US2016031874A1PendingUtilityA1
Substituted aminothiazoles for the treatment of tuberculosis
Est. expiryMar 13, 2033(~6.6 yrs left)· nominal 20-yr term from priority
C07D 417/14C07D 277/50C07D 417/04C07D 417/12
56
PatentIndex Score
0
Cited by
0
References
0
Claims
Abstract
Disclosed are substituted aminothiazoles, which can be used for, among other things, the treatment of tuberculosis, pharmaceutical compositions containing the same, and methods of using the same.
Claims
exact text as granted — not AI-modified1 . A compound of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:
wherein:
A 1 is NR 18 , O, or S, (CH 2 ) q , or —NH(CH 2 ) q ; —N(H)—N═C*—(CH 2 ) m CH 3
R 1 is optionally substituted alkyl, optionally substituted aryl, optionally substituted pyridyl, optionally substituted pyrimidinyl, optionally substituted pyrazinyl, optionally substituted pyridazinyl, or triazinyl; dd-dd
R 2 is , optionally substituted aryl, optionally substituted pyridyl, optionally substituted pyrimidinyl, optionally substituted pyrazinyl, optionally substituted pyridazinyl, or triazinyl;
R 3 is H, OR 4 , NR 5 R 6 , NO 2 , SO 2 NH 2 , halo, optionally substituted alkyl, optionally substituted heteroalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted carbocycle, optionally substituted heterocycle, optionally substituted carboxyl, optionally substituted alkoxycarbonyl, or optionally substituted aryloxycarbonyl;
R 4 , R 5 , and R 6 are each independently H, halo, optionally substituted alkyl, optionally substituted heteroalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted carbocycle, or optionally substituted heterocycle;
R 18 is H, optionally substituted alkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl, optionally substituted carbocycle, or optionally substituted heterocycle;
C* is where R 2 bonds with the group —N(H)—N═C*—(CH 2 ) m CH 3 ;
m is 0-6; and
q is 1-6.
2 . The compound of claim 1 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein A 1 is NR 18 , O or S.
3 - 4 . (canceled)
5 . The compound of claim 1 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein A 1 is (CH 2 ) q , NH(CH 2 ) q or —N(H)—N═C*—(CH 2 ) m CH 3 .
6 - 7 . (canceled)
8 . The compound of claim 1 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R 3 is H, halo, or optionally substituted C 1 -C 6 alkyl.
9 . The compound of claim 1 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R 3 is OR 4 , NR 5 R 6 , NO 2 , SO 2 NH 2 .
10 . (canceled)
11 . The compound of claim 1 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R 1 is:
wherein:
R 7 and R 8 are each independently H, OR 11 , NR 12 R 13 , NO 2 , SO 2 NH 2 , halo, optionally substituted alkyl, optionally substituted heteroalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted carbocycle, or optionally substituted heterocycle, R 11 , R 12 , and R 13 are each independently H, halo, optionally substituted alkyl, optionally substituted heteroalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted carbocycle, or optionally substituted heterocycle.
12 . The compound of claim 1 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein:
R 1 is
and
R 17 is C 1 -C 6 alkyl.
13 . (canceled)
14 . The compound of claim 1 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R 2 is:
wherein:
R 9 and R 10 are each independently H, OR 14 , NR 15 R 16 , NO 2 , SO 2 NH 2 , halo, optionally substituted alkyl, optionally substituted heteroalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted carbocycle, or optionally substituted heterocycle, R 14 , R 15 , and R 16 are each independently H, halo, optionally substituted alkyl, optionally substituted heteroalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted carbocycle, or optionally substituted heterocycle.
15 - 16 . (canceled)
17 . The compound of claim 14 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R 2 is
wherein R 10 is C 1 -C 6 alkyl, —O-R 21 -C(═O)OR 22 , wherein . R 21 is C 1 -C 6 alkyl and R 22 is C 1 -C 6 alkyl or H.
18 . (canceled)
19 . (canceled)
20 . The compound of claim 1 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R 3 is H, halo, —C(═O)OR 19 ,
wherein R 19 is C 1 -C 6 alkyl and R 20 is C 1 - C 6 alkyl.
21 - 22 . (canceled)
23 . The compound of claim 14 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R 9 and R 10 are independently H or OR 14 .
24 - 25 . (canceled)
26 . The compound of claim 14 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R 9 is H and R 10 is C 1 -C 6 alkyl.
27 - 28 . (canceled)
29 . The compound of claim 14 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R 9 and R 10 are independently H or halo.
30 . The compound of claim 14 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R 2 is
wherein R 9 and R 10 are independently H, halo, haloalkyl, OR 14 , NR 15 R 16 , or C 1 -C 6 alkyl.
31 . (canceled)
32 . The compound of claim 30 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R 9 and R 10 are independently:
H or OR 14 ; H or NR 15 R 16 ; H or C 1 -C 6 alkyl; or H or halo.
33 - 36 . (canceled)
37 . The compound of claim 30 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R 15 and R 16 are independently C 1 -C 6 alkyl.
38 - 42 . (canceled)
43 . The compound of claim 1 , or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein the compound is selected from the group consisting of:
44 . (canceled)
45 . A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt, ester or prodrug thereof.
46 . (canceled)
47 . A method of treating tuberculosis comprising administering to a subject a compound of claim 1 , or a pharmaceutically acceptable salt, ester or prodrug thereof.
48 - 49 . (canceled)
50 . The method of claim 47 , wherein the compound is selected from the group consisting of:Join the waitlist — get patent alerts
Track US2016031874A1 — get alerts on status changes and closely related new filings.
We store only your email — no account needed. See our privacy policy.