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    AROYLAMINO - AND HETEROAROYLAMINO-SUBSTITUTED PIPERIDINES AS GLYT-1 INHIBITORS
    1.
    发明申请
    AROYLAMINO - AND HETEROAROYLAMINO-SUBSTITUTED PIPERIDINES AS GLYT-1 INHIBITORS 审中-公开
    作为GLYT-1抑制剂的α-亚氨基 - 和异丁烯酰胺取代的哌啶

    公开(公告)号：WO2010086251A1

    公开(公告)日：2010-08-05

    申请号：PCT/EP2010/050551

    申请日：2010-01-19

    Applicant: F. HOFFMANN-LA ROCHE AG ,  KOLCZEWSKI, Sabine ,  PINARD, Emmanuel ,  STALDER, Henri

    Inventor： KOLCZEWSKI, Sabine ,  PINARD, Emmanuel ,  STALDER, Henri

    IPC: C07D211/56 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D417/10 ,  A61K31/445 ,  A61K31/4525 ,  A61K31/4535 ,  A61K31/4545

    CPC classification number: C07D407/04 ,  A61K31/451 ,  C07D211/56 ,  C07D213/56 ,  C07D221/20 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D417/10

    Abstract: The present invention relates to a compound of general formula (I) wherein R 1 is hydrogen, lower alkyl, CD 3 , -(CH 2 ) n -CHO, -(CH 2 ) n -O-lower alkyl, -(CH 2 ) n -OH, -(CH 2 ) n -cycloalkyl or is heterocycloalkyl; R 2 is hydrogen, halogen, hydroxy, lower alkyl, di-lower alkyl, -OCH 2 -O-lower alkyl, or lower alkoxy; or the piperidin ring form together with R 2 a spiro ring, selected from 4-aza-spiro[2.5]oct-6-yl; Ar is aryl or heteroaryl, which are optionally substituted by one, two or three substituents, selected from halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cycloalkyl, lower alkoxy, S-lower alkyl, heteroaryl, heterocycloalkyl, or by phenyl optionally substituted by R', and R' is halogen, lower alkyl, lower alkoxy or lower alkoxy substituted by halogen, or is heteroaryl; R is lower alkyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, wherein aryl and heteroaryl are optionally substituted by one or two R'; n is 0, 1 2 or 3; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. Furthermore, the present invention relates to pharmaceutical compositions containing the compounds of formula I and to their use in the treatment of neurological and neuropsychiatric disorders.

    Abstract translation: 本发明涉及通式（I）的化合物，其中R1是氢，低级烷基，CD3， - （CH2）n-CHO， - （CH2）nO-低级烷基， - （CH2）n-OH， - （ CH2）n-环烷基或杂环烷基; R2是氢，卤素，羟基，低级烷基，二低级烷基，-OCH2-O-低级烷基或低级烷氧基; 或哌啶环与R2一起形成选自4-氮杂 - 螺[2.5]辛-6-基的螺环; Ar是芳基或杂芳基，其任选被一个，两个或三个选自卤素，低级烷基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，环烷基，低级烷氧基，S-低级烷基，杂芳基，杂环烷基 ，或被R'任意取代的苯基，R'是卤素，低级烷基，低级烷氧基或被卤素取代的低级烷氧基，或是杂芳基; R是低级烷基，环烷基，杂环烷基，芳基或杂芳基，其中芳基和杂芳基任选被一个或两个R'取代; n为0，1 2或3; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体。 此外，本发明涉及含有式I化合物的药物组合物及其在治疗神经和神经精神障碍中的用途。

    PYRIDINECARBOXAMIDE AND BENZAMIDE DERIVATIVES AS TAAR1 LIGANDS
    2.
    发明申请
    PYRIDINECARBOXAMIDE AND BENZAMIDE DERIVATIVES AS TAAR1 LIGANDS 审中-公开
    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

    Applicant: F. HOFFMANN-LA ROCHE AG ,  GALLEY, Guido ,  GROEBKE ZBINDEN, Katrin ,  NORCROSS, Roger ,  STALDER, Henri

    Inventor： GALLEY, Guido ,  GROEBKE ZBINDEN, Katrin ,  NORCROSS, Roger ,  STALDER, Henri

    IPC: C07C233/66 ,  C07D213/82 ,  C07D235/06 ,  C07D401/12 ,  C07D407/12 ,  A61K31/497 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/44 ,  A61K31/404 ,  A61P3/00

    CPC classification number: C07D213/80 ,  C07C233/66 ,  C07D213/82 ,  C07D235/08 ,  C07D401/12 ,  C07D405/12

    Abstract: 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.

    Abstract translation: 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 。

    SUBSTITUTED 4-IMIDAZOLES
    4.
    发明申请
    SUBSTITUTED 4-IMIDAZOLES 审中-公开
    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

    Applicant: HOFFMANN LA ROCHE ,  GALLEY GUIDO ,  GROEBKE ZBINDEN KATRIN ,  NORCROSS ROGER ,  STALDER HENRI

    Inventor： GALLEY GUIDO ,  GROEBKE ZBINDEN KATRIN ,  NORCROSS ROGER ,  STALDER HENRI

    IPC: C07D403/06 ,  A61K31/4178 ,  C07D401/06 ,  C07D413/06

    CPC classification number: C07D401/06 ,  C07D403/06 ,  C07D413/06

    Abstract: 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.

