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    • 2. 发明授权
    • Phenyl-and phenylalkyl-substituted ethanolamines and ethylenediamines
    • 苯基和苯基烷基取代的乙醇胺和乙二胺
    • US06770636B2
    • 2004-08-03
    • US09912163
    • 2001-07-24
    • Klaus FuchsWerner StranskyMatthias GrauertAdrian CarterWolfram GaidaThomas WeiserHelmut Ensinger
    • Klaus FuchsWerner StranskyMatthias GrauertAdrian CarterWolfram GaidaThomas WeiserHelmut Ensinger
    • A61K3133
    • C07D295/125C07C211/35C07C217/48C07C2601/02C07C2601/14C07C2601/16C07D231/12C07D233/56C07D249/08C07D295/092
    • Compounds of formula 1, wherein: R1 is hydrogen, hydroxy, CF3, NO2, CN, halogen, C1-C8-alkyl, or C1-C8-alkoxy; R2, R3, and R4 independently of one another are hydrogen, C1-C8-alkyl, hydroxy, NO2, CN, C1-C8-alkoxyl, CF3, or halogen; R5 and R6 independently of one another are hydrogen or a group consisting of C1-C8-alkyl, C2-C8-alkenyl, C3-C8-alkynyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkylene, C5-C8-cycloalkenyl, C5-C8-cycloalkenyl-C1-C6-alkylene, C6-C10-aryl, and C6-C10-aryl-C1-C6-alkylene, each optionally substituted by a group consisting of C1-C6-alkyl, C2-C6-alkenyl, halogen, C1-C6-alkyloxy, —NH2, —NH(C1-C4-alkyl), —N(C1-C4-alkyl)2, hydroxy, ═O, —COOH, —CO—OC1-C4-alkyl, —CONH2, —CONH(C1-C4-alkyl), —CON(C1-C4-alkyl)2, and CF3, or R5 and R6 together with the nitrogen atom are a saturated or unsaturated 5-, 6-, 7-, or 8-membered heterocyclic group optionally containing one or two further heteroatoms consisting of sulfur, oxygen, and nitrogen, and optionally mono-, di-, or trisubstituted by a group consisting of C1-C4-alkyl, hydroxy, ═O, —COOH, —CO—OC1-C4-alkyl, —CONH2, —CONH(C1-C4-alkyl), —CON(C1-C4-alkyl)2, halogen, and benzyl; X is oxygen, —NH—, —N(CHO)—, —N(CO—C1-C6-alkyl), —N(C1-C6-alkyl), or —N(C3-C6-cycloalkyl-C1-C4-alkylene); and A is a group consisting of C1-C6-alkylene, C2-C6-alkenylene, and C3-C6-alkynylene, each optionally substituted by a group consisting of halogen, ═O, and hydroxy, or an optical isomer, enantiomer, tautomer, free base, or pharmacologically acceptable acid addition salt thereof; methods of making such compounds; pharmaceutical compositions thereof, and their use in treating or preventing certain diseases.
