IP Library Granted Patent US 11,806,335
Granted Patent B2
US 11,806,335 · App. 17/081,940 · Granted Nov 7, 2023

Heterocyclic carboxylate compounds as glycolate oxidase inhibitors

Inventors: Hongyan Guo (San Mateo, CA); Amy S. Lee (Palo Alto, CA); Hyung-Jung Pyun (Fremont, CA); Devleena M. Shivakumar (Menlo Park, CA); Manoj C. Desai (Martinez, CA); Lianhong Xu (Palo Alto, CA); John E. Knox (Alameda, CA); Zachary E R Newby (San Francisco, CA)
Assignee: Lilac Therapeutics, Inc.
A61K31/4192A61K31/19A61K31/194A61K31/351A61K31/381A61K31/382A61K31/415A61K31/4164A61K31/422A61K31/427A61K31/428A61K31/433A61K31/4439A61K31/454A61K31/4709A61K31/4725A61K31/497A61K31/501A61K31/506A61K31/5377A61K31/675A61K31/7048A61K38/51A61K45/06C07D231/14C07D233/90C07D249/06C07D401/04C07D401/10C07D401/12C07D401/14C07D403/04C07D403/10C07D403/14C07D405/04C07D405/10C07D405/14C07D413/10C07D417/04C07D417/10C07F9/65583C12N15/113C12N2310/14
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Quick Facts
Patent No.
US 11,806,335
App. No.
17/081,940
Granted
Nov 7, 2023
Kind
B2
Abstract

The present disclosure relates generally to modulators of human glycolate oxidase enzyme and methods of use and manufacture thereof.

Claims (33)

1. A compound of formula III:

or a pharmaceutically acceptable salt, tautomer, stereoisomer, mixture of stereoisomers, or deuterated analog thereof, wherein:

R 2 is hydrogen, —(CH 2 CH 2 O) 1-9 CH 2 CH 2 OCH 3 , C 1-6 alkyl optionally substituted with one to three R 4 , cycloalkyl, or heteroaryl optionally substituted with one to three R 5 ;

each R 3 is independently aryl, heteroaryl, or heterocyclyl, wherein each R 3 is optionally substituted with one to three R 6 ;

each R 4 is independently halo, hydroxy, —OC 1-6 alkyl, —NH 2 , —NHC 1-6 alkyl, —N(C 1-6 alkyl) 2 , —OC(O)R a , —OC(O)OR a , —OP(O)(OR b ) 2 , or monocyclic heterocyclyl; wherein each is optionally substituted with one to three R 5 ; provided only one R 4 is heterocyclyl;

each R 5 is independently cyano, halo, C 1-4 alkyl, hydroxy, —OC 1-4 alkyl, C 1-4 haloalkyl, or —OC 1-4 haloalkyl;

each R 6 is independently cyano, halo, —C(O)R 7 , —C(O)OR 7 , —C(O)NR 7 R 8 , —S(O) 2 NR 7 R 8 , —NR 7 C(O)R 8 , —OR 7 , C 1-4 alkyl, —OC 1-4 alkyl, C 1-4 haloalkyl, —OC 1-4 haloalkyl, phenyl, heterocyclyl, or heteroaryl; wherein each is optionally substituted with one to three C 1-4 alkyl, —C(O)OH or C 1-4 haloalkyl;

R 7 and R 8 are each independently hydrogen, C 1-4 alkyl or phenyl, pyridyl, or R 7 and R 8 together with the nitrogen atom to which they are attached form a heterocyclyl;

each R a is independently C 1-6 alkyl optionally substituted with —NH 2 , —NHC 1-6 alkyl, —N(C 1-6 alkyl) 2 , or —OP(O)(OR b ) 2 ;

each R b is independently hydrogen or C 1-4 alkyl.

