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51. 发明申请

US20110144333A1 4,5-DIHYDRO-OXAZOL-2YL DERIVATIVES 有权
标题翻译： 4,5-二氢 - 氧杂环戊二烯衍生物
公开(公告)号：US20110144333A1
公开(公告)日：2011-06-16
申请号：US13033645
申请日：2011-02-24
申请人： Guido Galley , Annick Goergler , Katrin Groebke Zbinden , Roger Norcross
发明人： Guido Galley , Annick Goergler , Katrin Groebke Zbinden , Roger Norcross
IPC分类号： C07D413/12 , C07F7/02 , C07D263/28
CPC分类号： A61K31/421 , A61K31/47 , C07D263/48 , C07D401/12 , C07D413/12 , C07F7/081
摘要： The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, 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.
摘要翻译：本发明涉及式I化合物，其中R1，R2，X，Y和n在本说明书中定义及其药学上可接受的酸加成盐。本发明还提供药物组合物和这种化合物的制造方法。这些化合物可用于治疗与微量胺相关受体的生物功能有关的疾病，这些疾病是抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，应激相关疾病，精神病，精神分裂症，神经系统疾病，帕金森病，神经变性疾病，阿尔茨海默病，癫痫，偏头痛，药物滥用和代谢障碍，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，体温平衡失调和失调，睡眠障碍昼夜节律和心血管疾病。

52. 发明授权

US07858653B2 2-imidazoles 失效
标题翻译： 2-咪唑
公开(公告)号：US07858653B2
公开(公告)日：2010-12-28
申请号：US11950446
申请日：2007-12-05
申请人： Guido Galley , Katrin Groebke Zbinden , Roger Norcross , Henri Stalder
发明人： Guido Galley , Katrin Groebke Zbinden , Roger Norcross , Henri Stalder
IPC分类号： A01N43/50 , C07D233/00
CPC分类号： C07D233/88 , C07D233/64
摘要： The present invention relates to compounds of formula I, wherein X is —CH2— or —NH—; Y is —CH(lower alkoxy)-, —CH(lower alkyl)-, —O—, —S—, —S(O)—, —S(O)2— or —CH2—; and Ar is phenyl or naphthyl, which rings are optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkoxy, lower alkyl and lower alkyl substituted by halogen; or a pharmaceutically-acceptable acid-addition salt thereof; with the proviso that, when X is —NH—, Y is —CH(lower alkyl)- or —CH2—; and the further proviso that the compound is not 2-phenethyl-1H-imidazole hydrochloride, 2-(3,4-dichloro-phenoxymethyl)-1H-imidazole hydrochloride, 2-(2-chloro-phenoxymethyl)-1H-imidazole hydrochloride, 2-(2,3-dichloro-phenoxymethyl)-1H-imidazole, benzyl-(1H-imidazol-2-yl)-amine, (4-chloro-benzyl)-(1H-imidazol-2-yl)-amine, or (2-chloro-benzyl)-(1H-imidazol-2-yl)-amine. The invention relates also to a pharmaceutically-acceptable acid-addition salt of such a compound, processes for making the compound, and a composition comprising such a compound.
摘要翻译：本发明涉及式I化合物，其中X是-CH 2 - 或-NH-; Y是-CH（低级烷氧基） - ， - CH（低级烷基） - ， - O - ， - S - ， - S（O） - ， - S（O）并且Ar是苯基或萘基，该环任选地被一个或两个选自卤素，低级烷氧基，低级烷基和被卤素取代的低级烷基的取代基取代; 或其药学上可接受的酸加成盐; 条件是当X是-NH-时，Y是-CH（低级烷基） - 或-CH 2 - ; 另外的条件是该化合物不是2-苯乙基-1H-咪唑盐酸盐，2-（3,4-二氯 - 苯氧基甲基）-1H-咪唑盐酸盐，2-（2-氯 - 苯氧基甲基）-1H-咪唑盐酸盐， 2-（2,3-二氯 - 苯氧基甲基）-1H-咪唑，苄基 - （1H-咪唑-2-基） - 胺，（4-氯 - 苄基） - （1H-咪唑-2-基） - 胺，或（2-氯 - 苄基） - （1H-咪唑-2-基） - 胺。本发明还涉及这种化合物的药学上可接受的酸加成盐，制备该化合物的方法和包含这种化合物的组合物。

