title: Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa.
abstract: Previously, potent factor Xa inhibitors were described based on the 1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one bicyclic core and a 4-methoxyphenyl P1 moiety. This manuscript describes 1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one and related bicyclic cores with the 3-aminobenzisoxazole P1 moiety. Many of these compounds are potent, selective, and efficacious inhibitors of coagulation factor Xa.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA.
authors.forename: Yun-Long
authors.initials: YL
authors.lastname: Li
authors.forename: John M
authors.initials: JM
authors.lastname: Fevig
authors.forename: Joseph
authors.initials: J
authors.lastname: Cacciola
authors.forename: Joseph
authors.initials: J
authors.lastname: Buriak
authors.forename: Karen A
authors.initials: KA
authors.lastname: Rossi
authors.forename: Janan
authors.initials: J
authors.lastname: Jona
authors.forename: Robert M
authors.initials: RM
authors.lastname: Knabb
authors.forename: Joseph M
authors.initials: JM
authors.lastname: Luettgen
authors.forename: Pancras C
authors.initials: PC
authors.lastname: Wong
authors.forename: Stephen A
authors.initials: SA
authors.lastname: Bai
authors.forename: Ruth R
authors.initials: RR
authors.lastname: Wexler
authors.forename: Patrick Y S
authors.initials: PY
authors.lastname: Lam
mesh_terms: D000925:Anticoagulants / Q000138:chemical synthesis* / Q000494:pharmacology; D065427:Factor Xa Inhibitors; D006801:Humans; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013379:Substrate Specificity; D013923:Thromboembolism / Q000188:drug therapy
chemical_list: D000925:Anticoagulants; D065427:Factor Xa Inhibitors; D011744:Pyrimidinones; D015842:Serine Proteinase Inhibitors