IP Library Granted Patent US 8,242,116
Granted Patent B2
US 8,242,116 · App. 12/306,151 · Granted Aug 14, 2012

Fused thiazole derivatives as kinase inhibitors

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Quick Facts
Patent No.
US 8,242,116
App. No.
12/306,151
Granted
Aug 14, 2012
Kind
B2
Abstract

A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

Claims (53)

1. A compound of formula (I), or a pharmaceutically acceptable salt thereof:

wherein

X represents oxygen or sulphur;

Y represents a group of formula CR 6 R 7 or NR 8 ;

R 1 represents hydrogen or C 1-6 alkyl; and

R 2 represents hydrogen; or C 1-6 alkyl, C 1-6 alkoxy, C 3-7 cycloalkyl, C 3-7 cycloalkyl(C 1-6 )alkyl, aryl, aryl(C 1-6 )alkyl, C 3-7 heterocycloalkyl, C 3-7 heterocycloalkyl(C 1-6 )alkyl, heteroaryl or heteroaryl(C 1-6 )alkyl, any of which groups may be optionally substituted by one or more substituents; or

R 1 and R 2 , when taken together with the carbon atom to which they are both attached, represent C 3-7 cycloalkyl or C 3-7 heterocycloalkyl, either of which groups may be optionally substituted by one or more substituents;

R 3 and R 4 independently represent hydrogen; or C 1-6 alkyl, C 2-6 alkynyl, C 3-7 cycloalkyl, C 3-7 cycloalkyl(C 1-6 )alkyl, aryl, aryl(C 1-6 )alkyl, aryl(C 2-6 )alkenyl, aryl(C 2-6 )-alkynyl, biaryl(C 1-6 )alkyl, C 3-7 heterocycloalkyl, C 3-7 heterocycloalkyl(C 1-6 )alkyl, C 3-7 heterocycloalkylcarbonyl, heteroaryl, heteroaryl(C 1-6 )alkyl, heteroaryl-aryl(C 1-6 )alkyl or arylheteroaryl(C 1-6 )alkyl, any of which groups may be optionally substituted by one or more substituents; or

R 3 and R 4 , when both are attached to the same carbon atom, represent, when taken together with the carbon atom to which they are both attached, C 3-7 cycloalkyl or C 3-7 heterocycloalkyl, either of which groups may be optionally substituted by one or more substituents; or

R 3 and R 4 , when attached to adjacent carbon atoms, represent, when taken together with the carbon atoms to which they are attached, C 5-7 cycloalkyl, phenyl or heteroaryl, any of which groups may be optionally benzo-fused and/or substituted by one or more substituents;

R 5 represents hydrogen or C 1-6 alkyl;

R 6 represents hydrogen; or C 1-6 alkyl, C 1-6 alkoxy, C 3-7 cycloalkyl, C 3-7 cycloalkyl(C 1-6 )alkyl, aryl, aryl(C 1-6 )alkyl, C 3-7 heterocycloalkyl, C 3-7 heterocycloalkyl(C 1-6 )alkyl, heteroaryl or heteroaryl(C 1-6 )alkyl, any of which groups may be optionally substituted by one or more substituents; and

R 7 represents hydrogen or C 1-6 alkyl; or

R 6 and R 7 , when taken together with the carbon atom to which they are both attached, represent C 3-7 cycloalkyl or C 3-7 heterocycloalkyl, either of which groups may be optionally substituted by one or more substituents; or

R 2 and R 6 , when taken together with the carbon atoms to which they are attached, represent C 5-7 cycloalkyl, phenyl or heteroaryl, any of which groups may be optionally benzo-fused and/or substituted by one or more substituents; and

R 8 represents hydrogen; or C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyl(C 1-6 )alkyl, aryl, aryl(C 1-6 )alkyl, C 3-7 heterocycloalkyl, C 3-7 heterocycloalkyl-(C 1-6 )alkyl, heteroaryl or heteroaryl(C 1-6 )alkyl, any of which groups may be optionally substituted by one or more substituents; or

R 2 and R 8 , when taken together with the carbon and nitrogen atoms to which they are respectively attached, represent C 5-7 heterocycloalkyl or heteroaryl, either of which groups may be optionally benzo-fused and/or substituted by one or more substituents.

