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1. 发明申请

WO2009016048A1 2-AZETIDINEMETHANEAMINES AND 2-PYRROLIDINEMETHANEAMINES AS TAAR-LIGANDS 审中-公开
标题翻译： 2-氨基乙酰胺和2-吡咯烷基磺酰胺作为TAAR-LIGANDS
公开(公告)号：WO2009016048A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/059429
申请日：2008-07-18
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
发明人： GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
IPC分类号： C07D205/04 , C07D207/09 , A61K31/397 , A61K31/40 , A61P25/00
CPC分类号： C07D205/04 , C07D207/09
摘要： The present invention relates to compounds of formula (I) wherein R 1 is hydrogen, lower alkyl or benzyl which may be optionally substituted by halogen or lower alkoxy; R 2 is hydrogen, halogen or OR, wherein R is lower alkyl, aryl or lower alkyl substituted by halogen; R 3 is hydrogen or fluorine; Ar is phenyl; n is 0 or 1; o is 0, 1 or 2; 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R 1是氢，可以被卤素或低级烷氧基任意取代的低级烷基或苄基; R2是氢，卤素或OR，其中R是被卤素取代的低级烷基，芳基或低级烷基; R3是氢或氟; Ar是苯基; n为0或1; o为0,1或2; 和其药物活性盐。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。

2. 发明申请

WO2008046757A1 AMINOMETHYL-4-IMIDAZOLES 审中-公开
标题翻译：氨基甲基-4-咪唑类
公开(公告)号：WO2008046757A1
公开(公告)日：2008-04-24
申请号：PCT/EP2007/060666
申请日：2007-10-09
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
发明人： GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
IPC分类号： C07D233/64 , A61K31/4178 , A61P25/00
CPC分类号： C07D233/64
摘要： The present invention relates to compounds of formula (I) wherein R 1 is hydrogen, lower alkyl, -(CR 2 ) n -OH, -(CH2) n -aryl or -(CH 2 ) n -heteroaryl, which are optionally substituted by halogen, lower alkoxy or lower alkyl substituted by halogen, or is -(CR 2 ) n - cycloalkyl, optionally substituted by hydroxy, -(CH 2 ) n -heterocyclyl, -(CH 2 ) n -NH-S(O) 2 CH 3 , or is -(CR 2 ) n O-lower alkyl or lower alkyl substituted by halogen; R is hydrogen or lower alkyl, and when two R-groups are present, they may or may not be the same; R 2 is 2,2-dioxo-2,3-dihydro-1 H -benzo[c]thiophenyl, 6,7-dihydro-5 H -cyclopentapyrimidin-2-yl, 2,2-difluoro-benzo[1,3]dioxol-5-yl, 2,2,3,3-tetrafluoro-2,3-dihydro-benzo[1,4]dioxin-6-yl, or is aryl or heteroaryl, optionally substituted by one or more substituents, selected from the group consisting of halogen, lower alkyl, cycloalkyl, -(CH 2 ) n -hydroxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, -S(O) 2 -lower alkyl, -(CH 2 ) n -S(O) 2 -NH-lower alkyl, -(CH 2 ) n -O-lower alkyl, nitro, amino, cyano, -NHC(O)-lower alkyl, -C(O)NH-lower alkyl, or O-tetrahydro-naphthalenyl, or are substituted by -(CH 2 ) n -aryl, optionally substituted by halogen, or by -CH=CH-aryl, optionally substituted by halogen, or by -(CH 2 ) n -O-aryl, optionally substituted by halogen, lower alkoxy or lower alkyl substituted by halogen, or by -O-(CH 2 ) n -aryl, optionally substituted by halogen, or by -(CH 2 ) n -heteroaryl, or by -(CH 2 ) n -O-heteroaryl or by -(CH 2 ) n -heterocyclyl, optionally substituted by =O, or by -(CH 2 ) n -O-heterocyclyl, optionally substituted by lower alkyl, or by -S-aryl, -CH(OH)-aryl, -C(CH 3 ) 2 -aryl, -NR-aryl, or by 2-oxo-2H-pyridin-1-yl; R 3 is hydrogen or lower alkyl; R 4 is hydrogen or lower alkyl; n is 0, 1, 2, 3 or 4 and to their pharmaceutically active salts 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，低级烷基， - （CR 2）n -OH， - （CH 2）n - 芳基或 - （CH 2）n - 杂芳基，其任选被卤素，低级烷氧基或低级烷基被卤素取代，或是 - （CR 2）n - 环烷基，任选被羟基取代， - （CH 2）n - （CH 2）n - 杂环基， - （CH 2）n -NH-S（O）2 CH 3 >或者是 - （CR 2）n - 低级烷基或被卤素取代的低级烷基; R是氢或低级烷基，当存在两个R基时，它们可以相同也可以不相同; R 2是2,2-二氧代-2,3-二氢-1H-苯并[c]噻吩基，6,7-二氢-5H-环戊基嘧啶-2-基，2,2-二氟 - 苯并[1,3]二氧杂环戊烯-5-基，2,2,3,3-四氟-2,3-二氢 - 苯并[1,4]二恶英-6-基，或者是芳基或杂芳基，任选被一个或更多取代基，选自卤素，低级烷基，环烷基， - （CH 2）n - 羟基，被卤素取代的低级烷基，被卤素，-S（O）2 - 低级烷基， - （CH 2）n - （O）2 - （CH 2）n - 低级烷基，硝基，氨基，氰基，-NHC（O） - 低级烷基， - （CH 2） C（O）NH-低级烷基或O-四氢 - 萘基，或被 - （CH 2 CH 2）n - 芳基取代，任选被卤素取代，或被 -CH = CH-芳基，任选被卤素取代，或被 - （CH 2 CH 2）n -O-取代的，被卤素，低级烷氧基或低级烷基取代的通过卤素或-O-（CH 2 CH 2）n

