Patent ID: 6319946
Filing Date: 2001-11-20
Classification: A61P,C07C,C07D,C07F

Abstract:
A compound of formula I: ##STR1587##or a pharmaceutically acceptable salt thereof, wherein:E' is --SO.sub.2 --;A is --R.sup.1 --Ht;R.sup.1 is --O--C(O)--;Ht is a 5-membered saturated or unsaturated heterocycle, containing one or more oxygen; wherein said heterocycle is optionally fused to Q; and wherein said Ht is optionally substituted with one or more substituents independently selected from oxo, --OR.sup.2, SR.sup.2, --R.sup.2, --N(R.sup.2)(R.sup.2), --R.sup.2 --OH, --CN, --CO.sub.2 R.sup.2, --C(O)--N(R.sup.2).sub.2, --S(O).sub.2 --N(R.sup.2).sub.2, --N(R.sup.2)--C(O)--R.sup.2, --N(R.sup.2)--C(O)O--R.sup.2, --C(O)--R.sup.2, --S(O).sub.n --R.sup.2, --OCF.sub.3, --S(O).sub.n --Q, methylenedioxy, --N(R.sup.2)--S(O).sub.2 (R.sup.2), halo, --CF.sub.3, --NO.sub.2, Q or --OQ;each Q is independently selected from a 3-7 membered saturated, partially saturated or unsaturated carbocyclic ring system; or a 5-7 membered saturated, partially saturated or unsaturated heterocyclic ring containing one or more heteroatoms selected from O, N, or S; wherein Q is optionally substituted with one or more groups selected from oxo, --OR.sup.2, --R.sup.2, --SO.sub.2 R.sup.2, --SO.sub.2 --N(R.sup.2).sub.2, --N(R.sup.2).sub.2, --N(R.sup.2)--C(O)--R.sup.2, --R.sup.2 --OH, --CN, --CO.sub.2 R.sup.2, --C(O)--N(R.sup.2).sub.2, halo, --CF.sub.3 ;each R.sup.2 is independently selected from H, or C.sub.1 -C.sub.4 alkyl; and wherein said alkyl, when not a substituent of Q, is optionally substituted with Q or --OR.sup.3 ; wherein when said R.sup.2 is an --OR.sup.3 substituted moiety, said R.sup.3 in --OR.sup.3 may not be --OR.sup.2 substituted;B, when present, is --N(R.sup.2)--C(R.sup.3).sub.2 --C(O)--;each x is independently 0 or 1;each R.sup.3 is independently selected from H, Ht, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 cycloalkyl or C.sub.5 -C.sub.6 cycloalkenyl; wherein any member of said R.sup.3, except H, is optionally substituted with one or more substituents selected from --OR.sup.2, --C(O)--NH--R.sup.2, --S(O).sub.n --N(R.sup.2)(R.sup.2), --N(R.sup.2).sub.2, --N(R.sup.2)--C(O)--O(R.sup.2), --N(R.sup.2)--C(O)--N(R.sup.2), --N(R.sup.2)--C(O)--(R.sup.2), Ht, --CN, --SR.sup.2, --CO.sub.2 R.sup.2, or NR.sup.2 --C(O)--R.sup.2 ;each n is independently 1 or 2;G, when present, is selected from R.sup.7 or C.sub.1 -C.sub.4 alkyl, or, when G is C.sub.1 -C.sub.4 alkyl, G and R.sup.7 are optionally bound to one another through a C.sub.1 -C.sub.3 linker to form a heterocyclic ring;D is selected from