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1. (WO2012176587) NOVEL COMPOUND WITH AMYLOID AFFINITY
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2012/176587 International Application No.: PCT/JP2012/063726
Publication Date: 27.12.2012 International Filing Date: 29.05.2012
IPC:
C07D 471/04 (2006.01) ,A61K 51/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51
Preparations containing radioactive substances for use in therapy or testing in vivo
Applicants:
日本メジフィジックス株式会社 NIHON MEDI-PHYSICS CO., LTD. [JP/JP]; 東京都江東区新砂3丁目4番10号 3-4-10, Shinsuna, Koto-ku, Tokyo 1360075, JP (AllExceptUS)
奥村 侑紀 OKUMURA Yuki [JP/JP]; JP (UsOnly)
眞矢 啓史 MAYA Yoshifumi [JP/JP]; JP (UsOnly)
正山 祥生 SHOYAMA Yoshinari [JP/JP]; JP (UsOnly)
大西 崇子 ONISHI Takako [JP/JP]; JP (UsOnly)
Inventors:
奥村 侑紀 OKUMURA Yuki; JP
眞矢 啓史 MAYA Yoshifumi; JP
正山 祥生 SHOYAMA Yoshinari; JP
大西 崇子 ONISHI Takako; JP
Agent:
井出正威 IDE Masatake; 東京都千代田区五番町3-1五番町グランドビル9階井出国際特許事務所 M. IDE & CO., 9F, Gobancho Grand Bldg., 3-1, Gobancho, Chiyoda-ku, Tokyo 1020076, JP
Priority Data:
2011-14006924.06.2011JP
Title (EN) NOVEL COMPOUND WITH AMYLOID AFFINITY
(FR) NOUVEAU COMPOSÉ AYANT UNE AFFINITÉ POUR L'AMYLOÏDE
(JA) 新規アミロイド親和性化合物
Abstract:
(EN) [Problem] To obtain: a compound effective as a diagnostic imaging probe that targets amyloid; and an Alzheimer's diagnostic agent that incorporates the compound therein. [Solution] A compound represented by formula (1) (In the formula, R1 represents a radioactive halogen substituent, and while 0-2 of A1, A2, A3 and A4 represent N, the remainder represent CH.) or a salt thereof, and an Alzheimer's diagnostic agent obtained by incorporating the compound represented by formula (1) or a salt thereof. This compound and this Alzheimer's diagnostic agent enter the brain following administration, and exhibit favorable clustering properties toward amyloid deposited in the brain.
(FR) L'invention a pour but d'obtenir : un composé efficace comme sonde d'imagerie diagnostique qui cible l'amyloïde ; et un agent de diagnostic d'Alzheimer qui incorpore le composé dans celui-ci. A cet effet, l'invention concerne un composé représenté par la formule (1) (dans la formule, R1 représente un substituant halogène radioactif et, alors que 0-2 de A1, A2, A3 et A4 représentent N, le reste représente CH) ou un sel de celui-ci, et un agent de diagnostic d'Alzheimer obtenu par incorporation du composé représenté par la formule (1) ou d'un sel de celui-ci. Ce composé et cet agent de diagnostic d'Alzheimer entrent dans le cerveau suite à une administration et présentent des propriétés favorables de formation d'agrégat à l'encontre de l'amyloïde déposée dans le cerveau.
(JA) 【課題】アミロイドを標的とした画像診断プローブとして有効な化合物及び該化合物を配合したアルツハイマー病診断剤を得る。 【解決手段】下記式(1):(式中、Rは放射性ハロゲン置換基、A1、A2、A3及びA4のうち0~2個がNであり残りはCHである。)で表される化合物又はその塩、及び前記式(1)で表される化合物又はその塩を配合してなるアルツハイマー病診断剤。本化合物及び本アルツハイマー病診断剤は、投与後脳内に移行し、脳に沈着したアミロイドへの良好な集積性を示す。
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)
Also published as:
CA2839199CN103596950EP2725027US20140121377JPWO2012176587KR1020140040735
AU2012274639ES2619830IN185/DELNP/2014