title: Design, synthesis and SAR of indazole and benzoisoxazole containing 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists.
abstract: A novel series of 4-azetidinyl-1-aryl-cyclohexanes containing indazole or benzoisoxazole moiety have been identified as potent CCR2 antagonists with high selectivity versus hERG.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, Welsh & McKean Roads, Spring House, PA 19477, United States. xzhang5@prdus.jnj.com
authors.forename: Xuqing
authors.initials: X
authors.lastname: Zhang
authors.forename: Heather
authors.initials: H
authors.lastname: Hufnagel
authors.forename: Cuifen
authors.initials: C
authors.lastname: Hou
authors.forename: Evan
authors.initials: E
authors.lastname: Opas
authors.forename: Sandra
authors.initials: S
authors.lastname: McKenney
authors.forename: Carl
authors.initials: C
authors.lastname: Crysler
authors.forename: John
authors.initials: J
authors.lastname: O'Neill
authors.forename: Dana
authors.initials: D
authors.lastname: Johnson
authors.forename: Zhihua
authors.initials: Z
authors.lastname: Sui
mesh_terms: D000818:Animals; D002460:Cell Line; D003510:Cyclohexanes / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004285:Dogs; D015195:Drug Design; D006801:Humans; D007191:Indazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D010080:Oxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D054390:Receptors, CCR2 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D015534:Trans-Activators / Q000378:metabolism; D000071230:Transcriptional Regulator ERG
chemical_list: D003510:Cyclohexanes; C072312:ERG protein, human; D007191:Indazoles; D010080:Oxazoles; D054390:Receptors, CCR2; D015534:Trans-Activators; D000071230:Transcriptional Regulator ERG