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1. 发明申请

WO2011131571A1 PYRRAZOLOPYRIDINE DERIVATIVES 审中-公开
标题翻译：吡咯并吡啶衍生物
公开(公告)号：WO2011131571A1
公开(公告)日：2011-10-27
申请号：PCT/EP2011/055971
申请日：2011-04-15
申请人： F. HOFFMANN-LA ROCHE AG , JABLONSKI, Philippe , NETTEKOVEN, Matthias , PATINY-ADAM, Angelique , RATNI, Hasane , STADLER, Heinz
发明人： JABLONSKI, Philippe , NETTEKOVEN, Matthias , PATINY-ADAM, Angelique , RATNI, Hasane , STADLER, Heinz
IPC分类号： C07D487/04 , A61K31/4353 , A61P25/18
CPC分类号： C07D487/04
摘要： The present invention relates to a compound of formula (I), wherein R 1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, benzyl, -C(0)-lower alkyl, -C(0)-CH 2 -lower alkoxy, -C(0)-C 3-6 -cycloalkyl, -(CH 2 ) ° -C(0)-NR,R', -(CH 2 ) ° S(0) 2 - lower alkyl or -S(0) 2 -NR,R'; o is 0 or 1; R,R' are independently from each other hydrogen or lower alkyl, or may form together with the N atom to which they are attached a 5 or 6 membered heterocycloalkyl ring; R 2 is hydrogen or lower alkyl; R 3 is halogen, lower alkoxy, lower alkyl substituted by halogen or lower alkoxy substituted by halogen; and may be the same or different in case n is 2; n is 1 or 2; Ar is phenyl optionally substituted by one or two substituents selected from lower alkyl, halogen, lower alkoxy, lower alkyl substituted by hydroxy or cyano, or is a five or six membered heteroaryl group, selected from thiophenyl or pyridinyl which are optionally substituted by lower alkyl or halogen; or to a pharmaceutically active acid addition salt. It has surprisingly been found that the compounds of formula I show a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢，低级烷基，被卤素取代的低级烷基，苄基，-C（O） - 低级烷基，-C（O）-CH 2 - 低级烷氧基， - C（O）-C 3-6环烷基， - （CH 2）-C（O）-NR，R'， - （CH 2） R'; o为0或1; R，R'彼此独立地为氢或低级烷基，或者与它们所连接的N原子一起形成5或6元杂环烷基环; R2是氢或低级烷基; R3是卤素，低级烷氧基，被卤素取代的低级烷基或被卤素取代的低级烷氧基; 并且在n为2的情况下可以相同或不同; n为1或2; Ar是任选被一个或两个选自低级烷基，卤素，低级烷氧基，被羟基或氰基取代的低级烷基的取代基取代的苯基，或者是选自噻吩基或吡啶基的五或六元杂芳基，其任选被低级烷基或卤素; 或药物活性的酸加成盐。惊奇地发现，式I化合物同时对NK1和NK3受体（双重NK1 / NK3受体拮抗剂）显示出高亲和力，可用于治疗精神分裂症。

2. 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。

3. 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。

4. 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。

5. 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。

6. 发明申请

WO2006037480A8 HEXAFLUOROISOPROPANOL SUBSTITUTED ETHER DERIVATIVES 审中-公开
标题翻译：十六烷基二醇取代的衍生物
公开(公告)号：WO2006037480A8
公开(公告)日：2006-05-18
申请号：PCT/EP2005010237
申请日：2005-09-22
申请人： HOFFMANN LA ROCHE , DEHMLOW HENRIETTA , KUHN BERND , PANDAY NARENDRA , RATNI HASANE , WRIGHT MATTHEW BLAKE
发明人： DEHMLOW HENRIETTA , KUHN BERND , PANDAY NARENDRA , RATNI HASANE , WRIGHT MATTHEW BLAKE
IPC分类号： C07C69/92 , A61K31/085 , A61K31/192 , A61K31/216 , A61K31/235 , A61K31/421 , A61K31/423 , A61K31/428 , C07C43/23 , C07C59/68 , C07C65/24 , C07C69/734 , C07D261/20 , C07D263/32 , C07D275/04
CPC分类号： C07D275/04 , C07C43/23 , C07C59/68 , C07C65/24 , C07C69/734 , C07C69/92 , C07D249/06 , C07D261/08 , C07D261/20 , C07D263/32
摘要： The invention is concerned with hexafluoroisopropanol substituted ether derivatives of formula (I), wherein R l to R 3 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.
摘要翻译：本发明涉及式（I）的六氟异丙醇取代的醚衍生物，其中R 1至R 3如在说明书和权利要求书中所定义，以及生理学上可接受的盐和酯。这些化合物与LXRα和LXRβ结合，可用作药物。

