Methods for treating hepatitis C
AssigneePTC Therapeutics, Inc.
InventorsGary Karp, Peter Hwang, James Takasugi, Hongyu Ren, Richard Wilde, Anthony Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey Campbell
Life of this patent
Estimating the term…
Abstract
The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.
Claims36
A compound of formula I
- wherein:
- X is:
- -a nitro group;
- -a cyano group;
- -a —CORa group, where Ra is:
- -a C1 to C6 alkyl,
- -a C6 to C8 aryl optionally substituted with an alkoxy or a halogen, or
- -a dialkyl-amino;
- -a —COORx group, where Rx is a C1 to C6 alkyl;
- -a formyl group;
- -a C6 to C8 aryl optionally substituted with an alkoxy;
- or
- -a 5 or 6-membered heteroaryl optionally substituted with:
- -a C1 to C6 alkyl,
- -a C6 to C8 aryl optionally substituted with an alkoxy or one or more halogen(s), or
- -a 5 to 6 membered heteroaryl;
- Y is:
- -a haloalkyl;
- -a halogen;
- -a benzofuran;
- -a benzothiophene;
- -a dibenzofuran;
- -a dibenzothiophene;
- -a benzothiazole;
- -a naphthalene;
- -an indole, optionally substituted on the nitrogen with a C1 to C6 alkyl;
- where Rb is a hydrogen or a C1 to C6 alkyl, and n is 0 or 1;
- where Rc is a hydrogen, a —CONHRx, where Rx is as defined above, or an —SO2Rx, where Rx is as defined above;
- or
- where Rd is a C1 to C6 alkyl or a C6 to C8 aryl;
- -a —NHCORe group, where Re is:
- -a C1 to C6 alkyl;
- -a C6 to C8 aryl optionally substituted with:
- -a C1 to C6 alkyl,
- -an alkoxy,
- -a cyano group,
- -a nitro group, or
- -a halogen;
- -a —NHCOORx group, where Rx is as defined above;
- -a —CH2O—Rf group, where Rf is a C6 to C8 aryl;
- -a —NRgRh group, where Rg is hydrogen or a C1 to C6 alkyl and Rh is hydrogen or a C6 to C8 aryl optionally substituted with an alkoxy;
- -a C1 to C6 alkyl;
- -a 5 or 6 membered heteroaryl, optionally substituted with:
- -a C1 to C6 alkyl, optionally substituted with a C6 to C8 aryl,
- -a C6 to C8 aryl, optionally substituted with —COORx, where Rx is as defined above, or
- -an amino group;
- -a 5 or 6 membered heterocycle optionally substituted with:
- -a —COORx group, where Rx is as defined above, or
- -a —NHCOORx group, where Rx is as defined above;
- -a C6 to C8 aryl, optionally substituted with one or more of the following:
- -an alkoxy, optionally substituted with:
- -an alkoxy,
- -a hydroxy,
- -one or more halogen(s),
- -a 5 or 6 membered heterocycle, optionally substituted with:
- -a C1 to C6 alkyl, or
- -a hydroxy,
- -an amino group optionally substituted with one or more C1 to C6 alkyl(s),
- -a —NRiSO2Rx group, where Rx is as defined above and Ri is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —NRjCORk group, where Rk is:
- -a C1 to C6 alkyl,
- -a hydrogen, or
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- and Rj is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —N═N+═N− group, or
- -a —CORl, where Rl is a 5 or 6 membered heterocycle optionally substituted with a hydroxy,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -a C1 to C6 alkyl group, optionally substituted with:
- -a —NHSO2Rx group, where Rx is as defined above, or
- -a —NRxSO2Rx group, where Rx is as defined above,
- -a haloalkoxy,
- -a halogen,
- -a hydroxy,
- -a —COORx group, where Rx is as defined above,
- -a —CORm group, where Rm is:
- -an amino optionally substituted with one or more C1 to C6 alkyl(s), where the one or more C1 to C6 alkyl(s) is/are optionally substituted with:
- -a hydroxy
- -a 5 or 6 membered heterocycle,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -an alkoxy,
- -a 3 to 7 membered heterocycle, optionally substituted with a C1 to C6 alkyl, optionally substituted with a dialkyl-amino,
- -a —NHRn group, where Rn is:
- -a —CH2CONH2, or
- -a C6 to C8 aryl optionally substituted with:
- -an alkyl,
- -one or more halogen(s),
- -a nitro group, or
- -one or more alkoxy(s),
- -a —NRoCORp group, where Rp is:
- -a C1 to C6 alkyl optionally substituted with:
- -a halogen,
- -an alkoxy, or
- -a C6 to C8 aryl,
- -a 5 or 6 membered heterocycle,
- -a C6 to C8 aryl, optionally substituted with a halogen,
- -a 5 or 6 membered heteroaryl optionally substituted with one or more C1 to C6 alkyl(s),
- -a hydrogen,
- and where Ro is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —NRqCONRqRr group, where Rq is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a haloalkoxy, or
- -a —CORx group, where Rx is as defined above,
- and where Rr is:
- -a C6 to C8 aryl optionally substituted with:
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a —ORs group, where Rs is a C6 to C8 aryl, or
- -a —COORx group, where Rx is as defined above,
- -a C1 to C6 alkyl optionally substituted with one or more of the following:
- -a halogen,
- -an alkylene,
- -a C6 to C8 aryl, and/or
- -a —COORx group, where Rx is as defined above,
- -a —COORx group, where Rx is as defined above,
- -a —NRtCOORu group, where Ru is:
- -a C1 to C12 alkyl, optionally substituted with:
- -a C6 to C8 aryl optionally substituted with a C1 to C6 alkyl or an alkoxy,
- -an alkylene,
- -an alkoxy,
- -an alkyne,
- -a halogen, or
- -a 5 or 6 membered heterocycle,
- -a C6 to C8 aryl, optionally substituted with:
- -an alkoxy,
- -a halogen, or
- -a C1 to C6 alkyl, or
