US 2009/0221600 A1 · PYRIDO-PYRIDIMIDINE DERIVATIVES USEFUL AS ANTIINFLAMMATORY AGENTS

Abstract

Provided are novel pyrido-pyrimidine derivatives, having the structure of Formula (I): which can be used as anti-inflammatory agents. Also provided are pharmaceutical compositions comprising one or more pyrido-pyrimidine derivatives, as well as methods of treating autoimmune diseases, inflammation or associated pathologies, including for example, sepsis, rheumatoid arthritis, inflammatory bowel disease, type-1 diabetes, asthma, chronic obstructive pulmonary disorder, organ transplant rejection and psoriasis, comprising administering such compounds or pharmaceutical compositions comprising them.

Claims6

Dependent claims

A compound having the structure of Formula I:

or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, ester, enantiomer, diastereomer, N-oxide, polymorph or metabolite thereof, wherein
R1 is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl, heteroaryl, heterocyclyl, heteroarylalkyl or heterocyclylalkyl;
R2 is oxygen, sulphur —NH, —N-acyl, —N(CN), —N(NO2), —C(R3)2 or —CH(NO2);
—
represents a single bond or a double bond;
R3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, heteroarylalkyl or heterocyclylalkyl;
R4 cycloalkyl or heterocyclyl;
and
Het is heterocyclyl.

6 more elements

A compound selected from:

tert-Butyl 4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxylate (Compound No. 1),
Hydrochloride salt of 6-(2-methylphenyl)-2-(piperidin-4-ylamino)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 2),
2-[(1-Acetylpiperidin-4-yl)amino]-6-(2-methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 3),
6-(2-Methylphenyl)-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 4),
2-[(1-Benzoylpiperidin-4-yl)amino]-6-(2-methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 5),
N-Isopropyl-4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxamide (Compound No. 6),
N-(4-Fluorophenyl)-4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxamide (Compound No. 7),
2-{[1-(Ethylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 8),
2-[(1-Benzyl-piperidin-4-yl)amino]-6-(2-methyl-phenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 9),
N-(4-Fluorophenyl)-4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carbothioamide (Compound No. 10),
Methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-[4-(trifluoromethyl)phenyl]piperidine-1-carboxamide (Compound No. 11),
6-(2-Methylphenyl)-2-[(1-methylpiperidin-4-yl)amino]-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 12),
6-(2-Methylphenyl)-2-[(4-methylpiperazin-1-yl)amino]-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 13),
2-{[1-(Isopropylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 14),
tert-Butyl 4-{[6-(2-chlorophenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxylate (Compound No. 15),
6-(2-Methylphenyl)-2-(piperidin-1-ylamino)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 16),
2-(Cyclobutylamino)-6-(2-methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 17),
4-{[6-(2-Methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-propylpiperidine-1-carboxamide (Compound No. 18),
N-[(1S)-1,2-Dimethylpropyl]-4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxamide-(Compound No. 19),
N-Cyclohexyl-4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxamide (Compound No. 20),
2-{[1-(4-Fluorobenzoyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 21),
N-(Cyclopentylmethyl)-4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxamide (Compound No. 22),
4-{[6-(2-Methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-(1,1,3,3-tetramethylbutyl)piperidine-1-carboxamide (Compound No. 23),
4-{[6-(2-Methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-octylpiperidine-1-carboxamide (Compound No. 24),
N-Cyclopentyl-4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxamide (Compound No. 25),
N-Isopropyl-4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carbothioamide (Compound No. 26),
4-{[6-(2-Methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-octylpiperidine-1-carbothioamide (Compound No. 27),
N-tert-Butyl-4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carbothioamide (Compound No. 28),
6-(2-Methylphenyl)-2-[(1-pyrimidin-2-ylpiperidin-4-yl)amino]-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 29),
N-Cyclopropyl-4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxamide (Compound No. 30),
N-[(1R)-1-Cyclohexylethyl]-4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxamide (Compound No. 31),
2-{[1-(Cyclopentylcarbonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 32),
6-(2-Methylphenyl)-2-{[1-(pyrrolidin-1-ylcarbonyl)piperidin-4-yl]amino}-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 33),
6-(2-Methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 34),
6-(2-Methylphenyl)-2-[(1,2,2,6,6-pentamethylpiperidin-4-yl)amino]-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 35),
tert-Butyl 4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydrofuran-3-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxylate (Compound No. 36),
N-Isopropyl-4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydrofuran-3-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxamide (Compound No. 37),
6-(2-Methylphenyl)-7-oxo-2-{[1-(pyrrolidin-1-ylcarbonyl)piperidin-4-yl]amino}-1-(tetrahydrofuran-3-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-1-ium (Compound No. 38),
2-{[1-(Ethylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-7-oxo-1-(tetrahydrofuran-3-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-1-ium (Compound No. 39),
6-(2-Methylphenyl)-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}-8-(tetrahydrofuran-3-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 40),
N-Cyclopropyl-4-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydrofuran-3-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxamide (Compound No. 41),
6-(2-Methylphenyl)-2-{[(3S)-1-(methylsulfonyl)pyrrolidin-3-yl]amino}-8-(tetrahydrofuran-3-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 42),
tert-Butyl 4-({6-(2-methylphenyl)-7-oxo-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxylate (Compound No. 43),
6-(2-Methylphenyl)-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}-8-[(3S)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 44),
