Compounds and compositions for the treatment of parasitic diseases

Patent metadata

Field	Value
Publication number	US-9926314-B2
Application number	US-201615220149-A
Country	US
Kind code	B2
Filing date	Jul 26, 2016
Priority date	Nov 19, 2012
Publication date	Mar 27, 2018
Grant date	Mar 27, 2018

Abstract

The present invention provides compounds of formula I:

or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.

First claim

We claim:

1. A compound selected from:

or a pharmaceutical acceptable salt thereof.

2. A method for treating, preventing, inhibiting, ameliorating, or eradicating malaria, comprising administering to a subject a therapeutically effective amount of a compound according to claim 1 , wherein the administering may be in combination with a second agent.

3. The method according to claim 2 , wherein the malaria is caused by a Plasmodium parasite, and wherein the Plasmodium parasite is at the blood stages or the hepatic stages.

4. A pharmaceutical composition comprising at least one compound of claim 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent or excipient.

5. A method for treating, preventing, inhibiting, ameliorating, or eradicating malaria, comprising administering to a subject a therapeutically effective amount of a pharmaceutical composition according to claim 4 , wherein the administering may be in combination with a second agent.

6. The method according to claim 5 , wherein the second agent is for the treatment of malaria.

7. The method according to claim 5 , wherein the second agent is an antimalarial drug selected from artemisinin, artemether, artesunate, arteflene, dihydroartemisinin, chlorproguanil, trimethoprim, chloroquine, quinine, mefloquine, amodiaquine, atovaquone, proguanil, lumefantrine, piperaquine, pyronaridine, halofantrine, pyrimethamine-sulfadoxine, quinacrine, pyrimethamine-dapsone, quinidine, amopyroquine, sulphonamides, primaquine, ferroquine, tafenoquine, arterolane, and pyronaridine.

8. A compound of formula:

or a pharmaceutical acceptable salt thereof.

9. A compound of formula:

or a pharmaceutical acceptable salt thereof.

10. A pharmaceutical composition comprising compound of claim 8 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent or excipient.

11. A pharmaceutical composition comprising compound of claim 9 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent or excipient.

12. A method for treating, preventing, inhibiting, ameliorating, or eradicating malaria, comprising administering to a subject a therapeutically effective amount of a compound according to claim 8 , wherein the administering may be in combination with a second agent.

13. A method for treating, preventing, inhibiting, ameliorating, or eradicating malaria, comprising administering to a subject a therapeutically effective amount of a compound according to claim 9 , wherein the administering may be in combination with a second agent.

14. A method for treating, preventing, inhibiting, ameliorating, or eradicating malaria, comprising administering to a subject a therapeutically effective amount of a pharmaceutical composition according to claim 10 , wherein the administering may be in combination with a second agent.

15. A method for treating, preventing, inhibiting, ameliorating, or eradicating malaria, comprising administering to a subject a therapeutically effective amount of a pharmaceutical composition according to claim 11 , wherein the administering may be in combination with a second agent.

16. The method according to claim 14 , wherein the second agent is for the treatment of malaria.

17. The method according to claim 15 , wherein the second agent is for the treatment of malaria.

18. The method according to claim 16 , wherein the second agent is an antimalarial drug selected from artemisinin, artemether, artesunate, arteflene, dihydroartemisinin, chlorproguanil, trimethoprim, chloroquine, quinine, mefloquine, amodiaquine, atovaquone, proguanil, lumefantrine, piperaquine, pyronaridine, halofantrine, pyrimethamine-sulfadoxine, quinacrine, pyrimethamine-dapsone, quinidine, amopyroquine, sulphonamides, primaquine, ferroquine, tafenoquine, arterolane, and pyronaridine.

19. The method according to claim 17 , wherein the second agent is an antimalarial drug selected from artemisinin, artemether, artesunate, arteflene, dihydroartemisinin, chlorproguanil, trimethoprim, chloroquine, quinine, mefloquine, amodiaquine, atovaquone, proguanil, lumefantrine, piperaquine, pyronaridine, halofantrine, pyrimethamine-sulfadoxine, quinacrine, pyrimethamine-dapsone, quinidine, amopyroquine, sulphonamides, primaquine, ferroquine, tafenoquine, arterolane, and pyronaridine.

Assignees

• Novartis Ag

Inventors

• Chatterjee Arnab Kumar
• Nagle Advait Suresh
• Paraselli Prasuna
• Kondreddi Ravinder Reddy
• Leong Seh Yong
• Mishra Pranab Kumar
• Moreau Robert Joseph
• Roland Jason Thomas
• Sim Wei Lin Sandra
• Simon Oliver
• Tan Liying Jocelyn
• Yeung Bryan K S
• Zou Bin
• Bollu Venkatataiah

Classifications

• C07D471/04 Primary

  Ortho-condensed systems · CPC title

• A61K31/506

  not condensed and containing further heterocyclic rings · CPC title

• C07D519/00

  Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00 · CPC title

• A61P33/00

  Antiparasitic agents · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title