IP Library Granted Patent US 10,144,731
Granted Patent B2
US 10,144,731 · App. 15/105,306 · Granted Dec 4, 2018

Nrf2 regulators

Inventors: Thomas Glanmor Davies (Cambridgeshire, GB); Alison Jo-anne Woolford (Cambridgeshire, GB); Hendrika Maria Gerarda Willems (Cambridgeshire, GB); David Norton (Cambridgeshire, GB); Thomas Daniel Heightman (Cambridgeshire, GB); Jeffrey K. Kerns (King of Prussia, PA)
Assignees: GlaxoSmithKline Intellectual Property Development Limited; Astex Therapeutics, Ltd
C07D417/10C07D249/18C07D281/02C07D291/08C07D401/12C07D403/12C07D405/12C07D417/14C07D419/10C07D419/14C07D471/04C07D513/04C07D515/04
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Quick Facts
Patent No.
US 10,144,731
App. No.
15/105,306
Granted
Dec 4, 2018
Kind
B2
Abstract

The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.

Claims (12)

1. A compound which is 3-(3-(((R)-4-ethyl-1,1-dioxido-3,4-dihydro-2H-pyrido[2,3-b][1,4,5]oxathiazepin-2-yl)methyl)-4-methylphenyl)-3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoic acid or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt thereof according to claim 1 and a pharmaceutically acceptable excipient.

3. A method of activating Nrf2 in a human in need thereof comprising administering to said human a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according to claim 1 .

4. A compound which is (R)-3-(3-(((R)-4-ethyl-1,1-dioxido-3,4-dihydro-2H-pyrido[2,3-b][1,4,5]oxathiazepin-2-yl)methyl)-4-methylphenyl)-3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoic acid or pharmaceutically acceptable salt thereof.

5. A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt thereof according to claim 4 and a pharmaceutically acceptable excipient.

6. A method of activating Nrf2 in a human in need thereof comprising administering to said human a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according to claim 4 .

7. A compound which is (S)-3-(3-(((R)-4-ethyl-1,1-dioxido-3,4-dihydro-2H-pyrido[2,3-b][1,4,5]oxathiazepin-2-yl)methyl)-4-methylphenyl)-3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoic acid or a pharmaceutically acceptable salt thereof.

8. A method of activating Nrf2 in a human in need thereof comprising administering to said human a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according to claim 7 .

9. A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt thereof according to claim 7 and a pharmaceutically acceptable carrier or excipient.

10. A compound which is (S)-3-(3-(((R)-4-ethyl-1, 1-dioxide-3,4-dihyrdro-2H-pyrido [2,3-b][1,4,5]oxathiazepin-2-yl)methyl)-4-methylphenyl) -3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoic acid.

11. A pharmaceutical composition comprising the compound according to claim 10 and a pharmaceutically acceptable excipient.

12. A method of activating Nrf2 in a human in need thererof comprising administering to said human a therapeutically effective amount of the compound according to claim 10 .

Assignments (4)
CORRECTIVE ASSIGNMENT TO CORRECT THE INCORRECT PCT NO. PROVIDED AS IDENTIFIER AND MISSPELLING OF ASSIGNOR WILLIAMS PREVIOUSLY RECORDED ON REEL 039146 FRAME 0780. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Jul 15, 2016
From: DAVIES, THOMAS GLANMOR; HEIGHTMAN, THOMAS DANIEL; WOOLFORD, ALISON JO-ANNE; GRIFFITHS-JONES, CHARLOTTE MARY; NORTON, DAVID; SAXTY, GORDON; WILLEMS, HENDRIKA MARIE GERARDA
To: ASTEX THERAPEUTICS LIMITED
Reel/Frame 039353/0192 →
CORRECTIVE ASSIGNMENT TO CORRECT THE INCORRECT NO. US2014067027 PREVIOUSLY RECORDED AT REEL: 039146 FRAME: 0258. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Jul 15, 2016
From: KERNS, JEFFREY K; BOEHM, JEFFREY CHARLES; LI, TINDY; DAVIS, RODERICK S; YAN, HONGXING
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Reel/Frame 039452/0467 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 13, 2016
From: KERNS, JEFFREY K; BOEHM, JEFFREY CHARLES; LI, TINDY; DAVIS, RODERICK S; YAN, HONGXING
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Reel/Frame 039146/0258 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 13, 2016
From: DAVIES, THOMAS GLANMOR; HEIGHTMAN, THOMAS DANIEL; WOOLFORD, ALISON JO-ANNE; GRIFFITHS-JONES, CHARLOTTE MARY; NORTON, DAVID; SAXTY, GORDON; WILLIAMS, HENDRIKA MARIE GERARDA
To: ASTEX THERAPEUTICS LIMITED
Reel/Frame 039146/0780 →
Continuity (3)
Provisional Application 61980091 · Apr 16, 2014
Provisional Application 61917466 · Dec 18, 2013
Related Publication 20160318917A1 · Nov 3, 2016