Pyrido-Pyrimidine Derivatives
AssigneeMerck Patent GmbH
InventorsWolfgang Stahle, Oliver Schadt, Christine Knuehl, Manja Friese-Hamim, Bayard Huck, Andreas Goutopoulos, Nadia Brugger
Life of this patent
Estimating the term…
Abstract
Compounds of the formula I in which Het, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of RON and can be employed, for the treatment of cancer
Claims17
1-12. (canceled)
Compounds of the formula I
- in which:
- Het denotes imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl or triazolyl, each of which is substituted by R1 and R2,
- R1 denotes Ar1,
- R2 denotes A′,
- R3 denotes F or Cl,
- R4 denotes H, CH2Ar2 or A,
- Ar1 denotes phenyl, which is unsubstituted or mono-, di- or trisubstituted by Hal, A, OH, OA, CONH2, COOH, COOA, CN, CHO, COA, SO2A, NHCOA and/or, SO2NH2,
- Ar2 denotes phenyl, which is unsubstituted or mono-, di- or trisubstituted by Hal, A, OH, OA, CONH2, COOH, COOA, CN, CHO, COA, SO2A, NHCOA and/or, SO2NH2,
- A′ denotes unbranched or branched alkyl having 1-6 C atoms, in which 1-7 H atoms may be replaced by F,
- A denotes unbranched or branched alkyl having 1-10 C atoms, in which one or two non-adjacent CH and/or CH2 groups may be replaced by N, O, S atoms and/or by —CH═CH— groups and/or in addition 1-7 H atoms may be replaced by F,
- and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
Medicaments comprising at least one compound of the formula I according to claim 1 and/or pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, and optionally excipients and/or adjuvants.
Compounds according to claim 1 and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for the use for the treatment of cancer, septic shock, Primary open Angle Glaucoma (POAG), hyperplasia, rheumatoid arthritis, psoriasis, artherosclerosis, retinopathy, osteoarthritis, endometriosis, chronic inflammation, and/or neurodegenerative diseases.
Compounds of the formula I according to claim 1 and/or physiologically acceptable salts, tautomers and stereoisomers thereof for the use for the treatment of tumours, where a therapeutically effective amount of a compound of the formula I is administered in combination with a compound from the group 1) oestrogen receptor modulator, 2) androgen receptor modulator, 3) retinoid receptor modulator, 4) cytotoxic agent, 5) antiproliferative agent, 6) prenyl-protein transferase inhibitor, 7) HMG-CoA reductase inhibitor, 8) HIV protease inhibitor, 9) reverse transcriptase inhibitor and 10) further angiogenesis inhibitors.
Compounds of the formula I according to claim 1 and/or physiologically acceptable salts, tautomers and stereoisomers thereof for the use for the treatment of tumours, where a therapeutically effective amount of a compound of the formula I is administered in combination with radiotherapy and a compound from the group 1) oestrogen receptor modulator, 2) androgen receptor modulator, 3) retinoid receptor modulator, 4) cytotoxic agent, 5) antiproliferative agent, 6) prenyl-protein transferase inhibitor, 7) HMG-CoA reductase inhibitor, 8) HIV protease inhibitor, 9) reverse transcriptase inhibitor and 10) further angiogenesis inhibitors.
Dependencies are inferred from the claim text.