IP Library Granted Patent US 10,420,788
Granted Patent B2
US 10,420,788 · App. 15/221,961 · Granted Sep 24, 2019

Substituted nucleosides, nucleotides and analogs thereof

Inventors: Guangyi Wang (Carlsbad, CA); David Bernard Smith (San Mateo, CA); Leonid Beigelman (San Mateo, CA); Jerome Deval (Pacifica, CA); Marija Prhavc (Encinitas, CA)
Assignee: ALIOS BIOPHARMA, INC.
A61K31/708A61K31/706A61K31/7068A61K31/7072A61K31/7076C07H19/06C07H19/10C07H19/12C07H19/16C07H19/20C07H19/207
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Quick Facts
Patent No.
US 10,420,788
App. No.
15/221,961
Granted
Sep 24, 2019
Kind
B2
Abstract

Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.

Claims (47)

1. A method of treating a metapneumovirus infection comprising administering to a subject infected with the metapneumovirus an effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt thereof, wherein the compound of Formula (I) has the following structure:

wherein:

B 1A is an optionally substituted purine-base or an optionally substituted pyrimidine-base;

R 1A is selected from the group consisting of hydrogen, an optionally substituted acyl and

the dashed line (------) is absent;

R 2A is selected from the group consisting of an unsubstituted C 1-6 alkyl, a halogen substituted C 1-6 alkyl, a hydroxy substituted C 1-6 alkyl, an alkoxy substituted C 1-6 alkyl and a sulfenyl substituted C 1-6 alkyl;

R 3A is selected from the group consisting of OH and —OC(═O)R″ A ;

R 4A is fluoro;

R 5A is hydrogen;

R 6A and R 7A are independently absent or hydrogen; or

R 6A is

and R 7A is absent or hydrogen;

R 12A , R 13A and R 14A are independently absent or hydrogen;

R″ A is an unsubstituted C 1-6 alkyl;

m is 0 or 1; and

Z 1A is O.

2. The method of claim 1 , wherein the metaphenumovirus is human metapneumovirus.

3. The method of claim 1 , wherein R 1A is

4. The method of claim 3 , wherein R 6A and R 7A are both hydrogen or both absent.

5. The method of claim 1 , wherein R 6A is

and R 7A is absent or hydrogen.

6. The method of claim 5 , wherein m is 0; and R 12A and R 13A are independently absent or hydrogen.

7. The method of claim 5 , wherein m is 1; and R 12A , R 13A and R 14A are independently absent or hydrogen.

8. The method of claim 1 , wherein R 1A is H.

9. The method of claim 1 , wherein R 1A is an unsubstituted acyl.

10. The method of claim 9 , wherein the unsubstituted acyl is —C(═O)R 39A , wherein R 39A is an unsubstituted C 1-6 alkyl.

11. The method of claim 1 , wherein B 1A is an optionally substituted purine-base.

12. The method of claim 1 , wherein B 1A is

13. The method of claim 1 , wherein B 1A is

14. The method of claim 1 , wherein B 1A is

15. The method of claim 1 , wherein B 1A is an optionally substituted pyrimidine-base.

16. The method of claim 1 , wherein R 2A is a halogen substituted C 1-6 alkyl.

17. The method of claim 16 , wherein R 3A is OH.

18. The method of claim 16 , wherein R 3A is —OC(═O)R ″A , wherein R ″A is an unsubstituted C 1-6 alkyl.

19. The method of claim 1 , wherein the compound of Formula (I) is

or a pharmaceutically acceptable salt thereof.

20. The method of claim 19 , wherein the compound of Formula (I) is

or a pharmaceutically acceptable salt thereof.

21. The method of claim 19 , wherein the compound of Formula (I) is

or a pharmaceutically acceptable salt thereof.

22. The method of claim 1 , wherein the compound of Formula (I) is

or a pharmaceutically acceptable salt thereof.

23. The method of claim 1 , wherein the compound of Formula (I) is

or a pharmaceutically acceptable salt thereof.

24. The method of claim 1 , wherein the compound of Formula (I), or a pharmaceutically acceptable salt thereof, is administered in a pharmaceutical composition that comprises a pharmaceutically acceptable excipient.

25. The method of claim 24 , wherein the compound of Formula (I) is

or a pharmaceutically acceptable salt thereof.

Assignments (2)
CHANGE OF NAME Recorded Dec 19, 2019
From: ALIOS BIOPHARMA, INC.
To: JANSSEN BIOPHARMA, INC.
Reel/Frame 051381/0440 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 12, 2017
From: WANG, GUANGYI; SMITH, DAVID BERNARD; BEIGELMAN, LEONID; DEVAL, JEROME; PRHAVC, MARIJA
To: ALIOS BIOPHARMA, INC.
Reel/Frame 040957/0963 →
Continuity (4)
Continuation 14386294
Continuation In Part 13721988 · Dec 20, 2012
Provisional Application 61613836 · Mar 21, 2012
Related Publication 20160331770A1 · Nov 17, 2016