- -a 5 or 6 membered heterocycle,
- and Rt is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —NRvSO2Rw group, where Rv is:
- -a hydrogen,
- -a —CORx, where Rx is as defined above, or
- -a C1 to C6 alkyl, optionally substituted with:
- -a halogen,
- -a —CORx group, where Rx is as defined above,
- -a —OCORx group, where Rx is as defined above,
- -a hydroxy, or
- -an alkoxy,
- and where Rw is:
- -a C1 to C6 alkyl optionally substituted with:
- -a halogen,
- -a haloalkyl,
- -a C6 to C8 aryl, or
- -a 5 or 6 membered heterocycle,
- -a C2 to C6 alkylene,
- -an alkyl- or dialkyl-amino optionally substituted with a halogen,
- -a 5 or 6 membered heterocycle, or
- -a 5 or 6 membered heteroaryl optionally substituted with:
- -a C1 to C6 alkyl,
- -a 5 or 6 membered heterocycle, or
- optionally substituted with a C1 to C6 alkyl, where Ry is a C1 to C6 alkyl or hydrogen,
- where Rz is hydrogen or a C1 to C6 alkyl, optionally substituted with a C6 to C8 aryl,
- -a —SRx group, where Rx is as defined above,
- -a —SO2Raa group, where Raa is:
- -a C1 to C6 alkyl,
- -an amino group,
- -an alkyl- or dialkyl-amino group optionally substituted with a hydroxy or a —COORx group, where Rx is as defined above,
- -a 5 or 6 membered heteroaryl,
- -a C6 to C8 aryl, and/or
- -a —NHRbb group, where Rbb is:
- -a —C(═S)NH2 group, or
- -a —PO(ORx)2 group, where Rx is as defined above;
- -a *Rcc group, where Rcc is:
- -a naphthalene,
- -a 5 or 6 membered heteroaryl,
- -a C6 to C8 aryl, optionally substituted with one or more of the following:
- -an alkoxy,
- -a hydroxy,
- -a halogen,
- -a C1 to C6 alkyl, optionally substituted with a cyano group,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -a —NHPORxRx, where Rx is as defined above,
- -a —NReeCONRffRff group, where Ree is a hydrogen or a C1 to C6 alkyl, optionally substituted with a halogen, and Rff is:
- -a hydrogen,
- -a haloalkyl,
- -a haloalkoxy,
- -a C1 to C6 alkyl, or
- -a —CORx, where Rx is as defined above,
- -a —NRggCORhh group, where Rhh is:
- -a hydrogen,
- -a C1 to C6 alkyl optionally substituted with:
- -an alkoxy,
- -a halogen, or
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -an amino optionally substituted with one or more C1 to C6 alkyl(s), where the one or more C1 to C6 alkyl(s) is/are optionally substituted with a halogen,
- -a 5 or 6 membered heterocycle,
- -a 5 or 6 membered heteroaryl,
- and Rgg is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a haloalkoxy, or
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl,
- -5 or 6 membered heterocycle groups,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s), and/or
- -a —NRiiSO2Rx group, where Rx is as defined above, and Rii is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a haloalkoxy,
- -a —CORx group, where Rx is as defined above;
- Z is:
- -a C1 to C6 alkyl optionally substituted with:
- -an alkoxy,
- -one or more halogen(s), or
- -a C6 to C8 aryl;
- -a C2 to C6 alkylene;
- -a C6 to C8 aryl optionally substituted with an alkoxy or one or more C1 to C6 alkyl(s);
- -a —COORx group, where Rx is as defined above;
- or
- R is a hydrogen, a halogen or an alkoxy;
- R1 is:
- -a hydrogen;
- -a hydroxy;
- -a halogen;
- -a haloalkyl;
- -a nitro group;
- -a 5 or 6 membered heteroaryl;
- -a 5 or 6 membered heterocycle;
- -an alkoxy optionally substituted with:
- -one or more halogen(s),
- -a C6 to C8 aryl, or
- -a 5 or 6 membered heterocycle;
- -a C6 to C8 aryl optionally substituted with an alkoxy;
- -a —CORx group, where Rx is as defined above;
- -a C1 to C6 alkyl optionally substituted with a dialkyl-amino or a 5 or 6 membered heterocycle;
- or
- R1 joins together with R2 to form:
- R2 is:
- -a nitro group;
- -a hydrogen;
- -a halogen;
- -a hydroxy group;
- -a C1 to C6 alkyl group, optionally substituted with one or more halogen(s);
- -an amino group;
- -an alkoxy group optionally substituted with:
- -one or more halogen(s),
- -an —OCORx group, where Rx is as defined above,
- -a dialkyl-amino optionally substituted with an alkoxy,
- -a 5 or 6 membered heterocycle group optionally substituted with a C1 to C6 alkyl,
- -a 5 or 6 membered heteroaryl group, or
- -a C6 to C8 aryl group;
- -a —COORx group, where Rx is as defined above;
- -a haloalkyl;
- -an amide group optionally substituted with:
- -a hydroxy group, or
- -a C6 to C8 aryl;
- -a 5 or 6 membered heteroaryl;
- -a —OCORx group, where Rx is as defined above;
- -a —NHCORjj group, where Rjj is:
- -an alkoxy, or
- -an amino optionally substituted with one or more C1 to C6 alkyl(s);
- -a —ORkk group, where Rkk is a 5 to 6 membered heteroaryl;
- -a —NHSO2Rx group, where Rx is as defined above;
- or
- R2 joins together with R1 to form:
- R3 is:
- -a hydrogen;
- or
- —CH2OCORx, and Rx is as defined above;
- provided that when X is phenyl substituted with alkoxy, Y is phenyl, R is hydrogen, R1 is a halogen, R2 is hydrogen, and R3 is hydrogen, and
- provided that when X is phenyl, hydroxyphenyl or pyridyl, Y is alkyl, R is hydrogen, R1 is hydrogen or hydroxy, R2 is hydrogen or hydroxy, and R3 is hydrogen,
- then Z is:
- -a C1 to C6 alkyl substituted with:
- -an alkoxy,
- -one or more halogen(s), or
- -a C6 to C8 aryl;
- -a C2 to C6 alkylene;
