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Non-steroidal ligands for the estrogen receptor

  • US 5,877,219 A
  • Filed: 06/18/1997
  • Issued: 03/02/1999
  • Est. Priority Date: 04/25/1994
  • Status: Expired due to Term
First Claim
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1. A compound of Formula I:

  • ##STR12## wherein;

    ##STR13## R1 is --(CH2)n CR5

    CR6 R7 !;

    --(CH2)m C(X)NR8 R9 ;

    orR2 and R3 are independently H, --CH3, --OH, --OCH3, --OCH2 CH3 or --CH2 (CH3)2 !--CH(CH3)2 ;

    R4 is --CN, --NO2, --CH3, --CH2 CH3, --CH2 CH2 --Y or --Y;

    R5 and R6 are independently H, --C1-4 alkyl, --C2-4 alkenyl, --C2-4 alkynyl, --X--C1-3 alkyl, --X--C2-4 alkenyl, --X--C2-4 alkynyl or --Y;

    R7 is --CN, --C1-4 alkyl-OH, --C(O)O(CH3)3, --C(O)NR10 R11, --C(O)NR12 R13, --C1-4 alkyl-NR10 R11, --C(O)R12, --C(O)OR12, --C(O)NR12 OR13, --C(O)NHC(O)R12, --C(O)NHCH2 R12, --C(NH2)(NOR12), --S(O)R12, --S(O)(O)(OR12), --S(O)(O)(NHCO2 R12), --PO3 R12, --P(O)(NR12 R13)(NR12 R13), --P(O)(NR12 R13)(OR14), --CONR12 (CH2)q OCH3, --CONR12 (CH2)q NR8 R9 or oxadiazole substituted with methyl;

    R8 and R9 are independently hydrogen, --C1-7 alkyl, --C3-7 cycloalkyl, --O--C1-7 alkyl, --C1-7 alkyl-Y or phenyl;

    R10 and R11 are independently methyl or ethyl or, taken together form a morpholino group bonded via its nitrogen atom;

    R12, R13 and R14 are independently H, --C1-12 alkyl, --C2-12 alkenyl, --C2-12 alkynyl, --O--C1-12 alkyl, --O--C2-12 alkenyl, --O--C2-12 alkynyl, --C3-7 cycloalkyl, --C3-7 cycloalkenyl, linear and cyclic heteroalkyl, aryl, heteroaryl or --Y;

    X is oxygen or sulfur;

    Y is a halogen;

    n is an integer selected from 0, 1 and 2;

    m is the integer 1 or 2;

    p is an integer selected from 1 to 4; and

    q is an integer from 1-12.

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