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    • 5. 发明申请
    • IMAGING AGENTS FOR DETECTING NEUROLOGICAL DISORDERS
    • 用于检测神经疾病的成像剂
    • WO2011119565A1
    • 2011-09-29
    • PCT/US2011/029368
    • 2011-03-22
    • SIEMENS MEDICAL SOLUTIONS USA, INC.CASHION, Daniel, KurtCHEN, GangKASI, DhanalakshmiKOLB, Hartmuth C.LIU, ChanghuiSINHA, AnjanaSZARDENINGS, Anna, KatrinWANG, EricYU, ChulZHANG, WeiGANGADHARMATH, Umesh, B.WALSH, Joseph, C.
    • CASHION, Daniel, KurtCHEN, GangKASI, DhanalakshmiKOLB, Hartmuth C.LIU, ChanghuiSINHA, AnjanaSZARDENINGS, Anna, KatrinWANG, EricYU, ChulZHANG, WeiGANGADHARMATH, Umesh, B.WALSH, Joseph, C.
    • C07D235/04C07D401/02A61K31/4184A61K31/4353A61P25/00
    • C07D235/04A61K51/04C07B59/002C07D215/06C07D235/14C07D277/62C07D401/02C07D401/04C07D403/06C07D413/10C07D413/14C07D471/04C07D487/04
    • Imaging agents of formulas (I)-(V) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formulas (I)-(V) capable of binding to tau proteins and β-amyloid peptides are presented herein. The invention also relates to methods of imaging Αβ and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formulas (I)-(V) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders. Formula (V) or a pharmaceutically acceptable salt thereof, and stereoisomers thereof, wherein: X 25 -X 28 are each independently CH, CR 11 , or N; X 29 is CH, N, O or S; X 30 is CH, C, or N; X 31-34 are each independently CH, CR 12 , CR 13 or N; RII-RU are each independently H, halogen, hydroxy, nitro, cyano, ammo, alkyl, alkylaryl, alkylamino, alkylamine, arylamine, arylamino, alkoxy,— (O-CH 2 - CH 2 ) n -, alkenyL alkynyl, aryloxy, NRl0COOalkyl, NRl0 COOaryU NRW COalkyl, NR 10 CO aryl, COOalkyl, COOaryl, COalkyl, COaryl, aryl, cycloalkyl, cycloalkylamino, cycloalkylamine, bicyclic, saturated heterocycle and unsaturated heterocycle, wherein at least one carbon of R 11 -R 13 is optionally replaced with N, Q, S, triazole, or halo, and, wherein at least one hydrogen is optionally replaced with halo, amine, amino, alkoxy, nitro, alkyl, alkenyL alkynyl, aryloxy, alkylaryl, alkylamino, alkylamine, NRioCOOalkyl, NR 10 COOaryl, NR 10 COalkyl, NR,0 CO aryl, COOalkyl, COOaryl, COalkyl, COaryl, aryl, cycloalkyl, cycloalkylamino, cycloalkylamine, bicyclic saturated heterocycle and unsaturated heterocycle, a leaving group, CN, OH or a radioactive isotope.
    • 式(I) - (V)的成像剂和用于检测神经障碍的方法包括向需要的患者施用能够结合tau蛋白和β-淀粉样肽的式(I) - (V)化合物。 本发明还涉及成像β和tau聚集体的方法,包括引入可检测量的包含放射性标记的式(I) - (V)化合物的药物制剂,并检测与淀粉样蛋白沉积物和/或tau蛋白相关的标记化合物 患者。 这些方法和组合使得临床前诊断和监测AD和其他神经障碍的进展。 式(V)或其药学上可接受的盐及其立体异构体,其中:X25-X28各自独立地为CH,CR11或N; X29是CH,N,O或S; X30是CH,C或N; X31-34各自独立地为CH,CR12,CR13或N; RII-RU各自独立地为H,卤素,羟基,硝基,氰基,氨基,烷基,烷基芳基,烷基氨基,烷基胺,芳基胺,芳基氨基,烷氧基, - (O-CH 2 -CH 2)n - 烯基炔基,芳氧基,NR 10 COO烷基, NR10 COOaryU NRW CO烷基,NR10CO芳基,COO烷基,COO芳基,CO烷基,芳基,芳基,环烷基,环烷基氨基,环烷基胺,双环,饱和杂环和不饱和杂环,其中R11-R13的至少一个碳任选被N,Q, 烷基,烯基炔基,芳氧基,烷基芳基,烷基氨基,烷基胺,NROCOO烷基,NR10 COO芳基,NR10CO烷基,NR 芳基,环烷基,环烷基氨基,环烷基胺,双环饱和杂环和不饱和杂环,离去基团,CN,OH或放射性同位素。