公开(公告)号：US20120149737A1

公开(公告)日：2012-06-14

申请号：US13391207

申请日：2010-09-01

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

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

IPC分类号： A61K31/4409 ,  C07D213/56 ,  A61P25/28 ,  A61K31/192 ,  A61K31/235 ,  A61K31/167 ,  C07C235/84 ,  C07C235/56

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

摘要： 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.

摘要翻译： 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。

公开(公告)号：US07145009B2

公开(公告)日：2006-12-05

申请号：US10685799

申请日：2003-10-16

申请人： David Reginald Adams ,  Jon Mark Bentley ,  James Davidson ,  Matthew Alexander James Duncton ,  Richard Hugh Phillip Porter

发明人： David Reginald Adams ,  Jon Mark Bentley ,  James Davidson ,  Matthew Alexander James Duncton ,  Richard Hugh Phillip Porter

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61P3/04

CPC分类号： C07D487/04

摘要： Chemical compounds of formula (I): and pharmaceutically acceptable salts and addition compounds and prodrugs thereof are useful in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes inspidus, and sleep apnea.

摘要翻译： 式（I）的化合物及其药学上可接受的盐和加成化合物及其前药可用于治疗，特别是用于治疗中枢神经系统疾病; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 糖尿病，睡眠呼吸暂停。

公开(公告)号：US06800627B1

公开(公告)日：2004-10-05

申请号：US09890186

申请日：2001-10-09

申请人： David Reginald Adams ,  Jon Mark Bentley ,  James Davidson ,  Matthew Alexander James Duncton ,  Richard Hugh Phillip Porter

发明人： David Reginald Adams ,  Jon Mark Bentley ,  James Davidson ,  Matthew Alexander James Duncton ,  Richard Hugh Phillip Porter

IPC分类号： C07D48704

CPC分类号： C07D487/04

摘要： Chemical compounds of formula (I): and pharmaceutically acceptable salts and addition compounds and prodrugs thereof are useful in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes inspidus, and sleep apnea.

摘要翻译： 式（I）的化合物及其药学上可接受的盐和加成化合物及其前药可用于治疗，特别是用于治疗中枢神经系统疾病; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 糖尿病，睡眠呼吸暂停。

公开(公告)号：US06552062B1

公开(公告)日：2003-04-22

申请号：US09763886

申请日：2001-02-28

申请人： David Reginald Adams ,  Jonathan Mark Bentley ,  Jonathan Richard Anthony Roffey ,  Richard John Hamlyn ,  Ashley Roger George

发明人： David Reginald Adams ,  Jonathan Mark Bentley ,  Jonathan Richard Anthony Roffey ,  Richard John Hamlyn ,  Ashley Roger George

IPC分类号： A61K31416

CPC分类号： C07D231/56

摘要： A chemical compound of formula (I) wherein R1 to R3 are independently selected from hydrogen and alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, monoalkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, arylthio, arylsulfoxyl, arylsulfonyl, alkylsulfoxyl, alkylsulfonyl, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino; and R8 is selected from alkyl and alkoxy, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

摘要翻译： 式（I）的化合物，其中R 1至R 3独立地选自氢和烷基; R4至R7独立地选自氢，卤素，羟基，烷基，芳基，氨基，单烷基氨基，二烷基氨基，烷氧基，芳氧基，烷硫基，芳硫基，芳基亚砜基，芳基磺酰基，烷基亚砜基，烷基磺酰基，硝基，氰基，甲醛，烷基羰基，芳基羰基，氨基羰基 单烷基氨基羰基，二烷基氨基羰基，烷氧基羰基氨基，氨基羰基氧基，单烷基氨基羰基氧基，二烷基氨基羰基氧基，单烷基氨基羰基氨基和二烷基氨基羰基氨基; 并且R 8选自烷基和烷氧基及其药学上可接受的盐和前药，及其在治疗中的用途，特别是用于治疗中枢神经系统疾病的用途; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 尿崩症和睡眠呼吸暂停，特别是用于治疗肥胖。