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1. 发明申请

WO2013037779A1 NEW DIHYDROQUINOLINE-2-ONE DERIVATIVES 审中-公开
标题翻译：新的二氢喹啉-2-酮衍生物
公开(公告)号：WO2013037779A1
公开(公告)日：2013-03-21
申请号：PCT/EP2012/067744
申请日：2012-09-12
申请人： F. HOFFMANN-LA ROCHE AG , AEBI, Johannes , AMREIN, Kurt , HORNSPERGER, Benoit , KNUST, Henner , KUHN, Bernd , LIU, Yongfu , MAERKI, Hans P. , MAYWEG, Alexander V. , MOHR, Peter , TAN, Xuefei , ZHOU, Mingwei
发明人： AEBI, Johannes , AMREIN, Kurt , HORNSPERGER, Benoit , KNUST, Henner , KUHN, Bernd , LIU, Yongfu , MAERKI, Hans P. , MAYWEG, Alexander V. , MOHR, Peter , TAN, Xuefei , ZHOU, Mingwei
IPC分类号： C07D401/04 , A61K31/4709 , A61P9/12
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/10 , C07F7/1856
摘要： The invention provides novel compounds having the general formula (I) wherein R 1 , R 2 , R 3 , R 4 ¸ R 5 , R 6 , R 7 , A 1 , A 2 and A 3 are as described herein, compositions including the compounds and methods of using the compounds.
摘要翻译：本发明提供具有通式（I）的新化合物，其中R 1，R 2，R 3，R 4 R 5，R 6，R 7，A 1，A 2和A 3如本文所述，包括该化合物的组合物和使用该化合物的方法。

2. 发明申请

WO2011073160A1 PYRROLIDINE DERIVATIVES AS NK - 3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为NK-3受体拮抗剂的吡咯烷衍生物
公开(公告)号：WO2011073160A1
公开(公告)日：2011-06-23
申请号：PCT/EP2010/069564
申请日：2010-12-14
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： C07D401/06 , C07D401/14 , C07D403/14 , C07D405/14 , A61P25/28 , A61K31/44
CPC分类号： C07D401/14 , C07D207/14 , C07D401/06 , C07D405/14
摘要： The present application relates to compounds of formula (I) wherein R 1 is hydrogen, halogen, cyano, lower alkyl or lower alkyl substituted by halogen; n is 1, 2 or 3, if n is 2 or 3, R 1 can be different; R 2 is C 2-7 -alkyl or C 3-6 -cycloalkyl; R 3 is the group (II) wherein X is CH or N; R 5 is hydrogen, -C(O)-lower alkyl, -C(O)O-lower alkyl, S(O) 2 -lower alkyl, -C(O)CH 2 O-lower alkyl, -C(O)-CH 2 -CN, or is - or -C(O)-cycloalkyl, cycloalkyl, or -CH 2 -cycloalkyl, wherein the cycloalkyl groups are optionally substituted by lower alkyl, -CH 2 -O-Iower alkyl, lower alkoxy, CF 3 , halogen or cyano, or is -C(O)-heterocycloalkyl or heterocycloalkyl, or is -C(O)-heteroaryl or is heteroaryl or is -C(O)-aryl or aryl, which heterocycloalkyl, heteroaryl or aryl groups are optionally substituted by halogen, lower alkyl, =O, lower alkoxy, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, -C(O)-CH 2 -N(di-lower alkyl), C(O)NH-lower alkyl, C(O)NH 2 , -O-C(O)- lower alkyl, C(O)-lower alkyl, S(O) 2 -lower alkyl or cyano; R 4 is aryl, which is optionally substituted by halogen, hydroxy, lower alkyl, lower alkyl substituted by halogen, S(O) 2 -lower alkyl, cyano or by lower alkoxy; 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：本申请涉及其中R 1为氢，卤素，氰基，低级烷基或被卤素取代的低级烷基的式（I）化合物; n为1,2或3，如果n为2或3，则R1可以不同; R2是C2-7烷基或C3-6-环烷基; R3是其中X是CH或N的基团（II）; R5是氢，-C（O） - 低级烷基，-C（O）O-低级烷基，S（O）2-低级烷基，-C（O）CH2O-低级烷基，-C（O） CN，或是 - 或-C（O） - 环烷基，环烷基或-CH 2 - 环烷基，其中环烷基任选被低级烷基，-CH 2 -O-低级烷基，低级烷氧基，CF 3，卤素或氰基取代，或是-C（O） - 杂环烷基或杂环烷基，或是-C（O） - 杂芳基或是杂芳基或是-C（O） - 芳基或杂芳基，该杂环烷基，杂芳基或芳基任选被卤素取代，低级烷基，= O，低级烷氧基，被卤素取代的低级烷基，被羟基取代的低级烷基，-C（O）-CH 2 -N（二低级烷基），C（O）NH-低级烷基，C（O），-OC（O） - 低级烷基，C（O） - 低级烷基，S（O）2 - 低级烷基或氰基; R4是芳基，其任选被卤素，羟基，低级烷基，被卤素，S（O）2 - 低级烷基，氰基或低级烷氧基取代的低级烷基取代; 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

