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21. 发明申请

WO2010139707A1 2-AMINOOXAZOLINES AS TAAR1 LIGANDS 审中-公开
标题翻译： 2-AMINOOXAZOLINES as TAAR1 LIGANDS
公开(公告)号：WO2010139707A1
公开(公告)日：2010-12-09
申请号：PCT/EP2010/057669
申请日：2010-06-02
申请人： F. HOFFMANN-LA ROCHE AG , DECORET, Guillaume , GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger
发明人： DECORET, Guillaume , GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger
IPC分类号： C07D263/28 , A61K31/421 , A61P25/00
CPC分类号： C07D263/28
摘要： The invention relates to compounds of formula (I) wherein R 1 is halogen; R 2 is lower alkyl or lower alkyl substituted by halogen; R 2' is hydrogen, lower alkyl or lower alkyl substituted by halogen; X is a bond, -CH 2 -, -CH 2 CH 2 - or -CH 2 CH 2 CH 2 -; Y is phenyl or cyclohexyl; and n is 0, 1 or 2; or to a pharmaceutically suitable acid addition salt thereof. The compounds of formula I are active on the TAAR1 receptor and are therefore suitable for the treatment of 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：本发明涉及其中R 1为卤素的式（I）化合物; R2是被卤素取代的低级烷基或低级烷基; R2'是氢，被卤素取代的低级烷基或低级烷基; X是键，-CH 2 - ， - CH 2 CH 2 - 或-CH 2 CH 2 CH 2 - ; Y是苯基或环己基; 且n为0,1或2; 或其药学上合适的酸加成盐。式I化合物对TAAR1受体具有活性，因此适用于治疗抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，应激相关疾病，精神病性精神病，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，药物滥用和代谢紊乱，饮食失调，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，睡眠和昼夜节律障碍以及心血管障碍。

22. 发明申请

WO2009019149A1 PYRIDINECARBOXAMIDE AND BENZAMIDE DERIVATIVES AS TAAR1 LIGANDS 审中-公开
标题翻译：吡啶甲酰胺和苯甲酰胺衍生物作为TAAR1配体
公开(公告)号：WO2009019149A1
公开(公告)日：2009-02-12
申请号：PCT/EP2008/059790
申请日：2008-07-25
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
发明人： GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
IPC分类号： C07C233/66 , C07D213/82 , C07D235/06 , C07D401/12 , C07D407/12 , A61K31/497 , A61K31/4439 , A61K31/444 , A61K31/44 , A61K31/404 , A61P3/00
CPC分类号： C07D213/80 , C07C233/66 , C07D213/82 , C07D235/08 , C07D401/12 , C07D405/12
摘要： The invention relates to a compound of formula (I) wherein R 1 , R 2 , W, L, X, n and o are defined herein. It has been found that the compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds 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：本发明涉及其中R1，R2，W，L，X，n和o如本文所定义的式（I）化合物。已经发现，式I化合物对微量胺相关受体（TAAR）具有良好的亲和力，特别是对于TAAR1。这些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。

23. 发明申请

WO2009016088A1 THE USE OF BENZAMIDE DERIVATIVES FOR THE TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：使用苯甲酸衍生物治疗中枢神经系统疾病
公开(公告)号：WO2009016088A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/059698
申请日：2008-07-24
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
发明人： GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
IPC分类号： A61K31/166 , A61K31/167 , C07D213/00 , A61P9/12 , A61P9/00 , A61P25/00 , A61P3/00
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 the use of a compound of formula (I), wherein R or a pharmaceutically acceptable acid addition salt thereof, for the manufacture of a medicament for the treatment of CNS disorders selected from 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：本发明涉及式（I）化合物或其药学上可接受的酸加成盐在制备用于治疗选自抑郁症，焦虑障碍，双相性精神障碍，注意力的中枢神经系统疾病的药物中的用途缺血性多动障碍（ADHD），压力相关障碍，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，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。

