首页> 外国专利> isolated compound, isolated cyclo {{(e) - and (z) - (2s, 3r, 4r) -3-hydroxy-4-methyl-2- (methylamino) -6,8-nonadien oil} -1- 2-Aminobutyryl-n-methyl-glycyl-n-methyl-1-leucyl-lv-allyl-n-methyl-1-leucyl-1-alanyl-d-alanyl-n-methyl-1-leucyl-n-methyl-1 -leucyl-n-methyl-1-valyl} (isa247) and their pharmaceutically acceptable salts and solvates, method of preparing isa247 metabolites in vitro, method of producing an isa247 hydroxylated metabolite, isolated isa247 hydroxylated metabolite, isolated hydroxylated metabolite, method of producing an isa247 epoxide metabolite in vitro, isolated isa247 epoxide metabolite, isolated epoxide metabolite, method of producing an isa247 diol metabolite in vitro, isa247 isolated diol metabolite, metabolite diol isolated, method of producing an isa247 diol metabolite, method of producing an isa247 diol metabolite and pharmaceutical composition

isolated compound, isolated cyclo {{(e) - and (z) - (2s, 3r, 4r) -3-hydroxy-4-methyl-2- (methylamino) -6,8-nonadien oil} -1- 2-Aminobutyryl-n-methyl-glycyl-n-methyl-1-leucyl-lv-allyl-n-methyl-1-leucyl-1-alanyl-d-alanyl-n-methyl-1-leucyl-n-methyl-1 -leucyl-n-methyl-1-valyl} (isa247) and their pharmaceutically acceptable salts and solvates, method of preparing isa247 metabolites in vitro, method of producing an isa247 hydroxylated metabolite, isolated isa247 hydroxylated metabolite, isolated hydroxylated metabolite, method of producing an isa247 epoxide metabolite in vitro, isolated isa247 epoxide metabolite, isolated epoxide metabolite, method of producing an isa247 diol metabolite in vitro, isa247 isolated diol metabolite, metabolite diol isolated, method of producing an isa247 diol metabolite, method of producing an isa247 diol metabolite and pharmaceutical composition

机译:分离的化合物,分离的环{{(e)-和(z)-(2s,3r,4r)-3-羟基-4-甲基-2-(甲基氨基)-6,8-壬二烯油} -1- 2-氨基丁酰基-正甲基-甘氨酰基-正甲基-1-亮氨酰-lv-烯丙基-正甲基-1-亮氨酰-1-丙氨酰基-d-丙氨酰基-正甲基-1-亮氨酰-正丙基甲基-n-甲基-1-亮氨酰基-n-甲基-1-戊基}(isa247)及其药学上可接受的盐和溶剂化物,体外制备isa247代谢物的方法,生产isa247羟基化代谢物的方法,分离的isa247羟基化代谢物,分离的羟基化代谢物,体外isa247环氧代谢物,分离的isa247环氧代谢物,分离的环氧代谢物,体外生产isa247二醇代谢物的方法,isa247分离的二醇代谢物,代谢物二醇的分离,生产isa247二醇代谢物的方法,生产isa247二醇代谢物的方法和药物组合物

摘要

ISOLATED COMPOUND, ISOLATED CYCLE METABOLITE {{(E) - E (Z) - (2S, 3R, 4R) -3-HYDROXY-4-METHYL-2- (METHYLAMINO) -6,8-NONADIENOIL} -L-2 -AMINOBUTYL-N-METHYL-GLYCIL-N-METHYL-L-LEUCIL-L-VALIL-N-METHYL-L-LEUCIL-D-ALANYL-N-METI LL-LEUCIL-N-METHYL-L- LEUCILI-N-METIL-L-VALAL} (ISA247) AND PHARMACEUTICALLY ACCEPTABLE SALTS AND SOLVATES OF THE SAME, ISA247 IN VITRO METABOLITE PREPARATION METHOD, METHYLITE HYDRO ISOLATED HYDROXIDE METHOLITE7 PRODUCT METHOD HYDROXYLATE ISOLATED, ISA247 IN VITRO EPOXIDE METABOLITE PRODUCTION METHOD, ISA247 EPOXIDE ISOLATED METABOLITE, IS724 DIOLITE ISOLATED METABOLITE ISOLATED7 METABOLITE ISOLATED EPOXIDE METABOLIT ISOLATED DIOL, ISA247 DIOL METABOLITE PRODUCTION METHOD, ISA247 DIOL METABOLITE PRODUCTION METHOD AND PHARMACEUTICAL COMPOSITION. These are metabolites isolated from the cyclosporine analog ISA247, including in vitro methods for their preparation. The metabolites comprise a chemical modification of ISA247, wherein the modification is at least one reaction selected from the group consisting of hydroxylation, N-demethylation, diol formation, epoxide formation, and intramolecular cyclization, phosphorylation, sulfation, glucuronide formation. and glycosylation. Methods of preparation include semi-synthetic methods, in which ISA247 metabolites are produced from microsomal extracts of animal liver cells, or from cultures using microorganisms, and fully synthetic methods, such as chemical modification of the parent compound or of isolated metabolites using organic synthetic methods.
机译:隔离的化合物,循环的代谢物{{(E)-E(Z)-(2S,3R,4R)-3-羟基-4-甲基-2-(甲基亚氨基)-6,8-壬二酚} -L-2-氨基丁基-N-甲基-甘氨酸-N-甲基-L-基-L-缬氨酸-N-甲基-L-基-D-芳基-N-基-L-VALAL}(ISA247)和该药物的药学可接受的盐和溶剂,ISA247体外代谢物制备方法,亚甲基羟基分离的氢氧化物METHOLITE7产品方法,羟基分离的羟基化合物,ISA247环氧化合物间苯二酚的代谢物,隔离的代谢物隔离的7代谢物隔离的环氧代谢物隔离的DIOL,ISA247 DIOL代谢物的制备方法,ISA247 DIOL代谢物的制备方法和药物组合物。这些是从环孢菌素类似物ISA247分离的代谢物,包括体外制备方法。代谢物包括ISA247的化学修饰,其中该修饰是选自羟基化,N-去甲基化,二醇形成,环氧化物形成和分子内环化,磷酸化,硫酸化,葡糖醛酸苷形成的至少一种反应。和糖基化。制备方法包括半合成方法,其中从动物肝细胞的微粒体提取物或使用微生物的培养物生产ISA247代谢物,以及完全合成的方法,例如使用有机合成方法对母体化合物或分离的代谢物进行化学修饰。

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