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compound, method for protecting a mammal against, or treating, a virus, microbial infection, parasite, an autoimmune disease, cancer, allergy or asthma, and, pharmaceutical composition

机译:化合物,保护哺乳动物抵抗或治疗病毒,微生物感染,寄生虫,自身免疫性疾病,癌症,过敏或哮喘的方法,以及药物组合物

摘要

COMPOUND, METHOD TO PROTECT A MAMMALIAN INDIVIDUAL AGAINST, OR TREAT, A VIRUS, MICROBIAL INFECTION, PARASITE, AN AUTO-IMMUNE DISEASE, CANCER, ALLERGY OR ASTHMA, AND, PHARMACEUTICAL COMPOSITION It is described that a compound of ~ 1 formula 1 ~ represents a hydrophobic portion adapted to occupy the human CDid C 'channel, R ~ 2 ~ represents a hydrophobic portion adapted to occupy the human CD 1d A' channel, such that R ~ 1 ~ fills at least at least 30% of the volume occupied by channel C 'compared to the volume occupied by nC ~ 14 ~ H ~ 29 ~ terminal of the cx-gaLactosylceramide chain sphingosine when bound to human CD1d and R2 fills at least 30% of the occupied volume of channel A' compared with the volume occupied by the nC ~ 25 ~ H ~ 51 ~ terminal of the 244 acyl chain - galactosylceramide when bound to human CD 1 d R3 represents hydrogen ab or OH, R and R each represent hydrogen, and additionally , when R3 represents hydrogen, R ^ a ^ and R ^ b ^ together , can form a single bond, X represents either -CHA (CHOH) ~ n ~ Y or - P (~ 0) (0) 0CH ~ 2 ~ (CH0H) ~ m ~ Y, where Y represents CHB ~ 1 ~ B ~ 2 ~, n represents an integer from 1 to 4, m represents 0 or 1, A represents hydrogen, one from B ~ 1 ~ and B ~ 2 ~ represents H, OH or phenyl, and the other represents hydrogen or one from B ~ 1 ~ and B ~ 2 ~ represent hydroxy and the other represents phenyl, in addition, when n represents 4, then A together with one of B ~ 1 ~ and B ~ 2 ~ forms, together, a single bond, and the other B ~ 1 ~ and B ~ 2 ~ represents H, OH or OSO ~ 3 ~ H and pharmaceutically acceptable salts thereof; the compounds of formula 1 are indicated for use in the treatment of a virus, microbial infection, parasite, an autoimmune disease, cancer, allergy or asthma.
机译:用于预防或治疗哺乳动物个体,病毒,微生物感染,寄生虫,自体免疫疾病,癌症,过敏或哮喘的化合物,方法,以及药物组合物描述了〜1式1〜的化合物适于占据人CDid C'通道的疏水部分,R〜2〜表示适于占据人CD 1d A'通道的疏水部分,以使R〜1至少填充被CDID C'通道占据的体积的30%通道C'与人CD1d和R2结合时相比,cx-gaLactosylceramide链鞘氨醇的nC〜14〜H〜29〜末端所占的体积至少占通道A所占体积的30%通过<244>酰基链的nC〜25〜H〜51〜末端连接至人CD 1 d时的半乳糖神经酰胺R3代表氢ab或OH,R和R分别代表氢,另外,当R3代表氢时,R ^ a ^和R ^ b ^一起可以形成单键, X代表-CHA(CHOH)〜n〜Y或-P(〜0)(0)0CH〜2〜(CH0H)〜m〜Y,其中Y代表CHB〜1〜B〜2〜,n代表整数从1到4,m代表0或1,A代表氢,一个代表B〜1〜,B〜2〜代表H,OH或苯基,另一个代表氢或一个B〜1〜和B〜2〜。另外,当n代表4时,则A与B〜1〜和B〜2〜之一一起形成单键,另一个B〜1〜和B〜2 〜代表H,OH或OSO〜3〜H及其药学上可接受的盐;式1化合物被指定用于治疗病毒,微生物感染,寄生虫,自身免疫性疾病,癌症,过敏或哮喘。

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