IP Library › Granted Patent US 9,962,388
Granted Patent B2
US 9,962,388 · App. 15/503,977 · Granted May 8, 2018

Pyrrolopyrimidine compounds used as TLR7 agonist

Inventors: Zhaozhong Ding (Shanghai, CN); Hao Wu (Shanghai, CN); Fei Sun (Shanghai, CN); Lifang Wu (Shanghai, CN); Ling Yang (Lianyungang, CN)
Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
A61K31/519C07D207/02C07D265/28C07D471/04
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Quick Facts
Patent No.
US 9,962,388
App. No.
15/503,977
Granted
May 8, 2018
Kind
B2
Abstract

The present invention relates to a pyrrolopyrimidine compound as TLR7 agonist, and particularly relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation process thereof, a pharmaceutical composition containing such compounds and use thereof for manufacturing a medicament against viral infection.

Claims (23)

1. A compound of formula (I) or a pharmaceutically acceptable salt thereof

wherein

L 1 is —O—;

L 2 is —CH 2 —;

R 1 is selected from the group consisting of hydrogen and C 1-10 alkyl, wherein the above C 1-10 alkyl is optionally substituted by one or more R 4 ;

R 2 is selected from the group consisting of hydrogen, cyano, COOH, and CONH 2 ;

B is selected from the group consisting of aryl and heteroaryl;

L 3 is selected from the group consisting of C 0-6 alkylene and imino, wherein the above C 0-6 alkylene and imino are optionally substituted by one or more R 4 ;

R 3 is selected from the group consisting of hydrogen, amino, C 1-10 alkyl, C 3-10 cyclohydrocarbyl, and 3-10 membered heterocyclohydrocarbyl, wherein the above amino, C 1-10 alkyl, C 3-10 cyclohydrocarbyl, and 3-10 membered heterocyclohydrocarbyl are optionally substituted by one or more R 4 ; or

R 3 and L 3 together with the adjacent atom at the ring B form a saturated or unsaturated 5-8 membered ring, the 5-8 membered ring is optionally substituted by one or more R 4 ;

n is 0, 1, 2, 3, 4 or 5;

R 4 is selected from the group consisting of halogen, —R, —OR, and ═O; and

R is independently selected from the group consisting of H and C 1-8 alkyl.

2. The compound according to claim 1 , characterized in that, R 1 is selected from the group consisting of hydrogen and C 1-6 alkyl, wherein the above C 1-6 alkyl is optionally substituted by one or more R 4 .

3. The compound according to claim 2 , characterized in that, R 1 is selected from the group consisting of C 1-6 alkyl, wherein the above C 1-6 alkyl is optionally substituted by one or more R 4 .

4. The compound according to claim 1 , characterized in that, R 2 is selected from the group consisting of hydrogen, cyano and —CONH 2 .

5. The compound according to claim 1 , characterized in that, B is selected from the group consisting of phenyl and pyridyl.

6. The compound according to claim 1 , characterized in that, L 3 is selected from the group consisting of C 0-6 alkylene, wherein the above C 0-6 alkylene is optionally substituted by one or more R 4 .

7. The compound according to claim 1 , characterized in that, R 3 is selected from the group consisting of hydrogen, amino, C 1-6 alkyl and 3-8 membered heterocyclohydrocarbyl, wherein the above amino, C 1-6 alkyl and 3-8 membered heterocyclohydrocarbyl are optionally substituted by one or more R 4 ; or R 3 and L 3 together with the adjacent atom at the ring B form a saturated or unsaturated 5-8 membered ring, the 5-8 membered ring is optionally substituted by one or more R 4 .

8. The compound according to claim 1 . selected from:

or the pharmaceutically acceptable salt thereof.

9. A pharmaceutical composition, comprising the compound according to claim 1 or the pharmaceutically acceptable salt thereof in a therapeutically effective amount and one or more pharmaceutically acceptable carriers or excipients.

10. A method for treating viral infection, comprising administering the compound according to claim 1 or the pharmaceutically acceptable salt thereof to a subject in need thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 9, 2017
From: DING, ZHAOZHONG; WU, HAO; SUN, FEI; WU, LIFANG; YANG, LING
To: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
Reel/Frame 041531/0034 →
Priority Claims (2)
CN 2014 1 0405136 · Aug 15, 2014 · national
CN 2015 1 0392499 · Jul 6, 2015 · national
Continuity (1)
Related Publication 20170273983A1 · Sep 28, 2017