专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

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

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。

3. 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。

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

WO2011092272A1 GAMMA SECRETASE MODULATERS 审中-公开
标题翻译： GAMMA秘密调制解调器
公开(公告)号：WO2011092272A1
公开(公告)日：2011-08-04
申请号：PCT/EP2011/051184
申请日：2011-01-28
申请人： F. HOFFMANN-LA ROCHE AG , BAUMANN, Karlheinz , GOETSCHI, Erwin , GREEN, Luke , JOLIDON, Synese , KNUST, Henner , LIMBERG, Anja , LUEBBERS, Thomas , THOMAS, Andrew
发明人： BAUMANN, Karlheinz , GOETSCHI, Erwin , GREEN, Luke , JOLIDON, Synese , KNUST, Henner , LIMBERG, Anja , LUEBBERS, Thomas , THOMAS, Andrew
IPC分类号： C07D471/04 , C07D487/04 , C07D498/04 , A61K31/4196 , A61P25/00
CPC分类号： C07D471/04 , C07D487/04 , C07D498/04
摘要： The invention relates to compounds of formula ( I ) wherein R 1 /R 1' are independently from each other hydrogen, halogen, lower alkoxy or cyano; R 2 is lower alkyl, halogen, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, lower alkyl substituted by OR, =0, -C(O)O-lower alkyl, -C(O)NH-lower alkyl, cyano, CH 2 -O-lower alkyl, cycloalkyl, NRR'or is -O-(CH 2 ) o -phenyl optionally substituted by halogen, or is -(CH 2 ) o -phenyl optionally substituted by one, two or three substituents, selected from halogen, -(CH 2 ) o -cyano, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, C(O)H, -CH 2 -NH 2 -, -CH 2 -NH-C(O)O-lower alkyl, -CH 2 -NH-C(O)-lower alkyl, -CH 2 -NH-lower alkyl, -CH 2 -NH-S(O) 2 -lower alkyl, lower alkoxy or by lower alkoxy substituted by halogen, or is -(CH 2 ) o -cycloalkyl, or is -(CH 2 ) o -heterocycloalkyl which is optionally substituted by halogen, CF 3 , lower alkyl, -CH 2 CN, -C(O)-lower alkyl, -C(O)O-lower alkyl or S(O) 2 -lower alkyl, or is heteroaryl selected from the group consisting of furanyl, pyrazinyl, pyridinyl, benzooxazolyl or benzoimidazolyl which are optionally substituted by lower alkyl, or is 4-methyl-3,4-dihydro-2H-benzo[l,4]oxazine R and R' are independently from each other hydrogen or lower alkyl, and o is 0 or 1; R 3 may occur once or twice and is lower alkyl; A is Formula a), b), c), d), e), f), h), i), j) and Formula k); R 2' is hydrogen, lower alkyl, lower alkyl substituted by halogen, C(O)-lower alkyl, S(O) 2 -lower alkyl or phenyl optionally substituted by halogen; hetaryl is a 5 or 6 membered N, S or O-containing heteroaryl group; n is O, 1, 2 or 3; if n is 2 or 3, R 2 may be the same or not; or to pharmaceutically active acid addition salts thereof. The present compounds of formula ( I ) are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi- infarct dementia, dementia pugilistica and Down syndrome.
摘要翻译：本发明涉及其中R 1 / R 1'彼此独立地为氢，卤素，低级烷氧基或氰基的式（I）化合物; R2是低级烷基，卤素，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，被OR取代的低级烷基，= 0，-C（O）O-低级烷基，-C（O），氰基，CH 2 -O-低级烷基，环烷基，NRR'或是任选被卤素取代的-O-（CH 2）o - 苯基，或是被选定的被一个，两个或三个取代基任选取代的 - （CH 2）卤代低级烷基，被卤素取代的低级烷基，被羟基取代的低级烷基，C（O）H，-CH 2 -NH 2 - ， - CH 2 -NH-C（O）O-低级烷基，-CH 2 -NH-C（O） - 低级烷基，-CH 2 -NH-低级烷基，-CH 2 -NH-S（O）2 - 低级烷基，低级烷氧基或被卤素取代的低级烷氧基，（CH 2）o - 环烷基，或者是 - （CH 2）o - 杂环烷基，其任选被卤素，CF 3，低级烷基，-CH 2 CN，-C（O） - 低级烷基，-C（O）O-低级烷基或 S（O）2-低级烷基，或者是选自呋喃基，吡嗪基，吡啶基，苯并恶唑基或苯并咪唑基的杂芳基。或是4-甲基-3,4-二氢-2H-苯并[1,4]恶嗪R和R'彼此独立地为氢或低级烷基，o为0或1; R3可以发生一次或两次，并且是低级烷基; A是公式a），b），c），d），e），f），h），i），j）和公式k）; R 2'是氢，低级烷基，被卤素取代的低级烷基，C（O） - 低级烷基，任选被卤素取代的S（O）2 - 低级烷基或苯基）杂芳基是5或6元N，S或O的杂芳基; n是0,1,2或3; 如果n为2或3，则R2可以相同或不相同; 或其药物活性的酸加成盐。本发明的式（I）化合物是淀粉样蛋白β的调节剂，因此它们可用于治疗或预防与脑中β-淀粉样蛋白沉积相关的疾病，特别是阿尔茨海默病，以及其他疾病，例如脑淀粉样血管病，遗传性脑出血伴淀粉样变性，荷兰型（HCHWA-D），多发梗死性痴呆，痴呆和唐氏综合征。