24. 发明申请

WO2006066778A2 NOVEL HETEROARYLACETAMIDES 审中-公开
标题翻译：新的杂芳基乙酰胺
公开(公告)号：WO2006066778A2
公开(公告)日：2006-06-29
申请号：PCT/EP2005/013460
申请日：2005-12-14
申请人： F. HOFFMANN-LA ROCHE AG , BOEHRINGER, Markus , GROEBKE ZBINDEN, Katrin , HAAP, Wolfgang , HILPERT, Hans , PANDAY, Narendra , RICKLIN, Fabienne
发明人： BOEHRINGER, Markus , GROEBKE ZBINDEN, Katrin , HAAP, Wolfgang , HILPERT, Hans , PANDAY, Narendra , RICKLIN, Fabienne
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) R d -C(O)-N(R e )-R c -CH 2 -C(O)-N(R a )(R b ), wherein R a to R 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）的新型杂芳基乙酰胺R d -C（O）-N（R e）（O）-N（R a）（R b），其中R 1，R 2，其中R 1至R e如说明书和权利要求中所定义，以及其生理上可接受的盐。这些化合物抑制凝血因子Xa并可以用作药物。

25. 发明申请

WO2006048152A3 DICARBOXAMIDE DERIVATIVES AND THEIR USE AS FACTOR XA INHIBITORS 审中-公开
公开(公告)号：WO2006048152A3
公开(公告)日：2006-05-11
申请号：PCT/EP2005/011430
申请日：2005-10-25
申请人： F. HOFFMANN-LA ROCHE AG , BOEHRINGER, Markus , GROEBKE ZBINDEN, Katrin , HAAP, Wolfgang , HILPERT, Hans , HIMBER, Jacques , HUMM, Roland , IDING, Hans , KNOPP, Dietmar , PANDAY, Narendra , RICKLIN, Fabienne , STAHL, Christoph, Martin
发明人： BOEHRINGER, Markus , GROEBKE ZBINDEN, Katrin , HAAP, Wolfgang , HILPERT, Hans , HIMBER, Jacques , HUMM, Roland , IDING, Hans , KNOPP, Dietmar , PANDAY, Narendra , RICKLIN, Fabienne , STAHL, Christoph, Martin
IPC分类号： C07D213/64 , C07D401/12 , C07D233/54 , C07D213/75 , C07D295/12 , C07D279/02 , C07D295/18 , A61K31/4412 , A61P7/02
摘要： The invention is concerned with novel dicarboxamide derivatives of formula (I) wherein A, B, R C , D and E are as defined in the description and in the claims, as well 5as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

26. 发明申请

WO2008058867A2 SUBSTITUTED 4-IMIDAZOLES 审中-公开
标题翻译：取代的4-咪唑
公开(公告)号：WO2008058867A2
公开(公告)日：2008-05-22
申请号：PCT/EP2007/061921
申请日：2007-11-06
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
发明人： GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
IPC分类号： C07D403/06 , C07D401/06 , C07D413/06 , A61K31/4178
CPC分类号： C07D401/06 , C07D403/06 , C07D413/06
摘要： The present invention relates to compounds of formula (I) wherein R 1 is hydrogen or lower alkyl; R 2 is hydrogen or lower alkyl; R 3 is hydrogen, lower alkyl, lower alkoxy, phenyloxy, benzyloxy, halogen or lower alkyl substituted by halogen; R 4 is hydrogen or lower alkyl; X is -CH 2 -, -CH- or -O-; Y is -CH 2 -, -CH 2 CH 2 -, -CH- or a bond; when X is -O-, then Y is -CH 2 -; Z is -CH 2 - or -CH-; m is 1 or 2; when m is 2, R 2 may be the same or not; n is 1 or 2; when n is 2, R 3 may be the same or not; and to pharmaceutically acceptable acid addition salts. It has been found that the compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds 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：本发明涉及式（I）的化合物，其中R 1为氢或低级烷基; R 2是氢或低级烷基; R 3是氢，低级烷基，低级烷氧基，苯氧基，苄氧基，卤素或被卤素取代的低级烷基; R 4是氢或低级烷基; X是-CH 2 - ， - CH-或-O-; Y是-CH 2 - ， - CH 2 CH 2 - ， - CH-或键; 当X是-O-时，则Y是-CH 2 - ; - Z为-CH 2 - 或-CH-; m是1或2; 当m是2时，R 2可以相同或不相同; n是1或2; 当n是2时，R 3可以相同或不同; 并涉及药学上可接受的酸加成盐。已经发现式I化合物对痕量胺相关受体（TAAR）具有良好的亲和力，特别是对于TAAR1。该化合物可用于治疗抑郁症，焦虑症，双相性精神障碍，注意力缺陷多动障碍（ADHD），压力相关障碍，精神障碍如精神分裂症，神经疾病如帕金森病，神经变性障碍如阿尔茨海默病，癫痫症，偏头痛，高血压，药物滥用和代谢障碍例如进食障碍，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，体温平衡紊乱和障碍，睡眠和昼夜节律紊乱以及心血管疾病

