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1. 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。

2. 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。

3. 发明申请

WO2009150110A1 PYRROLIDINE ETHER DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯烷酮衍生物作为NK3受体拮抗剂
公开(公告)号：WO2009150110A1
公开(公告)日：2009-12-17
申请号：PCT/EP2009/056989
申请日：2009-06-08
申请人： F. HOFFMANN-LA ROCHE AG , JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
发明人： JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
IPC分类号： C07D401/12 , C07D401/14 , A61K31/445 , A61P25/00
CPC分类号： C07D401/14 , C07D401/12
摘要： The present invention relates to a compounds of formula I wherein R 1 , R 2 , R 3 , R', Ar, o, n and m are as defined in the specification. 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，R 2，R 3，R'，Ar，O，n和m如说明书中所定义。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

WO2009153179A1 PYRROLIDINE DERIVATIVES AS NK2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为NK2受体拮抗剂
公开(公告)号：WO2009153179A1
公开(公告)日：2009-12-23
申请号：PCT/EP2009/056987
申请日：2009-06-08
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , KOBLET, Andreas , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
发明人： BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , KOBLET, Andreas , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
IPC分类号： C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10 , A61K31/40 , A61K31/4439 , A61K31/443 , A61P25/24
CPC分类号： C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10
摘要： The present invention relates to a compound of Formula (I) wherein R 1 is hydrogen, halogen, cyano or lower alkyl; n is 1, 2 or 3; R 2 is hydrogen or lower alkyl; R 3 is an aryl- or a heteroaryl ring, wherein the rings are optionally substituted by one or two substituents R'; R' is selected from hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen,-S(O) 2 -lower alkyl, CN, -NR 4 R 5 , -C(O)-lower alkyl, heterocyclyl or heteroaryl; R 4 /R 5 are independently from each other hydrogen, -(CO)CF 3 or lower alkyl or is a non aromatic heterocyclic group (II) wherein X is N or CH; Y is -CH(R 7 )-; -N(R 7' )-, or O or can be SO 2 ; R 6 is hydrogen, lower alkyl or hydroxy; R 7 is hydrogen, hydroxy, =0, lower alkyl, lower alkoxy, -S(O) 2 -lower alkyl, -C(O)-lower alkyl, -C(O)CH 2 O-lower alkyl, -CH 2 CN, -C(O)CH 2 CN, -C(O)-cycloalkyl wherein the cycloalkyl group is optionally substituted by cyano, lower alkyl, one or two halogen atoms, =0 or by amino, or is -C(O)O-lower alkyl, -NH-lower alkyl, -NRC(O)O-lower alkyl, -NRC(O)-lower alkyl or -CH 2 O-lower alkyl; and R 7' is hydrogen, lower alkyl, -(CH 2 ) q -S(O) 2 -lower alkyl, -(CH 2 ) q -S(O) 2 -cycloalkyl, -C(O)-lower alkyl, -(CH 2 ) q -cycloalkyl, -C(O)CH 2 -O-lower alkyl, -(CH 2 ) q CN, -C(O)CN, -C(O)CH 2 CN, lower alkyl substituted by halogen, lower alkenyl substituted by halogen, -C(O)-cycloalkyl wherein the cycloalkyl group is optionally substituted by cyano, lower alkyl, one or two halogen atoms, =0 or by amino, or is -C(O)O-lower alkyl or -(CH 2 )qO-lower alkyl and q is O - 3; or R 6 and R 7 may form together with the carbon atoms to which they are attach a five or six- membered non aromatic ring or R 6 and R 7 may form together with the nitrogen and carbon atoms to which they are attach a five or six-membered non aromatic ring; p is 0, 1 or 2; Ar is aryl- or heteroaryl, wherein the rings are optionally substituted by one or two substituents R"; R' ' is selected from hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, -O-CH 2 -cycloalkyl, -NR 4 R 5 , -CN, -CH(CH 3 )CN, -CH 2 O-lower alkyl or pyrrolyl; m is 0, 1 or 2 and o is 0; o is 0, 1 or 2 and m is 1 or pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or tautomeric forms thereof. The compounds may be used for the treatment of depression, anxiety or schizophrenia.
摘要翻译：本发明涉及式（I）的化合物，其中R 1是氢，卤素，氰基或低级烷基; n为1,2或3; R2是氢或低级烷基; R3是芳基或杂芳基环，其中环任选地被一个或两个取代基R'取代; R'选自氢，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（O）2 - 低级烷基，CN，-NR 4 R 5，-C（O） - 低级烷基，杂环基或杂芳基; R 4 / R 5彼此独立地为氢， - （CO）CF 3或低级烷基或为非芳族杂环基团（II），其中X为N或CH; Y是-CH（R 7） - ; -N（R 7'） - 或O或可以是SO 2; R6是氢，低级烷基或羟基; R 7是氢，羟基，= 0，低级烷基，低级烷氧基，-S（O）2 - 低级烷基，-C（O） - 低级烷基，-C（O）CH 2 O-低级烷基，-CH 2 CN，-C O）CH 2 CN，-C（O） - 环烷基，其中环烷基任选被氰基，低级烷基，一个或两个卤素原子取代，= 0或被氨基取代，或者是-C（O）O-低级烷基，-NH - 低级烷基，-NRC（O）O-低级烷基，-NRC（O） - 低级烷基或-CH 2 O-低级烷基; 并且R 7'是氢，低级烷基， - （CH 2）qS（O）2 - 低级烷基， - （CH 2）qS（O）2-环烷基，-C（O） - 低级烷基， - （CH 2），-C（O）CH 2 -O-低级烷基， - （CH 2）q CN，-C（O）CN，-C（O）CH 2 CN，被卤素取代的低级烷基，被卤素取代的低级链烯基，-C（O） - 环烷基，其中环烷基任选被氰基，低级烷基，一个或两个卤素原子，= O或氨基取代，或者是-C（O）O-低级烷基或 - （CH 2）q O-低级烷基，q是 O - 3; 或者R 6和R 7可以与它们所连接的五元或六元非芳香环的碳原子一起形成，或者R 6和R 7可以与它们所连接的五元或六元非芳环的氮和碳原子一起形成，芳香环 p为0,1或2; Ar是芳基或杂芳基，其中环任选地被一个或两个取代基R“取代; R”选自氢，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素取代的低级烷氧基， O-CH 2 - 环烷基，-NR 4 R 5，-CN，-CH（CH 3）CN，-CH 2 O-低级烷基或吡咯基; m为0,1或2，o为0; o为0,1或2，m为1 或其药物活性盐，外消旋混合物，对映异构体，旋光异构体或互变异构体形式。化合物可用于治疗抑郁症，焦虑或精神分裂症。

