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1. 发明申请

WO2007085557A3 USE OF SUBSTITUTED 2-IMIDAZOLE OF IMIDAZOLINE DERIVATIVES 审中-公开
标题翻译：使用取代的咪唑啉衍生物的2-咪唑
公开(公告)号：WO2007085557A3
公开(公告)日：2007-09-20
申请号：PCT/EP2007050443
申请日：2007-01-17
申请人： HOFFMANN LA ROCHE , GALLEY GUIDO , GROEBKE ZBINDEN KATRIN , HOENER MARIUS , KOLCZEWSKI SABINE , NORCROSS ROGER , STALDER HENRI
发明人： GALLEY GUIDO , GROEBKE ZBINDEN KATRIN , HOENER MARIUS , KOLCZEWSKI SABINE , NORCROSS ROGER , STALDER HENRI
IPC分类号： A61K31/4164 , A61K31/4174 , A61P25/00 , C07D233/06 , C07D233/54 , C07D401/04 , C07D405/06 , C07D409/06
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 to the use of compounds of Formula (I), wherein R is hydrogen, tritium, hydroxy, amino, lower alkyl, cycloalkyl, lower alkoxy, halogen, cyano, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, phenyl, O-phenyl, -S-phenyl, optionally substituted by halogen, or is benzyl, benzyloxy, NHC(O)-lower alkyl or pyridin-2,3 or 4-yl; R 1 is hydrogen, hydroxy or lower alkyl; R 2 is hydrogen or lower alkyl; aryl is an aromatic group, selected from phenyl, naphthalen-1-yl or naphthalen-2-yl; hetaryl is an aromatic group, containing at least one O, N or S ring atom, selected from the group consisting of pyridine-3-yl, pyrazolyl, benzofuran-3-yl, benzofuran-4-yl, benzofuran-5-yl, benzofuran-6-yl, benzofuran-7-yl, thiophen-2-yl, thiophen-3-yl, benzo[b]thiophen-3-yl or indol-3-yl; n is 1, 2, 3, 4 or 5; when n is 2, 3, 4 or 5, R may be the same or not; the dotted line may be a bond or not; and to their pharmaceutically active salts for the preparation of medicaments for the treatment of 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.
摘要翻译：本发明涉及式（I）化合物的用途，其中R是氢，氚，羟基，氨基，低级烷基，环烷基，低级烷氧基，卤素，氰基，被卤素取代的低级烷基，苯基，O-苯基，-S-苯基，任选被卤素取代，或者是苄基，苄氧基，NHC（O） - 低级烷基或吡啶-2,3或4-基; R 1是氢，羟基或低级烷基; R 2是氢或低级烷基; 芳基是选自苯基，萘-1-基或萘-2-基的芳族基团; 杂芳基是含有至少一个O，N或S环原子的芳族基团，其选自吡啶-3-基，吡唑基，苯并呋喃-3-基，苯并呋喃-4-基，苯并呋喃-5-基，苯并呋喃-6-基，苯并呋喃-7-基，噻吩-2-基，噻吩-3-基，苯并[b]噻吩-3-基或吲哚-3-基; n是1,2,3,4或5; 当n为2,3,4或5时，R可以相同或不同; 虚线可能是债券或不是; 及其药物活性盐在制备用于治疗抑郁症，焦虑症，双相性精神障碍，注意力缺陷多动障碍，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，神经变性病症例如阿尔茨海默病，癫痫，偏头痛，高血压，物质滥用和代谢障碍，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，体温平衡紊乱和功能障碍，睡眠和昼夜节律紊乱，和心血管疾病。

