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US 8,044,065 B2Granted
Benzothienopyridines for use as inhibitors of Eg5 kinesin
AssigneeAltana Pharma AG
InventorsMatthias Vennemann, Thomas Baer, Gudrun Groegor
Life of this patent
Estimating the term…
Abstract
Compounds of a certain formula I, in which R1, R2, R3, R4 and X have the meanings indicated in the description, are novel effective compounds with Eg5 inhibitory, anti-proliferative and/or apoptosis inducing activity.
Claims14
A combination comprising
- a first active ingredient, which is at least one compound of formula (I*)
- in which
- R1 is 1-4C-alkyl, 3-7C-cycloalkyl, 3-7C-cycloalkyl-1-4C-alkyl, or 2-7C-alkyl substituted by R11,
- R11 is —N(R111)R112,
- R111 is hydrogen, or 1-4C-alkyl,
- R112 is hydrogen, or 1-4C-alkyl,
- or R111 and R112 together, and with inclusion of the nitrogen atom to which they are bonded, form a ring Het,
- Het is piperidinyl, morpholinyl, thiomorpholinyl, or pyrrolidinyl,
- R2 is hydrogen, 1-4C-alkyl, halogen, trifluoromethyl, 1-4C-alkoxy, hydroxyl, 1-4C-alkoxy-2-4C-alkoxy, hydroxy-2-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkyl-1-4C-alkoxy, or completely or predominantly fluorine-substituted 1-4C-alkoxy,
- R3 is hydrogen, or 1-4C-alkoxy, and
- X is NH, oxygen or sulphur, and
- R4 is 1-4C-alkyl,
- or
- X is sulphur, and
- R4 is hydrogen,
- or
- X is oxygen, and
- R4 is hydrogen,
- or
- (±)-(3aSR,10RS)-10-(3-Hydroxy-phenyl)-2,3a-dimethyl-3a,4,9,10-tetrahydro-2,9,10a-triaza -cyclopenty[b]fluorene-1,3-dione;
- (3aSR,10RS)-10-(3-Hydroxy-phenyl)-2,3a-dimethyl-4,10-dihydro-3aH-9-thia-2,10a-diaza -cyclopenta[b]fluorene-1,3-dione;
- (3aSR,10RS)-2-(2-Dimethylamino-ethyl)-10-(3-hydroxy-phenyl)-3a-methyl-3a,4,9,10-tetrahydro -2,9,10a-triaza-cyclopenty[b]fluorene-1,3-dione;
- or
- (3aSR,10RS)-2-(2-Dimethylamino-ethyl)-10-(3-hydroxy-phenyl)-3a-methyl-4,10-dihydro-3aH-9-thia-2,10a-diaza-cyclopenta[b]fluorene-1,3-dione
- or a salt, stereoisomer or a salt of a stereoisomer thereof;
- and
- a second active ingredient, which is at least one anti-cancer agent selected from the group consisting of chemotherapeutic anti-cancer agents and target-specific anti-cancer agents.
24 more elements
Dependencies are inferred from the claim text.