27. 发明申请

WO2007025949A1 NOVEL CYCLOALKANE CARBOXAMIDES AS FACTOR XA INHIBITORS 审中-公开
标题翻译：新型循环卡波酰胺作为因子XA抑制剂
公开(公告)号：WO2007025949A1
公开(公告)日：2007-03-08
申请号：PCT/EP2006/065732
申请日：2006-08-28
申请人： F. HOFFMANN-LA ROCHE AG , GROEBKE ZBINDEN, Katrin , HAAP, Wolfgang , HILPERT, Hans , PANDAY, Narendra , RICKLIN, Fabienne
发明人： GROEBKE ZBINDEN, Katrin , HAAP, Wolfgang , HILPERT, Hans , PANDAY, Narendra , RICKLIN, Fabienne
IPC分类号： C07D409/12 , C07D413/12 , A61K31/4427 , A61K31/5377 , A61P7/02
CPC分类号： C07D413/12 , C07D409/12
摘要： The invention is concerned with novel cycloalkane carboxamides of Formula (I) wherein X, X 1 , Y, Y 1’ , R 1’’ , R 1 , R 2 , R 3 , m and n 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）的新型环烷甲酰胺，其中X，X 1，Y，Y 1'，R 1， R 1，R 2，R 3，m和n如说明书和权利要求书中所定义，以及生理上可接受的的盐。这些化合物抑制凝血因子Xa，并且可以用作药物。

28. 发明申请

WO2005092881A1 NOVEL PYRROLIDINE-3,4-DICARBOXAMIDE DERIVATIVES 审中-公开
标题翻译：新型吡咯烷-3,4-二酰胺衍生物
公开(公告)号：WO2005092881A1
公开(公告)日：2005-10-06
申请号：PCT/EP2005/002862
申请日：2005-03-17
申请人： F. HOFFMANN-LA ROCHE AG , ANSELM, Lilli , GROEBKE ZBINDEN, Katrin , HAAP, Wolfgang , HIMBER, Jacques , STAHL, Christoph, Martin , THOMI, Stefan
发明人： ANSELM, Lilli , GROEBKE ZBINDEN, Katrin , HAAP, Wolfgang , HIMBER, Jacques , STAHL, Christoph, Martin , THOMI, Stefan
IPC分类号： C07D401/12
CPC分类号： C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12
摘要： The invention is concerned with novel pyrrolidine-3,4-dicarboxamide derivatives of Formula (I) ; wherein R l to R 9 and X 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）的新型吡咯烷-3,4-二甲酰胺衍生物; 其中R 1至R 9和X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。

