IP Library Granted Patent US 9,555,030
Granted Patent B2
US 9,555,030 · App. 14/678,879 · Granted Jan 31, 2017

Therapeutic uses of selected pyrazolopyrimidine compounds with anti-Mer tyrosine kinase activity

Inventors: Xiaodong Wang (Chapel Hill, NC); Stephen Frye (Chapel Hill, NC)
Assignee: The University of North Carolina at Chapel Hill
A61K31/506A61K31/505A61K31/519A61K31/5377A61K31/55A61K31/551A61K31/5513A61K45/06C07D401/04C07D401/14C07D487/04C07D487/08
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Quick Facts
Patent No.
US 9,555,030
App. No.
14/678,879
Granted
Jan 31, 2017
Kind
B2
Abstract

Pyrazolopyrimidine compounds, methods of use, and processes for making compounds with anti-Mer tyrosine kinase activity comprising Formula I, II, III, IV, or a pharmaceutically acceptable composition, salt, isotopic analog, or prodrug thereof, are provided. The pyrazolopyrimidine compounds described herein have Mer tyrosine kinase (MerTK) inhibitory activity and are useful as anti-infective agents, immunostimulatory and immunomodulatory agents, anti-cancer agents (including against MerTK −/− tumors and ITD and TKD mutant forms of Acute Myeloid Leukemia (AML)), and as adjunctive agents in combination with chemotherapeutic, radiation or other standard of care for neoplasms.

Claims (11)

1. A method for treating a host with an infectious disease, comprising administering an effective amount of the following compound:

or a pharmaceutically acceptable salt, thereof.

2. The method of claim 1 , wherein the infectious disease is a viral infection.

3. The method of claim 1 , wherein the infectious disease is a bacterial infection.

4. The method of claim 2 , wherein the virus is selected from the group consisting of a Flavivirus, Hepacivirus, Pegivirus, Pestivirus, Filovirus, Togavirus, Coronavirus, Orthomyxovirus, Paramyxovirus, Calicivirus, and Lentivirus.

5. The method of claim 2 , wherein the virus is Chikungunya.

6. The method of claim 2 , wherein the virus is HCV.

7. The method of claim 2 , wherein the virus is HIV.

8. The method of claim 3 , wherein the bacterial disease is selected from the group consisting of Escherichia coli, Staphylococcus aureus, Enterococcus faecalis , and Streptococcus pneumoniae.

9. A method for treating a host with a medical disorder in need of immunostimulatory adjunctive therapy in combination with a direct acting drug for the medical disorder, comprising administering an adjunctively immunostimulatory effective amount of the following compound:

or a pharmaceutically acceptable composition or salt thereof.

Assignments (3)
CONFIRMATORY LICENSE Recorded Feb 23, 2018
From: UNIV OF NORTH CAROLINA CHAPEL HILL
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 045430/0046 →
CORRECTIVE ASSIGNMENT TO CORRECT THE FIRST INVENTOR LAST NAME PREVIOUSLY RECORDED AT REEL: 035620 FRAME: 0360. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Jun 2, 2015
From: WANG, XIAODONG; FRYE, STEPHEN
To: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL
Reel/Frame 035806/0655 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 12, 2015
From: ZHANG, XIAODONG; FRYE, STEPHEN
To: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL
Reel/Frame 035620/0360 →
Continuity (10)
Provisional Application 61978268 · Apr 11, 2014
Provisional Application 61978281 · Apr 11, 2014
Provisional Application 61978290 · Apr 11, 2014
Provisional Application 61978443 · Apr 11, 2014
Provisional Application 61978485 · Apr 11, 2014
Provisional Application 61978513 · Apr 11, 2014
Provisional Application 61978321 · Apr 11, 2014
Provisional Application 61994384 · May 16, 2014
Provisional Application 62088159 · Dec 5, 2014
Related Publication 20150290212A1 · Oct 15, 2015