- -a C6 to C8 aryl optionally substituted with an alkoxy or one or more C1 to C6 alkyl(s);
- -a —COORx group, where Rx is as defined above;
- or
- or
- or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising:
- (i) a compound of formula I
- wherein:
- X is:
- -a nitro group;
- -a cyano group;
- -a —CORa group, where Ra is:
- -a C1 to C6 alkyl,
- -a C6 to C8 aryl optionally substituted with an alkoxy or a halogen, or
- -a dialkyl-amino;
- -a —COORx group, where Rx is a C1 to C6 alkyl;
- -a formyl group;
- -a C6 to C8 aryl optionally substituted with an alkoxy;
- or
- -a 5 or 6-membered heteroaryl optionally substituted with:
- -a C1 to C6 alkyl,
- -a C6 to C8 aryl optionally substituted with an alkoxy or one or more halogen(s), or
- -a 5 to 6 membered heteroaryl;
- Y is:
- -a haloalkyl;
- -a halogen;
- -an amino optionally substituted with one or more C1 to C6 alkyl(s);
- -a benzofuran;
- -a benzothiophene;
- -a dibenzofuran;
- -a dibenzothiophene;
- -a benzothiazole;
- -a naphthalene;
- -an indole, optionally substituted on the nitrogen with a C1 to C6 alkyl;
- where Rb is a hydrogen or a C1 to C6 alkyl, and n is 0 or 1;
- where Rc is a hydrogen, a —CONHRx, where Rx is as defined above, or an —SO2Rx, where Rx is as defined above;
- or
- where Rd is a C1 to C6 alkyl or a C6 to C8 aryl;
- -a —NHCORe group, where Re is:
- -a C1 to C6 alkyl;
- -a C6 to C8 aryl optionally substituted with:
- -a C1 to C6 alkyl,
- -an alkoxy,
- -a cyano group,
- -a nitro group, or
- -a halogen;
- -a —NHCOORx group, where Rx is as defined above;
- -a —CH2O—Rf group, where Rf is a C6 to C8 aryl;
- -a —NRgRh group, where Rg is a C1 to C6 alkyl or a hydrogen and Rh is a C6 to C8 aryl optionally substituted with an alkoxy;
- -a C1 to C6 alkyl;
- -a 5 or 6 membered heteroaryl, optionally substituted with:
- -a C1 to C6 alkyl, optionally substituted with a C6 to C8 aryl,
- -a C6 to C8 aryl, optionally substituted with —COORx, where Rx is as defined above, or
- -an amino group;
- -a 5 or 6 membered heterocycle optionally substituted with:
- -a —COORx group, where Rx is as defined above, or
- -a —NHCOORx group, where Rx is as defined above;
- -a C6 to C8 aryl, optionally substituted with one or more of the following:
- -an alkoxy, optionally substituted with:
- -an alkoxy,
- -a hydroxy,
- -one or more halogen(s),
- -a 5 or 6 membered heterocycle, optionally substituted with:
- -a C1 to C6 alkyl, or
- -a hydroxy,
- -an amino group optionally substituted with one or more C1 to C6 alkyl(s),
- -a —NRiSO2Rx group, where Rx is as defined above and Ri is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —NRjCORk group, where Rk is:
- -a C1 to C6 alkyl,
- -a hydrogen, or
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- and Rj is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —N═N+═N− group, or
- -a —CORl, where Rl is a 5 or 6 membered heterocycle optionally substituted with a hydroxy,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -a nitro group,
- -a C1 to C6 alkyl group, optionally substituted with:
- -a —NHSO2Rx group, where Rx is as defined above, or
- -a —NRxSO2Rx group, where Rx is as defined above,
- -a haloalkoxy,
- -a halogen,
- -a hydroxy,
- -a —COORx group, where Rx is as defined above,
- -a —CORm group, where Rm is:
- -an amino optionally substituted with one or more C1 to C6 alkyl(s), where the C1 to C6 alkyls are optionally substituted with:
- -a hydroxy
- -a 5 or 6 membered heterocycle,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -an alkoxy,
- -a 3 to 7 membered heterocycle, optionally substituted with a C1 to C6 alkyl, optionally substituted with a dialkyl-amino,
- -a —NHRn group, where Rn is:
- -a —CH2CONH2, or
- -a C6 to C8 aryl optionally substituted with:
- -an alkyl,
- -one or more halogen(s),
- -a nitro group, or
- -one or more alkoxy(s),
- -a —NRoCORp group, where Rp is:
- -a C1 to C6 alkyl optionally substituted with:
- -a halogen,
- -an alkoxy, or
- -a C6 to C8 aryl,
- -a 5 or 6 membered heterocycle,
- -a C6 to C8 aryl, optionally substituted with a halogen,
- -a 5 or 6 membered heteroaryl optionally substituted with one or more C1 to C6 alkyl(s),
- -a hydrogen,
- and where Ro is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —NRqCONRqRr group, where Rq is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a haloalkoxy, or
- -a —CORx group, where Rx is as defined above,
- and where Rr is:
- -a C6 to C8 aryl optionally substituted with:
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a —ORs group, where Rs is a C6 to C8 aryl, or
- -a —COORx group, where Rx is as defined above,
- -a C1 to C6 alkyl optionally substituted with one or more of the following:
- -a halogen,
- -an alkylene,
- -a C6 to C8 aryl, and/or
- -a —COORx group, where Rx is as defined above,
- -a —COORx group, where Rx is as defined above,
- -a —NRtCOORu group, where Ru is:
- -a C1 to C12 alkyl, optionally substituted with:
- -a C6 to C8 aryl optionally substituted with a C1 to C6 alkyl or an alkoxy,
- -an alkylene,
- -an alkoxy,
- -an alkyne,
- -a halogen, or
- -a 5 or 6 membered heterocycle,
- -a C6 to C8 aryl, optionally substituted with:
- -an alkoxy,
- -a halogen, or
- -a C1 to C6 alkyl, or
- -a 5 or 6 membered heterocycle,
