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Last Updated: March 28, 2024

Claims for Patent: 9,622,992


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Summary for Patent: 9,622,992
Title:Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs)
Abstract: 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.
Inventor(s): Dalton; James T. (Lakeland, TN), Steiner; Mitchell S. (Germantown, TN), Narayanan; Ramesh (Cordova, TN), Ahn; Sunjoo (Daejeon, KR)
Assignee: GTX, INC. (Memphis, TN)
Application Number:14/293,632
Patent Claims:1. A method of treating, reducing, suppressing the severity of or inhibiting AR-positive breast cancer in a subject with AR-positive breast cancer, comprising administering to said subject a selective androgen receptor modulator (SARM) compound represented by a structure of formula I: ##STR00055## X is O; G is O; T is OH, OR, --NHCOCH.sub.3, or NHCOR; R is alkyl, dihaloalkyl, trihaloalkyl, CH.sub.2F, CHF.sub.2, CF.sub.3, CF.sub.2CF.sub.3, aryl, alkenyl or OH; R.sub.1 is CH.sub.3, CH.sub.2F, CHF.sub.2, CF.sub.3, CH.sub.2CH.sub.3, or CF.sub.2CF.sub.3; R.sub.2 is H, F, Cl, Br, I, CH.sub.3, CF.sub.3, OH, CN, NO.sub.2, NHCOCH.sub.3, NHCOCF.sub.3, NHCOR, alkyl, arylalkyl, OR, NH.sub.2, NHR, N(R).sub.2, or SR; R.sub.3 is H, F, Cl, Br, I, CN, NO.sub.2, COR, COOH, CONHR, CF.sub.3, or Sn(R).sub.3; Z is NO.sub.2, CN, COR, COOH, or CONHR; Y is CF.sub.3, F, Br, Cl, I, CN, or Sn(R).sub.3; Q is CN, alkyl, halogen, N(R).sub.2, NHCOCH.sub.3, NHCOCF.sub.3, NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH.sub.3, NHCSCF.sub.3, NHCSR, NHSO.sub.2CH.sub.3, NHSO.sub.2R, OR, COR, OCOR, OSO.sub.2R, SO.sub.2R or SR; n is an integer of 1-4; and m is an integer of 1-3, wherein said treating does not include preventing.

2. The method of claim 1, wherein said SARM compound is represented by a structure of formula XIII: ##STR00056## or formula XIV: ##STR00057##

3. The method of claim 1, wherein said SARM compound is represented by a structure of formula II: ##STR00058## wherein X is O; G is O; T is OH, OR, --NHCOCH.sub.3, or NHCOR; Z is NO.sub.2, CN, COR, COOH or CONHR; Y is I, CF.sub.3, Br, Cl, or Sn(R).sub.3; Q is CN, alkyl, halogen, N(R).sub.2, NHCOCH.sub.3, NHCOCF.sub.3, NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH.sub.3, NHCSCF.sub.3, NHCSR, NHSO.sub.2CH.sub.3, NHSO.sub.2R, OR, COR, OCOR, OSO.sub.2R, SO.sub.2R or SR; R is a C.sub.1-C.sub.4 alkyl, aryl, alkenyl, or hydroxyl; and R.sub.1 is CH.sub.3, CF.sub.3, CH.sub.2CH.sub.3, or CF.sub.2CF.sub.3.

4. The method of claim 3, wherein said SARM compound is represented by a structure of formula: ##STR00059##

5. The method of claim 1, wherein said breast cancer is a breast cancer that has failed selective estrogen receptor modulator (tamoxifen, toremifene), aromatase inhibitor, trastuzumab, ado-trastuzumab emtansine, pertuzumab, lapatinib, exemestane, bevacizumab, and/or fulvestrant treatments.

