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1. 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。

2. 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。

3. 发明申请

WO2009071477A1 ISOXAZOLO-PYRIDAZINE DERIVATIVES 审中-公开
标题翻译： ISOXAZOLO-PYRIDAZINE衍生物
公开(公告)号：WO2009071477A1
公开(公告)日：2009-06-11
申请号：PCT/EP2008/066226
申请日：2008-11-26
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , JAKOB-ROETNE, Roland , KNUST, Henner , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , JAKOB-ROETNE, Roland , KNUST, Henner , THOMAS, Andrew
IPC分类号： C07D413/12 , C07D413/14 , C07D487/04 , A61K31/501 , A61K31/5025 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14 , C07D487/04
摘要： The invention relates to compounds of formula (I) wherein X is O or NH; R 1 is phenyl, pyridinyl, or pyrimidinyl each optionally substituted with one, two or three halo, R 2 is C 1-4 alkyl, H or C 1-4 haloalkyl; R 3 , R 4 , and R 5 each are independently H, optionally substituted Ci-7alkyl, optionally substituted Cι.7alkoxy, CN, halo, NO2, -C(O)-R a -NR b R c , optionally substituted 3- to 7-membered heterocyclyl, optionally substituted 5- or 6-membered heteroaryl, -C(0)-NR d R e , or R 3 together with the neighboring pyridazine-nitrogen form a 5-membered optionally substituted annelated aromatic ring with two additional ring nitrogen atoms, or to a pharmaceutically acceptable salt thereof, having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as cognitive enhancers or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及其中X为O或NH的式（I）化合物; R 1是苯基，吡啶基或嘧啶基，每个任选被一个，两个或三个卤素取代，R 2是C 1-4烷基，H或C 1-4卤代烷基; R 3，R 4和R 5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，-C（O）-R a -NR b R c，任选取代的3-至7-元杂环基，任选取代的5-或6-元杂芳基，-C（O）-NR d R e或R 3与相邻的哒嗪 - 氮形成具有两个另外的环氮原子的5元任选取代的环状芳环，或与药学上可接受的盐具有对GABA A a5受体结合位点的亲和性和选择性，它们的制备，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用作认知增强剂或治疗认知障碍如阿尔茨海默氏病。

4. 发明申请

WO2009000662A1 ISOXAZOLE-IMIDAZOLE DERIVATIVES 审中-公开
标题翻译：异佛唑酮咪唑衍生物
公开(公告)号：WO2009000662A1
公开(公告)日：2008-12-31
申请号：PCT/EP2008/057384
申请日：2008-06-12
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , JAKOB-ROETNE, Roland , KNUST, Henner , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , JAKOB-ROETNE, Roland , KNUST, Henner , THOMAS, Andrew
IPC分类号： C07D413/04 , C07D413/14 , A61K31/42 , A61K31/44 , A61K31/497 , A61P25/00 , A61P25/28
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is concerned isoxazole-imidazole derivatives having affinity and selectivity for GABA A α5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease. In particular, the present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula (I): wherein R 1 , R 2 and R 3 are as described in the specification.
摘要翻译：本发明涉及对GABA A a5受体结合位点具有亲和性和选择性的异恶唑 - 咪唑衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物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。特别地，本发明涉及式（I）的芳基 - 异恶唑-4-基 - 咪唑衍生物：其中R1，R2和R3如说明书中所述。

5. 发明申请

WO2009071464A1 ISOXAZOLO-PYRAZINE DERIVATIVES 审中-公开
标题翻译： ISOXAZOLO-PYRAZINE DORIVATIVES
公开(公告)号：WO2009071464A1
公开(公告)日：2009-06-11
申请号：PCT/EP2008/066127
申请日：2008-11-25
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , JAKOB-ROETNE, Roland , KNUST, Henner , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , JAKOB-ROETNE, Roland , KNUST, Henner , THOMAS, Andrew
IPC分类号： C07D413/12 , C07D413/14 , A61K31/497 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with isoxazolo-pyrazine derivatives of formula (I) wherein X is O or NH; R 1 is phenyl or pyridine-2-yl, wherein the rings may be optionally substituted with one, two or three halo; R 2 is H or C 1-4 alkyl; R 3 and R 4 each are independently H, optionally substituted C 1-7 alkyl, optionally substituted C 1-7 alko.xy, CN, halo, NO 2 , -C(0)-R a -C(0)-NR b R c or R 3 and R 4 together form an optionally substituted annelated benzo ring, or a pharmaceutically acceptable salt thereof, having affinity and selectivity for GABA A α5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are 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）的异恶唑并吡嗪衍生物，其中X是O或NH; R 1是苯基或吡啶-2-基，其中环可以任选地被一个，两个或三个卤素取代; R2是H或C1-4烷基; R 3和R 4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烷基，CN，卤素，NO 2，-C（O）-R a -C（O）-NR b R c或R 3和R 4一起形成任选地其具有对GABA A a5受体结合位点的亲和性和选择性，其制备，含有它们的药物组合物及其作为药物的用途的取代的环状苯并环或其药学上可接受的盐。本发明的活性化合物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。