- and Rt is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —NRvSO2Rw group, where Rv is:
- -a hydrogen,
- -a —CORx, where Rx is as defined above, or
- -a C1 to C6 alkyl, optionally substituted with:
- -a halogen,
- -a —CORx group, where Rx is as defined above,
- -a —OCORx group, where Rx is as defined above,
- -a hydroxy, or
- -an alkoxy,
- and where Rw is:
- -a C1 to C6 alkyl optionally substituted with:
- -a halogen,
- -a haloalkyl,
- -a C6 to C8 aryl, or
- -a 5 or 6 membered heterocycle,
- -a C2 to C6 alkylene,
- -an alkyl- or dialkyl-amino optionally substituted with a halogen,
- -a 5 or 6 membered heterocycle, or
- -a 5 or 6 membered heteroaryl optionally substituted with:
- -a C1 to C6 alkyl,
- -a 5 or 6 membered heterocycle, or
- optionally substituted with a C1 to C6 alkyl, where Ry is a C1 to C6 alkyl or hydrogen,
- where Rz is hydrogen or a C1 to C6 alkyl, optionally substituted with a C6 to C8 aryl,
- -a —SRx group, where Rx is as defined above,
- -a —SO2Raa group, where Raa is:
- -a C1 to C6 alkyl,
- -an amino group,
- -an alkyl- or dialkyl-amino group optionally substituted with a hydroxy or a —COORx group, where Rx is as defined above,
- -a 5 or 6 membered heteroaryl,
- -a C6 to C8 aryl, and/or
- -a —NHRbb group, where Rbb is:
- -a —C(═S)NH2 group, or
- -a —PO(ORx)2 group, where Rx is as defined above;
- -a *Rcc group, where Rcc is:
- -a naphthalene,
- -a 5 or 6 membered heteroaryl,
- -a C6 to C8 aryl, optionally substituted with one or more of the following:
- -an alkoxy,
- -a hydroxy,
- -a halogen,
- -a C1 to C6 alkyl, optionally substituted with a cyano group,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -a —NHPORxRx, where Rx is as defined above,
- -a —NReeCONRffRff group, where Ree is a hydrogen or a C1 to C6 alkyl, optionally substituted with a halogen, and Rff is:
- -a hydrogen,
- -a haloalkyl,
- -a haloalkoxy,
- -a C1 to C6 alkyl, or
- -a —CORx, where Rx is as defined above,
- -a —NRggCORhh group, where Rhh is:
- -a hydrogen,
- -a C1 to C6 alkyl optionally substituted with:
- -an alkoxy,
- -a halogen, or
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -an amino optionally substituted with one or more C1 to C6 alkyl(s), where the alkyls are optionally substituted with a halogen,
- -a 5 or 6 membered heterocycle,
- -a 5 or 6 membered heteroaryl,
- and Rgg is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a haloalkoxy, or
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl,
- -5 or 6 membered heterocycle groups,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s), and/or
- -a —NRiiSO2Rx group, where Rx is as defined above, and Rii is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a haloalkoxy,
- -a —CORx group, where Rx is as defined above;
- Z is:
- -a C1 to C6 alkyl optionally substituted with:
- -an alkoxy,
- -one or more halogen(s), or
- -a C6 to C8 aryl;
- -a C2 to C6 alkylene;
- -a C6 to C8 aryl optionally substituted with an alkoxy or one or more C1 to C6 alkyl(s);
- -a —COORx group, where Rx is as defined above;
- or
- R is a hydrogen, a halogen or an alkoxy;
- R1 is:
- -a hydrogen;
- -a hydroxy;
- -a halogen;
- -a haloalkyl;
- -a nitro group;
- -a 5 or 6 membered heteroaryl;
- -a 5 or 6 membered heterocycle;
- -an alkoxy optionally substituted with:
- -one or more halogen(s),
- -a C6 to C8 aryl, or
- -a 5 or 6 membered heterocycle;
- -a C6 to C8 aryl optionally substituted with an alkoxy;
- -a —CORx group, where Rx is as defined above;
- -a C1 to C6 alkyl optionally substituted with a dialkyl-amino or a 5 or 6 membered heterocycle;
- or
- R1 joins together with R2 to form:
- R2 is:
- -a nitro group;
- -a hydrogen;
- -a halogen;
- -a hydroxy group;
- -a C1 to C6 alkyl group, optionally substituted with one or more halogen(s);
- -an amino group;
- -an alkoxy group optionally substituted with:
- -one or more halogen(s),
- -an —OCORx group, where Rx is as defined above,
- -a dialkyl-amino optionally substituted with an alkoxy,
- -a 5 or 6 membered heterocycle group optionally substituted with a C1 to C6 alkyl,
- -a 5 or 6 membered heteroaryl group, or
- -a C6 to C8 aryl group;
- -a —COORx group, where Rx is as defined above;
- -a haloalkyl;
- -an amide group optionally substituted with:
- -a hydroxy group, or
- -a C6 to C8 aryl;
- -a 5 or 6 membered heteroaryl;
- -a —OCORx group, where Rx is as defined above;
- -a —NHCORjj group, where Rjj is:
- -an alkoxy, or
- -an amino optionally substituted with one or more C1 to C6 alkyl(s);
- -a —ORkk group, where Rkk is a 5 to 6 membered heteroaryl;
- -a —NHSO2Rx group, where Rx is as defined above;
- or
- R2 joins together with R1 to form:
- R3 is:
- -a hydrogen;
- or
- —CH2OCORx, and Rx is as defined above;
- provided that when X is phenyl, hydroxyphenyl or pyridyl, Y is alkyl, R is hydrogen, R1 is hydrogen or hydroxy, R2 is hydrogen or hydroxy, and R3 is hydrogen,
- then Z is:
- -a C1 to C6 alkyl substituted with:
- -an alkoxy,
- -one or more halogen(s), or
- -a C6 to C8 aryl;
- -a C2 to C6 alkylene;
- -a C6 to C8 aryl optionally substituted with an alkoxy or one or more C1 to C6 alkyl(s);
- -a —COORx group, where Rx is as defined above;
- or
- or
- or one or more pharmaceutically acceptable salt(s) thereof;
- and
- (ii) one or more pharmaceutically acceptable excipient(s).
