首页> 外国专利> PURINERGIC AND PYRIMIDINERGIC RECEPTOR AGONISTS FOR THE TREATMENT OF ACTIVATED CD4+ T LYMPHOCYTE-MEDIATED IMMUNE DISEASES

PURINERGIC AND PYRIMIDINERGIC RECEPTOR AGONISTS FOR THE TREATMENT OF ACTIVATED CD4+ T LYMPHOCYTE-MEDIATED IMMUNE DISEASES

机译:用于治疗活化的CD4 + T淋巴细胞介导的免疫疾病的脓毒症和感冒药受体激动剂

摘要

The present invention in particular relates to the use of purinergic and pyrimidinergic receptor agonists of formula (1) or a pharmaceutically acceptable salt thereof for inhibition of CD4+ T lymphocytes activation or as an immunosuppressive agent, wherein B1 is adenine or uracil, optionally substituted by thioalkyl, R1 and R2 represent each independently OH, H, OR7, OCOR7, OCOR7COR7, wherein R7 represents alkyl or aryl and X is of formula (2), (3) or (4), wherein R10 represents hydrogen or is of formula (7),wherein B2 is selected from the group comprising adenine, uracil, thymine, cytosine, guanine, xanthine and hypoxanthine, optionally substituted by thioalkyl, wherein n is 0, 1, 2, 3 or 4, and wherein R4, R4a and R4b represent each independently O, NH, alkylene, monohaloalkylene or dihaloalkylene and R3, R5, R6, R8, R9 represent each independently OH or SH, and wherein R11 and R12 represent each independently OH, H, OR7, OCOR7, OCOR7COR7, wherein R7 is as defined above.
机译:本发明特别涉及式(1)的嘌呤能和嘧啶能受体激动剂或其药学上可接受的盐用于抑制CD4 + T淋巴细胞活化或用作免疫抑制剂的用途,其中B 1是腺嘌呤或尿嘧啶,任选地被硫代烷基取代,R 1和R 2分别独立地表示OH,H,OR 7,OCOR 7,OCOR 7 COR 7,其中R 7表示烷基或芳基和X为式(2),(3)或(4),其中R 10代表氢或为式(7),其中B 2选自腺嘌呤,尿嘧啶,胸腺嘧啶,胞嘧啶,鸟嘌呤,黄嘌呤和次黄嘌呤,任选地被硫代烷基取代,其中n为0、1、2、3或4,并且其中R 4,R 4a和R 4b各自独立地表示O,NH,亚烷基,单卤代亚烷基或二卤代亚烷基和R 3,R 5,R 6,R 8,R 9各自独立地表示OH或SH,并且其中R 11和R 12各自独立地表示OH,H,OR <7>,OCOR <7>,OCOR <7> CO R 7,其中R 7如上所定义。

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