Q; C.sub.1 -C.sub.6 alkyl optionally substituted with one or more groups selected from C.sub.3 -C.sub.6 cycloalkyl, --OR.sup.2, --S--Ht, --R.sup.3, --O--Q or Q; C.sub.2 -C.sub.4 alkenyl optionally substituted with one or more groups selected from --OR.sup.2, --S--Ht, --R.sup.3, --O--Q or Q; C.sub.3 -C.sub.6 cycloalkyl optionally substituted with or fused to Q; or C.sub.5 -C.sub.6 cycloalkenyl optionally substituted with or fused to Q;D' is selected from C.sub.1 -C.sub.15 alkyl, C.sub.2 -C.sub.15 alkenyl or C.sub.2 -C.sub.15 alkynyl, each of which contains one or more substituents selected from oxo, halo, --CF.sub.3, --OCF.sub.3, --NO.sub.2, azido, --SH, --SR.sup.3, --N(R.sup.3)--N(R.sup.3).sub.2, --O--N(R.sup.3).sub.2, --(R.sup.3)N--O--(R.sup.3), --N(R.sup.3).sub.2, --CN, --CO.sub.2 R.sup.3, --C(O)--N(R.sup.3).sub.2, --S(O).sub.n --N(R.sup.3).sub.2, --N(R.sup.3)--C(O)--R.sup.3, --N(R.sup.3)--C(O)--N(R.sup.3).sub.2, --N(R.sup.3)--C(O)--S(R.sup.3), --C(O)--R.sup.3, --S(O).sub.n --R.sup.3, --N(R.sup.3)--S(O).sub.n (R.sup.3), --N(R.sup.3)--S(O).sub.n --N(R.sup.3).sub.2, --S--NR.sup.3 --C(O)R.sup.3, --C(S)N(R.sup.3).sub.2, --C(S)R.sup.3, --NR.sup.3 --C(O)OR.sup.3, --O--C(O)OR.sup.3, --O--C(O)N(R.sup.3).sub.2, --NR.sup.3 --C(S)R.sup.3, .dbd.N--OH, .dbd.N--OR.sup.3, .dbd.N--N(R.sup.3).sub.2, .dbd.NR.sup.3, .dbd.NNR.sup.3 C(O)N(R.sup.3).sub.2, .dbd.NNR.sup.3 C(O)OR.sup.3, .dbd.NNR.sup.3 S(O).sub.n --N(R.sup.3).sub.2, --NR.sup.3 --C(S)OR.sup.3, --NR.sup.3 --C(S)N(R.sup.3).sub.2, --NR.sup.3 --C[.dbd.N(R.sup.3)]--N(R.sup.3).sub.2, --N(R.sup.3)--C[.dbd.N--NO.sub.2 ]--N(R.sup.3).sub.2, --N(R.sup.3)--C[.dbd.N--NO.sub.2 ]--OR.sup.3, --N(R.sup.3)--C[.dbd.N--CN]--OR.sup.3, --N(R.sup.3)--C[.dbd.N--CN]--(R.sup.3).sub.2, --OC(O)R.sup.3, --OC(S)R.sup.3, --OC(O)N(R.sup.3).sub.2, --C(O)N(R.sup.3)--N(R.sup.3).sub.2, --O--C(O)N(R.sup.3)--N(R.sup.3).sub.2, O--C(O)N(OR.sup.3)(R.sup.3), N(R.sup.3)--N(R.sup.3)C(O)R.sup.3, N(R.sup.3)--OC(O)R.sup.3, N(R.sup.3)--OC(O)R.sup.3, N(R.sup.3)--OC(O)R.sup.3, --OC(S)N(R.sup.3).sub.2, --OC(S)N(R.sup.3)(R.sup.3), or PO.sub.3 --R.sup.3 ;E is benzodioxole, which is optionally substituted with one or more substituents independently selected from oxo, --OR.sup.2, SR.sup.2, --R.sup.2, --N(R.sup.2)(R.sup.2), --R.sup.2 --OH, --CN, --CO.sub.2 R.sup.2, --C(O)--N(R.sup.2).sub.2, --S(O).sub.2 --N(R.sup.2).sub.2, --N(R.sup.2)--C(O)--R.sup.2, --N(R.sup.2)--C(O)O--R.sup.2, --C(O)--R.sup.2, --S(O).sub.n --R.sup.2, --OCF.sub.3, --S(O).sub.n --Q, methylenedioxy, --N(R.sup.2)--S(O).sub.2 (R.sup.2), halo, --CF.sub.3, --NO.sub.2, Q or --OQ; andeach R.sup.7 is hydrogen.