• 专利标题:   New piperidine derivative as sensors for rapid and specific determination of FKBP12 protein, peptidyl-prolyl cis-trans isomerase, levels of which in biological fluids of subject change, if subject is affected by pathological conditions.
  • 专利号:   WO2021124269-A1, EP4077280-A1, US2023033380-A1
  • 发明人:   CAMINATI G, PROCACCI P, MENICHETTI S, MARTINA M R, MARSILI L
  • 专利权人:   UNIV FIRENZE, UNIV FIRENZE, UNIV FIRENZE
  • 国际专利分类:   C07D211/60, G01N033/48, G01N033/50, B01L003/00, G01N033/553, G01N033/573, C07D211/06
  • 专利详细信息:   WO2021124269-A1 24 Jun 2021 202158 Pages: 44 English
  • 申请详细信息:   WO2021124269-A1 WOIB062214 18 Dec 2020
  • 优先权号:   IT00025066

▎ 摘  要

NOVELTY - Piperidine derivative (I) is new. USE - Piperidine derivative used as sensors for the rapid and specific determination of the FKBP12 protein, a peptidyl-prolyl cis-trans isomerase (PPlase), the levels of which in the biological fluids of a subject change if the subject is affected by pathological conditions, in particular neurodegenerative diseases, such as the Parkinson's disease and the Alzheimer's syndrome, tumor pathologies, autoimmune diseases and in monitoring the post-operative course in a subject who has undergone organ and/or tissue transplantation by determining the concentration of FKBP12 protein in a biological sample previously taken from the subject (claimed). DETAILED DESCRIPTION - Piperidine derivative of formula (I) is new.. L=thiol, organo-sulfur groups, such as sulfide (- SR), disulfide (-SSR), thiolesters (-SC(O)R), and dithiocarbammates (-SC(S)NRR ); R and R=alkyl or aryl residues, carboxylic acid, primary amine, trichlorosilane, trimethoxysilane, triethoxysilane, cholesterol, benzene, naphthalene, anthracene, phenanthrene, and pyrene; Y'=(CH2)n and (OCH2CH2)m; n=7-13; and m=2-6. INDEPENDENT CLAIMS are included for the following: (1) a sensor unit for detecting devices of the FKBP12 protein in biological samples, which comprises a substrate having a measurement surface on at least a portion of which there is a monolayer coating of piperidine derivative of formula (I), optionally immersed in a matrix of a spacer molecule of linear formula CH3-Z'-CH2-L, where the Z is equal to Y' or is a group (OCH2CH2)n-1-CH2CH2-L with n ranging between 4-100; (2) a method for preparing the sensor unit, which involves immersing at least portion of the measurement surface of the unit in a solution of piperidine derivative of formula (I) and of a spacer, in a solvent selected from water, an organic solvent such as ethanol, until the surface to be coated of the sensor unit is saturated, followed by rinsing in the same above the solvent; and (3) a device for detecting the FKBP12 protein in biological samples, which comprises as a sensor element the sensor unit and a detection system of the FKBP12 protein.