53. 发明授权

US07820699B2 Cyclic amines 有权
标题翻译：环胺
公开(公告)号：US07820699B2
公开(公告)日：2010-10-26
申请号：US11403973
申请日：2006-04-13
申请人： Katrin Groebke Zbinden , Wolfgang Haap , Hans Hilpert , Narendra Panday , Fabienne Ricklin , Beat Wirz
发明人： Katrin Groebke Zbinden , Wolfgang Haap , Hans Hilpert , Narendra Panday , Fabienne Ricklin , Beat Wirz
IPC分类号： A61K31/4436 , A61K31/4439 , C07D409/14 , C07D401/14
CPC分类号： C07D207/12 , C07D207/14 , C07D207/16 , C07D401/14 , C07D409/14 , C07D413/14 , C07D513/04
摘要： The invention is concerned with cyclic amines of formula (I) wherein X1 to X3, Y1 to Y3, R1′, R1″ and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit coagulation factor Xa and can be used as medicaments and for treating diseases associated with coagulation factor Xa.
摘要翻译：本发明涉及式（I）的环胺，其中X1至X3，Y1至Y3，R1'，R1“和n如说明书和权利要求书中所定义，以及其生理学上可接受的盐。这些化合物抑制凝血因子Xa，可用作药物和治疗与凝血因子Xa相关的疾病。

54. 发明申请

US20100204233A1 IMIDAZOLE DERIVATIVES 审中-公开
标题翻译：咪唑衍生物
公开(公告)号：US20100204233A1
公开(公告)日：2010-08-12
申请号：US12765898
申请日：2010-04-23
申请人： Guido Galley , Katrin Groebke Zbinden , Roger Norcross , Henri Stalder
发明人： Guido Galley , Katrin Groebke Zbinden , Roger Norcross , Henri Stalder
IPC分类号： A61K31/4164 , A61K31/5377 , A61K31/4178 , C07D413/10 , C07D405/12 , C07D233/64 , C07D233/58 , A61P25/00 , A61P25/22 , A61P25/24 , A61P25/16
CPC分类号： C07D233/64
摘要： The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1.The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound.The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.
摘要翻译：本发明涉及对微量胺相关受体（TAAR）具有良好亲和力的咪唑衍生物，特别是TAAR1。本发明还涉及上述化合物的药学上合适的酸加成盐。本发明还涉及包含如上所述的咪唑衍生物或其药学上合适的酸加成盐的组合物及其制备方法。

55. 发明授权

US07718659B2 Heteroarylacetamide inhibitors of factor Xa 有权
标题翻译：因子Xa的杂芳基乙酰胺抑制剂
公开(公告)号：US07718659B2
公开(公告)日：2010-05-18
申请号：US12025124
申请日：2008-02-04
申请人： Markus Boehringer , Katrin Groebke Zbinden , Wolfgang Haap , Hans Hilpert , Narendra Panday , Fabienne Ricklin
发明人： Markus Boehringer , Katrin Groebke Zbinden , Wolfgang Haap , Hans Hilpert , Narendra Panday , Fabienne Ricklin
IPC分类号： A61K31/381 , C07D417/12
CPC分类号： C07D401/10 , C07D277/46 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/10 , C07D417/14
摘要： The invention is concerned with novel heteroarylacetamides of formula (I) Rd—C(O)—N(Re)—Rc—CH2—C(O)—N(Ra)(Rb) (I) wherein Ra to Re are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
摘要翻译：本发明涉及式（I）Rd-C（O）-N（Re）-Rc-CH2-C（O）-N（Ra）（Rb）（Ⅰ）的新型杂芳基乙酰胺，其中Ra与Re的定义相同在说明书和权利要求书中，以及其生理上可接受的盐。这些化合物抑制凝血因子Xa，并且可以用作药物。