2. 发明申请

WO2007085556A2 USE OF 4-IMIDAZOLE DERIVATIVES FOR CNS DISORDERS 审中-公开
标题翻译： 4-咪唑衍生物用于CNS病症的用途
公开(公告)号：WO2007085556A2
公开(公告)日：2007-08-02
申请号：PCT/EP2007050441
申请日：2007-01-17
申请人： HOFFMANN LA ROCHE , GALLEY GUIDO , GROEBKE ZBINDEN KATRIN , HOENER MARIUS , NORCROSS ROGER , STALDER HENRI
发明人： GALLEY GUIDO , GROEBKE ZBINDEN KATRIN , HOENER MARIUS , NORCROSS ROGER , STALDER HENRI
IPC分类号： C07D405/06 , A61K31/4174 , A61K31/4178 , A61P25/00 , C07D233/54
CPC分类号： C07D233/64 , C07D405/06
摘要： The present invention relates to the use of compounds of formula (I) wherein R is hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, phenyl, S-phenyl or O-phenyl, which are optionally substituted by lower alkoxy or halogen, or is benzyloxy, C(O)O-lower alkyl, cycloalkyl, or is lower alkyl or lower alkoxy substituted by halogen; Ar is aryl or heteroaryl, selected from the group consisting of phenyl, naphthyl, pyridinyl, benzofuranyl, dihydrobenzofuranyl or pyrazole; R 1 /R 1' are independently from each other hydrogen, hydroxy, lower alkyl, lower alkoxy or are phenyl or benzyl, which are optionally substituted by halogen; R 2 is hydrogen or lower alkyl; n is 1, 2, 3 or 4; and to their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms for the preparation of medicaments for the treatment of 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.
摘要翻译：本发明涉及任选被低级烷氧基或卤素取代的式（I）化合物（其中R为氢，卤素，低级烷基，低级烷氧基，羟基，苯基，S-苯基或O-苯基）的用途，或是苄氧基，C（O）O-低级烷基，环烷基或是被卤素取代的低级烷基或低级烷氧基; Ar是选自苯基，萘基，吡啶基，苯并呋喃基，二氢苯并呋喃基或吡唑的芳基或杂芳基; R 1，R 1，R 1相互独立地为氢，羟基，低级烷基，低级烷氧基或是苯基或苄基，它们任选地被卤素取代; R 2是氢或低级烷基; n是1,2,3或4; 及其药学活性盐，外消旋混合物，对映异构体，光学异构体和互变异构形式，用于制备治疗抑郁症，焦虑症，双相性精神障碍，注意力缺陷多动障碍，压力相关障碍，精神障碍如精神分裂症，帕金森病等神经疾病，阿尔茨海默氏病等神经变性疾病，癫痫症，偏头痛，高血压，药物滥用，代谢障碍如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂障碍，能量消耗和同化障碍，体温平衡，睡眠和昼夜节律紊乱以及心血管疾病。

3. 发明申请

WO2008058867A3 SUBSTITUTED 4-IMIDAZOLES 审中-公开
标题翻译：取代的4-IMIDAZOLES
公开(公告)号：WO2008058867A3
公开(公告)日：2008-07-10
申请号：PCT/EP2007061921
申请日：2007-11-06
申请人： HOFFMANN LA ROCHE , 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 , A61K31/4178 , C07D401/06 , C07D413/06
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：本发明涉及其中R 1为氢或低级烷基的式（I）化合物; 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是-CH 2 - 或-CH-; m为1或2; 当m为2时，R 2可以相同或不相同; n为1或2; 当n为2时，R 3可以相同或不相同; 和药学上可接受的酸加成盐。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。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，物质滥用和代谢紊乱，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。

4. 发明申请

WO2008074679A3 4-IMIDAZOLINES AS TAAR'S LIGANDS 审中-公开
标题翻译： 4-咪唑啉作为TAAR的配体
公开(公告)号：WO2008074679A3
公开(公告)日：2008-10-09
申请号：PCT/EP2007063585
申请日：2007-12-10
申请人： HOFFMANN LA ROCHE , 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： C07D233/64 , A61K31/415 , A61P9/00 , A61P25/00
CPC分类号： C07D233/64
摘要： The invention relates to compounds of formula (I) wherein R is hydrogen, lower alkyl or amino; X-R 1 is -CH 2 -, -CH(lower alkoxy)- or -CH(OH)- and Y-R 2 is -CH 2 , -CH(lower alkyl)-, -CH(lower alkoxy)- -O-, -S-, -S(O)-, -S(O) 2 -, -CH(phenyl)- or -C(lower alkyl) 2 -; or X-R 1 is -NH- and Y-R 2 is -CH 2 , -CH(lower alkyl)-, -CH(lower alkoxy)-, -CH(phenyl)- or -C(lower alkyl) 2 -; Ar is phenyl, napthyl or benzofuranyl, which rings are unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy, lower alkoxy substituted by halogen, hydroxy, amino, di-alkylamino, morpholinyl, phenyl, benzyl or by O-benzyl; or to pharmaceutically suitable 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是氢，低级烷基或氨基; XR 1是-CH 2 - ， - CH（低级烷氧基） - 或-CH（OH） - 且YR 2是-CH 2 - （低级烷基） - ， - CH（低级烷氧基）-O - ， - S - ， - S（O） - ， - S（O）2

