Patent ID: 6090839
Filing Date: 2000-07-18
Classification: A61K,C07D

Abstract:
A compound having the formula I or Ia: ##STR48## or a pharmaceutically acceptable salt thereof, wherein: A is a single or double bond;R.sup.1 is selected from a group consisting of: H, C.sub.1-15 alkyl, C.sub.2-15 alkenyl, C.sub.2-15 alkynyl and C.sub.3-10 cycloalkyl, said alkyl, alkenyl, alkynyl, and cycloalkyl optionally substituted with 1 to 3 groups of R.sup.a ;R.sup.2 is selected from a group consisting of: H, C.sub.1-15 alkyl, C.sub.2-15 alkenyl, OR.sup.3, CO.sub.2 alkyl, COalkyl, OH, --OC(O)R.sup.3, C.sub.2-15 alkynyl, C.sub.5-10 aryl, and heteroaryl, wherein said heteroaryl is selected from the group consisting of indole, benzothiophene, benzofuran, and dihydro derivatives thereof, said alkyl, alkenyl, alkynyl, aryl and heteroaryl optionally substituted with 1 to 3 groups of R.sup.a ;R.sup.3 is selected from a group consisting of: H, NHR.sup.1, NHacyl, C.sub.1-15 alkyl, C.sub.2-15 alkenyl, C.sub.1-15 alkoxy, CO.sub.2 alkyl, OH, C.sub.2-15 alkynyl, C.sub.5-10 aryl, and heteroaryl, wherein said heteroaryl is selected from the group consisting of indole, benzothiophene, benzofuran, and dihydro derivatives thereof, said alkyl, alkenyl, alkynyl, aryl and heteroaryl optionally substituted with 1 to 3 groups of R.sup.a ;R.sup.4 is selected from the group consisting of: R.sup.2, --D--R.sup.5 or ##STR49## R.sup.5 is selected from the group consisting of: C.sub.5-10 aryl and heteroaryl, wherein said heteroaryl is selected from the group consisting of indole, benzothiophene, benzofuran, and dihydro derivatives thereof, and said aryl and heteroaryl are optionally substituted with 1 to 3 groups of R.sup.a ; ##STR50## R.sup.8 is selected from the group consisting of CR.sup.6 R.sup.7, O, NR.sup.6, and S(O).sub.p ;R.sup.6 and R.sup.7 are independently selected from the group consisting of H and C.sub.1-6 alkyl;B is a 5 membered heterocycle containing 0 to 2 double bonds, and 1 heteroatom selected from the group consisting of O, S and N, the heteroatom being located at any allowable position on the five membered heterocycle, the heterocycle being optionally unsubstituted or substituted with 1 to 3 groups of R.sup.a ;D is selected from the group consisting of: O, S(O).sub.p and NR.sup.1 ;X.sup.1 and X.sup.2 are independently selected from a group consisting of: H, OH, C.sub.1-15 alkyl, C.sub.2-15 alkenyl, C.sub.2-15 alkynyl, halo, OR.sup.3, C.sub.5-10 aryl, C.sub.5-10 aralkyl, heteroaryl selected from the group consisting of indole, benzothiophene, benzofuran, and dihydro derivatives thereof, and C.sub.1-10 acyl, said alkyl, alkenyl, alkynyl, aryl and heteroaryl optionally substituted with 1 to 3 groups of R.sup.a ;R.sup.a represents a member selected from the group consisting of: halo, aryl, heteroaryl selected from the group consisting of indole, benzothiophene, benzofuran, and dihydro derivatives thereof, CF.sub.3, OCF.sub.3, CN, NO.sub.2, R.sup.3, OR.sup.3 ; SR.sup.3, S(O)R.sup.3, SO.sub.2 R.sup.3, NR.sup.3 R.sup.3, NR.sup.3 COR.sup.3, NR.sup.3 CO.sub.2 R.sup.3, NR.sup.3 CON(R.sup.3).sub.2, NR.sup.3 SO.sub.2 R.sup.3, COR.sup.3, CO.sub.2 R.sup.3, CON(R.sup.3).sub.2, SO.sub.2 N(R.sup.3).sub.2, OCON(R.sup.3).sub.2 said aryl and heteroaryl optionally substituted with 1 to 3 groups of halo or C.sub.1-6 alkyl;Y is NR.sup.1, except that if B and the aromatic ring to which it is fused form an indole ring, then Y may be NR.sup.1, O, or S;Y.sup.2 is selected from the group consisting of: O, N(C.sub.1-15) alkyl, N(CO.sub.2)alkyl, N--Oalkyl, N--Oacyl and N--OH, with the proviso that if Y.sup.2 is O and R.sup.3 is CH.sub.3 then n is 2;Y.sup.1 is selected from the group consisting of: O, NH, S(O).sub.p and CH.sub.2 ;Z is selected from the group consisting of: CO.sub.2 R.sup.3, CONHSO.sub.2 Me, CONH.sub.2 and 5-(1H-tetrazole);t and v are independently 0 or 1 such that t+v=1;n is 2-4 andp is 0-2.