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1. 发明申请

WO2008148688A1 PROLINAMIDE-TETRAZOLE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为NK3受体拮抗剂的丙酰胺 - 四唑衍生物
公开(公告)号：WO2008148688A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/056587
申请日：2008-05-29
申请人： F. HOFFMANN-LA ROCHE AG , HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
发明人： HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
IPC分类号： C07D403/12 , A61K31/496 , A61P25/00
CPC分类号： C07D403/12
摘要： The present invention relates to a compound of formula (I) : wherein R 1 is cycloalkyl or is phenyl unsubstituted or substituted by one or two halogen atoms; R 2 is hydrogen or halogen; R 3 is hydrogen, CN, lower alkoxy, lower alkyl or halogen; n is 0, 1 or 2; 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).
摘要翻译：本发明涉及式（I）化合物：其中R 1是环烷基或未被取代或被一个或两个卤原子取代的苯基; R2是氢或卤素; R3是氢，CN，低级烷氧基，低级烷基或卤素; n为0,1或2; 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。

2. 发明申请

WO2008148689A1 PROLINAMIDE DERIVATIVES AS NK3 ANTAGONISTS 审中-公开
标题翻译：丙酰胺衍生物作为NK3拮抗剂
公开(公告)号：WO2008148689A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/056589
申请日：2008-05-29
申请人： F. HOFFMANN-LA ROCHE AG , HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
发明人： HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
IPC分类号： C07D207/16 , C07D401/06 , C07D487/10 , A61P25/16 , A61P25/18 , A61K31/401
CPC分类号： C07D207/16 , C07D401/06 , C07D471/10
摘要： The present invention relates to a compound of formula (I) wherein R 1 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, or lower alkoxy substituted by halogen; R 2 is hydrogen or lower alkyl; R 3 , R 4 form together with the N-atom to which they are attached a non aromatic heterocyclic group, selected from R 5 is hydrogen or halogen; R 6 is phenyl, unsubstituted or substituted by cyano, halogen, lower alkyl, lower alkoxy, CF 3 , -(CH 2 ) 2 O-lower alkyl, C(O)-lower alkyl or C(O)O-lower alkyl, or is pyridinyl, unsubstituted or substituted by CF 3 , or is -C(O)-phenyl; R 7 is hydrogen or lower alkoxy; R 8 is phenyl, lower alkyl or -C(O)O-lower alkyl; R 9 is hydrogen or S(O) 2 -lower alkyl; R 10 is hydrogen or cycloalkyl; X is -CH 2 - or -C(O)-; p is 1 or 2; n is 1, 2 or 3; o is 1 or 2; or to a pharmaceutically suitable acid addition salt thereof which 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）化合物，其中R 1为氢，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基或被卤素取代的低级烷氧基; R2是氢或低级烷基; R3，R4与它们所连接的N-原子一起形成非芳族杂环基，选自R5是氢或卤素; R 6为未取代或被氰基，卤素，低级烷基，低级烷氧基，CF 3， - （CH 2）2 O-低级烷基，C（O） - 低级烷基或C（O）O-低级烷基取代或被吡啶基取代的苯基，未取代或被CF 3取代，或为-C（O） - 苯基; R7是氢或低级烷氧基; R8是苯基，低级烷基或-C（O）O-低级烷基; R9是氢或S（O）2-低级烷基; R 10是氢或环烷基; X是-CH 2 - 或-C（O） - ; p为1或2; n为1,2或3; o是1或2; 或其药学上合适的酸加成盐，其是用于治疗抑郁症，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。

