Claims
- 1. A compound of formula XI
- 2. Compound of claim 1 wherein R is 6-indazolyl.
- 3. Compound of claim 1 wherein R is 1-oxo-2,3-dihydro-1H-isoindol-4-yl.
- 4. Compound of claim 1 wherein R is 2-oxo-2,3-dihydro-1H-benzoimidazol-5-yl.
- 5. Compound of claim 1 wherein R is 4-oxo-3,4-dihydro-quinazolin-6-yl.
- 6. Compound of claim 1 wherein R1 is selected from phenyl, tetrahydronaphthyl, indanyl, indenyl, naphthyl, cyclohexyl, isoxazolyl, pyrazolyl, thiazolyl, thiadiazolyl, thienyl, pyridyl, pyrimidinyl, pyridazinyl, 1,2-dihydroquinolyl, 1,2,3,4-tetrahydro-isoquinolyl, 1′,2′-dihydro-spiro[cyclopropane-1,3′-[3H]indol]-6′-yl, isoquinolyl, quinolyl, indolyl, isoindolyl, 2,3-dihydro-1H-indolyl, naphthyridinyl, 3,4-dihydro-[1,8]naphthyridinyl, 1,2,3,4-tetrahydro-[1,8]naphthyridinyl, quinozalinyl, benzo[d]isothiazolyl, 3,4-dihydro-quinazolinyl, 2,3,4,4a,9,9a-hexahydro-1H-3-aza-fluorenyl, 5,6,7-trihydro-1,2,4-triazolo[3,4-a]isoquinolyl, tetrahydroquinolinyl, indazolyl, 2,1,3-benzothiadiazolyl, benzodioxanyl, benzothienyl, benzofuryl, benzimidazolyl, dihydro-benzimidazolyl, benzoxazolyl and benzthiazolyl, where R1 is unsubstituted or substituted with one or more substituents selected from bromo, chloro, fluoro, iodo, nitro, amino, cyano, Boc-aminoethyl, hydroxy, oxo, fluorosulfonyl, methylsulfonyl, aminosulfonyl, 4-methylpiperazinylsulfonyl, cyclohexyl, phenyl, phenylmethyl, 4-pyridylmethyl, 4-morpholinylmethyl, 1-methylpiperazin-4-ylmethyl, 1-methylpiperazin-4-ylpropyl, morpholinylpropyl, piperidin-1-ylmethyl, 1-methylpiperidin-4-ylmethyl, 2-methyl-2-(1-methylpiperidin-4-yl)ethyl, 2-methyl-2-(4-pyrimidinyl)ethyl, 2-methyl-2-(5-methyloxadiazol-2-yl)ethyl, 2-methyl-2-(pyrazol-5-yl)ethyl, 2-methyl-2-(1-ethoxycarbonyl-1,2,3,6-tetrahydropyridin-4-yl)ethyl, morpholinylethyl, 1-(4-morpholinyl)-2,2-dimethylpropyl, 1-(4-morpholinyl)-2,2-dimethylethyl, piperidin-4-ylethyl, 1-Boc-piperidin-4-ylethyl, piperidin-1-ylethyl, 1-Boc-piperidin-4-ylethyl, piperidin-4-ylmethyl, 1-Boc-piperidin-4-ylmethyl, piperidin-4-ylpropyl, 1-Boc-piperidin-4-ylpropyl, piperidin-1-ylpropyl, pyrrolidin-1-ylpropyl, pyrrolidin-2-ylpropyl, 1-Boc-pyrrolidin-2-ylpropyl, 1-(pyrrolidin-1-yl)-2-methylpropyl, pyrrolidin-1-ylmethyl, pyrrolidin-2-ylmethyl, 1-Boc-pyrrolidin-2-ylmethyl, pyrrolidinylpropenyl, pyrrolidinylbutenyl, methylcarbonyl, Boc, piperidin-1-ylmethylcarbonyl, pyrrolidin-1-yl-carbonyl, 4-pyridylcarbonyl, 