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1. 发明授权

US07700638B2 1,5,7-trisubstituted benzimidazole derivatives and their use for modulating the GABAA receptor complex 失效
标题翻译： 1,5,7-三取代苯并咪唑衍生物及其用于调节GABA A受体复合物的用途
公开(公告)号：US07700638B2
公开(公告)日：2010-04-20
申请号：US10575380
申请日：2004-10-20
申请人： Niall Morton Hamilton , Susan Elizabeth Napier , Morag Ann MacCall Easson , Andrew John Cooke , Lene Teuber , Naheed Mirza , Frank Wätjen
发明人： Niall Morton Hamilton , Susan Elizabeth Napier , Morag Ann MacCall Easson , Andrew John Cooke , Lene Teuber , Naheed Mirza , Frank Wätjen
IPC分类号： A61K31/4184 , C07D235/04
CPC分类号： A61K31/4184 , C07D235/06 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/06 , C07D403/12 , C07D405/04
摘要： This invention relates to novel 1,5,7-trisubstituted benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith.The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex.
摘要翻译：本发明涉及新的1,5,7-三取代苯并咪唑衍生物，含有这些化合物的药物组合物及其处理方法。本发明的化合物可用于治疗对调节GABA A受体复合物有反应的中枢神经系统疾病和病症。

2. 发明授权

US06710044B2 Technical field 失效
标题翻译：技术领域
公开(公告)号：US06710044B2
公开(公告)日：2004-03-23
申请号：US10299854
申请日：2002-11-20
申请人： Lene Teuber , Frank Wätjen
发明人： Lene Teuber , Frank Wätjen
IPC分类号： A61K315377
CPC分类号： C07D235/06 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D413/04
摘要： Chemical compounds of the formula as well as pharmaceutical compositions containing them and methods for their use in the treatment of disorders and diseases responsive to modulation of the GABAA receptor complex of the central nervous system, such disorders and diseases including anxiety, sleep disorders, anesthesia, memory disorders, and epilepsy and other convulsive disorders.
摘要翻译：式的化合物以及含有它们的药物组合物及其用于治疗对中枢神经系统的GABA A受体复合物调节有响应的病症和疾病的方法，包括焦虑，睡眠障碍，麻醉，记忆等疾病和疾病疾病，癫痫和其他惊厥性疾病。

3. 发明授权

US06503925B1 1-phenyl-benzimidazole compounds and their use as GABA-A receptor modulators 失效
标题翻译： 1-苯基 - 苯并咪唑化合物及其作为GABA-A受体调节剂的用途
公开(公告)号：US06503925B1
公开(公告)日：2003-01-07
申请号：US09768506
申请日：2001-01-25
申请人： Lene Teuber , Frank Wätjen
发明人： Lene Teuber , Frank Wätjen
IPC分类号： C07D23502
CPC分类号： C07D235/06 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D413/04
摘要： Chemical compounds of the formula as well as pharmaceutical compositions containing them and methods for their use in the treatment of disorders and diseases responsive to modulation of the GABAA receptor complex of the central nervous system, such disorders and diseases including anxiety, sleep disorders, anesthesia, memory disorders, and epilepsy and other convulsive disorders.
摘要翻译：式的化合物以及含有它们的药物组合物及其用于治疗对中枢神经系统的GABA A受体复合物调节有响应的病症和疾病的方法，包括焦虑，睡眠障碍，麻醉，记忆等疾病和疾病疾病，癫痫和其他惊厥性疾病。

