Conolidine analogues as selective ACKR3 modulators for the treatment of cancer and cardiovascular diseases

Andy Chevigne (Inventor), Martyna Szpakowska (Inventor), Ojas A. Namjoshi (Inventor), Bruce E. Blough (Inventor), Ann M. Decker (Inventor), Max Meyrath (Inventor)

Research output: Patent


The present application discloses compounds of e.g. formulae (2), (1A), (1B) or (1C) as selective atypical chemokine receptor 3 (ACKR3) modulators for the treatment of e.g. cancer, atherosclerotic vascular disease, cardiovascular diseases, fibrosis (e.g. cardiac fibrosis), inflammatory or autoimmune diseases and conditions, conditions of excessive or abnormal vascularization (e.g. wound healing), stem cell differentiation and mobilization disorders, brain and neuronal dysfunctions (e.g. Alzheimer's disease, multiple sclerosis and demyelinating diseases), kidney dysfunction, renal dysfunction, preeclampsia, human immunodeficiency virus (HIV) infection and obesity. Further provided are said compounds for use in methods for in vitro or ex vivo diagnosis, prediction, prognosis and/or monitoring of a disease or condition characterized by an aberrant level of ACKR3 polypeptide, as well as for use in in vitro methods for identifying an agent useful as a therapeutic. An exemplary compound is e.g. WW-1.
Original languageEnglish
Patent number WO2022136486A1
IPCA61K31/397; A61K31/4025; A61K31/404; A61K31/407; A61K31/439; A61K31/4439; A61K31/454; A61K31/496; A61K31/499; A61K31/551; A61P13/12; A61P17/02; A61P25/28; A61P29/00; A61P3/04; A61P31/12; A61P31/18; A61P35/00; A61P37/08; A61P9/00; A61P9/10; C07D401/06; C07D403/06; C07D403/12; C07D471/18; C07D487/04;
Priority date22/12/20
Filing date22/12/21
Publication statusPublished - 30 Jun 2022


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