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1. 发明授权

US09096548B2 Pyrazine amide compounds 有权
标题翻译：吡嗪酰胺化合物
公开(公告)号：US09096548B2
公开(公告)日：2015-08-04
申请号：US14453642
申请日：2014-08-07
申请人： Dieter Wiedenmayer , Armin Heckel , Dieter Hamprecht
发明人： Dieter Wiedenmayer , Armin Heckel , Dieter Hamprecht
IPC分类号： C07D401/12 , C07D403/08 , C07D403/12 , C07D241/26 , A61K31/19 , A61K31/4965 , A61K31/497 , A61K31/4985 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/662 , A61K45/06 , C07C53/18 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07F9/54 , C07D241/20
CPC分类号： C07D241/26 , A61K31/19 , A61K31/4965 , A61K31/497 , A61K31/4985 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/662 , A61K45/06 , C07C53/18 , C07D241/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07F9/5456
摘要： The present invention relates to compounds of formula 1 or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, R4, R5, R6 and X− have the meanings as indicated in the specification, to their use as a medicament, to their use in the treatment of a disease selected from among respiratory diseases or complaints and allergic diseases of the airways, to pharmaceutical composition comprising at least one of said compound or a pharmaceutically acceptable salt thereof, as well as to medicament combinations containing one or more of said compounds or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及式1化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 5，R 4，R 5，R 6和X具有如说明书中所示的含义，用作药物，用于治疗选自呼吸系统疾病或呼吸道疾病和气道变应性疾病的疾病，以及包含至少一种所述化合物或其药学上可接受的盐的药物组合物，以及含有一种或多种所述化合物或其药学上可接受的盐。

2. 发明授权

US08841309B2 Substituted pyrazines and their use in the treatment of disease 有权
标题翻译：取代的吡嗪及其在治疗疾病中的应用
公开(公告)号：US08841309B2
公开(公告)日：2014-09-23
申请号：US14033552
申请日：2013-09-23
申请人： Dieter Hamprecht , Armin Heckel , Joerg Kley
发明人： Dieter Hamprecht , Armin Heckel , Joerg Kley
IPC分类号： A61K31/4965 , C07D241/16 , C07D401/12 , A61K31/498 , C07D241/32 , C07D453/02 , A61K31/5377 , A61K45/06 , A61K31/497 , C07D471/08 , C07D403/12
CPC分类号： C07D401/12 , A61K9/0075 , A61K31/497 , A61K31/498 , A61K31/5377 , A61K45/06 , C07D241/32 , C07D403/12 , C07D453/02 , C07D471/08 , A61K2300/00
摘要： The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
摘要翻译：本发明涉及通式（I）的化合物及其互变异构体及其盐，特别是其药学上可接受的盐，其具有有价值的药理学性质，特别是对上皮钠通道的抑制作用，其用于治疗疾病，特别是肺和气道疾病。

3. 发明申请

US20130109697A1 HETEROCYCLIC COMPOUNDS, MEDICAMENTS CONTAINING SAID COMPOUNDS, USE THEREOF AND PROCESSES FOR THE PREPARATION THEREOF 有权
标题翻译：杂环化合物，含有化合物的药物及其制备方法及其制备方法
公开(公告)号：US20130109697A1
公开(公告)日：2013-05-02
申请号：US13662791
申请日：2012-10-29
申请人： Armin HECKEL , Sara Frattini , Dieter Hamprecht , Joerg Kley
发明人： Armin HECKEL , Sara Frattini , Dieter Hamprecht , Joerg Kley
IPC分类号： A61K31/497 , C07D401/14 , A61P11/06 , A61P11/00 , A61P11/14 , A61P5/00 , C07D401/12 , A61P37/08
CPC分类号： C07D401/14 , C07D401/12
摘要： The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
摘要翻译：本发明涉及通式（I）化合物及其互变异构体及其盐，特别是其与无机或有机酸和碱的药物上可接受的盐，其具有有价值的药理学性质，特别是对上皮钠通道的抑制作用，以及其用于治疗疾病，特别是肺和气道疾病。

4. 发明授权

US09078909B2 Tertiary amines, medicaments containing said amines, use thereof and processes for the preparation thereof 有权
标题翻译：叔胺，含有胺的药物，其用途及其制备方法
公开(公告)号：US09078909B2
公开(公告)日：2015-07-14
申请号：US13899762
申请日：2013-05-22
申请人： Dieter Hamprecht , Armin Heckel , Joerg Kley
发明人： Dieter Hamprecht , Armin Heckel , Joerg Kley
IPC分类号： A61K31/495 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/08 , C07D453/02 , A61K31/675 , C07F9/6509 , C07F9/6558
CPC分类号： A61K31/675 , A61K31/495 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D453/02 , C07D471/08 , C07F9/650952 , C07F9/65583
摘要： The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
摘要翻译：本发明涉及通式（I）的化合物及其互变异构体及其盐，特别是其与无机或有机酸和碱的药学上可接受的盐，其具有有价值的药理学性质，特别是对上皮钠通道的抑制作用，其用于治疗疾病，特别是肺和气道疾病。

