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1. 发明授权

US07875645B2 Method for the treatment of CNS disorders with substituted 2-imidazoles or imidazole derivatives 失效
标题翻译：用取代的2-咪唑或咪唑衍生物治疗CNS障碍的方法
公开(公告)号：US07875645B2
公开(公告)日：2011-01-25
申请号：US11655468
申请日：2007-01-19
申请人： Guido Galley , Katrin Groebke Zbinden , Marius Hoener , Sabine Kolczewski , Roger Norcross , Henri Stalder
发明人： Guido Galley , Katrin Groebke Zbinden , Marius Hoener , Sabine Kolczewski , Roger Norcross , Henri Stalder
IPC分类号： A61K31/415 , C07D233/56
CPC分类号： C07D233/06 , A61K31/4164 , A61K31/4178 , C07D233/20 , C07D233/22 , C07D233/56 , C07D233/64 , C07D401/10 , C07D403/06 , C07D405/06 , C07D409/06
摘要： The present invention relates a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, R1, R2, A and n are as defined in the specification and to their pharmaceutically active salts. The invention also relates to novel compounds of formula I, pharmaceutical compositions containing them, and methods for their preparation.
摘要翻译：本发明涉及治疗抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，应激相关障碍，精神病如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢障碍如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管疾病，其包括给予个体治疗有效量的式I化合物，其中R，R 1，R 2，A和n如说明书中所定义，并且其药物活性盐。本发明还涉及式I的新型化合物，含有它们的药物组合物及其制备方法。

2. 发明申请

US20070197621A1 Method for the treatment of CNS disorders with substituted 2-imidazoles or imidazole derivatives 失效
标题翻译：用取代的2-咪唑或咪唑衍生物治疗CNS障碍的方法
公开(公告)号：US20070197621A1
公开(公告)日：2007-08-23
申请号：US11655468
申请日：2007-01-19
申请人： Guido Galley , Katrin Groebke Zbinden , Marius Hoener , Sabine Kolczewski , Roger Norcross , Henri Stalder
发明人： Guido Galley , Katrin Groebke Zbinden , Marius Hoener , Sabine Kolczewski , Roger Norcross , Henri Stalder
IPC分类号： A61K31/415 , C07D233/56
CPC分类号： C07D233/06 , A61K31/4164 , A61K31/4178 , C07D233/20 , C07D233/22 , C07D233/56 , C07D233/64 , C07D401/10 , C07D403/06 , C07D405/06 , C07D409/06
摘要： The present invention relates a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, R1, R2, A and n are as defined in the specification and to their pharmaceutically active salts. The invention also relates to novel compounds of formula I, pharmaceutical compositions containing them, and methods for their preparation.
摘要翻译：本发明涉及治疗抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，应激相关障碍，精神病如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢障碍如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管疾病，其包括给予个体治疗有效量的式I化合物，其中R，R 1，R 2，A和n如说明书中所定义，并且其药物活性盐。本发明还涉及式I的新型化合物，含有它们的药物组合物及其制备方法。

3. 发明申请

US20070197569A1 Method for treating central nervous system disorders with substituted 2-imidazoline derivatives 审中-公开
标题翻译：用取代的2-咪唑啉衍生物治疗中枢神经系统障碍的方法
公开(公告)号：US20070197569A1
公开(公告)日：2007-08-23
申请号：US11655484
申请日：2007-01-19
申请人： Marius Hoener , Sabine Kolczewski , Henri Stalder
发明人： Marius Hoener , Sabine Kolczewski , Henri Stalder
IPC分类号： A61K31/415 , A61K31/505 , C07D233/44 , C07D239/02
CPC分类号： A61K31/4164 , A61K31/4168 , A61K31/4174
摘要： The present invention relates to a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, X, A, and n are as defined in the specification and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms thereof.
摘要翻译：本发明涉及一种治疗抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍（ADHD），应激相关疾病，精神病如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢障碍如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管疾病其包括向个体施用治疗有效量的式I化合物，其中R，X，A和n如说明书中所定义，以及药学活性盐，外消旋混合物，对映异构体，旋光异构体及其互变异构形式。

