会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 28. 发明公开
    • Dérivés d'acide [alpha-(alkylaminométhyl)-benzylthio]-acétique, procédé de préparation et utilisation en thérapeutique
    • [α-(烷基氨基甲基) - 苄基硫基] - 醚基 - 衍生物,维他命Zur Herstellung und Verwendung in Therapie。
    • EP0158545A1
    • 1985-10-16
    • EP85400431.4
    • 1985-03-06
    • LABORATOIRE L. LAFON Société anonyme dite:
    • Lafon, Louis
    • C07C149/00C07C147/00A61K31/00
    • A61K31/265
    • La présente invention concerne en tant que produits industriels nouveaux les dérivés de formole
      où X est S ou SO, Y est alkoxy en C 1 -C 4 , NH 2 ou NHOH, R est H ou CH 3 , R 1 et R 2 , identiques ou différents, représentent chacun H, F, Cl ou Br, et Z est alkyle en C 1 -C 4 ; les isomères optiques correspondants; et leur sels d'addition.
      Elle concerne également le procédé de préparation de ces nouveaux produits, ainsi que leur utilisation en thérapeutique notamment en tant qu'agents antidépresseurs.
    • 对于缔约国BE,CH,DE,FR,GB,IT,LI,LU,NL,SE 1.(苄硫基)乙酸的胺衍生物,其特征在于其选自a) - (烷基氨基甲基) - 苄硫基] - 乙酸衍生物,参见图示:EP0158545,P13,F1,其中X是S或SO,Y是C1-C4烷氧基,NH2或NHOH,Z是C1-C4-烷基 R为H或CH 3,R 1和R 2可以相同或不同,表示H,F,Cl,Br; b)它们的光学异构体,和c)其加成盐。 对于缔约国:AT 1.制备下式的[α-(烷基氨基甲基) - 苄硫基] - 乙酸衍生物的方法:参见图示:EP0158545,P14,F1,其中X是S或SO,Y是C1-C4 - 烷氧基,NH 2或NHOH,Z为C 1 -C 4 - 烷基,R为H或CH 3,R 1和R 2可以相同或不同,表示H,F,Cl,Br; 其光学异构体及其加成盐,所述方法的特征在于其包括以下步骤:a)使下式的N-烷基-N-(2)卤代-2-苯基乙基) - 胺反应:参见图示:EP0158545, P14,F2其中Hal表示F,Cl或Br,Ar表示(R1R2)C6H3基团,其中R1和R2如上所定义,Z如上所定义,与式HS- 其中A为C1-C4烷氧基且R为H或CH3,在下式的醇中,其中A定义如上所述,在碱金属存在下,在室温 温度和反应介质的回流温度,以获得下式的[α-(烷基氨基甲基) - 苄硫基] - 乙酸烷基酯:参见图示:EP0158545,P14,F3 b)如果需要,反应至少5公顷的温度 在15至25℃之间,由化合物得到所述的α-(烷基氨基甲基) - 苄硫基] - 乙酸烷基酯 选自NH 3和NH 2 OH分别获得相应的下式的酰胺:参见图示:EP0158545,P14,F4和下式的异羟肟酸:参见图示:EP0158545,P14,F5和c)如果需要,对硫化物 选自式V,VI和VII的化合物的化合物与H 2 O 2进行氧化反应,以获得其中X为SO的式I的亚磺酰基化合物。
    • 29. 发明公开
    • Novel bicyclooctane compounds and production thereof
    • 新型双氰胺化合物及其生产
    • EP0139515A3
    • 1985-10-09
    • EP84306984
    • 1984-10-12
    • SUMITOMO CHEMICAL COMPANY, LIMITED
    • Sugie, AkihikoMuraoka, MasamiNakamura, ToshioOno, KeiichiYamamoto, Michihiro
    • C07C177/00C07C147/00C07C149/00A61K31/557
    • C07C405/0083
    • A compound which has strong anti-ulcer activity and is useful in the treatment of ulcers has the formula:
      wherein X 1 is a free or esterified carboxyl group, or a group of the formula:
      (R a and R b are each independently a hydrogen atom, a C 1 -C 4 alkyl group, a C 3 -C 7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C 1 -C 4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7 membered saturated heterocyclic group), Y' is a group of the formula:
      (R 6 is a hydrogen atom or C 1 -C 4 alkyl group), or
      R 6 is as defined above), R 1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R 2 is a hydrogen atom or R 1 and R 2 , when taken together, mean a single linkage to form a double bond between the carbon atoms to which they are linked, R 3 is a hydroxyl group or a protected hydroxyl group, R 4 is-a a hydrogen atom or a C 1 -C 4 alkyl group, R 5 is a hydrogen atom, a C 1 -C 12 alkyl group, a C 2 -C 12 alkenyl group, a C 2 -C 12 alkynyl group, a C 3 -C 10 cycloalkyl group, a C 4 -C 10 cycloalkenyl group, a hydroxy C 1 -C 12 alkyl group, a C 3 -C 10 heterocyclic group, a phenyl group optionally Substituted with a halogen atom a hydroxy group a C. C 4 alkyl group a trifluoromethyl group. or a C 1 -C 4 alkyl group or a group of the formula. A-B (A is a C 1 -C 7 alkylene chain and B is a C 3 -C 10 cycloalkyl group, a C 4 -C 10 cycloalkenyl group, a C 1 -C 12 alkoxy group, a C 3 -C 10 cycloalkoxy group, a C 4 -C 10 cycloalkenyloxy group, a C 3 -C 10 heterocyclic group, or a phenyl or phenoxy group optionally substituted with a halogen atom. a hydroxy group, a C 1 -C 4 alkyl group. a trifluoromethyl group or a C 1 -C 4 alkoxy group) m is 0, 1 or 2; or a non-toxic pharmaceutically acceptable salt thereof.
