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Small molecule stimulators of proteasome core particles

A compound and substituent technology, applied in the field of small molecule stimulators of proteasome core particles, can solve the problems of slow degradation process and slow entry of substrates

Pending Publication Date: 2022-03-22
PURDUE RES FOUND INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

3,4 However, this degradation process is slower than that performed by the 26S proteasome due to slow substrate entry

Method used

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  • Small molecule stimulators of proteasome core particles
  • Small molecule stimulators of proteasome core particles
  • Small molecule stimulators of proteasome core particles

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Embodiment Construction

[0062] For the purposes of promoting an understanding of the principles of the disclosure, reference will now be made to the embodiments illustrated in the drawings, and specific language will be used to describe the same. Nevertheless, it should be understood that no limitation of the scope of the present disclosure is intended thereby.

[0063] Those skilled in the art will recognize that many modifications can be made to the specific embodiments described above. The embodiments should not be limited to the specific limitations described. Other implementations are also possible.

[0064] Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this disclosure belongs. Although methods, materials, compositions, reagents, cells similar or equivalent to any methods, materials, compositions, reagents, cells described herein can be used in the practice or testing of the pre...

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Abstract

The present disclosure relates to a series of compounds and methods of use for the treatment of diseases caused by aberrant modulation of the ubiquitin-proteasome system (UPS), and wherein the compound is an effective stimulator of the 20S core particle (CP) of the UPS. Compositions and methods of use are within the scope of the present disclosure.

Description

[0001] Cross References to Related Applications [0002] This application for patent relates to and claims priority to U.S. Provisional Patent Application Serial No. 62 / 887732 filed August 16, 2019 under 35 U.S.C. § 119(e), the contents of which are hereby incorporated by reference in their entirety and into this disclosure. technical field [0003] The present disclosure relates to a series of compounds and methods of use for the treatment of diseases caused by dysregulation of the ubiquitin-proteasome system (UPS), and wherein the compounds are potent stimulators of the 20S core particle (CP) of the UPS. Compositions of matter and methods of use are within the scope of the present disclosure. Background technique [0004] The major protein degradation pathway in cells is the ubiquitin-proteasome system (UPS). 1 This system involves a protein network for polyubiquitination and degradation of protein substrates. The degradation process is carried out by the 26S proteasom...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4164A61K31/4174A61P35/00
CPCA61P35/00C07D233/60
Inventor D·J·特拉德R·A·科尔曼A·萨拉查-查帕罗
Owner PURDUE RES FOUND INC