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    DIHYDROOXAZOL-2-AMINE DERIVATIVES
    56.
    发明申请
    DIHYDROOXAZOL-2-AMINE DERIVATIVES 审中-公开
    二氢异喹啉-2-胺衍生物

    公开(公告)号：WO2012059371A1

    公开(公告)日：2012-05-10

    申请号：PCT/EP2011/068705

    申请日：2011-10-26

    Applicant: F. HOFFMANN-LA ROCHE AG ,  NETTEKOVEN, Matthias ,  NORCROSS, Roger ,  POLARA, Alessandra

    Inventor： NETTEKOVEN, Matthias ,  NORCROSS, Roger ,  POLARA, Alessandra

    IPC: C07D263/16 ,  C07D413/12 ,  C07D413/14 ,  A61K31/506 ,  A61P25/00

    CPC classification number: C07D263/28 ,  C07D263/16 ,  C07D413/12 ,  C07D413/14

    Abstract: The invention relates to compounds of formula (I) wherein R 1 is hydrogen or lower alkyl; R 2 is hydrogen or is heteroaryl, optionally substituted by one or more halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, cyano, S-lower alkyl, S(O)-lower alkyl, S(O) 2 -lower alkyl, C(O)-lower alkyl or C 3-6 -cycloalkyl; R 3 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, cyano, S-lower alkyl, S(O)-lower alkyl, S(O) 2 -lower alkyl, C(O)-lower alkyl or C 3-6 -cycloalkyl; R 4 is hydrogen or lower alkyl; (A) is phenyl or pyridinyl, wherein the N-atom may be in different positions; X is a bond or CH(CF 3 )-; Ar is aryl or heteroaryl, optionally substituted by one or more R 3 ; or to a pharmaceutically suitable acid addition salt thereof. It has now 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是氢或是杂芳基，任选被一个或多个卤素取代的低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素取代的低级烷氧基，氰基，S-低级烷基，S（O） - 低级烷基，S（ O）2-低级烷基，C（O） - 低级烷基或C 3-6 - 环烷基; 氰基，S-低级烷基，S（O） - 低级烷基，S（O）2 - 低级烷基，C（O）2 - 低级烷基， O） - 低级烷基或C 3-6 - 环烷基; R4是氢或低级烷基; （A）是苯基或吡啶基，其中所述N-原子可以在不同的位置; X是键或CH（CF 3） - ; Ar是芳基或杂芳基，任选被一个或多个R 3取代; 或其药学上合适的酸加成盐。 现已发现，式I化合物对微量胺相关受体（TAAR）具有良好的亲和力，尤其对于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。

    (3 -METHYLPYRROLIDIN- 3 - YL) METHYL PYRIDINYL ETHER DERIVATIVES AND THEIR USE AS NK-3 RECEPTOR ANTAGONISTS
    58.
    发明申请
    (3 -METHYLPYRROLIDIN- 3 - YL) METHYL PYRIDINYL ETHER DERIVATIVES AND THEIR USE AS NK-3 RECEPTOR ANTAGONISTS 审中-公开
    （3-甲基吡咯烷-3-基）甲基吡啶基醚衍生物及其作为NK-3受体拮抗剂的用途

    公开(公告)号：WO2012004207A1

    公开(公告)日：2012-01-12

    申请号：PCT/EP2011/061168

    申请日：2011-07-04

    Applicant: F. HOFFMANN-LA ROCHE AG ,  NETTEKOVEN, Matthias ,  RATNI, Hasane ,  VIFIAN, Walter

    Inventor： NETTEKOVEN, Matthias ,  RATNI, Hasane ,  VIFIAN, Walter

    IPC: C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  A61K31/4439 ,  A61P25/00

    CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14

    Abstract: The invention relates to a compound of general formula : (I) wherein A is selected from the groups (a), (b) or (c): formula (II) or formula (III) (b) or is cycloalkyl, (c) optionally substituted by lower alkyl (c);Ar 1 is phenyl or a six membered heteroaryl;X 1 is N or CH; X 2 is N-R 1 or O; R 1 is S(O) 2 -lower alkyl, C(O)-cycloalkyl substituted by lower alkyl, or is C(O)-lower alkyl, lower alkyl, cyano, cycloalkyl or is a six membered heteroaryl substituted by lower alkyl, cyano, C(O)-lower alkyl, halogen, lower alkyl substituted by halogen or lower alkoxy; or is phenyl substituted by cyano or halogen; R 2 is lower alkyl, halogen, pyrazolyl, 3-methyl-[1,2,4]oxazolyl, 5-methyl-[1,2,4]oxadiazol-3-yl, pyridyl substituted by cyano, or is phenyl substituted by halogen, or is cyano, lower alkoxy, or is piperidin-2-one; or to pharmaceutically active salts, sterioisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula I as well as racemic and non-racemic mixtures thereof..It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinsons disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

