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1. 发明授权

US5017608A Hydrocinnamic acid derivatives 失效
标题翻译：氢化肉桂酸衍生物
公开(公告)号：US5017608A
公开(公告)日：1991-05-21
申请号：US403532
申请日：1989-09-06
申请人： Werner Aschwanden , Rene Imhof , Roland Jakob-Roetne , Emilio Kyburz
发明人： Werner Aschwanden , Rene Imhof , Roland Jakob-Roetne , Emilio Kyburz
IPC分类号： C07D221/10 , A61K31/165 , A61K31/325 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/47 , A61K31/473 , A61P25/28 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/47 , C07C235/52 , C07C237/12 , C07C237/20 , C07C237/22 , C07C237/36 , C07C239/00 , C07C275/24 , C07D213/30 , C07D213/75 , C07D213/81 , C07D225/06 , C07D295/13 , C07D295/185
CPC分类号： C07D213/75 , C07D213/81 , C07D295/13 , C07D295/185
摘要： Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxycarbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxycarbonyl-(C.sub.2 -C.sub.5)-alkyl, piperidino-(C.sub.2 -C.sub.4)-alkyl or halopyridinecarboxamido-(C.sub.2 -C.sub.4)-alkyl or R.sup.13 and R.sup.14 taken together with the nitrogen atom are 4-(C.sub.1 -C.sub.4)-alkyl-piperazin-1-yl,as well as pharmaceutically accpetable salts or basic compounds of formula I with acids or of acidic compounds of formula I with bases are described. The compounds of formula I and their pharmaceutically acceptable salts are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions.

2. 发明授权

US4883815A Hydrocinnamic acid derivatives 失效
标题翻译：氢化肉桂酸衍生物
公开(公告)号：US4883815A
公开(公告)日：1989-11-28
申请号：US215003
申请日：1988-07-05
申请人： Werner Aschwenden , Rene Imhof , Roland Jakob-Roetne , Emilio Kyburz
发明人： Werner Aschwenden , Rene Imhof , Roland Jakob-Roetne , Emilio Kyburz
IPC分类号： C07D221/10 , A61K31/165 , A61K31/325 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/47 , A61K31/473 , A61P25/28 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/47 , C07C235/52 , C07C237/12 , C07C237/20 , C07C237/22 , C07C237/36 , C07C239/00 , C07C275/24 , C07D213/30 , C07D213/75 , C07D213/81 , C07D225/06 , C07D295/13 , C07D295/185
CPC分类号： C07D213/75 , C07D213/81 , C07D295/13 , C07D295/185
摘要： Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy carbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxy carbonyl-C.sub.2 -C.sub.5)-alky, piperidino-C.sub.2 -C.sub.4)-alkyl or halopyridinecarboxamido-(C.sub.2 -C.sub.4)-alkyl or R.sup.13 and R.sup.14 taken together with the nitrogen atom are 4-(C.sub.1 -C.sub.4)-alkyl-piperazin-1-yl,as well as pharmaceutically acceptable salts of basic compounds of formula I with acids or of acidic compounds of formula I with bases are described. The compounds of formula I and their pharmaceutically acceptable salts are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions.
摘要翻译：其中一个或两个符号R 1至R 4为卤素或甲氧基，而其余为氢的式I的氢化肉桂酸衍生物; R5是氢或苯基; R 6是下式的残基：R 7是（C 1 -C 4） - 烷基，（C 2 -C 5） - 烷酰基氨基 - （C 2 -C 5） - 烷基，氨基或（C 1 -C 4） - 烷氧基苯基; R 8和R 9各自独立地为氢或（C 1 -C 4） - 烷基; R 10是氢，R 11是羟基或R 10和R 11一起是氧代; R 12是氢，（C 1 -C 10） - 烷基，吡啶基甲基或氨基甲酰基甲基; R 1是氢，（C 1 -C 4） - 烷基，R 14是氢，（C 1 -C 4） - 烷基，吡啶基，苯基 - （C 1 -C 4） - 烷基，羧基 - （C 1 -C 4） - 烷基，氨基甲酰基 - -C 1-4） - 烷基，（C 1 -C 4） - 烷氧基羰基 - （C 1 -C 4） - 烷基，二 - （C 1 -C 4） - 烷氧基羰基-C 2 -C 5） - 烷基，哌啶子基-C 2 -C 4） - 烷基或卤代吡啶甲酰氨基 - （C 2 -C 4） - 烷基或R 13和R 14与氮原子一起是4-（C 1 -C 4） - 烷基 - 哌嗪-1-基，以及式I的碱性化合物与酸的药学上可接受的盐或具有碱的酸式酸式化合物。式I化合物及其药学上可接受的盐适用于控制或预防脑功能不全或改善认知功能。