4-methylpiperazin-1-ylcarbonylethyl, CH3O—C(═O)—CH2—, methoxycarbonyl, aminomethylcarbonyl, dimethylaminomethylcarbonyl, methylsulfonylamino, dimethylaminomethylcarbonylamino, 1-pyrrolidinyl-CH2—C(═O)—NH—, 4-morpholinyl-CH2—C(═O)—NH—, 3-tetrahydrofuryl-O—C(═O)—NH—, cyclohexyl-N(CH3)—, (4-pyrimidinyl)amino, (2-methylthio-4-pyrimidinyl)amino, 3-ethoxycarbonyl-2-methyl-fur-5-yl, 4-methylpiperazin-1-yl, 4-methyl-1-piperidyl, 1-Boc-4-piperidyl, piperidin-4-yl, 1-methylpiperidin-4-yl, 1-methyl-(1,2,3,6-tetrahydropyridyl), imidazolyl, morpholinyl, 4-trifluoromethyl-1-piperidinyl, hydroxybutyl, methyl, ethyl, propyl, isopropyl, butyl, tert-butyl, sec-butyl, trifluoromethyl, pentafluoroethyl, nonafluorobutyl, dimethylaminopropyl, 1,1-di(trifluoromethyl)-1-hydroxymethyl, 1,1-di(trifluoromethyl)-1-(piperidinylethoxy)methyl, 1,1-di(trifluoromethyl)-1-(pyrrolidin-2-ylmethoxy)methyl, 1,1-di(trifluoromethyl)-1-(methoxyethoxyethoxy)methyl, 1-hydroxyethyl, 2-hydroxyethyl, trifluoromethoxy, 1-aminoethyl, 2-aminoethyl, 1-(N-isopropylamino)ethyl, 2-(N-isopropylamino)ethyl, 3-tetrahydrofuryloxy, dimethylaminoethoxy, 4-chlorophenoxy, phenyloxy, azetidin-3-ylmethoxy, 1-Boc-azetidin-3-ylmethoxy, 3-tetrahydrofurylmethoxy, pyrrolidin-2-ylmethoxy, 1-methylcarbonyl-pyrrolidin-2-ylmethoxy, 1-Boc-pyrrolidin-2-ylmethoxy, pyrrolidin-1-ylmethoxy, 1-methyl-pyrrolidin-2-ylmethoxy, 1-isopropyl-pyrrolidin-2-ylmethoxy, 1-Boc-piperdin-4-ylmethoxy, (1-pyrrolidinyl)ethoxy, piperdin-4-ylmethoxy, piperdin-3-ylmethoxy, 1-methylpiperdin-4-yloxy, methylsulfonylaminoethoxy, isopropoxy, methoxy and ethoxy; and pharmaceutically acceptable derivatives thereof.
- 7. Compound of claim 6 wherein R1 is selected from phenyl, 1,2,3,4-tetrahydroisoquinolyl, 2,3-dihydro-1H-indolyl, 1,2,3,4-tetrahydro-[1,8]naphthyridinyl, 1′,2′-dihydro-spiro[cyclopropane-1,3′-[3H]indol]-6′-yl, and tetrahydroquinolinyl, where R1 is unsubstituted or substituted with one or more substituents selected from chloro, oxo, methylsulfonyl, 2-methyl-2-(1-methylpiperidin-4-yl)ethyl, pyrrolidin-1-yl-carbonyl, methylsulfonylamino, dimethylaminomethylcarbonylamino, 1-pyrrolidinyl-CH2—C(═O)—NH—, 4-morpholinyl-CH2—C(═O)—NH—, 3-tetrahydrofuryl-O—C(═O)—NH—, methyl, tert-butyl, trifluoromethyl, pentafluoroethyl, 1,1-di(trifluoromethyl)-1-hydroxymethyl, 1,1-di(trifluoromethyl)-1-(pyrrolidin-2-ylmethoxy)methyl, 3-tetrahydrofuryloxy, 1-methylcarbonyl-pyrrolidin-2-ylmethoxy, 1-methyl-pyrrolidin-2-ylmethoxy, and methylsulfonylaminoethoxy; and pharmaceutically acceptable derivatives thereof.
