Patent ID: 7473699
Filing Date: 2009-01-06
Classification: A61P,C07D

Abstract:
1. A compound of the formula (I), or a pharmaceutically acceptable salt, or an in-vivo hydrolysable ester thereof, wherein —N-HET is selected from structures I(d) to (If): R Q is selected from Q1 to Q6: R T is selected from the groups (TA) to (TE); (TA) T is selected from the following groups: wherein: R R R R (TAba) a group of the formula (TAba1) wherein Z X (TAbb) an acetylene of the formula —≡—H or —≡-(1-4C)alkyl; (TAbc) —X X X X with the following provisos; Y Y (TB) T is selected from halo, formyl, or —NRv (TBac) (1-4C)alkyl {optionally substituted with one or more groups each independently selected from hydroxy, (1-4C)alkoxy, (1-4C)alkanoyl, cyano, halo, trifluoromethyl, (1-4C)alkoxycarbonyl, —NRvRw, (1-6C)alkanoylamino, (1-4C)alkoxycarbonylamino, N-(1-4C)alkyl-N-(1-6C)alkanoylamino, (1-4C)alkylS(O) (TC) T is wherein in (TC4): n1 is 1 or 2; o1 is 1 or 2, and n1+o1=2 or 3; >A wherein in (TC4); m1; n1, and o1 are as defined hereinbefore in (TC): >A Rq is hydrogen, hydroxy, halo, (1-4C)alkyl, or (1-4C)alkanoyloxy; Rr is independently hydrogen or (1-4C)alkyl; R wherein Rc is selected from groups (Rc1) to (Rc5): (Rc1) (1-6C)alkyl {optionally substituted with one or more (1-4C)alkanoyl groups (including geminal disubstitution) or optionally monosubstituted with cyano, (1-4C)alkoxy,trifluoromethyl, (1-4C)alkoxycarbonyl, phenyl (optionally substituted as AR1), or (1-4C)alkylS(O) (Rc2) formyl, R wherein R (Rc2a) AR1, AR2, AR2a, AR2b, AR3, AR3a, AR3b, AR4, AR4a, CY1, or CY2; (Rc2b) (1-4C)alkoxycarbonyl, trifluoromethyl, —NRvRw [wherein Rv is hydrogen or (1-4C)alkyl; Rw is hydrogen or (1-4C)alkyl], ethenyl, 2-(1-4C)alkylethenyl, 2-cyanoethenyl, 2-cyano-2-((1-4C)alkyl)ethenyl, 2-nitroethenyl, 2-nitro-2-((1-4C)alkyl)ethenyl, 2-((1-4C)alkylaminocarbonyl)ethenyl, 2-((1-4C)alkoxycarbonyl)ethenyl, 2-(AR1)ethenyl, 2-(AR2)ethenyl, or 2-(AR2a)ethenyl; (Rc2c) (1-10C)alkyl {optionally substituted with one or more groups (including geminal disubstitution) each independently selected from hydroxy, (1-10C)alkoxy, (1-4C)alkoxy-(1-4C)alkoxy, (1-4C)alkoxy-(1-4C)alkoxy-(1-4C)alkoxy, (1-4C)alkanoyl, carboxy, phosphoryl [—O—P(O)(OH) (Rc2d) R (Rc2e) R (Rc3) hydrogen, cyano, 2-cyanoethenyl, 2-cyano-2-((1-4C)alkyl)ethenyl, 2-((1-4C)alkylaminocarbonyl)ethenyl, 2-((1-4C)alkoxycarbonyl)ethenyl, 2-nitroethenyl, 2-nitro-2-((1-4C)alkyl)ethenyl, 2-(AR1)ethenyl, 2-(AR2)ethenyl, or (Rc3a) wherein X 00 is —OR 17 , —SR 17 , —NHR 17 , or —N(R 17 ) 2 ; R R R (Rc4) trityl, AR1, AR2, AR2a, AR2b, AR3, AR3a, or AR3b; (Rc5) RdOC(Re)═CH(C═O)—, RfC(═O)C(═O)—, RgN═C(Rh)C(═O)—, or RiNHC(Rj)=CHC(═O)—, wherein Rd is (1-6C)alkyl; Re is hydrogen or (1-6C)alkyl, or Rd and Re together form a (3-4C)alkylene chain; Rf is hydrogen, (1-6C)alkyl, hydroxy(1-6C)alkyl, (1-6C)alkoxy(1-6C)alkyl, —NRvRw [wherein Rv is hydrogen or (1-4C)alkyl; Rw is hydrogen or (1-4C)alkyl], (1-6C)alkoxy, (1-6C)alkoxy(1-6C)alkoxy, hydroxy(2-6C)alkoxy, (1-4C)alkylamino(2-6C)alkoxy, di-(1-4C)alkylamino(2-6C)alkoxy; Rg is (1-6C)alkyl, hydroxy, or (1-6C)alkoxy; Rh is hydrogen or (1-6C)alkyl; Ri is hydrogen, (1-6C)alkyl, AR1, AR2, AR2a, or AR2b, and Rj is hydrogen or (1-6C)alkyl; wherein AR1 is an optionally substituted phenyl or optionally substituted naphthyl; AR2 is an optionally substituted 5- or 6-membered, fully unsaturated monocyclic heteroaryl ring containing up to four heteroatoms independently selected from O, N and S (but not containing any O—O, O—Se or S—S bonds), and linked via a ring carbon atom, or a ring nitrogen atom if the ring is not thereby quaternised; AR2a is a partially hydrogenated version of AR2, linked via a ring carbon atom or linked via a ring nitrogen atom if the ring is not thereby quaternised; AR2b is a fully hydrogenated version of AR2, linked via a ring carbon atom or linked via a ring nitrogen atom; AR3 is an optionally substituted 8-, 9- or 10-membered, fully unsaturated bicyclic heteroaryl ring containing up to four heteroatoms independently selected from O, N, and S (but not containing any O—O, O—S, or S—S bonds), and linked via a ring carbon atom in either of the rings comprising the bicyclic system; AR3a is a partially hydrogenated version of AR3, linked via a ring carbon atom, or linked via a ring nitrogen atom if the ring is not thereby quaternised, in either of the rings comprising the bicyclic system; AR3b is a fully hydrogenated version of AR3, linked via a ring carbon atom, or linked via a ring nitrogen atom, in either of the rings comprising the bicyclic system; AR4 is an optionally substituted 13- or 14-membered, fully unsaturated tricyclic heteroaryl ring containing up to four heteroatoms independently selected from O, N, and S (but not containing any O—O, O—S, or S—S bonds), and linked via a ring carbon atom in any of the rings comprising the tricyclic system; AR4a is a partially hydrogenated version of AR4, linked via a ring carbon atom, or linked via a ring nitrogen atom if the ring is not thereby quaternised, in any of the rings comprising the tricyclic system; CY1 is an optionally substituted cyclobutyl, cyclopentyl, or cyclohexyl ring; CY2 is an optionally substituted cyclopentenyl or cyclohexenyl ring; wherein; optional substituents on AR1, AR2, AR2a, AR2b, AR3, AR3a, AR3b, AR4, AR4a, CY1, and CY2 are (on an available carbon atom) up to three substituents independently selected from (1-4C)alkyl {optionally substituted with substituents selected independently from hydroxy, trifluoromethyl, (1-4C)alkyl S(O) and further optional substituents on AR1, AR2, AR2a, AR2b, AR3, AR3a, AR3b, AR4, AR4a, CY1, CY2 (on an available carbon atom), and alkyl groups (unless indicated otherwise) are up to three substituents independently selected from trifluoromethoxy, benzoylamino, benzoyl, phenyl {optionally substituted with up to three substituents independently selected from halo, (1-4C)alkoxy or cyano}, furan, pyrrole, pyrazole, imidazole, triazole, pyrimidine, pyridazine, pyridine, isoxazole, oxazole, isothiazole, thiazole, thiophene, hydroxyimino(1-4C)alkyl, (1-4C)alkoxyimino(1-4C)alkyl, halo-(1-4C)alkyl, (1-4C)alkanesulfonamido, or —SO