6. 发明申请

WO2010112475A1 HYDROXY-METHYL ISOXAZOLE DERIVATIVES AS GABA A MODULATORS 审中-公开
标题翻译：羟基 - 甲基异恶唑衍生物作为GABA A调节剂
公开(公告)号：WO2010112475A1
公开(公告)日：2010-10-07
申请号：PCT/EP2010/054141
申请日：2010-03-30
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , GABRIEL, Stephen, Deems , HANLON, Steven, Paul , JAKOB-ROETNE, Roland , LUCAS, Matthew, C. , SPURR, Paul , THOMAS, Andrew , WALDMEIER, Pius
发明人： BUETTELMANN, Bernd , GABRIEL, Stephen, Deems , HANLON, Steven, Paul , JAKOB-ROETNE, Roland , LUCAS, Matthew, C. , SPURR, Paul , THOMAS, Andrew , WALDMEIER, Pius
IPC分类号： C07D413/12 , C07D413/14 , A61K31/4439 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula (I) wherein R 1 , R 2 and R 3 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）的新型羟基 - 甲基异恶唑衍生物，其中R 1，R 2和R 3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的制备。

7. 发明申请

WO2010127974A1 ISOXAZOLE-THIAZOLE DERIVATIVES AS GABA A RECEPTOR INVERSE AGONISTS FOR USE IN THE TREATMENT OF COGNITIVE DISORDERS 审中-公开
标题翻译：异丙唑噻唑衍生物作为GABA受体逆转用于治疗认知障碍的反应
公开(公告)号：WO2010127974A1
公开(公告)日：2010-11-11
申请号：PCT/EP2010/055693
申请日：2010-04-28
申请人： F. HOFFMANN-LA ROCHE AG , JAKOB-ROETNE, Roland , LUCAS, Matthew, C. , THOMAS, Andrew
发明人： JAKOB-ROETNE, Roland , LUCAS, Matthew, C. , THOMAS, Andrew
IPC分类号： C07D417/06 , C07D417/12 , C07D417/14 , A61K31/425 , A61K31/4439 , A61P25/28
CPC分类号： C07D417/06 , C07D417/12 , C07D417/14
摘要： The present invention is concerned with isoxazole-thiazole derivatives of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及式I的异恶唑 - 噻唑衍生物，其具有对GABA A a5受体的亲和力和选择性，它们的制备，含有它们的药物组合物及其作为治疗活性物质的用途。本发明的活性化合物可用作认知增强剂或用于治疗和/或预防性治疗认知障碍如阿尔茨海默氏病。

8. 发明申请

WO2010127975A1 ISOXAZOLE-PYRAZOLE DERIVATIVES 审中-公开
标题翻译：异噻唑衍生物
公开(公告)号：WO2010127975A1
公开(公告)日：2010-11-11
申请号：PCT/EP2010/055694
申请日：2010-04-28
申请人： F. HOFFMANN-LA ROCHE AG , JAKOB-ROETNE, Roland , LUCAS, Matthew, C. , THOMAS, Andrew
发明人： JAKOB-ROETNE, Roland , LUCAS, Matthew, C. , THOMAS, Andrew
IPC分类号： C07D413/12 , C07D413/14 , A61K31/4155 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with isoxazole-pyrazole derivatives of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及式I的异恶唑 - 吡唑衍生物，其具有对GABA A a5受体的亲和性和选择性，它们的制备，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用作认知增强剂或用于治疗和/或预防性治疗认知障碍如阿尔茨海默氏病。

9. 发明申请

WO2010125042A1 ISOXAZOLE DERIVATIVES 审中-公开
标题翻译：异佛唑衍生物
公开(公告)号：WO2010125042A1
公开(公告)日：2010-11-04
申请号：PCT/EP2010/055591
申请日：2010-04-27
申请人： F. HOFFMANN-LA ROCHE AG , JAKOB-ROETNE, Roland , LUCAS, Matthew, C. , THOMAS, Andrew
发明人： JAKOB-ROETNE, Roland , LUCAS, Matthew, C. , THOMAS, Andrew
IPC分类号： C07D413/12 , C07D413/14 , A61K31/4427 , A61P25/14 , A61P25/16 , A61P25/18 , 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 , R 4 and R 5 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，R 4和R 5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。

10. 发明申请

WO2010094669A1 ISOXAZOLE-ISOXAZOLE AND ISOXAZOLE-ISOTHIAZOLE DERIVATIVES 审中-公开
标题翻译：异佛唑异恶唑和异辛唑 - 异噻唑衍生物
公开(公告)号：WO2010094669A1
公开(公告)日：2010-08-26
申请号：PCT/EP2010/051890
申请日：2010-02-16
申请人： F. HOFFMANN-LA ROCHE AG , HERNANDEZ, Maria-Clemencia , JAKOB-ROETNE, Roland , LUCAS, Matthew C. , THOMAS, Andrew
发明人： HERNANDEZ, Maria-Clemencia , JAKOB-ROETNE, Roland , LUCAS, Matthew C. , THOMAS, Andrew
IPC分类号： C07D261/18 , C07D413/14 , C07D417/12 , C07D487/10 , A61K31/422 , A61K31/427 , A61K31/4439 , A61P25/28
CPC分类号： C07D261/18 , C07D413/14 , C07D417/12 , C07D487/10
摘要： The present invention is concerned with isoxazole-isoxazole and isoxazole-isothiazole derivatives of Formula (I), having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及对于GABA A a5受体具有亲和性和选择性的式（I）的异恶唑 - 异恶唑和异恶唑 - 异噻唑衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用作认知增强剂或用于治疗和/或预防性治疗认知障碍如阿尔茨海默氏病。

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