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Use of progesterone receptor modulators

  • US 20070027201A1
  • Filed: 07/27/2006
  • Published: 02/01/2007
  • Est. Priority Date: 07/29/2005
  • Status: Abandoned Application
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Assignments
First Claim
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1. A method of inducing contraception, hormone replacement therapy, treating hormone-dependent disease, synchronizing estrus, or treating cycle-related symptoms in a mammal, the method comprising administering to a mammal in need thereof an effective amount of a compound having the structure of formula I, or a pharmaceutically acceptable salt thereof:

  • embedded imagewherein;

    R1 is selected from the group consisting of;

    H, SO2—

    C1-C6 alkyl, SO2—

    C3-C8 cycloalkyl, SO2-substituted C1-C6 alkyl, SO2-aryl, SO2-substituted aryl, SO2-heteroaryl, SO2-heterocycle, SO2—

    C3-C6 alkenyl, SO2—

    C3-C6 alkynyl, SO2—

    C3-C6 substituted alkenyl, SO2—

    C3-C6 substituted alkynyl, CN, C(O)—

    C1-C6 alkyl, C(O)—

    C3-C8 cycloalkyl, C(O)-substituted C1-C6 alkyl, C(O)-aryl, C(O)-substituted aryl, C(O)-heteroaryl, C(O)-heterocycle, C(O)—

    C3-C6 alkenyl, C(O)—

    C3-C6 alkynyl, C(O)-substituted C3-C6 alkenyl, C(O)-substituted C3-C6 alkynyl, C(O)O—

    C1-C6 alkyl, C(O)O—

    C3-C8 cycloalkyl, C(O)O-substituted C1-C6 alkyl, C(O)O-aryl, C(O)O-substituted aryl, C(O)O-heteroaryl, C(O)O-heterocycle, C(O)O—

    C3-C6 alkenyl, C(O)O—

    C3-C6 alkynyl, C(O)O—

    C3-C6 substituted alkenyl, C(O)O—

    C3-C6 substituted alkynyl, C(O)NH—

    C1-C6 alkyl, C(O)NH—

    C3-C8 cycloalkyl, C(O)N-di-C3-C8 cycloalkyl, C(O)N-di C1-C6 alkyl, C(O)N-di-substituted C1-C6 alkyl, C(O)NH-substituted C1-C6 alkyl, C(O)NH-aryl, C(O)N-(aryl)2, C(O)NH-substituted aryl, C(O)N-disubstituted aryl, C(O)NH-heteroaryl, C(O)N-diheteroaryl, C(O)NH-heterocycle, C(O)N-diheterocycle, C(O)NH—

    C3-C6 alkenyl, C(O)NH—

    C3-C6 alkynyl, C(O)O-substituted C3-C6 alkenyl, and C(O)O-substituted C3-C6 alkynyl;

    or R1 is a linking group to a second structure of formula I to form a dimer of formula I, said linking group selected from the group consisting of C(O)— and

    S(O)2—

    ;

    R2 is selected from the group consisting of H, C1-C6 alkyl, substituted C1-C6 alkyl, C3-C6 cycloalkyl, SO2-alkyl, and SO2-substituted alkyl;

    or R1 and R2 are joined to form —

    (C(R8)a(R9)b)c—

    SO2—

    (C(R8)d(R9)e)f;

    R8 and R9 are, independently, H, halogen, or C1 to C6 alkyl;

    a and b are, independently, 0 to 2, provided that a+b=2;

    d and e are, independently, 0 to 2, provided that a+b=2;

    c and f are, independently, 0 to 5, provided that one of c or f is greater than 0;

    R3, R4, R5 and R6 are independently selected from the group consisting of H, halogen, CN, C1-C6 alkyl, substituted C1-C6 alkyl, —

    (CHmXn)zCHpXq, C3-C6 cycloalkyl, O—

    C1-C6 alkyl, O—

    C1-C6 substituted alkyl, O—

    (CHmXn)zCHpXq, aryl, heteroaryl, heterocycle, substituted aryl, substituted heteroaryl, and substituted heterocycle;

    X is halogen;

    m and n are, independently, 0 to 2, provided that m+n=2;

    p and q are, independently, 0 to 3, provided that p+q=3;

    z is 0 to 10;

    R7 is selected from the group consisting of H, C1-C6 alkyl, C(O)O—

    C1-C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3-C6 cycloalkyl, and substituted C3-C6 cycloalkyl.

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