Patent number: 9469608
Abstract: Compounds of the invention, which may be useful in inhibiting thrombin and associated thrombotic occlusions, have the following structure: or a pharmaceutically acceptable salt thereof, wherein m is 0 or 1; R is a heterocycle, —(CR8R9)1-2NH2, or —(CR8R9)1-2OH, wherein R8and R9, each time in which they occur, are independently H, C1-6alkyl, —CH2F, —CHF2, CF3or —CH2OH; W is a) —CHR1R2, where R1is —C(CH3)3, and R2is —(CH2)1-2OH, b) a 5- or 6-membered unsubstituted or substituted heterocycle having 1 or 2 heteroatoms selected from N and O, wherein substituted heterocycle is substituted with R3, c) a 9- or 10-membered unsubstituted or substituted heterocycle having 1 or 2 heteroatoms selected from N, O and S, wherein substituted heterocycle is mono-substituted with R3, or disubstituted with R3and R4, or d) a 3-, 4-, or 5-membered carbocyclic ring which is unsubstituted, mono-substituted with R3, di-substituted with R3and R4, or tri-substituted with R3, R4and R5; R3is —CF3, —COOH, —COOR7, —C(O)R6, —CH(OH)R6,
Type:
Grant
Filed:
November 15, 2013
Date of Patent:
October 18, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Harry Chobanian, Tesfaye Biftu, Barbara Pio, Zhicai Wu
Publication number: 20150315141
Abstract: Compounds of the invention, which may be useful in inhibiting thrombin and associated thrombotic occlusions, have the following structure: or a pharmaceutically acceptable salt thereof, wherein m is 0 or 1; R is a heterocycle, —(CR8R9)1-2NH2, or —(CR8R9)1-2OH, wherein R8 and R9, each time in which they occur, are independently H, C1-6 alkyl, —CH2F, —CHF2, CF3 or —CH2OH; W is a) —CHR1R2, where R1 is —C(CH3)3, and R2 is —(CH2)1-2OH, b) a 5- or 6-membered unsubstituted or substituted heterocycle having 1 or 2 heteroatoms selected from N and O, wherein substituted heterocycle is substituted with R3, c) a 9- or 10-membered unsubstituted or substituted heterocycle having 1 or 2 heteroatoms selected from N, O and S, wherein substituted heterocycle is mono-substituted with R3, or disubstituted with R3 and R4, or d) a 3-, 4-, or 5-membered carbocyclic ring which is unsubstituted, mono-substituted with R3, di-substituted with R3 and R4, or tri-substituted with R3, R4 and R5; R3 is —CF3, —COOH, —COOR7, —C(O)R6, —CH
Type:
Application
Filed:
November 15, 2013
Publication date:
November 5, 2015
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Harry Chobanian, Tesfaye Biftu, Barbara Pio, Zhicai Wu