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公开(公告)号:EP2709992A1
公开(公告)日:2014-03-26
申请号:EP12722112.5
申请日:2012-05-11
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: 本发明提供了具有BACE1和/或BACE2抑制活性的式I化合物,它们的制造方法,含有它们的药物组合物以及它们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。
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公开(公告)号:EP2718287A1
公开(公告)日:2014-04-16
申请号:EP12725747.5
申请日:2012-06-04
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.
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公开(公告)号:EP2635560A1
公开(公告)日:2013-09-11
申请号:EP11776154.4
申请日:2011-10-26
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.-
公开(公告)号:EP2635560B1
公开(公告)日:2015-09-30
申请号:EP11776154.4
申请日:2011-10-26
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
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公开(公告)号:EP2499121B1
公开(公告)日:2015-10-07
申请号:EP10779293.9
申请日:2010-11-08
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
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公开(公告)号:EP2499121A1
公开(公告)日:2012-09-19
申请号:EP10779293.9
申请日:2010-11-08
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.
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