US2022135572A1PendingUtilityA1
Compounds and methods for targeting hsp90
Est. expiryApr 22, 2036(~9.7 yrs left)· nominal 20-yr term from priority
C07D 498/06C07D 491/107C07D 487/04C07D 403/14
67
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Claims
Abstract
Described herein are compounds that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. The compounds may allow for selective detection of Hsp90 in a sample.
Claims
exact text as granted — not AI-modified1 . A compound of formula (I):
and stereoisomers and salts thereof;
wherein
X is —CH 2 — or —C(O)—;
R N is H, —CH 2 (C 6 H 4 )—I, or —CH 2 (C 6 H 4 )—Sn(CH 3 ) 3 ;
R is
each X 1 and X 2 , if present, are independently selected from H and SO 3 H;
n is 0 or 1;
m is 0 or 1; and
the dotted lines show an optional fused ring.
2 . The compound according to claim 1 , wherein X is —CH 2 —.
3 . The compound according to claim 1 , wherein X is —C(O)—.
4 . The compound according to any one of claims 1 - 3 , wherein R N is H.
5 . The compound according to any one of claims 1 - 3 , wherein R N is —CH 2 (C 6 H 4 )—I.
6 . The compound according to any one of claims 1 - 5 , wherein n is 0.
7 . The compound according to any one of claims 1 - 5 , wherein n is 1.
8 . The compound according to any one of claims 1 - 7 , wherein m is 0.
9 . The compound according to any one of claims 1 - 7 , wherein m is 1.
10 . The compound according to any one of claims 1 - 5 , wherein R is
11 . The compound according to any one of claims 1 - 5 , wherein R is
12 . The compound according to any one of claims 1 to 11 , wherein each X 1 and X 2 , if present, are H.
13 . The compound of any one of claims 1 to 11 , wherein each X 1 is SO 3 H.
14 . The compound of any one of claims 1 to 11 , wherein each X 2 is SO 3 H.
15 . A compound according to any one of claims 1 - 14 selected from:
16 . A compound according to any one of claims 1 - 14 having the formula:
R
X
Y
Dye
H
H 2
H
12
H
O
H
12
H
H 2
H
13
H
H 2
H
14
H
O
H
14
H
H 2
H
15
H
H 2
H
16
H
H 2
H
17
H
O
H
17
H
H 2
H
18
H
H 2
—CH 2 C 6 H 4 —I
12
H
H 2
—CH 2 C 6 H 4 —I
15
H
H 2
—CH 2 C 6 H 4 —Sn(CH 3 ) 3
12
17 . A method of detecting Hsp90 in a sample, comprising:
a) contacting the sample with a compound according to any one of claims 1 - 16 ; and b) detecting a signal.
18 . The method of claim 17 , wherein the sample is an in vitro sample.
19 . The method of any one of claims 17 - 18 , wherein the sample is a cell culture.
20 . The method of any one of claims 17 - 19 , wherein the sample is a biological sample from a subject.
21 . The method of claim 20 , wherein the biological sample is selected from the group consisting of a tissue sample, bodily fluid, whole blood, plasma, serum, urine, bronchoalveolar lavage fluid, and a cell culture suspension or fraction thereof.
22 . The method of any one of claims 17 - 21 , wherein the Hsp90 is eHsp90.
23 . A method of detecting cancer in a subject, comprising:
a) contacting a biological sample from the subject with a compound according to any one of claims 1 - 16 ; and b) detecting a signal; wherein cancer is detected in the sample when the signal is higher relative to a signal from a reference sample.
24 . The method of claim 23 , wherein the method further comprises obtaining the biological sample from the subject.
25 . The method of any of claims 23 - 24 , wherein the subject is a human.
26 . The method of any of claims 23 - 25 , wherein the biological sample is selected from the group consisting of a tissue sample, bodily fluid, whole blood, plasma, serum, urine, bronchoalveolar lavage fluid, and a cell culture suspension or fraction thereof.
27 . The method of any of claims 23 - 26 , wherein the cancer is selected from the group consisting of breast cancer, prostate cancer, non-small cell lung cancer, colorectal cancer, pancreatic cancer, ovarian cancer and melanoma.
28 . The method of claim 27 , wherein the cancer is selected from the group consisting of breast cancer and prostate cancer.
29 . A method of treating cancer in a subject in need of treatment, comprising administering to the subject a therapeutically effective amount of a compound according to any one of claims 1 - 16 .
30 . The method of claim 29 , wherein the subject has a cancer selected from the group consisting of breast cancer, prostate cancer, non-small cell lung cancer, colorectal cancer, pancreatic cancer, ovarian cancer and melanoma.
31 . The method of claim 29 or 30 , wherein the subject has a cancer selected from the group consisting of breast cancer and prostate cancer.
32 . A pharmaceutical composition comprising a compound according to any one of claims 1 - 16 and a pharmaceutically acceptable carrier.
33 . A kit comprising a compound according to any of claims 1 - 16 .
34 . A compound selected from:
35 . A pharmaceutical composition comprising a compound according to claim 34 and a pharmaceutically acceptable carrier.
36 . A kit comprising a compound of formula (I) according to claim 34 .Join the waitlist — get patent alerts
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