PATENT CLAIM ANALYSIS

Application Number: 15753006
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-08
Patent Classification: ["424", "001890"]

Abstract:
The present invention discloses a radioisotope  18 F substituted thiamine, synthesis method, and use thereof in small animal PET/CT imaging. The radioisotope  18 F substituted thiamine has a structure of The synthesis method comprises radiochemical synthesis by using existing precursors. In the present invention, the hydroxyl in the hydroxyethyl on the thiazole cycle of thiamine is replaced by radioisotope  18 F, to prepare a PET tracer. The radioisotope  18 F substituted thiamine of the present invention successfully enters the brains of various strains of mice, and the uptake in the brains of thiamine-deficient mice is obviously greater than that in normal control. The present invention is useful in the preparation of a brain imaging tracer for clinical trials of Alzheimer's disease and tumors.

Claim (Index 4):
A method for synthesizing a radioisotope  18 F substituted thiamine hydrobromide according to  claim 3 , comprising:\n Step 1): generating H +  protons in a cyclotron, bombarding  18 O-heavy oxygen water with the H +  protons, and generating  18 F \u2212  ions through the nuclear reaction  18 O(p, n) 18 F; enriching  18 F \u2212  ions by a QMA column, and eluting it into a reaction vial with an eluant, to obtain [K/Kryptofix] +18 F \u2212 , evaporating water to dryness; and reacting 2-(4-methylthiazol-5-yl)ethyl 4-methylbenzenesulfonate with [K/Kryptofix] +18 F \u2212  to produce 5-(2-fluoroethyl)-4-methylthiazole through nucleophilic substitution in acetonitrile solvent, where the reaction equation for chemical synthesis is: Step 2): reacting the product 5-(2-fluoroethyl)-4-methylthiazole obtained in Step 1) with 2-methyl-5-bromomethyl-6-aminopyrimidine hydrobromide in acetonitrile solvent to produce  18 F substituted thiamine hydrobromide, where the reaction equation for chemical synthesis is:

Metadata:
- Claim Count in Document: 1.0
- Percentile: 88.0
- Lexical Diversity: 1.97059
- Patent Class: 424.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15807306', '15674701', '14031812', '12836926', '14101960']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7136468847180988
- 35 USC 102 Novelty (BERT): 0.4755354489068952
- Combined Prediction Score: 0.6898357411369784
- Mean Citation Score: 202.841408
- Max Citation Score: 217.18102
- Similarity Product: 183.0005436165655

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 1
- Label 101 Adjusted: 0

Dataset: test