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    2-AZETIDINEMETHANEAMINES AND 2-PYRROLIDINEMETHANEAMINES AS TAAR-LIGANDS
    3.
    发明公开
    2-AZETIDINEMETHANEAMINES AND 2-PYRROLIDINEMETHANEAMINES AS TAAR-LIGANDS 审中-公开
    2-氮杂萘甲酰胺和2-吡咯烷甲基乙胺作为塔配体

    公开(公告)号：EP2183216A1

    公开(公告)日：2010-05-12

    申请号：EP08775206.9

    申请日：2008-07-18

    申请人： F. Hoffmann-La Roche AG

    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 R1 is hydrogen, lower alkyl or benzyl which may be optionally substituted by halogen or lower alkoxy; R2 is hydrogen, halogen or OR, wherein R is lower alkyl, aryl or lower alkyl substituted by halogen; R3 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）的化合物，其中R 1为氢，低级烷基或苄基，其可以任选被卤素或低级烷氧基取代; 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是0或1; o是0,1或2; 和它们的药学活性盐。 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 。

    AMINOMETHYL-4-IMIDAZOLES
    4.
    发明公开
    AMINOMETHYL-4-IMIDAZOLES 有权
    氨基甲基-4-咪唑类

    公开(公告)号：EP2076497A1

    公开(公告)日：2009-07-08

    申请号：EP07821039.0

    申请日：2007-10-09

    申请人： F. Hoffmann-La Roche AG

    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 R1 is hydrogen, lower alkyl, -(CR2)n-OH, -(CH2)n-aryl or -(CH2)n-heteroaryl, which are optionally substituted by halogen, lower alkoxy or lower alkyl substituted by halogen, or is -(CR2)n- cycloalkyl, optionally substituted by hydroxy, -(CH2)n-heterocyclyl, -(CH2)n-NH-S(O)2CH3, or is -(CR2)nO-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; R2 is 2,2-dioxo-2,3-dihydro-1H-benzo[c]thiophenyl, 6,7-dihydro-5H-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, -(CH2)n-hydroxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, -S(O)2-lower alkyl, -(CH2)n-S(O)2-NH-lower alkyl, -(CH2)n-O-lower alkyl, nitro, amino, cyano, -NHC(O)-lower alkyl, -C(O)NH-lower alkyl, or O-tetrahydro-naphthalenyl, or are substituted by -(CH2)n-aryl, optionally substituted by halogen, or by -CH=CH-aryl, optionally substituted by halogen, or by -(CH2)n-O-aryl, optionally substituted by halogen, lower alkoxy or lower alkyl substituted by halogen, or by -O-(CH2)n-aryl, optionally substituted by halogen, or by -(CH2)n-heteroaryl, or by -(CH2)n-O-heteroaryl or by -(CH2)n-heterocyclyl, optionally substituted by =O, or by -(CH2)n-O-heterocyclyl, optionally substituted by lower alkyl, or by -S-aryl, -CH(OH)-aryl, -C(CH3)2-aryl, -NR-aryl, or by 2-oxo-2H-pyridin-1-yl; R3 is hydrogen or lower alkyl; R4 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.

    AROYLAMINO - AND HETEROAROYLAMINO-SUBSTITUTED PIPERIDINES AS GLYT-1 INHIBITORS
    7.
    发明公开
    AROYLAMINO - AND HETEROAROYLAMINO-SUBSTITUTED PIPERIDINES AS GLYT-1 INHIBITORS 有权
    酰氨和杂芳酰基取代的哌啶GLYT AS-1抑制剂

    公开(公告)号：EP2391603A1

    公开(公告)日：2011-12-07

    申请号：EP10700563.9

    申请日：2010-01-19

    申请人： F. Hoffmann-La Roche AG

    发明人： KOLCZEWSKI, Sabine ,  PINARD, Emmanuel ,  STALDER, Henri

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

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

    摘要： 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.

    NOVEL 2-AMINOOXAZOLINES AS TAAR1 LIGANDS FOR CNS DISORDERS
    8.
    发明公开
    NOVEL 2-AMINOOXAZOLINES AS TAAR1 LIGANDS FOR CNS DISORDERS 有权
    2- AMINOOXAZOLINVERBINDUNGEN ALS TAAR1配体，中央神经系统疾病

    公开(公告)号：EP2114906A1

    公开(公告)日：2009-11-11

    申请号：EP08701646.5

    申请日：2008-01-23

    申请人： F. Hoffmann-La Roche AG

    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 R1 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)CH2 -, -cycloalkyl-CH 2 - or SiRR'-CH 2 -; R/R' may be independently from each other hydrogen, lower alkyl or lower alkyl substituted by halogen; R2 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.