A novel series of triaryloxypyridines have been designed to inhibit factor Xa, a serine
protease strategically located in the coagulation cascade. Inhibitor 5e has a KI against factor …

A novel series of diaryloxypyridines have been designed as selective nanomolar factor Xa
(fXa) inhibitors for use as anticoagulants. In this paper, we describe our efforts to identify an …

A novel series of 2, 6-diphenoxypyridines has been designed to inhibit factor Xa, a serine
protease strategically located in the coagulation cascade. The evolution from the …

Publisher Summary This chapter focuses on the advances reported in 1999 in the design
and discovery of novel factor Xa inhibitors as potential orally active anticoagulants. Factor …

A systematic modification of the C3 side-chain of the β-aminoester class of factor Xa
inhibitors and a survey of P4 variations is described. These changes have resulted in the …

Factor Xa, a serine protease, is at the critical juncture between the intrinsic and extrinsic
pathways of the coagulation cascade. Inhibition of factor Xa has the potential to provide …

A series of novel 2, 7-disubstituted tetrahydroisoquinoline derivatives were designed and
synthesized. Among these derivatives, compounds 1 and 2 exhibited potent inhibitory …

Benzothiophene-anthranilamide 1 (3-chloro-N-[2-[[(4-fluorophenyl) amino] carbonyl]-4-
methylphenyl] benzo [b] thiophene-2-carboxamide) was discovered by high throughput …

A series of novel 2, 7-disubstituted tetrahydroisoquinoline derivatives were designed and
synthesized. Among these derivatives, compounds 1 and 2 (JTV-803) exhibited potent …

Highly potent and selective substrate analogue factor Xa inhibitors were obtained by
incorporation of non-basic or modestly basic P1 residues known from the development of …