2. A compound as claimed in claim 1 represented by formula (IIA), or a pharmaceutically acceptable salt thereof:

wherein

R 11 represents hydrogen or C 1-6 alkyl; and

R 12 represents hydrogen; or C 1-6 alkyl, C 1-6 alkoxy, C 3-7 cycloalkyl, C 3-7 cycloalkyl(C 1-6 )alkyl, aryl, aryl(C 1-6 )alkyl, C 3-7 heterocycloalkyl, C 3-7 heterocycloalkyl(C 1-6 )alkyl, heteroaryl or heteroaryl(C 1-6 )alkyl, any of which groups may be optionally substituted by one or more substituents; or

R 11 and R 12 , when taken together with the carbon atom to which they are both attached, represent C 3-7 cycloalkyl or C 3-7 heterocycloalkyl, either of which groups may be optionally substituted by one or more substituents; and

R 13 represents hydrogen; or C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyl(C 1-6 )alkyl, aryl, aryl(C 1-6 )alkyl, aryl(C 2-6 )alkenyl, aryl(C 2-6 )alkynyl, biaryl(C 1-6 )alkyl, C 3-7 heterocycloalkyl, C 3-7 heterocycloalkyl(C 1-6 )alkyl, C 3-7 heterocycloalkylcarbonyl, heteroaryl, heteroaryl(C 1-6 )alkyl, heteroaryl-aryl(C 1-6 )alkyl or aryl-heteroaryl(C 1-6 )alkyl, any of which groups may be optionally substituted by one or more substituents.

3. A compound as claimed in claim 2 represented by formula (IIB), or a pharmaceutically acceptable salt thereof:

wherein

R 11 represents hydrogen or C 1-6 alkyl; and

R 12 represents hydrogen; or C 1-6 alkyl, C 1-6 alkoxy, C 3-7 cycloalkyl, C 3-7 cycloalkyl(C 1-6 )alkyl, aryl, aryl(C 1-6 )alkyl, C 3-7 heterocycloalkyl, C 3-7 heterocycloalkyl(C 1-6 )alkyl, heteroaryl or heteroaryl(C 1-6 )alkyl, any of which groups may be optionally substituted by one or more substituents; or

R 11 and R 12 , when taken together with the carbon atom to which they are both attached, represent C 3-7 cycloalkyl or C 3-7 heterocycloalkyl, either of which groups may be optionally substituted by one or more substituents; and

T represents N—R 25 ;

V represents carbon or nitrogen;

W represents carbon or nitrogen;

