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    • 74. 发明授权
    • Butyrophenone derivatives
    • 丁酰苯衍生物
    • US4009173A
    • 1977-02-22
    • US617730
    • 1975-09-29
    • Kikuo SasajimaMasaru NakaoIsamu MaruyamaKeiichi OnoShigenari KatayamaShigeho InabaHisao Yamamoto
    • Kikuo SasajimaMasaru NakaoIsamu MaruyamaKeiichi OnoShigenari KatayamaShigeho InabaHisao Yamamoto
    • C07D211/64C07D403/04
    • C07D211/64
    • Novel butyrophenone derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydroxyl group or ##STR2## (wherein R.sub.6 and R.sub.7 are each a hydrogen atom or a lower alkyl group or, when taken together with the adjacent nitrogen atom, may form a heterocyclic group), R.sub.2 represents an optionally substituted phenyl group or ##STR3## (wherein R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl group or, when taken together with the adjacent nitrogen atom, may form a heterocyclic group), R.sub.4 represents a hydrogen atom, a lower alkyl group or an optionally substituted phenyl group, R.sub.5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or a trifluoromethyl group, R.sub.10 represents a hydrogen atom or an acyl group represented by R.sub.3 CO- (wherein R.sub.3 is a hydrogen atom, a lower alkyl group or an optionally substituted phenyl group) and Z represents two hydrogen atoms or an oxygen atom, provided that when Z is an oxygen atom and R.sub.1 is ##STR4## R.sub.10 can not be a hydrogen atom, and their acid addition salts, which are useful as central and autonomic nervous system depressants.
    • 下式的新型丁基苯酚衍生物:其中R 1表示羟基或(其中R 6和R 7各自为氢原子或低级烷基,或者当与相邻的氮原子一起形成杂环时 基团),R 2表示任选取代的苯基或者其中R 8和R 9各自为氢原子或低级烷基,或者当与相邻的氮原子一起形成杂环基时,R 4表示 氢原子,低级烷基或任选取代的苯基,R 5表示氢原子,卤素原子,低级烷基,低级烷氧基或三氟甲基,R 10表示氢原子或R 3 CO 3表示的酰基 - (其中R 3是氢原子,低级烷基或任选取代的苯基),Z代表两个氢原子或氧原子,条件是当Z是氧原子且R 1不能是 氢原子, 和它们的酸加成盐,其可用作中枢神经系统抑制剂和自主神经系统抑制剂。
    • 78. 发明授权
    • Analgesic compositions containing 2-cyanoalkylbenzomorphan derivatives
and salts thereof
    • 含有2-氰基烷基苯并喃衍生物及其盐的止痛组合物
    • US3962446A
    • 1976-06-08
    • US523412
    • 1974-11-13
    • Toshio AtsumiKenji KobayashiYoshiaki TakebayashiHisao Yamamoto
    • Toshio AtsumiKenji KobayashiYoshiaki TakebayashiHisao Yamamoto
    • A61K31/395A61K31/485
    • A61K31/395
    • An analgesic composition comprising an analgesically effective amount of at least one 6,7-benzomorphan derivative of the formula: ##SPC1##Wherein R is a hydrogen atom, a hydroxyl group, a C.sup.1 - C.sup.3 alkoxy group or a C.sup.1 - C.sup.8 alkanoyloxy group; R.sub.1 is a hydrogen atom, a C.sup.1 - C.sup.5 alkyl group, a phenyl group, a halophenyl group, an alkylphenyl group wherein the alkyl moiety has 1 to 3 carbon atoms, an alkoxyphenyl group wherein the alkoxy moiety has 1 to 3 carbon atoms, a trifluoromethylphenyl group, an alkylthiophenyl group wherein the alkylthio moiety has 1 to 3 carbon atoms or a group of the formula (C.sub.m H.sub.2m.sub.-p.sub.+1) - (R.sub.9).sub.p wherein m is an integer of 1 - 6, p is an integer of 1 - 2 and R.sub.9 is a C.sup.1 - C.sup.3 alkoxy group; R.sub. 2 is a hydrogen atom or a C.sup.1 - C.sup.3 alkyl group; R.sub.3 is a hydrogen atom, a C.sup.1 - C.sup.3 alkyl group, a phenyl group or an alkoxyphenyl group wherein the alkoxy moiety has 1 to 3 carbon atoms; R.sub.4 is a hydrogen atom or a hydroxyl group, or R.sub.3 and R.sub.4 may form a C.sup.1 - C.sup.3 alkylidene group or a carbonyl group together with a carbon atom to which these substituents are bonded; R.sub.5 is a hydrogen atom or C.sup.1 - C.sup.3 alkyl group; R.sub.6 is a hydrogen atom or a methyl group; R.sub.7 and R.sub.8 are independently a hydrogen atom or a C.sup.1 - C.sup.2 alkyl group; and n is an integer of 0 - 2; or an acid addition salt thereof, and a pharmaceutically acceptable carrier or diluent, is disclosed.
    • 一种止痛组合物,其包含镇痛有效量的至少一种下式的6,7-苯并吗啉衍生物:WHEREIN R是氢原子,羟基,C1-C3烷氧基或C1-C8烷酰氧基; R1为氢原子,C1-C5烷基,苯基,卤代苯基,烷基部分为碳原子数1〜3的烷基苯基,烷氧基部分为碳原子数1〜3的烷氧基苯基, 三氟甲基苯基,其中烷硫基部分具有1至3个碳原子的烷硫基苯基或式(CmH2m-p + 1) - (R9)p的基团,其中m是1-6的整数,p是整数1 - 2和R9是C1-C3烷氧基; R 2是氢原子或C 1 -C 3烷基; R3是氢原子,C1-C3烷基,苯基或烷氧基苯基,其中烷氧基部分具有1至3个碳原子; R4是氢原子或羟基,或者R3和R4可以与这些取代基结合的碳原子一起形成C1-C3亚烷基或羰基; R5是氢原子或C1-C3烷基; R6是氢原子或甲基; R 7和R 8独立地为氢原子或C 1 -C 2烷基; n为0-2的整数; 或其酸加成盐,以及药学上可接受的载体或稀释剂。