5. 发明授权

US08759349B2 Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof 有权
标题翻译：杂环化合物，含有所述化合物的药物，其用途及其制备方法
公开(公告)号：US08759349B2
公开(公告)日：2014-06-24
申请号：US13662791
申请日：2012-10-29
申请人： Armin Heckel , Sara Frattini , Dieter Hamprecht , Joerg Kley
发明人： Armin Heckel , Sara Frattini , Dieter Hamprecht , Joerg Kley
IPC分类号： A61K31/497
CPC分类号： C07D401/14 , C07D401/12
摘要： The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
摘要翻译：本发明涉及通式（I）化合物及其互变异构体及其盐，特别是其与无机或有机酸和碱的药物上可接受的盐，其具有有价值的药理学性质，特别是对上皮钠通道的抑制作用，以及其用于治疗疾病，特别是肺和气道疾病。

6. 发明授权

US09073954B2 5-substituted benzimidazolium compounds 有权
标题翻译： 5-取代的苯并咪唑鎓化合物
公开(公告)号：US09073954B2
公开(公告)日：2015-07-07
申请号：US14330017
申请日：2014-07-14
申请人： Joerg Kley , Sara Frattini , Dieter Hamprecht , Armin Heckel
发明人： Joerg Kley , Sara Frattini , Dieter Hamprecht , Armin Heckel
IPC分类号： C07D403/12 , C07D403/14 , C07D493/04 , C07F9/6509 , A61K31/675 , A61K45/06 , A61K31/497 , A61K31/683 , A61K31/5377
CPC分类号： C07F9/650952 , A61K31/497 , A61K31/5377 , A61K31/675 , A61K31/683 , A61K45/06 , C07D403/12 , C07D403/14 , C07D493/04
摘要： The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
摘要翻译：本发明涉及通式（I）的化合物及其互变异构体及其盐，特别是其与无机或有机酸和碱的药学上可接受的盐，其具有有价值的药理学性质，特别是对上皮钠通道的抑制作用，其用于治疗疾病，特别是肺和气道疾病。

7. 发明授权

US08642585B2 Indanyloxydihydrobenzofuranylacetic acids 有权
标题翻译：茚基二氢苯并呋喃基乙酸
公开(公告)号：US08642585B2
公开(公告)日：2014-02-04
申请号：US13803237
申请日：2013-03-14
申请人： Matthias Eckhardt , Sara Frattini , Dieter Hamprecht , Frank Himmelsbach , Elke Langkopf , Iain Lingard , Stefan Peters , Holger Wagner
发明人： Matthias Eckhardt , Sara Frattini , Dieter Hamprecht , Frank Himmelsbach , Elke Langkopf , Iain Lingard , Stefan Peters , Holger Wagner
IPC分类号： A61K31/553 , C07D267/10 , A61K31/443 , C07D405/02 , A61K31/4155 , C07D231/10 , A61K31/422 , C07D263/30 , A61K31/4178 , C07D233/54 , A61K31/4245 , C07D271/06 , A61K31/427 , C07D277/20 , A61K31/501 , C07D403/02 , A61K31/5377 , C07D413/14 , A61K31/497 , C07D307/77 , A61K31/343 , C07D257/02 , A61K31/506 , A61K31/41 , C07D249/08 , A61K31/4196 , A61K31/4025 , C07D409/02 , A61K31/382 , C07D413/02
CPC分类号： C07D405/12 , A61K31/343 , A61K31/351 , A61K31/382 , A61K31/397 , A61K31/4025 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/443 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/553 , A61K45/06 , C07D307/80 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
摘要翻译：本发明涉及通式I的化合物，其中R1，R2和m基团如权利要求1中所定义，其具有有价值的药理学性质，特别是与GPR40受体结合并调节其活性。该化合物适用于治疗和预防可受该受体影响的疾病，如代谢疾病，特别是2型糖尿病。