- 8. Compound of claim 6 wherein R1 is substituted with one or more substituents selected from 2-methyl-2-(1-ethoxycarbonyl-1,2,3,6-tetrahydropyridin-4-yl)ethyl, 1-(4-morpholinyl)-2,2-dimethylethyl, pyrrolidin-1-yl-carbonyl, CH3O—C(═O)—CH2—, methylsulfonylamino, dimethylaminomethylcarbonylamino, 1-pyrrolidinyl-CH2—C(═O)—NH—, 4-morpholinyl-CH2—C(═O)—NH—, 3-tetrahydrofuryl-O—C(═O)—NH—, 1,1-di(trifluoromethyl)-1-(pyrrolidin-2-ylmethoxy)methyl, 3-tetrahydrofuryloxy, 1-methylcarbonyl-pyrrolidin-2-ylmethoxy, and methylsulfonylaminoethoxy; and pharmaceutically acceptable derivatives thereof.
- 9. Compound of claim 6 wherein R1 is phenyl substituted with one or more substituents selected from chloro, 2-methyl-2-(1-methylpiperidin-4-yl)ethyl, methylsulfonylamino, dimethylaminomethylcarbonylamino, 1-pyrrolidinyl-CH2—C(═O)—NH—, 4-morpholinyl-CH2—C(═O)—NH—, 3-tetrahydrofuryl-O—C(═O)—NH—, tert-butyl, trifluoromethyl, pentafluoroethyl, 1,1-di(trifluoromethyl)-1-hydroxymethyl, 1,1-di(trifluoromethyl)-1-(pyrrolidin-2-ylmethoxy)methyl, 3-tetrahydrofuryloxy, 1-methylcarbonyl-pyrrolidin-2-ylmethoxy, 1-methyl-pyrrolindin-2-ylmethoxy, and methylsulfonylaminoethoxy; and pharmaceutically acceptable derivatives thereof.
- 10. Compound of claim 6 wherein R1 is 4,4-dimethyl-3,4-dihydro-2-oxo-1H-quinolinyl; and pharmaceutically acceptable derivatives thereof.
- 11. Compound of claim 6 wherein R1 is 4,4-dimethyl-1,2,3,4-tetrahydro-1H-quinolinyl; and pharmaceutically acceptable derivatives thereof.
- 12. Compound of claim 6 wherein R1 is 4,4-dimethyl-3,4-dihydro-2-oxo-1H-[1,8]naphthyridinyl; and pharmaceutically acceptable derivatives thereof.
- 13. Compound of claim 6 wherein R1 is 3,3-dimethyl-2,3-dihydro-1H-indolyl optionally substituted with a substituent selected from pyrrolidin-1-yl-carbonyl, methylcarbonyl, and methylsulfonyl; and pharmaceutically acceptable derivatives thereof.
- 14. Compound of claim 6 wherein R1 is 4,4-dimethyl-1,2,3,4-tetrahydro-1H-isoquinolinyl.
