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Imaging Agents for Positron Emission Tomography using radiolabelled with f-18 Aminoalcohol

机译:使用f-18氨基醇进行放射性标记的正电子发射断层显像成像剂

摘要

New Compounds of Aminoalcohol radiolabelled with f-18 suitable for marking or already labeled with 18F, Methods for the preparation of said Compound, compositions comprising such Compounds, combinations of elements that comprise these compounds or compositions and Uses of these compu These,Compositions and Kits for Diagnostic Imaging by Positron Emission Tomography.Claim 1, characterized because it responds to a compound of formula (1) or Pharmaceutical acceptable salts for use of an inorganic or organic acid of the same Complex, hydrates, solvates, esters, amides, or prodrugs thereof, wherein Y1 is selected from the Group comprising) - N - (A1) Q3 - (CH2) or and (b) - n = C (U1) (U2) Q1,.Q2 and Q3 are selected individually and independently of the Group comprising: a) b) L2 - Hydrogen, c1-4 alkyl, - c) L2 - 4 (d) alquenilo C2 and L2 - alquinilo c2-4; A1 is selected from the Group comprising Methyl ethyl), (b) and (c) L3 U1 and U2 are individually selected and shaped Hood You of the aryl Group that comprises (a), (b) Tert Butyl Hydrogen metilsulfanilo c), d), e) - aryl Halo,(f) Hydroxyl - aryl - aryl nitro, (g), (H) 4 - aryl - and alkyl C1 (i) - 4 - aryl alquiloxi C1, E1 is selected from a group comprising Hydrogen, L2) (b), (c) L2 c1-4 alkyl, (d) alquenilo C2 and L2 - 4 (e) L2 - alquinilo c2-4; L1 is selected from the group consisting of (a) hydrogen, and (b) protecting Group, L2 is u N Group outgoing but not chlorine, Bromine, iodine, or mesyloxy tosyloxy Group; L3 is a protector.U is an integer between 0 and 4, H is an integer between 0 and 3. Claim 1: the use of a compound of Formula 1, wherein it is for the production of drugs or Pharmaceutical compositions for Diagnostic Imaging, more preferably PET Images.Claim 1: a Pharmaceutical composition, which comprises compounds of Formula 1 are acceptable for pharmaceutical use of an inorganic or organic acid of the same Complex, hydrates, solvates, esters, amides, or prodrugs of the same.17: a Vindication of Radiolabelling method to obtain compounds of Formula 3, characterized in that it comprises the step of (a) reacting a compound of Formula 1 with a fluoridation Agent to obtain a compound of Formula 3.
机译:适用于标记或已用18F标记的f-18放射性标记的氨基醇新化合物,该化合物的制备方法,包含此类化合物的组合物,包含这些化合物的元素组合或组合物以及这些化合物的用途第1项,用于正电子发射断层成像诊断成像,其特征在于它对式(1)化合物或药学上可接受的盐有反应,可用于相同络合物的无机或有机酸,水合物,溶剂化物,酯,酰胺或前药其中,Y1选自:-N-(A1)Q3-(CH2)或和(b)-n = C(U1)(U2)。Q1,.Q2和Q3分别独立地选自组包括:a)b)L 2-氢,c 1-4烷基,-c)L 2-4(d)alquenilo C 2和L 2 -alquinilo c2-4; A1选自包括甲基乙基的组),(b)和(c)。L3分别选择U1和U2并使其形成芳基的Hood You,其包括(a),(b)叔丁基氢甲基磺胺基苯胺c),d ),e)-芳基卤代,(f)羟基-芳基-芳基硝基,(g),(H)4-芳基-和烷基C 1(i)-4-芳基烷氧基C 1,E 1选自氢。 ,L2)(b),(c)L2,C1-4烷基,(d)alquenilo C2和L2-4(e)L2-alquiniloc2-4; L 1选自:(a)氢和(b)保护基,L 2为N基团,但不为氯,溴,碘或甲氧基甲磺酰氧基; L3是保护剂。U是0至4之间的整数,H是0至3之间的整数。1.权利要求1的式1化合物的用途,其中其用于生产用于诊断成像的药物或药物组合物,权利要求1:包含式1化合物的药物组合物对于相同络合物的无机或有机酸,其水合物,溶剂化物,酯,酰胺或前药的药学用途是可接受的。17:一种证明标记式3的放射标记的方法,其特征在于,它包括以下步骤:(a)使式1的化合物与氟化剂反应以获得式3的化合物。

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