N-Isopropyl-4-({6-(2-methylphenyl)-7-oxo-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxamide (Compound No. 45),
6-(2-Methylphenyl)-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}-8-[(3R)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 46),
N-Isopropyl-4-({6-(2-methylphenyl)-7-oxo-8-[(3R)-tetrahydrofuran-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxamide (Compound No. 47),
tert-Butyl 4-({6-(2-methylphenyl)-7-oxo-8-[(3R)-tetrahydrofuran-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxylate (Compound No. 48),
Hydrochloride salt of 6-(2-methylphenyl)-2-(piperidin-4-ylamino)-8-[(3R)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 49),
Hydrochloride salt 6-(2-methylphenyl)-2-(piperidin-4-ylamino)-8-[(3S)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 50),
2-{([1-(Ethylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-[(3S)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 51),
N-Cyclopropyl-4-({6-(2-methylphenyl)-7-oxo-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxamide (Compound No. 52),
N-Cyclopropyl-4-({6-(2-methylphenyl)-7-oxo-8-[(3R)-tetrahydrofuran-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxamide (Compound No. 53),
2-[(1-Benzylpiperidin-4-yl)amino]-6-(2-methylphenyl)-8-[(3R)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 54),
2-(Cyclobutylamino)-6-(2-methylphenyl)-8-[(3R)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 55),
2-(Cyclopropylamino)-6-(2-methylphenyl)-8-[(3R)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 56),
2-{[1-(Ethylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-[(3R)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 57),
2-[(1-Acetylpiperidin-4-yl)amino]-6-(2-methylphenyl)-8-[(3R)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 58),
2-{[1-(4-Fluorobenzoyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-[(3R)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 59),
2-{[1-(Cyclopropylcarbonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-[(3R)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 60),
2-{[1-(Cyclopropylcarbonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-[(3S)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 61),
2-{[1-(Cyclopentylcarbonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-[(3S)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 62),
2-{[1-(Cyclopentylcarbonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-[(3R)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 63),
2-[(1-Benzoylpiperidin-4-yl)amino]-6-(2-methylphenyl)-8-[(3S)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 64),
2-[(1-Benzoylpiperidin-4-yl)amino]-6-(2-methylphenyl)-8-[(3R)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 65),
2-{[1-(4-Fluorobenzoyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-[(3S)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 66),
N-(4-Fluorophenyl)-4-({6-(2-methylphenyl)-7-oxo-8-[(3R)-tetrahydrofuran-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxamide (Compound No. 67),
2-[(1-Acetylpiperidin-4-yl)amino]-6-(2-methylphenyl)-8-[(3S)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 68),
N-(4-Fluorophenyl)-4-({6-(2-methylphenyl)-7-oxo-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxamide (Compound No. 69),
tert-Butyl (3S)-3-({6-(2-methylphenyl)-7-oxo-8-[(3R)-tetrahydrofuran-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxylate (Compound No. 70),
(3S)—N-Isopropyl-3-({6-(2-methylphenyl)-7-oxo-8-[(3R)-tetrahydrofuran-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxamide (Compound No. 71)
tert-Butyl (3S)-3-({6-(2-methylphenyl)-7-oxo-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxylate (Compound No. 72),
tert-Butyl (3R)-3-({6-(2-methylphenyl)-7-oxo-8-[(3R)-tetrahydrofuran-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxylate (Compound No. 73),
(3R)—N-Isopropyl-3-({6-(2-methylphenyl)-7-oxo-8-[(3R)-tetrahydrofuran-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxamide (Compound No. 74),
(3S)—N-Isopropyl-3-({6-(2-methylphenyl)-7-oxo-8-[(3S)-tetrahydrofuran-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxamide (Compound No. 75),
6-(2-Methylphenyl)-2-{[(3S)-1-(methylsulfonyl)piperidin-3-yl]amino}-8-[(3S)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 76),
6-(2-Methylphenyl)-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}-8-[(3S)-1-(methylsulfonyl)pyrrolidin-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 77),
6-(2-Methylphenyl)-2-{[1-(methylsulfonylpiperidin-4-yl]amino}-8-[(3S)-1-(methylsulfonyl)pyrrolidin-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 78),
tert-Butyl 4-({6-(2-methylphenyl)-7-oxo-8-[(3S)-pyrrolidin-3-yl]-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxylate (Compound No. 79)
4-({8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)-N-isopropylpiperidine-1-carboxamide (Compound No. 80),