3. 发明申请

WO2008046756A1 AMINOMETHYL-2-IMIDAZOLES WITH AFFINITY WITH THE TRACE AMINE ASSOCIATED RECEPTORS 审中-公开
标题翻译：与维生素A相关受体有亲和力的氨基甲基-2-咪唑烷
公开(公告)号：WO2008046756A1
公开(公告)日：2008-04-24
申请号：PCT/EP2007/060664
申请日：2007-10-09
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
发明人： GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
IPC分类号： C07D233/64 , C07D401/12 , C07D403/12 , C07D409/12 , A61K31/417 , A61P25/00
CPC分类号： C07D233/64 , C07D401/12 , C07D403/12 , C07D409/12
摘要： The present invention relates to compounds of Formula (I) 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）的化合物及其药学活性盐。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，体温平衡失调和失眠，睡眠障碍和昼夜节律和心血管疾病。

4. 发明申请

WO2010010014A1 4,5-DIHYDRO-OXAZOL-2-YL DERIVATIVES 审中-公开
标题翻译： 4,5-DIHYDRO-OXAZOL-2-YL衍生物
公开(公告)号：WO2010010014A1
公开(公告)日：2010-01-28
申请号：PCT/EP2009/059026
申请日：2009-07-15
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger
发明人： GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger
IPC分类号： C07D263/28 , C07D413/12 , A61K31/421 , A61K31/422 , A61P25/00 , A61P3/04 , A61P3/06 , A61P3/10
CPC分类号： C07D263/28 , C07D413/12
摘要： The invention relates to compounds of formula (I) wherein R 1 is hydrogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, halogen, cyano, nitro, hydroxy, C(O)O-lower alkyl, S(O) 2 -lower alkyl, C(O)OCH 2 -phenyl, OCH 2 -phenyl, tetrazol-1-yl, phenyl optionally substituted by halogen, or is phenyloxy optionally substituted by halogen, or is benzyl optionally substituted by halogen or is benzyloxy optionally substituted by halogen, wherein the substituents for n> 1 may be the same or different; X is -O-(CH 2 ) 2 -, -O-CHR"-CH 2 -, -O-CH 2 -CHR', -O-CR'' 2 -CH 2 -, -(CH 2 ) 2 -CHR', -CHR'-(CH 2 ) 2 -, -CR" 2 -(CH 2 ) 2 -, -CH 2 -CHR'-CH 2 -, -CH 2 -CR'' 2 -CH 2 -, -CHR"-O-CH 2 -, -CH 2 -O-CH 2 -, -CR'' 2 -O-CH 2 -, -CF 2 (CH 2 ) 2 -, -CR" 2 -CH 2 -, -SiR" 2 -(CH 2 ) 2 -, -S-(CH 2 ) 2 -, -S(O) 2 -(CH 2 ) 2 -, -(CH 2 ) 4 -, -CH 2 -O-(CH 2 ) 2 -, for m being 0, 1, 2 or 3; R' is lower alkyl, lower alkoxy or lower alkyl substituted by halogen; R'' is lower alkyl or lower alkyl substituted by halogen; R 2 is hydrogen or lower alkyl; Y is aryl, cycloalkyl or heteroaryl; n is 1, 2 or 3; or to a pharmaceutically suitable acid addition salt. The compounds disclosed in the present formula (I) may be used 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R 1是氢，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素，卤素，氰基，硝基，羟基，C（O）O-低级烷基取代的低级烷氧基， S（O）2 - 低级烷基，C（O）OCH 2 - 苯基，OCH 2 - 苯基，四唑-1-基，任选被卤素取代的苯基，或任选被卤素取代的苯氧基，或是任选被卤素取代的苄基，任选被卤素取代的苄氧基，其中n> 1的取代基可以相同或不同; X是-O-（CH 2）2 - ， - O-CHR“-CH 2 - ，-O-CH 2 -CHR'，-O-CR''2-CH 2 - ， - （CH 2）2 -CHR' ' - （CH 2）2 - ， - CR“2-（CH 2）2 - ， - CH 2 -CHR'-CH 2 - ， - CH 2 -CR''2-CH 2 - ， - CHR”-O-CH 2 - ， - CH 2 （CH 2）2 - ， - CR“2 -CH 2 - ，-SiR”2-（CH 2）2 - ， - S-（CH 2）2 - 2，-S（O）2 - （CH 2）2 - ， - （CH 2）4 - ， - CH 2 -O-（CH 2）2 - ，其中m为0,1,2或3; R' 低级烷氧基或被卤素取代的低级烷基; R“为被卤素取代的低级烷基或低级烷基; R 2为氢或低级烷基; Y为芳基，环烷基或杂芳基; n为1,2或3; 本发明式（I）中公开的化合物可用于治疗与微量胺相关受体的生物学功能有关的疾病，所述疾病是抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，压力相关疾病，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，睡眠和昼夜节律紊乱以及心血管疾病。

