IP Library › Granted Patent US 12,643,910
Granted Patent B2
US 12,643,910 · App. 17/788,262 · Granted Jun 2, 2026

Substituted pyrazolo[3,4-b]pyridines as ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) modulators

Inventors: Anthony Pinkerton (La Jolla, CA); Eduard Sergienko (La Jolla, CA); Yohei Kiyotsuka (Tokyo, JP); Katsuji Kagechika (Tokyo, JP); Yasunobu Kurosaki (Tokyo, JP); Yoshikazu Arai (Tokyo, JP); Masatoshi Nagamochi (Tokyo, JP); Koutaro Ishibashi (Tokyo, JP)
Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
C07D495/04A61P19/02A61P19/06C07D471/04C07D473/34C07D487/04C07D498/04
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Quick Facts
Patent No.
US 12,643,910
App. No.
17/788,262
Granted
Jun 2, 2026
Kind
B2
Abstract

Provided herein are small molecule modulators of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions comprising the compounds of Formula (XI), and methods of using the compounds and compositions comprising the compounds

Claims (33)

1 . A compound of Formula (XI):

or a pharmaceutically acceptable salt thereof,

wherein:

R 30 is C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, C 3 -C 6 heterocycloalkyl, phenyl, or monocyclic heteroaryl, wherein the C 1 -C 6 alkyl, phenyl, or monocyclic heteroaryl is optionally substituted with one, two, or three independently selected R 37 substituents;

each R 37 is independently halogen, CN, C 1 -C 4 alkyl, C 1 -C 4 fluoroalkyl, NR 1A R 1A , OR 1B , or SR 1B ;

R 31 is H, halogen, C 1 -C 6 alkyl, C 1 -C 4 fluoroalkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, or phenyl, wherein the phenyl is optionally substituted with one, two, or three independently selected R 38 substituents;

each R 38 is independently halogen, CN, C 1 -C 4 alkyl, C 1 -C 4 fluoroalkyl, NR 1A R 1A , OR 1B , or SR 1B ;

R 32 is H, halogen, CN, C 1 -C 6 alkyl, C 1 -C 4 fluoroalkyl, C 1 -C 6 alkyl-OH, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, NR 1A R 1A , OR 1B , OC 1 -C 4 fluoroalkyl, SR 1B , monocyclic C 2 -C 6 heterocycloalkyl, phenyl, or monocyclic 5- or 6-membered heteroaryl, wherein the C 1 -C 6 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, phenyl, or monocyclic 5- or 6-membered heteroaryl is optionally substituted with one, two, or three independently selected R 39 substituents;

each R 39 is independently halogen, CN, C 1 -C 4 alkyl, C 1 -C 4 fluoroalkyl, NR 1A R 1A , OR 1B , or SR 1B ;

Y a is CH;

R 34 is S(O) 2 NR 1A R 1A ;

w is 0, 1, 2, or 3;

each R 35 is independently halogen, CN, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 2 -C 4 alkynyl, OR 1B , or cycloalkyl;

each R 1A is independently H, C 1 -C 6 alkyl, CH 2 -phenyl, cycloalkyl, or aryl; and

each R 1B is independently H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl.

2 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 32 is H, halogen, CN, C 1 -C 6 alkyl, C 1 -C 4 fluoroalkyl, C 1 -C 6 alkyl-OH, NR 1A R 1A , or OR 1B .

3 . The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein R 32 is CH 3 , CH 2 CH 3 , NH 2 , NHCH 3 , NHCH 2 CH 3 , N(CH 3 ) 2 , or OCH 3 .

4 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 34 is S(O) 2 NH 2 , S(O) 2 NHC 1 -C 3 alkyl, or S(O) 2 N(C 1 -C 3 alkyl)(C 1 -C 3 alkyl).

5 . The compound of claim 4 , or a pharmaceutically acceptable salt thereof, wherein R 34 is S(O) 2 NH 2 .

6 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein w is 0.

7 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein each R 35 is independently halogen, CN, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, or OR 1B .

8 . The compound of claim 7 , or a pharmaceutically acceptable salt thereof, wherein each R 35 is independently F, Cl, Br, CH 3 , or CF 3 .

9 . The compound of claim 1 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

10 . The compound of claim 1 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

11 . A pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

12 . The pharmaceutical composition of claim 11 , wherein the pharmaceutical composition is formulated for administration to a mammal by dermal administration, inhalation, intravenous administration, ophthalmic administration, nasal administration, oral administration, or subcutaneous administration.

13 . The pharmaceutical composition of claim 11 , wherein the pharmaceutical composition is formulated as a capsule, a dispersion, an emulsion, a gel, a liquid, a lotion, an ointment, a pill, a solution, a suspension, or a tablet.

14 . A method for treating arthritis in a mammal, wherein the method comprises administering to the mammal in need thereof a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

15 . The method of claim 14 , wherein the arthritis is false gout or pseudogout.

16 . A compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 4, 2023
From: DAIICHI SANKYO COMPANY, LIMITED
To: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
Reel/Frame 065127/0091 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 4, 2023
From: KIYOTSUKA, YOHEI; KAGECHIKA, KATSUJI; KUROSAKI, YASUNOBU; ARAI, YOSHIKAZU; NAGAMOCHI, MASATOSHI; ISHIBASHI, KOUTARO
To: DAIICHI SANKYO COMPANY, LIMITED
Reel/Frame 065126/0972 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 4, 2023
From: PINKERTON, ANTHONY B.; SERGIENKO, EDUARD
To: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
Reel/Frame 065126/0884 →
Continuity (2)
Provisional Application 62953066 · Dec 23, 2019
Related Publication 20230121698A1 · Apr 20, 2023
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