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COMPOUNDS FOR USE IN VISUALIZATION, DIAGNOSTICS AND / OR TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM OR TUMORS

机译:用于可视化,诊断和/或治疗中枢神经系统或肿瘤疾病的化合物

摘要

1. The compound of formula Ia! ! or formula Ib! ! where W is selected from the group consisting of! —C (U1) (U2) —C≡CH and cyclopropyl, U1 and U2, which are independently selected from hydrogen and deuterium; ! A is selected from the group consisting of substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, such as furanyl, (C1-C10) alkyl, G4- (C2-C4) alkynyl, G4- (C1-C4) alkoxy, (G4- ( C1-C4) alkyl) aryl, (G4- (C1-C4) alkoxy) aryl, (G4- (C1-C4) alkyl) apyl, and (G4- (C1-C4) alkoxy) apyl, where preferably said heteroaryl is furanil yourself! G1, G2, G3 and G4 in formula Ia and formula Ib are independently and individually, in each case, selected from the group consisting of hydrogen, (C1-C4) alkyl, preferably methyl, L, and - (C1-C6) alkyl -L,! provided that it is precisely one of G1-G4 in formula Ia that is selected from L and - (C1-C6) alkyl-L, and! provided that it is precisely one of G3 and G4 in formula Ib that is selected from L and! - (C1-C6) alkyl-L,! L is a leaving group, or L is F, preferably 18F or 19F, where, preferably, if L is 19F, said compound contains precisely one 19F atom that is attached to the sp3 hybridized carbon atom,! where n is an integer from 0 to 6, preferably 1-3, more preferably 1-2,! and where m is an integer from 0 to 4, preferably 0 to 2, more preferably 0-1,! and where e and f are an integer from 0 to 1, provided that at least one of e and f is 1, including all isomeric forms of said compound, which include, but are not limited to, enantiomers and diastereoisomers, so same as racemic mixtures! and any pharmaceutically acceptable salt, ester, amide, complex compound or prodrug, respectively. !
机译:1.式Ia的化合物! !或公式Ib! !其中W从以下组成的组中选择! -C(U1)(U2)-C≡CH和环丙基,U1和U2,其独立地选自氢和氘; ! A选自取代或未取代的芳基,取代或未取代的杂芳基,例如呋喃基,(C1-C10)烷基,G4-(C2-C4)炔基,G4-(C1-C4)烷氧基,(G4- (C 1 -C 4)烷基)芳基,(G 4-(C 1 -C 4)烷氧基)芳基,(G 4-(C 1 -C 4)烷基)戊基和(G 4-(C 1 -C 4)烷氧基)己基,其中优选所述杂芳基自己是呋喃!式Ia和式Ib中的G 1,G 2,G 3和G 4在每种情况下独立且独立地选自氢,(C 1 -C 4)烷基,优选甲基,L和-(C 1 -C 6)烷基。 -L ,!只要它恰好是式Ia中的G1-G4之一,它选自L和-(C1-C6)烷基-L,和!前提是它恰好是选自I和I的式Ib中的G3和G4之一。 -(C1-C6)烷基-L ,! L为离去基团,或L为F,优选为18F或19F,其中,优选地,如果L为19F,则所述化合物恰好包含一个与sp3杂化碳原子相连的19F原子。其中n是0至6的整数,优选1-3,更优选1-2 ,!其中m是0至4的整数,优选0至2,更优选0-1 ,!并且其中e和f为0-1的整数,条件是e和f中的至少一个为1,包括所述化合物的所有异构体形式,包括但不限于对映异构体和非对映异构体,与外消旋相同混合物!以及任何药学上可接受的盐,酯,酰胺,复合化合物或前药。 !

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