/10 ,  A61K31/44

CPC分类号： C07D471/10

摘要： The present invention relates to compounds of the formula
wherein

R 1 and R 2 are, independently from each other, hydrogen, lower alkyl, lower alkoxy or halogen;
R 3 is phenyl, optionally substituted by lower alkyl,CF 3 , lower alkoxy or halogen; and
R 4 is hydrogen, lower alkyl, lower alkenyl, -C(O)-lower alkyl, -C(O)-phenyl, lower alkyl-C(O)-phenyl, lower alkylen-C(O)O-lower alkyl, lower alkantriyl-di-C(O)O-lower alkyl, hydroxy-lower alkyl, lower alkyl-O-lower alkyl, lower alkyl-CH(OH)CF 3 , phenyl or benzyl,
R 5 and R 6 are, independently from each other, hydrogen, phenyl, lower alkyl or di-lower alkyl or may form together a phenyl ring, and
R 5 and one of R 1 or R 2 may form together a saturated or unsaturated 6 membered ring,
A is a 4 - 7 membered saturated ring which may contain a heteroatom such as O or S,
and to pharmaceutically acceptable acid addition salts thereof which are agonists and/or antagonists of the OFQ receptor.

摘要翻译： 本发明涉及式CHEM的化合物，其中R 1和R 2彼此独立地为氢，低级烷基，低级烷氧基或卤素; R 3是任选被低级烷基，CF 3，低级烷氧基或卤素取代的苯基; （O） - 低级烷基，-C（O） - 苯基，低级烷基-C（O） - 苯基，低级亚烷基-C（O）O- 低级烷基，低级三烷基 - 二-C（O）O-低级烷基，羟基 - 低级烷基，低级烷基-O-低级烷基，低级烷基-CH（OH）CF 3，苯基或苄基，R 5和R' 6>彼此独立地为氢，苯基，低级烷基或二 - 低级烷基，或者可以一起形成苯环，R 5和R 1或R 2中的一个可以一起形成饱和的 或不饱和6元环，A为可含有杂原子如O或S的4-7元饱和环，以及作为OFQ受体的激动剂和/或拮抗剂的药学上可接受的酸加成盐。