6. A method of treating, reducing, suppressing the severity of or inhibiting metastatic or advanced AR-positive breast cancer in a subject with metastatic AR-positive breast cancer or advanced AR-positive breast cancer, comprising administering to said subject a selective androgen receptor modulator (SARM) compound represented by a structure of formula I: ##STR00060## X is O; G is O; T is OH, OR, --NHCOCH.sub.3, or NHCOR; R is alkyl, dihaloalkyl, trihaloalkyl, CH.sub.2F, CHF.sub.2, CF.sub.3, CF.sub.2CF.sub.3, aryl, alkenyl or OH; R.sub.1 is CH.sub.3, CH.sub.2F, CHF.sub.2, CF.sub.3, CH.sub.2CH.sub.3, or CF.sub.2CF.sub.3; R.sub.2 is H, F, Cl, Br, I, CH.sub.3, CF.sub.3, OH, CN, NO.sub.2, NHCOCH.sub.3, NHCOCF.sub.3, NHCOR, alkyl, arylalkyl, OR, NH.sub.2, NHR, N(R).sub.2, or SR; R.sub.3 is H, F, Cl, Br, I, CN, NO.sub.2, COR, COOH, CONHR, CF.sub.3, or Sn(R).sub.3; Z is NO.sub.2, CN, COR, COOH, or CONHR; Y is CF.sub.3, F, Br, Cl, I, CN, or Sn(R).sub.3; Q is CN, alkyl, halogen, N(R).sub.2, NHCOCH.sub.3, NHCOCF.sub.3, NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH.sub.3, NHCSCF.sub.3, NHCSR, NHSO.sub.2CH.sub.3, NHSO.sub.2R, OR, COR, OCOR, OSO.sub.2R, SO.sub.2R or SR; n is an integer of 1-4; and m is an integer of 1-3, wherein said treating does not include preventing.

7. The method of claim 6, wherein said SARM compound is represented by a structure of formula XIII. ##STR00061## or formula XIV: ##STR00062##

8. The method of claim 6, wherein said SARM compound is represented by a structure of formula II: ##STR00063## wherein X is O; G is O; T is OH, OR, --NHCOCH.sub.3, or NHCOR; Z is NO.sub.2, CN, COR, COOH or CONHR; Y is I, CF.sub.3, Br, Cl, or Sn(R).sub.3; Q is CN, alkyl, halogen, N(R).sub.2, NHCOCH.sub.3, NHCOCF.sub.3, NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH.sub.3, NHCSCF.sub.3, NHCSR, NHSO.sub.2CH.sub.3, NHSO.sub.2R, OR, COR, OCOR, OSO.sub.2R, SO.sub.2R or SR; R is a C.sub.1-C.sub.4 alkyl, aryl, phenyl, alkenyl, or hydroxyl; and R.sub.1 is CH.sub.3, CF.sub.3, CH.sub.2CH.sub.3, or CF.sub.2CF.sub.3.

9. The method of claim 8, wherein said SARM compound is represented by a structure of formula: ##STR00064##

10. The method of claim 6, wherein said metastatic or advanced breast cancer is AR-positive ER-positive metastatic or advanced breast cancer.

11. A method of treating, reducing, suppressing the severity of, or inhibiting refractory AR-positive breast cancer in a subject with refractory AR-positive breast cancer, comprising administering to said subject a selective androgen receptor modulator (SARM) compound represented by a structure of formula I: ##STR00065## X is O; G is O; T is OH, OR, --NHCOCH.sub.3, or NHCOR; R is alkyl, dihaloalkyl, trihaloalkyl, CH.sub.2F, CHF.sub.2, CF.sub.3, CF.sub.2CF.sub.3, aryl, alkenyl or OH; R.sub.1 is CH.sub.3, CH.sub.2F, CHF.sub.2, CF.sub.3, CH.sub.2CH.sub.3, or CF.sub.2CF.sub.3; R.sub.2 is H, F, Cl, Br, I, CH.sub.3, CF.sub.3, OH, CN, NO.sub.2, NHCOCH.sub.3, NHCOCF.sub.3, NHCOR, alkyl, arylalkyl, OR, NH.sub.2, NHR, N(R).sub.2, or SR; R.sub.3 is H, F, Cl, Br, I, CN, NO.sub.2, COR, COOH, CONHR, CF.sub.3, or Sn(R).sub.3, Z is NO.sub.2, CN, COR, COOH, or CONHR; Y is CF.sub.3, F, Br, Cl, I, CN, or Sn(R).sub.3; Q is CN, alkyl, halogen, N(R).sub.2, NHCOCH.sub.3, NHCOCF.sub.3, NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH.sub.3, NHCSCF.sub.3, NHCSR, NHSO.sub.2CH.sub.3, NHSO.sub.2R, OR, COR, OCOR, OSO.sub.2R, SO.sub.2R or SR; n is an integer of 1-4; and m is an integer of 1-3, wherein said treating does not include preventing.

