Activating pyruvate kinase R

Patent metadata

Field	Value
Publication number	US-10675274-B2
Application number	US-201916576360-A
Country	US
Kind code	B2
Filing date	Sep 19, 2019
Priority date	Sep 19, 2018
Publication date	Jun 9, 2020
Grant date	Jun 9, 2020

Abstract

This disclosure provides compounds and compositions for activating pyruvate kinase R (PKR) and related methods of manufacturing and using these compounds and compositions.

First claim

We claim:

1. A composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof:

2. The composition of claim 1 , wherein the compound of Formula I is Compound 1, or a pharmaceutically acceptable salt thereof:

3. The composition of claim 2 , wherein the composition comprises a mixture of Compound 1 and Compound 2, or a pharmaceutically acceptable salt thereof:

4. The composition of claim 1 , wherein the composition comprises Compound 2, or a pharmaceutically acceptable salt thereof:

5. The composition of claim 1 , comprising the compound: (S)-1-(5-((2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-7-yl)sulfonyl)-3,4,5,6-tetrahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)-3-hydroxy-2-phenylpropan-1-one.

6. A composition comprising Compound 1

7. The composition of claim 6 , wherein Compound 1 is the only PKR Activating Compound in the composition.

8. The composition of claim 6 , further comprising Compound 2:

9. A pharmaceutical composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof:

and a pharmaceutically acceptable carrier.

10. The pharmaceutical composition of claim 9 , wherein the compound of Formula I is Compound 1, or a pharmaceutically acceptable salt thereof:

11. A compound of Formula I, or a pharmaceutically acceptable salt thereof:

12. The compound of claim 11 , wherein the compound of Formula I is Compound 1, or a pharmaceutically acceptable salt thereof:

13. The compound of claim 11 , wherein the compound of Formula I is Compound 1:

Assignees

• Forma Therapeutics Inc

Inventors

• Ericsson Anna
• Green Neal
• Gustafson Gary
• Lancia Jr David R
• Marshall Gary
• Mitchell Lorna
• Richard David
• Wang Zhongguo

Classifications

• A61K31/436 Primary

  the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin · CPC title

• A61K9/2054

  Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose · CPC title

• A61P7/06

  Antianaemics · CPC title

• C07D491/056

  with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring · CPC title

• C07D487/04

  Ortho-condensed systems · CPC title