5. 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。

6. 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。

7. 发明申请

WO2009003868A3 2 -IMIDAZOLINES HAVING A GOOD AFFINITY TO THE TRACE AMINE ASSOCIATED RECEPTORS (TAARS) 审中-公开
公开(公告)号：WO2009003868A3
公开(公告)日：2009-01-08
申请号：PCT/EP2008/057989
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： C07D233/10 , C07D233/20 , C07D233/22 , C07D233/24 , C07D233/42 , C07D233/50 , C07D233/52 , C07D405/12 , A61K31/415 , A61K31/4155 , A61P25/00
摘要： The present invention relates to compounds of formula (I) wherein X-Y is -N(R 2 ) -CH(R 3 )-, CH(R 3 )-N(R 2 )-, -NH-NH-, -O-CHR 3 -, -CHR 3 -O-, -S-CHR 3 , -CHR 3 -S- or -CHR 3 -CHR 3 -; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy, -(CH 2 ) o -phenyl optionally substituted by lower alkoxy, -(CH 2 ) o -C(O)-phenyl optionally substituted by lower alkoxy, -(CH 2 ) o -O-phenyl optionally substituted by lower alkoxy, -(CH 2 ) o -O-phenyl, CF 3 , cycloalkyl, NO 2 , amino or hydroxy; R 2 is hydrogen, lower alkyl, phenyl optionally substituted by hydroxy or benzyl; R 3 /R 3' 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.

8. 发明申请

WO2007085557A2 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-咪唑烷
公开(公告)号：WO2007085557A2
公开(公告)日：2007-08-02
申请号：PCT/EP2007/050443
申请日：2007-01-17
申请人： F. HOFFMANN-LA ROCHE AG , 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
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，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，被卤素取代的低级烷氧基，苯基，O-苯基，-S-苯基，任选被卤素取代，或为苄基，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-基的芳基; 杂芳基是芳族基团，其含有至少一个选自吡啶-3-基，吡唑基，苯并呋喃-3-基，苯并呋喃-4-基，苯并呋喃-5-基的O，N或S环原子，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为1,2,3,4或5; 当n为2,3,4或5时，R可以相同或不相同; 虚线可能是一个债券; 以及用于制备用于治疗抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，应激相关疾病，精神病性精神病如精神分裂症，神经性疾病如帕金森病，神经变性疾病如神经变性疾病的药物的药学活性盐阿尔茨海默氏病，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，和心血管疾病。

