Patent ID: 6214807
Filing Date: 2001-04-10
Classification: A61P,C07H

Abstract:
A composition of matter having the formula: ##STR26##wherein R.sup.1 is --CH.sub.2 OH, and --C(.dbd.O)NR.sup.5 R.sup.6 ;R.sup.2 is selected from the group consisting of hydrogen, C.sub.1-15 alkyl, C.sub.2-15 alkenyl, C.sub.2-15 alkynyl, heterocyclyl, aryl, and heteroaryl, wherein the alkyl, alkenyl, alkynyl, aryl, heterocyclyl, and heteroaryl substituents are optionally substituted with from 1 to 3 substituents independently selected from the group consisting of halo, NO.sub.2, heterocyclyl, aryl, heteroaryl, CF.sub.3, CN, OR.sup.20, SR.sup.20, N(R.sup.20).sub.2, S(O)R.sup.22, SO.sub.2 R.sup.22, SO.sub.2 N(R.sup.20).sub.2, SO.sub.2 NR.sup.20 COR.sup.22, SO.sub.2 NR.sup.20 CO.sub.2 R.sup.22, SO.sub.2 NR.sup.20 CON(R.sup.20).sub.2, N(R.sup.20).sub.2 NR.sup.20 COR.sup.22, NR.sup.20 CO.sub.2 R.sup.22, NR.sup.20 CON(R.sup.20).sub.2, NR.sup.20 C(NR.sup.20)NHR.sup.23, COR.sup.20, CO.sub.2 R.sup.20, CON(R.sup.20).sub.2, CONR.sup.20 SO.sub.2 R.sup.22, NR.sup.20 SO.sub.2 R.sup.22, SO.sub.2 NR.sup.20 CO.sub.2 R.sup.22, OCONR.sup.20 SO.sub.2 R.sup.22, OC(O)R.sup.20, C(O)OCH.sub.2 OC(O)R.sup.20, and OCON(R.sup.20).sub.2 and wherein each optional heteroaryl, aryl, and heterocyclyl substituent is optionally substituted with halo, NO.sub.2, alkyl, CF.sub.3, amino, mono- or di- alkylamino, alkyl or aryl or heteroaryl amide, NCOR.sup.22, NR.sup.20 SO.sub.2 R.sup.22, COR.sup.20, CO.sub.2 R.sup.20, CON(R.sup.20).sub.2, NR.sup.20 CON(R.sup.20).sub.2, OC(O)R.sup.20, OC(O)N(R.sup.20).sub.2, SR.sup.20, S(O)R.sup.22, SO.sub.2 R.sup.22, SO.sub.2 N(R.sup.20).sub.2, CN, or OR.sup.20 ;R.sup.3, R.sup.4 are each individually selected from the group consisting of hydrogen, C.sub.1-15 alkyl, C.sub.2-15 alkenyl, C.sub.2-15 alkynyl, heterocyclyl, aryl, and heteroaryl, halo, NO.sub.2, CF.sub.3, CN, OR.sup.20, SR.sup.20, N(R.sup.20).sub.2, S(O)R.sup.22, SO.sub.2 R.sup.22, SO.sub.2 N(R.sup.20).sub.2, SO.sub.2 NR.sup.20 COR.sup.22, SO.sub.2 NR.sup.20 CO.sub.2 R.sup.22, SO.sub.2 NR.sup.20 CON(R.sup.20).sub.2, N(R.sup.20).sub.2 NR.sup.20 COR.sup.22, NR.sup.20 CO.sub.2 R.sup.22, NR.sup.20 CON(R.sup.20).sub.2, NR.sup.20 C(NR.sup.20)NHR.sup.23, COR.sup.20, CO.sub.2 R.sup.20, CON(R.sup.20).sub.2, CONR.sup.20 SO.sub.2 R.sup.22, NR.sup.20 SO.sub.2 R.sup.22, SO.sub.2 NR.sup.20 CO.sub.2 R.sup.22, OCONR.sup.20 SO.sub.2 R.sup.22, OC(O)R.sup.20, C(O)OCH.sub.2 OC(O)R.sup.20, and OCON(R.sup.20).sub.2 wherein the alkyl, alkenyl, alkynyl, aryl, heterocyclyl, and heteroaryl substituents are optionally substituted with from 1 to 3 substituents individually selected from the group consisting of halo, NO.sub.2, heterocyclyl, aryl, heteroaryl, CF.sub.3, CN, OR.sup.20, SR.sup.20, N(R.sup.20).sub.2, S(O)R.sup.22, SO.sub.2 R.sup.22, SO.sub.2 N(R.sup.20).sub.2, SO.sub.2 NR.sup.20 COR.sup.22, SO.sub.2 NR.sup.20 CO.sub.2 R.sup.22, SO.sub.2 NR.sup.20 CON(R.sup.20).sub.2, N(R.sup.20).sub.2 NR.sup.20 COR.sup.22, NR.sup.20 CO.sub.2 R.sup.22, NR.sup.20 CON(R.sup.20).sub.2, NR.sup.20 