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US 5,627,211 AGranted
Cyclohexyl amine derivatives and their use as tachykinin antagonists
AssigneeMerck Sharp & Dohme Corp.
InventorMartin R. Teall
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I), and salts and prodrugs thereof wherein X, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.7 and R.sup.8 are defined herein, are tachykinin receptor antagonists. ##STR1##
Claims14
A compound of formula (I), or a salt or prodrug thereof:
- ##STR9## wherein X represents O or S;
- R.sup.1 represents phenyl optionally substituted by 1, 2 or 3 groups selected from C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, --OR.sup.a, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a CO.sub.2 R.sup.b, --CO.sub.2 R.sup.a or --CONR.sup.a R.sup.b ;
- R.sup.2 represents phenyl optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo or trifluoromethyl;
- R.sup.3 and R.sup.4 each independently represent H, COR.sup.a, CO.sub.2 R.sup.a or C.sub.1-6 alkyl optionally substituted by a group selected from (CO.sub.2 R.sup.a, CONR.sup.a R.sup.b, hydroxy, cyano, COR.sup.a, NR.sup.a R.sup.b, and phenyl optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo or trifluoromethyl);
- R.sup.5 represents H or XCH.sub.2 R.sup.6 wherein R.sup.6 represents phenyl optionally substituted by 1, 2 or 3 groups selected from C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, --OR.sup.a, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a CO.sub.2 R.sup.b, --CO.sub.2 R.sup.a or --CONR.sup.a R.sup.b and X is as previously defined;
- R.sup.7 and R.sup.8 each independently represent H or C.sub.1-6 alkyl;
- and
- R.sup.a and R.sup.b each independently represent H, C.sub.1-6 alkyl, phenyl or trifluoromethyl
- with the exception of 2-amino-2-phenyl-1-benzyloxycyclohexane.
6 more elements
A compound which is selected from:
- 1-(3,5-dimethylbenzyloxy)-2-amino-2-phenylcyclohexane;
- 1-(3,5-dimethylbenzyloxy)-2-dimethylamino-2-phenylcyclohexane;
- 1-(3,5-dimethylbenzyloxy)-2-methoxycarbonylmethylamino-2-phenylcyclohexane;
- 1-(3,5-dimethylbenzyloxy)-2-(carboxamido)methylamino-2-phenylcyclohexane;
- 1-(bis-3,5-trifluoromethylbenzyloxy)-2-amino-2-phenylcyclohexane;
- 1-(bis-3,5-trifluoromethylbenzyloxy)-2-(carboxamido)methylamino-2-phenylcyc lohexane;
- 1,5-bis-(3,5-dimethylbenzyloxy)-2-amino-2-phenylcyclohexane;
- and salts and prodrugs thereof.
5 more elements
Dependencies are inferred from the claim text.