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    • 3. 发明授权
    • Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines and their use as pharmaceutical compositions
    • 取代的1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并吖嗪及其作为药物组合物的用途
    • US06387921B1
    • 2002-05-14
    • US09995382
    • 2001-11-27
    • Matthias GrauertAdrian CarterThomas WeiserHelmut EnsingerWolfram GaidaJoachim Mierau
    • Matthias GrauertAdrian CarterThomas WeiserHelmut EnsingerWolfram GaidaJoachim Mierau
    • A61K314748
    • C07D405/06C07D221/26
    • Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines of general formula 1: wherein: R1 and R2, which are identical or different, are each hydrogen, C1-C6-alkyl, C1--C6-alkyloxy, OH, F, Cl, or Br; R3 is hydrogen, F, Cl, Br, methyl, ethyl, OH, or methoxy; R4 and R5, which are identical or different, are each hydrogen, methyl, or ethyl; R6 is hydrogen; X is NH2, NH—(C1-C6-alkyl), N(C1-C6-alkyl)2, the two C1-C6-alkyl groups of which are identical or different, NH—COH, NH—CO(C1-C6-alkyl), or F; A is —(CH2)3—, —CH2—CH2—O—, —CH2—O—CH2—, —(CH2)4—, —CH(C1-C6-alkyl)-O—CH2—, —(CH2)2—O—CH2—, —(CH2)3—O—, —(CH2)5—, —CH2—O—(CH2)3—, —(CH2)2—O—(CH2)2—, —(CH2)3—O—CH2—, —(CH2)4—O—, —CH2—O—CH2—CH2—O—, the racemates thereof, the enantiomers thereof, the diastereomers thereof, and mixtures thereof, and the pharmacologically acceptable acid addition salts thereof, processes for preparing them, and their use as pharmaceutical compositions.
    • 取代的通式1的1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并吖嗪:其中:R 1和R 2各自相同或不同,为氢,C 1 -C 6 - 烷基 ,C 1 -C 6烷氧基,OH,F,Cl或Br; R 3是氢,F,Cl,Br,甲基,乙基,OH或甲氧基; R 4和R 5各自相同或不同, 甲基或乙基; R6是氢; X是NH2,NH-(C1-C6-烷基),N(C1-C6-烷基)2,它们的两个C1-C6-烷基相同或不同,NH- COH,NH-CO(C1-C6-烷基)或F; A是 - (CH2)3-,-CH2-CH2-O-,-CH2-O-CH2-, - (CH2) (C 1 -C 6 - 烷基)-O-CH 2 - , - (CH 2)2 -O-CH 2 - , - (CH 2)3 -O - , - (CH 2) , - (CH 2)2 -O-(CH 2)2 - , - (CH 2)3 -O-CH 2 - , - (CH 2)4 -O - , - CH 2 -O-CH 2 -CH 2 -O-, ,其对映异构体,其非对映体及其混合物,及其药学上可接受的酸加成盐,其制备方法及其作为药物组合物的用途。
    • 4. 发明授权
    • Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines and their use as pharmaceutical compositions
    • 取代的1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并吖嗪及其作为药物组合物的用途
    • US06355652B1
    • 2002-03-12
    • US09699748
    • 2000-10-30
    • Matthias GrauertAdrian CarterThomas WeiserHelmut EnsingerWolfram GaidaJoachim Mierau
    • Matthias GrauertAdrian CarterThomas WeiserHelmut EnsingerWolfram GaidaJoachim Mierau
    • A61K31439
    • C07D405/06C07D221/26
    • Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines of general formula 1: wherein: R1 and R2, which may be identical or different, are each hydrogen, C1-C6-alkyl, C1-C6-alkyloxy, OH, F, Cl, or Br; R3 is hydrogen, F, Cl, Br, methyl, ethyl, OH, or methoxy; R4, R5, and R6, which may be identical or different, are each hydrogen, methyl, or ethyl; X is NH2, NH-(C1-C6-alkyl), N(C1-C6-alkyl)2, the two C1-C6-alkyl groups of which may be identical or different, NH—COH, NH—CO(C1-C6-alkyl), or F; A is —(CH2)3—, —CH2—CH2—O—, —CH2—O—CH2—, —(CH2)4—, —CH(C1-C6-alkyl)-O—CH2—, —(CH2)2—O—CH213 , —(CH2)3—O—, —(CH2)5—, —CH2—O—(CH2)3—, —(CH2)2—O—(CH2)2—, —(CH2)3—O—CH2—, —(CH2)4—O—, —CH2—O—CH2—CH2—O—,  the racemates thereof, the enantiomers thereof, the diastereomers thereof, and mixtures thereof, and the pharmacologically acceptable acid addition salts thereof, processes for preparing them, and their use as pharmaceutical compositions.
    • 取代的通式1的1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并吖嗪:其中:R 1和R 2可以相同或不同,各自为氢,C 1 -C 6 - 烷基,C 1 -C 6烷氧基,OH,F,Cl或Br; R 3是氢,F,Cl,Br,甲基,乙基,OH或甲氧基; R 4,R 5和R 6可以相同或不同, 各自为氢,甲基或乙基; X为NH 2,NH-(C 1 -C 6 - 烷基),N(C 1 -C 6烷基)2,其两个C 1 -C 6 - 烷基可以相同或不同,NH -COH,NH-CO(C 1 -C 6烷基)或F; A是 - (CH 2)3 - , - CH 2 -CH 2 -O - , - CH 2 -O-CH 2 - , - (CH 2) CH(C 1 -C 6 - 烷基)-O-CH 2 - , - (CH 2)2 -O-CH 2 13, - (CH 2)3 -O-, - (CH 2) , - (CH 2)2 -O-(CH 2)2 - , - (CH 2)3 -O-CH 2 - , - (CH 2)4 -O - , - CH 2 -O-CH 2 -CH 2 -O-, ,其对映异构体,其非对映体及其混合物,及其药学上可接受的酸加成盐,其制备方法及其作为药物组合物的用途。