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11. 发明申请

WO2008151969A1 PIPERAZINE AND [1,4] DIAZEPAN DERIVATIVES AS NK ANTAGONISTS 审中-公开
标题翻译：哌嗪和[1,4] DIAZEPAN衍生物作为NK拮抗剂
公开(公告)号：WO2008151969A1
公开(公告)日：2008-12-18
申请号：PCT/EP2008/056878
申请日：2008-06-04
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
发明人： KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
IPC分类号： C07D513/04 , C07D295/26 , A61K31/495 , A61K31/551 , A61K31/4985 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24
CPC分类号： C07D295/26 , C07D513/04
摘要： The present invention relates to a compound of Formula (I) wherein R 1 is hydrogen or lower alkyl; is hydrogen, fluoro, hydroxy or lower alkyl; R 3 is hydrogen or lower alkyl; R 4 is -CHR 5 -A R 5 is hydrogen, lower alkyl, fluoro, CF 3 , CH 2 OH or cycloalkyl; A is aryl or heteroaryl, which rings are unsubstituted or substituted by (R 6 )o; R 6 may be the same or not when o is more than one, and is heteroaryl, lower alkyl, lower alkoxy, cyano, halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or NR 7 R 8 ; o is 1, 2 or 3; R 7 , R 8 are independently hydrogen or lower alkyl; R 9 is lower alkyl; R 10 is lower alkyl, lower alkoxy or halogen; n is 1 or 2; m is 1 or 2; or to a pharmaceutically suitable acid addition salt thereof. The invention includes all sterioisomeric forms, including individual diastereoisomers and enantiomers of the compound of Formula (I) as well as racemic and non-racemic mixtures 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).
摘要翻译：本发明涉及式（I）的化合物，其中R 1是氢或低级烷基; 是氢，氟，羟基或低级烷基; R3是氢或低级烷基; R4是-CHR5-A R5是氢，低级烷基，氟，CF3，CH2OH或环烷基; A是芳基或杂芳基，该环是未取代的或被（R 6）o取代; 当O大于1时，R 6可以相同或不同，并且是杂芳基，低级烷基，低级烷氧基，氰基，卤素，被卤素取代的低级烷基，被卤素或NR 7 R 8取代的低级烷氧基; o是1,2或3; R 7，R 8独立地为氢或低级烷基; R9是低级烷基; R 10为低级烷基，低级烷氧基或卤素; n为1或2; m为1或2; 或其药学上合适的酸加成盐。本发明包括所有异构体形式，包括式（I）化合物的单独的非对映异构体和对映异构体以及其外消旋和非外消旋混合物。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。

12. 发明申请

WO2008128891A1 PYRROLIDINE DERIVATIVES AS DUAL NK1/NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为NK1 / NK3受体拮抗剂
公开(公告)号：WO2008128891A1
公开(公告)日：2008-10-30
申请号：PCT/EP2008/054261
申请日：2008-04-09
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , HOFFMANN, Torsten , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
发明人： BISSANTZ, Caterina , HOFFMANN, Torsten , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
IPC分类号： C07D207/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D471/10 , A61K31/5377 , A61P25/28
CPC分类号： C07D207/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D471/10
摘要： The invention relates to pyrrolidine derivatives of formula (I) wherein R 1 is hydrogen, halogen or lower alkyl; R 2 is hydrogen, halogen, lower alkoxy or lower alkyl substituted by halogen; R 3 is -(CH 2 ) p -heterocyclyl optionally substituted by lower alkyl, halogen, -S(O) 2 -lower alkyl, -C(O)-lower alkyl, -C(O)O-lower alkyl, hydroxy, lower alkyl substituted by hydroxy, -(CH 2 ) p -O-lower alkyl, -NHCO-lower alkyl, or is C 3-6 -cycloalkyl optionally substituted by =O, -(CH 2 ) p -O-lower alkyl or lower alkinyl, or is unsubstituted or substituted aryl or heteroaryl, wherein the substituents are selected from the group consisting of lower alkyl, CN, -S(O) 2 -lower alkyl, halogen, -C(O) -lower alkyl, hydroxy, lower alkoxy or lower alkoxy substituted by halogen; or is -(CH 2 ) P -NR 4 R 5 ; R 4 /R 5 are independently from each other hydrogen, lower alkyl, -(CRR')p-lower alkyl substituted by hydroxy, -(CRR')p-O-lower alkyl, -(CRR')p-S-lower alkyl, -(CRR') p -O-lower alkyl substituted by hydroxy or C 3-6 -cycloalkyl; R/R' are independently from each other hydrogen, lower alkyl or lower alkyl substituted by hydroxyl; n is 1 or 2; o is 1 or 2; P is 0, 1, 2, 3 or 4; or to pharmaceutically active acid-addition salts thereof.
摘要翻译：本发明涉及式（I）的吡咯烷衍生物，其中R 1是氢，卤素或低级烷基; R 2是氢，卤素，低级烷氧基或被卤素取代的低级烷基; R 3是 - 任选被低级烷基，卤素，-S（O）2取代的 - （CH 2）2 - 杂环基）低级烷基，-C（O） - 低级烷基，-C（O）O-低级烷基，羟基，被羟基取代的低级烷基， - （CH 2）或低级烷基，-NHCO-低级烷基，或为任选被= O， - （CH 2）2取代的C 3-6环烷基，低级烷基或低级炔基，或未取代或取代的芳基或杂芳基，其中取代基选自低级烷基，CN，-S（O）2，低级烷基，卤素，-C（O） - 低级烷基，羟基，低级烷氧基或被卤素取代的低级烷氧基; 或是 - （CH 2）2 - - - - - - - - - - - - - - - R 4和R 5彼此独立地是氢，低级烷基， - 被羟基取代的 - （CRR'）对 - 低级烷基， - （CRR'）pO-低级烷基， - （CRR'）pS-低级烷基， - （CRR'）由羟基或C 3-6 - 环烷基取代的-O-低级烷基; R / R'彼此独立地为氢，被羟基取代的低级烷基或低级烷基; n为1或2; o是1或2; P为0,1,2,3或4; 或其药学活性的酸加成盐。

13. 发明申请

WO2002100350A2 DOPAMINE RECEPTOR LIGANDS AND THERAPEUTIC METHODS BASED THEREON 审中-公开
标题翻译：多巴胺受体配体及其治疗方法
公开(公告)号：WO2002100350A2
公开(公告)日：2002-12-19
申请号：PCT/US2002/018914
申请日：2002-06-13
申请人： THE REGENTS OF UNIVERSITY OF MICHIGAN , WANG, Shaomeng , VARADY, Judith , WU, Xihan , MIN, Ji , DING, Ke , LEVANT, Beth
发明人： WANG, Shaomeng , VARADY, Judith , WU, Xihan , MIN, Ji , DING, Ke , LEVANT, Beth
IPC分类号： A61K
CPC分类号： C07D471/04 , A61K31/495
摘要： The present invention relates to compounds designed as ligands ( e . g ., agonists, antagonists, and partial agonists) for dopamine receptors ( e . g ., D 1 , D 2 , D 3 , D 4 , and D 5 ), and in particular, the D 1 , D 2 , and D 3 dopamine receptors. The present invention also relates to methods for rationally designing these compounds and to therapeutic methods of using these compounds.
摘要翻译：本发明涉及被设计为多巴胺受体（例如，D1，D2，D3，D4和D5）的配体（例如激动剂，拮抗剂和部分激动剂）的化合物，特别是D1，D2和D3多巴胺受体。本发明还涉及合理设计这些化合物的方法和使用这些化合物的治疗方法。

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