4. 发明授权

US06599900B2 1-oxa-3,9-diaza-spiro[5,5]undecan-2-ones 失效
标题翻译： 1-氧杂-3,9-二氮杂 - 螺[5,5]十一烷-2-酮
公开(公告)号：US06599900B2
公开(公告)日：2003-07-29
申请号：US10143431
申请日：2002-05-10
申请人： Hai-Ying Cai , Michael Patrick Dillon , Guido Galley , Annick Goergler , Sabine Kolczewski , Dawn Muszynski Barsy
发明人： Hai-Ying Cai , Michael Patrick Dillon , Guido Galley , Annick Goergler , Sabine Kolczewski , Dawn Muszynski Barsy
IPC分类号： C07D49810
CPC分类号： C07D498/10 , A61K31/537
摘要： The invention relates to compounds of the general formula wherein (R1)n is independently from from each other halogen, lower alkyl or lower alkoxy; R2 is hydrogen, lower alkyl, lower halogen-alkyl, —(CH2)m—OH, —(CH2)m—NR2, —(CH2)mO-lower alkyl, —(CH2)m—C(O)—NR2, or is —(CH2)m-6-membered heteroaryl, optionally substituted by one or more lower alkoxy, —(CH2)m-5 or 6-membered not aromatic heterocyclyl, optionally substituted by hydroxy or lower alkyl; R is hydrogen or lower alkyl and may be the same or different in case of R2; n is 0, 1, or 2; m is 0, 1, 2, 3 or 4; and pharmaceutically acceptable acid addition salts thereof. These compounds have a good affinity to the NK-1 receptor and they are therefore suitable for the treatment of diseases, related to this receptor.
摘要翻译：本发明涉及通式化合物（R1）的化合物，n彼此独立地为卤素，低级烷基或低级烷氧基; R2为氢，低级烷基，低级卤代烷基， - （CH2）m-OH， - （CH2 ）m-NR 2， - （CH 2）m O - 低级烷基， - （CH 2）m C（O）-NR 2或 - （CH 2）m-6-元杂芳基，任选被一个或多个低级烷氧基取代， - ）m-5或6元不是芳族杂环基，任选被羟基或低级烷基取代; R是氢或低级烷基，在R2的情况下可以相同或不同; n是0,1或2; m是0 ，1,2,3或4;及其药学上可接受的酸加成盐。这些化合物对NK-1受体具有良好的亲和性，因此它们适用于治疗与该受体有关的疾病。

5. 发明授权

US06482829B2 Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor 失效
标题翻译：作为神经激肽1受体的拮抗剂活性的取代的杂环螺癸烷化合物
公开(公告)号：US06482829B2
公开(公告)日：2002-11-19
申请号：US09861795
申请日：2001-05-21
申请人： Guido Galley , Thierry Godel , Annick Goergler , Torsten Hoffmann , Sabine Kolczewski , Stephan Roever
发明人： Guido Galley , Thierry Godel , Annick Goergler , Torsten Hoffmann , Sabine Kolczewski , Stephan Roever
IPC分类号： A61K311454
CPC分类号： C07D471/10 , A61K9/0031 , A61K9/02 , A61K9/2018 , A61K9/4858
摘要： The invention relates to compounds of the formula as described herein and pharmaceutically acceptable acid addition salts thereof. The described compounds have a good affinity to the NK1 receptor.
摘要翻译：本发明涉及本文所述的式的化合物及其药学上可接受的酸加成盐。所述化合物对NK1受体具有良好的亲和力。

6. 发明申请

US20120232033A1 AMINES OR AMINO ALCOHOLS AS GLYT1 INHIBITORS 失效
标题翻译：氨基或氨基醇作为GLYT1抑制剂
公开(公告)号：US20120232033A1
公开(公告)日：2012-09-13
申请号：US13480520
申请日：2012-05-25
申请人： Sabine Kolczewski , Hans-Peter Marty , Robert Narquizian , Emmanuel Pinnard , Henri Stalder
发明人： Sabine Kolczewski , Hans-Peter Marty , Robert Narquizian , Emmanuel Pinnard , Henri Stalder
IPC分类号： C07C217/70 , A61K31/137 , C07D213/61 , A61K31/4418 , C07D309/10 , A61K31/351 , C07D213/38 , C07D401/04 , A61K31/444 , C07D405/12 , A61K31/443 , C07D307/20 , A61K31/341 , A61K31/4433 , A61K31/44 , C07D305/06 , A61K31/337 , C07F7/10 , A61K31/695 , C07D239/26 , A61K31/505 , C07D413/04 , A61K31/5377 , A61P25/18 , A61P25/28 , A61P25/00 , C07C317/32
CPC分类号： A61K31/16 , C07C215/30 , C07C215/68 , C07C217/70 , C07C233/43 , C07C237/30 , C07C317/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D211/46 , C07D213/38 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/71 , C07D213/73 , C07D239/26 , C07D277/28 , C07D305/06 , C07D307/12 , C07D307/20 , C07D309/06 , C07D309/12 , C07D333/20 , C07D335/02 , C07D405/12
摘要： The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式I化合物的用途，其中取代基在描述和权利要求中描述用于治疗精神病，记忆障碍和学习功能障碍，精神分裂症，痴呆，注意力缺陷障碍或阿尔茨海默病。本发明还涉及一些式I化合物和含有它们的药物组合物。