8. 发明申请

US20120289526A1 IMIDAZOLIDINEDIONE DERIVATIVES 有权
标题翻译：咪唑啉衍生物
公开(公告)号：US20120289526A1
公开(公告)日：2012-11-15
申请号：US13515097
申请日：2010-12-06
申请人： Giuseppe Alvaro , Anne Décor , Stefano Fontana , Dieter Hamprecht , Charles Large , Agostino Marasco
发明人： Giuseppe Alvaro , Anne Décor , Stefano Fontana , Dieter Hamprecht , Charles Large , Agostino Marasco
IPC分类号： A61K31/4439 , C07D401/04 , A61K31/4166 , C07D403/04 , A61K31/506 , A61P25/20 , A61P25/00 , A61P27/16 , A61P25/18 , A61P25/30 , A61P25/08 , C07D233/72 , A61P25/24
CPC分类号： A61K31/506 , A61K31/4166 , A61K31/4439 , C07D213/643 , C07D233/72 , C07D233/76 , C07D239/22 , C07D239/47 , C07D401/04 , C07D403/04
摘要： The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy.
摘要翻译：本发明提供式（Ia）化合物及其药学上可接受的盐。本发明还提供了化合物或盐作为Kv3.1和/或Kv3.2的调节剂的用途，以及用于治疗需要Kv3.1和/或Kv3.2调节剂的疾病或病症，例如抑郁症情绪障碍，听觉障碍，精神分裂症，物质滥用障碍，睡眠障碍或癫痫。

9. 发明授权

US07875643B2 Azabicyclo (3.1.0) hexane derivatives useful as modulators of dopamine D3 receptors 失效
标题翻译：可用作多巴胺D3受体调节剂的氮杂双环（3.1.0）己烷衍生物
公开(公告)号：US07875643B2
公开(公告)日：2011-01-25
申请号：US11911229
申请日：2006-04-13
申请人： Dieter Hamprecht , Caterina Mazzoni , Fabrizio Micheli
发明人： Dieter Hamprecht , Caterina Mazzoni , Fabrizio Micheli
IPC分类号： A61K31/41 , C07D249/08
CPC分类号： C07D403/12
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl and indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R5; each R2 is independently hydrogen or C1-4alkyl; n is 2, 3, 4 or 5; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl and SF5; R5 is selected from a group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl and 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from a group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; and when R1 corresponds to R5, p is 1; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐：其中G选自：苯基，吡啶基，苯并噻唑基和吲唑基; p为0〜5的整数。 R 1独立地选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5; 或对应于R5组; 每个R 2独立地是氢或C 1-4烷基; n为2，3，4或5; R3是C1-4烷基; R 4是氢或苯基，杂环基，5或6元杂芳族基团或8至11元双环基团，其中任何基团任选被1,2,3或4个取代基取代选自卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基和SF 5; R5选自：异恶唑基，-CH2-N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基和2-吡咯烷基，并且该基团任选被一个或两个取代基取代选自：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基和C 1-4烷酰基; 当R1对应于R5时，p为1; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D3受体的调节剂。治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症，早泄或认知障碍。

10. 发明授权

US07776904B2 Azabicyclo [3.1.0] hexylphenyl derivatives as modulators of dopamine D3 receptors 失效
标题翻译：氮杂双环[3.1.0]己基苯基衍生物作为多巴胺D3受体的调节剂
公开(公告)号：US07776904B2
公开(公告)日：2010-08-17
申请号：US12064121
申请日：2006-08-18
申请人： Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Adolfo Prandi , Silvia Terreni
发明人： Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Adolfo Prandi , Silvia Terreni
IPC分类号： A61K31/403 , C07D209/52
CPC分类号： C07D209/52
摘要： The present invention relates to novel compounds of formula (IA) or a salt thereof: wherein: A is attached to the phenyl group at the meta position or the para position relative to the cyclopropyl group, and is selected from the group consisting of: —SO2NR5—, —SO2CR2R3—, —CR2R3SO2— and —NR5SO2—; R1 is hydrogen, C1-6alkyl, haloC1-6alkyl or C2-6alkylene; R2 and R3 are independently hydrogen or C1-6alkyl; R4 is hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; R5 is hydrogen, C1-6alkyl, or a phenyl optionally substituted by R4; and R6 is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（IA）化合物或其盐：其中：A相对于环丙基在间位或对位与苯基连接，并且选自： - SO 2 NR 5 - ， - SO 2 CR 2 R 3 - ， - CR 2 R 3 SO 2 - 和-NR 5 SO 2 - ; R1是氢，C1-6烷基，卤代C 1-6烷基或C 2-6亚烷基; R2和R3独立地是氢或C1-6烷基; R 4是氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; R5是氢，C1-6烷基或任选被R4取代的苯基; 并且R 6是氢，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D3受体的调节剂。治疗物质相关疾病，作为抗精神病药物早泄或认知障碍。

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