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O-substituted-dibenzyl urea- or thiourea- derivatives as trpv1 receptor antagonists

机译:O取代的二苄基脲或硫脲衍生物作为trpv1受体拮抗剂

摘要

The invention relates to compounds of formula (I)whereinR is halogen;R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, aminomethyl, 2-aminoethyl, 3-aminopropyl, 3-amino-2-hydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxypropen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, 4-hydroxybenzyl, and 4-aminobenzyl;R2 is O or S;R3 is tert-butyl or trifluoromethyl;n is an integer selected from 0, 1 or 2.;The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, haemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases.
机译:本发明涉及式(I)的化合物其中R为卤素;R 1 选自2-羟乙基,2,3-二羟丙基,3-羟丙基,2,2-二羟乙基,3,3-二羟丙基,氨基甲基,2-氨基乙基,3-氨基丙基,3-氨基-2-羟丙基,1,3-二氧戊环-乙基,1,3-二氧六环-甲基,1,3-二氧戊环-甲基,1,3-二氧六环-乙基,3-氟-2-羟丙基,3-氯- 2-羟丙基,2-羟丙基,2-羟丙基-2-基,吗啉代乙基,哌嗪基乙基,羟甲基,苄基,4-(羟甲基)苄基,4-氯苄基,4-氟苄基,4-羟苄基和4-氨基苄基;R 2 是O或S;R 3 是叔丁基或三氟甲基;n是选自0、1或2的整数;式(I)的化合物可用于制备用于治疗炎性状态例如慢性神经性疼痛,膀胱过度活动症,肿瘤疼痛的药物组合物。 ,痔疮,炎症性痛觉过敏,干预后疼痛,拔牙,气道和胃肠道疾病。

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