Identification of novel azaindazole CCR1 antagonist clinical candidates

Christian Harcken,Daniel Kuzmich, Brain Cook,Can Mao,Darren Disalvo,Hossein Razavi,Alan Swinamer,Pingrong Liu,Qiang Zhang,Alison Kukulka,Donna Skow,Mita Patel,Monica Patel,Kimberly Fletcher, Tara Sherry,David Joseph,Dustin Smith,Melissa Canfield,Donald Souza, Matthew Bogdanffy

Bioorganic & Medicinal Chemistry Letters（2019）

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摘要

•Scaffold hopping approach led to identification of novel indazole CCR1 antagonists.•Multi parameter optimization led to three clinical candidate compounds.•Sub-micromolar CCR1 antagonists with attractive drug-like properties.•Candidates show >1000-fold improved CCR1 potency compared to initial hit.

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关键词

Chemokine receptors,CCR1,Indazole,Scaffold hopping,Clinical compound

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