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    • 3. 发明公开
    • Bicyclooctane derivatives, processes for producing them, pharmaceutical compositions containing them, their use as pharmaceuticals and precursors thereof
    • 二氯化钛衍生物,生产它们的方法,含有它们的药物组合物,它们作为药物及其前体使用
    • EP0036730A3
    • 1982-09-08
    • EP81301063
    • 1981-03-13
    • SUMITOMO CHEMICAL COMPANY, LIMITED
    • Ono, KeiichiSugie, AkihikoKawakami, HajimeSami, ShunsukeKojima, AtsuyukiKatsube, Junki
    • C07C43/18C07C59/00C07C69/66C07C91/00C07C93/00C07C47/00C07D211/14C07C121/75C07C103/30C07C177/00A61K31/00A61K31/557
    • C07C255/00C07B2200/07C07B2200/09C07C29/095C07C29/1285C07C35/32C07C43/196C07C405/0083C07C2602/24C07D211/32Y10S514/925C07C29/143
    • Certain novel bicyclooctanes and their pharmaceutically acceptable salts are useful in the treatment of gastrointestinal ulcers. These compounds can be prepared by various methods and have the formula
      wherein X 1 is a free or esterified carboxyl group, a hydroxymethyl group, a cyano group, 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) or a group of the formula:
      (R a and R b are each as defined above), Y is an ethylene group or a vinylene group, 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, means a single linkage to form a double bond between the carbon atoms which they are linked, R 3 is a hydroxyl group or a protected hydroxyl group, R 4 is a hydrogen atom or a C 1 -C 4 alkyl group, R 5 is a hydrogen atom, a C 3 -C 8 alkenyl group, a C 3 -C 8 alkynyl group, a C 1 -C 8 alkyl group, a C 3 -C 7 cycloalkyl group or a group of the formula: -(CH 2 ) n- B (n is 1 or 2 and B is a C 1 -C 4 alkoxyl group, a C 3 -C 7 cycloalkyl group, or a phenyl or phenoxy group optionally substituted with a halogen atom, a C 1 -C 4 alkyl group, a trifluoromethyl group or a C 1 -C 4 alkoxyl group), A is a group of either one of the formulae: -CH=CH-,
      (R 6 and R 7 are each independently a hydrogen atom or a C 1 -C 4 alkyl group) and m 1 is 1 or 2 and m 2 is 0, 1 or 2.
    • 某些新颖的双环辛烷及其药学上可接受的盐可用于治疗胃肠溃疡。 这些化合物可以通过各种方法制备,并具有式... ...其中X 1是游离或酯化的羧基,羟甲基,氰基,下式的基团:... ...( R a和R b各自独立地为氢原子,C 1 -C 4烷基,C 3 -C 7环烷基,苄基,苯基,被卤素原子取代的苯基或C1- C4烷基,或者当与它们所连接的相邻氮原子一起时,它们表示5至7元饱和杂环基团)或下式的基团:... ...(R a和 R b各自如上所定义),Y是亚乙基或亚乙烯基,R 1是氢原子,羟基或保护的羟基,R 2是氢原子或R 1和 当R 2一起表示单键以在它们连接的碳原子之间形成双键时,R 3是羟基或被保护的羟基,R 4是氢原子或 C 1 -C 4烷基,R 5是氢原子,C 3 -C 8烯基,C 3 -C 8炔基,C 1 -C 8烷基,C 3 -C 7环烷基或下式的基团: - (CH 2)n B(n为1或2,B为C 1 -C 4烷氧基,C 3 -C 7环烷基或任选被卤素原子取代的苯基或苯氧基,C 1 -C 4烷基, 基团或C 1 -C 4烷氧基),A是下式中的任何一个:-CH = CH-,... ...(R 6和R 7各自独立地是氢原子或 C1-C4烷基)和... ... m1为1或2,m2为0,1或2。