title: A dual CCR2/CCR5 chemokine antagonist, BMS-813160? Evaluation of WO2011046916.
abstract: This application claims the dual CCR2/CCR5 antagonist (S)-1-[(1S,2R,4R)-4-isopropyl(methyl)amino)-2-propylcyclohexyl]-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-2-one, crystalline form N-1, a process for its preparation and therapeutic uses of it. The compound is shown to be a potent, well-absorbed, drug with a good duration of action. It shows better properties than similar compounds previously claimed by Bristol-Myers Squibb and appears to be a clinical development candidate.
authors.affiliation: Norman Consulting, 18 Pink Lane, Burnham, Bucks, SL1 8JW, UK. petrosn@bigfoot.com
authors.forename: Peter
authors.initials: P
authors.lastname: Norman
mesh_terms: D000818:Animals; D065100:CCR5 Receptor Antagonists; D002317:Cardiovascular Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D010330:Patents as Topic; D011720:Pyrazoles / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D054390:Receptors, CCR2 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D019713:Receptors, CCR5 / Q000378:metabolism; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: C570874:BMS-813160; D065100:CCR5 Receptor Antagonists; D002317:Cardiovascular Agents; D011720:Pyrazoles; D054390:Receptors, CCR2; D019713:Receptors, CCR5; D014227:Triazines