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    • 2. 发明公开
    • Immuno-suppressing enepyranose derivatives
    • 免疫抑制剂。
    • EP0560055A1
    • 1993-09-15
    • EP93101822.0
    • 1993-02-05
    • ISHIHARA SANGYO KAISHA, LTD.
    • Mizukoshi, Sadanori, c/o Ishihara Sangyo KaishaKato, Fuminori, c/o Ishihara Sangyo KaishaTsukamoto, Masamitsu, c/o Ishihara Sangyo KaishaKon, Kenji, c/o Ishihara Sangyo Kaisha
    • C07H3/08C07H3/10A61K31/70C07H13/04C07H13/06C07H13/08C07H13/10C07H13/12C07H15/04C07H15/207C07D491/08
    • C07H13/04C07H3/08C07H3/10C07H7/02C07H11/00C07H13/06C07H13/08C07H13/12C07H15/04C07H15/18C07H15/207
    • An immuno-suppressive agent containing, as an effective component, an enopyranose derivative of the following formula (I) or its salt:
      wherein R 1 is a hydrogen atom, alkyl which may be substituted, alkenyl, alkynyl, -OSO 2 R 7 , a halogen atom, -OCOR 7 , -NHCOR 8 , alkoxy, phenyl which may be substituted or a saccharose residue, R 2 is a hydrogen atom or alkyl, R 3 is a hydrogen atom or a halogen atom, R 4 is a hydrogen atom, -COR 9 , silyl which may be substituted or alkyl which may be substituted, one of R 5 and R 6 is hydroxyl, alkoxy which may be substituted, a saccharose residue, cycloalkyloxy which may be substituted or -OCOR 10 and the other is a hydrogen atom or alkyl which may be substituted, or R 4 and R 5 together form a single bond, while R 6 is a hydrogen atom or alkyl which may be substituted, each of R 7 , R 9 and R 10 is alkyl or phenyl which may be substituted, R 8 is alkyl, phenyl which may be substituted or benzyloxy, X is a hydrogen atom, alkyl which may be substituted, alkenyl which may be substituted, alkynyl which may be substituted, cycloalkyl which may be substituted, phenyl which may be substituted, pyridyl which may be substituted, furanyl which may be substituted, thienyl which may be substituted, formyl, -COR 11 , -C(W 1 )W 2 R 11 or -SO 2 R 11 , R 11 is a chain hydrocarbon group which may be substituted, a monocyclic hydrocarbon group which may be substituted, a polycyclic hydrocarbon group which may be substituted, a monocyclic heterocycle group which may be substituted, or a polycyclic heterocycle group which may be substituted, W 1 is an oxygen atom or a sulfur atom, W 2 is an oxygen atom, a sulfur atom or -NH-, Y is a hydrogen atom, alkyl which may be substituted, alkenyl which may be substituted or alkynyl which may be substituted.
    • 含有作为有效成分的下式(I)的吡喃葡萄糖衍生物或其盐的免疫抑制剂:其中R 1为氢原子,可被取代的烷基,烯基,炔基, - OSO 2 R 7,卤素原子,-OCOR 7,-NHCOR 8,烷氧基,可被取代的苯基或蔗糖残基,R 2是氢原子或烷基,R 3是 氢原子或卤素原子,R 4是氢原子,-COR 9,可被取代的甲硅烷基或可被取代的烷基,R 5和R 6之一是羟基,烷氧基 可以被取代,可以被取代的蔗糖残基,可以被取代的环烷氧基或-OCOR 1,另一个是可以被取代的氢原子或烷基,或者R 4和R 5一起形成一个 键,而R 6为氢原子或可被取代的烷基,R 7,R 9和R 10各自为可被取代的烷基或苯基,R 8, 是烷基,可被取代的苯基或苄氧基,X是氢原子,烷基 可被取代的烯基,可被取代的链烯基,可被取代的环烷基,可被取代的苯基,可被取代的吡啶基,可被取代的呋喃基,可被取代的噻吩基,甲酰基, -COR 1,-C(W 1)W 2 R 1或-SO 2 R 1,R 1是链烃基 可被取代的单环烃基,可被取代的多环烃基,可被取代的多环烃基,可被取代的单环杂环基或可被取代的多环杂环基,W 1是氧原子 或硫原子,W 2为氧原子,硫原子或-NH-,Y为氢原子,可被取代的烷基,可被取代的烯基或可被取代的炔基。