R 23 represents hydrogen, halogen, cyano, nitro, C 1-6 alkyl, hydroxy(C 1-6 )alkyl, trifluoromethyl, aryl(C 1-6 )alkyl, oxazolinyl, triazolyl, hydroxy, C 1-6 alkoxy, difluoromethoxy, trifluoromethoxy, C 3-7 cycloalkoxy, C 3-7 cycloalkyl(C 1-6 )alkoxy, morpholinyl(C 1-6 )alkoxy, aryloxy, aryl(C 1-6 )alkoxy, C 1-6 alkylthio, C 1-6 alkylsulphinyl, arylsulphinyl, arylsulphonyl, C 1-6 alkylsulphonyloxy, amino, azetidinyl, morpholinyl, C 2-6 alkylcarbonylamino, C 2-6 alkylcarbonylaminomethyl, C 2-6 alkoxycarbonylamino, [(C 2-6 )alkoxycarbonyl][(C 1-6 )alkyl]amino, C 1-6 alkylsulphonylamino, C 2-6 alkylcarbonyl, C 2-6 alkylcarbonyl oxime, C 2-6 alkylcarbonyl O-(methyl)oxime, trifluoromethylcarbonyl, carboxy, C 2-6 alkoxycarbonyl, aminocarbonyl, C 1-6 alkylaminocarbonyl, [hydroxy(C 1-6 )alkyl]aminocarbonyl, [di(C 1-6 )alkylamino(C 1-6 )alkyl]aminocarbonyl, di(C 1-6 )alkylaminocarbonyl, [(C 1-6 )alkyl][cyano(C 1-6 )alkyl]aminocarbonyl, [(C 1-6 )alkyl][hydroxy(C 1-6 )alkyl]aminocarbonyl, [(C 1-6 )alkoxy(C 1-6 )alkyl][(C 1-6 )alkyl]aminocarbonyl, [di(C 1-6 )alkylamino(C 1-6 )alkyl][(C 1-6 )alkyl]aminocarbonyl, C 3-7 cycloalkyl(C 1-6 )alkylaminocarbonyl, aryl(C 1-6 )alkylaminocarbonyl, heteroarylaminocarbonyl, heteroaryl(C 1-6 )alkylamino-carbonyl, azetidinylcarbonyl, hydroxyazetidinylcarbonyl, aminoazetidinylcarbonyl, C 2-6 alkoxycarbonylaminoazetidinylcarbonyl, pyrrolidinylcarbonyl, (C 1-6 )alkylpyrrolidinylcarbonyl, C 1-6 alkoxy(C 1-6 )alkylpyrrolidinylcarbonyl, di(C 1-6 )alkylaminopyrrolidinyl-carbonyl, thiazolidinylcarbonyl, oxothiazolidinylcarbonyl, piperidinylcarbonyl, (C 1-6 )alkylpiperazinylcarbonyl, morpholinylcarbonyl, C 1-6 alkylsulphonyl, C 1-6 alkylsulphonylmethyl or di(C 1-6 )alkylaminosulphonyl; and

R 24 represents hydrogen, halogen, C 1-6 alkoxy or di(C 1-6 )alkylaminocarbonyl; or

R 23 and R 24 , when situated on adjacent carbon atoms, together represent methylenedioxy or difluoromethylenedioxy; and

R 25 represents hydrogen.

4. A compound as claimed in claim 2 represented by formula (IIC), or a pharmaceutically acceptable salt thereof:

wherein

R 11 represents hydrogen or C 1-6 alkyl; and

R 12 represents hydrogen; or C 1-6 alkyl, C 1-6 alkoxy, C 3-7 cycloalkyl, C 3-7 cycloalkyl(C 1-6 )alkyl, aryl, aryl(C 1-6 )alkyl, C 3-7 heterocycloalkyl, C 3-7 heterocycloalkyl-(C 1-6 )alkyl, heteroaryl or heteroaryl(C 1-6 )alkyl, any of which groups may be optionally substituted by one or more substituents; or

R 11 and R 12 , when taken together with the carbon atom to which they are both attached, represent C 3-7 cycloalkyl or C 3-7 heterocycloalkyl, either of which groups may be optionally substituted by one or more substituents; and

R 33 represents halogen or —NHR 34 ; or aryl or heteroaryl, either of which groups may be optionally substituted by one or more substituents; and