4. 发明授权

US06288079B1 Tropane-derivatives, their preparation and use 失效
标题翻译：托烷衍生物，其制备和用途
公开(公告)号：US06288079B1
公开(公告)日：2001-09-11
申请号：US09101524
申请日：1998-07-10
申请人： Jørgen Scheel-Krüger , Peter Moldt , Frank Wätjen
发明人： Jørgen Scheel-Krüger , Peter Moldt , Frank Wätjen
IPC分类号： A61K3146
CPC分类号： C07D451/02 , C07D451/00
摘要： Compounds of formula (a), (b), (c), or (d), or any mixture thereof, or a pharmaceutically-acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; R3 is —CH2—X—R′, wherein X is O, S or NR″, wherein R″ is hydrogen or alkyl and R′ is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, or —CO-alkyl; R4 is phenyl optionally substituted with halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl, or aryl; 3,4-methylenedioxyphenyl; benzyl optionally substituted with halogen, CF3, CH, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino nitro, heteroaryl, or aryl; heteroaryl optionally substituted with halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl, or aryl; or naphthyl optionally substituted with halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl, or aryl. The compounds are monoamine neurotransmitter, i.e., dopamine, serotonin, noradrenaline, reuptake inhibitors.
摘要翻译：式（a），（b），（c）或（d）的化合物或其任何混合物或其药学上可接受的盐;其中R是氢，烷基，烯基，炔基，环烷基，环烷基烷基或2- 羟乙基 R3是-CH2-X-R'，其中X是O，S或NR“，其中R”是氢或烷基，R'是烷基，烯基，炔基，环烷基，环烷基烷基或-CO-烷基; R4是任选被卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基或芳基取代的苯基; 3,4-亚甲二氧基苯基; 任选被卤素，CF 3，CH，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基硝基，杂芳基或芳基取代的苄基; 任选被卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基或芳基取代的杂芳基; 或任选被卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基或芳基取代的萘基。化合物是单胺神经递质，即多巴胺，5-羟色胺，去甲肾上腺素，再摄取抑制剂。

5. 发明授权

US07632948B2 Method of preparing enantiomers of indole-2,3-dione-3-oxime derivatives 失效
标题翻译：制备吲哚-2,3-二酮-3-肟衍生物的对映异构体的方法
公开(公告)号：US07632948B2
公开(公告)日：2009-12-15
申请号：US10524441
申请日：2003-08-13
申请人： Alex H. Gouliaev , William Dalby Brown , Frank Wätjen
发明人： Alex H. Gouliaev , William Dalby Brown , Frank Wätjen
IPC分类号： C07D457/14
CPC分类号： C07D471/04 , C12P17/04 , C12P41/004
摘要： The present invention is directed to a method of preparing enantiomers of indole-2,3-dione-3-oxime derivatives.
摘要翻译：本发明涉及制备吲哚-2,3-二酮-3-肟衍生物的对映异构体的方法。

6. 发明授权

US07560562B2 Piperidine derivatives and their use as monoamine neurotransmitter re-uptake inhibitors 失效
标题翻译：哌啶衍生物及其作为单胺神经递质再摄取抑制剂的用途
公开(公告)号：US07560562B2
公开(公告)日：2009-07-14
申请号：US10530012
申请日：2003-10-30
申请人： Frank Wätjen
发明人： Frank Wätjen
IPC分类号： C07D211/20 , A61K31/445
CPC分类号： C07D211/22 , C07D211/60
摘要： This invention relates to novel piperidine derivatives useful as monoamine neurotransmitter re-uptake inhibitors.In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
摘要翻译：本发明涉及用作单胺神经递质再摄取抑制剂的新型哌啶衍生物。在其它方面，本发明涉及这些化合物在治疗方法中的用途以及包含本发明化合物的药物组合物。

7. 发明授权

US06727260B2 Inhibitors of proton-gated cation channels and their use in the treatment of ischaemic disorders 失效
标题翻译：质子门控阳离子通道的抑制剂及其在治疗缺血性疾病中的应用
公开(公告)号：US06727260B2
公开(公告)日：2004-04-27
申请号：US09985887
申请日：2001-11-06
申请人： Thomas Varming , Frank Wätjen
发明人： Thomas Varming , Frank Wätjen
IPC分类号： A61K314745
CPC分类号： A61K31/47 , A61K31/4745 , A61K31/498
摘要： This invention relates to the use of compounds capable of inhibiting the activity of a proton-gated cation channel in the treatment of alleviation of diseases or disorders associated with, or mediated by a drop in extra cellular pH.
摘要翻译：本发明涉及能够抑制质子门控阳离子通道活性的化合物在治疗与细胞内细胞pH降低有关或由其介导的疾病或病症的缓解中的用途。