12. The method of claim 11, wherein said SARM compound is represented by a structure of formula XIII: ##STR00066## or formula XIV: ##STR00067##

13. The method of claim 11, wherein said SARM compound is represented by a structure of formula II: ##STR00068## wherein X is O; G is O; T is OH, OR, --NHCOCH.sub.3, or NHCOR; Z is NO.sub.2, CN, COR, COOH or CONHR; Y is I, CF.sub.3, Br, Cl, or Sn(R).sub.3; Q is CN, alkyl, halogen, N(R).sub.2, NHCOCH.sub.3, NHCOCF.sub.3, NHCOR, NHCONHR, NHCOOR, OCONHR, CONHR, NHCSCH.sub.3, NHCSCF.sub.3, NHCSR, NHSO.sub.2CH.sub.3, NHSO.sub.2R, OR, COR, OCOR, OSO.sub.2R, SO.sub.2R or SR; R is a C.sub.1-C.sub.4 alkyl, aryl, phenyl, alkenyl, or hydroxyl; and R.sub.1 is CH.sub.3, CF.sub.3, CH.sub.2CH.sub.3, or CF.sub.2CF.sub.3.

14. The method of claim 13, wherein said SARM compound is represented by a structure of formula: ##STR00069##

15. The method of claim 11, wherein said refractory AR-positive breast cancer is AR-positive ER-positive refractory breast cancer.

16. The method of claim 1, wherein said AR-positive breast cancer is AR-positive ER-positive breast cancer.

17. The method of claim 1, wherein said AR-positive breast cancer is ER-negative PR-negative and HER2-negative.

18. The method of claim 1, wherein said AR-positive breast cancer is ER-negative PR-negative and HER2-positive.

19. The method of claim 1, wherein said AR-positive breast cancer is ER-negative PR-positive and HER2-negative.

20. The method of claim 1, wherein said AR-positive breast cancer is ER-positive, PR-positive and HER2-positive.

21. The method of claim 1, wherein said AR-positive breast cancer is ER-positive, PR-negative and HER2-positive.

22. The method of claim 1, wherein said AR-positive breast cancer is ER-positive, PR-positive and HER2-negative.

23. The method of claim 6, wherein said AR-positive breast cancer is ER-positive, PR-positive and HER2-negative.

24. The method of claim 11, wherein said AR-positive breast cancer is ER-positive, PR-positive and HER2-negative.

25. The method of claim 1, comprising administering a racemic mixture of said SARM compound, or an isomer, a metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or crystal of said selective androgen receptor modulator, or any combination thereof.

26. The method of claim 25, wherein said administering comprises intravenously, intraarterially, or intramuscularly injecting to said subject said pharmaceutical product in liquid form; subcutaneously implanting in said subject a pellet containing said pharmaceutical product; orally administering to said subject said pharmaceutical product in a liquid or solid form; or topically applying to said subject said pharmaceutical product.

27. The method of claim 26, wherein said pharmaceutical product is a pellet, a tablet, a capsule, a solution, a suspension, an emulsion, an elixir, a gel, a cream, a suppository or a parenteral formulation.

28. The method of claim 6, comprising administering a racemic mixture of said SARM compound, or an isomer, a metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or crystal of said selective androgen receptor modulator, or any combination thereof.

29. The method of claim 11, comprising administering a racemic mixture of said SARM compound, or an isomer, a metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or crystal of said selective androgen receptor modulator, or any combination thereof.

Details for Patent 9,622,992

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 09/25/1998 ⤷  Try a Trial 2032-07-13
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 02/10/2017 ⤷  Try a Trial 2032-07-13
Genentech, Inc. AVASTIN bevacizumab Injection 125085 02/26/2004 ⤷  Try a Trial 2032-07-13
Genentech, Inc. PERJETA pertuzumab Injection 125409 06/08/2012 ⤷  Try a Trial 2032-07-13
Genentech, Inc. KADCYLA ado-trastuzumab emtansine For Injection 125427 02/22/2013 ⤷  Try a Trial 2032-07-13
Genentech, Inc. HERCEPTIN HYLECTA trastuzumab and hyaluronidase-oysk Injection 761106 02/28/2019 ⤷  Try a Trial 2032-07-13
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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