Selective androgen receptor modulators and methods of use thereof
AssigneeUniversity of Tennessee Research Foundation
InventorsJames T. Dalton, Duane D. Miller, Craig A. Marhefka, Wenqing Gao
Life of this patent
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Abstract
This invention provides a class of androgen receptor targeting agents (ARTA). The compounds are selective androgen receptor modulators (SARM) useful for, inter-alia, suppressing spermatogenesis, treating a subject having a hormone related condition, treating a subject suffering from prostate cancer, delaying the progression of prostate cancer, preventing the recurrence of prostate cancer, and treating the recurrence of prostate cancer.
Claims7
A method of binding an androgen receptor antagonist compound to an androgen receptor, comprising the step of contacting an androgen receptor compound of formula I:
- wherein
- X is a NH, or NR;
- Z is NO2, CN, COOH, COR, or CONHR;
- Y is CF3, F, I, Br, Cl, CN or Sn(R)3;
- R is alkyl, haloalkyl, aryl, phenyl, halogen, alkenyl or OH;
- and
- Q is alkyl, halogen, N(R)2, NHCOCH3, NHCOCF3, NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH3, NHCSCF3, NHCSR, NHSO2CH3, NHSO2R, OR, COR, OCOR, OSO2R, SO2R or SR;
- and/or its isomer, pharmaceutically acceptable salt, or any combination thereof, in an amount effective to bind the androgen receptor compound to the androgen receptor.
A method of suppressing spermatogenesis in a subject comprising contacting an androgen receptor of the subject with an androgen receptor compound of formula I:
- wherein
- X is a NH, or NR;
- Z is NO2, CN, COOH, COR, or CONHR;
- Y is CF3, F, I, Br, Cl, CN or Sn(R)3;
- R is alkyl, haloalkyl, aryl, phenyl, halogen, alkenyl or OH;
- and
- Q is alkyl, halogen, N(R)2, NHCOCH3, NHCOCF3, NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH3, NHCSCF3, NHCSR, NHSO2CH3, NHSO2R, OR, COR, OCOR, OSO2R, SO2R or SR;
- and/or its isomer, pharmaceutically acceptable salt, or any combination thereof, in an amount effective to suppress sperm production.
A method of hormone therapy comprising the step of contacting an androgen receptor of a subject with an androgen receptor compound of formula I:
- wherein
- X is a NH or NR;
- Z is NO2, CN, COOH, COR, or CONHR;
- Y is CF3, F, I, Br, Cl, CN or Sn(R)3;
- R is alkyl, haloalkyl, aryl, phenyl, halogen, alkenyl or OH;
- and
- Q is alkyl, halogen, N(R)2, NHCOCH3, NHCOCF3, NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH3, NHCSCF3, NHCSR, NHSO2CH3, NHSO2R, OR, COR, OCOR, OSO2R, SO2R or SR;
- and/or its isomer, pharmaceutically acceptable salt, or any combination thereof, in an amount effective to effect a change in an androgen-dependent condition.
A method of treating a subject having a hormone related condition, comprising the step of administering to said subject an androgen receptor compound of formula I:
- wherein
- X is a NH, or NR;
- Z is NO2, CN, COOH, COR, or CONHR;
- Y is CF3, F, I, Br, Cl, CN or Sn(R)3;
- R is alkyl, haloalkyl, aryl, phenyl, halogen, alkenyl or OH;
- and
- Q is alkyl, halogen, N(R)2, NHCOCH3, NHCOCF3, NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH3, NHCSCF3, NHCSR, NHSO2CH3, NHSO2R, OR, COR, OCOR, OSO2R, SO2R or SR;
- and/or its isomer, pharmaceutically acceptable salt, or any combination thereof, in an amount effective to effect a change in an androgen-dependent condition.
A method of treating a subject suffering from prostate cancer, comprising the step of administering to said subject an androgen receptor compound of formula I:
- wherein
- X is a NH, or NR;
- Z is NO2, CN, COOH, COR, or CONHR;
- Y is CF3, F, I, Br, Cl, CN or Sn(R)3;
- R is alkyl, haloalkyl, aryl, phenyl, halogen, alkenyl or OH;
- and
- Q is alkyl, halogen, N(R)2, NHCOCH3, NHCOCF3, NUCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH3, NHCSCF3, NHCSR, NHSO2CH3, NHSO2R, OR, COR, OCOR, OSO2R, SO2R or SR;
- and/or its isomer, pharmaceutically acceptable salt, or any combination thereof, in an amount effective to treat prostate cancer in said subject.
A method of delaying the progression of prostate cancer in a subject suffering from prostate cancer, comprising the step of administering to said subject an androgen receptor compound of formula I:
- wherein
- X is a NH, or NR;
- Z is NO2, CN, COOH, COR, or CONHR;
- Y is CF3, F, I, Br, Cl, CN or Sn(R)3;
- R is alkyl, haloalkyl, aryl, phenyl, halogen, alkenyl or OH;
- and
- Q is alkyl, halogen, N(R)2, NHCOCH3, NHCOCF3, NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH3, NHCSCF3, NHCSR, NHSO2CH3, NHSO2R, OR, COR, OCOR, OSO2R, SO2R or SR;
- and/or its isomer, pharmaceutically acceptable salt, or any combination thereof, in an amount effective to delay the progression of prostate cancer in said subject.
A method of treating the recurrence of prostate cancer in a subject suffering from prostate cancer, comprising the step of administering to said subject an androgen receptor compound of formula I:
- wherein
- X is a NH, or NR;
- Z is NO2, CN, COOH, COR, or CONHR;
- Y is CF3, F, I, Br, Cl, CN or Sn(R)3;
- R is alkyl, haloalkyl, aryl, phenyl, halogen, alkenyl or OH;
- and
- Q is alkyl, halogen, N(R)2, NHCOCH3, NHCOCF3, NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH3, NHCSCF3, NHCSR, NHSO2CH3, NHSO2R, OR, COR, OCOR, OSO2R, SO2R or SR;
- and/or its isomer, pharmaceutically acceptable salt, or any combination thereof, in an amount effective to treat the recurrence of prostate cancer in said subject.
Dependencies are inferred from the claim text.