8. 发明授权

US07700619B2 2-methoxymethyl-3-(3,4-dichlorophenyl)-8-azabicyclo[3.2.1]octane tartrate salts 有权
标题翻译： 2-甲氧基甲基-3-（3,4-二氯苯基）-8-氮杂双环[3.2.1]辛烷酒石酸盐
公开(公告)号：US07700619B2
公开(公告)日：2010-04-20
申请号：US10566384
申请日：2004-07-29
申请人： Brian Frøstrup , Frank Wätjen , Klaus Snej Jensen
发明人： Brian Frøstrup , Frank Wätjen , Klaus Snej Jensen
IPC分类号： A01N43/42
CPC分类号： C07D451/02
摘要： This invention relates to novel (1R,2R,3S,5S)-2-methoxymethyl-3-(3,4-dichlorophenyl)-8-azabicyclo[3.2.1]octane tartrate salts, such as L-tartrate monohydrates and anhydrates, wherein the salts are useful as monoamine neurotransmitter re-uptake inhibitors. Additionally, the invention also relates to the use of these salts in a method for therapy and to pharmaceutical compositions comprising the salts of the invention.
摘要翻译：本发明涉及新型的（1R，2R，3S，5S）-2-甲氧基甲基-3-（3,4-二氯苯基）-8-氮杂双环[3.2.1]辛酸酒石酸盐，如L-酒石酸盐一水合物和水合物，其中所述盐可用作单胺神经递质再摄取抑制剂。此外，本发明还涉及这些盐在治疗方法中的用途以及包含本发明的盐的药物组合物。

9. 发明授权

US07288653B2 Inhibitors of proton-gated cation channels and their use in the treatment of ischaemic disorders 失效
标题翻译：质子门控阳离子通道的抑制剂及其在治疗缺血性疾病中的应用
公开(公告)号：US07288653B2
公开(公告)日：2007-10-30
申请号：US11241805
申请日：2005-09-30
申请人： Thomas Varming , Frank Wätjen
发明人： Thomas Varming , Frank Wätjen
IPC分类号： C07D471/02
CPC分类号： A61K31/47 , A61K31/4745 , A61K31/498
摘要： This invention relates to the use of compounds capable of inhibiting the activity of a proton-gated cation channel in the treatment of alleviation of diseases or disorders associated with, or mediated by a drop in extra cellular pH.
摘要翻译：本发明涉及能够抑制质子门控阳离子通道活性的化合物在治疗与细胞内细胞pH降低有关或由其介导的疾病或病症的缓解中的用途。

10. 发明授权

US06395748B2 Tropane-derivatives, their preparation and use 失效
标题翻译：托烷衍生物，其制备和用途
公开(公告)号：US06395748B2
公开(公告)日：2002-05-28
申请号：US09814413
申请日：2001-03-21
申请人： Jørgen Scheel-Krüger , Peter Moldt , Frank Wätjen
发明人： Jørgen Scheel-Krüger , Peter Moldt , Frank Wätjen
IPC分类号： A61K3146
CPC分类号： C07D451/02 , C07D451/00
摘要： Compounds of formula (a), (b), (c), or (d), or any mixture thereof, or a pharmaceutically-acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; R3 is —CH2—X—R′, wherein X is O, S or NR″, wherein R″ is hydrogen or alkyl and R′ is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, or —CO-alkyl; R4 is phenyl optionally substituted with halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl, or aryl; 3,4-methylenedioxyphenyl; benzyl optionally substituted with halogen, CF3, CH, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl, or aryl; heteroaryl optionally substituted with halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl, or aryl; or naphthyl optionally substituted with halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl, or aryl. The compounds are monoamine neurotransmitter, i.e., dopamine, serotonin, noradrenaline, reuptake inhibitors.
摘要翻译：式（a），（b），（c）或（d）的化合物或其任何混合物或其药学上可接受的盐;其中R是氢，烷基，烯基，炔基，环烷基，环烷基烷基或2- 羟乙基 R3是-CH2-X-R'，其中X是O，S或NR“，其中R”是氢或烷基，R'是烷基，烯基，炔基，环烷基，环烷基烷基或-CO-烷基; R4是任选被卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基或芳基取代的苯基; 3,4-亚甲二氧基苯基; 任选被卤素，CF 3，CH，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基或芳基取代的苄基; 任选被卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基或芳基取代的杂芳基; 或任选被卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基或芳基取代的萘基。化合物是单胺神经递质，即多巴胺，5-羟色胺，去甲肾上腺素，再摄取抑制剂。

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