5. 发明申请

WO2009003868A2 2-IMIDAZOLINES 审中-公开
标题翻译： 2-咪唑啉
公开(公告)号：WO2009003868A2
公开(公告)日：2009-01-08
申请号：PCT/EP2008057989
申请日：2008-06-24
申请人： HOFFMANN LA ROCHE , 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： C07D233/10 , A61K31/415 , A61K31/4155 , A61P25/00 , C07D233/20 , C07D233/22 , C07D233/24 , C07D233/42 , C07D233/50 , C07D233/52 , C07D405/12
CPC分类号： C07D233/24 , C07D233/20 , C07D233/22 , C07D233/42 , C07D233/52 , C07D405/12
摘要： The present invention relates to compounds of formula (I) wherein X-Y is -N(R2) -CH(R3)-, CH(R3)-N(R2)-, -NH-NH-, -O-CHR3-, -CHR3-O-, -S-CHR3, -CHR3-S- or -CHR3-CHR3 -; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, -(CH2)o-phenyl optionally substituted by lower alkoxy, -(CH2)o-C(O)-phenyl optionally substituted by lower alkoxy, -(CH2)o-O-phenyl optionally substituted by lower alkoxy, -(CH2)o-O-phenyl, CF3, cycloalkyl, NO2, amino or hydroxy; R2 is hydrogen, lower alkyl, phenyl optionally substituted by hydroxy or benzyl; R3/R3' are independently from each other hydrogen, lower alkyl or benzyl; Ar is phenyl, naphthyl, benzofuranyl or benzo [1,3] dioxolyl; n is 1, 2, 3 or 4; o is 0, 1, 2, 3 and to their pharmaceutically active 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）化合物，其中XY是-N（R2）-CH（R3） - ，CH（R3）-N（R2） - ， - NH-NH-，-O-CHR3-， - CHR 3 -O-，-S-CHR 3，-CHR 3 -S-或-CHR 3 -CHR 3 - ; 任选被低级烷氧基取代的 - （CH 2）o C（O） - 苯基，任选被低级烷氧基取代的 - （CH 2）o O-苯基， - （CH 2）（CH 2）o O-苯基，CF 3，环烷基，NO 2，氨基或羟基; R2是氢，低级烷基，任意被羟基或苄基取代的苯基; R3 / R3'彼此独立地为氢，低级烷基或苄基; Ar是苯基，萘基，苯并呋喃基或苯并[1,3]二氧杂环戊烯基; n为1,2,3或4; o是0,1,2,3及其药学活性盐。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。

6. 发明申请

WO2011057973A9 OXAZOLINE DERIVATIVES FOR TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：用于治疗CNS病症的OXAZOLINE衍生物
公开(公告)号：WO2011057973A9
公开(公告)日：2012-02-02
申请号：PCT/EP2010066960
申请日：2010-11-08
申请人： HOFFMANN LA ROCHE , GALLEY GUIDO , NORCROSS ROGER , POLARA ALESSANDRA
发明人： GALLEY GUIDO , NORCROSS ROGER , POLARA ALESSANDRA
IPC分类号： C07D263/28 , A61K31/421 , A61K31/422 , A61K31/4439 , A61K31/506 , A61P25/00 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
CPC分类号： C07D263/28 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The invention relates to compounds of formula (I) wherein the definitions of X, R and R1 are provided in claim 1. It has now been found that the compounds of formula (I) have a good affinity to the trace amine associated receptors (TAARs), especially for TAARl. 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X，R和R 1的定义在权利要求1中提供。现已发现式（I）化合物对微量胺相关受体（TAARs）具有良好的亲和力），特别是对于TAARl。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，物质滥用和代谢紊乱，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。

7. 发明申请

WO2007147770A2 SUBSTITUTED PHENYL METHANONE DERIVATIVES 审中-公开
标题翻译：取代苯甲酮衍生物
公开(公告)号：WO2007147770A2
公开(公告)日：2007-12-27
申请号：PCT/EP2007055871
申请日：2007-06-14
申请人： HOFFMANN LA ROCHE , JOLIDON SYNESE , NARQUIZIAN ROBERT , NORCROSS ROGER , PINARD EMMANUEL
发明人： JOLIDON SYNESE , NARQUIZIAN ROBERT , NORCROSS ROGER , PINARD EMMANUEL
IPC分类号： C07D205/04 , A61K31/445 , A61P25/18 , C07D207/06 , C07D211/16 , C07D407/10
CPC分类号： C07D207/06 , C07D207/08 , C07D211/16 , C07D403/10 , C07D407/10
摘要： The present invention relates to compounds of the general formula (i), wherein R 1 is -OR 1
摘要翻译：本发明涉及通式（ⅰ）的化合物，其中R 1是-OR 1，

