IP Library Granted Patent US 10,980,807
Granted Patent B2
US 10,980,807 · App. 16/073,679 · Granted Apr 20, 2021

Inhibitor of indoleamine-2,3-dioxygenase (IDO)

Inventors: Xing Dai (Short Hills, NJ); Yaolin Wang (Short Hills, NJ)
Assignee: InventisBio LLC
A61K31/505A61K31/196A61K31/351A61K31/382A61K31/41A61K31/415A61K31/4155A61K31/4184C07C275/42C07D233/88C07D239/42C07D257/04C07D261/14C07D309/08C07D309/14C07D335/02C07D413/12
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Quick Facts
Patent No.
US 10,980,807
App. No.
16/073,679
Granted
Apr 20, 2021
Kind
B2
Abstract

The present disclosure provides compounds of Formula (I). The compounds described herein may be useful in treating a disease associated with IDO, for example, cancer or an infectious disease (e.g., viral or bacterial infectious diseases). Also, provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.

Claims (29)

1. A compound of Formula (I):

or a pharmaceutically acceptable salt thereof,

wherein:

W is a bond;

Q is a bond;

Y is —N═;

R 1 is —C(═O)OH, —C(═O)OR 10 , or

R 2 and R 3 are each independently hydrogen, halogen, C 1 -C 6 alkyl, or R 2 and R 3 are joined to form a cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or tetrahydropyranyl ring, each of which is unsubstituted or substituted with fluorine;

R 4 and R 5 are each independently hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 5 -C 8 cycloalkenyl, C 2 -C 10 alkynyl, C 3 -C 8 cycloalkyl, or 3- to 12-membered heterocyclyl, wherein the alkyl, alkenyl, cycloalkenyl, alkynyl, cycloalkyl, or heterocyclyl is unsubstituted or substituted with a substituent selected from hydroxyl, methyl, CF 3 , cyclopropyl, fluorine, C 1-6 alkoxy substituted phenyl, CF 30 -phenyl, C 1-6 alkoxy, and CF 3 O—; or R 4 and R 5 are joined together with the N they are attached to form one of the following:

R 6 is C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl; C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 5 -C 8 cycloalkenyl, aryl, 4 to 7-membered monocyclic heterocyclyl, 7 to 10-membered bicyclic heterocyclyl, 5 to 6-membered monocyclic heteroaryl, or 8- to 10-membered bicyclic heteroaryl, wherein the alkyl, cycloalkyl, alkenyl, alkynyl, cycloalkenyl, aryl, heterocyclyl, or heteroaryl is unsubstituted or substituted with a substituent selected from C 1 -C 6 alkyl, halogen, —CN, OH, C 1 -C 6 alkoxy, and CH 3 SO 2 ; and

R 10 is substituted or unsubstituted C 1 -C 6 alkyl, or substituted or unsubstituted C 2 -C 6 alkenyl.

2. The compound of claim 1 , wherein R 1 is: —C(═O)OH or

3. The compound of claim 1 , wherein R 2 and R 3 are joined to form an unsubstituted cyclopropyl, unsubstituted cyclobutyl,

unsubstituted cyclopentyl, or unsubstituted cyclohexyl ring.

4. The compound of claim 1 , wherein R 4 and R 5 are each independently C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, or 3- to 12-membered heterocyclyl, wherein the alkyl, cycloalkyl, or heterocyclyl is unsubstituted or substituted with a substituent selected from hydroxyl, methyl, CF 3 , cyclopropyl, fluorine, C 1-6 alkoxy substituted phenyl, CF 3 O-phenyl, C 1-6 alkoxy, and CF 3 O—.

5. The compound of claim 4 , wherein R 4 and R 5 are each independently of the formula:

wherein R is C 1 -C 6 alkyl or CF 3 .

6. The compound of claim 1 , wherein R 6 is of the formula:

wherein R 6A is hydrogen, C 1 -C 6 alkyl, halogen, —CN, OR 6a , or CH 3 SO 2 ;

wherein R 6a is hydrogen, or C 1 -C 6 alkyl; and

k is 0, 1, or 2.

7. The compound of claim 1 , wherein R 6 is of the formula:

8. The compound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

9. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

10. The compound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

11. The compound of claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 13, 2021
From: INVENTISBIO INC.
To: INVENTISBIO LLC
Reel/Frame 054905/0491 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 28, 2019
From: DAI, XING; WANG, YAOLIN
To: SHANGHAI SHALETECH TECHNOLOGY, INC.
Reel/Frame 048463/0507 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 28, 2019
From: SHANGHAI SHALETECH TECHNOLOGY, INC.
To: INVENTISBIO INC.
Reel/Frame 048465/0665 →
Continuity (3)
Provisional Application 62362875 · Jul 15, 2016
Provisional Application 62293219 · Feb 9, 2016
Related Publication 20200046697A1 · Feb 13, 2020
Cited By (2)
US 12,453,731 US 12,509,448