5. 发明申请

WO2010094667A1 PYRROLIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为NK3受体拮抗剂
公开(公告)号：WO2010094667A1
公开(公告)日：2010-08-26
申请号：PCT/EP2010/051887
申请日：2010-02-16
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
发明人： KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
IPC分类号： C07D207/08 , C07D401/12 , C07D401/14 , C07D403/14 , A61P25/00 , A61K31/496 , A61K31/506 , A61K31/4439 , A61K31/4545 , A61K31/501
CPC分类号： C07D207/08 , C07D207/09 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
摘要： The present invention relates to a compounds of formula I wherein A is -NR'-, -S-, -S(O)- or -S(O) 2 -; R' is hydrogen or lower alkyl; Ar is aryl or is a five or six membered heteroaryl group, containing one or two N-atoms; R is a five or six membered heterocyclic group X 1 is N or CH; and X 2 is -N(R 1 )-, -CH 2 -, -O-, -S-, -S(O)-, or -S(O) 2 -, R 1 is hydrogen, lower alkyl, S(O) 2 -lower alkyl, C(O)-lower alkyl, C(O)-cycloalkyl optionally substituted by lower alkyl; with the proviso that at least one of X 1 or X 2 contains a heteroatom, or is a five or six membered heteroaryl group, containing one or two N-atoms, which groups are unsubstituted or may be substituted by one or two R 1 ; wherein R 1 is lower alkyl or cyano; R 2 is lower alkyl substituted by halogen, halogen, cyano or nitro; R 3 is halogen; R 4 is hydrogen or lower alkyl; 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; 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, bipolar disorders, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及式I化合物，其中A为-NR' - ， - S - ， - S（O） - 或-S（O）2 - ; R'是氢或低级烷基; Ar是芳基或是含有一个或两个N-原子的五或六元杂芳基; R是五或六元杂环基，X 1是N或CH; 并且X 2为-N（R 1） - ， - CH 2 - ， - O - ， - S - ， - S（O） - 或-S（O）2 - ，R 1为氢，低级烷基，S（O）低级烷基，C（O） - 低级烷基，任选被低级烷基取代的C（O） - 环烷基; 条件是X 1或X 2中的至少一个含有杂原子，或是含有一个或两个N原子的五或六元杂芳基，该基团是未取代的或可被一个或两个R 1取代; 其中R1是低级烷基或氰基; R2是被卤素，卤素，氰基或硝基取代的低级烷基; R3是卤素; R4是氢或低级烷基; 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; 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，双相情感障碍，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

