TETRAHYDROPYRIMIDINE DERIVATIVES

Abstract

Claim 1: A tetrahydropyridopyrimidine derivative of formula (1), and / or pharmaceutically acceptable tautomers and / or N-oxides and / or salts thereof, wherein: Y is selected from O or NR³; R1 is selected from phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,2,3-triazinyl, 1,2,4-triazinyl, 1,3,5-triazinyl, or -C(O)-R4 where: R4 is selected from C₁₋₈ alkyl, C₁₋₈ haloalkyl, C₁₋₈ hydroxyalkyl, C₁₋₈ alkoxy-C₁₋₈ alkyl, C₁₋₈ alkyl-C₁₋₈ sulfonyl-C₁₋₈ alkyl, heterocyclyl, heterocyclyloxyl, C₁₋₈ heterocyclyl-C₁₋₈, C₃₋₁₂ cycloalkyl, C₃₋₁₂-cycloalkyl C₁₋₈ alkyl, heteroaryl, heteroaryloxyl, C₁₋₈ heteroaryl-alkyl, hydroxyl, C₁₋₈ alkoxyl, amino, C₁₋₈ N-alkyl amino, or C₁₋₈ N-di-alkyl amino, wherein 'C₁₋₈ alkyl' in C₁₋₈ N-alkyl amino and C₁₋₈ N-di-alkyl amino may be unsubstituted or substituted by halogen, hydroxyl, or C₁₋₄ alkoxyl;wherein 'C₃₋₁₂cycloalkyl' in C₃₋₁₂cycloalkyl and C₃₋₁₂cycloalkyl-C₁₋₈alkyl, may be unsubstituted or substituted by 1 to 5 substituents independently selected from oxo, halogen, C₁₋₈alkyl, C₁₋₈haloalkyl, C₁₋₈hydroxyalkyl, hydroxyl, C₁₋₈alkoxyl, C₁₋₈alkoxyl-C₁₋₈alkyl, amino, C₁₋₈N-alkyl-amino, N,N-di-alkyl-C₁₋₈-amino, alkyl C₁₋₈-carbonyl, C₁₋₈-carbonyl halo-alkyl, C₁₋₈-carbonyl hydroxy-alkyl or C₁₋₈-carbonyl alkoxyl; wherein 'heterocyclyl' is selected from oxiranyl, aziridinyl, oxetanyl, thietanyl, azetidinyl, pyrrolidinyl, tetrahydro-furanyl, tetrahydro-thiophenyl, 2,3-dihydro-furanyl, 2,5-dihydro-furanyl, 2,3-dihydro-thiophenyl, 1-pyrrolinyl, 2-pyrrolinyl, 3-pyrrolinyl, tetrahydro-pyranyl, piperidinyl, tetrahydro-thiopyranyl, morpholinyl, thiomorpholinyl, piperazinyl, azepanyl, tiepanyl or oxepanyl;each of which is unsubstituted or substituted by 1 to 5 substituents independently selected from oxo, halogen, C₁₋₈ alkyl, C₁₋₈ halo-alkyl, C₁₋₈ hydroxy-alkyl, hydroxyl, C₁₋₈ alkoxy, C₁₋₈ alkoxy-C₁₋₈ alkyl, amino, C₁₋₈ N-alkyl-amino, C₁₋₈ N-di-alkyl-amino, C₁₋₈ alkyl-carbonyl, C₁₋₈ halo-alkyl-carbonyl, C₁₋₈ hydroxy-alkyl-carbonyl, or C₁₋₈ alkoxy-alkyl C₁₋₈-carbonyl; wherein 'heterocyclyl' can be attached to a heteroatom or a carbon atom, and wherein the N and / or S heteroatoms can also be optionally oxidized to different oxidation states;wherein 'heteroaryl' is selected from furanyl, thiophenyl, pyrrolyl, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, 1,2,5-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,3-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,5-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,3-thiadiazolyl, 1,3,4-thiadiazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,5-triazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,2,3-triazinyl, 1,2,4-triazinyl or 1,3,5-triazinyl; each of which is unsubstituted or substituted by 1 to 5 substituents independently selected from halogen, C₁₋₈ alkyl, C₁₋₈ halo-alkyl, C₁₋₈ hydroxy-alkyl, hydroxyl, C₁₋₈ alkoxy, C₁₋₈ alkoxy-C₁₋₈ alkyl, amino, C₁₋₈ N-alkyl-amino, C₁₋₈ N-di-alkyl-amino, C₁₋₈ alkyl-carbonyl, C₁₋₈ halo-alkyl-carbonyl, C₁₋₈ hydroxy-alkyl-carbonyl, or C₁₋₈ alkoxy-alkyl C₁₋₈carbonyl;where 'heteroaryl' can be attached to a heteroatom or a carbon atom, and where the N and / or S heteroatoms can also be optionally oxidized to different oxidation states; R² is selected from phenyl, naphthyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinolinyl, or isoquinolinyl, each of which is unsubstituted or substituted by 1 to 5 substituents independently selected from halogen, cyano, nitro, C₁₋₈ alkyl, C₁₋₈ haloalkyl, C₁₋₈ hydroxyalkyl, hydroxyl, C₁₋₈ alkoxy, C₁₋₈ alkoxy-C₁₋₈ alkyl, amino, C₁₋₈ N-alkyl-amino, C₁₋₈ N,N-dialkyl-amino, C₁₋₈ alkyl-carbonyl, haloalkyl C₁₋₈-carbonyl, C₁₋₈-hydroxyalkyl or C₁₋₈-alkyl alkoxy; R³ is selected from H, C₁₋₄ alkyl, or C₁₋₄ haloalkyl; ym is selected from 0 or 1.;

Claims

1. Un compuesto caracterizado porque se selecciona a partir del grupo que consiste en: {(S)-3-[6-(6-metoxi-5-metil-piridin-3-il)-5,6,7,8-tetrahidro-pirido-[4,3-d]-pirimidin-4-iloxi]-pirrolidin-1-il}-(tetrahidro-piran-4-il)-metanona; {(S)-3-[6-(6-metoxi-5-metil-piridin-3-il)-5,6,7,8-tetrahidro-pirido-[4,3-d]-pirimidin-4-iloxi]-pirrolidin-1-il}-(1-metil-1H-imidazol-4-il)-metanona; (S)-(3-(6-(6-methoxy-5-(trifluoro-methyl)-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido-[4,3-d]-pyrimidin-4-yl-amino)-pyrrolidin-1-yl)-(tetrahydro-2H-pyran-4-yl)-methanone; (S)-1-(3-(6-(6-methoxy-5-methyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido-[4,3-d]-pyrimidin-4-yl-amino)-pyrrolidin-1-yl)-propan-1-one; 1-{(S)-3-[6-(6-methoxy-5-trifluoromethyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-ylamino]-pyrrolidin-1-yl}-propan-1-one; y / o a tautomer y / o an N-oxide y / o a pharmaceutically acceptable salt of the same. Siguen 3 Reivindicaciones