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    • 1. 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。
    • 3. 发明授权
    • Preparation of 2-benzoylalkylbenzomorphan
    • 2-苯甲酰基烷基苯并咪唑的制备
    • US3953441A
    • 1976-04-27
    • US150841
    • 1971-06-07
    • Toshio AtsumiKenji KobayashiYoshiaki TakebayashiHisao Yamamoto
    • Toshio AtsumiKenji KobayashiYoshiaki TakebayashiHisao Yamamoto
    • C07D211/70C07D221/26
    • C07D221/26C07D211/70
    • A novel process for preparing 2-benzoylalkylbenzomorphan derivatives and salts thereof, represented by the formula ##SPC1##Wherein n, R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification. The process comprises reacting a pyridinium derivative of the formula, ##SPC2##Wherein X is a halogen atom and Y' is an ethylenedioxy group; with a Grignard reagent of the formula, ##SPC3##Wherein R' is a hydrogen atom or a C.sub.1 -C.sub.3 alkoxy group and Z is a halogen atom, to yield a 1,2-dihydropyridine derivative of the formula; ##SPC4##And then reducing the said 1,2-dihydropyridine derivative to give a 1,2,5,6-tetrahydropyridine derivative of the formula, ##SPC5##Wherein Y is an oxygen atom or an ethylenedioxy group, and further cyclizing the obtained 1,2,5,6-tetrahydropyridine derivative.
    • 由式WHEREIN N,R,R1,R2,R3和R4表示的用于制备2-苯甲酰基烷基苯并喃衍生物及其盐的新方法如本说明书中所定义。 该方法包括使下式的吡啶鎓衍生物WHEREIN X是卤素原子,Y'是亚乙二氧基; 与下式的格利雅试剂,其中R'是氢原子或C1-C3烷氧基,Z是卤素原子,得到下式的1,2-二氢吡啶衍生物; 然后减少所得的1,2-二氢吡啶衍生物,得到本发明的1,2,5,6-四氢吡啶衍生物,其中Y是氧原子或亚乙二氧基,进一步环化得到的1,2,5,6-四氢吡啶衍生物, 6-四氢吡啶衍生物。