Discovery of a new class of potent, selective, and orally bioavailable CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases

Autor: Alexander Scheer, Jean-François Arrighi, Lucia Golzio, Marc Missotten, Yaroslav Filinchuk, Véronique Colovray, Pierre-André Pittet, Christophe Cleva, André Chollet, Thierry Martin, Atherall John Frederick, Claudio Giachetti, Maurizio Maio, Cynthia Rocha, Matthias Schwarz, Jackie Macritchie, Patrick Page, Gérald Bernardinelli, Stefano Crosignani, Yves Humbert, Doris Pupowicz, Marilène Gaudet

Publikováno v: Journal of medicinal chemistry. 51(7)

A novel chemical class of potent chemoattractant receptor-homologous expressed on Th2 lymphocytes (CRTH2 or DP2) antagonists is reported. An initial and moderately potent spiro-indolinone compound (5) was found during a high-throughput screening camp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6e9569591f6a7caff3d3dccb696fa37a
https://pubmed.ncbi.nlm.nih.gov/18318469

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Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor.

Autor: Chan BK; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Estrada AA; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Chen H; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Atherall J; Departments of Chemistry, Biochemical and Cellular Pharmacology, and Drug Metabolism and Pharmacokinetics, BioFocus, Chesterford Research Park , Saffron Walden, Essex CB10 1XL, United Kingdom., Baker-Glenn C; Departments of Chemistry, Biochemical and Cellular Pharmacology, and Drug Metabolism and Pharmacokinetics, BioFocus, Chesterford Research Park , Saffron Walden, Essex CB10 1XL, United Kingdom., Beresford A; Departments of Chemistry, Biochemical and Cellular Pharmacology, and Drug Metabolism and Pharmacokinetics, BioFocus, Chesterford Research Park , Saffron Walden, Essex CB10 1XL, United Kingdom., Burdick DJ; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Chambers M; Departments of Chemistry, Biochemical and Cellular Pharmacology, and Drug Metabolism and Pharmacokinetics, BioFocus, Chesterford Research Park , Saffron Walden, Essex CB10 1XL, United Kingdom., Dominguez SL; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Drummond J; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Gill A; Departments of Chemistry, Biochemical and Cellular Pharmacology, and Drug Metabolism and Pharmacokinetics, BioFocus, Chesterford Research Park , Saffron Walden, Essex CB10 1XL, United Kingdom., Kleinheinz T; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Le Pichon CE; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Medhurst AD; Departments of Chemistry, Biochemical and Cellular Pharmacology, and Drug Metabolism and Pharmacokinetics, BioFocus, Chesterford Research Park , Saffron Walden, Essex CB10 1XL, United Kingdom., Liu X; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Moffat JG; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Nash K; Departments of Chemistry, Biochemical and Cellular Pharmacology, and Drug Metabolism and Pharmacokinetics, BioFocus, Chesterford Research Park , Saffron Walden, Essex CB10 1XL, United Kingdom., Scearce-Levie K; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Sheng Z; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Shore DG; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Van de Poël H; Departments of Chemistry, Biochemical and Cellular Pharmacology, and Drug Metabolism and Pharmacokinetics, BioFocus, Chesterford Research Park , Saffron Walden, Essex CB10 1XL, United Kingdom., Zhang S; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Zhu H; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States., Sweeney ZK; Departments of Discovery Chemistry, Biochemical and Cellular Pharmacology, Drug Metabolism and Pharmacokinetics, and Neuroscience, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2012 Nov 23; Vol. 4 (1), pp. 85-90. Date of Electronic Publication: 2012 Nov 23 (Print Publication: 2013).