A method for treating an infection by a virus in a subject in need thereof, wherein the virus contains an internal ribosome entry site (IRES), comprising administering to the subject one or more compound(s) of formula I or a pharmaceutical composition comprising one or more compound(s) of formula I
- wherein:
- X is:
- -a nitro group;
- -a cyano group;
- -a —CORa group, where Ra is:
- -a C1 to C6 alkyl,
- -a C6 to C8 aryl optionally substituted with an alkoxy or a halogen, or
- -a dialkyl-amino;
- -a —COORx group, where Rx is a C1 to C6 alkyl;
- -a formyl group;
- -a C6 to C8 aryl optionally substituted with an alkoxy;
- or
- -a 5 or 6-membered heteroaryl optionally substituted with:
- -a C1 to C6 alkyl,
- -a C6 to C8 aryl optionally substituted with an alkoxy or one or more halogen(s), or
- -a 5 to 6 membered heteroaryl;
- Y is:
- -a haloalkyl;
- -a halogen;
- -an amino optionally substituted with one or more C1 to C6 alkyl(s);
- -a benzofuran;
- -a benzothiophene;
- -a dibenzofuran;
- -a dibenzothiophene;
- -a benzothiazole;
- -a naphthalene;
- -an indole, optionally substituted on the nitrogen with a C1 to C6 alkyl;
- where Rb is a hydrogen or a C1 to C6 alkyl, and n is 0 or 1;
- where Rc is a hydrogen, a —CONHRx, where Rx is as defined above, or an —SO2Rx, where Rx is as defined above;
- or
- where Rd is a C1 to C6 alkyl or a C6 to C8 aryl;
- -a —NHCORe group, where Re is:
- -a C1 to C6 alkyl;
- -a C6 to C8 aryl optionally substituted with:
- -a C1 to C6 alkyl,
- -an alkoxy,
- -a cyano group,
- -a nitro group, or
- -a halogen;
- -a —NHCOORx group, where Rx is as defined above;
- -a —CH2O—Rf group, where Rf is a C6 to C8 aryl;
- -a —NRgRh group, where Rg is a C1 to C6 alkyl or a hydrogen and Rh is a C6 to C8 aryl optionally substituted with an alkoxy;
- -a C1 to C6 alkyl;
- -a 5 or 6 membered heteroaryl, optionally substituted with:
- -a C1 to C6 alkyl, optionally substituted with a C6 to C8 aryl,
- -a C6 to C8 aryl, optionally substituted with —COORx, where Rx is as defined above, or
- -an amino group;
- -a 5 or 6 membered heterocycle optionally substituted with:
- -a —COORx group, where Rx is as defined above, or
- -a —NHCOORx group, where Rx is as defined above;
- -a C6 to C8 aryl, optionally substituted with one or more of the following:
- -an alkoxy, optionally substituted with:
- -an alkoxy,
- -a hydroxy,
- -one or more halogen(s),
- -a 5 or 6 membered heterocycle, optionally substituted with:
- -a C1 to C6 alkyl, or
- -a hydroxy,
- -an amino group optionally substituted with one or more C1 to C6 alkyl(s),
- -a —NRiSO2Rx group, where Rx is as defined above and Ri is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —NRjCORk group, where Rk is:
- -a C1 to C6 alkyl,
- -a hydrogen, or
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- and Rj is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —N═N+═N− group, or
- -a —CORl, where Rl is a 5 or 6 membered heterocycle optionally substituted with a hydroxy,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -a nitro group,
- -a C1 to C6 alkyl group, optionally substituted with:
- -a —NHSO2Rx group, where Rx is as defined above, or
- -a —NRxSO2Rx group, where Rx is as defined above,
- -a haloalkoxy,
- -a halogen,
- -a hydroxy,
- -a —COORx group, where Rx is as defined above,
- -a —CORm group, where Rm is:
- -an amino optionally substituted with one or more C1 to C6 alkyl(s), where the one or more C1 to C6 alkyl(s) is/are optionally substituted with:
- -a hydroxy
- -a 5 or 6 membered heterocycle,
- -an amino optionally substituted with one or more C1 to C6 alkyls, and/or
- -an alkoxy,
- -a 3 to 7 membered heterocycle, optionally substituted with a C1 to C6 alkyl, optionally substituted with a dialkyl-amino,
- -a —NHRn group, where Rn is:
- -a —CH2CONH2, or
- -a C6 to C8 aryl optionally substituted with:
- -an alkyl,
- -one or more halogen(s),
- -a nitro group, or
- -one or more alkoxy(s),
- -a —NRoCORp group, where Rp is:
- -a C1 to C6 alkyl optionally substituted with:
- -a halogen,
- -an alkoxy, or
- -a C6 to C8 aryl,
- -a 5 or 6 membered heterocycle,
- -a C6 to C8 aryl, optionally substituted with a halogen,
- -a 5 or 6 membered heteroaryl optionally substituted with one or more C1 to C6 alkyl(s),
- -a hydrogen,
- and where Ro is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —NRqCONRqRr group, where Rq is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a haloalkoxy, or
- -a —CORx group, where Rx is as defined above,
- and where Rr is:
- -a C6 to C8 aryl optionally substituted with:
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a —ORs group, where Rs is a C6 to C8 aryl, or
- -a —COORx group, where Rx is as defined above,
- -a C1 to C6 alkyl optionally substituted with one or more of the following:
- -a halogen,
- -an alkylene,
- -a C6 to C8 aryl, and/or
- -a —COORx group, where Rx is as defined above,
- -a —COORx group, where Rx is as defined above,
- -a —NRtCOORu group, where Ru is:
- -a C1 to C12 alkyl, optionally substituted with:
