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TREATMENT OF IMMUNE DISEASES MEDIATED BY TYPE 2 ASSISTANT CELLS.

机译:2型辅助细胞介导的免疫疾病的治疗。

摘要

The use of a compound selected from the group consisting of the retinoid antagonists a) RAR-alpha- antagonists of formulas in which R1 is C5-10 alkyl, and R2 and R3 independently of each other are hydrogen or fluorine; b) RAR-alpha beta antagonists of formulas in which R4 is diamantil, X is O or NH, R5 is phenyl or benzyl, and in which optionally ring A or ring B are optionally present; c) RAR-beta, gamma antagonists of the formula wherein R6 and R7 are independently of each other hydroxy, C1-4 alkoxy, optionally branched C1-5 alkyl or adamantyl; d) RAR-gamma antagonists of formulas e) RAR-alpha, beta, gamma antagonists of formulas in which Y is -CH2- or sulfur and Z is -CH = or nitrogen, and R8 is hydrogen or C1-4 alkyl ; f) RXR antagonists of the formula in which the dotted bond is optional; and, when the dotted bond is present, R9 is methyl and R10 is hydrogen; and, when the dotted bond is not present, R9 and R10 together are methylene to form a cis-substituted cyclopropyl ring; R11 is C1-4 alkoxy; and pharmaceutically acceptable salts, and pharmaceutically acceptable hydrolysable esters thereof, as an active ingredient for the preparation of a medicament for the treatment of immune diseases mediated by type 2 helper T cells (Th2), such as allergic diseases mediated by immunoglobulin E (IgE), or for the treatment of immune diseases mediated by Th2-related cytokines, such as IL-4 and IL-5, in which the active ingredient is used in combination with a pharmaceutically acceptable carrier.
机译:选自类视黄醇拮抗剂的化合物的使用a)下式的RAR-α-拮抗剂:其中R1是C5-10烷基,且R2和R3彼此独立地是氢或氟; b)下式的RAR-αβ拮抗剂,其中R 4是二苯甲基,X是O或NH,R 5是苯基或苄基,并且任选存在环A或环B; c)下式的RAR-β,γ拮抗剂,其中R 6和R 7彼此独立地是羟基,C 1-4烷氧基,任选地支链的C 1-5烷基或金刚烷基; d)通式为RAR-γ的拮抗剂e)通式为RAR-α,β,γ的拮抗剂,其中Y为-CH 2-或硫,Z为-CH =或氮,R 8为氢或C 1-4烷基; f)式中的RXR拮抗剂,其中点键是任选的;当存在点键时,R9为甲基,R10为氢。当不存在点键时,R9和R10一起为亚甲基,形成顺式取代的环丙基环; R11为C1-4烷氧基;及其药学上可接受的盐及其药学上可接受的水解酯,作为活性成分,用于制备用于治疗由2型辅助T细胞(Th2)介导的免疫疾病,例如由免疫球蛋白E(IgE)介导的过敏性疾病的药物或用于治疗由Th2相关细胞因子介导的免疫疾病,例如IL-4和IL-5,其中活性成分与可药用载体结合使用。

著录项

  • 公开/公告号ES2270537T3

    专利类型

  • 公开/公告日2007-04-01

    原文格式PDF

  • 申请/专利权人 F. HOFFMANN-LA ROCHE AG;

    申请/专利号ES19980959850T

  • 申请日1998-11-05

  • 分类号A61K9/06;A61K31/38;A61K9/08;A61K9/107;A61K9/12;A61K9/14;A61K9/20;A61K9/48;A61K9/72;A61K31/166;A61K31/19;A61K31/192;A61K31/195;A61K31/196;A61K31/20;A61K31/201;A61K31/202;A61K31/216;A61K31/35;A61K31/352;A61K31/353;A61K31/382;A61K31/385;A61K31/407;A61K31/415;A61K31/4162;A61K31/4184;A61K31/44;A61K31/4439;A61K31/55;A61K31/551;A61K31/5513;A61K45;A61P11;A61P11/02;A61P11/06;A61P17;A61P27/16;A61P29;A61P37;A61P37/06;A61P37/08;A61P43;C07C57/42;C07C57/48;C07D235/02;C07D243/38;C07D311/58;C07D335/06;C07D339/02;C07D401/06;C07D495/04;

  • 国家 ES

  • 入库时间 2022-08-21 20:54:35

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