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1. 发明申请

WO2012168175A1 [1,3]OXAZINES 审中-公开
标题翻译： [1,3]恶嗪
公开(公告)号：WO2012168175A1
公开(公告)日：2012-12-13
申请号：PCT/EP2012/060476
申请日：2012-06-04
申请人： F. HOFFMANN-LA ROCHE AG , BORRONI, Edilio , GOBBI, Luca , HILPERT, Hans , HONER, Michael , MURI, Dieter , NARQUIZIAN, Robert , POLARA, Alessandra
发明人： BORRONI, Edilio , GOBBI, Luca , HILPERT, Hans , HONER, Michael , MURI, Dieter , NARQUIZIAN, Robert , POLARA, Alessandra
IPC分类号： C07D413/12 , A61K31/5355 , A61P25/28
CPC分类号： C07D413/12
摘要： The present invention provides compounds of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes. The invention further provides a radio-labelled derivative thereof.
摘要翻译：本发明提供具有BACE1和/或BACE2抑制活性的式（I）化合物，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默病和2型糖尿病。本发明还提供其放射性标记的衍生物。

2. 发明申请

WO2012156284A1 1,3-OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS 审中-公开
标题翻译：作为BACE1和/或BACE2抑制剂的1,3-氧化物
公开(公告)号：WO2012156284A1
公开(公告)日：2012-11-22
申请号：PCT/EP2012/058707
申请日：2012-05-11
申请人： F. HOFFMANN-LA ROCHE AG , SIENA BIOTECH S.P.A , HILPERT, Hans , NARQUIZIAN, Robert , PINARD, Emmanuel , POLARA, Alessandra , ROGERS-EVANS, Mark , WOLTERING, Thomas , WOSTL, Wolfgang
发明人： HILPERT, Hans , NARQUIZIAN, Robert , PINARD, Emmanuel , POLARA, Alessandra , ROGERS-EVANS, Mark , WOLTERING, Thomas , WOSTL, Wolfgang
IPC分类号： C07D265/08 , C07D413/10 , C07D413/12 , A61K31/5355 , A61K31/535 , A61P25/28
CPC分类号： C07D413/10 , C07D265/08 , C07D413/12
摘要： The present invention provides compounds of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译：本发明提供具有BACE1和/或BACE2抑制活性的式I化合物，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默病和2型糖尿病。

3. 发明申请

WO2012059371A1 DIHYDROOXAZOL-2-AMINE DERIVATIVES 审中-公开
标题翻译：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
申请人： F. HOFFMANN-LA ROCHE AG , NETTEKOVEN, Matthias , NORCROSS, Roger , POLARA, Alessandra
发明人： NETTEKOVEN, Matthias , NORCROSS, Roger , POLARA, Alessandra
IPC分类号： C07D263/16 , C07D413/12 , C07D413/14 , A61K31/506 , A61P25/00
CPC分类号： C07D263/28 , C07D263/16 , C07D413/12 , C07D413/14
摘要： 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.
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。

4. 发明申请

WO2011057973A1 OXAZOLINE DERIVATIVES FOR TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：用于治疗CNS病症的OXAZOLINE衍生物
公开(公告)号：WO2011057973A1
公开(公告)日：2011-05-19
申请号：PCT/EP2010/066960
申请日：2010-11-08
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , NORCROSS, Roger , POLARA, Alessandra
发明人： GALLEY, Guido , NORCROSS, Roger , POLARA, Alessandra
IPC分类号： C07D263/28 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , A61K31/421 , A61K31/4439 , A61K31/506 , A61K31/422 , A61P25/00
CPC分类号： C07D263/28 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The invention relates to compounds of formula (I) wherein the definitions of X, R and R 1 are provided in claim 1. It has now been found that the compounds of formula (I) have a good affinity to the trace amine associated receptors (TAARs), especially for TAARl. 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X，R和R 1的定义在权利要求1中提供。现已发现式（I）化合物与微量胺相关受体（TAARs）具有良好的亲和力），特别是TAARl。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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