7. 发明申请

WO2005105791A1 INDOLYL DERIVATIVES AS LIVER-X-RECEPTOR MODULATORS 审中-公开
标题翻译：作为肝脏受体调节剂的吲哚衍生物
公开(公告)号：WO2005105791A1
公开(公告)日：2005-11-10
申请号：PCT/EP2005/004454
申请日：2005-04-26
申请人： F. HOFFMANN-LA ROCHE AG , DEHMLOW, Henrietta , KUHN, Bernd , PANDAY, Narendra , RATNI, Hasane , SCHULZ-GASCH, Tanja , WRIGHT, Matthew, Blake
发明人： DEHMLOW, Henrietta , KUHN, Bernd , PANDAY, Narendra , RATNI, Hasane , SCHULZ-GASCH, Tanja , WRIGHT, Matthew, Blake
IPC分类号： C07D413/06
CPC分类号： C07D413/06 , C07D209/08 , C07D209/12 , C07D209/30 , C07D401/06 , C07D403/06 , C07D409/06 , C07D413/10 , C07D417/06
摘要： Compounds of formula (I) and pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A, m, n and p are defined as in claim 1. These compounds can be used as medicaments in the treatment of diseases such as artherosclerosis and diabetes.
摘要翻译：式（I）化合物及其药学上可接受的盐和药学上可接受的酯，其中R 1，R 2，R 3，R 4，R 5，R 6，A，m ，n和p如权利要求1中所定义。这些化合物可用作治疗诸如动脉粥样硬化和糖尿病的疾病的药物。

8. 发明申请

WO2013024168A1 PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE 审中-公开
标题翻译：用于治疗诸如阿尔茨海默病的TAUOPATHIES的哌嗪衍生物
公开(公告)号：WO2013024168A1
公开(公告)日：2013-02-21
申请号：PCT/EP2012/066136
申请日：2012-08-17
申请人： REMYND NV , GRIFFIOEN, Gerard , CECERE, Giuseppe , NETTEKOVEN, Matthias , PRINCEN, Katrien , RATNI, Hasane , ROGERS-EVANS, Mark , VIFIAN, Walter
发明人： GRIFFIOEN, Gerard , CECERE, Giuseppe , NETTEKOVEN, Matthias , PRINCEN, Katrien , RATNI, Hasane , ROGERS-EVANS, Mark , VIFIAN, Walter
IPC分类号： C07D285/08 , C07D417/04 , C07D417/12 , A61K31/433 , A61P25/28
CPC分类号： A61K31/496 , C07D285/08 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to a compound of formula (IA), wherein G 1 is lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is -NR 2 R 3 ; R 2 is hydrogen or lower alkyl; R 3 is lower alkyl; tetrahydropyran-4-yl; -CH 2 -cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or R 2 and R 3 form together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is -CH 2 - or -(CH 2 ) 2 -; Ar is phenyl or pyridinyl; R 4 is halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a compound of formula (IA) for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.
摘要翻译：本发明涉及式（IA）化合物，其中G 1为低级烷基; 被一个或多个卤素取代的低级烷基; 环烷基; 四氢吡喃-4-基; 苯; 被一个或多个卤素取代的苯乙基; 苯氧基; 被一个或多个卤素取代的苯氧基甲基; 苄氧; 由一个或多个卤素取代的苄氧基 - 乙基; 或为-NR2R3; R2是氢或低级烷基; R3是低级烷基; 四氢吡喃-4-基; -CH 2 - 环烷基; 或任选被被一个或多个卤素取代的低级烷基取代的环烷基; 或R 2和R 3与它们所连接的N-原子一起形成具有4或5个碳原子的杂环烷基，其任选被一个或多个选自卤素的取代基取代; 或被一个或多个卤素取代的低级烷基; X是-CH 2 - 或 - （CH 2）2 - ; Ar是苯基或吡啶基; R4是卤素; 低级烷基被一个或多个卤素取代的低级烷基; 或低级烷氧基; n为1或2; 或其药物活性盐与立体异构体形式，包括式（IA）化合物的单独非对映异构体或对映异构体以及其外消旋或非外消旋混合物。本发明还涉及式（IA）化合物用于治疗以细胞毒性TAU错误折叠和/或聚集为特征的某些神经变性疾病的用途。

9. 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。

10. 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。

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