WO2009071476A1 ISOXAZOLO-PYRIDINE DERIVATIVES 审中-公开
标题翻译： ISOXAZOLO-PYRIDINE衍生物
公开(公告)号：WO2009071476A1
公开(公告)日：2009-06-11
申请号：PCT/EP2008/066225
申请日：2008-11-26
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , JAKOB-ROETNE, Roland , KNUST, Henner , LUCAS, Matthew C. , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , JAKOB-ROETNE, Roland , KNUST, Henner , LUCAS, Matthew C. , THOMAS, Andrew
IPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , C07D487/04 , C07D491/10 , C07D491/08 , A61K31/4439 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , C07D487/04 , C07D491/08 , C07D491/10
摘要： The present invention is concerned with isoxazole-pyridine derivatives of formula (I) wherein: X is O or NH; R 1 is phenyl, pyridinyl, or pyrimidinyl, each optionally substituted with 1, 2 or 3 halo, R 2 is H or CH 3 or CF 3 ; R 3 , R 4 , R 5 , and R 6 are each independently H optionally substituted C 1-7 alkyl optionally substituted C 1-7 alkoxy CN, halo, NO 2 , S-C 1-7 alkyl, S(O)-C 1-7 alkyl optionally substituted benzyloxy -C(O)-R a , -C(O)-NR b R c , or a pharmaceutically acceptable salt thereof. The compounds are active on the GABA A α5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
摘要翻译：本发明涉及式（I）的异恶唑 - 吡啶衍生物，其中：X是O或NH; R1是苯基，吡啶基或嘧啶基，各自任选被1,2或3个卤素取代，R 2是H或CH 3或CF 3; R3，R4，R5和R6各自独立地为H任选取代的C 1-7烷基任选取代的C 1-7烷氧基CN，卤素，NO 2，S-C 1-7烷基，S（O）-C 1-7烷基任选取代的苄氧基-C（O） -R a，-C（O）-NR b R c或其药学上可接受的盐。这些化合物对GABA A a5受体结合位点是有活性的，可用于治疗认知障碍，如阿尔茨海默病。

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

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。

6. 发明申请

WO2007054444A2 3-ARYL-ISOXAZOLE-4-CARBONYL-BENZOFURAN DERIVATIVES 审中-公开
标题翻译： 3-芳基 - 异恶唑-4-羰基苯并呋喃衍生物
公开(公告)号：WO2007054444A2
公开(公告)日：2007-05-18
申请号：PCT/EP2006067879
申请日：2006-10-27
申请人： HOFFMANN LA ROCHE , BUETTELMANN BERND , HAN BO , KNUST HENNER , NETTEKOVEN MATTHIAS , THOMAS ANDREW
发明人： BUETTELMANN BERND , HAN BO , KNUST HENNER , NETTEKOVEN MATTHIAS , THOMAS ANDREW
IPC分类号： C07D413/06 , A61K31/42 , A61P25/28 , C07D413/14
CPC分类号： C07D413/06 , C07D413/14
摘要： The present invention is concerned with 3-aryl-isoxazole-4-carbonyl-benzofuran derivatives of formula (I) wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, hydroxy, lower alkoxy, OCF3, -OCH2-R, R3 is hydrogen or lower alkoxy; or R2 and R3 form together with the carbon atom to which they are attached a ring with -CH=CH-CH=-CH-; R is aryl or heteroaryl, optionally substituted by halogen or lower alkyl, or is C(O)NH-lower alkyl, or is -C(O)-heteroaryl, wherein the heteroaryl group is optionally substituted by lower alkyl or phenyl, and with their pharmaceutically acceptable acid addition salts. It has been found that this class of compounds show high affinity and selectivity for GABA A cc5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及其中R 1为氢或卤素的式（I）的3-芳基 - 异恶唑-4-羰基 - 苯并呋喃衍生物; R2是氢，卤素，羟基，低级烷氧基，OCF3，-OCH2-R，R3是氢或低级烷氧基; 或者R2和R3与它们所连接的碳原子一起形成具有-CH = CH-CH = -CH-的环; R 2为芳基或杂芳基，任选被卤素或低级烷基取代，或为C（O）NH-低级烷基，或为-C（O） - 杂芳基，其中杂芳基任选被低级烷基或苯基取代，其药学上可接受的酸加成盐。已经发现，这类化合物对GABA A cc5受体结合位点显示出高亲和力和选择性，并可用作认知增强剂或用于治疗认知障碍如阿尔茨海默氏病。