29. 发明申请

WO2009003867A1 4-IMIDAZOLINES AND THEIR USE AS ANTIDEPRESSANTS 审中-公开
标题翻译： 4-咪唑啉及其作为抗生素的用途
公开(公告)号：WO2009003867A1
公开(公告)日：2009-01-08
申请号：PCT/EP2008/057980
申请日：2008-06-24
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
发明人： GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
IPC分类号： C07D233/06 , C07D233/12 , C07D233/22 , C07D233/24 , A61K31/4174 , A61P25/24
CPC分类号： C07D233/06 , C07D233/12 , C07D233/22 , C07D233/24
摘要： The present invention relates to compounds of formula (I) wherein R 1 is hydrogen, halogen or lower alkyl; R 2 is hydrogen or amino; X-Y is -(CH 2 ) n -, N(R)-CH 2 -, -O-CH 2 - or -S-CH 2 -; Ar is phenyl or naphthyl; n is 1 or 2; R is hydrogen or lower alkyl; and to their pharmaceutically active salts, with the exclusion of the racemic compound 4-benzyl-4,5-dihydro-lH-imidazole or its tautomer (CAS 131548-83-9). It has been found that the compounds of formula (I) have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds 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：本发明涉及式（I）化合物，其中R 1是氢，卤素或低级烷基; R2是氢或氨基; X-Y是 - （CH 2）n - ，N（R）-CH 2 - ， - O-CH 2 - 或-S-CH 2 - ; Ar是苯基或萘基; n为1或2; R是氢或低级烷基; 和其药物活性盐，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）。已经发现式（I）化合物对微量胺相关受体（TAAR）具有良好的亲和力，特别是对于TAAR1。这些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。

30. 发明申请

WO2008098857A1 2-AMINOOXAZOLINES AS TAAR1 LIGANDS 审中-公开
标题翻译： 2-AMINOOXAZOLINES as TAAR1 LIGANDS
公开(公告)号：WO2008098857A1
公开(公告)日：2008-08-21
申请号：PCT/EP2008/051377
申请日：2008-02-05
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
发明人： GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
IPC分类号： C07D263/28 , C07D413/06 , A61P25/00 , A61K31/421 , A61K31/422
CPC分类号： C07D263/28 , C07D413/06
摘要： The invention relates to compounds of formula (I) wherein R 1 is aryl or heteroaryl, wherein the aryl and heteroaryl groups may be unsubstituted or substituted by one to three substituents, selected from the group consisting of cycloalkyl, phenyl, phenyloxy, benzyl, benzyloxy, halogen, lower alkyl, lower alkoxy, heteroaryl, piperidin-1-yl or by lower alkyl substituted by halogen, or is aryl or heteroaryl wherein at least one hydrogen atom is replaced by deuterium or tritium; R 2 is hydrogen, lower alkyl or is benzyl unsubstituted or substituted by alkoxy or halogen; or R 1 and R 2 form together with the N-atom to which they are attached 2,3-dihydroindol-1-yl or 3,4-dihydro-quinolin-1-yl; R 3 is hydrogen or lower alkyl or to a pharmaceutically suitable acid addition salt thereof for the treatment of CNS disorders.
摘要翻译：本发明涉及其中R 1为芳基或杂芳基的式（I）化合物，其中芳基和杂芳基可以是未被取代的或被1至3个选自以下的取代基取代：环烷基，苯基，苯氧基，苄基，苄氧基，卤素，低级烷基，低级烷氧基，杂芳基，哌啶-1-基或被卤素取代的低级烷基，或是芳基或杂芳基，其中至少一个氢原子被氘或氚代替; R 2是氢，低级烷基或未被取代或被烷氧基或卤素取代的苄基; 或R 1和R 2 2形式与它们所连接的N-原子一起形成2,3-二氢吲哚-1-基或3,4-二氢 - 喹啉-2-基， -1-基; R 3是氢或低级烷基或其药学上合适的酸加成盐，用于治疗CNS障碍。

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