IP Library Granted Patent US 9,499,549
Granted Patent B2
US 9,499,549 · App. 14/434,021 · Granted Nov 22, 2016

Pyrrolo[3,2-]pyrimidine derivatives for the treatment of viral infections and other diseases

Inventors: David Craig McGowan (Brussels, BE); Stefaan Julien Last (Lint, BE); Serge Maria Aloysius Pieters (Hulst, NL); Werner Embrechts (Beerse, BE); Tim Hugo Maria Jonckers (Heist-op-den-Berg, BE); Pierre Jean-Marie Bernard Raboisson (Rosieres, BE)
Assignee: JANSSEN SCIENCES IRELAND UC
C07D487/04A61K31/519C07D519/00
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,499,549
App. No.
14/434,021
Granted
Nov 22, 2016
Kind
B2
Abstract

This invention concerns pyrrolo[3,2-d]pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treatment and/or therapy of diseases.

Claims (14)

1. A compound of formula (I)

a pharmaceutically acceptable salt or solvate thereof wherein;

R 1 is H, fluorine or methyl;

R 2 is H, halogen or C 1-3 alkyl;

R 3 is C 1-6 alkyl optionally substituted by aryl wherein said aryl is optionally-substituted by one or more substituents independently selected from the group consisting of aryloxy, halogen, aryl, alkylamino, dialkylamino, C 1-6 alkyl, —CO 2 H, —C(O)OC 1-6 alkyl, —CONH 2 , —CN, and C 1-6 alkoxy; or

R 3 is C 1-6 alkyl optionally substituted by C 1-6 alkene, C 3-7 cycloalkyl or C 3-7 heterocycloalkyl; or

R 3 is C 1-6 alkyl optionally substituted by C 1-6 alkoxy wherein said C 1-6 alkoxy is optionally substituted by aryl; and

R 4 is C 1-8 alkyl optionally substituted by one or more substituents independently selected from the group consisting of hydroxyl, C 1-6 alkoxy, C 1-6 alkyl, C 3-7 cycloalkyl, C 2-6 alkenyl, aryl, heteroaryl, and C 3-7 cycloalkyl wherein said heteroaryl and said C 3-7 cycloalkyl are optionally substituted by C 1-6 alkyl;

with the proviso that 2-amino, 4-(N-butylamino)-5-(alphamethylbenzyl)pyrrolo[3,2-d] pyrimidine is excluded.

2. A compound as claimed in claim 1 , wherein R 3 is methyl optionally substituted by aryl.

3. A compound as claimed in claim 1 , wherein each of R 3 and R 4 is independently C 1-3 alkyl substituted by aryl.

4. A compound as claimed in claim 1 , wherein R 1 is fluorine and R 2 is hydrogen.

5. A pharmaceutical composition comprising a compound as claimed in claim 1 together with one or more pharmaceutically acceptable excipients, diluents or carriers.

6. A compound as claimed in claim 1 , wherein R 3 is aryl-substituted C 1-3 alkyl and the aryl in said aryl-substituted C 1-3 alkyl is optionally substituted by one or more substituents independently selected from the group consisting of aryloxy, halogen, aryl, alkylamino, dialkylamino, C 1-6 alkyl, —CO 2 H, C(O)OC 1-6 alkyl, —CONH 2 , —CN, and C 1-6 alkoxy; and R 4 is aryl-substituted C 1-3 alkyl.

Assignments (9)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 29, 2016
From: JANSSEN R&D IRELAND
To: JANSSEN SCIENCES IRELAND UC
Reel/Frame 038426/0248 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 5, 2015
From: MC GOWAN, DAVID CRAIG
To: JANSSEN INFECTIOUS DISEASES BVBA
Reel/Frame 035797/0034 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 5, 2015
From: LAST, STEFAAN JULIEN
To: JANSSEN INFECTIOUS DISEASES BVBA
Reel/Frame 035797/0068 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 5, 2015
From: PIETERS, SERGE MARIA ALOYSIUS
To: JANSSEN PHARMACEUTICA NV
Reel/Frame 035797/0075 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 5, 2015
From: EMBRECHTS, WERNER
To: JANSSEN PHARMACEUTICA NV
Reel/Frame 035797/0081 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 5, 2015
From: JONCKERS, TIM HUGO MARIA
To: JANSSEN INFECTIOUS DISEASES BVBA
Reel/Frame 035797/0121 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 5, 2015
From: RABOISSON, PIERRE JEAN-MARIE BERNARD
To: JANSSEN INFECTIOUS DISEASES BVBA
Reel/Frame 035797/0128 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 5, 2015
From: JANSSEN INFECTIOUS DISEASES BVBA
To: JANSSEN R&D IRELAND
Reel/Frame 035797/0130 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 5, 2015
From: JANSSEN PHARMACEUTICA NV
To: JANSSEN R&D IRELAND
Reel/Frame 035797/0159 →
Priority Claims (1)
EP 12187994 · Oct 10, 2012 · regional
Continuity (1)
Related Publication 20150239892A1 · Aug 27, 2015