US2020392105A1PendingUtilityA1
Acyl Sulfonamides that are BCL Family Antagonists for Use in Clinical Management of Conditions Caused or Mediated by Senescent Cells and for Treating Cancer
Est. expiryJun 13, 2038(~11.9 yrs left)· nominal 20-yr term from priority
C07D 401/10C07D 403/10A61P 35/00A61P 27/00C07D 401/14A61P 9/10
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Claims
Abstract
The aryl sulfonamide compounds of this invention have powerful and cell-type specific Bcl inhibitory activity. Selected compounds in this class promote apoptosis in senescent cells, and are being developed for treating senescent-related conditions. Selected compounds in this class promote apoptosis in cancer cells, and can be developed as chemotherapeutic agents.
Claims
exact text as granted — not AI-modified1 . A compound according to formula (I):
wherein:
X 1 is —Cl;
X 2 is —COOH;
X 3 is —SO 2 CF 3 ; —SO 2 CH 3 ; or —NO 2
X 5 is —F or —H;
R 1 is —CH(CH 3 ) 2 ;
R 2 is —CH 3 ;
R 3 and R 4 are both —H;
n 1 is 2; and
R 6 is selected from —OH,
wherein the hydroxyl group in R 6 is optionally phosphorylated,
with the proviso that if X 3 is —SO 2 CF 3 , then the hydroxyl group in R 6 must be phosphorylated.
2 .- 20 . (canceled)
21 . A method of eliminating senescent cells from a mixed cell population or tissue, comprising contacting the cell population or tissue with a compound according to Formula (I):
wherein:
X 1 is —Cl;
X 2 is —COOH;
X 3 is —SO 2 CF 3 ; —SO 2 CH 3 ; or —NO 2
X 5 is —F or —H;
R 1 is —CH(CH 3 ) 2 ;
R 2 is —CH 3 ;
R 3 and R 4 are both —H;
n 1 is 2; and
R 6 is selected from —OH,
wherein the hydroxyl group in R 6 is optionally phosphorylated.
22 . The method of claim 21 , wherein X 3 is —SO 2 CF 3 .
23 . The method of claim 21 , wherein X 3 is —SO 2 CH 3 .
24 . The method of claim 21 , wherein X 3 is —NO 2
25 . The method of claim 21 , wherein X 5 is —F.
26 . The method of claim 21 , wherein X 5 is —H.
27 . The method of claim 21 , wherein R 6 is —OH.
28 . The method of claim 21 , wherein R 6 is
29 . The method of claim 21 , wherein R 6 is
30 . The method of claim 21 , wherein the hydroxyl group in R 6 is phosphorylated.
31 . The method of claim 21 , wherein if X 3 is —SO 2 CF 3 , then the hydroxyl group in R 6 is phosphorylated.
32 . The method of claim 21 , wherein the hydroxyl group in R 6 is phosphorylated with —PO 3 H 2 .
33 . The method of claim 21 , wherein the compound is selected from the group consisting of:
34 . The method of claim 21 , wherein the compound is selected from the group consisting of:
35 . The method of claim 21 , wherein the compound is:
36 . The method of claim 21 , wherein the compound is:
37 . The method of claim 21 , wherein the compound is:Cited by (0)
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