2. A compound of formula IV:

or a pharmaceutically acceptable salt, tautomer, stereoisomer, mixture of stereoisomers, or deuterated analog thereof, wherein:

R 2 is hydrogen, —(CH 2 CH 2 O) 1-9 CH 2 CH 2 OCH 3 , C 1-6 alkyl optionally substituted with one to three R 4 , cycloalkyl, or heteroaryl optionally substituted with one to three R 5 ;

each R 4 is independently halo, hydroxy, —OC 1-6 alkyl, —NH 2 , —NHC 1-6 alkyl, —N(C 1-6 alkyl) 2 , —OC(O)R a , —OC(O)OR a , —OP(O)(OR b ) 2 , or monocyclic heterocyclyl; wherein each is optionally substituted with one to three R 5 ; provided only one R 4 is heterocyclyl;

each R 5 is independently cyano, halo, C 1-4 alkyl, hydroxy, —OC 1-4 alkyl, C 1-4 haloalkyl, or —OC 1-4 haloalkyl;

each R a is independently C 1-6 alkyl optionally substituted with —NH 2 , —NHC 1-6 alkyl, —N(C 1-6 alkyl) 2 , or —OP(O)(OR b ) 2 ;

each R b is independently hydrogen or C 1-4 alkyl.

3. The compound of claim 2 , wherein:

R 2 is hydrogen, C 1-6 alkyl optionally substituted with one to three R 4 , or cycloalkyl;

each R 4 is independently —OC 1-6 alkyl, —OC(O)R a , —OC(O)OR a , —OP(O)(OR b ) 2 , or monocyclic heterocyclyl;

each R a is independently C 1-6 alkyl optionally substituted with —NH 2 or —OP(O)(OR b ) 2 ; and

R b is hydrogen.

4. A compound selected from:

5. A compound having the structure:

or a pharmaceutically acceptable salt, tautomer, stereoisomer, mixture of stereoisomers, or deuterated analog thereof.

6. A compound having the structure:

or a pharmaceutically acceptable salt, tautomer, stereoisomer, mixture of stereoisomers, or deuterated analog thereof.

7. A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable excipient.

8. A pharmaceutical composition comprising the compound of claim 2 and a pharmaceutically acceptable excipient.

9. A pharmaceutical composition comprising the compound of claim 3 and a pharmaceutically acceptable excipient.

10. A pharmaceutical composition comprising the compound of claim 4 and a pharmaceutically acceptable excipient.

11. A pharmaceutical composition comprising the compound of claim 5 and a pharmaceutically acceptable excipient.

12. A pharmaceutical composition comprising the compound of claim 6 and a pharmaceutically acceptable excipient.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 14, 2023
From: NEWBY, ZACHARY ER
To: LILAC THERAPEUTICS, INC.
Reel/Frame 062971/0184 →
CHANGE OF ADDRESS Recorded Aug 26, 2022
From: LILAC THERAPEUTICS, INC.
To: LILAC THERAPEUTICS, INC.
Reel/Frame 061327/0854 →
CHANGE OF NAME Recorded Jun 24, 2022
From: GYANRX SCIENCES, INC.
To: LILAC THERAPEUTICS, INC.
Reel/Frame 060441/0293 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 17, 2021
From: XU, LIANHONG; KNOX, JOHN E.
To: GYANRX SCIENCES, INC.
Reel/Frame 058416/0511 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 6, 2021
From: GILEAD SCIENCES, INC.,
To: GYANRX SCIENCES, INC.
Reel/Frame 054829/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 28, 2020
From: CODELLI, JULIAN A.; DESAI, MANOJ C.; GUO, HONGYAN; LEE, AMY S.; MITRA, AURPON W.; PYUN, HYUNG-JUNG; SHIVAKUMAR, DEVLEENA M.
To: GILEAD SCIENCES, INC.
Reel/Frame 054202/0258 →
Continuity (3)
Provisional Application 63093094 · Oct 16, 2020
Provisional Application 62929476 · Nov 1, 2019
Related Publication 20210128532A1 · May 6, 2021