| 主权项 |
1. An 11β-hydroxyandrosta-4-ene-3-one compound of formula I, or a physiologically acceptable salt thereof:wherein
represents double bond and represents α or β-configuration; Z represents O or S; R1 represents hydrogen or methyl which may be either in α or β-configuration; R2 and R3 are the same or different and each independently represents hydrogen, halogen, or methyl; R5 is independently selected from the group consisting of (C1-C4)-alkyl, (C3-C6)-cycloalkyl, —O—(C1-C4)-alkyl, and a phenyl ring or heterocyclic ring selected from the group consisting of thienyl and furyl, wherein the ring or ring system is unsubstituted or substituted by one or more of halogen, —OH, and (C1-C3)-alkyl, wherein the alkyl or cycloalkyl groups are optionally substituted by one or more of halogen, (C1-C3)-alkyl, —O—(C1-C3)-alkyl, and (C3-C6)-cycloalkyl; R4 represents moiety:wherein
m1 is 1; m2 is 0 or 1; m3 is 0 or 1; n1 is 0, 1 or 2; P and Q are hydrogen; X represents either a double bond or a triple bond; J and K are independently selected from the group consisting of hydrogen and (C1-C3)-alkyl; and L is selected from the group consisting of halogen, —OH, —O—(C1-C4)-alkyl, —OCO—(C1-C6)-alkyl, —OCO—(C3-C13)-cycloalkyl, —OCO—CO—O—(C1-C4)-alkyl, —OCO—O—(C1-C10)-alkyl, —OCO—O—(C3-C6)-cycloalkyl, —OCO—NH—(C1-C4)-alkyl, —OCO—N—[(C1-C4)-alkyl]2, and —N—[(C1-C8)-alkyl]2; wherein
the alkyl or cycloalkyl groups of J, K or L are optionally substituted by one or more of halogen, —OH, (C1-C3)-alkyl, —O—(C1-C3)-alkyl, —OCO—(C1-C3)-alkyl, —COOH, —COO—(C1-C5)-alkyl, —COO—(C1-C5)-haloalkyl, —NHCO—(C1-C8)-alkyl, —ONO2, and (C3-C6)-cycloalkyl;J and K are optionally joined together with the carbon atom to which they are attached to represent a (C3-C6)-cycloalkyl or —CO— group and L is selected from hydroxyl and O(C1-C3)alkyl; andJ, K and L are absent when n1 is 0. |