WO2010106081A1 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：WO2010106081A1
公开(公告)日：2010-09-23
申请号：PCT/EP2010/053417
申请日：2010-03-16
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
发明人： KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
IPC分类号： C07D211/32 , C07D401/10 , C07D401/14 , C07D409/14 , C07D413/10 , C07D417/10 , C07D417/14 , A61K31/4409 , A61K31/4465 , A61P3/04
CPC分类号： C07D401/10 , A61K31/4409 , A61K31/4465 , C07D211/32 , C07D401/14 , C07D409/14 , C07D413/10 , C07D417/10 , C07D417/14
摘要： The present application relates to compounds of formula (I) wherein the definitions are as described in claim 1. 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：本申请涉及式（I）的化合物，其中定义如权利要求1所述。已经发现本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病的高潜力NK-3受体拮抗剂，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）。

7. 发明申请

WO2010054968A1 QUINAZOLINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：喹唑啉衍生物作为NK3受体拮抗剂
公开(公告)号：WO2010054968A1
公开(公告)日：2010-05-20
申请号：PCT/EP2009/064604
申请日：2009-11-04
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
发明人： KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
IPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , A61K31/517 , A61P25/16 , A61P25/18
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14
摘要： The present invention relates to a compounds of formula I wherein R 1 is hydroxy or NR'R"; R' and R" are independently from each other hydrogen, lower alkyl, cycloalkyl, or may form together with the N-atom to which they are attached a heteroalkyl ring; R 2 is hydrogen, lower alkyl, lower alkoxy, halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano or S(O) 2 -Iower alkyl; R 3 is lower alkyl, -(CH 2 ) m -aryl, optionally substituted by halogen, or is -(CH 2 ) m -cycloalkyl; R 4 and R 5 are independently from each other hydrogen or lower alkyl substituted by halogen, or are -(CR 2 ) m -aryl or -(CR 2 ) m -heteroaryl, wherein the rings may be substituted by one or more substituents, selected from halogen, lower alkyl, lower alkyl substituted by halogen, cyano, hydroxy, NR'R" or by lower alkoxy substituted by halogen, or are -(CR 2 ) m -cycloalkyl, optionally substituted by hydroxy or by aryl, or are a heteroalkyl ring, optionally substituted by =O or -(CR 2 ) m -aryl, or R 4 and R 5 are together with the N-atom to which they are attached a heterocyclic ring system, optionally substituted by lower alkyl, aryl or halogen-substituted aryl, and R may be independently from each other hydrogen, lower alkyl or lower alkyl substituted by hydroxyl; n is 1 or 2; m is 0, 1 or 2; 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 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R1是羟基或NR'R“; R'和R”彼此独立地是氢，低级烷基，环烷基，或者可以与它们所在的N-原子一起形成连接杂烷基环; R 2是氢，低级烷基，低级烷氧基，卤素，被卤素取代的低级烷基，被卤素取代的低级烷氧基，氰基或S（O）2 - 低级烷基） R 3是低级烷基， - （CH 2）m - 芳基，任选被卤素取代，或是 - （CH 2）m - 环烷基; R 4和R 5彼此独立地为氢或被卤素取代的低级烷基，或是 - （CR 2）m - 芳基或 - （CR 2）m - 杂芳基，其中所述环可以被一个或多个选自卤素，低级烷基，被卤素，氰基，羟基，NR'R“取代的低级烷基或被卤素取代的低级烷氧基取代，或者是任选被羟基或芳基取代的 - （CR 2）m - 环烷基，或者是杂烷基环，被取代为= O或 - （CR 2）m - 芳基，或者R 4和R 5与它们所连接的N-原子一起是杂环体系，任选地被低级烷基，芳基或卤素取代的芳基取代，R可以彼此独立地为氢，被羟基取代的低级烷基或低级烷基; n为1或2; m为0,1或2;或者为药物活性盐，外消旋混合物，对映体，旋光异构体或互变异构体已经发现本发明化合物是高潜在的NK-3受体拮抗剂治疗抑郁症，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）。

