US2020140425A1PendingUtilityA1
Compounds for the treatment of tuberculosis
Est. expiryMar 13, 2033(~6.6 yrs left)· nominal 20-yr term from priority
Inventors:Timothy A. LewisSivaraman DandapaniDeborah HungBenito MunozPartha P. NagSarah GrantTomohiko Kawate
C07D 417/12C07D 413/04C07D 285/125C07D 413/14C07D 263/46C07D 413/12C07D 417/04C07D 271/10C07D 271/113A61P 31/06
57
PatentIndex Score
0
Cited by
0
References
0
Claims
Abstract
Disclosed are compounds that can be used for treating tuberculosis.
Claims
exact text as granted — not AI-modified1 - 24 . (canceled)
25 . A compound of Formula I or a pharmaceutically acceptable salt thereof:
wherein:
A 1 , is O;
A 2 is N;
R 1 is S, N, O, optionally substituted C 1 -C 6 linear or branched alkyl, or sulfonyl, as valence and stability permit;
R 2 is null or optionally substituted linear or branched C 1 -C 12 alkyl;
R 3 is null, O, H, optionally substituted C 1 -C 6 linear or branched alkyl, or
as valence and stability permit;
R 4 is H, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted heterocycle, optionally substituted C 1 -C 6 alkoxy, or an optionally substituted amide;
R 5 is an optionally substituted heteroaryl, optionally substituted C 4 -C 6 carbocycle, or optionally substituted C 1 -C 6 linear or branched alkyl.
26 . The compound of claim 25 or a pharmaceutically acceptable salt thereof, wherein R 4 is H,
optionally substituted C 1 -C 6 alkoxy, or optionally substituted alkylamino,
wherein
R 7 is H,
halo, cyano, C 1 -C 6 alkoxy, linear or branched alkyl, haloalkyl, optionally substituted aryl; optionally substituted arylalkyl, halogen substituted C 1 -C 6 alkoxy; and
R 8 and R 9 are independently H, OH, halo, or C 1 -C 6 alkyl.
27 . The compound of claim 25 or or a pharmaceutically acceptable salt thereof, wherein R 5 is C 1 -C 6 linear or branched alkyl,
wherein
R 6 is H, halo, optionally substituted aryl, C 1 -C 6 linear or branched alkyl, C 1 -C 6 alkoxy, haloalkyl, halogen substituted C 1 -C 6 alkoxy, cyano, or
28 - 30 . (canceled)
31 . The compound of claim 25 or a pharmaceutically acceptable salt thereof, wherein R 3 is null.
32 . The compound of claim 25 or a pharmaceutically acceptable salt thereof, wherein R 2 is null or C 1 -C 12 alkyl.
33 . The compound of claim 25 or a pharmaceutically acceptable salt thereof, wherein
R 1 is S; and
R 3 is null.
34 . (canceled)
35 . The compound of claim 25 , or a pharmaceutically acceptable salt thereof wherein R 5 is C 1 -C 6 linear or branched alkyl,
wherein
R 6 is H, halo, optionally substituted aryl, C 1 -C 6 linear or branched alkyl, C 1 -C 6 alkoxy, haloalkyl, halogen substituted C 1 -C 6 alkoxy, cyano, or
36 . The compound of claim 35 , or a pharmaceutically acceptable salt thereof wherein R 5 is:
wherein
R 6 is H, halo, C 1 -C 6 linear or branched alkyl, C 1 -C 6 haloalkyl, cyano, C 1 -C 6 alkoxy, halogen substituted C 1 -C 6 alkoxy, OH, —O(CH 2 ) q C(═O)O(CH 2 ) p CH 3 , —O(CH 2 ) q C(═O)N(H)(CH 2 ) p O(CH 2 ) m N 3 , —O(CH 2 ) q C≡CH, or
wherein m, p and q are independently 1-4.
37 . (canceled)
38 . The compound of claim 36 , or a pharmaceutically acceptable salt thereof wherein R 6 is H, halo, methyl, ethyl, or propyl, CF 3 , cyano, OH, —O(CH 2 ) q C(═O)O(CH 2 ) p CH 3 , —O(CH 2 ) q C(═O)N(H)(CH 2 ) p O(CH 2 ) m N 3 , or —O(CH 2 ) q C≡CH.