    • 30. 发明公开
    • Diaminocyclohexane platinum complexes, process for preparing same and pharmaceutical compositions containing same
    • 二氨基环己烷铂络合物,其制备方法和含有它们的药物组合物。
    • EP0130482A1
    • 1985-01-09
    • EP84107104.6
    • 1984-06-20
    • Research Corporation
    • Brown, Davis B.Khokhar, Abdul R.Hacker, Miles P.McCommack, John J.
    • C07C87/38A61K31/28C07D307/00C07D205/04C07H23/00C07C61/00C07C62/32C07C101/00C07C143/08C07C147/00C07C161/00
    • C07C309/00C07C51/418C07C55/28C07C59/105C07C61/04C07C61/06C07C61/08C07C61/09C07C61/20C07C61/22C07F15/0093
    • Diaminocyclohexane platinum complexes having the structural formula
      or
      wherein: X is a monovalent anion selected from the group consisting of ascorbate, isoascorbate, monosaccharate, saccharate-4-lactone, shikimate, isethionate, 2-aminoethylsulfate, azetidinecarboxylate, proline, hydroxyproline, pipecolinate, cyclopropanecarboxylate, cyclobutanecarboxylate, cyclopentanecarboxylate, cyclopentenecarboxylate, cyclohexanecarboxylate, cyclohexenecarboxylate, bicine, glycine, 2-aminoethanesulfonate, 2-chloroethanesulfonate and
      Y is a divalent anion selected from the group consisting of iminodiacetate, isocitratelactone, furanedicarboxylate, cyclopropane-1,1-dicarboxylate, isocitratomonoethylester, N-methyliminodiacetate, N-(2-hydroxyethyl)-iminodiacetate, N-benzyl- iminodiacetate, N-phenyliminodiacetate, N-(2-acetamido)-iminodiacetate, cyclohexane-1,1-diacetate, trans-1,2-cyclopropanedicarboxylate, trans-1,2-cyclobutanedicarboxylate, trans-1,2-cyclopentanedicarboxylate and trans-1,2-cyclohexanedicarboxylate and pharmaceutical compositions for the treatment of tumors. Disclosed is also a process for preparing the new complexes.
    • 具有结构式Diaminocyclohexanes铂络合物 worin; X是选自抗坏血酸,isoascorbates,monosaccharate,蔗糖-4-内酯,莽草酸,羟乙磺酸盐,2- aminoethylsulfate,氮杂环丁烷,脯氨酸,羟基脯氨酸,2-哌啶,环丙烷羧酸,环丁烷羧酸,环戊烷羧酸,cyclopentenecarboxylate,环己烷羧酸,环己烯羧酸的一价阴离子 ,BICINE,甘氨酸,2- aminoethanesulfonate,2- chloroethanesulfonate和Y是选自iminodiacetates,isocitratelactone,furanedicarboxylate,环丙烷-1,1-二羧酸二乙酯,isocitratomonoethylester,N- methyliminodiacetate,N-(2-羟乙基中选出的二价阴离子 )-iminodiacetate,N- benzyliminodiacetate,N- phenyliminodiacetate,N-(2-乙酰氨基)-iminodiacetate,环己烷-1,1-二乙酸,反式-1,2-环丙烷,反式-1,2-环丁烷,反式1, 2环戊烷和反式1,2-环己烷和用于肿瘤的治疗药物组合物。 因此,本发明公开了一种制备新型配合物的方法。