| 摘要 |
The indole derivatives have the formula I wherein: A is alkoxy, C0-5 alkyl-S(O)n-C0-5 alkyl, C0-5 alkyl-O-C0-5 alkyl, C0-5 alkyl-N(R18)-C0-5 alkyl or optionally substituted alkyl, cycloalkyl, alkenyl or alkynyl or is -C(R16)=N-(CH2)p- or a single bond; R0 is H, optionally substituted alkyl, aryl or aralkyl; R1 is nitrogen containing heterocyclic ring system as defined in the specification such as benzofuran, indole, pyridyl, benzimidazole, tetrazolyl, furan or thiazolyl; R2 is H, optionally substituted alkyl, aryl or aralkyl or is alkyl-OR11, alkyl-NR11R12, alkyl-CONR11R12, or C(NR11R12)NH or R2 and A together can form a ring of 5-7 atoms; R3, R4 and R5 are independently H, CN, nitro, perfluoroalkyl, perfluoroalkoxy, R11O-(CH2)p-, R11C(O)O-(CH2)p-, R11OC(O)-(CH2)p-, -(CH2)p-S(O)n-R17, -(CH2)p-C(O)-NR11R12 or halogen or are optionally substituted alkyl, alkenyl, alkynyl, aryl or aralkyl or R3 and R4 taken together can form a carbocyclic ring of 3-7 carbon atoms or a heterocyclic ring containing 1-3 heteroatoms of N, O or S; R6 is H, optionally substituted alkyl or aryl, perfluoroalkyl, CN, NO2, halo, R11O-(CH2)p-, NR12C(O)R11, NR12C(O)NR11R12 or -S(O)nR11; R7 is H or optionally substituted alkyl unless X is H or halo then R7 is absent; R8 is C(O)OR9, C(O)NR11R12, NR11R12, C(O)R11, NR12C(O)R11, NR12C(O)NR11R12, NR12-S(O)2R12, NR12S(O)2NR11R12, OC(O)R11, OC(O)NR11R12, OR11, S(O)nR11, S(O)nNR11R12 or optionally substituted alkyl unless X is H or halogen, then R8 is absent or R7 and R8 taken together form a carbocyclic ring of 3-7 ring atoms; R9 and R9a are independently H, optionally substituted alkyl, aralkyl or aryl when m is not 0 or are taken together to form a carbocyclic ring of 3-7 atoms or =O when m is not 0 or R9 and A are taken together to form a heterocyclic ring containing 3-7 carbons and one or more heteroatoms when m is not 0 or R10 and R10a are independently H, optionally substituted alkyl, aralkyl or aryl or are taken together to form a carbocyclic ring of 3-7 atoms or =O or R9 and R10 are taken together to form a carbocyclic ring of 3-7 carbons or a heterocyclic ring containing one or more heteroatoms when m is not 0 or R9 and R2 are taken together to form a heterocyclic ring of 3-7 carbons and one or more heteroatoms when m is not 0 or R10 and R2 are taken together to form a heterocyclic ring of 3-7 carbons and one or more heteroatoms or R10 and A are taken together to form a heterocyclic ring of 3-7 carbons and one or more heteroatoms and the rest of the variables are as defined in the specification. A pharmaceutical composition thereof is useful in the treatment of sex hormone dependent cancer or condition, benign prostatic hypertrophy or myoma of the uterus.
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