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Modulators of toll-like receptors for the treatment of hiv

A treatment plan, pharmaceutical technology, applied in antiviral agents, antibody medical ingredients, resistance to vector-borne diseases, etc.

Active Publication Date: 2017-05-24
GILEAD SCI INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although combination antiretroviral therapy (cART) and highly active antiretroviral therapy (HAART) have been able to reduce HIV viral reactivation, usually below 50 HIV RNA copies / ml plasma, no therapy has been able to eliminate non-actively replicating HIV ( HIV-infected cells, often referred to as the patient's HIV latent reservoir

Method used

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  • Modulators of toll-like receptors for the treatment of hiv
  • Modulators of toll-like receptors for the treatment of hiv
  • Modulators of toll-like receptors for the treatment of hiv

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 119

[0396] Example 119: 6-Amino-2-butoxy-9-(3-(pyrrolidin-1-ylmethyl)benzyl)-9H-purin-8-ol

[0397]

[0398] The compound of Example 119 can be prepared using the method of US Patent No. 7,968,544 (Graupe et al.), where it appears as Compound W.

Embodiment 120

[0399] Example 120: 4-Amino-6-(2-methoxyethoxy)-1-((4'-(pyrrolidin-1-ylmethyl)-[1,1'-biphenyl]- 4-yl)methyl)-1H-imidazo[4,5-c]pyridin-2(3H)-one

[0400]

[0401] The compound of Example 120 can be prepared using the methods of WO 2011 / 049825 and U.S. 8,507,507 (Halcomb et al.), where it appears as Compound AX.

Embodiment 121

[0402]Example 121: 4-Amino-7-chloro-6-(2-methoxyethoxy)-1-((4'-(pyrrolidin-1-ylmethyl)-[1,1'-bi Phenyl]-4-yl)methyl)-1H-imidazo[4,5-c]pyridin-2(3H)-one

[0403]

[0404] The compound of Example 121 can be prepared using the methods of WO 2011 / 049825 and U.S. 8,507,507 (Halcomb et al.), where it appears as compound AY.

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PUM

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Abstract

Provided are methods, uses, pharmaceutical regimens, pharmaceutical compositions, and kits comprising modulators of TLR7, including those of Formula (II); and pharmaceutically acceptable salts thereof, useful in treating HIV infections.

Description

technical field [0001] The present application relates generally to compounds and pharmaceutical compositions that selectively modulate toll-like receptors, such as TLR7, and methods of using these compounds to treat human immunodeficiency virus (HIV) infection. Background technique [0002] The innate immune system provides the body's first line of defense against invading pathogens. In the innate immune response, invading pathogens are recognized by germline-encoded receptors, whose activation initiates a signaling cascade that induces cytokine expression. Innate immune system receptors have broad specificity, recognizing molecular structures that are highly conserved among different pathogens. One family of these receptors is known as Toll-like receptors (TLRs) because of their homology to receptors first identified and named in Drosophila and are present in cells such as macrophages, dendritic cells and in epithelial cells. [0003] There are at least ten different TL...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/437A61K31/496A61K31/4985A61K31/513A61K31/519A61K31/52A61K31/527A61K31/5365A61K31/5377A61K31/551A61K31/675A61P31/18
CPCA61K45/06A61K39/39A61K2039/55511A61K31/437A61K31/519A61K31/52A61K31/5377A61P31/18A61P37/04A61P43/00Y02A50/30A61K31/4985A61K31/5365A61K31/551A61K31/513A61K31/527A61K31/675
Inventor R·格勒兹纳斯J·E·赫塞尔格塞
Owner GILEAD SCI INC
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