R 34 represents methylenedioxyphenyl, morpholinyl(C 1-6 )alkylphenyl, oxazolinylphenyl, [(C 1-6 )alkyl](oxo)pyrazolylphenyl, oxazolylphenyl, isoxazolylphenyl, triazolyl-phenyl, (C 1-6 )alkyltriazolylphenyl, (C 1-6 )alkylpyrimidinylphenyl, pyrazolyl(C 1-6 )alkyl-phenyl, triazolyl(C 1-6 )alkylphenyl, C 1-6 alkylsulphonylaminophenyl, morpholinylcarbonyl-phenyl, C 1-6 alkylsulphonylphenyl, morpholinylsulphonylphenyl, dihydrobenzofuranyl, C 1-6 alkylsulphonylindolinyl, chromanonyl, dihydroquinolinonyl, benzoxazinonyl, benzothienyl, indolyl, dioxoindolyl, [(C 1-6 )alkyl](halo)pyrazolyl, tri(C 1-6 )alkylpyrazolyl, (C 1-6 )alkylindazolyl, benzoxazolyl, benzoxazolonyl, di(C 1-6 )alkylisoxazolyl, benzothiazolyl, (C 1-6 )alkylisothiazolyl, (C 1-6 )alkylbenzimidazolyl, benzimidazolonyl, di(C 1-6 )alkylbenzimidazolonyl, (C 1-6 )alkyloxadiazolyl, furyloxadiazolyl, pyridinyl, halopyridinyl, (C 1-6 )alkylpyridinyl, di(C 1-6 )alkylpyridinyl, (C 1-6 )alkoxypyridinyl, oxopyridinyl, oxopyrimidinyl, thioxopyrimidinyl, [(C 1-6 )alkoxy](halo)pyridazinyl, (C 1-6 )alkylcinnolinyl, quinoxalinyl or (C 1-6 )alkylchromenyl.

5. A compound as claimed in claim 1 represented by formula (IID-1) or (IID-2), or a pharmaceutically acceptable salt thereof:

wherein

R 11 represents hydrogen or C 1-6 alkyl; and

R 12 represents hydrogen; or C 1-6 alkyl, C 1-6 alkoxy, C 3-7 cycloalkyl, C 3-7 cycloalkyl(C 1-6 )alkyl, aryl, aryl(C 1-6 )alkyl, C 3-7 heterocycloalkyl, C 3-7 heterocycloalkyl(C 1-6 )alkyl, heteroaryl or heteroaryl(C 1-6 )alkyl, any of which groups may be optionally substituted by one or more substituents; or

R 11 and R 12 , when taken together with the carbon atom to which they are both attached, represent C 3-7 cycloalkyl or C 3-7 heterocycloalkyl, either of which groups may be optionally substituted by one or more substituents; and