7. 发明授权

US08367838B2 Amines or amino alcohols as GLYT1 inhibitors 失效
标题翻译：胺或氨基醇作为GLYT1抑制剂
公开(公告)号：US08367838B2
公开(公告)日：2013-02-05
申请号：US13480520
申请日：2012-05-25
申请人： Sabine Kolczewski , Hans-Peter Marty , Robert Narquizian , Emmanuel Pinard , Henri Stalder
发明人： Sabine Kolczewski , Hans-Peter Marty , Robert Narquizian , Emmanuel Pinard , Henri Stalder
IPC分类号： C07D213/00 , C07D213/63 , C07D405/00 , A61K31/44
CPC分类号： A61K31/16 , C07C215/30 , C07C215/68 , C07C217/70 , C07C233/43 , C07C237/30 , C07C317/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D211/46 , C07D213/38 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/71 , C07D213/73 , C07D239/26 , C07D277/28 , C07D305/06 , C07D307/12 , C07D307/20 , C07D309/06 , C07D309/12 , C07D333/20 , C07D335/02 , C07D405/12
摘要： The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式I化合物的用途，其中取代基在描述和权利要求中描述用于治疗精神病，记忆障碍和学习功能障碍，精神分裂症，痴呆，注意力缺陷障碍或阿尔茨海默病。本发明还涉及一些式I化合物和含有它们的药物组合物。

8. 发明申请

US20100210592A1 AMINES OR AMINO ALCOHOLS AS GLYT1 INHIBITORS 审中-公开
标题翻译：氨基或氨基醇作为GLYT1抑制剂
公开(公告)号：US20100210592A1
公开(公告)日：2010-08-19
申请号：US12703802
申请日：2010-02-11
申请人： Sabine Kolczewski , Hans-Peter Marty , Robert Narquizian , Emmanuel Pinard , Henri Stalder
发明人： Sabine Kolczewski , Hans-Peter Marty , Robert Narquizian , Emmanuel Pinard , Henri Stalder
IPC分类号： A61K31/44 , C07D211/70 , C07D401/04 , C07D211/22 , C07D239/26 , C07D413/04 , A61K31/444 , A61K31/445 , A61K31/505 , A61K31/5377 , A61P25/18 , A61P25/28 , A61K31/695
CPC分类号： A61K31/16 , C07C215/30 , C07C215/68 , C07C217/70 , C07C233/43 , C07C237/30 , C07C317/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D211/46 , C07D213/38 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/71 , C07D213/73 , C07D239/26 , C07D277/28 , C07D305/06 , C07D307/12 , C07D307/20 , C07D309/06 , C07D309/12 , C07D333/20 , C07D335/02 , C07D405/12
摘要： The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式I化合物的用途，其中取代基在描述和权利要求中描述用于治疗精神病，记忆障碍和学习功能障碍，精神分裂症，痴呆，注意力缺陷障碍或阿尔茨海默病。本发明还涉及一些式I化合物和含有它们的药物组合物。

9. 发明申请

US20100197715A1 PIPERIDINE DERIVATIVES 审中-公开
标题翻译：哌啶衍生物
公开(公告)号：US20100197715A1
公开(公告)日：2010-08-05
申请号：US12690128
申请日：2010-01-20
申请人： Sabine Kolczewski , Emmanuel Pinard , Henri Stalder
发明人： Sabine Kolczewski , Emmanuel Pinard , Henri Stalder
IPC分类号： A61K31/445 , A61K31/438 , A61K31/4545 , A61K31/4525 , A61K31/451 , C07D221/20 , C07D405/04 , C07D401/04 , C07D417/10 , C07D211/56 , A61P25/18 , A61P25/28 , A61P25/00
CPC分类号： C07D407/04 , A61K31/451 , C07D211/56 , C07D213/56 , C07D221/20 , C07D401/04 , C07D401/12 , C07D405/04 , C07D417/10
摘要： The present invention relates to a compound of formula I wherein R1, R2, and Ar are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. These compounds and their pharmaceutical compositions are useful in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及其中R 1，R 2和Ar如本文所定义或其药学上可接受的酸加成盐的式I化合物与外消旋混合物或其相应的对映异构体和/或其光学异构体。这些化合物及其药物组合物可用于治疗神经和神经精神障碍。

10. 发明授权

US08399674B2 Quinolines 失效
标题翻译：喹啉
公开(公告)号：US08399674B2
公开(公告)日：2013-03-19
申请号：US13359933
申请日：2012-01-27
申请人： Sabine Kolczewski , Claus Riemer , Lucinda Steward , Juergen Wichmann , Thomas Woltering
发明人： Sabine Kolczewski , Claus Riemer , Lucinda Steward , Juergen Wichmann , Thomas Woltering
IPC分类号： C07D215/38
CPC分类号： C11D11/0017 , C07D215/38 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/12 , C11D3/001 , C11D3/50 , C11D3/502 , C11D17/0086
摘要： The present invention relates to 2-aminoquinolines of formula I wherein R1, R2 and R3 are as defined in the specification, as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of CNS disorders.
摘要翻译：本发明涉及式I的2-氨基喹啉，其中R 1，R 2和R 3如本说明书中所定义，为5-HT5A受体拮抗剂，其制备方法，含有它们的药物组合物及其用于治疗CNS障碍的用途。

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