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1. 发明申请

WO2013020993A1 COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS DISEASE 审中-公开
标题翻译：用于治疗和预防呼吸道感染病毒性疾病的化合物
公开(公告)号：WO2013020993A1
公开(公告)日：2013-02-14
申请号：PCT/EP2012/065499
申请日：2012-08-08
申请人： F. HOFFMANN-LA ROCHE AG , CHEN, Li , FENG, Lichun , FENG, Song , GAO, Lu , GUO, Tao , HUANG, Mengwei , LIANG, Chungen , LIU, Yongfu , WANG, Lisha , WONG, Jason Christopher , WU, Jim Zhen , WU, Xihan , YUN, Hongying , ZHENG, Xiufang
发明人： CHEN, Li , FENG, Lichun , FENG, Song , GAO, Lu , GUO, Tao , HUANG, Mengwei , LIANG, Chungen , LIU, Yongfu , WANG, Lisha , WONG, Jason Christopher , WU, Jim Zhen , WU, Xihan , YUN, Hongying , ZHENG, Xiufang
IPC分类号： C07D403/04 , C07D413/04 , C07D417/04 , C07D417/14 , A61K31/553 , A61K31/554 , A61P11/00 , A61P31/12
CPC分类号： C07D493/10 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D487/04 , C07D491/107
摘要： A compound of formula (I), as well as pharmaceutically acceptable salt thereof, wherein R 1 to R 10 , A, Q, X and Y are as defined in description and in claims, can be used as a medicament for the treatment of respiratory syncytial virus.
摘要翻译：式（I）化合物及其药学上可接受的盐，其中R 1至R 10，A，Q，X和Y如描述和权利要求中所定义，可用作治疗呼吸道合胞病毒的药物。

2. 发明申请

WO2010031708A3 ORTHO-AMINOANILIDES FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2010031708A3
公开(公告)日：2010-03-25
申请号：PCT/EP2009/061533
申请日：2009-09-07
申请人： F. HOFFMANN-LA ROCHE AG , LIANG, Chungen , TANG, Guozhi , WONG, Jason Christopher , WU, Xihan
发明人： LIANG, Chungen , TANG, Guozhi , WONG, Jason Christopher , WU, Xihan
IPC分类号： C07D207/06 , C07D207/12 , C07D211/42 , C07D265/30 , C07D265/34 , C07D413/06 , A61K31/535 , A61K31/5377 , A61K31/40 , A61P35/00
摘要： The present invention is directed to the compounds of formula (I), wherein R 1 to R 5 have the significances given herein, to processes for the manufacture of said compounds as well as medicaments containing said compounds. The compounds according to this invention show anti-proliferative and differentiation-inducing activity and are thus useful for the treatment of diseases such as cancer in humans or animals.

3. 发明申请

WO2010094678A1 NOVEL ORTHO-AMINOAMIDES FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的新型对羟基氨基酚
公开(公告)号：WO2010094678A1
公开(公告)日：2010-08-26
申请号：PCT/EP2010/051909
申请日：2010-02-16
申请人： F. HOFFMANN-LA ROCHE AG , LIANG, Chungen , TANG, Guozhi , WONG, Jason Christopher , WU, Xihan , ZHANG, Zhenshan
发明人： LIANG, Chungen , TANG, Guozhi , WONG, Jason Christopher , WU, Xihan , ZHANG, Zhenshan
IPC分类号： C07D207/16 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/14 , C07D409/04 , A61K31/435
CPC分类号： C07D207/16 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/14 , C07D409/04
摘要： The present invention is directed to the compounds of formula (I) wherein R, R 1 and R 2 have the significances given herein, to processes for the manufacture of said compounds as well as medicaments containing said compounds. The compounds according to this invention show anti-proliferative and differentiation-inducing activity and are thus useful for the treatment of diseases such as cancer in humans or animals.
摘要翻译：本发明涉及其中R，R 1和R 2具有本文给出的意义的式（I）化合物，所述化合物的制备方法以及含有所述化合物的药物。根据本发明的化合物显示抗增殖和分化诱导活性，因此可用于治疗诸如人或动物中的癌症的疾病。

4. 发明申请

WO2009138338A1 NOVEL N-(2-AMINO-PHENYL)-ACRYLAMIDES 审中-公开
标题翻译：新型N-（2-氨基 - 苯基） - 丙烯酰胺
公开(公告)号：WO2009138338A1
公开(公告)日：2009-11-19
申请号：PCT/EP2009/055441
申请日：2009-05-06
申请人： F. HOFFMANN-LA ROCHE AG , WONG, Jason Christopher , WU, Xihan
发明人： WONG, Jason Christopher , WU, Xihan
IPC分类号： C07D207/10 , C07D207/12 , C07D207/14 , C07D401/12 , C07D405/12 , C07D491/08 , A61K31/40 , A61K31/4433 , A61K31/444 , A61P35/00
CPC分类号： C07D207/10 , C07D207/12 , C07D207/14 , C07D401/12 , C07D405/12 , C07D491/08
摘要： The present invention is directed to the compounds of formula (I), wherein R 1 to R 4 have the significances given herein, to processes for the manufacture of said compounds as well as medicaments containing said compounds. The compounds according to this invention show anti-proliferative and differentiation-inducing activity and are thus useful for the treatment of diseases such as cancer in humans or animals.
摘要翻译：本发明涉及式（I）化合物，其中R1至R4具有本文给出的意义，涉及制备所述化合物的方法以及含有所述化合物的药物。根据本发明的化合物显示抗增殖和分化诱导活性，因此可用于治疗诸如人或动物中的癌症的疾病。

5. 发明申请

WO2007071348A1 ISOQUINOLINE AMINOPYRAZOLE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：异喹啉氨基吡唑衍生物及其制造和用作治疗癌症的药物代理
公开(公告)号：WO2007071348A1
公开(公告)日：2007-06-28
申请号：PCT/EP2006/012112
申请日：2006-12-15
申请人： F. HOFFMANN-LA ROCHE AG , CHEN, Li , GEORGES, Guy , MERTENS, Alfred , WU, Xihan
发明人： CHEN, Li , GEORGES, Guy , MERTENS, Alfred , WU, Xihan
IPC分类号： C07D401/12 , C07D401/14 , C07D409/14 , A61K31/4725 , A61P35/00
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
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。

6. 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。

7. 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。

8. 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。

9. 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。

10. 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。

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