IP Library Granted Patent US 10,301,294
Granted Patent B2
US 10,301,294 · App. 14/776,477 · Granted May 28, 2019

Compounds for the treatment of tuberculosis

Inventors: Timothy A. Lewis (Marlborough, MA); Sivaraman Dandapani (Malden, MA); Deborah Hung (Cambridge, MA); Benito Munoz (Newtonville, MA); Partha Nag (Somerville, MA); Sarah Grant (Boston, MA); Tomohiko Kawate (Cambridge, MA)
Assignees: THE BROAD INSTITUTE INC.; MASSACHUSETTS GENERAL HOSPITAL; BRIGHAM AND WOMEN'S HOSPITAL
C07D413/12C07D263/46C07D271/10C07D271/113C07D285/125C07D413/04C07D413/14C07D417/04C07D417/12
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Quick Facts
Patent No.
US 10,301,294
App. No.
14/776,477
Granted
May 28, 2019
Kind
B2
Abstract

Disclosed are compounds that can be used for treating tuberculosis.

Claims (21)

1. A method of treating tuberculosis comprising administering to a subject a pharmaceutical composition comprising a compound of Formula I-b, I-c, I-d, or I-e, or a pharmaceutically acceptable salt, ester or prodrug thereof:

wherein

R 3 is null, O, H, optionally substituted C 1 -C 6 linear or branched alkyl, or

R 4 is —C≡CH, —C≡C(CH 2 ) t OH, —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 3 -C 6 carbocycle;

R 5 is

and,

z is 1-6,

wherein

R 6 and R 10 are each independently 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

R 7 is H,

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;

R 8 and R 9 are independently H, OH, ═O, halo, or C 1 -C 6 alkyl;

p and q are independently 1-6; and

t and u are independently 0-6,

wherein

m is 1-6.

2. The method of treating tuberculosis of claim 1 , wherein the tuberculosis is a non-replicating tuberculosis.

3. The method of treating tuberculosis of claim 1 , wherein the tuberculosis is a replicating tuberculosis.

4. The method of treating tuberculosis of claim 1 , wherein the compound is selected from the group consisting of:

5. The method of treating tuberculosis of claim 1 , wherein the compound is:

Assignments (4)
CONFIRMATORY LICENSE Recorded Jan 16, 2019
From: THE GENERAL HOSPITAL CORPORATION
To: NIH - DEITR
Reel/Frame 048025/0608 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 6, 2017
From: LEWIS, TIMOTHY A.; DANDAPANI, SIVARAMAN; HUNG, DEBORAH; MUNOZ, BENITO; NAG, PARTHA PRATIM
To: THE BROAD INSTITUTE INC.
Reel/Frame 042925/0673 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 30, 2015
From: HUNG, DEBORAH; KAWATE, TOMOHIKO
To: MASSACHUSETTS GENERAL HOSPITAL
Reel/Frame 036927/0162 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 30, 2015
From: GRANT, SARAH
To: BRIGHAM AND WOMEN'S HOSPITAL
Reel/Frame 036927/0200 →
Continuity (2)
Provisional Application 61779051 · Mar 13, 2013
Related Publication 20160031870A1 · Feb 4, 2016