39 . The compound of claim 36 , or a pharmaceutically acceptable salt thereof wherein R 6 is H, methyl, ethyl, or propyl, CF 3 , halo, C 1 -C 6 alkoxy, OH, —O(CH 2 ) q C(═O)O(CH 2 ) p CH 3 , —O(CH 2 ) q C(═O)N(H)(CH 2 ) p O(CH 2 ) m N 3 , or —O(CH 2 ) q C≡CH.
40 . The compound of claim 36 , or a pharmaceutically acceptable salt thereof wherein R 6 is halo.
41 . The compound of claim 25 , or a pharmaceutically acceptable salt thereof wherein R 1 is S or sulfonyl.
42 . The compound of claim 25 , or a pharmaceutically acceptable salt thereof wherein R 1 is N.
43 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein R 1 is optionally substituted C 1 -C 6 linear or branched alkyl.
44 . The compound of claim 25 , or a pharmaceutically acceptable salt thereof wherein:
R 1 is S; R 2 null or optionally substituted linear or branched C 1 -C 12 alkyl; R 3 is null or O; and R 4 is H, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted heterocycle, optionally substituted C 1 -C 6 alkoxy, or an optionally substituted amide.
45 . The compound of claim 44 , or a pharmaceutically acceptable salt thereof wherein:
R 4 is H, —C≡CH, —C≡C(CH 2 ) t OH, —C(═O)O(CH 2 ) t CH 3 , —O(CH 2 ) u CH 3 , —O(CH 2 ) q C(═O)O(CH 2 ) p CH 3
optionally substituted C 1 -C 6 alkoxy, optionally substituted alkylamino, or C 1 -C 6 carbocycle, wherein
R 7 is H, O,
halo, cyano, —C(═O)N(H)(CH 2 ) p O(CH 2 ) m N 3 , —O(CH 2 ) q C(═O)N(H)(CH 2 ) p O(CH 2 ) m N 3 , —O(CH 2 ) m N 3 , —O(CH 2 ) m C≡CH, C 1 -C 6 alkoxy, optionally substituted C 1 -C 6 linear or branched alkyl, haloalkyl, optionally substituted aryl; optionally substituted arylalkyl, or halogen substituted C 1 -C 6 alkoxy; and
R 8 and R 9 are independently H, OH, ═O, halo, or C 1 -C 6 alkyl.
m, p and q are independently 1-6; and
t and u are independently 0-6.
46 . The compound of claim 25 or a pharmaceutically acceptable salt thereof, wherein the compound has the Formula I-b, I-c, I-d, or I-e:
wherein
R 4 is H, —C≡CH, —C≡C(CH 2 ) t OH, —C(═O)O(CH 2 ) t CH 3 , —O(CH 2 ) u CH 3 , —O(CH 2 ) q C(═O)(O)CH 2 ) p CH 3 ,
optionally substituted C 1 -C 6 alkoxy, optionally substituted alkylamino, or C 1 -C 6 carbocycle,
R 7 is H, O,
halo, cyano, —C(═O)N(H)(CH 2 ) p O(CH 2 ) m N 3 , —O(CH 2 ) q C(═O)N(H)(CH 2 ) p O(CH 2 ) m N 3 , —O(CH 2 ) m N 3 , —O(CH 2 ) m C≡CH, C 1 -C 6 alkoxy, optionally substituted C 1 -C 6 linear or branched alkyl, haloalkyl, optionally substituted aryl; optionally substituted arylalkyl, or halogen substituted C 1 -C 6 alkoxy; and
R 8 and R 9 are independently H, OH, ═O, halo, or C 1 -C 6 alkyl;
R 5 is
R 6 is H, halo, C 1 -C 6 linear or branched alkyl, C 1 -C 6 haloalkyl, cyano, C 1 -C 6 alkoxy, halogen substituted C 1 -C 6 alkoxy, OH, —O(CH 2 ) q C(═O)O(CH 2 ) p CH 3 , —O(CH 2 ) q C(═O)N(H)(CH 2 ) p O(CH 2 ) m N 3 , —O(CH 2 ) q C≡CH, or
wherein m, p, q, and z are independently 1-6;
t and u are independently 0-6.
47 . The compound of claim 25 , or a pharmaceutically acceptable salt thereof, wherein the compound is selected from
48 . The compound of claim 25 , or a pharmaceutically acceptable salt thereof, provided that the compound is not selected from:
49 - 55 . (canceled)Join the waitlist — get patent alerts
Track US2020140425A1 — get alerts on status changes and closely related new filings.
We store only your email — no account needed. See our privacy policy.