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    • 41. 发明授权
    • Pharmaceutical phenylacetonitrile derivatives
    • 药用苯乙腈衍生物
    • US4612313A
    • 1986-09-16
    • US774354
    • 1985-09-10
    • Herbert LeinertWolfgang KampeKlaus StreinBernd Muller-BeckmannWolfgang Bartsch
    • Herbert LeinertWolfgang KampeKlaus StreinBernd Muller-BeckmannWolfgang Bartsch
    • A61K31/21A61K31/275A61K31/445A61P9/08A61P9/10A61P9/12C07C67/00C07C253/00C07C255/24C07C255/32C07C255/42C07C255/43C07C255/53C07C255/58C07C255/59C07D207/08C07D211/22C07D241/04C07D295/16C07D295/18A61K31/495C07C121/80
    • C07C255/00C07D211/22
    • The present invention provides phenylacetonitrile derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, are hydrogen or haolgen atoms or alkyl, alkoxy, nitro, amino or acylamino radicals and two adjacent substituents can together also form a methylenedioxy or ethylenedioxy radical, A is a radical of the general formula: ##STR2## in which R.sub.6 is a straight-chained, cyclic or branched, saturated or unsaturated alkyl radical containing 2 to 12 carbon atoms, R.sub.7 is a hydrogen atom or a straight-chained or branched, saturated alkyl radical containing up to 6 carbon atoms, m and n, which can be the same or different, are 2 or 3, p is 1 or 2 and X is a straight-chained, cyclic or branched alkyl radical containing 2 to 10 carbon atoms which is optionally substituted by an amino group or is a grouping of the general formula: ##STR3## wherein Y and Z, which can be the same or different, are straight-chained or branched alkyl radicals containing up to 8 carbon atoms or cycloalkyl, alkylcycloalkyl or cycloalkylalkyl radicals, in which these radicals are optionally interrupted by an oxygen or sulphur atom, and one of the groups Z in general formula II can also be a hydrogen atom or both Z groups are joined to form a ring containing 4 to 6 carbon atoms which is optionally interrupted by a further nitrogen atom which can be substituted by alkyl or alkanoyl, the --O--NO.sub.2 groups being substituents of Y as well as of Z; as well as the salts thereof with physiologically acceptable acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.
    • 本发明提供以下通式的苯乙腈衍生物:其中R 1,R 2,R 3,R 4和R 5可以相同或不同,为氢或卤素原子或烷基,烷氧基,硝基,氨基或 酰基氨基和两个相邻的取代基可以一起形成亚甲二氧基或亚乙二氧基,A是下列通式的基团:其中R 6是含有2至12个直链的直链,环状或支链的饱和或不饱和烷基 碳原子,R7是氢原子或含有至多6个碳原子的直链或支链饱和烷基,m和n可相同或不同,为2或3,p为1或2,X为 是含有2至10个碳原子的直链,环状或支链烷基,其任选被氨基取代,或者是通式如下的基团:其中Y和Z可以相同或不同, 是直链或支链烷基基团 引入多达8个碳原子或环烷基,烷基环烷基或环烷基烷基,其中这些基团任选地被氧或硫原子中断,通式II中的基团Z之一也可以是氢原子或两个Z基团连接 形成含有4至6个碳原子的环,其任选被可被烷基或烷酰基取代的另外的氮原子中断,-O-NO 2基团是Y和Z的取代基; 以及其与生理上可接受的酸的盐。 本发明还提供了制备这些化合物的方法和含有它们的药物组合物。
    • 44. 发明授权
    • Preparation of aminoitriles
    • 氨基腈的制备
    • US4478759A
    • 1984-10-23
    • US283649
    • 1981-07-15
    • Harry DistlerKarl-Ludwig Hock
    • Harry DistlerKarl-Ludwig Hock
    • C07C255/24C07C255/25C07C120/00
    • C07C255/00
    • Aminonitriles are prepared by reacting a nitrogen compound with formaldehyde and hydrogen cyanide in the presence of an additional acid at a pH below 2 and at from 10.degree. to 70.degree. C., the concentration of the hydrogen cyanide during the reaction being not more than 3 per cent by weight, based on the reaction mixture.The aminoacetonitriles obtained by the novel process are valuable starting materials for the preparation of dyes, fungicides, bactericides, textile assistants, rubber additives, and auxiliaries used in water softening, cosmetics, the photographic industry, the paper industry and the electroplating industry.
    • 氨基腈是通过使氮化合物与甲醛和氰化氢在另外的酸存在下,在低于2和10至70℃的pH下反应制备的,反应中氰化氢的浓度不大于3 基于反应混合物的重量百分比。 通过新方法获得的氨基乙腈是用于制备染料,杀真菌剂,杀菌剂,纺织助剂,橡胶添加剂和用于水软化,化妆品,摄影工业,造纸工业和电镀工业的助剂的有价值的起始材料。
    • 50. 发明授权
    • Process for preparing 1-(N-.beta.-cyanethylaminol-3-acylaminobenzenes
    • 制备1-(N- {62-氰乙基氨基-3-酰氨基苯
    • US4007213A
    • 1977-02-08
    • US680706
    • 1976-04-27
    • Rudolf Schickfluss
    • Rudolf Schickfluss
    • C07C253/00B01J27/00B01J27/20B01J31/00B01J31/04C07B61/00C07C20060101C07C67/00C07C231/00C07C255/24C07C121/78
    • C07C253/30
    • Process for the manufacture of 1-(N-.beta.-cyanethylamino)-3-acylaminobenzenes of the formula (1) ##STR1## in which R.sub.1 represents hydrogen, methyl or alkoxy of 1 to 4 carbon atoms, R.sub.2 represents hydrogen, alkyl from 1 to 3 carbon atoms or phenyl, R.sub.3 represents hydrogen or alkyl from 1 to 3 carbon atoms, and n represents the integer 0 or 1, which comprises reacting 1 mole of an amino of the formula (2) ##STR2## in which R.sub.1, R.sub.2 and R.sub.3 are defined as above, with 1 to 1.75 moles of acrylonitrile between 70.degree. and 150.degree. C in water with the addition of 1 to 30% by weight of an organic carboxylic acid or carbonic acid, and oxethylating the compound at the said formula (1) obtained, if n stands for the integer 0, without or after isolation, with 1 to 10 moles of ethylene oxide between 50.degree. and 100.degree. C.
    • 制备式(1)的1-(N-β-氰基乙基氨基)-3-酰氨基苯的方法其中R1代表氢,甲基或1-4个碳原子的烷氧基,R2代表氢, 1至3个碳原子的烷基或苯基,R 3表示氢或1至3个碳原子的烷基,n表示整数0或1,其包括使1摩尔式(2)的氨基 ),其中R 1,R 2和R 3如上定义,在水中加入1至30重量%的有机羧酸或碳酸,其中1至1.75摩尔丙烯腈在70至150℃之间,并加入氧乙基化 所述式(1)中的化合物,如果n代表整数0,则在分离后没有或分离后,其中1至10摩尔环氧乙烷在50至100℃之间。