    Abstract translation: 本发明涉及通式（I）的化合物，其中A选自（a），（b）或（c）：式（II）或式（III）（b）或环烷基，（c ），任选被（C）的低级烷基取代; Ar 1是苯基或6元杂芳基; X 1是N或CH; X2是N-R1或O; R 1是S（O）2-低级烷基，被低级烷基取代的C（O） - 环烷基，或是C（O） - 低级烷基，低级烷基，氰基，环烷基或是被低级烷基，氰基取代的六元杂芳基 ，C（O） - 低级烷基，卤素，被卤素或低级烷氧基取代的低级烷基; 或被氰基或卤素取代的苯基; R2是低级烷基，卤素，吡唑基，3-甲基 - [1,2,4]恶唑基，5-甲基 - [1,2,4]恶二唑-3-基，被氰基取代的吡啶基，或被卤素取代的苯基 或氰基，低级烷氧基或哌啶-2-酮; 或药学活性盐，异构异构体形式，包括式I化合物的单独的非对映异构体和对映异构体，以及外消旋和非外消旋混合物。已经发现，本发明化合物是高潜在的NK-3受体拮抗剂 抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的治疗。

    HSL INHIBITORS USEFUL IN THE TREATMENT OF DIABETES
    59.
    发明申请
    HSL INHIBITORS USEFUL IN THE TREATMENT OF DIABETES 审中-公开
    HSL抑制剂有助于治疗糖尿病

    公开(公告)号：WO2011029808A1

    公开(公告)日：2011-03-17

    申请号：PCT/EP2010/063078

    申请日：2010-09-07

    Applicant: F. HOFFMANN-LA ROCHE AG ,  ACKERMANN, Jean ,  CONTE, Aurelia ,  NEIDHART, Werner ,  NETTEKOVEN, Matthias ,  WERTHEIMER, Stanley

    Inventor： ACKERMANN, Jean ,  CONTE, Aurelia ,  NEIDHART, Werner ,  NETTEKOVEN, Matthias ,  WERTHEIMER, Stanley

    IPC: C07D211/62 ,  C07D211/96 ,  C07D401/12 ,  C07D405/12 ,  A61K31/445 ,  A61P3/00 ,  A61P9/10

    CPC classification number: C07D211/96 ,  C07D211/62 ,  C07D401/12 ,  C07D405/12

    Abstract: Compounds of formula (I), as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A 1 , A 2 , R 1 ,R 2 R 3 ,R 4 R 5 and R 6 have the significance given in claim 1. Objects of the present invention are the compounds of formula (I) and their aforementioned salts and esters and their use as therapeutically active substances, a process for the manufacture of the said compounds, intermediates, pharmaceutical compositions, medicaments containing the said compounds, their pharmaceutically acceptable salts or esters, the use of the said compounds, salts or esters for the treatment or prophylaxis of illnesses, especially in the treatment or prophylaxis of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis or obesity and the use of the said compounds, salts or esters for the production of medicaments for the treatment or prophylaxis of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis or obesity.

    Abstract translation: 式（I）化合物及其药学上可接受的盐可以以药物组合物的形式使用，其中A1，A2，R1，R2 R3，R4 R5和R6具有权利要求1中给出的含义。 发明是式（I）化合物及其上述盐和酯及其作为治疗活性物质的用途，制备所述化合物，中间体，药物组合物，含有所述化合物的药物，其药学上可接受的盐或酯的方法 ，所述化合物，盐或酯用于治疗或预防疾病，特别是用于治疗或预防糖尿病，代谢综合征，血脂异常，动脉粥样硬化或肥胖的用途，以及所述化合物，盐或酯在生产中的用途 用于治疗或预防糖尿病，代谢综合征，血脂异常，动脉粥样硬化或肥胖的药物。

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