Hydrochloride salt of 8-[(3S)-1-acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-2-(piperidin-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 81),
tert-Butyl (3S)-3-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}pyrrolidine-1-carboxylate (Compound No. 82),
(3S)—N-Isopropyl-3-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}pyrrolidine-1-carboxamide (Compound No. 83),
(3S)—N-Isopropyl-3-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}pyrrolidine-1-carbothioamide (Compound No. 84),
6-(2-Methylphenyl)-2-{[(3S)-1-(methylsulfonyl)pyrrolidin-3-yl]amino}-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 85),
2-{[(3S)-1-(Ethylsulfonyl)pyrrolidin-3-yl]amino}-6-(2-methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 86),
2-{[(3S)-1-Acetylpyrrolidin-3-yl]amino}-6-(2-methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 87),
(3S)—N-Cyclopropyl-3-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}pyrrolidine-1-carboxamide (Compound No. 88),
(3S)—N-Butyl-3-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}pyrrolidine-1-carboxamide (Compound No. 90),
(3S)—N-Cyclopentyl-3-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}pyrrolidine-1-carboxamide (Compound No. 91),
(3S)—N-[(1S)-1,2-Dimethylpropyl]-3-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}pyrrolidine-1-carboxamide (Compound No. 92),
2-{[(3R)-1-Benzylpyrrolidin-3-yl]amino}-6-(2-methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 93),
2-{[(3S)-1-Benzylpyrrolidin-3-yl]amino}-6-(2-methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 94),
(3S)—N-Cyclohexyl-3-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}pyrrolidine-1-carboxamide (Compound No. 95),
(3S)-3-{[6-(2-Methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-octylpyrrolidine-1-carboxamide (Compound No. 96),
2-{[(3S)-1-(Cyclopropylcarbonyl)pyrrolidin-3-yl]amino}-6-(2-methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 97),
2-{[(3S)-1-(Cyclopentylcarbonyl)pyrrolidin-3-yl]amino}-6-(2-methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 98),
6-(2-Methylphenyl)-2-{[(3S)-1-pyrimidin-2-yl-pyrrolidin-3-yl]amino}-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 99)
(3S)—N-[(1R)-1-Cyclohexylethyl]-3-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydro-2H-pyran-4-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}pyrrolidine-1-carboxamide (Compound No. 100),
6-(2-Methylphenyl)-2-{[(3S)-1-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]amino}-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 101),
2-{[(3S)-1-(Cyclopentylacetyl)pyrrolidin-3-yl]amino}-6-(2-methylphenyl)-8-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 102),
tert-Butyl (3S)-3-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydrofuran-3-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}pyrrolidine-1-carboxylate (Compound No. 103),
tert-Butyl 4-({8-[(3S)-1-benzylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxylate (Compound No. 104),
(3S)—N-Isopropyl-3-{[6-(2-methylphenyl)-7-oxo-8-(tetrahydrofuran-3-yl)-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}pyrrolidine-1-carboxamide (Compound No. 105),
tert-Butyl 4-{[8-(1-benzylpiperidin-4-yl)-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxylate (Compound No. 106),
tert -Butyl 4-{[6-(2-methylphenyl)-8-(1-methylpiperidin-4-yl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxylate (Compound No. 107)
8-(1-Benzylpiperidin-4-yl)-6-(2-methylphenyl)-2-[(1-methylpiperidin-4-yl)amino]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 108),
8-(1-Benzylpiperidin-4-yl)-2-(cyclobutylamino)-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 109),
tert-Butyl (3S)-3-{[8-(1-benzylpiperidin-4-yl)-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}pyrrolidine-1-carboxylate (Compound No. 110),
(3S)-3-{[8-(1-Benzylpiperidin-4-yl)-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-isopropylpyrrolidine-1-carboxamide (Compound No. 111),
Hydrochloride salt of S-(1-benzylpiperidin-4-yl)-6-(2-methylphenyl)-2-(piperidin-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 112),
Hydrochloride salt of 6-(2-methylphenyl)-8-(1-methylpiperidin-4-yl)-2-(piperidin-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 113),
4-{[8-(1-Benzylpiperidin-4-yl)-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-isopropylpiperidine-1-carboxamide (Compound No. 114),
4-{[8-(1-Benzylpiperidin-4-yl)-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-cyclohexylpiperidine-1-carboxamide (Compound No. 115),
4-{[8-(1-Benzylpiperidin-4-yl)-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-cyclopentylpiperidine-1-carboxamide (Compound No. 116),
4-{[8-(1-Benzylpiperidin-4-yl)-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-isobutylpiperidine-1-carboxamide (Compound No. 117),
4-{[8-(1-Benzylpiperidin-4-yl)-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-[(1R)-1-cyclohexylethyl]piperidine-1-carboxamide (Compound No. 118),
