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    • 14. 发明申请
    • DIAGNOSTIC AND THERAPEUTIC ALKYL PIPERIDINE/PIPERAZINE COMPOUNDS AND PROCESS
    • 诊断和治疗碱性哌啶/哌嗪化合物和方法
    • WO2004063150A2
    • 2004-07-29
    • PCT/US2003/041731
    • 2003-12-31
    • THE GENERAL HOSPITAL CORPORATION
    • ELMALEH, David, R.CHOI, SangwoonFISHMAN, Alan, J.
    • C07D
    • C07D213/75C07D211/26C07D211/58C07D295/215C07D401/12
    • Piperidine or piperazine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided. The compounds are characterized by the formulae: (I), (II), (III), (IV), (V) wherein: n is an integer of 1 to 6; X, Y, Z 1 and Z 2 can be the same or different and are hydrogen, halo, haloalkyl, alkyl, aryl, (C 1 -C 6 )alkoxy, N-alkyl, (C 2 -C 6 )acyloxy, N-alkylene, -SH, -SR, wherein R is from the same group as R 1 and R 2 and can be the same or different than R 1 and R 2 , amino, nitro, cyano, hydroxy, C(=O)OR 6 , -C(=O)NR 5 R 4 , NR 3 R 2 , or S(=O) k R 1 wherein k is 1 0r 2, and R 1 to R 6 are independently hydrogen or (C 1 -C 6 )alkyl; R 1 and R 2 can be the same or different and are hydrogen, (C 1 -C 6 )alkyl, hydroxyalkyl or mercaptoalkyl, -C(=O)OR 1 , cyano, (C 1 -C 6 )alkenyl, (C 2 -C 6 ) alkynyl, or 1, 2, 4-oxadiazol-5-yl optionally substituted at the 3-position by Z 4 wherein any (C 1 -C 6 )alky, (C 1 -C 6 )alkanoyl, (C 2 -C 6 )alkenyl or (C 2 -C 6 )alkynyl can optionally be substituted by 1, 2 or 3 Z; R 7 can be hydrogen, O or phenyl; R 8 can be hydrogen, phenyl, halophenyl, nitrophenyl, pyridyl, piperonyl or sulfoxonitrophenyl; Z 4 is (C 1 -C 6 )alkyl or phenyl, optionally substituted by 1, 2 or 3 Z 1 ; W is O or S; T is amino or C 1 -C 6 aminoalkyl; A is N or C; T is C 1 -C 6 alkyl or sulfonyl and V is alkyl (C 0 -C 6 ), alkenyl, alkynyl, haloaryl, alkyl phenol, alkyl halophenyl, and R 1 or R 2 as indicated above and D is phenyl, naphrhyl, thienyl or pyridinyl.
    • 提供了可用于治疗特征在于缺乏多巴胺神经元活性或成像多巴胺神经元的神经变性疾病的哌啶或哌嗪化合物。 该化合物的特征为:(I),(II),(III),(IV),(V)其中:n为1至6的整数; X,Y,Z 1和Z 2可以相同或不同,为氢,卤素,卤代烷基,烷基,芳基,(C1-C6)烷氧基,N-烷基,(C2-C6)酰氧基,N-亚烷基, -SR,其中R是与R1和R2相同的基团,并且可以与R1和R2相同或不同,氨基,硝基,氰基,羟基,C(= O)OR6,-C(= O)NR5R4,NR3R2 或S(= O)kR1,其中k为10r 2,并且R 1至R 6独立地为氢或(C 1 -C 6)烷基; R 1和R 2可以相同或不同,为氢,(C 1 -C 6)烷基,羟基烷基或巯基烷基,-C(= O)OR 1,氰基,(C 1 -C 6)烯基,(C 2 -C 6)炔基或1 任选通过Z 4在3位被取代的2,4-二唑-5-基,其中任何(C 1 -C 6)烷基,(C 1 -C 6)烷酰基,(C 2 -C 6)烯基或(C 2 -C 6) 由1,2或3个Z代替; R7可以是氢,O或苯基; R8可以是氢,苯基,卤代苯基,硝基苯基,吡啶基,胡椒基或磺基亚硝基苯基; Z4是(C1-C6)烷基或苯基,任选被1,2或3个Z1取代; W为O或S; T是氨基或C 1 -C 6氨基烷基; A是N或C; T是C1-C6烷基或磺酰基,V是如上所述的烷基(C 0 -C 6),烯基,炔基,卤代芳基,烷基苯酚,烷基卤代苯基和R 1或R 2,D是苯基,萘基,噻吩基或吡啶基。
    • 16. 发明申请
    • F-18 LABELED TRACER AND METHODS OF MANUFACTURE
    • F-18标签跟踪器及其制造方法
    • WO2016070074A1
    • 2016-05-06
    • PCT/US2015/058357
    • 2015-10-30
    • THE GENERAL HOSPITAL CORPORATION
    • ELMALEH, David, R.SHOUP, Timothy, M.
    • C07B59/00
    • C07B59/004C07B2200/05C07F9/5442
    • A method of producing a radiofluorinated compound comprising the steps of forming a reaction mixture comprising a reactant having a formula of R-Y and a radiofluorinating agent having a formula of R'- 18 F; and contacting the reaction mixture with microwave radiation to achieve a temperature of between 100°C and 250°C for a time sufficient to convert at least 10% of the reactant into the radiofluorinated compound having a formula of R- 18 F, wherein R is selected from the group consisting of an alkyl (C 1 -C 20 ), a cycloalkyl (C 3 -C 10 ), an aryl, a heteroaryl, an aralkyl and an alkenyl group (C 2 -C 20 ); Y is selected from the group consisting of a sulfonate, a nitro, an acetate and a halogen; and R' is selected from the group consisting of an alkali metal cation, an alkaline earth metal cation, a transition metal cation, an ammonium cation, and a tetraalkylammonium cation is provided.
    • 一种制备放射性氟化合物的方法,包括以下步骤:形成含有式R-Y的反应物和具有式R'-18F的放射性氟化剂的反应混合物; 并将反应混合物与微波辐射接触以达到100℃至250℃之间的温度足以将至少10%的反应物转化为具有式R-18F的放射性氟化化合物的时间,其中R选自 (C 1 -C 20),环烷基(C 3 -C 10),芳基,杂芳基,芳烷基和链烯基(C 2 -C 20)组成的组。 Y选自磺酸酯,硝基,乙酸酯和卤素; 并且提供R'选自碱金属阳离子,碱土金属阳离子,过渡金属阳离子,铵阳离子和四烷基铵阳离子。