8. 发明申请

WO2011023626A1 PYRROLIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为NK3受体拮抗剂
公开(公告)号：WO2011023626A1
公开(公告)日：2011-03-03
申请号：PCT/EP2010/062141
申请日：2010-08-20
申请人： F. HOFFMANN-LA ROCHE AG , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , PATINY-ADAM, Angélique , RATNI, Hasane , RIEMER, Claus
发明人： JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , PATINY-ADAM, Angélique , RATNI, Hasane , RIEMER, Claus
IPC分类号： C07D401/14 , C07D413/14 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61P25/16 , A61P25/18 , A61P25/24 , A61P29/00
CPC分类号： C07D401/14 , C07D413/14
摘要： The present invention relates to a compounds of formula (I) wherein R 1 is hydrogen or lower alkyl; R 2 is hydrogen, lower alkyl, lower alkyl substituted by halogen or is halogen or CN, and may be independently from each other if o is 2; Ar 1 is aryl or heteroaryl; Ar 2 is aryl or heteroaryl; R'/R" are independently from each other hydrogen, lower alkyl, lower alkoxy, halogen, C(O)- lower alkyl, cyano or lower alkyl substituted by halogen; m is 0, 1, or 2 when n is 0; or m is 0 or 1 when n is 1; n is 0 or 1; o is 1 or 2; or to pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or to tautomeric forms 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是氢或低级烷基; R 2是氢，低级烷基，被卤素取代的低级烷基，或者是卤素或CN，如果o是2，可以彼此独立地表示; Ar 1是芳基或杂芳基; Ar2是芳基或杂芳基; R'/ R“彼此独立地为氢，低级烷基，低级烷氧基，卤素，C（O） - 低级烷基，氰基或被卤素取代的低级烷基;当n为0时，m为0,1或2;或当n为1时，m为0或1; n为0或1; o为1或2;或者为药物活性盐，外消旋混合物，对映异构体，光学异构体或其互变异构形式。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）的高潜在NK-3受体拮抗剂。