- 15. Compound of claim 1 and pharmaceutically acceptable salts thereof selected from
N-(4,4-Dimethyl-2-oxo-1,2,3,4-tetrahydro-quinolin-7-yl)-2-(1H-indazol-6-ylamino)-nicotinamide; 2-(1H-Indazol-6-ylamino)-N-(3-((((2R)-1-methyl-2-pyrrolidinyl)methyl)oxy)-5-(trifluoromethyl)phenyl)-3-pyridinecarboxamide; N-(3-((((2R)-1-Acetyl-2-pyrrolidinyl)methyl)oxy)-5-(trifluoromethyl)phenyl)-2-(1H-indazol-6-ylamino)-3-pyridinecarboxamide; (3S)-Tetrahydro-3-furanyl 3-(((2-(1H-indazol-6-ylamino)-3-pyridinyl)carbonyl)amino)-5-(trifluoromethyl)phenylcarbamate; 2-(1H-Indazol-6-ylamino)-N-(3-((((2S)-1-(1-methylethyl)-2-pyrrolidinyl)methyl)oxy)-5-(trifluoromethyl)phenyl)-3-pyridinecarboxamide; 2-(1H-Indazol-6-ylamino)-N-(3-((methylsulfonyl)amino)-5-(trifluoromethyl)phenyl)-3-pyridinecarboxamide; N-(4-(1,1-Dimethylethyl)-3-((1-pyrrolidinylacetyl)amino)phenyl)-2-(1H-indazol-6-ylamino)-3-pyridinecarboxamide; N-(4-(1,1-Dimethylethyl)-3-((4-morpholinylacetyl)amino)phenyl)-2-(1H-indazol-6-ylamino)-3-pyridinecarboxamide; N-(5,5-Dimethyl-7-oxo-5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-2-(1H-indazol-6-ylamino)-nicotinamide; N-(4,4-Dimethyl-1,2,3,4-tetrahydro-isoquinolin-7-yl)-2-(2-oxo-2,3-dihydro-1H-benzoimidazol-5-ylamino)-nicotinamide; N-(4-tert-Butyl-phenyl)-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; 2-(1-Oxo-2,3-dihydro-1H-isoindol-4-ylamino)-N-(4-pentafluoroethyl-phenyl)-nicotinamide; N-{4-[1-Methyl-1-(1-methyl-piperidin-4-yl)-ethyl]-phenyl}-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; 2-(1H-Indazol-6-ylamino)-N-{4-[2,2,2-trifluoro-1-(pyrrolidin-2-ylmethoxy)-1-trifluoromethyl-ethyl]-phenyl}-nicotinamide; 2-(1-Oxo-2,3-dihydro-1H-isoindol-4-ylamino)-N-[4-(2,2,2-trifluoro-1-hydroxy-1-trifluoromethyl-ethyl)-phenyl]-nicotinamide; 2-(1-Oxo-2,3-dihydro-1H-isoindol-4-ylamino)-N-[3-(2,2,2-trifluoro-1-hydroxy-1-trifluoromethyl-ethyl)-phenyl]-nicotinamide; N-(4-(1,1-Dimethylethyl)-3-((N,N-dimethylglycyl)amino)phenyl)-2-(1H-indazol-6-ylamino)-3-pyridinecarboxamide; 2-(1H-indazol-6-ylamino)-N-(3-((((2S)-1-methyl-2-pyrrolidinyl)methyl)oxy)-4-(trifluoromethyl)phenyl)-3-pyridinecarboxamide; N-(3,3-dimethyl-1-(methylsulfonyl)-2,3-dihydro-1H-indol-6-yl)-2-(1H-indazol-6-ylamino)-3-pyridinecarboxamide; N-(4,4-Dimethyl-1,2,3,4-tetrahydro-isoquinolin-7-yl)-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; N-(4,4-Dimethyl-1,2,3,4-tetrahydro-isoquinolin-7-yl)-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; and N-[3,3-Dimethyl-1-(pyrrolidine-2-carbonyl)-2,3-dihydro-1H-indol-6-yl]-2-(1H-indazol-6-ylamino)-nicotinamide.