C(NR.sup.20)NHR.sup.23, COR.sup.20, CO.sub.2 R.sup.20, CON(R.sup.20).sub.2, CONR.sup.20 SO.sub.2 R.sup.22, NR.sup.20 SO.sub.2 R.sup.22, SO.sub.2 NR.sup.20 CO.sub.2 R.sup.22, OCONR.sup.20 SO.sub.2 R.sup.22, OC(O)R.sup.20, C(O)OCH.sub.2 OC(O)R.sup.20, and OCON(R.sup.20).sub.2 and wherein each optional heteroaryl, aryl, and heterocyclyl substituent is optionally substituted with halo, NO.sub.2, alkyl, CF.sub.3, amino, mono- or di- alkylamino, alkyl or aryl or heteroaryl amide, NCOR.sup.22, NR.sup.20 SO.sub.2 R.sup.22, COR.sup.20, CO.sub.2 R.sup.20, CON(R.sup.20).sub.2, NR.sup.20 CON(R.sup.20).sub.2, OC(O)R.sup.20, OC(O)N(R.sup.20).sub.2, SR.sup.20, S(O)R.sup.22, SO.sub.2 R.sup.22, SO.sub.2 N(R.sup.20).sub.2, CN, or OR.sup.20 ;R.sup.5 and R.sup.6 are each individually H, C.sub.1-15 alkyl with from 1 to 2 substituents independently selected from the group consisting of halo, NO.sub.2, heterocyclyl, aryl, heteroaryl, CF.sub.3, CN, OR.sup.20, SR.sup.20, N(R.sup.20).sub.2, S(O)R.sup.22, SO.sub.2 R.sup.22, SO.sub.2 N(R.sup.20).sub.2, SO.sub.2 NR.sup.20 COR.sup.22, SO.sub.2 NR.sup.20 CO.sub.2 R.sup.22, SO.sub.2 NR.sup.20 CON(R.sup.20).sub.2, N(R.sup.20).sub.2 NR.sup.20 COR.sup.22, NR.sup.20 CO.sub.2 R.sup.22, NR.sup.20 CON(.sup.20).sub.2, NR.sup.20 C(NR.sup.20)NHR.sup.23, COR.sup.20, CO.sub.2 R.sup.20, CON(R.sup.20).sub.2, CONR.sup.20 SO.sub.2 R.sup.22, NR.sup.20 SO.sub.2 R.sup.22, SO.sub.2 NR.sup.20 CO.sub.2 R.sup.22, OCONR.sup.20 SO.sub.2 R.sup.22, OC(O)R.sup.20, C(O)OCH.sub.2 OC(O)R.sup.20, and OCON(R.sup.20).sub.2 and wherein each optional heteroaryl, aryl, and heterocyclyl substituent is optionally substituted with halo, NO.sub.2, alkyl, CF.sub.3, amino, mono- or di- alkylamino, alkyl or aryl or heteroaryl amide, NCOR.sup.22, NR.sup.20 SO.sub.2 R.sup.22, COR.sup.20, CO.sub.2 R.sup.20, CON(R.sup.20).sub.2, NR.sup.20 CON(R.sup.20).sub.2, OC(O)R.sup.20, OC(O)N(R.sup.20).sub.2, SR.sup.20, S(O)R.sup.22, SO.sub.2 R.sup.22, SO.sub.2 N(.sup.20).sub.2, CN, or OR.sup.20 ;R.sup.20 is selected from the group consisting of H, C.sub.1-15 alkyl, C.sub.2-15 alkenyl, C.sub.2-15 alkynyl, heterocyclyl, aryl, and heteroaryl, wherein the alkyl, alkenyl, alkynyl, heterocyclyl, aryl, and heteroaryl substituents are optionally substituted with from 1 to 3 substituents independently selected from halo, alkyl, mono- or dialkylamino, alkyl or aryl or heteroaryl amide, CN, O--C.sub.1-6 alkyl, CF.sub.3, aryl, and heteroaryl; andR.sup.22 is a member selected from the group consisting of C.sub.1-15 alkyl, C.sub.2-15 alkenyl, C.sub.2-15 alkynyl, heterocyclyl, aryl, and heteroaryl, wherein the alkyl, alkenyl, alkynyl, heterocyclyl, aryl, and heteroaryl substituents are optionally substituted with from 1 to 3 substituents independently selected from halo, alkyl, mono- or dialkylamino, alkyl or aryl or heteroaryl amide, CN, O--C.sub.1-6 alkyl, CF.sub.3, and heteroaryl wherein, when R.sup.1.dbd.CH.sub.2 OH,R.sup.3 is H, R.sup.4 is H, and the pyrazole ring is attached through C.sup.4, and R.sup.2 is not H.