    Abstract translation: 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 。

    2-AZETIDINEMETHANEAMINES AND 2-PYRROLIDINEMETHANEAMINES AS TAAR-LIGANDS
    6.
    发明申请
    2-AZETIDINEMETHANEAMINES AND 2-PYRROLIDINEMETHANEAMINES AS TAAR-LIGANDS 审中-公开
    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

    Applicant: F. HOFFMANN-LA ROCHE AG ,  GALLEY, Guido ,  GOERGLER, Annick ,  GROEBKE ZBINDEN, Katrin ,  NORCROSS, Roger ,  STALDER, Henri

    Inventor： GALLEY, Guido ,  GOERGLER, Annick ,  GROEBKE ZBINDEN, Katrin ,  NORCROSS, Roger ,  STALDER, Henri

    IPC: C07D205/04 ,  C07D207/09 ,  A61K31/397 ,  A61K31/40 ,  A61P25/00

    CPC classification number: C07D205/04 ,  C07D207/09

    Abstract: 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.

    Abstract translation: 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 。

    4-IMIDAZOLINES AS TAAR'S LIGANDS
    7.
    发明申请
    4-IMIDAZOLINES AS TAAR'S LIGANDS 审中-公开
    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

    Applicant: HOFFMANN LA ROCHE ,  GALLEY GUIDO ,  GROEBKE ZBINDEN KATRIN ,  NORCROSS ROGER ,  STALDER HENRI

    Inventor： GALLEY GUIDO ,  GROEBKE ZBINDEN KATRIN ,  NORCROSS ROGER ,  STALDER HENRI

    IPC: C07D233/64 ,  A61K31/415 ,  A61P9/00 ,  A61P25/00

    CPC classification number: C07D233/64

    Abstract: 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.

    Abstract translation: 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

    NOVEL 2-AMINOOXAZOLINES AS TAAR1 LIGANDS FOR CNS DISORDERS
    8.
    发明申请
    NOVEL 2-AMINOOXAZOLINES AS TAAR1 LIGANDS FOR CNS DISORDERS 审中-公开
    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

    Applicant: F. HOFFMANN-LA ROCHE AG ,  GALLEY, Guido ,  GROEBKE ZBINDEN, Katrin ,  NORCROSS, Roger ,  STALDER, Henri

    Inventor： GALLEY, Guido ,  GROEBKE ZBINDEN, Katrin ,  NORCROSS, Roger ,  STALDER, Henri

    IPC: C07D263/28 ,  C07D413/04 ,  A61K31/421 ,  A61K31/422 ,  A61P25/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10

    CPC classification number: C07D263/28 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07F7/0812

    Abstract: 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.

    Abstract translation: 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。

    NOVEL 2 -IMIDAZOLES AS LIGANDS FOR TRACE AMINE ASSOCIATED RECEPTORS (TAAR)
    9.
    发明申请
    NOVEL 2 -IMIDAZOLES AS LIGANDS FOR TRACE AMINE ASSOCIATED RECEPTORS (TAAR) 审中-公开
    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

    Applicant: F. HOFFMANN-LA ROCHE AG ,  GALLEY, Guido ,  GROEBKE ZBINDEN, Katrin ,  NORCROSS, Roger ,  STALDER, Henri

    Inventor： GALLEY, Guido ,  GROEBKE ZBINDEN, Katrin ,  NORCROSS, Roger ,  STALDER, Henri

    IPC: A61K31/4164 ,  C07D233/64 ,  C07D233/66 ,  A61P25/00

    CPC classification number: C07D233/88 ,  C07D233/64

    Abstract: 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.

    Abstract translation: 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 。

    SUBSTITUTED 2-IMIDAZOLES AS MODULATORS OF THE TRACE AMINE ASSOCIATED RECEPTORS
    10.
    发明申请
    SUBSTITUTED 2-IMIDAZOLES AS MODULATORS OF THE TRACE AMINE ASSOCIATED RECEPTORS 审中-公开
    作为跟踪胺相关受体的调节剂的替代的2-IMIDAZOLES

    公开(公告)号：WO2008052907A1

    公开(公告)日：2008-05-08

    申请号：PCT/EP2007/061334

    申请日：2007-10-23

    Applicant: F. HOFFMANN-LA ROCHE AG ,  GALLEY, Guido ,  GROEBKE ZBINDEN, Katrin ,  NORCROSS, Roger ,  STALDER, Henri

    Inventor： GALLEY, Guido ,  GROEBKE ZBINDEN, Katrin ,  NORCROSS, Roger ,  STALDER, Henri

    IPC: C07D401/06 ,  C07D403/06 ,  C07D413/06 ,  A61P25/00 ,  A61K31/4178 ,  A61K31/4709 ,  A61K31/538

    CPC classification number: C07D413/06 ,  C07D401/06 ,  C07D403/06

    Abstract: The present invention relates to a compound 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 is hydrogen or lower alkyl and in case when n is 2, R may be the same or not; X is -CH 2 -, -CH- or -O-; Y is -CH 2 -, -CH- or a bond; when X is -O-, Y may not be a bond; Z is -CH 2 - or -CH-; m is 0, 1 or 2; when m is 2, R 2 may be the same or not; n is 0, 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.

    Abstract translation: 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为氢或低级烷基，n为2的情况下，R可相同或不相同; X是-CH 2 - ， - CH-或-O-; Y是-CH 2 - ， - CH-或键; 当X是-O-时，Y可能不是键; Z是-CH 2 - 或-CH-; m为0,1或2; 当m为2时，R 2可以相同或不相同; n为0,1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。 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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