公开(公告)号：US20160039747A1

公开(公告)日：2016-02-11

申请号：US14879340

申请日：2015-10-09

Applicant: Kings College London

Inventor： Jonathan Patrick Thomas Corcoran ,  Sarkis Barret Kalindjian ,  Alan David Borthwick ,  David Reginald Adams ,  Jane Theresa Brown ,  David Michel Adrien Taddei ,  Jason John Shiers

IPC: C07C235/84

CPC classification number: C07C235/84 ,  C07C233/75 ,  C07C235/56 ,  C07C237/42 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/30 ,  C07D213/80 ,  C07D213/81 ,  C07D237/24

Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as “AAA compounds”), which, inter alia, are (selective) retinoic acid receptor α (RARα) 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 RARα, and in the treatment of diseases and conditions that are mediated by RARα, that are ameliorated by the activation of RARα, etc., including cognitive disorders, memory impairment, memory deficit, senile dementia, Alzheimer's disease, early stage Alzheimer's disease, intermediate stage Alzheimer's disease, late stage Alzheimer's disease, cognitive impairment, and mild cognitive impairment.

Abstract translation: 本发明一般涉及治疗化合物的领域，更具体地涉及以下式的某些芳基 - 酰氨基 - 芳基化合物（为了方便起见，统称为“AAA化合物”），其特别是（选择性的 ）视黄酸受体α（RARα）激动剂。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途（选择性地）激活RARα，以及在治疗由RARα介导的疾病和病症中的应用， 通过RARα等的激活改善，包括认知障碍，记忆障碍，记忆缺陷，老年痴呆，阿尔茨海默病，早期阿尔茨海默氏病，中期阿尔茨海默病，晚期阿尔茨海默氏病，认知障碍和轻度认知障碍。