R 43 represents hydrogen, halogen, nitro, C 1-6 alkyl, C 2-6 alkenyl, C 3-7 cycloalkyl, (C 1-6 )alkylaryl, di(C 1-6 )alkylaryl, piperidinyl(C 1-6 )alkylaryl, piperazinyl(C 1-6 )alkylaryl, (C 1-6 )alkylpiperazinyl(C 1-6 )alkylaryl, morpholinyl(C 1-6 )alkylaryl, (C 1-6 )alkoxyaryl, cyano(C 1-6 )alkoxyaryl, di(C 1-6 )alkylamino(C 1-6 )alkylaryl, (C 1-6 )alkylaminocarbonylaryl, aryl(C 1-6 )alkyl, haloarylpyrrolidinyl, dioxopyrrolidinyl, aminopyrrolidinyl, di(C 1-6 )alkylaminopyrrolidinyl, indolinyl, oxoindolinyl, arylpiperidinyl, arylcarbonylpiperidinyl, di(C 1-6 )alkylaminocarbonylpiperidinyl, piperazinyl, (C 1-6 )alkylpiperazinyl, haloaryl-piperazinyl, pyridinylpiperazinyl, furoylpiperazinyl, homopiperazinyl, (C 1-6 )alkyl-homopiperazinyl, (C 1-6 )alkylpiperazinyl(C 1-6 )alkyl, morpholinyl(C 1-6 )alkyl, benzofuryl, benzothienyl, pyrazolyl, (C 1-6 )alkylpyrazolyl, di(C 1-6 )alkylpyrazolyl, tri(C 1-6 )alkyl-pyrazolyl, [di(C 1-6 )alkyl](trifluoromethyl)pyrazolyl, cyano(C 1-6 )alkylpyrazolyl, [cyano(C 1-6 )alkyl][di(C 1-6 )alkyl]pyrazolyl, hydroxy(C 1-6 )alkylpyrazolyl, [hydroxy(C 1-6 )alkyl][di(C 1-6 )alkyl]pyrazolyl, methoxy(C 1-6 )alkylpyrazolyl, [(hydroxy)(methoxy)(C 1-6 )alkyl]pyrazolyl, amino(C 1-6 )alkylpyrazolyl, [(C 1-6 )alkyl][amino(C 1-6 )alkyl]pyrazolyl, [amino(C 1-6 )alkyl][di(C 1-6 )alkyl]pyrazolyl, di(C 1-6 )alkylamino(C 1-6 )alkylpyrazolyl, di(C 1-6 )alkoxyphosphono(C 1-6 )alkylpyrazolyl, (C 2-6 )alkenylpyrazolyl, (C 3-7 )cycloalkyl(C 1-6 )alkylpyrazolyl, [(C 3-7 )cycloalkyl(C 1-6 )alkyl][di(C 1-6 )alkyl]pyrazolyl, [(C 1-6 )alkyl]-(aryl)pyrazolyl, (aryl)(trifluoromethyl)pyrazolyl, aryl(C 1-6 )alkylpyrazolyl, aminoaryl(C 1-6 )alkylpyrazolyl, piperidinylpyrazolyl, tetrahydropyranyl(C 1-6 )alkylpyrazolyl, [di(C 1-6 )alkyl][tetrahydropyranyl(C 1-6 )alkyl]pyrazolyl, pyrrolidinyl(C 1-6 )alkylpyrazolyl, piperidinyl(C 1-6 )alkylpyrazolyl, (C 1-6 )alkylpiperidinyl(C 1-6 )alkylpyrazolyl, morpholinyl(C 1-6 )alkylpyrazolyl, pyridinyl(C 1-6 )alkylpyrazolyl, oxypyridinyl(C 1-6 )alkylpyrazolyl, [arylcarbonyl(C 1-6 )alkyl][di(C 1-6 )alkyl]pyrazolyl, [(C 1-6 )alkyl](piperazinylcarbonyl)pyrazolyl, [(C 1-6 )alkylaminocarbonyl][(C 1-6 )alkylaryl]pyrazolyl, [(C 1-6 )alkyl]-[amino(C 1-6 )alkylaminocarbonyl]pyrazolyl, aminocarbonyl(C 1-6 )alkylpyrazolyl, [aminocarbonyl(C 1-6 )alkyl][di(C 1-6 )alkyl]pyrazolyl, di(C 1-6 )alkylaminocarbonyl(C 1-6 )alkylpyrazolyl, pyrazolo[1,5-c]pyridinyl, di(C 1-6 )alkylisoxazolyl, (amino)[(C 1-6 )alkyl]-isoxazolyl, thiazolyl, di(C 1-6 )alkylthiazolyl, imidazolyl, (C 1-6 )alkylimidazolyl, di(C 1-6 )-alkylimidazolyl, imidazo[1,2-c]pyridinyl, (C 1-6 )alkylimidazo[1,2-c]pyridinyl, (C 1-6 )-alkylimidazo[4,5-b]pyridinyl, imidazo[1,2-c]pyrimidinyl, imidazo[1,2-c]pyrazinyl, (C 1-6 )-alkylthiadiazolyl, pyridinyl, halopyridinyl, (C 1-6 )alkyl-pyridinyl, [(C 1-6 )alkyl](halo)-pyridinyl, di(C 