755039-80-6Relevant articles and documents
Storage stable perfusion solution for dihydropteridinones
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Page/Page column 19, (2008/06/13)
Disclosed are storage stable aqueous infusible or injectable solutions containing an active substance of general formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and in the specification, and an amount of a physiologically acceptable acid or mixture of acids sufficient to dissolve the active substance and act as a stabiliser, optionally together with other formulating excipients suitable for parenteral administration, and a process for preparing the infusible or injectable solutions according to the invention.
New pteridinones as PLK inhibitors
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Page/Page column 9; 12, (2008/06/13)
Disclosed compounds of general formula (1) wherein L, Q1, Q2, X, Y, Ra, Rb, Rc, R1, R2, R3 and R4 are defined as in claim 1, which are suitable for the trea
PTERIDINONES USED AS PLK (POLO LIKE KINASE) INHIBITORS
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Page/Page column 25-26; 32-33, (2010/10/20)
The invention relates to compounds of general formula (1), wherein L, Q1, Q2, X, Y, Ra, Rb, Rc, R1, R2, R3, and R4 are defined as indicated in claim 1. Said
2-Arylaminopyrimidine derivatives as PLK inhibitors
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Page/Page column 54; 55, (2010/02/14)
Anilino-pyrimidine and 1,2,4-triazine compounds (1) are new. Anilino-pyrimidine and 1,2,4-triazine compounds of formula (1), their tautomers, racemates, enantiomers and/or diastereomers and acid-addition salts are new. X : NR 1a>, O or S; Y : CH or N; Z : hydrogen, halo, (halo)1-3C alkyl, 2-3C alkenyl, 2-3C alkynyl, formyl, 1-3C (halo)alkylcarbonyl, 2-3C alkenyl-, 2-3C alkynyl-carbonyl or pseudohalo; A : (hetero)aryl group (i) or (ii); R a> - R f>e.g. hydrogen, halo or nitro; R 1> and R 1a>hydrogen or methyl; R 2>e.g. Cl, Br, I, OR 6>; R 3>e.g. -CONR 1>-L-Q 3-Q 4-R 9>, -NR 1>-CO-L-Q 3-Q 4-R 9>; R 4>e.g. OR 6>, COR 6>, CONR 6>R 7>, NR 6>R 7>, NR 6>COR 7>, NR 6>SO 2R 7>, N=CR 6>R 7>, SR 6>, SOR 6>, SO 2R 6>, SO 2NR 6>R 7> or pseudohalogen, or any of 1-8C alkyl, 2-10C alkenyl or alkynyl, 3-8C cycloalkyl, (hetero)aryl or heterocyclyl; R 5>hydrogen, halo, trifluoromethyl, 1-3C alkyl or OR 6>; R 6>, R 7>e.g. hydrogen or any of 1-5C alkyl, 2-5C alkenyl or alkynyl, 3-10C cycloalkyl, (hetero)aryl or heterocyclyl; L : e.g. bond or residue of 1-16C alkyl, 2-16C alkenyl or alkynyl, 3-10C cycloalkyl, (hetero)aryl or heterocyclyl; Q 3 and Q 4bond or a mono- or bi-cyclic heterocyclyl, optionally substituted by one or more of Me, Et, halo, amino, hydroxy or pseudohalo; R 9>as L but not a bond; and T : N, O or S. Full definitions are given in the DEFINITIONS (Full Definitions) field. [Image] [Image] ACTIVITY : Cytostatic; Antiinflammatory; Immunosuppressive; Virucide; Anti-HIV; Dermatological; Nootropic; Neuroprotective; Nephrotropic; Vulnerary; Antibacterial; Fungicide; Antiparasitic; Antipsoriatic; Osteopathic; Cardiovascular-Gen; Vasotropic; Gastrointestinal-Gen. MECHANISM OF ACTION : Kinase inhibitor; Polo-like kinase (PLK) inhibitor. In a trial, (1) was found to have EC 50 against recombinant human PLK1 of below 5, generally 1 mu M. No results for specific compounds were given.
DIHYDROPTERIDINONES, METHOD FOR THE PRODUCTION AND USE THEREOF IN THE FORM OF DRUGS
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Page/Page column 43, (2010/02/08)
The invention relates to novel dihydropteridinones of general formula (I), wherein rests L, R1-R5 have the significance indicated in claims and a specification, in the isomers thereof, in a method for producing and using said dihydropteridinones in the form of drugs.