9. 发明申请

WO2008092785A1 NOVEL 2-AMINOOXAZOLINES AS TAAR1 LIGANDS FOR CNS DISORDERS 审中-公开
标题翻译：新的2-AMINOOXAZOLINES作为TAAR1中枢神经系统疾病的配偶
公开(公告)号：WO2008092785A1
公开(公告)日：2008-08-07
申请号：PCT/EP2008/050765
申请日：2008-01-23
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 , C07D413/04 , A61K31/421 , A61K31/422 , A61P25/00 , A61P3/04 , A61P3/06 , A61P3/10
CPC分类号： C07D263/28 , C07D413/04 , C07D413/06 , C07D413/12 , C07F7/0812
摘要： The invention relates to the use of compounds of Formula (I) wherein R 1 is hydrogen, deuterium, tritium, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, halogen, phenyl optionally substituted by halogen, or is phenyloxy, benzyl, benzyloxy, -COO-lower alkyl, -O-(CH 2 ) o -O-lower alkyl, NH-cycloalkyl, cycloalkyl or tetrahydropyran-4-yloxy, wherein the substituents for n> 1 may be the same or different; X is a bond, -CHR-, -CHRCHR'-, -OCH 2 -, -CH 2 OCHR-, -CH 2 CH 2 CH 2 -, -SCH 2 -, -S(O) 2 CH 2 -, -CH 2 SCH 2 -, -CH 2 N(R)CH 2 -, -cycloalkyl-CH 2 - or SiRR'-CH 2 -; R/R' may be independently from each other hydrogen, lower alkyl or lower alkyl substituted by halogen; R 2 is hydrogen, phenyl or lower alkyl; Y is phenyl, naphthyl, thiophenyl, pyridinyl, cycloalkyl, 1,2,3,4-tetrahydro-naphthalen-2-yl, 2,3-dihydrobenzo[1,4]dioxin-6-yl or benzo[1,3]dioxol-5-yl; n is 0, 1, 2 or 3; o is 2 or 3; or to a pharmaceutically suitable acid addition salt for the manufacture of medicaments 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R 1为氢，氘，氚，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，卤素，任选被卤素取代的苯基，或苯氧基，苄基，苄氧基，-COO-低级烷基，-O-（CH 2）n -O-低级烷基，NH- 环烷基，环烷基或四氢吡喃-4-基氧基，其中n> 1的取代基可以相同或不同; X是键，-CHR-， - CHRCHR' - ， - OCH 2 - ， - CH 2 OCHR - ， - CH 2 CH ，-SCH 2 - ， - S（O）2 CH 2 - ， - CH（CH 2）2 - ， - CH 2 2 - （CH 2）2 - ， - CH 2 N（R）CH 2 - ， - 环烷基-CH _{2 - 或SiRR'-CH 2 - ; R / R'可以彼此独立地是氢，被卤素取代的低级烷基或低级烷基; R 2是氢，苯基或低级烷基; Y是苯基，萘基，噻吩基，吡啶基，环烷基，1,2,3,4-四氢 - 萘-2-基，2,3-二氢苯并[1,4]二恶英-6-基或苯并[1,3] 二氧杂环戊烯-5-基; n为0,1,2或3; o是2或3; 或药学上合适的酸加成盐，用于制备用于治疗与微量胺相关受体的生物功能有关的疾病的药物，所述疾病是抑郁症，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，神经退行性疾病，阿尔茨海默氏病，癫痫，偏头痛，药物滥用和代谢紊乱，进食障碍，糖尿病，糖尿病并发症，肥胖，血脂异常，能量消耗和同化障碍，体温平衡，睡眠障碍和昼夜节律，以及心血管疾病。}

10. 发明申请

WO2008071574A1 NOVEL 2 -IMIDAZOLES AS LIGANDS FOR TRACE AMINE ASSOCIATED RECEPTORS (TAAR) 审中-公开
标题翻译：新型2 -IMIDAZOLES作为追踪胺相关受体（TAAR）的配体
公开(公告)号：WO2008071574A1
公开(公告)日：2008-06-19
申请号：PCT/EP2007/063153
申请日：2007-12-03
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： A61K31/4164 , C07D233/64 , C07D233/66 , A61P25/00
CPC分类号： C07D233/88 , C07D233/64
摘要： The present invention relates to compounds of formula (I) wherein X-R 1 is -CH 2 - and 2 Y-R is -CH(lower alkoxy)-, -CH(lower alkyl)-, -O-, -S-, -S(O)-, -S(O) 2 - or -CH 2 -; or X-R 1 is -NH- and Y-R 2 is - CH(lower alkyl)- or -CH 2 -; 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 or by lower alkyl substituted by halogen; 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）化合物，其中XR 1为-CH 2 - ，且2 YR为-CH（低级烷氧基） - ， - （低级烷基） - ， - O - ， - S - ， - S（O） - ， - S（O）2 - 或-CH 2 - 或X-R 1是-NH-，Y-R 2是-CH（低级烷基） - 或-CH 2 - 。 Ar是苯基或萘基，该环任选被一个或两个选自卤素，低级烷氧基，低级烷基或被卤素取代的低级烷基取代基取代; 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。

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