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1. 发明申请

WO9616046A2 NOVEL BENZYL PYRIMIDINES 审中-公开
标题翻译：新颖的苄基吡啶
公开(公告)号：WO9616046A2
公开(公告)日：1996-05-30
申请号：PCT/EP9504451
申请日：1995-11-13
申请人： HOFFMANN LA ROCHE , GUERRY PHILIPPE , JOLIDON SYNESE , MASCIADRI RAFFAELLO , STALDER HENRI , THEN RUDOLF
发明人： GUERRY PHILIPPE , JOLIDON SYNESE , MASCIADRI RAFFAELLO , STALDER HENRI , THEN RUDOLF
IPC分类号： A61K31/505 , A61K31/506 , A61K31/53 , A61K31/535 , A61K31/675 , A61K31/695 , A61P31/04 , C07C255/37 , C07D215/56 , C07D239/48 , C07D239/49 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/10 , C07D413/10 , C07D417/10 , C07D471/04 , C07F7/10 , C07F7/18 , C07F9/6512
CPC分类号： C07D239/49 , C07D401/10 , C07D403/10 , C07D405/10 , C07D405/14 , C07D471/04 , C07F7/1856 , C07F9/65122
摘要： Substituted 5-benzyl-2,4-diaminopyrimidines of general formula (I) in which R represents lower alkoxy, R represents bromine or lower alkoxy and R represents aryl, heteroaryl or a group -Q-R , wherein Q signifies ethylene, vinylene or ethynylene and R signifies aryl, heteroaryl, lower alkoxy-carbonyl or carbamoyl, as well as readily hydrolyzable esters of carboxylic acids of formula I and pharmaceutically acceptable salts of these compounds can be used in the control or prevention of infectious diseases.
摘要翻译：取代的通式（I）的5-苄基-2,4-二氨基嘧啶，其中R 1表示低级烷氧基，R 2表示溴或低级烷氧基，R 3表示芳基，杂芳基或基团-QR 30>，其中Q表示乙烯，亚乙烯基或亚乙炔基，R 30表示芳基，杂芳基，低级烷氧基 - 羰基或氨基甲酰基，以及式I的羧酸的易水解的酯和这些化合物的药学上可接受的盐在控制或预防传染病方面。

2. 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

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

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。

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

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。

7. 发明申请

WO2007090720A3 USE OF 2-IMIDAZOLES FOR THE TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：使用2-咪唑烷治疗CNS病症
公开(公告)号：WO2007090720A3
公开(公告)日：2007-09-20
申请号：PCT/EP2007050445
申请日：2007-01-17
申请人： HOFFMANN LA ROCHE , HOENER MARIUS , KOLCZEWSKI SABINE , STALDER HENRI
发明人： HOENER MARIUS , KOLCZEWSKI SABINE , STALDER HENRI
IPC分类号： A61K31/4164 , A61K31/4168 , A61K31/4174 , A61P25/00
CPC分类号： A61K31/4164 , A61K31/4168 , A61K31/4174
摘要： The present invention relates to the use of compounds of formula ( I ), wherein R is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, lower alkyl substituted by halogen, or is 4-(CH 2 ) 2 C(O)-naphthyl; X is -S- or -NH-; aryl is an aromatic group, selected from phenyl, naphthalen-1-yl, naphthalen- 2-yl or 5,6,7,8-tetrahydronaphthalen-1-yl, ; hetaryl is an aromatic group, containing at least one N or S ring atom, selected from the group consisting of thiophen-3-yl or pyrimidin-5-yl; n is 1, 2 or 3; 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 (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）化合物的用途，其中R是氢，羟基，低级烷基，低级烷氧基，卤素，被卤素取代的低级烷基，或是4-（CH 2 CH 2））_{2 C（O） - 萘基; X是-S-或-NH-; 芳基是选自苯基，萘-1-基，萘-2-基或5,6,7,8-四氢萘-1-基的芳基; 杂芳基是含有至少一个选自噻吩-3-基或嘧啶-5-基的N或S环原子的芳族基团; n为1,2或3; 以及它们的药物活性盐，外消旋混合物，对映异构体，旋光异构体和互变异构体形式，用于制备用于治疗抑郁症，焦虑症，双相情感障碍，注意缺陷多动障碍（ADHD），应激相关疾病，精神病性障碍精神分裂症，神经性疾病如帕金森病，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，睡眠障碍和昼夜节律紊乱以及心血管疾病。}

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. 发明申请

WO0248124A2 PIPERAZINE DERIVATIVES 审中-公开
标题翻译：哌嗪衍生物
公开(公告)号：WO0248124A2
公开(公告)日：2002-06-20
申请号：PCT/EP0114343
申请日：2001-12-06
申请人： HOFFMANN LA ROCHE , VERNALIS RES LTD
发明人： ADAMS DAVID REGINALD , BENTLEY JONATHAN MARK , DAVIDSON JAMES EDWARD PAUL , DAWSON CLAIRE ELIZABETH , GEORGE ASHLEY ROGER , MANSELL HOWARD LANGHAM , MATTEI PATRIZIO , MIZRAHI JACQUES , NETTEKOVEN MATTHIAS HEINRICH , PRATT ROBERT MARK , ROFFEY JONATHAN RICHARD ANTHON , ROEVER STEPHAN , SPECKLIN JEAN-LUC , STALDER HENRI , WILKINSON KERRY
IPC分类号： C07D295/20 , A61K31/365 , A61K31/495 , A61K31/496 , A61P1/04 , A61P1/14 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/02 , A61P15/00 , A61P15/10 , A61P17/02 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P43/00 , C07D207/32 , C07D207/325 , C07D213/30 , C07D213/64 , C07D213/643 , C07D233/86 , C07D241/04 , C07D261/08 , C07D277/24 , C07D285/14 , C07D295/205 , C07D295/21 , C07D307/12 , C07D307/42 , C07D333/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12
CPC分类号： C07D207/325 , C07D213/30 , C07D213/64 , C07D213/643 , C07D261/08 , C07D277/24 , C07D285/14 , C07D295/205 , C07D295/21 , C07D307/12 , C07D307/42 , C07D333/16 , C07D413/04
摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R to 4 , A , A m and n have the significance given in claim 1. They can be used in the form of pharmaceutically preparations for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.
摘要翻译：本发明涉及式（I）化合物及其可药用的盐，溶剂合物和酯，其中R 1至4 4，A 1，A 2 m和n具有重要性它们可以以用于治疗或预防中枢神经系统疾病，心血管疾病，胃肠道疾病，糖尿病，肥胖症和睡眠呼吸暂停的药学制剂的形式使用。

10. 发明专利

BRPI1007410A2 piperidinas aroilamino- e heteroaroilamino-substituídas como inibidores de glyt-1 未知
公开(公告)号：BRPI1007410A2
公开(公告)日：2016-02-16
申请号：BRPI1007410
申请日：2010-01-19
申请人： HOFFMANN LA ROCHE
发明人： PINARD EMMANUEL , STALDER HENRI , KOLCZEWSKI SABINE
IPC分类号： A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/4545 , C07D211/56 , C07D401/04 , C07D401/12 , C07D405/04 , C07D417/10

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