	US 7,579,353 B2
	Pyridinone derivatives against malaria
Jose Maria Fiandor Roman, Madrid (Spain); Jose Maria Bueno Calderon, Madrid (Spain); and Araceli Mallo Rubio, Madrid (Spain)
Assigned to Glaxo Group Limited, Greenford, Middlesex (United Kingdom)
Appl. No. 11/817,508 PCT Filed Mar. 02, 2006, PCT No. PCT/EP2006/002160 § 371(c)(1), (2), (4) Date Jun. 25, 2008, PCT Pub. No. WO2006/094799, PCT Pub. Date Sep. 14, 2006.
Claims priority of application No. 05381011 (EP), filed on Mar. 04, 2005.
Prior Publication US 2008/0287461 A1, Nov. 20, 2008
Int. Cl. C07D 401/04 (2006.01); A61K 31/444 (2006.01)

U.S. Cl. 514—256 [514/333; 544/333; 546/257]

13 Claims

1. A compound represented by the following Formula I:

or a pharmaceutically acceptable salt thereof, wherein:

Het represents a 6-membered monocyclic heteroaromatic ring containing at least one nitrogen atom, wherein Het is substituted through a carbon atom with one group Z, wherein Z represents:

i) a phenyl or methylenedioxyphenyl group, either of which is optionally substituted with one or more R^Xgroups;

ii) a —OC_1-6alkylphenyl group, wherein the phenyl portion is optionally substituted with one or more R^Xgroups;

iii) a C_1-10alkyl, an Oaryl, a —C_1-6alkylaryl, a —C_2-6alkenylaryl or a —C_2-6alkynylaryl group, wherein any aryl portion is optionally substituted with one or more R^Xgroup;

R^Xrepresents halogen, cyano, —NR^AR^B, C_1-6alkyl, C_1-6alkoxy or C_1-6alkylS(O)_m—;

m represents 0-2;

R¹represents halogen, hydrogen, or cyano;

R²resents hydrogen, hydroxy, —C(O)R^Y, —C(O)OH or C_1-6alkyl optionally substituted by halogen, hydroxy, —C(O)OH, —C(O)R^Yor —NR^AR^B;

R^Aand R^Bindependently represent hydrogen or C_1-6alkyl;

R^Yrepresents C_1-6alkoxy or C_1-6alkyl; and

R³and R⁴are independently C_1-6alkyl.