N-Isopropyl-4-{[6-(2-methylphenyl)-8-(1-methylpiperidin-4-yl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxamide (Compound No. 119),
N-Cyclopropyl-4-{[6-(2-methylphenyl)-8-(1-methylpiperidin-4-yl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxamide (Compound No. 120),
8-(1-Benzylpiperidin-4-yl)-2-{[1-(cyclopentylacetyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 121),
8-(1-Benzylpiperidin-4-yl)-2-{[1-(cyclopropylcarbonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 122),
8-(1-Benzylpiperidin-4-yl)-6-(2-methylphenyl)-2-{[1-(phenylsulfonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 123),
8-(1-Benzylpiperidin-4-yl)-6-(2-methylphenyl)-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 124),
8-(1-Benzylpiperidin-4-yl)-2-{[1-(ethylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound no. 125),
6-(2-Methylphenyl)-8-(1-methylpiperidin-4-yl)-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 126),
2-{[1-(Ethylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-(1-methylpiperidin-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 127),
2-{[1-(Isopropylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-(1-methylpiperidin-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 128),
6-(2-Methylphenyl)-8-(1-methylpiperidin-4-yl)-2-{[1-(pyrrolidin-1-ylcarbonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 129),
2-[(1-Benzoylpiperidin-4-yl)amino]-6-(2-methylphenyl)-8-(1-methylpiperidin-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 130),
2-[(1-Benzoylpiperidin-4-ylamino]-6-(2-methylphenyl)-8-(1-methylpiperidin-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 130),
tert-Butyl 4-{[6-(2-methylphenyl)-7-oxo-8-piperidin-4-yl-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxylate (Compound No. 131),
6-(2-Methylphenyl)-8-piperidin-4-yl-2-(piperidin-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 132),
N-Isopropyl-4-{[6-(2-methylphenyl)-7-oxo-8-piperidin-4-yl-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxamide (Compound No. 133),
tert-Butyl 4-{[8-{1-[(isopropylamino)carbonyl]piperidin-4-yl}-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxylate (Compound No. 134),
Hydrochloride salt of N-isopropyl-4-[6-(2-methylphenyl)-7-oxo-2-(piperidin-4-ylamino)pyrido[2,3-d]pyrimidin-8(7H)-yl]piperidine-1-carboxamide (Compound No. 135),
N-Isopropyl-4-[2-({1-[(isopropylamino)carbonyl]piperidin-4-yl}amino)-6-(2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]piperidine-1-carboxamide (Compound No. 136),
4-[2-({1-[(Cyclopropylamino)carbonyl]piperidin-4-yl}amino)-6-(2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]-N-isopropylpiperidine-1-carboxamide (Compound No. 137),
4-[2-({1-[(tert-Butylamino)carbonyl]piperidin-4-yl}amino)-6-(2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]-N-isopropylpiperidine-1-carboxamide (Compound No. 138),
4-[2-({1-[(Cyclohexylamino)carbonyl]piperidin-4-yl}amino)-6-(2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]-N-isopropylpiperidine-1-carboxamide (Compound No. 139),
N-Isopropyl-4-[6-(2-methylphenyl)-2-{[1-(morpholin-4-ylcarbonyl)piperidin-4-yl]amino}-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]piperidine-1-carboxamide (Compound No. 140),
4-[2-{[1-(4-Fluorobenzoyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]-N-isopropylpiperidine-1-carboxamide (Compound No. 141),
N-Isopropyl-4-[6-(2-methylphenyl)-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]piperidine-1-carboxamide (Compound No. 142),
4-[2-{[1-(Ethylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]-N-isopropylpiperidine-1-carboxamide (Compound No. 143),
N-Isopropyl-4-[2-{[1-(isopropylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]piperidine-1-carboxamide (Compound No. 144),
4-[2-{[1-(Cyclopropylcarbonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]-N-isopropylpiperidine-1-carboxamide (Compound No. 145),
4-[2-[(1-Benzoylpiperidin-4-yl)amino]-6-(2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]-N-isopropylpiperidine-1-carboxamide (Compound No. 146),
4-[2-[(1-Acetylpiperidin-4-yl)amino]-6-(2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]-N-isopropylpiperidine-1-carboxamide (Compound No. 147),
N-Isopropyl-4-[6-(2-methylphenyl)-2-[(1-methylpiperidin-4-yl)amino]-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]piperidine-1-carboxamide (Compound No. 148),
4-[2-[(1-Benzylpiperidin-4-yl)amino]-6-(2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]-N-isopropylpiperidine-1-carboxamide (Compound No. 149),
8-(1-Acetylpiperidin-4-yl)-2-[(1-acetylpiperidin-4-yl)amino]-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 150),
4-[2-{[1-(4-Fluorobenzoyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]-N-isopropylpiperidine-1-carboxamide (Compound No. 151),
tert-Butyl 4-({6-(2-methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxylate (Compound No. 152),