3. 发明申请

WO2009033995A1 PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为NK3受体拮抗剂的哌啶衍生物
公开(公告)号：WO2009033995A1
公开(公告)日：2009-03-19
申请号：PCT/EP2008/061649
申请日：2008-09-04
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter , WU, Xihan
发明人： KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter , WU, Xihan
IPC分类号： C07D211/58 , C07D401/04 , A61K31/4468 , A61P25/18
CPC分类号： C07D211/58 , C07D401/04
摘要： The invention relates to a compound of general formula (I) wherein Ar 1 /Ar 2 are independently from each other phenyl or pyridinyl, which are optionally substituted by one or two substituents, selected from the group consisting of halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, lower alkyl substituted by alkoxy, lower alkyl substituted by cyano, lower di-alkyl amino, pyridinyl or cyano; R 1 is hydrogen, lower alkyl, -(CH 2 ) 2 O-lower alkyl, or cycloalkyl: R 2 is -S(O) 2 -lower alkyl or -C(O) -lower alkyl; or R 1 and R 2 form together with the N-atom to which they are attached a pyrrolidin-2- one or a piperidin-2-one group; R 3 is hydrogen, halogen or lower alkyl; R 4 is hydrogen or lower alkyl; R 5 /R 5' are independently from each other hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy or cycloalkyl; or R 5 and R 5' form together with the carbon-atom to which they are attached a cycloalkyl group; or to a pharmaceutically active 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).
摘要翻译：本发明涉及通式（I）的化合物，其中Ar 1 / Ar 2彼此独立地为苯基或吡啶基，其任选被一个或两个选自以下的取代基取代：卤素，低级烷基，低级烷氧基，低级被卤素取代的烷基，被卤素取代的低级烷氧基，被烷氧基取代的低级烷基，被氰基取代的低级烷基，低级二烷基氨基，吡啶基或氰基; R 1是氢，低级烷基， - （CH 2）2 O-低级烷基或环烷基：R 2是-S（O）2 - 低级烷基或-C（O） - 低级烷基; 或R 1和R 2与它们所连接的N-原子一起形成吡咯烷-2-酮或哌啶-2-酮基; R3是氢，卤素或低级烷基; R4是氢或低级烷基; R5 / R5'彼此独立地为氢，低级烷基，被卤素取代的低级烷基，被羟基或环烷基取代的低级烷基; 或R 5和R 5'与它们所连接的碳原子一起形成环烷基; 或其药物活性盐。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。

4. 发明申请

WO2009019163A1 PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯烷酮ARYL-ETHER作为NK3受体拮抗剂
公开(公告)号：WO2009019163A1
公开(公告)日：2009-02-12
申请号：PCT/EP2008/059908
申请日：2008-07-29
申请人： F. HOFFMANN-LA ROCHE AG , JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , WU, Xihan
发明人： JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , WU, Xihan
IPC分类号： C07D401/08 , C07D401/06
CPC分类号： C07D401/06 , C07D401/08
摘要： The invention relates to a compound of general formula (I) wherein Ar 1 is aryl or a five or six membered heteroaryl; Ar 2 is aryl or a five or six membered heteroaryl; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, S-lower alkyl, -S(O) 2 -lower alkyl, -S(O) 2 -di-lower alkyl amino, -(CH 2 ) q R, cyano, amino, mono or di-lower alkyl amino, NHC(O)-lower alkyl, cycloalkyl or is or a five membered heteroaryl, optionally substituted by lower alkyl; wherein R is cyano, di-lower alkyl amino or pyrrolidin-1-yl; R 2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R 3 is hydrogen or lower alkyl or CH 2 OH; R 4 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; n is 1, 2 or 3; in case n is 2 or 3, R 1 may be the same or different; o is 1, 2 or 3; in case o is 2 or 3, R 2 may be the same or different; p is 1, 2 or 3; in case p is 2 or 3, R 4 may be the same or different; q is 1 or 2; or to a pharmaceutically active salt thereof, including all stereoisomeric forms, 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：本发明涉及通式（I）的化合物，其中Ar 1是芳基或五或六元杂芳基; Ar 2是芳基或五或六元杂芳基; R 1是氢，卤素，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，S-低级烷基，-S（O）2 - 低级烷基，-S（O）氨基， - （CH 2）q R，氰基，氨基，一或二低级烷基氨基，NHC（O） - 低级烷基，环烷基或任选被低级烷基取代的五元杂芳基; 其中R是氰基，二低级烷基氨基或吡咯烷-1-基; R2是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; R3是氢或低级烷基或CH2OH; R4是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; n为1,2或3; 在n为2或3的情况下，R 1可以相同或不同; o是1,2或3; 在o为2或3的情况下，R 2可以相同或不同; p为1,2或3; 在p为2或3的情况下，R 4可以相同或不同; q为1或2; 或其药物活性盐，包括式（I）化合物的所有立体异构形式，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。

