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公开(公告)号：EP2925292A1
公开(公告)日：2015-10-07
申请号：EP13782683.0
申请日：2013-10-21
IPC分类号： A61K9/00 , A61K31/00 , A61K31/444 , A61K31/519 , A61P25/00 , A61P25/28
CPC分类号： A61K31/519 , A61K9/0019 , A61K9/0031 , A61K9/0095 , A61K9/02 , A61K9/1652 , A61K9/2018 , A61K9/2054 , A61K9/4825 , A61K9/4858 , A61K9/4866 , A61K31/00 , A61K31/444 , A61K47/10 , A61K2121/00 , C07D401/04 , C07D487/04
摘要： This invention relates to a new medical use for certain chemical compounds and pharmaceutical compositions containing them. The invention relates to compounds which are mGlu2/3 negative allosteric modulators for use in the treatment of Autistic Spectrum Disorder (ASD), in particular, autism. In another aspect, the invention relates to a pharmaceutical composition for use in the treatment of ASD comprising a compound according to the invention and a pharmaceutically acceptable carrier.
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22.发明公开N-(3-(2-AMINO-6,6-DIFLUORO-4,4A,5,6,7,7A-HEXAHYDRO-CYCLOPENTA[E][1,3]OXAZIN-4-YL)-PHENYL)-AMIDES AS BACE1 INHIBITORS 审中-公开N-（3-（2-氨基-6-六氟-4,4A，5,6,7,7a-十六氢 - 环戊二烯并[E] [1,3]氧杂-4-基） - 苯基） - 胺 ALS BACE1-INHIBITOREN
公开(公告)号：EP2758393A1
公开(公告)日：2014-07-30
申请号：EP12759458.8
申请日：2012-09-18
IPC分类号： C07D413/12 , A61K31/536 , A61P25/28
CPC分类号： C07D413/12
摘要： The present invention provides N-(3-(2-amino-6,6-difluoro-4,4a,5,6,7,7a-hexahydro- cyclopenta[e][1,3]oxazin-4-yl)-phenyl)-amides of formula (I), having BACE1 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.
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公开(公告)号：EP2807155B1
公开(公告)日：2017-04-12
申请号：EP13701072.4
申请日：2013-01-23
发明人： HILPERT, Hans , HUMM, Roland , WOLTERING, Thomas
IPC分类号： C07D401/12 , C07D403/12 , C07D413/12 , A61K31/535 , A61K31/5355
CPC分类号： C07D413/12 , C07D401/12 , C07D403/12
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公开(公告)号：EP2855469A1
公开(公告)日：2015-04-08
申请号：EP13725321.7
申请日：2013-05-21
发明人： HILPERT, Hans , WOLTERING, Thomas
IPC分类号： C07D417/12 , A61K31/541 , A61P25/28
CPC分类号： C07D417/12
摘要： The present invention provides a compound of formula I having BACE1 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.
摘要翻译： 本发明提供具有BACE1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。 阿尔茨海默氏病。
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公开(公告)号：EP2099763A1
公开(公告)日：2009-09-16
申请号：EP07847380.8
申请日：2007-11-27
IPC分类号： C07D215/38 , C07D215/20 , C07D401/12 , C07D409/12 , C07D405/12 , C07D405/14 , C07D403/12 , C07D413/12 , A61K31/47 , A61K31/4709 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/16 , A61P25/30
CPC分类号： C07D215/38 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12
摘要： The present invention relates to 2-Aminoquinoline derivatives which are represented by the general formula (I) wherein R1, R2 and X are as defined in the specification as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. Compounds of general formula I are useful in the prevention and/or treatment of anxiety depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, withdrawal from abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
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公开(公告)号：EP2076495A1
公开(公告)日：2009-07-08
申请号：EP07803542.5
申请日：2007-09-18
IPC分类号： C07D215/38 , C07D401/12 , C07D403/12 , C07D405/14 , A61K31/4725
CPC分类号： C07D215/38 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12
摘要： Compounds of the formula ( I) or pharmaceutically acceptable salts thereof, wherein X is a bond, -CH2CH2-, -CH=CH-, -CH2O-, -CH2NR-, -CH2S(O) -, CH2S(O)-, -O-,OCH2CH2S(O)2-, -CH2NRCO-, -CH2NRCH2-, (a), (b), (c), -NRS(O) 2NR-,-NHCHR-, or -NRS(O)2-; and wherein X can be inserted in both directions into formula (I); Y is a bond, -CHR- or -OCH2CH2-; R is hydrogen or lower alkyl; Ar1/Ar2 are independently from each other aryl or 5 to 10 membered heteroaryl, optionally substituted by lower alkyl, lower alkoxy, lower haloalkoxy, halogen, -CF3, -CH2OH, -CH2O-lower alkyl, 3 to 10 membered cycloalkyl, 5 to 10 membered heterocycloalkyl, -CH2O(CH2)2O-lower alkyl, -S(O)2-lower alkyl or -S(O)2NHR.
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