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标题翻译：替代物1,6-萘啶

公开(公告)号：EP2922540A1

公开(公告)日：2015-09-30

申请号：EP13795705.6

申请日：2013-11-18

申请人： F.Hoffmann-La Roche AG

发明人： CECCARELLI, Simona, M. , JAGASIA, Ravi , JAKOB-ROETNE, Roland , MARTIN, Rainer, E. , PETERS, Jens-Uwe , WICHMANN, Juergen

IPC分类号： A61K31/4375 , A61P25/24 , A61P25/28 , A61P25/30

CPC分类号： C07D471/04 , A61K31/4375 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541

摘要： The present invention relates to the use of compounds of general formula wherein R′ is hydrogen or lower alkyl; R1 is halogen, lower alkyl, cycloalkyl or cyano; or is phenyl, optionally substituted by one to three substituents, selected from lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, halogen, cyano, hydroxy, C(O)—NH-lower alkyl, CH2—C(O)—NH-lower alkyl, CH2—NH—C(O)-lower alkyl, CH2NH2, S(O)2CH3, S(O)2N(CH3)2, or by heterocycloalkyl groups; or is pyrazol-1, 4 or 5-yl, optionally substituted by lower alkyl; or is thiazol-5-yl, optionally substituted by one or two lower alkyl groups; or is pyridine 2, 3 or 4-yl, optionally substituted by lower alkyl, lower alkoxy, halogen or N(CH3)2; or is 3,6-dihydro-2H-pyran; or is benzo[d][1,3]dioxol-5-yl; or is 2,3-dihydrobenzo[b][1,4]dioxin-6-yl; R2 is hydrogen, lower alkyl or lower alkyl substituted by alkoxy; R3 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, NH—S(O)2—CH3, —(CH2)m—O-lower alkyl or —(CH2)n—S(O)2—CH3; or is —(CR2)n-phenyl, optionally substituted by —S(O)2CH3 or lower alkoxy; or is —(CH2)n-heterocycloalkyl, optionally substituted by lower alkyl and ═O; or is —(CH2)n-heteroaryl, optionally substituted by one or two lower alkyl groups; or is —(CH2)n-cycloalkyl, optionally substituted by cyano; or R2 and R3 form together with the N atom to which they are attached a heterocyclic ring, selected from morpholine, piperidine, 1,1-dioxo-thiomorpholine or piperazine which may be substituted by lower alkyl or C(O)O-lower alkyl, or may form a pyrrolidine ring, optionally substituted by hydroxy; R is independently from n hydrogen or lower alkyl; n is 0, 1, 2, 3; m is 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof, for the treatment of schizophrenia, obsessive-compulsive personality disorder, depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction (“chemobrain”), Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, and disturbances due to radiation therapy, chronic stress, optic neuropathy or macular degeneration, or abuse of neuro-active drugs selected from alcohol, opiates, methamphetamine, phencyclidine or cocaine.

摘要翻译：本发明涉及通式化合物的用途，其中R'是氢或低级烷基; R1是卤素，低级烷基，环烷基或氰基; 或者为被卤素取代的低级烷基，被低级烷氧基取代的低级烷氧基，卤素，氰基，氰基，羟基，C（O）-NH-低级烷基，CH 2 - C（O）-NH-低级烷基，CH 2 -NH-C（O） - 低级烷基，CH 2 NH 2，S（O）2 CH 3，S（O）2 N（CH 3）2或杂环烷基; 或是任选被低级烷基取代的吡唑-1,4或5-基; 或是任选被一个或两个低级烷基取代的噻唑-5-基; 或任选被低级烷基，低级烷氧基，卤素或N（CH 3）2取代的吡啶2,3或4-基; 或是3,6-二氢-2H-吡喃; 或者是苯并[d] [1,3]二氧杂环戊烯-5-基; 或是2,3-二氢苯并[b] [1,4]二恶英-6-基; R2是氢，被烷氧基取代的低级烷基或低级烷基; R 3是氢，低级烷基，被卤素取代的低级烷基，被羟基取代的低级烷基，NH-S（O）2 -CH 3， - （CH 2）m -O-低级烷基或 - （CH 2）n -S（O） 2-CH 3; 或是 - （CR 2）n - 苯基，任选被-S（O）2 CH 3或低级烷氧基取代; 或是 - （CH 2）n - 杂环烷基，任选地被低级烷基取代和= = O; 或是 - （CH 2）n - 杂芳基，任选被一个或两个低级烷基取代; 或为 - （CH 2）n - 环烷基，任选被氰基取代; 或R 2和R 3与它们所连接的N原子一起形成杂环，该杂环选自吗啉，哌啶，1,1-二氧代硫代吗啉或哌嗪，其可被低级烷基或C（O）O-低级烷基取代，或可形成任选被羟基取代的吡咯烷环; R独立地为氢或低级烷基; n为0,1,2,3; m为2; 或其药学上可接受的酸加成盐与外消旋混合物或其相应的对映体和/或光学异构体反应，用于治疗精神分裂症，强迫症人格障碍，抑郁症，双相性精神障碍，焦虑症，正常老化，癫痫，视网膜变性，创伤性脑损伤，脊髓损伤，创伤后应激障碍，惊恐障碍，帕金森病，痴呆，阿尔茨海默病，轻度认知障碍，化疗诱发的认知功能障碍（“chemobrain”），唐氏综合征，自闭症谱系障碍，听力损失，耳鸣，脊髓小脑性共济失调，肌萎缩性侧索硬化，多发性硬化，亨廷顿舞蹈病，中风以及由于放射治疗引起的干扰，慢性应激，视神经病变或黄斑变性，或滥用选自酒精，阿片剂，甲基苯丙胺的神经活性药物，苯环利定或可卡因。

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