- -a C6 to C8 aryl optionally substituted with a C1 to C6 alkyl or an alkoxy,
- -an alkylene,
- -an alkoxy,
- -an alkyne,
- -a halogen, or
- -a 5 or 6 membered heterocycle,
- -a C6 to C8 aryl, optionally substituted with:
- -an alkoxy,
- -a halogen, or
- -a C1 to C6 alkyl, or
- -a 5 or 6 membered heterocycle,
- and Rt is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —NRvSO2Rw group, where Rv is:
- -a hydrogen,
- -a —CORx, where Rx is as defined above, or
- -a C1 to C6 alkyl, optionally substituted with:
- -a halogen,
- -a —CORx group, where Rx is as defined above,
- -a —OCORx group, where Rx is as defined above,
- -a hydroxy, or
- -an alkoxy,
- and where Rw is:
- -a C1 to C6 alkyl optionally substituted with:
- -a halogen,
- -a haloalkyl,
- -a C6 to C8 aryl, or
- -a 5 or 6 membered heterocycle,
- -a C2 to C6 alkylene,
- -an alkyl- or dialkyl-amino optionally substituted with a halogen,
- -a 5 or 6 membered heterocycle, or
- -a 5 or 6 membered heteroaryl optionally substituted with:
- -a C1 to C6 alkyl,
- -a 5 or 6 membered heterocycle, or
- optionally substituted with a C1 to C6 alkyl, where Ry is a C1 to C6 alkyl or hydrogen,
- where Rz is hydrogen or a C1 to C6 alkyl, optionally substituted with a C6 to C8 aryl,
- -a —SRx group, where Rx is as defined above,
- -a —SO2Raa group, where Raa is:
- -a C1 to C6 alkyl,
- -an amino group,
- -an alkyl- or dialkyl-amino group optionally substituted with a hydroxy or a —COORx group, where Rx is as defined above,
- -a 5 or 6 membered heteroaryl,
- -a C6 to C8 aryl, and/or
- -a —NHRbb group, where Rbb is:
- -a —C(═S)NH2 group, or
- -a —PO(ORx)2 group, where Rx is as defined above;
- -a *Rcc group, where Rcc is:
- -a naphthalene,
- -a 5 or 6 membered heteroaryl,
- -a C6 to C8 aryl, optionally substituted with one or more of the following:
- -an alkoxy,
- -a hydroxy,
- -a halogen,
- -a C1 to C6 alkyl, optionally substituted with a cyano group,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -a —NHPORxRx, where Rx is as defined above,
- -a —NReeCONRffRff group, where Ree is a hydrogen or a C1 to C6 alkyl, optionally substituted with a halogen, and Rff is:
- -a hydrogen,
- -a haloalkyl,
- -a haloalkoxy,
- -a C1 to C6 alkyl, or
- -a —CORx, where Rx is as defined above,
- -a —NRggCORhh group, where Rhh is:
- -a hydrogen,
- -a C1 to C6 alkyl optionally substituted with:
- -an alkoxy,
- -a halogen, or
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -an amino optionally substituted with one or more C1 to C6 alkyl(s), where the alkyls are optionally substituted with a halogen,
- -a 5 or 6 membered heterocycle,
- -a 5 or 6 membered heteroaryl,
- and Rgg is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a haloalkoxy, or
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl,
- -5 or 6 membered heterocycle groups,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s), and/or
- -a —NRiiSO2Rx group, where Rx is as defined above, and Rii is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a haloalkoxy,
- -a —CORx group, where Rx is as defined above;
- Z is:
- -a C1 to C6 alkyl optionally substituted with:
- -an alkoxy,
- -one or more halogen(s), or
- -a C6 to C8 aryl;
- -a C2 to C6 alkylene;
- -a C6 to C8 aryl optionally substituted with an alkoxy or one or more C1 to C6 alkyl(s);
- -a —COORx group, where Rx is as defined above;
- or
- R is a hydrogen, a halogen or an alkoxy;
- R1 is:
- -a hydrogen;
- -a hydroxy;
- -a halogen;
- -a haloalkyl;
- -a nitro group;
- -a 5 or 6 membered heteroaryl;
- -a 5 or 6 membered heterocycle;
- -an alkoxy optionally substituted with:
- -one or more halogen(s),
- -a C6 to C8 aryl, or
- -a 5 or 6 membered heterocycle;
- -a C6 to C8 aryl optionally substituted with an alkoxy;
- -a —CORx group, where Rx is as defined above;
- -a C1 to C6 alkyl optionally substituted with a dialkyl-amino or a 5 or 6 membered heterocycle;
- or
- R1 joins together with R2 to form:
- R2 is:
- -a nitro group;
- -a hydrogen;
- -a halogen;
- -a hydroxy group;
- -a C1 to C6 alkyl group, optionally substituted with one or more halogen(s);
- -an amino group;
- -an alkoxy group optionally substituted with:
- -one or more halogen(s),
- -an —OCORx group, where Rx is as defined above,
- -a dialkyl-amino optionally substituted with an alkoxy,
- -a 5 or 6 membered heterocycle group optionally substituted with a C1 to C6 alkyl,
- -a 5 or 6 membered heteroaryl group, or
- -a C6 to C8 aryl group;
- -a —COORx group, where Rx is as defined above;
- -a haloalkyl;
- -an amide group optionally substituted with:
- -a hydroxy group, or
- -a C6 to C8 aryl;
- -a 5 or 6 membered heteroaryl;
- -a —OCORx group, where Rx is as defined above;
- -a —NHCORjj group, where Rjj is:
- -an alkoxy, or
- -an amino optionally substituted with one or more C1 to C6 alkyl(s);
- -a —ORkk group, where Rkk is a 5 to 6 membered heteroaryl;
- -a —NHSO2Rx group, where Rx is as defined above;
- or
- R2 joins together with R1 to form:
- R3 is:
- -a hydrogen;
- or
- —CH2OCORx, and Rx is as defined above;
- or
- one or more pharmaceutically acceptable salt(s) thereof.