56. 发明申请

US20100029589A1 4,5-DIHYDRO-OXAZOL-2YL DERIVATIVES 有权
标题翻译： 4,5-二氢 - 氧杂环戊二烯衍生物
公开(公告)号：US20100029589A1
公开(公告)日：2010-02-04
申请号：US12558772
申请日：2009-09-14
申请人： Guido Galley , Annick Goergler , Katrin Groebke Zbinden , Roger Norcross
发明人： Guido Galley , Annick Goergler , Katrin Groebke Zbinden , Roger Norcross
IPC分类号： A61K31/695 , C07D263/08 , A61K31/421 , C07F7/02 , C07D413/02 , A61K31/4439 , C07D239/02 , A61K31/506 , C07D215/16 , A61K31/47 , A61P25/00 , A61P3/00 , A61P9/00
CPC分类号： A61K31/421 , A61K31/47 , C07D263/48 , C07D401/12 , C07D413/12 , C07F7/081
摘要： The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, 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.
摘要翻译：本发明涉及式I化合物，其中R1，R2，X，Y和n在本说明书中定义及其药学上可接受的酸加成盐。本发明还提供药物组合物和这种化合物的制造方法。这些化合物可用于治疗与微量胺相关受体的生物功能有关的疾病，这些疾病是抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，应激相关疾病，精神病，精神分裂症，神经系统疾病，帕金森病，神经变性疾病，阿尔茨海默病，癫痫，偏头痛，药物滥用和代谢障碍，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，体温平衡失调和失调，睡眠障碍昼夜节律和心血管疾病。

57. 发明申请

US20090270360A1 DICARBOXAMIDE DERIVATIVES 审中-公开
公开(公告)号：US20090270360A1
公开(公告)日：2009-10-29
申请号：US12354953
申请日：2009-01-16
申请人： Markus Boehringer , Katrin Groebke Zbinden , Wolfgang Haap , Hans Hilpert , Jacques Himber , Roland Humm , Hans Iding , Dietmar Knopp , Narendra Panday , Fabienne Ricklin , Christoph Martin Stahl
发明人： Markus Boehringer , Katrin Groebke Zbinden , Wolfgang Haap , Hans Hilpert , Jacques Himber , Roland Humm , Hans Iding , Dietmar Knopp , Narendra Panday , Fabienne Ricklin , Christoph Martin Stahl
IPC分类号： A61K31/4427 , C07D213/64 , A61K31/4418 , A61K31/444 , C07D265/32 , C07D279/02 , A61K31/5377 , A61K31/55 , C07D413/02 , A61K31/54 , A61K31/5375 , A61K31/506 , C07D401/02 , C07D405/02
CPC分类号： C07D213/64 , C07D213/75 , C07D233/64 , C07D279/02 , C07D295/135 , C07D295/185 , C07D401/12
摘要： The invention is concerned with novel dicarboxamide derivatives of formula (I) wherein A, B, Rc, D and E are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型二甲酰胺衍生物，其中A，B，Rc，D和E如说明书和权利要求书中所定义，以及其生理上可接受的盐。这些化合物抑制凝血因子Xa，并且可以用作药物。

