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Proteasome activity enhancing compounds

A compound and clathrate technology, applied in the direction of active ingredients of heterocyclic compounds, organic active ingredients, compounds of elements of Group 4/14 of the periodic table, etc.

Pending Publication Date: 2021-03-30
优曼尼蒂公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, many oncoproteins are substrates of the proteasome, and their ability to enhance cancer may be attenuated by enhancing proteasome activity

Method used

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  • Proteasome activity enhancing compounds
  • Proteasome activity enhancing compounds
  • Proteasome activity enhancing compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0499] Example 1: A compound of formula (IA):

[0500]

[0501] or a pharmaceutically acceptable salt, solvate, clathrate or prodrug thereof; wherein:

[0502] E is selected from the group consisting of optionally substituted aryl or optionally substituted heteroaryl;

[0503] R 1 and R 2 each independently selected from the group consisting of hydrogen, optionally substituted C 1 -C 10 Alkyl, optionally substituted C 2 -C 10 alkenyl, optionally substituted C 2 -C 10 Alkynyl, optionally substituted C 3 -C 12 Cycloalkyl, optionally substituted C 3 -C 12 Cycloalkenyl;

[0504] Z is an optionally substituted 6 to 12 membered bridged N-heterocycle;

[0505] R 3a , R 3b , R 3c and R 3d each independently selected from the group consisting of hydrogen, optionally substituted C 1 -C 10 Alkyl, optionally substituted C 2 -C 10 alkenyl, optionally substituted C 2 -C 10 Alkynyl, optionally substituted C 3 -C 12 Cycloalkyl, optionally substituted C 3 -C 12 Cy...

Embodiment 2

[0511] Embodiment 2: The compound according to embodiment 1, or a pharmaceutically acceptable salt, solvate, clathrate or prodrug thereof, wherein R 5 is optionally substituted by C 1 -C 4 alkyl.

Embodiment 3

[0512] Embodiment 3: The compound according to embodiment 1, or a pharmaceutically acceptable salt, solvate, clathrate or prodrug thereof, wherein R 5 is methyl.

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Abstract

The present invention is directed towards compounds having the Formula (lb) or the Formulae (III) and pharmaceutically acceptable salts, solvates and clathrates thereof, compositions thereof, as wellas towards the use of said compounds in methods for the treatment of a condition associated with a dysfunction in proteostasis.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of priority to U.S. Patent Application Serial No. 62 / 690,563, filed June 27, 2018, the disclosure of which is incorporated herein by reference in its entirety. This application claims the benefit of priority to U.S. Patent Application Serial No. 62 / 690,565, filed June 27, 2018, the disclosure of which is incorporated herein by reference in its entirety. Background technique [0003] Cells generally use sensors and networks of pathways to maintain a balance between protein synthesis, folding, transport, aggregation, and degradation, known as protein homeostasis [Sitia et al., Nature 426:891-894, 2003; Ron et al. al., NatRev Mol Cell Biol 8:519-529, 2007]. The cellular maintenance of proteostasis (or proteostasis) refers to the control of the conformation, binding interactions, position, and concentration of the individual proteins that make up the proteome. Protein folding in vivo is ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/14C07D491/08C07D403/06C07D403/14C07D417/14C07D451/02C07D451/06A61P25/00A61P25/16A61P25/28A61K31/4025A61K31/405
CPCC07D451/06C07D403/06C07D405/14C07D451/02C07D403/14C07D491/08C07D417/14A61P25/00A61P25/16A61P25/28C07D487/08A61K31/407A61K31/46C07D491/22C07F7/0812
Inventor M·卡伦C·M·巴斯托斯D·帕克斯B·穆诺茨
Owner 优曼尼蒂公司
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