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    • 35. 发明授权
    • Benzenesulfonamide derivatives
    • 苯磺酰胺衍生物
    • US4157257A
    • 1979-06-05
    • US837911
    • 1977-09-29
    • Tetsuo TakematsuMakoto KonnaiHiroyoshi Omokawa
    • Tetsuo TakematsuMakoto KonnaiHiroyoshi Omokawa
    • A01N41/06C07C311/15A01N9/14C07C143/79C07C143/82
    • C07C255/00A01N41/06
    • A compound of the general formula ##STR1## wherein R.sub.0 represents an alkyl group optionally having a substituent selected from the class consisting of a cyano group, lower alkoxy groups and di-(lower alkyl)amino groups, a lower alkenyl group, or a lower alkynyl group; R.sub.1, R.sub.2 and R.sub.3, independently from each other, represent a hydrogen atom, a halogen atom, a lower alkyl group, or a lower alkoxy group; R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8, independently from each other, represent a hydrogen atom, a halogen atom, a lower alkyl group, or a lower alkoxy group; Y represents a group of the formula ##STR2## or a group of the formula ##STR3## in which one of R.sub.9 and R.sub.10 is a lower alkyl group and the other is a hydrogen atom or a lower alkyl group; with the proviso that when Y is the group ##STR4## and R.sub.0 represents an unsubstituted alkyl group, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 do not represent hydrogen atoms at the same time. The compounds of formula (I) are produced by the reaction of the corresponding benzenesulfonamide derivatives with the corresponding benzyl or benzoyl halides; the reaction of the corresponding benzenesulfonyl halides with the corresponding benzylamines or benzoyl amides; or by the alkylation, alkenylation or alkynylation of the corresponding compounds of formula (I) in which R.sub.0 is hydrogen. The compounds of formula (I) have superior selective herbicidal effects, and are useful as active ingredients of herbicides, especially those for application to aquatic rice paddies.
    • 通式(I)的化合物,其中R 0表示任选具有选自氰基,低级烷氧基和二 - (低级烷基)氨基的取代基的烷基,低级烯基, 或低级炔基; R 1,R 2和R 3彼此独立地表示氢原子,卤素原子,低级烷基或低级烷氧基; R4,R5,R6,R7和R8彼此独立地表示氢原子,卤素原子,低级烷基或低级烷氧基; Y表示式为“IMAGE”的基团或其中R9和R10中的一个为低级烷基且另一个为氢原子或低级烷基的式“IMAGE”的基团; 条件是当Y为基团时,R 0表示未取代的烷基,R 4,R 5,R 6,R 7和R 8不同时表示氢原子。 式(I)化合物通过相应的苯磺酰胺衍生物与相应的苄基或苯甲酰基卤化物的反应产生; 相应的苯磺酰卤与相应的苄胺或苯甲酰胺的反应; 或通过其中R 0是氢的相应的式(I)化合物的烷基化,烯基化或炔基化。 式(I)的化合物具有优异的选择性除草效果,并且可用作除草剂的活性成分,特别是用于水稻的施用。
    • 40. 发明公开
    • Ethanolamine derivatives, process for their preparation and pharmaceutical compositions containing them
    • 乙酰胺衍生物及其制备方法及含有它们的药物组合物
    • EP0091749A3
    • 1984-12-05
    • EP83301652
    • 1983-03-24
    • BEECHAM GROUP PLC
    • Duckworth, David Malcolm
    • C07C143/78C07C143/79C07D295/22A61K31/18A61K31/445A61K31/535
    • C07D295/26C07C309/00
    • AA compound of formula (I):
      or a salt thereof, wherein;
      R 1 is hydrogen, halogen or trifluoromethyl. R 2 is hydrogen or halogen, R 3 is hydrogen or methyl, R 4 is hydrogen or methyl, R 6 is hydrogen, C 1-10 straight or branched alkyl or optionally substituted benzyl, R 6 is hydrogen, C 1-10 straight or branched alkyl, or optionally substituted benzyl, or R 6 and R 6 taken together with the attached nitrogen atom represent a heterocyclic ring, R 7 is hydrogen or halogen, and n is 1 or 2;
      are useful in the treatment of obesity and/or diabetes. Anti-hypertensive compounds of formula (I):
      wherein
      one of R 1 and R 2 is nitro, cyano or C 1-3 alkylcarbonyl, and the other is methoxy or amino optionally substituted by one or two C 1-6 alkyl or by C 2-7 alkanoyl; one of R 3 and R 4 is hydrogen or C 1-4 alkyl and the other is C 1-4 alkyl, or R 3 and R 4 together with the carbon atom to which they are attached are C 3-6 spiroalkyl; R 5 is hydrogen, C 1-3 alkyl or C 1-8 acyl; and n is 1 or 2; the lactam group being trans to the OR 5 group; or, when the other of R, and R 2 is amino, a pharmaceutically acceptable salt thereof.
    • 式(I)的化合物:或其盐,其中; R 1是氢,卤素或三氟甲基,R 2是氢或卤素,R 3是氢或甲基,R 4是氢或甲基,R 5是氢,C 1-10直链或 支链烷基或任选取代的苄基,R 6是氢,C 1-10直链或支链烷基或任选取代的苄基,或R 5和R 6与连接的氮原子一起表示杂环R 7是氢或卤素,n是1或2; 可用于治疗肥胖和/或糖尿病。