3. 发明授权

US5318967A 2,3,3a,4,5,9b-hexahydro-1H-benzo[e]indole derivatives 失效
标题翻译： 2,3,3a，4,5,9b-六氢-1H-苯并[e]吲哚衍生物
公开(公告)号：US5318967A
公开(公告)日：1994-06-07
申请号：US118831
申请日：1993-09-03
申请人： Hans Bruderer , Thierry Godel , Rene Imhof , Roland Jakob-Roetne
发明人： Hans Bruderer , Thierry Godel , Rene Imhof , Roland Jakob-Roetne
IPC分类号： A61K31/40 , A61K20060101 , A61K31/403 , A61K31/405 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/535 , A61P25/28 , C07D20060101 , C07D209/00 , C07D209/04 , C07D209/08 , C07D209/56 , C07D209/60 , C07D209/90 , C07D401/04 , C07D401/06 , C07D403/06 , C07D413/04 , C07D413/06
CPC分类号： C07D209/60
摘要： The invention relates to cis-2,3,3a,4,5,9b-Hexahydro-1H-benzo[b]indole derivatives of the formula ##STR1## wherein R.sup.1 is a residue of the formula --O--CO--NR.sup.4 R.sup.5, R.sup.2 is lower alkyl, lower cycloalkyl or lower alkyl substituted by lower cycloalkyl, aryl, aroyl, aroylamino, amino or by a cyclic amino, amide or imide group, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is lower alkyl and R.sup.5 is hydrogen or lower alkyl,the corresponding trans isomers or cis-trans isomeric mixtures and pharmaceutically acceptable salts thereof. These compounds and salts are especially suitable for the treatment or prophylaxis of cognitive disorders and senile dementia particularly, Alzheimer's disease, and for the improvement of memory capacity.
摘要翻译：本发明涉及式a--CO-NR4R5的顺式-2,3,3a，4,5,9b-六氢-1H-苯并[b]吲哚衍生物，R2是低级烷基，低级环烷基或低级烷基取代的芳基，芳酰基，芳酰基氨基，氨基或环状氨基，酰胺或酰亚胺基，R 3是氢或低级烷基，R 4是低级烷基，R 5是氢或低级烷基，相应的反式异构体或顺反异构体其混合物和药学上可接受的盐。这些化合物和盐特别适用于治疗或预防认知障碍和老年性痴呆，特别是阿尔茨海默氏病，以及改善记忆能力。

4. 发明授权

US5318966A Method of inhibiting aretylcholine esterase using 2,3,3a,4,5,9b-hexahydro-1H-benzo[e]indole derivatives 失效
标题翻译：使用2,3,3a，4,5,9b-六氢-1H-苯并[e]吲哚衍生物抑制鸟苷酸酯酶的方法
公开(公告)号：US5318966A
公开(公告)日：1994-06-07
申请号：US93412
申请日：1993-07-16
申请人： Hans Bruderer , Thierry Godel , Rene Imhof , Roland Jakob-Roetne
发明人： Hans Bruderer , Thierry Godel , Rene Imhof , Roland Jakob-Roetne
IPC分类号： A61K31/40 , A61K20060101 , A61K31/403 , A61K31/405 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/535 , A61P25/28 , C07D20060101 , C07D209/00 , C07D209/04 , C07D209/08 , C07D209/56 , C07D209/60 , C07D209/90 , C07D401/04 , C07D401/06 , C07D403/06 , C07D413/04 , C07D413/06
CPC分类号： C07D209/60
摘要： The invention relates to cis-2,3,3a,4,5,9b-Hexahydro-1H-benzo[b]indole derivatives of the formula ##STR1## wherein R.sup.1 is a residue of the formula --O--CO--NR.sup.4 R.sup.5, R.sup.2 is lower alkyl, lower cycloalkyl or lower alkyl substituted by lower cycloalkyl, aryl, aroyl, aroylamino, amino or by a cyclic amino, amide or imide group, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is lower alkyl and R.sup.5 is hydrogen or lower alkyl,the corresponding trans isomers or cis-trans isomeric mixtures and pharmaceutically acceptable salts thereof. These compounds and salts are especially suitable for the treatment or prophylaxis of cognitive disorders and senile dementia particularly, Alzheimer's disease, and for the improvement of memory capacity.
摘要翻译：本发明涉及式a--CO-NR4R5的顺式-2,3,3a，4,5,9b-六氢-1H-苯并[b]吲哚衍生物，R2是低级烷基，低级环烷基或低级烷基取代的芳基，芳酰基，芳酰基氨基，氨基或环状氨基，酰胺或酰亚胺基，R3是氢或低级烷基，R4是低级烷基，R5是氢或低级烷基，相应的反式异构体或顺反异构体其混合物和药学上可接受的盐。这些化合物和盐特别适用于治疗或预防认知障碍和老年性痴呆，特别是阿尔茨海默氏病，以及改善记忆能力。