8. 发明专利

JP2013173779A Aminomethyl-4-imidazole 有权
标题翻译：氨基甲基-4-咪唑烷
公开(公告)号：JP2013173779A
公开(公告)日：2013-09-05
申请号：JP2013096834
申请日：2013-05-02
申请人： F Hoffmann La Roche Ag , エフ.ホフマン−ラロシュアーゲーF. Hoffmann−La Roche Aktiengesellschaft
发明人： GALLEY GUIDO , GOERGLER ANNICK , GROEBKE ZBINDEN KATRIN , NORCROSS ROGER , STALDER HENRI
IPC分类号： C07D233/64 , A61K31/417 , A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/517 , A61K31/5377 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/12 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D233/64
摘要： PROBLEM TO BE SOLVED: To provide a compound which has a good affinity to the trace amine associated receptor (TAAR) and which can be used for the treatment of depression, an anxiety disorder, a bipolar disorder, an attention deficit hyperactivity disorder (ADHD), a stress-related disorder, a psychotic disorder, and a cardiovascular disorder or the like.SOLUTION: A compound is selected from a group of aminomethyl-4-imidazole compounds exemplified by formula.
摘要翻译：要解决的问题：提供对微量胺相关受体（TAAR）具有良好亲和力的化合物，其可用于治疗抑郁症，焦虑症，双相情感障碍，注意缺陷多动障碍（ADHD），应激相关疾病，精神病性障碍和心血管疾病等。溶液：化合物选自由式表示的氨基甲基-4-咪唑化合物。

9. 发明专利

MA37944B2 Dérivés de pyrazole-carboxamide en tant que modulateurs de taar pour utilisation dans le traitement de plusieurs troubles, tels que la dépression, le diabète et la maladie de parkinson 未知
公开(公告)号：MA37944B2
公开(公告)日：2017-10-31
申请号：MA37944
申请日：2013-09-11
申请人： HOFFMANN LA ROCHE , HOFFMANN-LA ROCHE INC
发明人： GALLEY GUIDO , NORCROSS ROGER , PFLIEGER PHILIPPE
IPC分类号： A61K31/4155 , A61K31/454 , A61K31/5377 , A61P25/00 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要： La présente invention concerne des composés de formule (i) dans laquelle r1 est phényle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, alcoxy inférieur, cyano, alkyle inférieur substitué par halogène, alkyle inférieur substitué par hydroxy, alcoxy inférieur substitué par halogène ou alcoxy inférieur substitué par hydroxy ; ou est pyridine-2, 3 ou 4-yle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, cyano, alkyle inférieur substitué par halogène, alkyle inférieur substitué par hydroxy, alcoxy inférieur, alcoxy inférieur substitué par halogène ou alcoxy inférieur substitué par hydroxyle ; ou est pyrimidin-2, 4 ou 5-yle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, alkyle inférieur substitué par hydroxy ou alkyle inférieur substitué par halogène ; ou est pyrazin-2-yle, facultativement substitué par halogène, alkyle inférieur, cycloalkyle inférieur, alkyle inférieur substitué par halogène, alkyle inférieur substitué par hydroxy ou cyano ; ou est 2,2-difluorobenzo[d][1,3]dioxol-5-yle, ou est thiazolyle, facultativement substitué par alkyle inférieur substitué par halogène ; r2 est hydrogène ou alkyle inférieur ; r3 est hydrogène, amino ou alkyle inférieur ; z est une liaison, -ch2- ou -o- ; ou un sel d'addition d’acide pharmaceutiquement adapté. Il a maintenant été découvert que les composés de formule i ont une bonne affinité pour les récepteurs associés aux amines traces (taar), notamment taar1. Les composés peuvent être utilisés pour le traitement de la dépression, des troubles anxieux, du trouble bipolaire, de l'hyperactivité avec déficit de l'attention (adhd), des troubles relatifs au stress, des troubles psychotiques tels que la schizophrénie, des maladies neurologiques telles que la maladie de parkinson, des maladies neurodégénératives telles que la maladie d'alzheimer, de l'épilepsie, de la migraine, de l'hypertension, de l'abus d'alcool ou d'autres drogues et de troubles métaboliques tels que les troubles de l'alimentation, le diabète, les complications diabétiques, l'obésité, la dyslipidémie, les troubles de la consommation d'énergie et de l'assimilation, les troubles et le mauvais fonctionnement de l'homéostasie de la température corporelle, les troubles du sommeil et du rythme circadien, et les troubles cardiovasculaires.

10. 发明专利

CA2943575C MORPHOLIN-PYRIDINE DERIVATIVES 未知
公开(公告)号：CA2943575C
公开(公告)日：2022-08-30
申请号：CA2943575
申请日：2015-04-27
申请人： HOFFMANN LA ROCHE
发明人： GALLEY GUIDO , PFLIEGER PHILIPPE , NORCROSS ROGER , CECERE GIUSEPPE , SHEN HONG , HU YIMIN
IPC分类号： C07D413/12 , A61K31/5377 , A61P25/00 , C07D413/14
摘要： The present invention relates to compounds of formula (I) wherein X is CR or N; R is hydrogen, halogen or lower alkyl; L is a bond, -C(O)- or -C(O)NH-; Ar is phenyl or a five or six membered heteroaryl group, containing one or two N atoms; R1 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or cycloalkyl; n is 0, 1, 2 or 3; or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, all their corresponding enantiomers and/or optical isomers, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, 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.

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