US2021024464A1PendingUtilityA1
Binding function 3 (bf3) site compounds as therapeutics and methods for their use
Est. expiryApr 9, 2034(~7.7 yrs left)· nominal 20-yr term from priority
C07D 401/06C07D 403/14A61P 5/28C07D 417/04C07D 209/34C07D 235/18C07D 401/04C07D 235/30C07D 405/14C07D 209/08C07D 413/10C07D 277/82C07D 209/42C07D 417/10C07D 231/56C07D 209/14C07D 417/14C07D 471/04C07C 243/22C07D 209/30C07D 405/12C07D 209/10C07D 403/04C07D 413/04A61P 35/00C07D 401/10
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Claims
Abstract
This invention provides compound having a structure of Formulas: Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provide.
Claims
exact text as granted — not AI-modified1 - 20 . (canceled)
21 . A compound having the structure of Formula I:
wherein,
is a double bond;
A 1 is H;
A 2 is H;
A 3 is H;
A 4 is H;
D 1 is E 37 ;
E 37 is NH;
D 2 is
G 1 is CH or CCH 3 ;
D 3 is
J 2 is C;
J 3 is C═S, C═O, NH, or CH 2 .
J 4 is CH or N;
J 5 is CH 2 , NH, S or O;
J 6 , J 7 , J 8 , J 9 , J 10 , J 11 , J 12 , and J 13 are each independently H, OH, Br, Cl, F, I, or CH 3 ;
J 14 is C;
J 15 is C═S, C═O, NH, or CH 2 ;
J 16 , J 17 , J 18 , J 19 , and J 20 are each independently H, OH, Br, Cl, F, I,
NO 2 , or CH 3 ;
J 21 is C;
J 22 is CH 2 , or NH;
J 23 is CH, or N;
J 24 , J 25 , J 26 , and J 27 are each independently H, OH, Br, C, F, I, or CH 3 ;
J 28 is C;
J 31 is H, OH, Br, F, I, C(O)NH 2 , OCH 3 , or CH 3 ;
J 29 , J 30 , J 32 , and J 33 are each independently H, OCH 3 , OH, Br, C, F, I, C(O)NH 2 , CF 3 , NO 2 , NH 2 , or CH 3 ;
J 34 is C;
J 35 , J 36 , J 37 , J 38 , and J 39 are each independently H, OCH 3 , OH, Br, C, F, I, C(O)NH 2 , CF 3 , NO 2 , NH 2 , or CH 3 ;
J 40 is C;
J 41 is H, OH, Br, C, F, I, NH 2 , or CH 3 , or
J 42 , J 43 , J 44 , J 45 , and J 46 are each independently H, OH, Br, C, F, I, NH 2 , or CH 3 ;
J 47 is C;
J 48 is S, CH 2 , C═O, or NH;
J 49 is CH 2 , C═O, S, O, or NH;
J 55 is C, or N;
J 50 , J 51 , J 52 , J 53 , and J 54 , are each independently H, OH, NH 2 , Br, C, F, I, NO 2 , OCH 3 , CF 3 , CH 3 or is absent when J 50 , J 51 , J 52 , J 53 , or J 54 is N;
J 56 is C;
J 57 is N, or CH;
J 58 , J 59 , J 60 , J 61 , and J 62 , are each independently H, OH, NH 2 , Br, C, F, I, NO 2 , OCH 3 , CF 3 , or CH 3 ; and
J 63 , J 64 , J 65 , J 66 , and J 67 , are each independently H, OH, NH 2 , Br, C, F, I, NO 2 , OCH 3 , CF 3 , or CH 3 .
22 . The compound of claim 21 , wherein D is
23 . The compound of claim 22 , wherein
D 3 is
J 28 is C;
J 31 is H, Br, OCH 3 , or CH 3 ; and
J 29 , J 30 , J 32 , and J 33 are each independently H, OCH 3 , OH, Br, C, F, I, C(O)NH 2 , CF 3 , NO 2 , NH 2 , or CH 3 .
24 . The compound of claim 22 , wherein
D 3 is
J 34 is C; and
J 35 , J 36 , J 37 , J 38 , and J 39 are each independently H, OCH 3 , OH, Br, C, F, C(O)NH 2 , CF 3 , NH 2 , or CH 3 .
25 . The compound of claim 22 , wherein
D 3 is
J 56 is C;
J 57 is CH; and
J 58 , J 59 , J 60 , J 61 , and J 62 , are each independently H, OH, NH 2 , Br, C, F, OCH 3 , CF 3 , or CH 3 .
26 . The compound of claim 22 , wherein
D 3 is
J 40 is C;
J 41 is H or
and
J 42 , J 43 , J 44 , J 45 , and J 46 are each independently H, OH, Br, Cl, F, I, NH 2 , or CH 3 .
27 . A compound selected from the group consisting of
or a pharmaceutically acceptable salt thereof.
28 . A pharmaceutical composition comprising a compound or pharmaceutically acceptable salt thereof according to claim 1 and a pharmaceutically acceptable excipient.
29 . A pharmaceutical composition comprising a compound or pharmaceutically acceptable salt thereof according to claim 27 and a pharmaceutically acceptable excipient.
30 . A method of modulating AR activity, the method comprising (a) administering a compound of claim 1 to a subject in need thereof.
31 . The method of claim 30 , wherein the modulating AR activity is for the treatment of at least one indication selected from the group consisting of: AR-mediated cancer, prostate cancer, breast cancer, ovarian cancer, endometrial cancer, bladder cancer, Taxene resistant triple negative breast cancer, hair loss, acne, hirsutism, ovarian cysts, polycystic ovary disease, precocious puberty, and age-related macular degeneration.
32 . The method of claim 31 , wherein the modulating AR activity is for the treatment of prostate cancer.
33 . The method of claim 31 , wherein the modulating AR activity is for the treatment of Taxene resistant triple negative breast cancer.
34 . The method of claim 31 , wherein the modulating AR activity is for the treatment of ovarian cancer.
35 . The method of claim 31 , wherein the modulating AR activity is for the treatment of endometrial cancer.Join the waitlist — get patent alerts
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