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US 8,895,575 B2Granted
1 H-pyrrolo[2,3-b]pyridine derivatives
AssigneeMerck Patent GmbH
InventorsTimo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
Life of this patent
Estimating the term…
Abstract
1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.
Claims12
A method for the treatment of a tumour, tumour growth, or tumour metastases where the tumour, tumour growth, or tumour metastases originates from acute myeloid leukaemia, chronic myeloid leukaemia, acute lymphatic leukaemia or chronic lymphatic leukaemia, comprising administering to a subject in need thereof an effective amount of one of the following compounds
- No.
- Structure/name
- “A1”
- N4-(3-Fluorophenyl)-N4-methyl-6-[5-(1-methyl-1H-pyrazol-4-yl)-
- 1H-pyrrolo[2,3-b]pyridin-3-yl]pyrimidine-2,4-diamine
- “A2”
- 4-(1-Methyl-1-phenylethyl)-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-
- pyrrolo[2,3-b]pyridin-3-yl]pyrimidin-2-ylamine
- “A3”
- 4-[5-(1-Methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-
- 6-(1-phenylcyclopropyl)pyrimidin-2-ylamine
- “A4”
- 2-({2-Amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]-
- pyridin-3-yl]pyrimidin-4-yl}phenylamino)ethanol
- “A5”
- (S)-3-[{2-Amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-
- b]-pyridin-3-yl]pyrimidin-4-yl}-(4-methoxyphenyl)amino]
- propane-1,2-diol
- “A6”
- 4-[5-(1-Methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-
- 6-(1-phenylcyclopentyl)pyrimidin-2-ylamine
- “A7”
- 4-[1-(4-Chlorophenyl)cyclopentyl]-6-[5-(1-methyl-1H-pyrazol-4-
- yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]pyrimidin-2-ylamine
- “A8”
- N4-(3-Chlorophenyl)-N4-methyl-6-[5-(1-methyl-1H-pyrazol-4-yl)-
- 1H-pyrrolo[2,3-b]pyridin-3-yl]pyrimidine-2,4-diamine
- “A9”
- N4-(2-Fluorophenyl)-N4-methyl-6-[5-(1-methyl-1H-pyrazol-4-yl)-
- 1H-pyrrolo[2,3-b]pyridin-3-yl]pyrimidine-2,4-diamine
- “A10”
- N4-(2-Chlorophenyl)-N4-methyl-6-[5-(1-methyl-1H-pyrazol-4-yl)-
- 1H-pyrrolo[2,3-b]pyridin-3-yl]pyrimidine-2,4-diamine
- “A11”
- N4-Methyl-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]-
- pyridin-3-yl]-N4-phenylpyrimidine-2,4-diamine
- “A12”
- N4-Ethyl-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-
- b]pyridin-3-yl]-N4-phenylpyrimidine-2,4-diamine
- “A13”
- N4-(4-Chlorophenyl)-N4-ethyl-6-[5-(1-methyl-1H-pyrazol-4-yl)-
- 1H-pyrrolo[2,3-b]pyridin-3-yl]pyrimidine-2,4-diamine
- “A14”
- N4-Benzyl-N4-ethyl-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-
- pyrrolo[2,3-b]pyridin-3-yl]pyrimidine-2,4-diamine
- “A15”
- 2-[{2-Amino-6-[5-(1-isopropyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-
- b]-pyridin-3-yl]pyrimidin-4-yl}-(2-chlorophenyl)amino]ethanol
- “A16”
- 2-[{2-Amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]-
- pyridin-3-yl]pyrimidin-4-yl}-(2-chlorophenyl)amino]ethanol
- “A17”
- 4-(5-Fluoro-2,3-dihydroindol-1-yl)-6-[5-(1-methyl-1H-pyrazol-4-
- yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]pyrimidin-2-ylamine
- “A18”
- 4-(5-Fluoro-2,3-dihydroindol-1-yl)-6-[5-(1-isopropyl-1H-pyrazol-
- 4-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]pyrimidin-2-ylamine
- “A19”
- N4-(2-Chlorophenyl)-6-[5-(1-isopropyl-1H-pyrazol-4-yl)-1H-
- pyrrolo[2,3-b]pyridin-3-yl]-N4-methylpyrimidine-2,4-diamine
- “A20”
- N4-Ethyl-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-
- b]pyridin-3-yl]-N4-1,3,4-thiadiazol-2-ylpyrimidine-2,4-diamine
- “A21”
- 1-({2-Amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]-
- pyridin-3-yl]pyrimidin-4-yl}phenylamino)-3-methoxypropan-2-ol
- “A22”
