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

• Main Authors: BROWN JANE THERESA, DE CASTRO VASCONCELOS GONCALVES MARIA BEATRIZ, BORTHWICK ALAN DAVID, MILLS MARK TREVOR, CORCORAN JONATHAN PATRICK THOMAS, KALINDJIAN SARKIS BARRET
• Format: Patent
• Language: English; Korean
• Published: 25.08.2017
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

본 발명은 치료 화합물 분야, 그리고 더욱 구체적으로는 다음 화학식의 특정한 바이사이클로헤테로아릴-헤테로아릴-벤조산 화합물 (편의상, 본 출원에서 집합적으로 "BHBA 화합물"로 지칭됨),, (선택적) 레티노산 수용체 베타 (RARβ) (예컨대, RARβ2) 작동제에 관한 것이다. 본 발명은 또한 이러한 화합물을 포함하는 제약학적 조성물 그리고, RARβ (예컨대, RARβ2)를 (선택적으로) 활성화시키기 위한, 신경돌기 발달, 신경돌기 성장, 및/또는 신경돌기 재생을 유발 또는 촉진시키기 위한, 그리고 RARβ (예컨대, RARβ2)에 의해 매개되는, RARβ (예컨대, RARβ2)의 활성화에 의해 개선되는 등의 질환 및 병태, 예컨대, 신경학적 손상, 가령, 척수 손상을 비롯한 질환 및 병태의 치료에 있어서, 이러한 화합물과 조성물의및모두에서의 용도에 관한 것이다. 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 (RARβ) (e.g., RARβ2) 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 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.