Literature DB >> 27690432

Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).

Kevin Doyle1, Hans Lönn2, Helena Käck2, Amanda Van de Poël1, Steve Swallow3, Philip Gardiner2, Stephen Connolly2, James Root2, Cecilia Wikell2, Göran Dahl2, Kristina Stenvall2, Petra Johannesson2.   

Abstract

A novel series of second generation DPP1 inhibitors free from aorta binding liabilities found for earlier compound series was discovered. This work culminated in the identification of compound 30 (AZD7986) as a highly potent, reversible, and selective clinical candidate for COPD, with predicted human PK properties suitable for once daily human dosing.

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Year:  2016        PMID： 27690432     DOI： 10.1021/acs.jmedchem.6b01127

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  9 in total

1.  DPP1 Inhibitors: Exploring the Role of Water in the S2 Pocket of DPP1 with Substituted Pyrrolidines.

Authors:  Helena Käck; Kevin Doyle; Samantha J Hughes; Michael S Bodnarchuk; Hans Lönn; Amanda Van De Poël; Nicholas Palmer
Journal:  ACS Med Chem Lett       Date:  2019-07-15       Impact factor: 4.345

Review 2.  Targets of Neutrophil Influx and Weaponry: Therapeutic Opportunities for Chronic Obstructive Airway Disease.

Authors:  Carina Kärrman Mårdh; James Root; Mohib Uddin; Kristina Stenvall; Anna Malmgren; Kostas Karabelas; Matthew Thomas
Journal:  J Immunol Res       Date:  2017-05-15       Impact factor: 4.818

3.  AWZ1066S, a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis.

Authors:  W David Hong; Farid Benayoud; Gemma L Nixon; Louise Ford; Kelly L Johnston; Rachel H Clare; Andrew Cassidy; Darren A N Cook; Amy Siu; Motohiro Shiotani; Peter J H Webborn; Stefan Kavanagh; Ghaith Aljayyoussi; Emma Murphy; Andrew Steven; John Archer; Dominique Struever; Stefan J Frohberger; Alexandra Ehrens; Marc P Hübner; Achim Hoerauf; Adam P Roberts; Alasdair T M Hubbard; Edward W Tate; Remigiusz A Serwa; Suet C Leung; Li Qie; Neil G Berry; Fabian Gusovsky; Janet Hemingway; Joseph D Turner; Mark J Taylor; Stephen A Ward; Paul M O'Neill
Journal:  Proc Natl Acad Sci U S A       Date:  2019-01-07       Impact factor: 11.205

4.  Safety, Tolerability, and Pharmacokinetic Evaluation of Single and Multiple Doses of the Dipeptidyl Peptidase 1 Inhibitor Brensocatib in Healthy Japanese and White Adults.

Authors:  Helen Usansky; Esther Yoon; Ariel Teper; Jun Zou; Carlos Fernandez
Journal:  Clin Pharmacol Drug Dev       Date:  2022-04-11

5.  An optimized method of extracting and quantifying active Neutrophil serine proteases from human whole blood cells.

Authors:  Jessica Basso; Jimin Zhang; Daniel Lasala; Sasha J Rose; Kuan-Ju Chen; David Cipolla
Journal:  PLoS One       Date:  2022-08-31       Impact factor: 3.752

6.  Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.

Authors:  Christopher M Woodley; Gemma L Nixon; Nicoletta Basilico; Silvia Parapini; Weiqian David Hong; Stephen A Ward; Giancarlo A Biagini; Suet C Leung; Donatella Taramelli; Keiko Onuma; Takashi Hasebe; Paul M O'Neill
Journal:  ACS Med Chem Lett       Date:  2021-06-24       Impact factor: 4.632

7.  Dipeptidyl Peptidase 1 Inhibitor AZD7986 Induces a Sustained, Exposure-Dependent Reduction in Neutrophil Elastase Activity in Healthy Subjects.

Authors:  Robert Palmér; Jukka Mäenpää; Alexandra Jauhiainen; Bengt Larsson; John Mo; Muir Russell; James Root; Susanne Prothon; Ligia Chialda; Pablo Forte; Torbjörn Egelrud; Kristina Stenvall; Philip Gardiner
Journal:  Clin Pharmacol Ther       Date:  2018-04-16       Impact factor: 6.875

8.  Industrial scale high-throughput screening delivers multiple fast acting macrofilaricides.

Authors:  Rachel H Clare; Catherine Bardelle; Paul Harper; W David Hong; Ulf Börjesson; Kelly L Johnston; Matthew Collier; Laura Myhill; Andrew Cassidy; Darren Plant; Helen Plant; Roger Clark; Darren A N Cook; Andrew Steven; John Archer; Paul McGillan; Sitthivut Charoensutthivarakul; Jaclyn Bibby; Raman Sharma; Gemma L Nixon; Barton E Slatko; Lindsey Cantin; Bo Wu; Joseph Turner; Louise Ford; Kirsty Rich; Mark Wigglesworth; Neil G Berry; Paul M O'Neill; Mark J Taylor; Stephen A Ward
Journal:  Nat Commun       Date:  2019-01-02       Impact factor: 14.919

Review 9.  Lung Protection by Cathepsin C Inhibition: A New Hope for COVID-19 and ARDS?

Authors:  Brice Korkmaz; Adam Lesner; Sylvain Marchand-Adam; Celia Moss; Dieter E Jenne
Journal:  J Med Chem       Date:  2020-08-07       Impact factor: 7.446
  9 in total

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