Back to results
US 5,495,047 AGranted
Fused tricyclic compounds, pharmaceutical compositions containing them and their use in therapy
AssigneeMerck Sharp & Dohme Corp.
InventorsMonique B. Van Niel, Brian J. Williams, Walfred S. Saari
Life of this patent
Estimating the term…
Abstract
Fused tricyclic compounds of formula (I) as disclosed herein, and salts and prodrugs thereof, are tachykinin antagonists, useful for treating pain.
Claims12
A compound of formula (I), or a salt or prodrug thereof:
- ##STR9## wherein Q represents a group ##STR10## where W represents a bond, O, S, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or a group NR.sup.6, where R.sup.6 is H or C.sub.1-6 alkyl and one or both of the phenyl rings may be replaced by a heteroaryl moiety;
- X and Y each represent H or X and Y together form a group .dbd.O;
- Z represents O, S or NR.sup.8, where R.sup.8 represents H or C.sub.1-6 alkyl;
- R.sup.1 and R.sup.2 independently represent H;
- C.sub.1-6 alkyl optionally substituted by hydroxy, cyano, COR.sup.a, COOR.sup.a, CONR.sup.a R.sup.b, COC.sub.1-4 alkylNR.sup.a R.sup.b, CONR.sup.a C.sub.1-4 alkylCONR.sup.a R.sup.b or NR.sup.a R.sup.b, (where R.sup.a and R.sup.b each independently represent H, C.sub.1-6 alkyl, phenyl (optionally substituted by one or more of C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo and trifluoromethyl) or phenyl(C.sub.1-4 alkyl) (optionally substituted in the phenyl ring by one or more of C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo and trifluoromethyl));
- phenyl(C.sub.1-4 alkyl), (optionally substituted by one or more of C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo and trifluoromethyl in the phenyl ring);
- C.sub.2-6 alkylene;
- COC.sub.1-6 alkylhalo;
- COR.sup.a ;
- COOR.sup.a ;
- CONHR.sup.a ;
- COC.sub.1-4 alkylNR.sup.a R.sup.b ;
- or CONR.sup.a C.sub.1-4 alkylCONR.sup.a R.sup.b ;
- (where R.sup.a and R.sup.b are as previously defined) or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.p where p is 4 or 5 and where one non-terminal methylene group may optionally be replaced by an oxygen atom or a group NR.sup.x, where R.sup.x is H or C.sub.1-6 alkyl;
- R.sup.3 represents H or C.sub.1-6 alkyl;
- R.sup.4 represents H, C.sub.1-6 alkyl or phenyl (optionally substituted by one or more of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, SR.sup.c, SOR.sup.c, SO.sub.2 R.sup.c, OR.sup.c, NR.sup.c R.sup.d, NR.sup.c COR.sup.d, NR.sup.c COOR.sup.d, COOR.sup.c or CONR.sup.c R.sup.d, where R.sup.c and R.sup.d each independently represent H, C.sub.1-6 alkyl, phenyl or trifluoromethyl);
- R.sup.5 represents (CH.sub.2).sub.q phenyl, wherein q is 0, 1, 2 or 3 which may optionally be substituted in the phenyl ring by one or more of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, , SR.sup.c, SOR.sup.c, SO.sub.2 R.sup.c, OR.sup.c, NR.sup.c R.sup.d, NR.sup.c COR.sup.d, NR.sup.c COOR.sup.d, COOR.sup.c or CONR.sup.c R.sup.d, where R.sup.c and R.sup.d are as above defined;
- each R.sup.7 and R.sup.8 independently represents C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, SR.sup.c, SOR.sup.c, SO.sub.2 R.sup.c, OR.sup.c, NR.sup.c R.sup.d, NR.sup.c COR.sup.d, NR.sup.c COOR.sup.d, COOR.sup.c or CONR.sup.c R.sup.d, where R.sup.c and R.sup.d are as above defined;
- and
- m and n independently represent 0, 1, 2, 3 or 4.
17 more elements
Dependencies are inferred from the claim text.