Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties

Bioorganic and Medicinal Chemistry Letters

Volumn 26, Issue 18, 2016, Pages 4455-4461

  René, Olivier ^a   Fauber, Benjamin P ^a,c   Barnard, Adrian ^b   Chapman, Kerry ^b   Deng, Yuzhong ^a   Eidenschenk, Céline ^a   Everett, Christine ^a   Gobbi, Alberto ^a   Johnson, Adam R ^a   La, Hank ^a   Norman, Maxine ^b   Salmon, Gary ^b   Summerhill, Susan ^b   Wong, Harvey ^a,d  

^a GENENTECH INC   (United States)

^b Charles River   (United Kingdom)

^c Independent Consultant   (United States)

^d UNIVERSITY OF BRITISH COLUMBIA   (Canada)

Author keywords

IL 17; Inverse agonist; Oxa sultam; PBMCs; RORc; ROR

Indexed keywords

LIPID; NAPHTHALENESULFONIC ACID DERIVATIVE; NAPHTHOSULTONE; RETINOID RELATED ORPHAN RECEPTOR ALPHA;

AGONISTS; CHEMISTRY; DRUG DEVELOPMENT; INVERSE AGONISM;

DRUG DISCOVERY; DRUG INVERSE AGONISM; LIPIDS; NAPHTHALENESULFONATES; NUCLEAR RECEPTOR SUBFAMILY 1, GROUP F, MEMBER 1;

EID: 84981727586     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2016.07.081     Document Type: Article

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