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US 8,557,977 B2Granted
4 (pyrrolopyridinyl)pyrimidin-2-ylamine derivatives
AssigneeMerck Patent GmbH
InventorsDieter Dorsch, Christian Sirenberg, Thomas J. J. Mueller, Eugen Merkul
Life of this patent
Estimating the term…
Abstract
Compounds of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in Claim 1, are inhibitors of cell proliferation\cell vitality and can be employed for the treatment of tumors.
Claims20
A method for treating a tumour, comprising administering to a subject in need thereof an effective amount of a compounds of formula I
- in which
- R1 denotes H, A, —[C(R6)2]nAr, —[C(R6)2]nHet or —[C(R6)2]ncycloalkyl,
- R2 denotes H or A,
- R3, R4 each, independently of one another, denote H, A, Hal, CN, —[C(R6)2]nAr, —[C(R6)2]nHet or -[C(R6)2]ncycloalkyl,
- R5 denotes H, A, —[C(R6)2]nAr, —[C(R6)2]nHet or —[C(R6)2]ncycloalkyl,
- R6 denotes H or alkyl having 1-6 C atoms,
- A, A′ each, independently of one another, denote unbranched or branched alkyl having 1-10 C atoms, in which one or two CH2 groups may be replaced by O or S atoms and/or by —CH═CH— groups, and/or 1-7 H atoms may be replaced by F,
- Hal denotes F, Cl, Br or I,
- Ar denotes a saturated, unsaturated or aromatic carbocycle having 5-14 C atoms which is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted by OH, OA, SH, SA, SOA, SO2A, Hal, NO2, NH2, NHA, NAA′, A, SO2NH2, SO2NHA, SO2NAA′, CONH2, CONHA, CONAA′, NACOA′, NASO2A′, COOH, COOA, COA, CHO and/or CN,
- Het denotes furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyrimidinyl, triazolyl, tetrazolyl, thiadiazole, pyridazinyl, pyrazinyl, indolyl, isoindolyl, benzimidazolyl, indazolyl, quinolyl or 1,3-benzodioxolyl, each of which is unsubstituted or mono- or disubstituted by OH, OA, Hal and/or A, and
- n denotes 0, 1 or 2,
- or a pharmaceutically acceptable derivative, solvate, salt, tautomer or stereoisomer thereof.
9 more elements
A method for treating a tumour, comprising administering to a subject in need thereof an effective amount of one of the following compounds
- Com-
- pound
- No.
- Name and/or structure
- “A1”
- Phenyl[4-(1H-pyrrolo[3,2-c]pyridin-3-yl)pyrimidin-2-yl]amine
- “A2”
- 4-Phenyl-6-(1H-pyrrolo[3,2-c]pyridin-3-yl)pyrimidin-2-ylamine
- “A3”
- 4-Butyl-6-(1H-pyrrolo[3,2-c]pyridin-3-yl)pyrimidin-2-ylamine
- “A4”
- “A5”
- “A6”
- “A7”
- “A8”
- “A9”
- “A10”
- “A11”
- “A12”
- “A13”
- “A14”
- “A15”
- “A16”
- “A17”
- “A18”
- “A19”
- “A20”
- “A21”
- “A22”
- “A23”
- “A24”
- “A25”
- “A26”
- “A27”
- “A28”
- or a pharmaceutically acceptable salt thereof.
33 more elements
Dependencies are inferred from the claim text.