- 16. A compound and pharmaceutically acceptable salts thereof selected from
2-(1H-Indazol-6-ylamino)-N-(3-((((2R)-1-methyl-2-pyrrolidinyl)methyl)oxy)-5-(trifluoromethyl)phenyl)-3-pyridinecarboxamide; 2-(1H-Indazol-6-ylamino)-N-(3-(((2S)-tetrahydro-2-furanylmethyl)oxy)-5-(trifluoromethyl)phenyl)-3-pyridinecsarboxamide; 2-(1H-Indazol-6-ylamino)-N-(3-(((2R)-tetrahydro-2-furanylmethyl)oxy)-5-(trifluoromethyl)phenyl)-3-pyridinecsarboxamide; 2-(1H-Indazol-6-ylamino)-N-(3-((3R)-tetrahydro-3-furanyloxy)-5-(trifluoromethyl)phenyl)-3-pyridinecarboxamide; N-(3-((((2R)-1-Acetyl-2-pyrrolidinyl)methyl)oxy)-5-(trifluoromethyl)phenyl)-2-(1H-indazol-6-ylamino)-3-pyridinecarboxamide; (3S)-Tetrahydro-3-furanyl 3-(((2-(1H-indazol-6-ylamino)-3-pyridinyl)carbonyl)amino)-5-(trifluoromethyl)phenylcarbamate; 2-(1H-Indazol-6-ylamino)-N-(3-((2-((methylsulfonyl)amino)ethyl)oxy)-5-(trifluoromethyl)phenyl)-3-pyridinecarboxamide; 2-(1H-Indazol-6-ylamino)-N-(3-((((2S)-1-(1-methylethyl)-2-pyrrolidinyl)methyl)oxy)-5-(trifluoromethyl)phenyl)-3-pyridinecarboxamide; N-(2-Oxo-3,3-bis(trifluoromethyl)-2,3-dihydro-1H-indol-6-yl)-2-((1-oxo-2,3-dihydro-1H-isoindol-4-yl)amino)-3-pyridinecarboxamide; N-(3-((((2R)-1-Methyl-2-pyrrolidinyl)methyl)oxy)-4-(trifluoromethyl)phenyl)-2-((1-oxo-2,3-dihydro-1H-isoindol-4-yl)amino)-3-pyridinecarboxamide; 2-(1H-Indazol-6-ylamino)-N-(3-((methylsulfonyl)amino)-5-(trifluoromethyl)phenyl)-3-pyridinecarboxamide; N-(4-(1,1-Dimethylethyl)-3-((1-pyrrolidinylacetyl)amino)phenyl)-2-(1H-indazol-6-ylamino)-3-pyridinecarboxamide; N-(4-(1,1-Dimethylethyl)-3-((4-morpholinylacetyl)amino)phenyl)-2-(1H-indazol-6-ylamino)-3-pyridinecarboxamide; 4-((3-((3-(2-(1-Acetyl-2-pyrrolidinyl)ethyl)-5-(trifluoromethyl)phenyl)acetyl)-2-pyridinyl)amino)-2,3-dihydro-1H-isoindol-1-one; N-[3-Chloro-5-(2-dimethylamino-acetylamino)-phenyl]-2-(1H-indazol-6-ylamino)-nicotinamide; N-{4-[1-Methyl-1-(1-methyl-piperidin-4-yl)-ethyl]-phenyl}-2-(4-oxo-3,4-dihydro-quinazolin-6-ylamino)-nicotinamide; N-{4-[1-Methyl-1-(1-methyl-piperidin-4-yl)-ethyl]-phenyl}-2-(2-oxo-2,3-dihydro-1H-indol-6-ylamino)-nicotinamide; N-(5,5-Dimethyl-7-oxo-5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-2-(1H-indazol-6-ylamino)-nicotinamide; N-(4,4-Dimethyl-1,2,3,4-tetrahydro-isoquinolin-7-yl)-2-(2-oxo-2,3-dihydro-1H-benzoimidazol-5-ylamino)-nicotinamide; N-(1-Acetyl-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-2-(2-oxo-2,3-dihydro-1H-benzoimidazol-5-ylamino)-nicotinamide; N-(3,3-Dimethyl-2,3-dihydro-1H-indol-6-yl)-2-(2-oxo-2,3-dihydro-1H-benzoimidazol-5-ylamino)-nicotinamide; N-{4-[1-Methyl-1-(1-methyl-piperidin-4-yl)-ethyl]-phenyl}-2-(2-oxo-2,3-dihydro-1H-benzoimidazol-5-ylamino)-nicotinamide; 2-(2-Oxo-2,3-dihydro-1H-benzoimidazol-5-ylamino)-N-(3-trifluoromethyl-phenyl)-nicotinamide; N-[3-(1-Methyl-pyrrolidin-2-ylmethoxy)-5-trifluoromethyl-phenyl]-2-(2-oxo-2,3-dihydro-1H-benzoimidazol-5-ylamino)-nicotinamide; N-(4-tert-Butyl-phenyl)-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; 