首页> 外国专利> (1R, 9S, 12S, 13R, 14S, 17R, 18E, 21S, 23S, 24R, 25S, 27R) -12 - ((1E) -2 - ((1R, 3R, 4S) -4-chloro-3- méthoxycyclohenyl) -17-ethyl-1,14-dihydroxy-23.25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo (22.3.1.04,9) octacos-18-ene-2 , 3,10,16-tetraone or 4 '-epichloro-4' deoxyascomycin; in any form including, where appropriate, its salts and esters

(1R, 9S, 12S, 13R, 14S, 17R, 18E, 21S, 23S, 24R, 25S, 27R) -12 - ((1E) -2 - ((1R, 3R, 4S) -4-chloro-3- méthoxycyclohenyl) -17-ethyl-1,14-dihydroxy-23.25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo (22.3.1.04,9) octacos-18-ene-2 , 3,10,16-tetraone or 4 '-epichloro-4' deoxyascomycin; in any form including, where appropriate, its salts and esters

机译:(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-12-((1E)-2-(((1R,3R,4S)-4-chloro-3-甲氧基环hen基)-17-乙基-1,14-二羟基-23.25-二甲氧基-13,19,21,27-四甲基-11,28-二恶唑-4-氮杂三环(22.3.1.04,9)octacos-18-ene-2 ,3,10,16-四酮或4“ -epichloro-4”脱氧阿霉素(以适当的形式包括其盐和酯)

摘要

The invention concerns the compounds of formula I CHEM wherein the substituents have various significances. They are prepared by several processes including epimerizing replacement, treatment with cyanogen bromide or thiophosgene, treatment with an acid having a non-nucleophilic anion, treatment with dimethylsulfoxide and acetic anhydride, acylation, treatment with an oxalyl derivative and ammonia, methylation, oxidation, deprotection and protection. They possess interesting pharmacological activity as antiinflammatory, immunosuppressant, antiproliferative and chemotherapeutic drug resistance reversing agents.
机译:本发明涉及式I 的化合物,其中所述取代基具有各种意义。它们通过几种方法制备,包括差向异构取代,溴化氰或硫光气处理,具有非亲核阴离子的酸处理,二甲基亚砜和乙酸酐处理,酰化,草酰衍生物和氨处理,甲基化,氧化,脱保护和保护。它们具有令人感兴趣的药理活性,如抗炎药,免疫抑制剂,抗增殖药和化学治疗药耐药性逆转剂。

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