Patent ID: 6228868
Filing Date: 2001-05-08
Classification: A61P,C07D

Abstract:
A compound having Formula I ##STR7##or a pharmaceutically acceptable salt or prodrug thereof, whereinR.sup.A, R.sup.B, and R.sup.C are independently selected from the group consisting of(1) alkyl,(2) alkoxy,and(3) thioalkoxy;R.sup.D and R.sup.E are independently selected from the group consisting of(1) hydrogenand(2) alkyl;R.sup.2 is selected from the group consisting of(1) aryl and(2) heterocycle, wherein the heterocycle is selected from the group consisting of oxazole, isoxazole, thiazole, isothiazole, pyridine, pyridizine, pyrimidine, pyrazine, indole, isoindole, indolizine, indoline, benzo(b)thiene, 2,3-dihydrobenzothiene, benzo(b)furan, 2,3-dihydrobenzofuran, quinoline, isoguinoline, tetrahydrocuinoline, 4H-quinolizine, and imidazo(1,5-a)pyridine,wherein (1) and (2) can be optionally substituted with one, two, three, four, or five substituents independently selected from -L.sup.1 R.sup.6 wherein L.sup.1 is selected from the group consisting of(a) a covalent bond,(b) --C(X)--, wherein X is O or S,(c) --S(O).sub.t --, wherein t is 0, 1, or 2,(d) --NR3--, wherein R.sup.3 is selected from the group consisting of(i) hydrogen,(ii) carboxaldehyde,(iii) alkanoyl,(iv) --C(O)OR.sup.11, wherein R.sup.11 is alkyl which can be optionally substituted with one or two aryl substituents,(v) cycloalkyl,(vi) alkyl, wherein the alkyl can be optionally substituted with one substituent selected from the group consisting of(1') alkoxy,(2') cycloalkyl,and(3') aryl,and(vii) --C(O)R.sup.13, wherein R.sup.13 is perfluoroalkyl,(e) --O--,(f) --X'C(X)--, wherein X is defined previously and X' is O or S,(g)--C(X)X--,(h) --N(R.sup.3')C(O)N(R.sup.4')-- wherein R.sup.3' and R.sup.4' are independently selected from the group consisting of(i) hydrogenand(ii) alkyl,(i) --N(R )C(X)--, wherein R.sup.3' is defined above,(j) --C(X)N(R.sup.3')--, wherein R.sup.3' is defined above,(k) --NR.sup.3' S(O).sub.t --, wherein R.sup.3' is defined above,and(l) --S(O).sub.t NR.sup.3' -- wherein t and R.sup.3' are defined above,wherein (f)-(g) and (i)-(l) are drawn with their left ends attached to --R.sup.2 -- and their right ends attached to R.sup.6, and R.sup.6 is selected from the group consisting of(a) cyano,(b) nitro,(c)--XH,(d) halo,(e) --S(O).sub.t' NR.sup.3 R.sup.4, wherein R.sup.3 is defined above, t' is one or two, and R.sup.4 is selected from the group consisting of(i) hydrogen,(ii) cycloalkyl, and(iii) alkyl, wherein the alkyl can be optionally substituted with one substituent selected from the group consisting of(1') cycloalkyland(2) aryl,(f) --NR.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are hydrogen,with the proviso that when R.sup.6 is (a)-(f), --L.sup.1 -- is a covalent bond,(g) perfluoroalkyl,with the proviso that when R.sup.6 is perfluoroalkyl, --L.sup.1 -- is a covalent bond or --C(X)--, wherein X is O,(h) alkenyl,(i) alkynyl,(j) alkyl,and(k) cycloalkyl,wherein (h)-(k) can be optionally substituted with one, two, three, four, or five substituents independently selected from thegroup consisting of(i) hydroxyl,(ii) halo,(iii) --OR.sup.10, wherein R.sup.10 is defined above,(iv) --SR.sup.10, wherein R.sup.10 is defined above,(v) --CO.sub.2 R.sup.5, wherein R.sup.5 is defined above,(vi) --CHO,(vii) .dbd.X, wherein X is defined above,(viii) --N.sub.3,(ix) .dbd.C(H)NR.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are defined above,(x) cyano,(xi) --NOR.sup.3, wherein R.sup.3 is defined above,(xii) --NR.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are defined above,(xiii) --S(O).sub.t' NR.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are defined above,and(xiv) nitro,with the proviso that when R.sup.A, R.sup.B, and R.sup.C are alkoxyR.sup.2 is not dialkoxyphenylor trialkoxyphenyl.