5. 发明授权

US08415379B2 Pyridines 有权
标题翻译：吡啶类
公开(公告)号：US08415379B2
公开(公告)日：2013-04-09
申请号：US12768762
申请日：2010-04-28
申请人： Roland Jakob-Roetne , Matthew C. Lucas , Andrew Thomas
发明人： Roland Jakob-Roetne , Matthew C. Lucas , Andrew Thomas
IPC分类号： A61K31/443 , C07D413/14
CPC分类号： C07D413/12 , C07D413/14 , C07D417/14
摘要： The present invention is concerned with isoxazole-pyridines of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as pharmaceuticals. 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 - 吡啶，对GABA Aα5受体具有亲和性和选择性，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。

6. 发明授权

US08357703B2 Pyridines 有权
标题翻译：吡啶类
公开(公告)号：US08357703B2
公开(公告)日：2013-01-22
申请号：US12772250
申请日：2010-05-03
申请人： Bernd Buettelmann , Roland Jakob-Roetne , Henner Knust , Matthew C. Lucas , Andrew Thomas
发明人： Bernd Buettelmann , Roland Jakob-Roetne , Henner Knust , Matthew C. Lucas , Andrew Thomas
IPC分类号： A61K31/4427 , C07D413/12
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with novel isoxazoles of formula I wherein X, R1, R2, R3 and R4 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 therapeutics.
摘要翻译：本发明涉及式I的新异恶唑，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 Aα5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治疗剂的用途。

7. 发明授权

US08178522B2 Thiazoles 有权
标题翻译：噻唑
公开(公告)号：US08178522B2
公开(公告)日：2012-05-15
申请号：US12768779
申请日：2010-04-28
申请人： Roland Jakob-Roetne , Matthew C. Lucas , Andrew Thomas
发明人： Roland Jakob-Roetne , Matthew C. Lucas , Andrew Thomas
IPC分类号： A61K31/397 , A61K31/427 , A61K31/4439 , A61K31/541 , A61K31/5377 , C07D417/06 , C07D417/14
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 Aα5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. 发明授权

US07943619B2 Isoxazolo-pyridazine derivatives 有权
标题翻译：异恶唑并哒嗪衍生物
公开(公告)号：US07943619B2
公开(公告)日：2011-05-17
申请号：US12277331
申请日：2008-11-25
申请人： Bernd Buettelmann , Roland Jakob-Roetne , Henner Knust , Andrew Thomas
发明人： Bernd Buettelmann , Roland Jakob-Roetne , Henner Knust , Andrew Thomas
IPC分类号： C07D417/12 , A61K31/501 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14 , C07D487/04
摘要： The invention relates to isoxazolo-pyridazine compounds, in particular those of formula I as described above and to a pharmaceutically acceptable salts thereof, having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及异恶唑并哒嗪化合物，特别是上述式I化合物及其可药用盐，对GABA Aα5受体结合位点具有亲和力和选择性，其制备方法，含有它们的药物组合物及其作为认知增强剂或用于治疗认知障碍如阿尔茨海默病。

9. 发明申请

US20100286116A1 THIAZOLES 有权
公开(公告)号：US20100286116A1
公开(公告)日：2010-11-11
申请号：US12768779
申请日：2010-04-28
申请人： Roland Jakob-Roetne , Matthew C. Lucas , Andrew Thomas
发明人： Roland Jakob-Roetne , Matthew C. Lucas , Andrew Thomas
IPC分类号： A61K31/397 , C07D417/06 , A61K31/427 , C07D417/14 , A61K31/4439 , A61K31/541 , A61K31/5377 , A61P25/00
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 Aα5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。

10. 发明授权

US07618973B2 Isoxazolo-pyrazine derivatives 有权
标题翻译：异恶唑并吡嗪衍生物
公开(公告)号：US07618973B2
公开(公告)日：2009-11-17
申请号：US12277326
申请日：2008-11-25
申请人： Bernd Buettelmann , Roland Jakob-Roetne , Henner Knust , Andrew Thomas
发明人： Bernd Buettelmann , Roland Jakob-Roetne , Henner Knust , Andrew Thomas
IPC分类号： A61K31/4965
CPC分类号： C07D413/12 , C07D413/14
摘要： The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of present invention are inverse agonists of GABA A α5. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及对于GABA Aα5受体结合位点具有亲和性和选择性的异恶唑并吡嗪衍生物及其药学上可接受的盐，其制备方法以及含有它们的药物组合物。本发明的化合物是GABA Aα5的反向激动剂。本发明还涉及增强认知和治疗认知障碍如阿尔茨海默病的方法。

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