IP Library Granted Patent US 10,968,184
Granted Patent B2
US 10,968,184 · App. 16/338,256 · Granted Apr 6, 2021

Pyrimidine prodrugs for the treatment of viral infections and further diseases

Inventors: Jérôme Émile Georges Guillemont (Andé, FR); Tim Hugo Maria Jonckers (Heist-op-den-Berg, BE); Pierre Jean-Marie Bernard Raboisson (Wavre, BE); David Craig McGowan (Brussels, BE); Werner Constant Johan Embrechts (Beerse, BE); Bart Henri Theresia Stoops (Wechelderzande, BE); Florence Marie Herschke (Antwerp, BE); Jacques Armand Henri Bollekens (Ixelles, BE); Laurent Jacques Emile Calmus (Braine l'Alleud, BE)
Assignee: Janssen Sciences Ireland Unlimited Company
C07D239/48C07D405/12C07F9/6512
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Quick Facts
Patent No.
US 10,968,184
App. No.
16/338,256
Granted
Apr 6, 2021
Kind
B2
Abstract

This invention relates to pyrimidine prodrug derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy.

Claims (18)

1. A compound of formula (I)

or a pharmaceutically acceptable salt, solvate or polymorph thereof, wherein

R 1A is hydrogen or a substituted or unsubstituted C 1-3 alkyl,

R 1B is selected from, a substituted or unsubstituted C 1-3 alkyl, heterocycle, or a substituted or unsubstituted phosphoramidate, and

R 2 is a C 1-8 alkyl optionally substituted by a hydroxyl group.

2. A compound according to claim 1 wherein R 1A or R 1B are a substituted or unsubstituted phosphoramidate and wherein R 2 is a C 1-6 alkyl substituted by a hydroxyl group.

3. A compound according to claim 1 wherein R 1A or R 1B are methyl and wherein R 2 is a C 6 -alkyl substituted by a hydroxyl group.

4. A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof according to claim 1 together with one or more pharmaceutically acceptable excipients, diluents or carriers.

5. A compound according to claim 1 wherein R 1A and R 1B are a substituted or unsubstituted phosphoramidate and wherein R 2 is a C 1-6 alkyl substituted by a hydroxyl group.

6. A compound according to claim 1 wherein R 1A and R 1B are methyl and wherein R 2 is a C 6 -alkyl substituted by a hydroxyl group.

7. A pharmaceutical composition comprising a compound according to claim 2 together with one or more pharmaceutically acceptable excipients, diluents or carriers.

8. A pharmaceutical composition comprising a compound according to claim 5 together with one or more pharmaceutically acceptable excipients, diluents or carriers.

9. A method for treating a virus infection, comprising administering to a subject in need thereof the pharmaceutical composition according to claim 4 in an effective amount to treat the virus infection.

10. A method for treating according to claim 9 , wherein the virus infection is a hepatitis B infection.

11. A method for treating an immune disorder, comprising administering to a subject in need thereof the pharmaceutical composition according to claim 4 in an effective amount to treat the immune disorder.

12. A method for treating cancer, comprising administering to a subject in need thereof the pharmaceutical composition according to claim 4 in an effective amount to treat the cancer.

13. The compound of claim 1 selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

Assignments (7)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 23, 2021
From: MC GOWAN, DAVID CRAIG; HERSCHKE, FLORENCE MARIE; STOOPS, BART HENRI THERESIA; EMBRECHTS, WERNER CONSTANT J; BOLLEKENS, JACQUES ARMAND HENRI; RABOISSON, PIERRE JEAN-MARIE BERNARD; JONCKERS, TIM HUGO MARIA
To: JANSSEN PHARMACEUTICA NV
Reel/Frame 055376/0771 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 23, 2021
From: GUILLEMONT, JÉRÔME ÉMILE GEORGES
To: JANSSEN-CILAG
Reel/Frame 055376/0952 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 23, 2021
From: CALMUS, LAURENT JACQUES EMILE
To: NOVALIX SAS
Reel/Frame 055377/0152 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 23, 2021
From: JANSSEN PHARMACEUTICA NV
To: JANSSEN SCIENCES IRELAND UC
Reel/Frame 055377/0187 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 23, 2021
From: JANSSEN-CILAG
To: JANSSEN SCIENCES IRELAND UC
Reel/Frame 055377/0271 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 23, 2021
From: NOVALIX SAS
To: JANSSEN SCIENCES IRELAND UC
Reel/Frame 055377/0317 →
CHANGE OF NAME Recorded Feb 23, 2021
From: JANSSEN SCIENCES IRELAND UC
To: JANSSEN SCIENCES IRELAND UNLIMITED COMPANY
Reel/Frame 055377/0354 →
Priority Claims (1)
EP 16191568 · Sep 29, 2016 · regional
Continuity (1)
Related Publication 20200031779A1 · Jan 30, 2020