Substituted urea depsipeptide analogs as activators of the clpp endopeptidase
US-2016200770-A1 · Jul 14, 2016 · US
US10676510B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10676510-B2 |
| Application number | US-201815863673-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jan 5, 2018 |
| Priority date | Aug 30, 2013 |
| Publication date | Jun 9, 2020 |
| Grant date | Jun 9, 2020 |
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In one aspect, the invention relates to substituted urea depsipeptide analogs, derivatives thereof, and related compounds, which are useful as activators the C1pP endopeptidease; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating infectious disease using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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What is claimed is: 1. A method for the treatment of a bacterial infection in a mammal, the method comprising the step of administering to the mammal a therapeutically effective amount of a compound having a structure represented by a formula: wherein R 3 and R 4 are covalently bonded, together with the intermediate atoms, comprise a piperazinyl ring substituted with methyl group; wherein each of R 60a , R 60b , R 60c , R 60d , and R 60e is independently selected from hydrogen, —F, —Cl, and methyl, provided that no more than three of R 60a , R 60b , R 60c , R 60d , and R 60e are not hydrogen; and wherein R 70a is methyl, or a pharmaceutically acceptable salt thereof, thereby treating the bacterial infection in the mammal. 2. The method of claim 1 , wherein the mammal is a human. 3. The method of claim 2 , wherein the human has been diagnosed with a bacterial infection. 4. The method of claim 2 , wherein the human has been diagnosed with a biofilm mediated disease. 5. The method of claim 4 , wherein the biofilm mediated disease is bacterial endocarditis and osteomyelitis. 6. The method of claim 4 , further comprising the step of identifying a mammal in need of treatment of the biofilm mediated disease. 7. The method of claim 1 , wherein the mammal has been diagnosed with a need for treatment of the bacterial infection prior to the administering step. 8. The method of claim 1 , further comprising the step of identifying a mammal in need of treatment of the bacterial infection. 9. The method of claim 1 , further comprising administering to the mammal a therapeutically effective amount of at least one antibacterial agent.
Cross-Sectional Technologies · mapped topic
Cross-Sectional Technologies · mapped topic
Proteinases {, e.g. Endopeptidases (3.4.21-3.4.25)} · CPC title
Depsipeptides; Derivatives thereof · CPC title
Cross-Sectional Technologies · mapped topic
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