9. 发明申请

WO2011101304A2 PIPERIDINE DERIVATIVES 审中-公开
标题翻译：哌啶衍生物
公开(公告)号：WO2011101304A2
公开(公告)日：2011-08-25
申请号：PCT/EP2011/052101
申请日：2011-02-14
申请人： F. HOFFMANN-LA ROCHE AG , BAUMANN, Karlheinz , FLOHR, Alexander , GOETSCHI, Erwin , GREEN, Luke , JOLIDON, Synese , KNUST, Henner , LIMBERG, Anja , LUEBBERS, Thomas , THOMAS, Andrew
发明人： BAUMANN, Karlheinz , FLOHR, Alexander , GOETSCHI, Erwin , GREEN, Luke , JOLIDON, Synese , KNUST, Henner , LIMBERG, Anja , LUEBBERS, Thomas , THOMAS, Andrew
IPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04 , A61K31/4523 , A61P25/28
CPC分类号： C07D471/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D498/04
摘要： The invention relates to compounds of formula (I). Hetaryl I is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N; hetaryl II is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N, or is a two membered ring system containing 1 to 4 heteroatoms selected from S, O or N, wherein at least one ring is aromatic in nature; R 1 is lower alkyl, lower alkoxy, lower alkyl substituted by halogen, or halogen; R 2 is halogen, lower alkyl, lower alkoxy, hydroxy, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy or benzo[1,3]dioxolyl, or is -(CHR) p -phenyl, optionally substituted by halogen, lower alkyl, lower alkoxy, S(O) 2 -lower alkyl, cyano, nitro, lower alkoxy substituted by halogen, dimethylamino, -(CH 2 )P-NHC(O)O-Iower alkyl, or lower alkyl substituted by halogen, and R is hydrogen, halogen, hydroxy or lower alkoxy, or is cycloalkenyl or cycloalkyl, optionally substituted by hydroxy or lower alkyl substituted by halogen, or is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N, which is optionally substituted by halogen, lower alkyl, lower alkoxy or dimethylamino, or is O-phenyl, optionally substituted by halogen, or is heterocycloalkyl, optionally substituted by halogen, hydroxy, lower alkyl substituted by halogen or C(O)O-lower alkyl; R 3 is hydrogen, lower alkyl, cyano or phenyl; R 4 is lower alkoxy, lower alkyl or halogen; p is 0 or 1; n is 0, 1 or 2; if n is 2 then R 4 may be the same or different; m is 0, 1 or 2; if m is 2 then R 1 may be the same or different; o is 0, 1, 2 or 3, if o is 2 or 3 then R 2 may be the same or different; or to pharmaceutically active acid addition salts thereof. The compounds of formula (I) are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
摘要翻译：本发明涉及式（I）的化合物。 Hetary11是含有1至3个选自O，S或N的杂原子的五元或六元杂芳基; 杂芳基II是含有1至3个选自O，S或N的杂原子的五元或六元杂芳基，或者是含有1至4个选自S，O或N的杂原子的二元环体系，其中至少一个环本质上是芳香的; R 1为低级烷基，低级烷氧基，被卤素取代的低级烷基或卤素; R 2是卤素，低级烷基，低级烷氧基，羟基，被卤素取代的低级烷基，被羟基或苯并[1,3]二氧杂环戊烯基取代的低级烷基，或者是 - （CHR）p 低级烷基，低级烷氧基，S（O）2 - 低级烷基，氰基，硝基，被卤素取代的低级烷氧基，二甲基氨基， - （CH 2）（O）O-低级烷基或被卤素取代的低级烷基，且R为氢，卤素，羟基或低级烷氧基，或者为环烯基或环烷基，任选被羟基或低级被卤素取代的烷基，或者是含有1至3个选自O，S或N的杂原子的五元或六元杂芳基，其任选被卤素，低级烷基，低级烷氧基或二甲基氨基取代，或者是O-苯基，任选被卤素取代，或者为任选被卤素，羟基，被卤素取代的低级烷基或C（O）O-低级烷基取代的杂环烷基; R 3是氢，低级烷基，氰基或苯基; R 4是低级烷氧基，低级烷基或卤素; p是0或1; n是0,1或2; 如果n是2，则R 4可以相同或不同; m是0,1或2; 如果m是2，则R 1可以相同或不同; o是0,1,2或3，如果o是2或3，则R 2可以相同或不同; 或其药学活性酸加成盐。式（I）化合物是β-淀粉样蛋白的调节剂，因此它们可用于治疗或预防与β-淀粉状蛋白在脑中沉积相关的疾病，特别是阿尔茨海默氏病和其他疾病，如脑具有淀粉样变性的遗传性脑出血，荷兰型（HCHWA-D），多发性梗塞型痴呆，拳击员痴呆和唐氏综合症。

10. 发明申请

WO2007107346A1 SUBSTITUTED INDAZOLE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译：取代的吲哚衍生物，其制造和用作药物代理
公开(公告)号：WO2007107346A1
公开(公告)日：2007-09-27
申请号：PCT/EP2007/002487
申请日：2007-03-21
申请人： F. HOFFMANN-LA ROCHE AG , GEORGES, Guy , GOLLER, Bernhard , LIMBERG, Anja , RUEGER, Petra , RUETH, Matthias , SCHUELL, Christine , STAHL, Mark
发明人： GEORGES, Guy , GOLLER, Bernhard , LIMBERG, Anja , RUEGER, Petra , RUETH, Matthias , SCHUELL, Christine , STAHL, Mark
IPC分类号： C07D487/04 , A61K31/4188 , A61P35/00
CPC分类号： C07D487/04
摘要： Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明的目的是式（I）化合物的药学上可接受的盐，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物及其制备方法，以及上述用途，提及的化合物在控制或预防诸如癌症的疾病中。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式