9. 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。

10. 发明申请

WO2010060703A1 3-(BENZYLAMINO)-PYRROLIDINE DERIVATIVES AND THEIR USE AS NK-3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 3-（苯甲酰胺） - 吡咯烷衍生物及其作为NK-3受体拮抗剂的用途
公开(公告)号：WO2010060703A1
公开(公告)日：2010-06-03
申请号：PCT/EP2009/064031
申请日：2009-10-26
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
发明人： BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
IPC分类号： C07D207/14 , A61K31/401 , A61K31/4025 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D491/08
CPC分类号： C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D491/08
摘要： The present invention relates to a compounds of formula I wherein Ar is aryl; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano, amino, mono or di-lower alkyl amino, C(O)-lower alkyl, or is aryl or heteroaryl; R 2 is hydrogen or halogen; R 3 is -(CH 2 ) p -heterocyclyl, optionally substituted by one or two substituents R 4 ; or is lower alkyl, lower alkoxy, -(CH 2 ) p -O-lo wer alkyl, -(CH 2 ) P -CN, -O-(CH 2 ) p -CN, -(CH 2 ) p -heteroaryl, -(CH 2 ) p -C(O)-heteroaryl, -O-(CH 2 ) p -heterocyclyl, -(CH 2 ) p -aryl, optionally substituted by lower alkoxy or halogen, -(CH 2 ) p -O-aryl, optionally substituted by lower alkyl, -(CH 2 ) p -NR'-heterocyclyl, optionally substituted by lower alkyl, -CH 2 ) p -NR'R", -CH 2 ) p -NR'-CH 2 ) p' -NR'R", -CH 2 ) p -NR'-CH 2 ) p' -CN, -CH 2 ) p -C(O)-NR'R" or is -O-(CH 2 ) p -NR'R"; R 4 is hydroxy, lower alkyl, -(CH 2 ) P -OH, -(CH 2 ) P -NR'R", -NR'-C(O)-lower alkyl, -(CH 2 ) p -CN, -S(O) 2 -lower alkyl, -NR'-S(O) 2 -lower alkyl, -S(O)2-NR'R", -C(O)-lower alkyl, -C(O)-lower cycloalkyl, wherein the cycloalkyl may be substituted by lower alkyl, or is -C(O)-NR'R", heterocyclyl, optionally substituted by =0, or is heteroaryl, optionally substituted by alkoxy or cyano, or is aryl optionally substituted by alkoxy, cyano or is 2-oxa-5-aza-bicyclo[2.2.1]hept-5-yl; R' and R' ' are independently from each other hydrogen, lower alkyl or -(CH 2 ) P -OH; n is 1 or 2; in case n is 1 or 2, R 1 may be the same or different; o is 1 or 2; in case o is 1 or 2, R 2 may be the same or different; p,p' are the same or different and are O, 1, 2 3 or 4; 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 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Ar为芳基; R 1为氢，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，氰基，氨基，一或二低级烷基氨基，C（O） - 低级烷基，或为芳基或杂芳基; R2是氢或卤素; R3是 - （CH2）对 - 杂环基，任选被一个或两个取代基R 4取代; 或（CH 2）p-CN，-O-（CH 2）p -CN， - （CH 2）p - 杂芳基， - （CH 2）p C（ - （CH 2）p - 芳基，任选被低级烷氧基或卤素取代的 - （CH 2）p - 芳基， - （CH 2） -CH 2）p-NR'R“，-CH 2）p-NR'-CH 2）p'-NR'R”，-CH 2）p -NR'-CH 2） p'-CN，-CH2）pC（O）-NR'R“或是-O-（CH2）p-NR'R”; R4是羟基，低级烷基， - （CH2）P-OH， - （CH2）P-NR'R“，-NR'-C（O） - 低级烷基， - （CH2）p-CN，-S ）低级烷基，-NR'-S（O）2 - 低级烷基，-S（O）2 -NR'R“，-C（O） - 低级烷基，-C（O） - 低级环烷基，其中可以被低级烷基取代，或者是-C（O）-NR'R“，任选地被0取代的杂环基，或被任选被烷氧基或氰基取代的杂芳基，或者是被烷氧基任意取代的芳基，氰基或是2-氧杂-5-氮杂 - 双环[2.2.1]庚-5-基; R'和R“彼此独立地为氢，低级烷基或 - （CH 2）P-OH; n为1或 2;在n为1或2的情况下，R 1可以相同或不同; o为1或2;在o为1或2的情况下，R 2可以相同或不同; p，p'相同或不同， O，1,2,3或4;或其药学活性盐，外消旋混合物，对映异构体，旋光异构体或互变异构体形式。已经发现本发明化合物是高潜在的NK-3受体拮抗剂治疗抑郁症，疼痛，精神病，P 阿金森氏病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）。

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