A method for treating a Hepatitis C viral (HCV) infection in a subject in need thereof, comprising administering to the subject one or more compound(s) of formula I or a pharmaceutical composition comprising one or more compound(s) of formula I
- wherein:
- X is:
- -a nitro group;
- -a cyano group;
- -a —CORa group, where Ra is:
- -a C1 to C6 alkyl,
- -a C6 to C8 aryl optionally substituted with an alkoxy or a halogen, or
- -a dialkyl-amino;
- -a —COORx group, where Rx is a C1 to C6 alkyl;
- -a formyl group;
- -a C6 to C8 aryl optionally substituted with an alkoxy;
- or
- -a 5 or 6-membered heteroaryl optionally substituted with:
- -a C1 to C6 alkyl,
- -a C6 to C8 aryl optionally substituted with an alkoxy or one or more halogen(s), or
- -a 5 to 6 membered heteroaryl;
- Y is:
- -a haloalkyl;
- -a halogen;
- -an amino optionally substituted with one or more C1 to C6 alkyl(s);
- -a benzofuran;
- -a benzothiophene;
- -a dibenzofuran;
- -a dibenzothiophene;
- -a benzothiazole;
- -a naphthalene;
- -an indole, optionally substituted on the nitrogen with a C1 to C6 alkyl;
- where Rb is a hydrogen or a C1 to C6 alkyl, and n is 0 or 1;
- where Rc is a hydrogen, a —CONHRx, where Rx is as defined above, or an —SO2Rx, where Rx is as defined above;
- or
- where Rd is a C1 to C6 alkyl or a C6 to C8 aryl;
- -a —NHCORe group, where Re is:
- -a C1 to C6 alkyl;
- -a C6 to C8 aryl optionally substituted with:
- -a C1 to C6 alkyl,
- -an alkoxy,
- -a cyano group,
- -a nitro group, or
- -a halogen;
- -a —NHCOORx group, where Rx is as defined above;
- -a —CH2O—Rf group, where Rf is a C6 to C8 aryl;
- -a —NRgRh group, where Rg is a C1 to C6 alkyl or a hydrogen and Rh is a C6 to C8 aryl optionally substituted with an alkoxy;
- -a C1 to C6 alkyl;
- -a 5 or 6 membered heteroaryl, optionally substituted with:
- -a C1 to C6 alkyl, optionally substituted with a C6 to C8 aryl,
- -a C6 to C8 aryl, optionally substituted with —COORx, where Rx is as defined above, or
- -an amino group;
- -a 5 or 6 membered heterocycle optionally substituted with:
- -a —COORx group, where Rx is as defined above, or
- -a —NHCOORx group, where Rx is as defined above;
- -a C6 to C8 aryl, optionally substituted with one or more of the following:
- -an alkoxy, optionally substituted with:
- -an alkoxy,
- -a hydroxy,
- -one or more halogen(s),
- -a 5 or 6 membered heterocycle, optionally substituted with:
- -a C1 to C6 alkyl, or
- -a hydroxy,
- -an amino group optionally substituted with one or more C1 to C6 alkyl(s),
- -a —NRiSO2Rx group, where Rx is as defined above and Ri is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —NRjCORk group, where Rk is:
- -a C1 to C6 alkyl,
- -a hydrogen, or
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- and Rj is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —N═N+═N− group, or
- -a —CORl, where Rl is a 5 or 6 membered heterocycle optionally substituted with a hydroxy,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -a nitro group,
- -a C1 to C6 alkyl group, optionally substituted with:
- -a —NHSO2Rx group, where Rx is as defined above, or
- -a —NRxSO2Rx group, where Rx is as defined above,
- -a haloalkoxy,
- -a halogen,
- -a hydroxy,
- -a —COORx group, where Rx is as defined above,
- -a —CORm group, where Rm is:
- -an amino optionally substituted with one or more C1 to C6 alkyl(s), where the one or more C1 to C6 alkyl(s) is/are optionally substituted with:
- -a hydroxy
- -a 5 or 6 membered heterocycle,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -an alkoxy,
- -a 3 to 7 membered heterocycle, optionally substituted with a C1 to C6 alkyl, optionally substituted with a dialkyl-amino,
- -a —NHRn group, where Rn is:
- -a —CH2CONH2, or
- -a C6 to C8 aryl optionally substituted with:
- -an alkyl,
- -one or more halogen(s),
- -a nitro group, or
- -one or more alkoxy(s),
- -a —NRoCORp group, where Rp is:
- -a C1 to C6 alkyl optionally substituted with:
- -a halogen,
- -an alkoxy, or
- -a C6 to C8 aryl,
- -a 5 or 6 membered heterocycle,
- -a C6 to C8 aryl, optionally substituted with a halogen,
- -a 5 or 6 membered heteroaryl optionally substituted with one or more C1 to C6 alkyl(s),
- -a hydrogen,
- and where Ro is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —NRqCONRqRr group, where Rq is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a haloalkoxy, or
- -a —CORx group, where Rx is as defined above,
- and where Rr is:
- -a C6 to C8 aryl optionally substituted with:
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a —ORs group, where Rs is a C6 to C8 aryl, or
- -a —COORx group, where Rx is as defined above,
- -a C1 to C6 alkyl optionally substituted with one or more of the following:
- -a halogen,
- -an alkylene,
- -a C6 to C8 aryl, and/or
- -a —COORx group, where Rx is as defined above,
- -a —COORx group, where Rx is as defined above,
- -a —NRtCOORu group, where Ru is:
- -a C1 to C12 alkyl, optionally substituted with:
- -a C6 to C8 aryl optionally substituted with a C1 to C6 alkyl or an alkoxy,
- -an alkylene,
- -an alkoxy,
- -an alkyne,
- -a halogen, or
