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PSMA (Prostate-Specific Membrane Antigen) inhibitor, compound and application

A compound and inhibitor technology, applied in the field of PSMA inhibitors and PSMA inhibitor compounds with functional groups, can solve the problems of few application prospects, decreased binding constants, unstable compound structures, etc.

Active Publication Date: 2019-05-14
PEKING UNIV FIRST HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the conservative structure of PSMA inhibitors, some slight changes to the core structure of urea inhibitors will lead to a rapid decrease in binding constants (Bioorganic & Medicinal Chemistry Letters 20 (2010) 392-397)
At present, there have been hundreds of improved compounds for PSMA inhibitors reported in the literature. Only a few improved inhibitors show binding constants similar to those of urea inhibitors, and some of the compounds are not stable in structure. Very few have promising applications

Method used

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  • PSMA (Prostate-Specific Membrane Antigen) inhibitor, compound and application
  • PSMA (Prostate-Specific Membrane Antigen) inhibitor, compound and application
  • PSMA (Prostate-Specific Membrane Antigen) inhibitor, compound and application

Examples

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Embodiment 1-2

[0083] This example is used to illustrate the synthesis and characterization of compound S1 and compound S2. Synthetic route such as Figure 4 shown.

[0084] (1) Synthesis of compound 2 tert-butyl 2-chloro-2-oxoacetate:

[0085] In a 100mL round-bottomed flask, oxalyl chloride (1g, 7.88mmol) was dissolved in anhydrous dichloromethane (15mL), and tert-butanol (584mg, 7.88mmol) was dissolved in anhydrous dichloromethane (15mL) under ice-cooling stirring. The solution was slowly added dropwise into the reaction liquid, and after the dropwise addition was completed, the reaction was carried out at room temperature under nitrogen protection for 24 hours, and the solvent was removed under reduced pressure to obtain a colorless liquid product 2, which was directly used in the next reaction.

[0086] (2) Synthesis of compound 4 (S)-tert-butyl 2-(((benzyloxy)carbonyl)amino)-3-(2-(tert-butoxy)-2-oxoacetamido)propanoate:

[0087] In a 100mL round bottom flask, compound 3 (1g, 3.40mmo...

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Abstract

The invention belongs to the technical field of biomedicines and in particular relates to a PSMA (Prostate-Specific Membrane Antigen) inhibitor, a compound and application. The PSMA inhibitor of a novel core structure, which is provided by the invention, has very high affinity, is stable in structure and has wide application prospects.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and more specifically relates to a compound having a PSMA inhibitor core structure, a PSMA inhibitor obtained therefrom, PSMA inhibitor compounds with functional groups and applications thereof. Background technique [0002] Prostate cancer is one of the most common malignant tumors in men, and its incidence rate ranks first in European and American countries all the year round. Although the incidence of prostate cancer in China is lower than that in Europe and the United States, with the advent of China's aging society and the change of westernized living habits, the incidence of prostate cancer has increased rapidly in recent years. At the same time, there are more middle-, high-risk and advanced-stage prostate cancer patients in my country, and the proportion is significantly higher than that in Europe and the United States. The curative effect of tumor is closely related to the stage of ...

Claims

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Application Information

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IPC IPC(8): C07D311/16C07C275/16A61P35/00A61P35/04A61K41/00A61K49/00A61K49/22A61K51/04
CPCA61K41/0057A61K47/18A61K49/0002A61P35/00C07C275/16C07D311/16G01R33/5601Y02P20/55
Inventor 杨兴杨志席真刘福涛段小江
Owner PEKING UNIV FIRST HOSPITAL
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