2-(1-Oxo-2,3-dihydro-1H-isoindol-4-ylamino)-N-(4-trifluoromethyl-phenyl)-nicotinamide; 2-(1-Oxo-2,3-dihydro-1H-isoindol-4-ylamino)-N-(4-pentafluoroethyl-phenyl)-nicotinamide; N-{4-[1-Methyl-1-(1-methyl-piperidin-4-yl)-ethyl]-phenyl}-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; 2-(1-Oxo-2,3-dihydro-1H-isoindol-4-ylamino)-N-(3-trifluoromethyl-phenyl)-nicotinamide; 2-(1H-Indazol-6-ylamino)-N-{3-[2,2,2-trifluoro-1-(pyrrolidin-2-ylmethoxy)-1-trifluoromethyl-ethyl]-phenyl}-nicotinamide; 2-[2,2,2-Trifluoro-1-(4-{[2-(1H-indazol-6-ylamino)-pyridine-3-carbonyl]-amino}-phenyl)-1-trifluoromethyl-ethoxymethyl]-pyrrolidine-1-carboxylic acid tert-butyl ester; 2-(1H-Indazol-6-ylamino)-N-{4-[2,2,2-trifluoro-1-(pyrrolidin-2-ylmethoxy)-1-trifluoromethyl-ethyl]-phenyl}-nicotinamide; 2-(1-Oxo-2,3-dihydro-1H-isoindol-4-ylamino)-N-[4-(2,2,2-trifluoro-1-hydroxy-1-trifluoromethyl-ethyl)-phenyl]-nicotinamide; 2-(1-Oxo-2,3-dihydro-1H-isoindol-4-ylamino)-N-[3-(2,2,2-trifluoro-1-hydroxy-1-trifluoromethyl-ethyl)-phenyl]-nicotinamide; N-(1-Acetyl-3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; N-(3,3-Dimethyl-2,3-dihydro-1H-indol-6-yl)-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; 2-(1-Oxo-2,3-dihydro-1H-isoindol-4-ylamino)-N-[3-(tetrahydro-furan-3-yloxy)-5-trifluoromethyl-phenyl]-nicotinamide; N-(4-(1,1-Dimethylethyl)-3-((N,N-dimethylglycyl)amino)phenyl)-2-(1H-indazol-6-ylamino)-3-pyridinecarboxamide; N-(2-Oxo-3,3-bis(trifluoromethyl)-2,3-dihydro-1H-indol-6-yl)-2-((1-oxo-2,3-dihydro-1H-isoindol-4-yl)amino)-3-pyridinecarboxamide; N-(3-((((2R)-1-Methyl-2-pyrrolidinyl)methyl)oxy)-4-(trifluoromethyl)phenyl)-2-((1-oxo-2,3-dihydro-1H-isoindol-4-yl)amino)-3-pyridinecarboxamide; 2-(1H-indazol-6-ylamino)-N-(3-((((2S)-1-methyl-2-pyrrolidinyl)methyl)oxy)-4-(trifluoromethyl)phenyl)-3-pyridinecarboxamide; N-[3-(1-Methyl-pyrrolidin-2-ylmethoxy)-4-pentafluoroethyl-phenyl]-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; N-[3-(1-Methyl-pyrrolidin-2-ylmethoxy)-4-trifluoromethyl-phenyl]-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; N-[3-(2-Dimethylamino-ethoxy)-4-trifluoromethyl-phenyl]-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; N-[3-(1-Methyl-pyrrolidin-2-ylmethoxy)-4-pentafluoroethyl-phenyl]-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; N-(3,3-Bis-trifluoromethyl-2,3-dihydro-1H-indol-6-yl)-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; N-[1-(2-Dimethylamino-acetyl)-3,3-bis-trifluoromethyl-2,3-dihydro-1H-indol-6-yl]-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; N-(4,4-Bis-trifluoromethyl-1,2,3,4-tetrahydro-isoquinolin-7-yl)-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; N-(2-Methyl-4,4-bis-trifluoromethyl-1,2,3,4-tetrahydro-isoquinolin-7-yl)-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; N-(3,3-dimethyl-1-(methylsulfonyl)-2,3-dihydro-1H-indol-6-yl)-2-(1H-indazol-6-ylamino)-3-pyridinecarboxamide; 