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1. 发明授权

US5247080A Substituted benzazepines useful as intermediates for producing pharmaceutically active compounds 失效
标题翻译：取代苯并吖庚因可用作生产药物活性化合物的中间体
公开(公告)号：US5247080A
公开(公告)日：1993-09-21
申请号：US646574
申请日：1991-02-21
申请人： Joel G. Berger , Wei K. Chang , Marjorie Peters
发明人： Joel G. Berger , Wei K. Chang , Marjorie Peters
IPC分类号： C07D223/16 , C07D223/32 , C07D401/04 , C07D403/04 , C07D521/00
CPC分类号： C07D223/16 , C07D223/32 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D403/04
摘要： Disclosed herein are novel compounds of formula II ##STR1## and pharmaceutically acceptable salts thereof, wherein: Q represents H, halo or --OSO.sub.2 R" wherein R" is CH.sub.3, CF.sub.3, phenyl or tolyl;R.sup.3a represents H, alkyl, allyl, cyclopropylmethyl or COOR.sup.14 wherein R.sup.14 is alkyl, aryl, aralkyl or haloalkyl;R.sup.4 represents H, halo, alkyl, haloalkyl or alkoxy;R.sup.5a represents --OR.sup.10, --N(R.sup.9).sub.2, --O--C(R.sup.7).sub.2 .multidot.OCOR.sup.13, or alkoxy; wherein each R.sup.9 independently represents H, alkyl, alkoxy, alkoxyalkyl, aralkyl or aryl;R.sup.10 represents H, --COR.sup.9 or --CON(R.sup.9).sub.2 ; andR.sup.13 represents alkyl, aralkyl or aryl,with the proviso that R.sup.3a can not be hydrogen or alkyl when Q is hydrogen, R.sup.4 is hydrogen, and R.sup.5a is hydroxy.Compounds of formula II are useful intermediates for producing compounds having valuable pharmaceutical properties in treating psychosis, depression, pain and hypertension.
摘要翻译：本文公开了新的式II化合物及其药学上可接受的盐，其中：Q表示H，卤素或-OSO 2 R“，其中R”为CH 3，CF 3，苯基或甲苯基; R3a代表H，烷基，烯丙基，环丙基甲基或COOR14，其中R14是烷基，芳基，芳烷基或卤代烷基; R4表示H，卤素，烷基，卤代烷基或烷氧基; R5a代表-OR10，-N（R9）2，-O-C（R7）2xOCOR13或烷氧基; 其中每个R 9独立地表示H，烷基，烷氧基，烷氧基烷基，芳烷基或芳基; R 10表示H，-COR 9或-CON（R 9）2; R 13表示烷基，芳烷基或芳基，条件是当Q为氢时，R 3a不能为氢或烷基，R4为氢，R5a为羟基。式II化合物是制备具有治疗精神病，抑郁症，疼痛和高血压的有价值药物性质的化合物的有用中间体。

2. 发明授权

US5015639A Substituted benzazepines, their preparation and pharmaceutical compositions containing them 失效
标题翻译：取代苯并吖庚因，其制剂和含有它们的药物组合物
公开(公告)号：US5015639A
公开(公告)日：1991-05-14
申请号：US322801
申请日：1989-03-13
申请人： Joel G. Berger , Wei K. Chang , Marjorie Peters
发明人： Joel G. Berger , Wei K. Chang , Marjorie Peters
IPC分类号： C07D223/16 , C07D223/32 , C07D401/04 , C07D403/04 , C07D521/00
CPC分类号： C07D223/16 , C07D223/32 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D403/04
摘要： Disclosed herein are novel 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines of the general formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are specified substituents.R.sup.1 is preferably --X.sup.6, --CHR.sup.7 R.sup.8, cycloalkyl, cycloalkenyl, ##STR2## or pyrrolyl where m is 1, R.sup.6 represents .dbd.H, phenyl, substituted phenyl, aralkyl, alkyl, cycloalkyl, haloalkyl or alkoxyalkyl, R.sup.7 represents H or alkyl preferably H, R.sup.8 represents cycloalkyl, cycloalkenyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl and R.sup.9 represents alkyl, aloxy or alkoxyalkyl.R.sup.2 preferably represents --H and R.sup.3 --CH.sub.3, and R.sup.4 is preferably halogen and R.sup.5 is preferably OH, OCO.R.sup.9 or --O(CR.sup.7).sub.2.OCO.R.sup.13 where R.sup.7 represents hydrogen, R.sup.9 is as defined above and R.sup.13 represents alkyl. The compounds of the formula I are indicated as being useful in the treatment of psychoses, depression and pain. Also disclosed are process for the preparation of the novel compounds as well as pharmaceutical compositions comprising them.
摘要翻译：本文公开了通式I的新的1-取代-2,3,4,5-四氢-1H-3-苯并吖庚因：其中R 1，R 2，R 3，R 4和R 5是指定的取代基。 R1优选为-X6，-CHR7R8，环烷基，环烯基，或吡咯基，其中m为1，R6表示= H，苯基，取代的苯基，芳烷基，烷基，环烷基，卤代烷基或烷氧基烷基，R7表示H或烷基， R8表示环烷基，环烯基，卤代烷基，烷氧基烷基，烯基或炔基，R9代表烷基，氧基或烷氧基烷基。 R2优选表示-H和R3-CH3，R4优选为卤素，R5优选为OH，OCO.R9或-O（CR7）2.OCO.R13，其中R7表示氢，R9如上所定义，R13表示烷基。式I化合物表示可用于治疗精神病，抑郁症和疼痛。还公开了制备新化合物的方法以及包含它们的药物组合物。

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