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BICYCLOHETEROARYL-HETEROARYL-BENZOIC ACID COMPOUNDS AS RETINOIC ACID RECEPTOR BETA (RAR.BETA.) AGONISTS

机译:双环戊芳基-杂芳基-苯甲酸化合物作为视黄酸受体β(RAR.BETA。)激动剂

摘要

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicycloheteroaryl-heteroaryl-benzoic acid compounds of the following formula (for convenience, collectively referred to herein as "BHBA compounds"), which, inter alia, are (selective) retinoic acid receptor beta (RARß) (e.g., RARß2) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RARß (e.g., RARß2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RARß (e.g., RARß2), that are ameliorated by the activation of RARß (e.g., RARß2), etc., including, e.g., neurological injuries such as spinal cord injuries.
机译:本发明总体上涉及治疗化合物的领域,并且更具体地涉及某些下式的双环杂芳基-杂芳基-苯甲酸化合物(为了方便起见,在本文中统称为“ BHBA化合物”),其尤其是:选择性)视黄酸受体β(RARß)(例如RARß2)激动剂。本发明还涉及包含此类化合物的药物组合物,以及此类化​​合物和组合物在体外和体内在(选择性地)激活RARß(例如RARß2),引起或促进神经突发育,神经突增生,和/或神经突再生,以及在由RARß(例如RARß2)介导的疾病和病症的治疗中,由于RARß(例如RARß2)的激活等而得到改善,包括例如神经损伤等脊髓损伤。

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