    • 式1的化合物,其中:R 1是氢,羟基,CF 3,NO 2,CN,卤素,C 1 -C 8 - 烷基或C 1 -C 8 - 烷氧基; R 2,R 3, 4>彼此独立地是氢,C 1 -C 8 - 烷基,羟基,NO 2,CN,C 1 -C 8 - 烷氧基,CF 3或卤素; R 5和R 6彼此独立地是氢或基团 由C 1 -C 8 - 烷基,C 2 -C 8 - 烯基,C 3 -C 8 - 炔基,C 3 -C 8 - 环烷基,C 3 -C 8 - 环烷基-C 1 -C 6亚烷基,C 5 -C 8 - 环烯基,C 5 -C 8 - 环烯基 - C 1 -C 6 - 亚烷基,C 6 -C 10 - 芳基和C 6 -C 10 - 芳基-C 1 -C 6亚烷基,各自任选被C 1 -C 6 - 烷基,C 2 -C 6 - 烯基,卤素,C 1 -C 6 - 烷氧基,-NH 2,-NH(C 1 -C 4 - 烷基),-N(C 1 -C 4 - 烷基)2,羟基,= O,-COOH,-CO-OC 1 -C 4烷基,-CONH 2,-CONH C 1 -C 4烷基),-CON(C 1 -C 4 - 烷基)2和CF 3或R 5和R 6与氮原子一起为饱和或不饱和的5-,6-,7-或 任选地含有一个或两个由硫,氧和氮组成的另外的杂原子的8-元杂环基,以及任选的单 - ,二 - ,或被由C 1 -C 4 - 烷基,羟基,O,-COOH,-CO-OC 1 -C 4烷基,-CONH 2,-CONH(C 1 -C 4 - 烷基),-CON(C 1 -C 4) - 烷基)2,卤素和苄基; X是氧,-NH-,-N(CHO) - , - N(CO-C 1 -C 6烷基), - N(C 1 -C 6 - 烷基) (C 3 -C 6 - 环烷基-C 1 -C 4 - 亚烷基); 并且A是由C 1 -C 6亚烷基,C 2 -C 6亚烯基和C 3 -C 6亚炔基组成的基团,各自任选地被卤素,= O和羟基取代,或光学异构体,对映体,互变异构体, 游离碱或其药理学上可接受的酸加成盐; 制备此类化合物的方法; 其药物组合物及其在治疗或预防某些疾病中的用途。
    • 5. 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。
    • 6. 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。
    • 8. 发明授权
    • 1,2,3,4,5,6-Hexahydro-2,6-methano-3-benzazocin-10-ols
    • 1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并吖庚因-10-ols
    • US06455538B1
    • 2002-09-24
    • US09523473
    • 2000-03-10
    • Matthias GrauertAdrian CarterWolf-Dietrich BechtelThomas WeiserRainer PallukUwe Pschorn
    • Matthias GrauertAdrian CarterWolf-Dietrich BechtelThomas WeiserRainer PallukUwe Pschorn
    • A61K31439
    • C07D221/26
    • Compounds of general formula I wherein X is a single bond, —O—, C-C4-alkylene, or an alkylene bridge having 1 to 8 carbon atoms which may be branched or unbranched and optionally have one or two oxygen atom(s) anywhere in the bridge; R1 is hydrogen, methyl, ethyl, or phenyl; R2 is hydrogen or methyl; R3 is hydrogen, fluorine, chlorine, bromine, hydroxy, methyl, or methoxy; R4 is hydrogen, methyl, or ethyl; R5 is hydrogen, methyl, or ethyl; R6 is hydrogen, methyl, or ethyl; R7 is tert-butyl, cyclohexyl, phenyl optionally substituted by R9 and R10, which may be identical or different, or; R8 is hydrogen or C1-C4-alkyl; Z is oxygen, NH, or sulfur; R9 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; R10 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; optionally in the form of the individual optical isomers, mixtures of the individual enantiomers or racemates as well as in the form of the free bases or the corresponding acid addition salts with pharmaceutically acceptable acids.
    • 通式I的化合物,其中X是单键,-O-,C-C4-亚烷基或具有1至8个碳原子的亚烷基桥,其可以是支链或非支链的,并且任选地在一个或多个氧原子中具有一个或两个氧原子 桥梁 R1是氢,甲基,乙基或苯基; R2是氢或甲基; R3是氢,氟,氯,溴,羟基,甲基或甲氧基; R4是氢,甲基或乙基; R5是氢,甲基或乙基; R6是氢,甲基或乙基; R 7是叔丁基,环己基,任选被R 9和R 10取代的苯基,其可以相同或不同,或者R 8是氢或C 1 -C 4 - 烷基; Z是氧,NH或硫; R9是氢,甲基,氟,氯,溴或甲氧基; R 10为氢,甲基,氟,氯,溴或甲氧基; 任选以各种旋光异构体的形式,各个对映异构体或外消旋体的混合物,以及游离碱的形式或与药学上可接受的酸的相应的酸加成盐。