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US 7,547,695 B2Granted
Pyridopyrimidinones
AssigneeMerck Patent GmbH
InventorsGuenter Hoelzemann, Helene Crassier, Karl-August Ackermann, Wolfgang Staehle, Alfred Jonczyk, Wilfried Rautenberg, Francesc Mitjans, Elisabet Rosell-Vives, Jaume Adan, Marta Soler Riera
Life of this patent
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Abstract
The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and X′ have the designations cited in patent claim 1. Said compounds are inhibitors of tyrosine kinases, especially TIE-2, and Raf kinases, and can, inter alia, be used for the treatment of tumors.
Claims13
A compound or compounds of formula I
- wherein
- R1, R2, R3, R4, R5 each, independently of one another, are selected from the group consisting of H, A, OH, OA, alkenyl, alkynyl, NO2, NH2, NHA, NA2, Hal, CN, COOH, COOA, —OHet, —O-alkylene-Het, —O-alkylene-NR8R9, CONR8R9, CH(OH)-A and —C(═O)-A, or
- two adjacent radicals selected from R1, R2, R3, R4, R5 together are selected from the group consisting of —O—CH2—CH2—, —O—CH2—O—, —O—CH2—CH2—O—, —O—CA2-O— and —O—CF2—O—
- R6, R7 each, independently of one another, are selected from the group consisting of H, A, Hal, OH, OA and CN,
- R8, R9 each, independently of one another, are H or alkyl having 1-6 C atoms, wherein one or two CH2 groups optionally are replaced by O,
- Het is a mono- or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O or S atoms, which heterocycle optionally is or mono-, di- or trisubstituted by Hal, A, OA, COOA, CN or carbonyl oxygen (═O),
- A is alkyl having 1 to 10 C atoms, wherein, in addition, 1-7 H atoms optionally are replaced by F or chlorine,
- X is NH or a bond,
- X′ is NH
- Hal is selected from the group consisting of F, Cl, Br and I, or
- pharmaceutically acceptable salts, tautomers, stereoisomers thereof, or mixtures thereof in all ratios.
8 more elements
A compound or compounds of formula I-1
- wherein
- R6, R7 each, independently of one another, are selected from the group consisting of H, A, Hal, OH, OA and CN,
- R8, R9 each, independently of one another, are H or A,
- R10 is NH2 or NO2,
- A in each case, independently of one another, is alkyl having 1 to 10 C atoms, wherein, in addition, 1-7 H atoms may be replaced by F or chlorine,
- Hal are selected from the group consisting of F, Cl, Br and I,
- or pharmaceutically acceptable salts, tautomers or stereoisomers thereof, or mixtures thereof in all ratios.
4 more elements
Dependencies are inferred from the claim text.