7. 发明申请

WO2007042420A1 ISOXAZOLE DERIVATIVES 审中-公开
标题翻译：异佛唑衍生物
公开(公告)号：WO2007042420A1
公开(公告)日：2007-04-19
申请号：PCT/EP2006/066959
申请日：2006-10-02
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , THOMAS, Andrew
IPC分类号： C07D413/06 , C07D413/14 , A61K31/41 , A61P25/00
CPC分类号： C07D413/14
摘要： The present invention is concerned with aryl-isoxazole-4-carbonyl-indole-carboxylic acid amide derivatives of formula (I) wherein R 1 is hydrogen, lower alkyl or aryl; R 2 is lower alkyl; R 3 is hydrogen or halogen; R 4 /R 5 is independently from each other hydrogen, lower alkyl, lower alkinyl, -(CH 2 )n-cycloalkyl, -(CH 2 ) n -heteroaryl, -(CH 2 ) n -heterocyclyl or -(CH 2 ) n -OH; n is 0, 1, 2 or 3; and with their pharmaceutically acceptable acid addition salts. It has been found that this class of compounds show high affinity and selectivity for GABA α 5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及式（I）的芳基 - 异恶唑-4-羰基 - 吲哚 - 羧酸酰胺衍生物，其中R 1是氢，低级烷基或芳基; R 2是低级烷基; R 3是氢或卤素; R 4和R 5彼此独立地为氢，低级烷基，低级炔基， - （CH 2 CH 2）n - 环烷基， - （（CH 2）n - 杂环基， - （CH 2）n - 杂环基或 - （CH 2）n - 2 ）_{名词 -OH; n为0,1,2或3; 和其药学上可接受的酸加成盐。已经发现，这类化合物显示出对GABA 5受体结合位点的高亲和力和选择性，并且可以用作认知增强剂或用于治疗诸如阿尔茨海默病的认知障碍。}

8. 发明申请

WO2006045429A1 HALOGEN SUBSTITUTED BENZODIAZEPINE DERIVATIVES 审中-公开
标题翻译：卤素取代的苯甲酸衍生物
公开(公告)号：WO2006045429A1
公开(公告)日：2006-05-04
申请号：PCT/EP2005/010907
申请日：2005-10-11
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , THOMAS, Andrew, William
发明人： KNUST, Henner , THOMAS, Andrew, William
IPC分类号： C07D487/14 , A61K31/55 , A61P25/00
CPC分类号： C07D487/14
摘要： The invention relates to halogen substituted imidazo [1,5-a] [1,2,4] triazolo [1,5d] [1,4]benzodiazepine derivatives of formula (I), and to their pharmaceutically acceptable acid addition salts. The compounds may be used for the treatment of cognitive enhancer, cognitive disorders, anxiety, Alzheimer's disease and schizophrenia.
摘要翻译：本发明涉及式（I）的卤素取代的咪唑并[1,5-a] [1,2,4]三唑并[1,5d] [1,4]苯并二氮杂衍生物及其药学上可接受的酸加成盐。该化合物可用于治疗认知增强剂，认知障碍，焦虑，阿尔茨海默病和精神分裂症。

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

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。

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