Hydrochloride salt of 6-(2-methylphenyl)-8-[1-(methylsulfonylpiperidin-4-yl]-2-(piperidin-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 153),
N-Isopropyl-4-({6-(2-methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxamide (Compound No. 154),
N-(tert-Butyl)-4-({6-(2-methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxamide (Compound No. 155),
N-Cyclohexyl-4-({6-(2-methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxamide (Compound No. 156),
N-(4-Fluorophenyl)-4-({6-(2-methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxamide (Compound No. 157),
6-(2-Methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]-2-{[1-(morpholin-4-ylcarbonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 158),
6-(2-Methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 159),
2-{[1-(Ethylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 160),
2-{[1-(Isopropylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 161),
2-{[1-(Cyclopropylcarbonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound 162),
2-[(1-Acetylpiperidin-4-yl)amino]-6-(2-methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 163),
2-[(1-Benzoylpiperidin-4-yl)amino]-6-(2-methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 164),
2-{[1-(4-Fluorobenzoyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 165),
tert-Butyl 4-{[8-(1-acetylpiperidin-4-yl)-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxylate (Compound No. 166),
8-(1-Acetylpiperidin-4-yl)-6-(2-methylphenyl)-2-(piperidin-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 167),
4-{[8-(1-Acetylpiperidin-4-yl)-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-isopropylpiperidine-1-carboxamide (Compound No. 168),
4-{[8-(1-Acetylpiperidin-4-yl)-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-cyclopropylpiperidine-1-carboxamide (Compound No. 169),
4-{[8-(1-Acetylpiperidin-4-yl)-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-(tert-butylpiperidine-1-carboxamide (Compound No. 170),
4-{[8-(1-Acetylpiperidin-4-yl)-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-cyclohexylpiperidine-1-carboxamide (Compound No. 171),
4-{[8-(1-Acetylpiperidin-4-yl)-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-(4-fluorophenyl)piperidine-1-carboxamide (Compound No. 172),
8-(1-Acetylpiperidin-4-yl)-6-(2-methylphenyl)-2-{[1-(morpholin-4-ylcarbonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 173),
8-(1-Acetylpiperidin-4-yl)-6-(2-methylphenyl)-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 174),
8-(1-Acetylpiperidin-4-yl)-2-{[1-(ethylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 175),
8-(1-Acetylpiperidin-4-yl)-2-{[1-(isopropylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 176),
8-(1-Acetylpiperidin-4-yl)-2-{[1-(cyclopropylcarbonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 177),
8-(1-Acetylpiperidin-4-yl)-2-{[1-(4-fluorobenzoyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 178),
tert-Butyl 4-{[8-[(3S)-1-acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxylate (Compound No. 179),
Hydrochloride salt of 8-[(3S)-1-acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-2-(piperidin-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 180),
8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 181),
2-[(1-Acetylpiperidin-4-yl)amino]-6-(2-methylphenyl)-8-(1-methylpiperidin-4-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 182),
Hydrochloride salt of 6-(2-methylphenyl)-8-[(3S)-1-(methylsulfonyl)pyrrolidin-3-yl]-2-(piperidin-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 183),
tert-Butyl 4-{[8-[(3R)-1-acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}piperidine-1-carboxylate (Compound No. 184),
Hydrochloride salt of 6-(2-methylphenyl)-2-[(3S)-pyrrolidin-3-ylamino]-8-(tetrahydrofuran-3-yl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 185),
Hydrochloride salt of 6-(2-methylphenyl)-2-[(3S)-piperidin-3-ylamino]-8-[(3R)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 186),
Hydrochloride salt of 6-(2-methylphenyl)-2-[(3S)-piperidin-3-ylamino]-8-[(3S)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 187),
Hydrochloride salt of 6-(2-methylphenyl)-2-[(3R)-piperidin-3-ylamino]-8-[(3R)-tetrahydrofuran-3-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 188),
4-[2-[(1-{[(4-Fluorophenyl)amino]carbonyl}piperidin-4-yl)amino]-6-(2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]-N-isopropylpiperidine-1-carboxamide (Compound No. 189),
4-{[8-{1-[(Isopropylamino)carbonyl]piperidin-4-yl}-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-morpholin-4-ylpiperidine-1-carboxamide (Compound No. 190),
4-[2-{[1-(2,2-Dimethylpropanoyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]-N-isopropylpiperidine-1-carboxamide (Compound No. 191),
8-[(3S)-1-Acetylpyrrolidin-3-yl]-2-[(1-benzylpiperidin-4-yl)amino]-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 192),