1-6 )alkylpyridinyl, (C 2-6 )alkenylpyridinyl, (C 1-6 )alkylpiperazinylpyridinyl, [(C 1-6 )alkyl](piperazinyl)pyridinyl, [(C 1-6 )alkoxycarbonylpiperazinyl][(C 1-6 )alkyl]-pyridinyl, piperidinyl(C 1-6 )alkylpyridinyl, [(C 1-6 )alkyl](oxy)pyridinyl, hydroxypyridinyl, hydroxy(C 1-6 )alkylpyridinyl, (C 1-6 )alkoxypyridinyl, [(C 1-6 )alkoxy][(C 1-6 )alkyl]pyridinyl, [(C 1-6 )alkoxy][di(C 1-6 )alkyl]pyridinyl, (C 1-6 )alkoxy(C 1-6 )alkylpyridinyl, aminopyridinyl, carboxy(C 1-6 )alkylpyridinyl, (C 1-6 )alkoxycarbonyl(C 1-6 )alkylpyridinyl, pyridazinyl, (C 1-6 )alkylpyridazinyl, piperidinylpyridazinyl, oxypyridazinyl, (C 1-6 )alkoxypyridazinyl, aminopyridazinyl, hydroxy(C 1-6 )alkylaminopyridazinyl, di(C 1-6 )alkylaminopyridazinyl, pyrimidinyl, (C 1-6 )alkylpyrimidinyl, [(C 1-6 )alkyl](halo)pyrimidinyl, di(C 1-6 )alkyl-pyrimidinyl, pyrrolidinylpyrimidinyl, (C 1-6 )alkylpiperazinylpyrimidinyl, [(C 1-6 )alkyl](piperazinyl)pyrimidinyl, [(C 1-6 )alkoxycarbonyl][(C 1-6 )alkyl]piperazinylpyrimidinyl, hydroxypyrimidinyl, [(C 1-6 )alkyl](hydroxy)pyrimidinyl, [(C 1-6 )alkyl]-[hydroxy(C 1-6 )alkyl]pyrimidinyl, [(C 1-6 )alkyl][hydroxy(C 2-6 )alkynyl]pyrimidinyl, (C 1-6 )alkoxypyrimidinyl, aminopyrimidinyl, di(C 1-6 )alkylaminopyrimidinyl, [di(C 1-6 )alkylamino](halo)pyrimidinyl, carboxypyrimidinyl, [(C 1-6 )alkoxycarbonyl(C 1-6 )alkyl][(C 1-6 )alkyl]pyrimidinyl, aminocarbonylpyrimidinyl, pyrazinyl, (C 1-6 )alkoxypyrazinyl, aminopyrazinyl, hydroxy, (C 1-6 )alkoxy, aryl(C 1-6 )alkoxycarbonylpiperidinyloxy, morpholinyl(C 1-6 )alkoxy, aryloxy, haloaryloxy, di(C 1-6 )alkylpyrazolyloxy, halopyridinyloxy, pyrrolidinylpyridinyloxy, (C 1-6 )alkylpiperazinylpyridinyloxy, (C 1-6 )alkylpyrazolylpyridinyloxy, (C 1-6 )alkylaminopyridinyloxy, carboxypyridinyloxy, aminocarbonylpyridinyloxy, (C 1-6 )alkylpyridazinyloxy, pyrimidinyloxy, (C 1-6 )alkylpyrimidinyloxy, [(C 1-6 )alkyl](halo)pyrimidinyloxy, hydroxy(C 1-6 )alkyl, dihydroxy(C 1-6 )alkyl, pyridinyloxy(C 1-6 )alkyl, amino, (C 1-6 )alkylamino, dihydroxy(C 1-6 )alkylamino, (C 1-6 )alkoxy(C 1-6 )alkylamino, N—[(C 1-6 )alkoxy(C 1-6 )alkyl]-N—[(C 1-6 )alkyl]amino, di(C 1-6 )alkylamino(C 1-6 )alkylamino, N—[(C 1-6 )alkyl]-N-[di(C 1-6 )alkylamino(C 1-6 )alkyl]amino, N—[(C 1-6 )alkyl]-N—[(C 3-7 )cycloalkyl]amino, haloarylamino, N—[(C 1-6 )alkyl]-N-(haloaryl)amino, N—[(C 1-6 )alkyl]-N—[aryl(C 1-6 )alkyl]amino, N-[di(C 1-6 )alkylamino(C 1-6 )alkyl]-N—[aryl(C 1-6 )alkyl]amino, cyanoaryl(C 1-6 )alkylamino, (cyano)(halo)aryl(C 1-6 )alkylamino, methylenedioxyaryl(C 1-6 )alkylamino, N—[(C 1-6 )alkyl]-N—[(C 1-6 )alkylpyrrolidinyl]amino, piperidinylamino, N—[(C 1-6 )alkyl]-N-(piperidinyl)amino, N—[(C 3-7 )cycloalkyl(C 1-6 )alkyl]-N(piperidinyl)amino, (C 1-6 )alkylpiperidinylamino, N—[(C 1-6 )alkyl]-N—[(C 1-6 )alkylpiperidinyl]amino, N—[(C 1-6 )alkyl]-N—[(C 3-7 )cycloalkylpiperidinyl]amino, N—[(C 1-6 )alkyl]-N—[(C 2-6 )alkylcarbonylpiperidinyl]amino, pyrrolidinyl(C 1-6 )alkylamino, N—[(C 1-6 )alkyl]-N—[pyrrolidinyl(C 1-6 )alkyl]amino, N—[(C 1-6 )alkyl]-N-[piperidinyl(C 1-6 )alkyl]amino, (C 1-6 )alkylpyrazolylamino, di(C 1-6 )alkylpyrazolylamino, tri(C 1-6 )alkylpyrazolylamino, N—[(C 1-6 )alkyl]-N—[(C 1-6 )alkylpyrazolyl]amino, thiazolylamino, imidazolylamino, [(C 1-6 )alkoxycarbonyl][(C 1-6 )alkyl]imidazolylamino, (C 1-6 )alkylthiadiazolylamino, pyridinylamino, halopyridinylamino, (C 1-6 )alkylpyridinylamino, di(C 1-6 )alkylpyridinylamino, trifluoromethylpyridinylamino, hydroxypyridinylamino, hydroxy(C 1-6 )alkylpyridinylamino, dihydroxy(C 1-6 )alkylpyridinylamino, (C 1-6 )alkoxypyridinylamino, dihydroxy(C 1-6 )alkoxypyridinylamino, di(C 1-6 )alkyldioxolanyl(C 1-6 )alkoxypyridinylamino, (C 1-6 )alkoxy(C 1-6 )alkylpyridinylamino, (C 1-6 )alkoxy(C 2-6 )alkenylpyridinylamino, dihydroxy(C 1-6 )alkylaminopyridinylamino, di(C 1-6 )alkylaminopyridinylamino, (C 1-6 )alkylamino(C 1-6 )alkylpyridinylamino, di(C 1-6 )alkylamino(C 1-6 )alkylpyridinylamino, carboxypyridinylamino, N—[(C 1-6 )alkyl]-N—[(C 1-6 )alkylpyridinyl]amino, bis[(C 1-6 )alkylpyridinyl]amino, bis(trifluoromethylpyridinyl)amino, isoquinolinylamino, (C 1-6 )alkylpyridazinylamino, N—[(C 1-6 )alkyl]-N—[(C 1-6 )alkylpyridazinyl]amino, N-[aryl(C 1-6 )alkyl]-N—[(C 1-6 )alkylpyridazinyl]amino, di(C 1-6 )alkylpyridazinylamino, arylpyridazinylamino, piperidinylpyridazinylamino, (C 1-6 )alkoxypyridazinylamino, di(C 1-6 )alkylaminopyridazinylamino, bis[(C 1-6 )alkylpyridazinyl]-amino, benzofuryl(C 1-6 )alkylamino, thienyl(C 1-6 )alkylamino, indolyl(C 1-6 )alkylamino, (C 1-6 )alkylpyrazolyl(C 1-6 )alkylamino, [di(C 1-6 )alkyl](halo)pyrazolyl(C 1-6 )alkylamino, di(C 1-6 )alkylisoxazolyl(C 1-6 )alkylamino, thiazolyl(C 1-6 )alkylamino, imidazolyl(C 1-6 )alkylamino, (C 1-6 )alkylimidazolyl(C 1-6 )alkylamino, pyridinyl(C 1-6 )alkylamino, (C 1-6 )alkylpyridinyl(C 1-6 )alkylamino, N—[(C 1-6 )alkyl]-N-[pyridinyl(C 1-6 )alkyl]amino, N-[dihydroxy(C 1-6 )alkyl]-N-[pyridinyl(C 1-6 )alkyl]amino, N—[(C 1-6 )alkylpyridinyl(C 1-6 )alkyl]-N-[dihydroxy(C 1-6 )alkyl]amino, amino(C 1-6 )alkyl, (C 1-6 )alkylamino(C 1-6 )alkyl, di(C 1-6 )alkylamino(C 1-6 )alkyl, pyridinylamino(C 1-6 )alkyl, N—[(C 2-6 )alkylcarbonyl]-N—[(C 1-6 )alkylpyridinyl(C 1-6 )alkyl]amino, di(C 1-6 )alkylamino(C 1-6 )alkylcarbonylamino, (C 3-7 )cycloalkylcarbonylamino, (C 1-6 )alkylpiperidinylcarbonylamino, (C 1-6 )alkylimidazolylcarbonylamino, formyl, C 2-6 alkylcarbonyl, (C 1-6 )alkylpiperidinylaminocarbonyl, N—[(C 1-6 )alkyl]-N—[(C 1-6 )alkylpiperidinyl]aminocarbonyl, piperidinyl(C 1-6 )alkylaminocarbonyl, (C 1-6 )alkylpiperazinylcarbonyl, C 1-6 alkylthio, C 1-6 alkylsulphinyl, C 1-6 alkylsulphonyl, C 2-6 alkoxycarbonyloxy or tetra(C 1-6 )alkyldioxaborolanyl; and

