Patent ID: 6127371
Filing Date: 2000-10-03
Classification: A61P,C07D

Abstract:
A compound of Formula (I): ##STR18## wherein Z is ##STR19## wherein D, E, F and G may be N, or CR.sub.1 provided: 1) no more than two are nitrogens;2) not all are CR.sub.1 ;3) the ring formed is not pyrimidine or pyridine;P is tetraxol-2-yl, CO.sub.2 R.sub.6 or C(O)N(R.sub.6)S(O).sub.1 R.sub.10 ;R.sub.a is hydrogen or C.sub.1-6 alkyl;R.sub.1 is independently hydrogen, Ar, C.sub.1-6 alkyl, or C.sub.1-6 alkoxy;R.sub.2 is Ar, C.sub.1-8 alkyl, C(O)R.sub.14 or ##STR20## R.sub.3 and R.sub.5 are independently R.sub.13 OH, C.sub.1-8 alkoxy, S(O).sub.q R.sub.11, N(R.sub.6).sub.2, NO.sub.2, Br, F, I, Cl, CF.sub.3 NHCOR.sub.6 R.sub.13 CO.sub.2 R.sub.7, --X--R.sub.9 --Y, --X(C(R.sub.6).sub.2)OR.sub.6, --(CH.sub.2).sub.m X'R.sub.8 or --X(CH.sub.2).sub.n R.sub.8 wherein each methylene group with --X(CH.sub.2).sub.n R.sub.8 may be unsubstituted or substituted by one or two --(CH.sub.2).sub.n Ar groups;R.sub.4 is independently R.sub.11, OH, C.sub.1-5 alkoxy, S(O).sub.1 R.sub.11, N(R.sub.6).sub.2, Br, F, I, Cl or NHCOR.sub.6, wherein the C.sub.1-5 alkoxy may be unsubstituted or substituted by OH, methoxy or halogen;R.sub.6 is independently hydrogen or C.sub.1-8 alkyl;R.sub.7 is independently hydrogen, C.sub.1-10 alkyl, C.sub.2-10 alkenyl or C.sub.2-8 alkynyl, all of which may be unsubsidized or substituted by one or more OH, N(R.sub.6).sub.2, CO.sub.2 R.sub.12, halogen or XC.sub.1-10 alkyl; or R.sub.7 is (CH.sub.2).sub.n Ar;R.sub.8 is independently R.sub.11, CO.sub.2 R.sub.7, CO.sub.2 C(R.sub.11).sub.2 O(CO)XR.sub.7, PO.sub.3 (R.sub.7).sub.2, SO.sub.2 NR.sub.7 R.sub.11, NR.sub.7 SO.sub.2 R.sub.11, CONR.sub.7 SO.sub.2 R.sub.11, SO.sub.3 R.sub.7, SO.sub.2 R.sub.7, P(O)(OR.sub.7)R.sub.7, CN, CO.sub.2 (CH.sub.2).sub.m (C(O)N(R.sub.6).sub.2, C(R.sub.11).sub.2 N(R.sub.7).sub.2, C(O)N(R.sub.6).sub.2, NR.sub.7 C(O)NR.sub.7 C(O)NR.sub.7 SO.sub.2 R.sub.11, OR.sub.6, or tetraxole which is substituted or unsubstituted by C.sub.1-6 alkyl;R.sub.9 is independently a bond, C.sub.1-10 alkylene, C.sub.1-10 alkenylene, C.sub.1-10 alkylidene, C.sub.1-10 alkenylene, all of which may be linear or branched, or phenylene, all of which may be unsubsidized or substituted by one or more OH, N(R.sub.6).sub.2, COOH or halogen;R.sub.10 is independently C.sub.1-10 alkyl, N(R.sub.6).sub.2 or Ar;R.sub.11 is independently hydrogen, Ar, C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, all of which may be unstubsituted or substituted by one or more OH, CH.sub.2 OH, N(R.sub.6).sub.2 or hydrogen;R.sub.12 is independently hydrogen, C.sub.1-6 alkenyl or C.sub.2-7 alkynyl;R.sub.13 is independently divalent, AR, C.sub.1-10 alkylene, C.sub.1-10 alkylidene, C.sub.2-10 alkenylene, all of which may be unsubstituted substituted by one ore more OH, CH.sub.2 OH, N(R.sub.6).sub.2 or halogen,R.sub.14 is independently hydrogen, C.sub.1-10 alkyl, XC.sub.1-10 alkyl, Ar or X Ar;R.sub.15 is independently C.sub.1-6 alkyl or phenyl substituted by one or two C.sub.1-6 alkyl, OH, C.sub.1-5 alkoxy, S(O).sub.1 R.sub.6 N(R.sub.6).sub.2, Br, F, I, Cl, CF.sub.3 or NHCOR.sub.6 ;X is independently (CH.sub.2).sub.n, O, NR.sub.6 or S(O).sub.q ;X' is independently O, NR.sub.6 or S(O).sub.q ; Y is independently CH.sub.3 X(CH.sub.2).sub.n Ar;Ar is independently: ##STR21## naphtyl, indoyly, pyridyl, thienyl, ozaolidinyl, thiazolyl, isothiazolyl, pyraxolyl, triazolyl, tetrazoly, imidazolyl, imidazolindinyl, thiazolindinyl, isoxazolyl, oxadiazolyl, thiadiazolyl, morpholinyl, piperidinyl, piperazinyl, pyrrolyl, or pyrimidyl; all of which may be unsubstituted or substituted by one or more Z.sub.1 or Z.sub.2 groups;A is independently C.dbd.O, or (C(R.sub.6 .sub.2).sub.m ;B is independently --CH.sub.2 -- or --O--;Z.sub.1 and Z.sub.2 are independently hydrogen, XR.sub.6, C.sub.1-8 alkyl, (CH.sub.2).sub.q CO.sub.2 R.sub.6, C(O)N(R.sub.6).sub.2, CN, (CH.sub.2).sub.n OH, NO.sub.2, F, Cl, Br, I, N(R.sub.6).sub.2, NHC(O)R.sub.6, O(CH.sub.2).sub.m C(O)NR.sub.a SO.sub.2 R.sub.15, (CH.sub.2).sub.m OC(O)NR.sub.a SO.sub.2 R.sub.15, O(CH.sub.2).sub.m NR.sub.a C(O)NR.sub.a SO.sub.2 R.sub.15 or tetrazolyl which may be substituted or unsubstituted by C.sub.1-6 alkyl, CF.sub.3 or C(O)R.sub.6 ;m is independently 1 to 3;n is independently 0 to 6;q is independently 0, 1 or 2;provided R.sub.3 and R.sub.5 are not O--O--(CH.sub.2).sub.n Ar or O--0 R.sub.6 ; or a pharmaceutically acceptable salt thereof.