[EN] CRYSTALLINE FORMS OF 4-(5-(4,7-DIMETHYLBENZOFURAN-2-YL)-1,2,4-OXADIAZOL-3-YL)BENZOIC ACID AND PROCESSES FOR THEIR PREPARATION<br/>[FR] FORMES CRISTALLINES DE L'ACIDE 4-(5-(4,7-DIMÉTHYLBENZOFURAN-2-YL)-1,2,4-OXADIAZOL-3-YL) BENZOÏQUE ET LEURS PROCÉDÉS DE PRÉPARATION
申请人:KING'S COLLEGE LONDON
公开号:WO2017220446A1
公开(公告)日:2017-12-28
The present invention pertains generally to the field of therapeutic compounds, and more specifically to crystalline forms of 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid (referred to herein as "BHBA-001"), which, inter alia, is a (selective) retinoic acid receptor beta (RARβ) (e.g., RARβ2) agonist. The present invention also pertains to pharmaceutical compositions comprising such crystalline forms, and the use of such crystalline forms and compositions, both in vitro and in vivo, to (selectively) activate RARβ (e.g., RARβ2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RARβ (e.g., RARβ2), that are ameliorated by the activation of RARβ (e.g., RARβ2), etc., including, e.g., neurological injuries such as spinal cord injuries.
本发明一般涉及治疗化合物领域,更具体地涉及4-(5-(
4,7-二甲基苯并呋喃-2-基)-1,2,4-噁二唑-3-基)
苯甲酸的结晶形式(以下简称为"BHBA-001"),该化合物是一种(选择性)
视黄酸受体β(RARβ)(例如RARβ2)激动剂。本发明还涉及包含这种结晶形式的药物组合物,以及利用这种结晶形式和组合物在体内外(选择性地)激活RARβ(例如RARβ2),促进神经元发育、神经元生长和/或神经元再生,以及治疗通过RARβ(例如RARβ2)介导的疾病和症状,通过激活RARβ(例如RARβ2)得到改善等。这些疾病和症状包括神经系统损伤如脊髓损伤。