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Bicyclic inhibitors of pad4

A compound and optional technology, applied in the directions of antitoxins, anti-inflammatory agents, antiviral agents, etc., can solve the problems of unmet identification and development of PAD4 inhibitors, etc.

Active Publication Date: 2018-12-21
ПЭДЛОК ТЕРАПЬЮТИКС ИНК
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, there remains an unmet need to identify and develop PAD4 inhibitors for the treatment of PAD4-mediated disorders

Method used

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  • Bicyclic inhibitors of pad4
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  • Bicyclic inhibitors of pad4

Examples

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[0195] As shown in the Examples below, in certain exemplary embodiments, compounds are prepared according to the following general procedures. It will be appreciated that although the general methods illustrate the synthesis of certain compounds of the invention, the following general methods and others known to those of skill in the art are applicable to all compounds described herein and each of such compounds subclasses and species.

[0196] Method A

[0197] MET / u-HPLC (low pH 7min method)

[0198] Column: Phenomenex Kinetex-XB C18, 2.1mm×100mm, 1.7μm

[0199] Flow rate: 0.6ml / min

[0200] Mobile phases: A, 0.1% formic acid (aq); and B, 0.1% formic acid (MeCN)

[0201] Injection volume: 3 μl

[0202] Temperature: 40℃

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PUM

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Abstract

The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.

Description

Background of the Invention [0001] PAD4 is a member of the peptidyl arginine deiminase (PAD) family of enzymes capable of catalyzing the citrullination of arginine to citrulline within a peptide sequence. PAD4 is responsible for the deimidation or citrullination of various proteins in vitro and in vivo, resulting in different functional responses in various diseases (Jones J.E. et al., Curr. Opin. DrugDiscov.Devel., 12 ( 5), (2009), 616-627). Examples of exemplary diseases include rheumatoid arthritis, diseases in which neutrophils contribute to pathogenesis (eg, vasculitis, systemic lupus erythematosus, ulcerative colitis), and oncological indications. PAD4 inhibitors also have broad applicability as tools and therapeutics for human disease via epigenetic mechanisms. [0002] PAD4 inhibitors have utility against rheumatoid arthritis (RA). RA is an autoimmune disease affecting approximately 1% of the population (Wegner N. et al, Immunol. Rev., 233(1) (2010), 34-54). It is ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P19/02A61K31/00A61P35/00C07D401/14C07D471/04
CPCA61K45/06A61K31/4375A61K31/437A61K31/439A61K31/519A61K31/5383C07D403/14C07D471/04C07D519/00A61P1/02A61P1/04A61P1/14A61P1/16A61P1/18A61P11/00A61P11/02A61P11/04A61P11/06A61P11/14A61P11/16A61P13/12A61P15/00A61P17/00A61P17/02A61P17/04A61P17/06A61P17/08A61P17/10A61P17/14A61P19/02A61P19/04A61P19/08A61P21/00A61P21/04A61P25/00A61P25/02A61P25/04A61P25/14A61P25/20A61P25/28A61P27/02A61P27/06A61P27/12A61P27/14A61P27/16A61P29/00A61P29/02A61P3/00A61P3/02A61P3/04A61P31/04A61P31/06A61P31/18A61P31/22A61P33/02A61P35/00A61P35/02A61P3/06A61P3/10A61P37/00A61P37/06A61P37/08A61P39/02A61P43/00A61P5/14A61P5/38A61P7/00A61P7/04A61P7/06A61P7/10A61P9/00A61P9/10A61P9/12A61P9/14A61K2300/00A61K31/4184
Inventor R.德夫拉伊G.库马拉维尔M.F.帕克E.博蒙L.鲍尔斯S.布罗姆布里奇S.库珀E.加杜莱奥L.格利夫P.克里A.科泰T.克鲁尔C.莱茨P.洛克M.梅尼科尼N.蒙克C.诺尔思J.帕尔弗里S.帕罗特M.里吉尔H.泰
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