N-Cyclopropyl-4-({6-(2-methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)piperidine-1-carboxamide (Compound No. 193),
4-({6-(2-Methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl}amino)-N-morpholin-4-ylpiperidine-1-carboxamide (Compound No. 194),
2-{[1-(2,2-Dimethylpropanoyl)piperidin-4-yl]amino}-6-(2-methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 195),
6-(2-Methylphenyl)-2-[(1-methylpiperidin-4-yl)amino]-8-[1-(methylsulfonyl)piperidin-4-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 196),
2-[(1-Benzylpiperidin-4-yl)amino]-6-(2-methylphenyl)-8-[1-(methylsulfonyl)piperidin-4-yl]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 197),
8-(1-Acetylpiperidin-4-yl)-2-[(1-benzoylpiperidin-4-yl)amino]-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 198),
8-(1-Acetylpiperidin-4-yl)-2-{[1-(2,2-dimethylpropanoyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 199),
8-(1-Acetylpiperidin-4-yl)-6-(2-methylphenyl)-2-[(1-methylpiperidin-4-yl)amino]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 200),
8-(1-Acetylpiperidin-4-yl)-2-[(1-benzylpiperidin-4-yl)amino]-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 201),
4-{[8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-cyclopropylpiperidine-1-carboxamide (Compound No. 202),
4-{[8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-(tert-butyl)piperidine-1-carboxamide (Compound No. 203),
4-{[8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-cyclohexylpiperidine-1-carboxamide (Compound No. 204),
4-{[8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-(4-fluorophenyl)piperidine-1-carboxamide (Compound No. 205),
4-{[8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-morpholin-4-ylpiperidine-1-carboxamide (Compound No. 206),
8-[(3S)-1-Acetylpyrrolidin-3-yl]-2-{[1-(ethylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 207),
8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-2-{[1-(propylsulfonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one ((Compound No. 208),
8-[(3R)-1-Acetylpyrrolidin-3-yl]-2-{[1-(cyclopropylcarbonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 209),
2-[(1-Acetylpiperidin-4-yl)amino]-8-[(3R)-1-acetylpyrrolidin-3-yl]-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 210),
8-[(3R)-1-Acetylpyrrolidin-3-yl]-2-[(1-benzoylpiperidin-4-yl)amino]-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 211),
8-[(3R)-1-Acetylpyrrolidin-3-yl]-2-{[1-(4-fluorobenzoyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 212),
8-[(3R)-1-Acetylpyrrolidin-3-yl]-2-{[1-(2,2-dimethylpropanoyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 213),
8-[(3R)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-2-[(1-methylpiperidin-4-yl)amino]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 214),
8-[(3R)-1-Acetylpyrrolidin-3-yl]-2-[(1-benzylpiperidin-4-yl)amino]-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 215),
8-[(3S)-1-Acetylpyrrolidin-3-yl]-2-{[1-(2,2-dimethylpropanoyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 216),
8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-2-[(1-methylpiperidin-4-yl)amino]pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 217),
4-{[8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-isopropylpiperidine-1-carboxamide (Compound No. 218),
4-{[8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-cyclopropylpiperidine-1-carboxamide (Compound No. 219),
4-{[8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-(tert-butyl)piperidine-1-carboxamide (Compound No. 220),
4-{[8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-cyclohexylpiperidine-1-carboxamide (Compound No. 221)
4-{[8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-(4-fluorophenyl)piperidine-1-carboxamide (Compound No. 222),
4-{[8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}-N-morpholin-4-ylpiperidine-1-carboxamide (Compound No. 223),
8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 224),
8-[(3S)-1-Acetylpyrrolidin-3-yl]-2-{[1-(ethylsulfonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 225),
8-[(3S)-1-Acetylpyrrolidin-3-yl]-6-(2-methylphenyl)-2-{[1-(propylsulfonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 226),
8-[(3S)-1-Acetylpyrrolidin-3-yl]-2-{[1-(cyclopropylcarbonyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 227),
2-[(1-Acetylpiperidin-4-yl)amino]-8-[(3S)-1-acetylpyrrolidin-3-yl]-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 228),
8-[(3S)-1-Acetylpyrrolidin-3-yl]-2-[(1-benzoylpiperidin-4-yl)amino]-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 229),
8-[(3S)-1-Acetylpyrrolidin-3-yl]-2-{[1-(4-fluorobenzoyl)piperidin-4-yl]amino}-6-(2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one (Compound No. 230).

227 more elements

Dependencies are inferred from the claim text.

Pyrido-pyridimidine derivatives useful as antiinflammatory agents

Life of this patent

Pyrido-pyridimidine derivatives useful as antiinflammatory agents

Life of this patent

Abstract

Claims6