R 44 represents hydrogen, halogen, C 1-6 alkyl or C 1-6 alkoxy.

6. A compound as claimed in claim 1 represented by formula (IIE), or a pharmaceutically acceptable salt thereof:

wherein

R 13 represents hydrogen; or C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyl(C 1-6 )alkyl, aryl, aryl(C 1-6 )alkyl, aryl(C 2-6 )alkenyl, aryl(C 2-6 )alkynyl, biaryl(C 1-6 )alkyl, C 3-7 heterocycloalkyl, C 3-7 heterocycloalkyl(C 1-6 )alkyl, C 3-7 heterocycloalkylcarbonyl, heteroaryl, heteroaryl(C 1-6 )alkyl, heteroaryl-aryl(C 1-6 )alkyl or aryl-heteroaryl(C 1-6 )alkyl, any of which groups may be optionally substituted by one or more substituents.

7. A pharmaceutical composition comprising a compound of formula (I) as defined in claim 1 , or a pharmaceutically acceptable salt thereof, in association with a pharmaceutically acceptable carrier.

Assignments (2)
CONFIRMATORY ASSIGNMENT Recorded Jun 10, 2016
From: UCB PHARMA, S.A.
To: UCB BIOPHARMA SPRL
Reel/Frame 038953/0312 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 6, 2012
From: ALEXANDER, RIKKI PETER; AUJLA, PAYANDEEP SINGH; CREPY, KAREN VIVIANE LUCILE; FOLEY, ANNE MARIE; FRANKLIN, RICHARD JEREMY; HAUGHAN, ALAN FINDLAY; HORSLEY, HELEN TRACEY; JONES, WILLIAM MARK; LALLEMAND, BENEDICTE IRMA LEONCE FREDERIQUE; MACK, STEPHEN ROBERT; MORGAN, TREVOR; PASAU, PATRICK MARIE GHISLAIN; PHILLIPS, DAVID JONATHAN; SABIN, VERITY MARGARET; BUCKLEY, GEORGE MARTIN; JENKINS, KERRY; PERRY, BENJAMIN GARFIELD
To: UCB PHARMA S.A.
Reel/Frame 028501/0765 →