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1. 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。}

2. 发明申请

WO2007054444A3 3-ARYL-ISOXAZOLE-4-CARBONYL-BENZOFURAN DERIVATIVES 审中-公开
公开(公告)号：WO2007054444A3
公开(公告)日：2007-05-18
申请号：PCT/EP2006/067879
申请日：2006-10-27
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 , A61K31/42 , A61P25/28
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.

3. 发明申请

WO2007074089A1 ARYL-ISOXAZOL-4-YL-IMIDAZO[1, 5-A]PYRIDINE DERIVATIVES 审中-公开
标题翻译： ARYL-ISOXAZOL-4-YL-IMIDAZO [1,5-A]吡啶衍生物
公开(公告)号：WO2007074089A1
公开(公告)日：2007-07-05
申请号：PCT/EP2006/069792
申请日：2006-12-18
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , DONG, Jiaqiang , HAN, Bo , KNUST, Henner , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , DONG, Jiaqiang , HAN, Bo , KNUST, Henner , THOMAS, Andrew
IPC分类号： C07D471/04 , A61K31/4188 , A61K31/437 , A61P25/28
CPC分类号： C07D471/04
摘要： The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives of formula (I) wherein: R 1 is hydrogen, halogen, hydroxy, lower alkyl, benzyloxy or -O-(CH 2 )-(CO)-5 or 6 membered heteroaryl optionally substituted by aryl and lower alkyl; R 2 is hydrogen, lower alkyl, or -(CO)-R a ; R 3 is hydrogen, halogen, cyano, lower alkyl, or -(CO)-R a ; R a is hydroxy, lower alkoxy, NR'R'', wherein R' and R'' are each independently hydrogen, cycloalkyl, 5 or 6-membered heterocycloalkyl or lower alkyl optionally substituted by cycloalkyl, cyano, 5 or 6-membered heterocycloalkyl or 5 or 6-membered heteroaryl; as well as pharmaceutically acceptable acid addition salts thereof. It has been found that this class of compounds show high affinity and selectivity for GABA A α5 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-基 - 咪唑并[1,5-a]吡啶衍生物，其中：R 1是氢，卤素，羟基，低级烷基，任选被芳基和低级烷基取代的苄氧基或-O-（CH 2）2 - （CO）-5或6元杂芳基; R 2是氢，低级烷基或 - （CO）-R a; R 3是氢，卤素，氰基，低级烷基或 - （CO）-R a）。 R“是羟基，低级烷氧基，NR'R”，其中R'和R“各自独立地为氢，环烷基，5或6元杂环烷基或任选被环烷基取代的低级烷基，氰基，5或6元杂环烷基或5或6元杂芳基; 以及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 A a5受体结合位点的高亲和力和选择性，并且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。

4. 发明申请

WO2007082806A1 ARYL-ISOXAZOL-4-YL-IMIDAZO[1,2-A]PYRIDINE USEFUL FOR THE TREATMENT OF ALZHEIMER’S DISEASE VIA GABA RECEPTORS 审中-公开
标题翻译： ARYL-ISOXAZOL-4-YL-IMIDAZO [1,2-A]吡啶可用于通过GABA受体治疗阿尔茨海默病
公开(公告)号：WO2007082806A1
公开(公告)日：2007-07-26
申请号：PCT/EP2007/050137
申请日：2007-01-08
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , THOMAS, Andrew
IPC分类号： C07D471/04 , A61K31/437 , A61P25/28
CPC分类号： C07D471/04
摘要： The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives of formula (I): wherein R 1 is hydrogen, halogen, hydroxy, lower alkyl, benzyloxy or -O-(CH 2 )-(CO)-5 or 6 membered heteroaryl optionally substituted by aryl or by lower alkyl; R 2 is hydrogen, halogen, lower alkyl, lower alkynyl, amino, -NHC(O)-R a or -(CO)-R a ; R 3 is hydrogen, halogen, cyano, lower alkyl, lower alkynyl, amino, -NHC(O)-R a , -(CO)-R a , -5 or 6-membered heterocycloalkyl in 1-position, optionally substituted 10 by =O or is a -5 or 6-membered heteroaryl in 1-position; R 4 is hydrogen or -5 or 6-membered heteroaryl; R 5 is lower alkyl or cycloalkyl; R a is lower alkoxy or NR'R'', wherein R' and R'' are each independently hydrogen, lower alkyl optionally substituted by hydroxy, lower alkynyl, -(CH 2 ) n -cycloalkyl, 15 -(CH 2 ) n -5 or 6-membered heterocycloalkyl or -(CH 2 ) n -5 or 6-membered heteroaryl; n is 0 to 3; as well as pharmaceutically acceptable acid addition salts thereof. It has been found that this class of compounds show high affinity and selectivity for GABA A α5 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-基 - 咪唑并[1,2-a]吡啶衍生物：其中R 1是氢，卤素，羟基，低级烷基，任选被芳基或低级烷基取代的苄氧基或-O-（CH 2 - ） - （CO）-5或6元杂芳基; R 2是氢，卤素，低级烷基，低级炔基，氨基，-NHC（O）-R a或 - （CO）-R a， SUP>; R 3是氢，卤素，氰基，低级烷基，低级炔基，氨基，-NHC（O）-R a， - （CO）-R a 1-位的-5或6-元杂环烷基，任选地被10取代或被1位置的5或6元杂芳基取代; R 4是氢或-5或6元杂芳基; R 5是低级烷基或环烷基; R“是低级烷氧基或NR'R”，其中R'和R“各自独立地为氢，任选被羟基取代的低级烷基，低级炔基， - （CH 2） 15 - （CH 2）n - 或 - 或 - 6元杂环烷基或 - （CH 2） -5或6元杂芳基; n为0〜3; 以及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 A a5受体结合位点的高亲和力和选择性，并且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。