5. 发明申请

WO2009024502A1 PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯烷酮ARYL-ETHER作为NK3受体拮抗剂
公开(公告)号：WO2009024502A1
公开(公告)日：2009-02-26
申请号：PCT/EP2008/060566
申请日：2008-08-12
申请人： F. HOFFMANN-LA ROCHE AG , JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , WU, Xihan
发明人： JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , WU, Xihan
IPC分类号： C07D207/08 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D487/04 , C07D491/04 , C07D491/10 , A61K31/4468 , A61K31/496 , A61K31/506 , A61K31/5377 , A61P23/00 , A61P25/00 , A61P25/16
CPC分类号： C07D401/14 , C07D207/08 , C07D401/06 , C07D403/06 , C07D403/14 , C07D487/04 , C07D491/04 , C07D491/10
摘要： The invention relates to a compound of general formula (I) wherein is aryl or a five or six membered heteroaryl; is a six to nine membered mono or bi-heterocyclic group, wherein X may be a carbon atom, SO 2 or a further hetero atom, selected from the group consisting of N or O; if X is a carbon atom, O, SO 2 or unsubstituted N, then R 1 is hydrogen, hydroxy, cyano, -(CH 2 ) q -OH, -(CH 2 ) q -NRR', -(CH 2 ) q -CN, lower alkyl, -S(O) 2 -lower alkyl, -NR-S(O) 2 -lower alkyl, -C(O)-lower alkyl, -NR-C(O)-lower alkyl, phenyl, or is a heterocyclic group selected from piperidinyl- 2 -one; if X is a N-atom, substituted by R 1 , then R 1 is hydrogen, -(CH 2 ) q -OH, -(CH 2 ) q -NRR', -(CH 2 ) q -CN, lower alkyl, -S(O) 2 - lower alkyl, aryl or a five or six membered heteroaryl or -C(O)-lower alkyl, provided that q is 2 or 3. R/R' are independently from each other hydrogen or lower alkyl; R 2 is hydrogen, halogen, lower alkyl, cyano, lower alkoxy substituted by halogen, lower alkyl substituted by halogen or is a five or six membered heteroaryl; R 3 is hydrogen or halogen; R 4 is hydrogen or lower alkyl; n is 1 or 2; in case n is 2, R 1 may be the same or different; o is 1 or 2; in case o is 2, R 2 may be the same or different; p is 1 or 2; in case p is 2, R 3 may be the same or different; q is 1, 2 or 3; s is 0, 1, 2, 3 or 4; or to a pharmaceutically active salt thereof, including all stereoisomeric forms, 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：本发明涉及通式（I）的化合物，其中芳基或五或六元杂芳基; 是6至9元单或双杂环基团，其中X可以是选自N或O的碳原子，SO 2或另外的杂原子; 如果X是碳原子，O，SO2或未取代的N，那么R 1是氢，羟基，氰基， - （CH 2）q -OH， - （CH 2）q -NRR'， - （CH 2）q-CN ，低级烷基，-S（O）2 - 低级烷基，-NR-S（O）2 - 低级烷基，-C（O） - 低级烷基，-NR-C（O） - 低级烷基，苯基或选自哌啶-2-酮的杂环基; 如果X是被R 1取代的N-原子，则R 1是氢， - （CH 2）q -OH， - （CH 2）q -NRR'， - （CH 2）q-CN，低级烷基， -S（O）2 - 低级烷基，芳基或五或六元杂芳基或-C（O） - 低级烷基，条件是q为2或3.R / R'彼此独立地为氢或低级烷基; R 2是氢，卤素，低级烷基，氰基，被卤素取代的低级烷氧基，被卤素取代的低级烷基或是五或六元杂芳基; R 3是氢或卤素; R 4是氢或低级烷基; n为1或2; 在n为2的情况下，R 1可以相同或不同; o是1或2; 在o为2的情况下，R 2可以相同或不同; p为1或2; 在p为2的情况下，R 3可以相同或不同; q为1,2或3; s为0，1，2，3或4; 或其药物活性盐，包括式（I）化合物的所有立体异构形式，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。

