首页> 外国专利> Use of 7-Adamantyl-naphth-2-yl(hetero)aryl carboxylic acids, derivatives thereof (retinoid analogues) in preparing medicaments; compounds having a polyether radical bound to a moiety of at least two carbon atoms in position-beta

Use of 7-Adamantyl-naphth-2-yl(hetero)aryl carboxylic acids, derivatives thereof (retinoid analogues) in preparing medicaments; compounds having a polyether radical bound to a moiety of at least two carbon atoms in position-beta

机译:7-金刚烷基-萘-2-基(杂)芳基羧酸及其衍生物(类维生素A类似物)在制备药物中的用途; β位置具有至少两个碳原子的部分键合有聚醚基的化合物

摘要

A retinoid analogue or a salt thereof or its chiral analogues has the formula (I) wherein: R1 is methyl, CH2OH, -OR3 or -CO-R4; Ar is a radical of formula (a) to (d); R2 is a polyether radical having carbon in the position a to the carbon which is in the 6th position of the naphthyl radical; R3 is H, alkyl or -(CH2)m(CO)n-R8; R4 is H, alkyl, -N(R')(R"), or -OR9; R5 is H or halogen, alkyl, hydroxy, -OR9 or -OCOOR10; R8 is alkyl or a saturated heterocycle; R9 is H, alkyl, alkenyl, mono- or polyhydroxyalkyl, optionally substituted aryl or aralkyl or a sugar residue, amino acid or peptide residue; R10 is alkyl; R' and R" are independently H, alkyl, mono- or polyhydroxyalkyl, optionally substituted aryl, or a sugar residue, amino acid or peptide residue or together can form a saturated heterocycle and m is 1 to 3. The compound is useful in treating disorders and/or aliments related to an over-regulation of RAR receptors and/or a hypervitaminosis A.
机译:类维生素A类似物或其盐或其手性类似物具有式(I),其中:R 1为甲基,CH 2 OH,-OR 3或-CO-R 4; Ar是式(a)至(d)的基团; R 2是在萘基的第6位的碳上的a位具有碳的聚醚基。 R3是H,烷基或-(CH2)m(CO)n-R8; R4为H,烷基,-N(R')(R“)或-OR9; R5为H或卤素,烷基,羟基,-OR9或-OCOOR10; R8为烷基或饱和杂环; R9为H,烷基,烯基,单或多羟烷基,任选取代的芳基或芳烷基或糖残基,氨基酸或肽残基; R 10为烷基; R'和R“独立地为H,烷基,单或多羟烷基,任选取代的芳基或糖残基,氨基酸或肽残基或一起可以形成饱和杂环,m为1至3。该化合物可用于治疗与RAR受体过度调节和/或高维生素A相关的疾病和/或饮食。

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