Patent ID: 6011028
Filing Date: 2000-01-04
Classification: A61P,C07D

Abstract:
A compound having the formula: ##STR334## R.sup.1 is selected from the group consisting of C.sub.3 -C.sub.10 -cycloalkyl, C.sub.4 -C.sub.10 -heterocyclyl, and aryl, which may optionally be substituted by one or more of the following: C.sub.1 -C.sub.10 -alkyl, C.sub.2 -C.sub.10 -alkenyl, C.sub.2 -C.sub.10 -alkynyl, hydroxy, C.sub.1 -C.sub.10 -alkoxy, thiol, C.sub.1 -C.sub.10 -thioalkoxy, S(O)R.sup.9, S(O).sub.2 R.sup.9, halogen, nitro, amino, alkylamino, dialkylamino, aminoalkyl, dialkylaminoalkyl, arylamino, aminoaryl, alkylaminoaryl, acylamino, amidino, carboxyl, carboalkoxy, carboaryloxy, carboarylalkyloxy, cyano, aminocarbonylalkoxy, aminocarbonylamino, aminocarbonylaminoalkyl, haloalkyl, SO.sub.2 NR.sup.7 R.sup.9, wherein all said substitutions may be optionally substituted with one or more of the following: halogen, C.sub.1 -C.sub.10 -alkyl, amino, alkylamino, dialkylamino, aminoalkyl, aminoacyl, carboxyl, carboalkoxy, carboaryloxy, carboalkylaryloxy, hydroxy, C.sub.1 -C.sub.10 -alkoxy;L is selected from the group consisting of C.sub.1 -C.sub.10 -alkylene, C.sub.2 -C.sub.10 -alkenylene, C.sub.2 -C.sub.10 -alkynylene, and --(CH.sub.2).sub.m --D--(CH.sub.2).sub.n --;D is selected from the group consisting of O, S, SO, SO.sub.2, SO.sub.2 NR.sup.7, NR.sup.7 SO.sub.2, NR.sup.8, POOR.sup.7, PON(R.sup.7).sub.2, POOR.sup.7 NR.sup.7, NR.sup.7 POOR.sup.7, C(O), C(O)O;R.sup.7 is hydrogen, C.sub.1 -C.sub.10 -- alkyl, or aryl;R.sup.8 is hydrogen, C.sub.1 -C.sub.10 -alkyl, COR.sup.9, or CO.sup.2 R.sup.9 ;R.sup.9 is C.sub.1 -C.sub.10 -alkyl, or aryl;m=0 to 7;n=0 to 5;wherein L may optionally be substituted by one or more of the following: C.sub.1 -C.sub.10 -alkyl, C.sub.2 -C.sub.10 -alkenyl, C.sub.2 -C.sub.10 -alkynyl, hydroxy, C.sub.1 -C.sub.10 -alkoxy, thiol, C.sub.1 -C.sub.10 -thioalkoxy, S(O)R.sup.9, S(O).sub.2 R.sup.9, halogen, nitro, amino, alkylamino, dialkylamino, aminoalkyl, dialkylaminoalkyl, arylamino, aminoaryl, alkylaminoaryl, acylamino, carboxyl, carboalkoxy, carboaryloxy, carboarylalkyloxy, cyano, aminocarbonylalkoxy, aminocarbonylamino, aminocarbonylaminoalkyl, haloalkyl, SO.sub.2 NR.sup.7 R.sup.9, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.4 -C.sub.10 -heterocyclyl, aryl, heteroaryl, lactonyl, lactamyl, amidino, isourea, isothiourea, guanidino, substituted guanidino, wherein all said substitutions may be optionally substituted with one or more of the following: C.sub.1 -C.sub.10 -alkyl, amino, alkylamino, dialkylamino, aminoalkyl, aminoacyl, carboxyl, carboalkoxy, carboaryloxy, carboalkylaryloxy, hydroxy, C.sub.1 -C.sub.10 -alkoxy, nitro, amidino, guanidino, substituted guanidino, isourea, isothiourea andp=0 to 4A is selected from the group consisting of O, NR.sup.7, (CH.sub.2).sub.q, CH.dbd.CH;q is 1 to 2;B is selected from the group consisting of (CH.sub.2).sub.v, CH.dbd.CH;v=1 to 2;R.sup.2, R.sup.3 and R.sup.4 are independently selected from hydrogen C.sub.1 -C.sub.10 -alkyl, C.sub.2 -C.sub.10 -alkenyl, C.sub.2 -C.sub.10 -alkynyl, hydroxy, C.sub.1 -C.sub.10 -alkoxy, thiol, C.sub.1 -C.sub.10 -thioalkoxy, S(O)R.sup.9, S(O).sub.2 R.sup.9, halogen, nitro, amino, alkylamino, dialkylamino, aminoalkyl, dialkylaminoalkyl, arylamino, aminoaryl, alkylaminoaryl, acylamino, carboxyl, carboalkoxy, carboaryloxy, carboarylalkyloxy, cyano, aminocarbonylalkoxy, aminocarbonylamino, aminocarbonylaminoalkyl, haloalkyl, SO.sub.2 NR.sup.7 R.sup.9, wherein all said substitutions may be optionally substituted with one or more of the following: halogen, C.sub.1 -C.sub.10 -alkyl, amino, alkylamino, dialkylamino, aminoalkyl, aminoacyl, carboxyl, carboalkoxy, carboaryloxy, carboalkylaryloxy, hydroxy, C.sub.1 -C.sub.10 -alkoxy, andR.sup.2, R.sup.3 may optionally be taken together to form an exocyclic double bond, C.sub.3 -C.sub.10 -alicyclic hydrocarbon, C.sub.4 -C.sub.10 -heterocyclyl or aromatic hydrocarbon and said optionally formed unit may be optionally substituted with one or more of the following: C.sub.1 -C.sub.10 -alkyl, C.sub.2 -C.sub.10 -alkenyl, C.sub.2 -C.sub.10 -alkynyl which may be optionally substituted with carboxyl, carboalkoxy, carboaryloxy, carboxyalkylaryloxy and C.sub.1 -C.sub.10 -alkoxy; andR.sup.5, R.sup.6 are independently selected from the group consisting of hydrogen, hydroxy, and alkylalkoxy, wherein aryl wherever occurring means a 5- or 6-membered single aromatic radical which may include 0 to 4 heteroatoms,with the proviso that when X=S, A=(CH.sub.2).sub.q, B=(CH.sub.2).sub.v, q+v=2, or one of A or B is HC.dbd.CH and the other is not present, R.sup.2, R.sup.3, R.sup.4 are H, then R.sup.1 is not ##STR335## with the further proviso that when B is HC.dbd.CH and A is HC.dbd.CH, then X cannot be (CH.sub.2).sub.2 where p=0;and with the further provis that when X is (CH.sub.2).sub.p, p=1, A=(CH.sub.2).sub.q and B=(CH.sub.2).sub.v, where q, v is 1, R.sup.2 -R.sup.6 are H, L is CH.sub.2, R.sup.1 is not phenyl.