Patent ID: 6011059
Filing Date: 2000-01-04
Classification: A61P,C07C,C07D

Abstract:
A compound having the structure ##STR452## wherein n is an integer from 1 to 5; X is C--R.sup.5 wherein R.sup.5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl;R.sup.1 is H, alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, (alkyl or aryl).sub.3 Si (where each alkyl or aryl group is independent), cycloalkyl, cycloalkenyl, amino, alkylamino, alkenylamino, alkynylamino, arylalkylamino, aryl, arylalkyl, arylamino, aryloxy, cycloheteroalkyl, cycloheteroalkylalkyl, heteroaryl, heteroarylamino, heteroaryloxy, arylthio, arylsulfinyl, arylsulfonyl, thio, alkylthio, alkylsulfinyl, alkylsulfonyl, heteroarylthio, heteroarylsulfinyl, heteroarylsulfonyl, halogen, haloalkyl, polyhaloalkyl, polyhaloalkoxy, aminothio, aminosulfinyl, aminosulfonyl, alkylsulfonylamino, alkenylsulfonylamino, alkynylsulfonylamino, arylsulfonylamino, heteroarylsulfonylamino, alkylaminocarbonyl, arylaminocarbonyl, heteroarylaminocarbonyl, hydroxy, acyl, carboxy, aminocarbonyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonyloxy, alkylcarbonylamino, arylcarbonyl, arylcarbonyloxy, arylcarbonylamino, heteroarylcarbonyl, heteroaryl-carbonyloxy, heteroarylcarbonylamino, cyano, nitro, alkenylcarbonylamino, alkynylcarbonylamino, alkylaminocarbonylamino, alkenylaminocarbonylamino, alkynylaminocarbonylamino, arylaminocarbonylamino, heteroarylaminocarbonylamino, alkoxycarbonylamino, alkenyloxycarbonylamino, alkynyloxycarbonylamino, aryloxycarbonylamino, heteroaryloxycarbonylamino, aminocarbonylamino, alkylaminocarbonyloxy, alkoxycarbonylamino; 1,1-(alkoxyl or aryloxy).sub.2 alkyl (where the two aryl or alkyl substituents can be independently defined, or linked to one another to form a ring), S(O).sub.2 R.sup.6 R.sup.7, --NR.sup.6 (C.dbd.NR.sup.7)alkyl, --NR.sup.6 (C.dbd.NR.sup.7)alkenyl, --NR.sup.6 (C.dbd.NR.sup.7)alkynyl, --NR.sup.6 (C.dbd.NR.sup.7)heteroaryl, --NR.sup.8 (C.dbd.NCN)-amino, ##STR453## pyridine-N-oxide, ##STR454## (where Z is O or H.sub.2 and n' is 0, 1, 2 or 3) or ##STR455## tetrazolyl, imidazole, oxazole or triazole, --PO(R.sup.13) (R.sup.14), (where R.sup.13 and R.sup.14 are independently alkyl, aryl, alkoxy, aryloxy, heteroaryl, heteroarylalkyl, heteroaryloxy, heteroarylalkoxy, cycloheteroalkyl, cycloheteroalkylalkyl, cycloheteroalkoxy, or cycloheteroalkylalkoxy);R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are independently hydrogen, alkyl, haloalkyl, aryl, heteroaryl, arylalkyl, cycloalkyl or (cycloalkyl)alkyl, or cycloheteroalkyl;and R.sup.1 is optionally substituted with from one to five substituentsR.sup.2, R.sup.3 and R.sup.4 are the same or different and are independently any of the groups set out for R.sup.1 and is optionally substituted with from one to five substituents or R.sup.1. R.sup.2, R.sup.3 and/or R.sup.4 is optionally joined together with the carbons to which they are attached to form a non-aromatic ring;or a pharmaceutically acceptable salt thereof, a prodrug ester thereof, or a stereoisomers thereof;with the proviso that (1) at least one of R.sup.1, R.sup.2, R.sup.3, R.sup.4 is other than H; (2) R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is other than alkyl having an amino substituent.