Thiadiazole irak4 inhibitors

A technology of R12 and compounds, applied in the field of novel compounds, can solve problems such as no approved IRAK4 inhibitory drugs

Pending Publication Date: 2021-03-26
GILEAD SCI INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] There are currently no approved IRAK4 inhibitors

Method used

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  • Thiadiazole irak4 inhibitors
  • Thiadiazole irak4 inhibitors
  • Thiadiazole irak4 inhibitors

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0140] Prepare hard gelatin capsules containing:

[0141]

[0142] The above ingredients are mixed and filled into hard gelatin capsules.

preparation Embodiment 2

[0144] Tablets are prepared using the following ingredients:

[0145]

[0146]

[0147] The ingredients are mixed and compressed to form tablets.

preparation Embodiment 3

[0149] A dry powder inhaler formulation is prepared containing the following components:

[0150] Composition Weight %

[0151] active ingredient 5

[0152] Lactose 95

[0153] Mix the active ingredient with lactose and add the mixture to a dry powder inhaler device.

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PUM

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Abstract

A compound of Formula (I), pharmaceutically acceptable salts thereof, deuterated analogs thereof, compositions thereof, and methods of treating disease by using a compound thereof are disclosed.

Description

technical field [0001] The present disclosure relates to novel compounds that are inhibitors of the kinase IRAK4. The present disclosure also relates to methods of preparing compounds and pharmaceutical compositions comprising such compounds. Background technique [0002] Interleukin-1 receptor-associated kinase-4 (IRAK4) is a serine-threonine kinase that acts as a mediator in the interleukin-1 / Toll-like receptor (IL-1 / TLR) signaling cascade. More specifically, IRAK4 is involved in the activation of the adapter protein myeloid differentiation primary response gene 88 (MyD88) signaling cascade and is hypothesized to play a role in inflammatory and fibrotic diseases such as rheumatoid arthritis (RA), inflammatory bowel disease (IBD). ), gout, Lyme disease, arthritis, psoriasis, pelvic inflammatory disease, systemic lupus erythematosus (SLE), Sjogren syndrome, viral myocarditis, acute and chronic tissue damage, nonalcoholic steatohepatitis ( NASH), alcoholic hepatitis and kid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61P29/00A61K31/5025
CPCC07D487/04A61P29/00Y02A50/30A61K31/5025A61P19/02C07D471/04C07D519/00
Inventor S.阿曼E.M.培根G.布里兹吉斯E.陈C.周J.J.科特尔M.杜克维M.沙特斯基克J.G.泰勒N.E.赖特Z-Y.杨S.M.齐普费尔
Owner GILEAD SCI INC
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