6. 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。

7. 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。

8. 发明申请

WO2012093109A1 PYRROLIDINE DERIVATIVES AS NK3 ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为NK3拮抗剂
公开(公告)号：WO2012093109A1
公开(公告)日：2012-07-12
申请号：PCT/EP2012/050034
申请日：2012-01-03
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter
发明人： KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter
IPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D413/10 , A61K31/4025 , A61P25/00
CPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D407/06 , C07D413/10
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).
摘要翻译：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。

9. 发明申请

WO2010086259A1 PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为NK3受体拮抗剂的哌啶衍生物
公开(公告)号：WO2010086259A1
公开(公告)日：2010-08-05
申请号：PCT/EP2010/050591
申请日：2010-01-19
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
发明人： KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , A61K31/454 , A61K31/4545 , A61P25/24 , A61P25/04 , A61P25/18 , A61P25/16 , A61P25/22
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14
摘要： The present invention relates to a compounds of formula (I) wherein Ar 1 is aryl or a six membered heteroaryl; Ar 2 is aryl or a six membered heteroaryl; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen; R 2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R 3 is hydrogen or lower alkyl; R 4 is hydrogen, lower alkyl, phenyl, optionally substituted by halogen, or is a five membered heteroaryl, optionally substituted by lower alkyl, or is aryl optionally substituted by halogen; is a six membered heterocyclic group, wherein X is -N(SO 2 CH 3 ); R 6 is hydrogen; Y is -N(R 7' )- R 7' is a 6-membered heteroaryl group, optionally substituted by cyano or C(O)-cycloalkyl, wherein the cycloalkyl group is optionally substituted by lower alkyl, n is 1; m is 1; o is1; p is 1; s is 0; t is 1; u is 1; or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. It has been found that the present compounds are high potential NK-3 receptor antagonist 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Ar 1是芳基或6元杂芳基; Ar 2是芳基或六元杂芳基; R1是氢，卤素，低级烷基，低级烷氧基或被卤素取代的低级烷基; R2是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; R3是氢或低级烷基; R4是氢，低级烷基，任选被卤素取代的苯基，或是任选被低级烷基取代的五元杂芳基，或者是被卤素任意取代的芳基; 是六元杂环基，其中X是-N（SO 2 CH 3）; R6是氢; Y是-N（R 7'）-R 7'是任选被氰基或C（O） - 环烷基取代的6元杂芳基，其中环烷基任选被低级烷基取代，n是1; m为1; o is1; p为1; s是0; t为1; 你是1 或其药物活性盐，外消旋混合物，对映体，旋光异构体或其互变异构形式。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。

10. 发明申请

WO2011085886A1 PYRROLIDINE DERIVATIVES 审中-公开
标题翻译：吡咯烷衍生物
公开(公告)号：WO2011085886A1
公开(公告)日：2011-07-21
申请号：PCT/EP2010/069434
申请日：2010-12-13
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , KOBLET, Andreas , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
发明人： KNUST, Henner , KOBLET, Andreas , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
IPC分类号： C07D207/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D407/04 , C07D413/06 , C07D417/14 , A61K31/5377 , A61P25/18
CPC分类号： A61K31/40 , A61K31/4025 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D207/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D407/04 , C07D413/06 , C07D417/14
摘要： The present invention relates to compounds of formula (I) or to a pharmaceutically active 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).
摘要翻译：本发明涉及式（I）化合物或其药物活性盐。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。

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