Patent ID: 6048869
Filing Date: 2000-04-11
Classification: A61P,C07D

Abstract:
A compound of structural formula (I) having the natural steroidal trans-anti-trans relative configuration at the A,B and B,C ring junctures: ##STR145## or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein:the bonds designated with dotted lines ""a"", ""b"", ""c"" and ""d"" may be single bonds or double bonds, provided that when ""a"" is a double bond, the dotted lines ""b"", ""c"" and ""d"" must represent single bonds; and further provided that when ""b"" is a double bond, ""c"" or both ""c"" and ""d"" must represent double bonds;R.sup.1 is selected from hydrogen, C.sub.1-5 alkyl and CH.sub.2 R.sup.5 ;R.sup.2 is selected from:(1) hydrogen,(2) CO.sub.2 R.sup.4,(3) CONR.sup.4 R.sup.5,(4) ##STR146## (5) COR.sup.5, (6) S(O).sub.n R.sup.5,(7) NHCO.sub.2 R.sup.4,(8) NHCOR.sup.4,(9) NHCOR.sup.5,(10) CN,(11) COSR.sup.5,(12) C.sub.15 alkyl, and(13) C.sub.x X.sub.y ;R.sup.3 is selected from:(1) hydrogen,(2) C.sub.1-5 alkyl,(3) CO.sub.2 R.sup.4,(4) CONR.sup.4 R.sup.5,(5) COR.sup.5,(6) S(O).sub.n R.sup.5,(7) CN, and(8) C.sub.x X.sub.y ;R.sup.4 is selected from: hydrogen, and C.sub.1-10 straight or branched-chain alkyl;R.sup.5 is selected from:(1) hydrogen,(2) aryl,(3) aryl C.sub.1-4 alkyl,(4) diaryl C.sub.1-4 alkyl,(5) heteroaryl,(6) heteroaryl C.sub.1-4 alkyl,(7) C.sub.3-10 cycloalkyl, and(8) substituted aryl substituted by one, two or three substituents independently selected from:(a) --SH,(b) --SC.sub.1 -C.sub.4 alkyl,(c) --CN,(d) --CO--C.sub.1-8 alkyl,(e) --CO--aryl,(f) --C.sub.1-8 alkyl,(g) --C.sub.3 -C.sub.8 cycloalkyl,(h) -aryl,(i) -heteroaryl,(j ) --CO--heteroaryl,(k) --C.sub.1-4 alkyl-aryl,(l) --CONR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are independently selected from:(i) H,(ii) C.sub.1-8 alkyl,(iii) C.sub.3-8 cycloalkyl,(iv) aryl,or R.sup.6 and R.sup.7 together with the nitrogen to which they are attached form a 5-7 membered saturated heterocyclic ring containing 1-2 nitrogen atoms, and 0-1 oxygen atoms;(m) --NHCOR.sup.6,(n) --OCOR.sup.6,(o) --NR.sup.6 (CO)R.sup.7,(p) --NR.sup.6 (CO)NHR.sup.7,(q) --NHSO.sub.2 R.sup.6,(r) --OR.sup.6,(s) --NR.sup.6 R.sup.7,(t) --CO.sub.2 R.sup.6, and(u) C.sub.x X.sub.y ;X is independently selected from F and Cl at each occurrence;n is selected from 1 and 2;x is an integer from 1 to 4;y is 2x+1; andz is an integer from 3 to 5.