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ARYLOXY-AND HETEROARYLOXY-SUBSTITUTED TETRAHYDROBENZAZEPINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN
专利权人:
ALBANY MOLECULAR RESEARCH; INC.
发明人:
LIU, SHUANG,YANG, YUH-LIN, ALLEN,SAMBANDAM, ARUNA,MOLINO, BRUCE, F,OLSON, RICHARD, E
申请号:
NZ58080208
公开号:
NZ580802A
申请日:
2008.05.08
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed are 5-aryl-2,3,4,5-tetrahydro-lH-benzo[c]azepine derivatives as represented by the general formula I(A-E), wherein: X represents a phenyl, pyridyl, naphthyl or quinolinyl group optionally substituted with one or two R14 substituents R1 is hydrogen or alkyl R2, R3, R5, R6, R7, R8, R9, R10 and R11 are each H R4 is H, halogen, alkyl, piperazinyl, phenyl, pyridyl, 2-oxo-pyridin-1-yl, pyrimidinyl, pyridazinyl, 6-oxopyridazin-1-yl, pyrazinyl, pyrazolyl, [1,2,4]triazolo[4,3-a]pyridinyl, [1,2,4]triazolo[1,5-a]pyridinyl, or 3-oxo-[1,2,4]triazolo[4,3-a]pyridin-2-yl, optionally substituted R14 R12 is alkyl, optionally substituted with 1 to 3 R15 substituents R13 is selected from the group consisting of NR10R11 and alkyl R14 is independently selected at each occurrence from a substituent in the group consisting of halogen, OR12, NR10R11, S(O)2R13, CN, C(O)R13 and alkyl each optionally substituted with 1 to 3 halogen atoms or a pharmaceutically acceptable salt thereof. Representative compounds include 8-bromo-2-methyl-5-phenoxy-2,3,4,5-tetrahydro-1H-benzo[c]azepine, 2-methyl-5-phenoxy-8-(pyridazin-3-yl)-2,3,4,5-tetrahydro-lH-benzo[c]azepine, 5-(2-fluorophenoxy)-2-methyl-8-(pyrimidin-5-yl)-2,3,4,5-tetrahydro-1H-benzo[c]azepine, 2-methyl-5-(4-(trifluoromethyl)phenoxy)-2,3,4,5-tetrahydro-1H-benzo[c]azepine and 8-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(4-fluorophenoxy)-2-methyl-2,3,4,5-tetrahydro-1H-benzo[c]azepine. Further disclosed is a pharmaceutical composition which comprises a pharmaceutically acceptable carrier and a therapeutically effective amount of the compound as defined above, for treating a disorder selected from pain, attention deficit hyperactivity disorder (ADHD), cognition impairment, anxiety disorders, panic disorder, bipolar disorder, manic depression, obsessive compulsive disorder (OCD), posttraumatic stress disorder (PTSD), acute stress disorder, social phobia, simple phobias, pre-menstrual dysphoric disorder (PMDD), social anxiety disorder (SAD), maj
来源网站:
中国工程科技知识中心
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