1,1-Dimethylethyl 3-(((2-(1,1-dimethylethyl)-5-(((2-(1H-indazol-6-ylamino)-3-pyridinyl)carbonyl) amino)phenyl)oxy)methyl)-1-azetidinecarboxylate; N-[4-tert-Butyl-3-(2-dimethylamino-acetylamino)-phenyl]-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; N-[4-tert-Butyl-3-(2-methylamino-acetylamino)-phenyl]-2-(3H-indazol-5-ylamino)-nicotinamide; N-(4,4-Dimethyl-1,2,3,4-tetrahydro-isoquinolin-7-yl)-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; N-(4,4-Dimethyl-1,2,3,4-tetrahydro-isoquinolin-7-yl)-2-(1-oxo-2,3-dihydro-1H-isoindol-4-ylamino)-nicotinamide; and N-[3,3-Dimethyl-1-(pyrrolidine-2-carbonyl)-2,3-dihydro-1H-indol-6-yl]-2-(1H-indazol-6-ylamino)-nicotinamide.
- 17. A pharmaceutical composition comprising a pharmaceutically-acceptable carrier and a compound as in any of claims 1-16.
- 18. A method of treating cancer in a subject, said method comprising administering an effective amount of a compound as in any of claims 1-16.
- 19. The method of claim 18 comprising a combination with a compound selected from antibiotic-type agents, alkylating agents, antimetabolite agents, hormonal agents, immunological agents, interferon-type agents and miscellaneous agents.
- 20. A method of treating angiogenesis in a subject, said method comprising administering an effective amount of a compound as in any of claims 1-16.
- 21. A method of treating KDR-related disorders in a mammal, said method comprising administering an effective amount of a compound of claims 1-16.
- 22. A method of treating proliferation-related disorders in a mammal, said method comprising administering an effective amount of a compound of any of claim 1-16.
- 23. Method of claim 22 wherein the disorder is inflammation or an inflammation-related disorder.
- 24. A method of reducing blood flow in a tumor in a subject, said method comprising administering an effective amount of a compound as in any of claims 1-16.
- 25. A method of reducing tumor size in a subject, said method comprising administering an effective amount of a compound as in any of claims 1-16.
- 26. A method of treating diabetic retinopathy in a subject, said method comprising administering an effective amount of a compound as in any of claims 1-16.
Parent Case Info
[0001] This application is a continuation-in-part of U.S. patent application Ser. No. 10/046,622 filed Jan. 10, 2002 claiming the benefit of U.S. Provisional Application Nos. 60/261,882, filed Jan. 12, 2001, and 60/323,808 filed Sep. 19, 2001, which are hereby incorporated by reference.
Provisional Applications (2)
|
Number |
Date |
Country |
|
60261882 |
Jan 2001 |
US |
|
60323808 |
Sep 2001 |
US |
Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
10046622 |
Jan 2002 |
US |
Child |
10197918 |
Jul 2002 |
US |