- 3-[{2-Amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-
- pyrrolo[2,3-b]-pyridin-3-yl]pyrimidin-4-yl}-(2,3-
- dihydroxypropyl)amino]benzonitrile
- “A23”
- 3-[{2-Amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]-
- pyridin-3-yl]pyrimidin-4-yl}-(2-chlorophenyl)amino]propionic
- acid
- “A24”
- Methyl [{2-amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-
- pyrrolo[2,3-b]pyridin-3-yl]pyrimidin-4-yl}-(4-
- chlorophenyl)amino]-acetate
- “A25”
- 2-[{2-Amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]-
- pyridin-3-yl]pyrimidin-4-yl}-(2,4-difluorophenyl)amino]ethanol
- “A26”
- 2-[{2-Amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]-
- pyridin-3-yl]pyrimidin-4-yl}-(2-fluorophenyl)amino]ethanol
- “A27”
- 4-(2,3-Dihydrobenzo-1,4-oxazin-4-yl)-6-[5-(1-methyl-1H-pyrazol-
- 4-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]pyrimidin-2-ylamine
- “A28”
- N4-(3-Fluorophenyl)-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-
- pyrrolo[2,3-b]pyridin-3-yl]-N4-(2-morpholin-4-
- ylethyl)pyrimidine-2,4-diamine
- “A29”
- N4-(2-Chlorophenyl)-N4-(2-methoxyethyl)-6-[5-(1-methyl-1H-
- pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]pyrimidine-2,4-
- diamine
- “A30”
- 3-({2-Amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]-
- pyridin-3-yl[pyrimidin-4-yl}phenylamino)propionitrile
- “A30a”
- (3-Fluorophenyl)methyl-{6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-
- pyrrolo[2,3-b]pyridin-3-yl[pyrimidin-4-yl}amine
- “A31”
- N4-(3-Aminopropyl)-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-
- pyrrolo[2,3-b]pyridin-3-yl]-N4-phenylpyrimidine-2,4-diamine
- “A32”
- N4-(3-Aminopropyl)-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-
- pyrrolo[2,3-b]pyridin-3-yl]-N4-(2-methylpyridin-4-yl)pyrimidine-
- 2,4-diamine
- “A33”
- 3-[{2-Amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]-
- pyridin-3-yl]pyrimidin-4-yl}-(2-methylpyridin-4-yl)amino]-
- propionitrile
- “A34”
- 4-[5-(1-Methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-
- 6-[1-(2-methylpyridin-4-yl)cyclopropyl]pyrimidin-2-ylamine
- “A35”
- 3-({2-Amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]-
- pyridin-3-yl]pyrimidin-4-yl}phenylamino)propionamide
- “A36”
- 3-[{2-Amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]-
- pyridin-3-yl]pyrimidin-4-yl}-(2-methylpyridin-4-yl)amino]-
- propionamide
- “A37”
- N4-(2-Methoxyethyl)-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-
- pyrrolo[2,3-b]pyridin-3-yl]-N4-(2-methylpyridin-4-yl)pyrimidine-
- 2,4-diamine
- “A38”
- N4-(2-Methoxyethyl)-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-
- pyrrolo[2,3-b]pyridin-3-yl]-N4-(1-methylpyrazol-4-yl)pyrimidine-
- 2,4-diamine
- “A39”
- N4-(3-Aminopropyl)-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-
- pyrrolo[2,3-b]pyridin-3-yl]-N4-(2-chlorophenyl)pyrimidine-2,4-
- diamine
- “A40”
- 3-[{2-Amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]-
- pyridin-3-yl]pyrimidin-4-yl}-(2-chlorophenyl)amino]propionamide
- “A41”
- 3-[{2-Amino-6-[5-(1-isopropyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-
- b]-pyridin-3-yl]pyrimidin-4-yl}-(2-methylpyridin-4-yl)amino]-
- propionamide
- “A42”
- 4-[1-(2-Fluorophenyl)cyclopropyl]-6-[5-(1-methyl-1H-pyrazol-4-
- yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]pyrimidin-2-ylamine
- “A43”
- N-[3-({2-Amino-6-[5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-
- b]-pyridin-3-yl]pyrimidin-4-yl}phenylamino)propyl]acetamide
- or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof.
145 more elements
Dependencies are inferred from the claim text.