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    • 1. 发明授权
    • Amino sugar derivatives
    • 氨基糖衍生物
    • US5432267A
    • 1995-07-11
    • US40987
    • 1993-03-31
    • Tsuneo KusamaTsunehiko SogaAkiko Tohgo
    • Tsuneo KusamaTsunehiko SogaAkiko Tohgo
    • C07H15/04C07H5/04C07H11/04C07H13/02
    • C07H15/04
    • A compound represented by formula (I): ##STR1## wherein R.sup.1 represents --CO--Z.sup.1 --N(Z.sup.11)--CO--Z.sup.2 --H or --CO--Z.sup.3 --H, wherein Z.sup.1, Z.sup.2, and Z.sup.3 each represent an alkylene group having from 1 to 20 carbon atoms, a phenylene group, or a combination thereof, and Z.sup.11 represents a hydrogen atom, an alkyl group having from 1 to 20 carbon atoms which may be substituted with a phenyl group, a phenyl group which may be substituted with an alkyl group having from 1 to 20 carbon atoms, or an alkylene group having from 1 to 20 carbon atoms which may contain therein a phenylene group; R.sup.2 represents --CO--Z.sup.4 --N(Z.sup.12)--CO--Z.sup.5 --H, --CO--Z.sup.6 --H or a hydrogen atom, wherein Z.sup.4, Z.sup.5, and Z.sup.6 each have the same meaning as Z.sup.1, and Z.sup.12 has the same meaning as Z.sup.11 ; Q.sup.1 and Q.sup.2 each represent a carboxyl group or a phosphonoxy group; Q.sup.3 represents a hydrogen atom, a carboxyl group or a phosphonoxy group; m represents 0 or an integer of from 1 to 20; n represents 0 or an integer of from 1 to 20; Y.sup.1 represents an alkylene group having from 1 to 10 carbon atoms which may contain one or more substituents selected from --OCOR.sup.11 and --NHCOR.sup.12, wherein R.sup.11 represents --Z.sup.13 or --Z.sup.7 --N (Z.sup.14)--CO--Z.sup.8 --H (wherein Z.sup.7 and Z.sup.8 each have the same meaning as Z.sup.1, and Z.sup.13 and Z.sup.14 each have the same meaning as Z.sup.11) and R.sup.12 represents --Z.sup.15 or --Z.sup.9 --N(Z.sup.16)--CO--Z.sup.10 --H (wherein Z.sup.9 and Z.sup.10 each have the same meaning as Z.sup.1, and Z.sup.15 and Z.sup.16 each have the same meaning as Z.sup.11), and a salt thereof. The compound inhibits TNF derivation by endotoxin and is therefore useful for the treatment of multiorganic insufficiencies.
    • 由式(I)表示的化合物:其中Z 1,Z 2和Z 3各自表示具有1至20个碳原子的亚烷基,亚苯基或其组合,和 Z 11表示氢原子,可以被苯基取代的碳原子数1〜20的烷基,可以被碳原子数1〜20的烷基取代的苯基或具有碳原子数1〜20的亚烷基 可含有亚苯基的1至20个碳原子; R2表示-CO-Z4-N(Z12)-CO-Z5-H,-CO-Z6-H或氢原子,其中Z4,Z5和Z6各自与Z1相同,Z12具有相同的含义 如Z11; Q1和Q2各自表示羧基或膦酰氧基; Q3表示氢原子,羧基或膦氧基; m表示0或1〜20的整数, n表示0或1〜20的整数, Y1表示可含有一个或多个选自-OCOR 11和-NHCOR 12的取代基的具有1至10个碳原子的亚烷基,其中R11表示-Z13或-Z7-N(Z14)-CO-Z8-H(其中Z7和 Z 8各自具有与Z1相同的含义,Z 13和Z 14各自具有与Z 11相同的含义,R 12表示-Z 15或-Z 9 -N(Z 16)-CO-Z 10 -H(其中Z 9和Z 10各自具有相同的含义 Z1,Z15和Z16各自具有与Z11相同的含义)及其盐。 该化合物通过内毒素抑制TNF衍生,因此可用于治疗多机能不足。