58. 发明申请

US20090036420A1 BENZAMIDE DERIVATIVES AND THEIR USE FOR TREATING CNS DISORDERS 审中-公开
标题翻译：苯扎林衍生物及其用于治疗中枢神经系统疾病的用途
公开(公告)号：US20090036420A1
公开(公告)日：2009-02-05
申请号：US12180566
申请日：2008-07-28
申请人： Guido Galley , Katrin Groebke Zbinden , Roger Norcross , Henri Stalder
发明人： Guido Galley , Katrin Groebke Zbinden , Roger Norcross , Henri Stalder
IPC分类号： A61K31/397 , A61K31/55 , A61K31/5377 , A61K31/5375 , A61K31/505 , A61K31/4545 , A61K31/445 , A61K31/4427 , A61K31/4439 , A61K31/44 , A61K31/426 , A61K31/421 , A61K31/415 , A61K31/382 , A61K31/165 , A61K31/34 , C07D413/02 , C07D233/08 , C07D401/02 , C07D265/30 , C07D239/02 , C07D211/68 , C07D211/32 , C07D405/02 , C07D213/56 , C07D275/02 , C07D263/34 , C07D231/02 , C07D207/46 , C07D205/02 , C07D337/08 , C07D307/02 , C07C323/41 , C07C233/88 , A61P25/18 , A61P25/28 , A61P25/24 , A61P25/16
CPC分类号： A61K31/166 , A61K31/167 , C07C233/65 , C07C233/75 , C07C235/56 , C07C237/40 , C07C255/57 , C07C311/16 , C07C311/21 , C07C317/44 , C07D205/06 , C07D211/14 , C07D213/82 , C07D231/12 , C07D263/32 , C07D275/06 , C07D295/155 , C07D295/26 , C07D401/04
摘要： The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明涉及用式I化合物治疗CNS障碍的方法，其中X，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如本说明书中所定义及其药学上可接受的酸加成盐。

59. 发明申请

US20090012138A1 4-IMIDAZOLINES 失效
标题翻译： 4-咪唑啉
公开(公告)号：US20090012138A1
公开(公告)日：2009-01-08
申请号：US12146497
申请日：2008-06-26
申请人： Guido Galley , Katrin Groebke Zbinden , Roger Norcross , Henri Stalder
发明人： Guido Galley , Katrin Groebke Zbinden , Roger Norcross , Henri Stalder
IPC分类号： A61K31/4164 , C07D233/10
CPC分类号： C07D233/06 , C07D233/12 , C07D233/22 , C07D233/24
摘要： The present invention relates to compounds of formula wherein R1, R2, X, Y and Ar are as defined herein and to their pharmaceutically active salts, with the exclusion of the racemic compound 4-benzyl-4,5-dihydro-1H-imidazole or its tautomer (CAS 131548-83-9). Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of 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.
摘要翻译：本发明涉及下式的化合物，其中R 1，R 2，X，Y和Ar如本文所定义及其药学活性盐，排除外消旋化合物4-苄基-4,5-二氢-1H-咪唑或其互变异构体（CAS 131548-83-9）。式I化合物对微量胺相关受体（TAAR）具有良好的亲和力，尤其对于TAAR1，可用于治疗抑郁症，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，精神病性诸如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默氏病，癫痫，偏头痛，高血压，药物滥用和代谢性疾病如进食障碍，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等疾病，体温平衡紊乱和失眠，睡眠障碍和昼夜节律，以及心血管疾病。

60. 发明申请

US20080119535A1 AMINOMETHYL-4-IMIDAZOLES 失效
标题翻译：氨基甲基-4-咪唑烷
公开(公告)号：US20080119535A1
公开(公告)日：2008-05-22
申请号：US11872203
申请日：2007-10-15
申请人： Guido Galley , Annick Goergler , Katrin Groebke Zbinden , Roger Norcross , Henri Stalder
发明人： Guido Galley , Annick Goergler , Katrin Groebke Zbinden , Roger Norcross , Henri Stalder
IPC分类号： A61K31/417 , C07D233/64 , C07D401/12 , C07D403/12 , C07D413/12 , A61P25/00 , A61P25/16 , A61P25/28 , A61P25/06 , A61P3/10
CPC分类号： C07D233/64
摘要： The present invention relates to amino-4-methyl imidazoles and pharmaceutically-acceptable salts thereof.The compound may be used for the treatment of 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.
摘要翻译：本发明涉及氨基-4-甲基咪唑及其药学上可接受的盐。该化合物可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意力缺陷多动障碍（ADHD），应激相关疾病，精神病性精神障碍如精神分裂症，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。

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