- -a 5 or 6 membered heterocycle,
- -a C6 to C8 aryl, optionally substituted with:
- -an alkoxy,
- -a halogen, or
- -a C1 to C6 alkyl, or
- -a 5 or 6 membered heterocycle,
- and Rt is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl, or
- -a haloalkoxy,
- -a —NRvSO2Rw group, where Rv is:
- -a hydrogen,
- -a —CORx, where Rx is as defined above, or
- -a C1 to C6 alkyl, optionally substituted with:
- -a halogen,
- -a —CORx group, where Rx is as defined above,
- -a —OCORx group, where Rx is as defined above,
- -a hydroxy, or
- -an alkoxy,
- and where Rw is:
- -a C1 to C6 alkyl optionally substituted with:
- -a halogen,
- -a haloalkyl,
- -a C6 to C8 aryl, or
- -a 5 or 6 membered heterocycle,
- -a C2 to C6 alkylene,
- -an alkyl- or dialkyl-amino optionally substituted with a halogen,
- -a 5 or 6 membered heterocycle, or
- -a 5 or 6 membered heteroaryl optionally substituted with:
- -a C1 to C6 alkyl,
- -a 5 or 6 membered heterocycle, or
- optionally substituted with a C1 to C6 alkyl, where Ry is a C1 to C6 alkyl or hydrogen,
- where Rz is hydrogen or a C1 to C6 alkyl, optionally substituted with a C6 to C8 aryl,
- -a —SRx group, where Rx is as defined above,
- -a —SO2Raa group, where Raa is:
- -a C1 to C6 alkyl,
- -an amino group,
- -an alkyl- or dialkyl-amino group optionally substituted with a hydroxy or a —COORx group, where Rx is as defined above,
- -a 5 or 6 membered heteroaryl,
- -a C6 to C8 aryl, and/or
- -a —NHRbb group, where Rbb is:
- -a —C(═S)NH2 group, or
- -a —PO(ORx)2 group, where Rx is as defined above;
- -a *Rcc group, where Rcc is:
- -a naphthalene,
- -a 5 or 6 membered heteroaryl,
- -a C6 to C8 aryl, optionally substituted with one or more of the following:
- -an alkoxy,
- -a hydroxy,
- -a halogen,
- -a C1 to C6 alkyl, optionally substituted with a cyano group,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -a —NHPORxRx, where Rx is as defined above,
- -a —NReeCONRffRff group, where Ree is a hydrogen or a C1 to C6 alkyl, optionally substituted with a halogen, and Rff is:
- -a hydrogen,
- -a haloalkyl,
- -a haloalkoxy,
- -a C1 to C6 alkyl, or
- -a —CORx, where Rx is as defined above,
- -a —NRggCORhh group, where Rhh is:
- -a hydrogen,
- -a C1 to C6 alkyl optionally substituted with:
- -an alkoxy,
- -a halogen, or
- -an amino optionally substituted with one or more C1 to C6 alkyl(s),
- -an amino optionally substituted with one or more C1 to C6 alkyl(s), where the one or more C1 to C6 alkyl(s) is/are optionally substituted with a halogen,
- -a 5 or 6 membered heterocycle,
- -a 5 or 6 membered heteroaryl,
- and Rgg is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a haloalkoxy, or
- -a —CORx group, where Rx is as defined above,
- -a haloalkyl,
- -5 or 6 membered heterocycle groups,
- -an amino optionally substituted with one or more C1 to C6 alkyl(s), and/or
- -a —NRiiSO2Rx group, where Rx is as defined above, and Rii is:
- -a hydrogen,
- -a C1 to C6 alkyl,
- -a haloalkyl,
- -a haloalkoxy,
- -a —CORx group, where Rx is as defined above;
- Z is:
- -a C1 to C6 alkyl optionally substituted with:
- -an alkoxy,
- -one or more halogen(s), or
- -a C6 to C8 aryl;
- -a C2 to C6 alkylene;
- -a C6 to C8 aryl optionally substituted with an alkoxy or one or more C1 to C6 alkyl(s);
- -a —COORx group, where Rx is as defined above;
- or
- R is a hydrogen, a halogen or an alkoxy;
- R1 is:
- -a hydrogen;
- -a hydroxy;
- -a halogen;
- -a haloalkyl;
- -a nitro group;
- -a 5 or 6 membered heteroaryl;
- -a 5 or 6 membered heterocycle;
- -an alkoxy optionally substituted with:
- -one or more halogen(s),
- -a C6 to C8 aryl, or
- -a 5 or 6 membered heterocycle;
- -a C6 to C8 aryl optionally substituted with an alkoxy;
- -a —CORx group, where Rx is as defined above;
- -a C1 to C6 alkyl optionally substituted with a dialkyl-amino or a 5 or 6 membered heterocycle;
- or
- R1 joins together with R2 to form:
- R2 is:
- -a nitro group;
- -a hydrogen;
- -a halogen;
- -a hydroxy group;
- -a C1 to C6 alkyl group, optionally substituted with one or more halogen(s);
- -an amino group;
- -an alkoxy group optionally substituted with:
- -one or more halogen(s),
- -an —OCORx group, where Rx is as defined above,
- -a dialkyl-amino optionally substituted with an alkoxy,
- -a 5 or 6 membered heterocycle group optionally substituted with a C1 to C6 alkyl,
- -a 5 or 6 membered heteroaryl group, or
- -a C6 to C8 aryl group;
- -a —COORx group, where Rx is as defined above;
- -a haloalkyl;
- -an amide group optionally substituted with:
- -a hydroxy group, or
- -a C6 to C8 aryl;
- -a 5 or 6 membered heteroaryl;
- -a —OCORx group, where Rx is as defined above;
- -a —NHCORjj group, where Rjj is:
- -an alkoxy, or
- -an amino optionally substituted with one or more C1 to C6 alkyl(s);
- -a —ORkk group, where Rkk is a 5 to 6 membered heteroaryl;
- -a —NHSO2Rx group, where Rx is as defined above;
- or
- R2 joins together with R1 to form:
- R3 is:
- -a hydrogen;
- or
- —CH2OCORx, and Rx is as defined above;
- or
- one or more pharmaceutically acceptable salt(s) thereof.
Dependencies are inferred from the claim text.