METHOD OF TREATING ANDROGEN RECEPTOR (AR) -POSITIVE BREAST CANCERS WITH SELECTIVE ANDROGEN RECEPTOR MODULATOR (SARMS)

摘要

This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer advanced breast cancer; breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

主权项

1. A method of treating a subject suffering from AR-positive breast cancer, comprising the step of administering to said subject a selective androgen receptor modulator (SARM) compound represented by a structure of formula I: X is a bond, O, CH2, NH, S, Se, PR, NO or NR; G is O or S; T is OH, OR, —NHCOCH3, or NHCOR; R is alkyl, haloalkyl, dihaloalkyl, trihaloalkyl, CH2F, CHF2, CF3, CF2CF3, aryl, phenyl, halogen, alkenyl or OH; R1 is CH3, CH2F, CHF2, CF3, CH2CH3, or CF2CF3; R2 is H, F, Cl, Br, I, CH3, CF3, OH, CN, NO2, NHCOCH3, NHCOCF3, NHCOR, alkyl, arylalkyl, OR, NH2, NHR, N(R)2, SR; R3 is H, F, Cl, Br, I, CN, NO2, COR, COOH, CONHR, CF3, Sn(R)3, or R3 together with the benzene ring to which it is attached forms a fused ring system represented by the structure: Z is NO2, CN, COR, COOH, or CONHR; Y is CF3, F, Br, Cl, I, CN, or Sn(R)3; Q is CN, alkyl, halogen, N(R)2, NHCOCH3, NHCOCF3, NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH3, NHCSCF3, NHCSR, NHSO2CH3, NHSO2R, OR, COR, OCOR, OSO2R, SO2R or SR; or Q together with the benzene ring to which it is attached is a fused ring system represented by structure A, B or C: n is an integer of 1-4; and m is an integer of 1-3.