公开(公告)号：US08956589B2

公开(公告)日：2015-02-17

申请号：US13203589

申请日：2010-02-26

申请人： Ikuo Tooyama ,  Hiroyasu Taguchi ,  Shigehiro Morikawa ,  Makoto Urushitani ,  Daijiro Yanagisawa ,  Tomone Nagae ,  Nobuaki Shirai ,  Koichi Hirao ,  Masanari Kato ,  Hirohiko Kimura ,  Takashi Okada

发明人： Ikuo Tooyama ,  Hiroyasu Taguchi ,  Shigehiro Morikawa ,  Makoto Urushitani ,  Daijiro Yanagisawa ,  Tomone Nagae ,  Nobuaki Shirai ,  Koichi Hirao ,  Masanari Kato ,  Hirohiko Kimura ,  Takashi Okada

IPC分类号： A61K49/06 ,  C07C69/738 ,  A61K31/12 ,  G01N33/68 ,  A61K49/10 ,  A61K51/04 ,  C07C49/255 ,  C07C59/70 ,  C07C59/90 ,  C07C225/22 ,  C07C235/78 ,  C07C255/40 ,  C07D213/50 ,  C07D307/46

CPC分类号： G01N33/6896 ,  A61K49/10 ,  A61K51/04 ,  C07C49/255 ,  C07C59/70 ,  C07C59/90 ,  C07C69/738 ,  C07C225/22 ,  C07C235/78 ,  C07C255/40 ,  C07D213/50 ,  C07D307/46 ,  G01N33/6839 ,  G01N2800/2821

摘要： Disclosed are a curcumin derivative or a salt thereof, which contains a fluorine atom, represented by formula (I): (wherein R1a and R1b are each independently a hydrogen atom, alkyl, acetyl, or methoxycarbonyl; R2s are each independently a fluorine atom, CHF2—, CF3—, CHF2O—, or CF3O—; R3s are each independently a hydrogen atom or a fluorine atom; A is alkyl, cyano, carboxyl, alkoxycarbonyl, or R4—(CH2)m—; R4 is hydroxy, carboxy, cyano, acetyloxy, alkoxycarbonyl, alkoxyalkoxy, hydroxyalkoxy, or CONR5R6; R5 and R6 are each independently a hydrogen atom or alkyl; and m is an integer from 1 to 5), and a diagnostic imaging agent for diagnosing a disease in which an amyloid β peptide aggregate accumulates, the diagnostic imaging agent containing a compound having a 1,3-dicarbonyl structure, wherein the compound exists in a keto form and an enol form, and the keto form and the enol form have different affinities, respectively, to the amyloid β peptide aggregate.

摘要翻译： 公开了含有由式（I）表示的氟原子的姜黄素衍生物或其盐：其中R 1a和R 1b各自独立地为氢原子，烷基，乙酰基或甲氧基羰基; R 2各自独立地为氟原子， CH 2 - ，CF 3 - ，CHF 2 O-或CF 3 O-; R 3各自独立地为氢原子或氟原子; A为烷基，氰基，羧基，烷氧基羰基或R 4 - （CH 2）m - ; R 4为羟基， 氰基，乙酰氧基，烷氧基羰基，烷氧基烷氧基，羟基烷氧基或CONR5R6; R5和R6各自独立地为氢原子或烷基; m为1至5的整数），以及用于诊断淀粉样蛋白和bgr的疾病的诊断显像剂 ; 肽聚集体积累，诊断成像剂含有具有1,3-二羰基结构的化合物，其中化合物以酮形式和烯醇形式存在，酮形式和烯醇形式分别具有与淀粉样蛋白不同的亲和力 ＆bgr 肽聚集体。

公开(公告)号：US20110311444A1

公开(公告)日：2011-12-22

申请号：US13203589

申请日：2010-02-26

申请人： Ikuo Tooyama ,  Hiroyasu Taguchi ,  Shigehiro Morikawa ,  Makoto Urushitani ,  Daijiro Yanagisawa ,  Tomone Nagae ,  Nobuaki Shirai ,  Koichi Hirao ,  Masanari Kato ,  Hirohiko Kimura ,  Takashi Okada

发明人： Ikuo Tooyama ,  Hiroyasu Taguchi ,  Shigehiro Morikawa ,  Makoto Urushitani ,  Daijiro Yanagisawa ,  Tomone Nagae ,  Nobuaki Shirai ,  Koichi Hirao ,  Masanari Kato ,  Hirohiko Kimura ,  Takashi Okada

IPC分类号： A61K49/06 ,  C07C69/738 ,  A61P43/00 ,  C07C49/255 ,  C07D309/32 ,  A61K49/00 ,  G01N21/64 ,  C07C59/90

CPC分类号： G01N33/6896 ,  A61K49/10 ,  A61K51/04 ,  C07C49/255 ,  C07C59/70 ,  C07C59/90 ,  C07C69/738 ,  C07C225/22 ,  C07C235/78 ,  C07C255/40 ,  C07D213/50 ,  C07D307/46 ,  G01N33/6839 ,  G01N2800/2821

摘要： Disclosed are a curcumin derivative or a salt thereof, which contains a fluorine atom, represented by formula (I): (wherein R1a and R1b are each independently a hydrogen atom, alkyl, acetyl, or methoxycarbonyl; R2s are each independently a fluorine atom, CHF2—, CF3—, CHF2O—, or CF3O—; R3s are each independently a hydrogen atom or a fluorine atom; A is alkyl, cyano, carboxyl, alkoxycarbonyl, or R4—(CH2)m—; R4 is hydroxy, carboxy, cyano, acetyloxy, alkoxycarbonyl, alkoxyalkoxy, hydroxyalkoxy, or CONR5R6; R5 and R6 are each independently a hydrogen atom or alkyl; and m is an integer from 1 to 5), and a diagnostic imaging agent for diagnosing a disease in which an amyloid β peptide aggregate accumulates, the diagnostic imaging agent containing a compound having a 1,3-dicarbonyl structure, wherein the compound exists in a keto form and an enol form, and the keto form and the enol form have different affinities, respectively, to the amyloid β peptide aggregate.

摘要翻译： 公开了含有由式（I）表示的氟原子的姜黄素衍生物或其盐：其中R 1a和R 1b各自独立地为氢原子，烷基，乙酰基或甲氧基羰基; R 2各自独立地为氟原子， CH 2 - ，CF 3 - ，CHF 2 O-或CF 3 O-; R 3各自独立地为氢原子或氟原子; A为烷基，氰基，羧基，烷氧基羰基或R 4 - （CH 2）m - ; R 4为羟基， 氰基，乙酰氧基，烷氧基羰基，烷氧基烷氧基，羟基烷氧基或CONR5R6; R5和R6各自独立地为氢原子或烷基; m为1至5的整数），以及用于诊断淀粉样蛋白和bgr的疾病的诊断显像剂 ; 肽聚集体积累，诊断成像剂含有具有1,3-二羰基结构的化合物，其中化合物以酮形式和烯醇形式存在，酮形式和烯醇形式分别具有与淀粉样蛋白不同的亲和力 ＆bgr 肽聚集体。