5. 发明申请

WO2007074078A3 ARYL-ISOXAZOL-4-YL-IMIDAZOLE DERIVATIVES 审中-公开
公开(公告)号：WO2007074078A3
公开(公告)日：2007-07-05
申请号：PCT/EP2006/069722
申请日：2006-12-14
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , THOMAS, Andrew
IPC分类号： C07D413/04 , A61K31/42 , A61K31/4178
摘要： The present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula (I), wherein R 1 to R 3 are each independently hydrogen or halogen; R 4 is hydrogen, lower alkyl, cycloalkyl, -(CH 2 ) n -O-lower alkyl or lower alkyl substituted by hydroxy; R 5 is -(CH 2 ) m -aryl or -(CH 2 ) m -heteroaryl which are optionally substituted by one or more substituents selected from the group consisting of halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkylsulfanyl, lower alkyl substituted by halogen, -C(O)-lower alkyl, -C(O)-O-lower alkyl, -NH-C(O)-O-lower alkyl or -C(O)-NH-R', wherein R' is lower alkynyl or lower alkyl substituted by halogen, or is -(CH 2 ) n -cycloalkyl, -(CH 2 ) n -heterocyclyl, -(CH 2 ) n -heteroaryl or -(CH 2 ) n -aryl, optionally substituted by halogen; R 6 is hydrogen, -C(O)H, -(CH 2 ) n -O-lower alkyl, -C(O)O-lower alkyl, lower alkyl substituted by hydroxy or halogen, or is cycloalkyl, aryl, or is -(CH 2 ) n -O-CH 2 -aryl, optionally substituted by halogen or lower alkyl, or is -(CH 2 ) n -O-CH 2 -heteroaryl, optionally substituted by halogen, lower alkyl or lower alkyl substituted by halogen, or is -(CH 2 ) n -NH-(CH 2 ) o -heterocyclyl; n is 0, 1, 2 or 3 m is 0 or 1; o is 1, 2 or 3; as well as with pharmaceutically acceptable acid addition salts thereof. It has been found that this class of compounds show high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

6. 发明申请

WO2007071598A1 ARYL-ISOXAZOLO-4-YL-OXADIAZOLE DERIVATIVES 审中-公开
公开(公告)号：WO2007071598A1
公开(公告)日：2007-06-28
申请号：PCT/EP2006/069625
申请日：2006-12-13
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , KOBLET, Andreas , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , HAN, Bo , KNUST, Henner , KOBLET, Andreas , THOMAS, Andrew
IPC分类号： C07D413/04 , C07D413/14 , A61K31/4245 , A61K31/4439 , A61P25/28
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is concerned with isoxazol-4-yl-oxadiazole derivatives of formula (I) wherein R 1 is hydrogen, halogen, aryl, heterocyclyl, heteroaryl, cyano, lower alkyl, -(CH 2 ) n -cycloalkyl, -(CH 2 ) n -N(R) 2 , -(CH 2 ) n -O-lower alkyl or -(CH 2 ) n -OH; n is 0,1 or 2 R is hydrogen or lower alkyl; R 2 is cycloalkyl, aryl, heteroaryl or heterocyclyl, which are optionally substituted by one or more substituents, selected from the group consisting of halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkoxy substituted by halogen, lower alkyl substituted by halogen, C(O)O-lower alkyl, lower alkylsulfonyl, -NR a R b , -C(O)-NR a R b , -C(O)-heterocyclyl, benzyloxy, heterocyclyl optionally substituted by hydroxy, halogen or lower alkyl, or is heteroaryl optionally substituted by lower alkyl; R a and R b are independently hydrogen, lower alkylsulfonyl, -C(O)H, -(CH 2 ) n -N(R) 2 , -(CH 2 ) n -O-lower alkyl, -(CH 2 ) n -S-lower alkyl, -(CH 2 ) n -S(O) 2 -lower alkyl, heteroarylsulfonyl, lower alkyl, -(CH2)n-heterocyclyl, optionally substituted by lower alkyl, or is -(CH 2 ) n -cycloalkyl, -(CH 2 ) n -heteroaryl, -(CH 2 ) n -OH, -(CO)-R', wherein R' is lower alkyl, cycloalkyl or heteroaryl; R 3 is aryl or heteroaryl, which are optionally substituted by halogen or lower alkyl substituted by halogen; as well as pharmaceutically acceptable acid addition salts thereof. It has been found that this class of compounds show high affinity and selectivity for GABA α5 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）的异恶唑-4-基 - 恶二唑衍生物，其中R 1是氢，卤素，芳基，杂环基，杂芳基，氰基，低级烷基， - （CH

7. 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。

8. 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。

9. 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。

10. 发明申请

WO2010127978A1 ISOXAZOLE-PYRIDINE DERIVATIVES AS GABA MODULATORS 审中-公开
标题翻译：作为GABA调节剂的异噻唑衍生物
公开(公告)号：WO2010127978A1
公开(公告)日：2010-11-11
申请号：PCT/EP2010/055701
申请日：2010-04-28
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 , A61K31/4439 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with novel isoxazole derivatives of formula (I) wherein X, R 1 , R 2 , R 3 and R 4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A α5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula (I), pharmaceutical compositions containing them and their use as medicaments.
摘要翻译：本发明涉及式（I）的新的异恶唑衍生物，其中X，R 1，R 2，R 3和R 4如本文所述，以及其药学上可接受的盐和酯。本发明的活性化合物对GABA A a5受体具有亲和性和选择性。此外，本发明涉及制备式（I）的活性化合物，含有它们的药物组合物及其作为药物的用途。

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