Revisiting the role of dihydroorotate dehydrogenase as a therapeutic target for cancer.

The present invention provides triazolone compounds of general formula (I): in which R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

4,5-annulated 1,2,4-triazolones

The present invention provides Compound (I), 2-butoxy-N-(2-chloro-6-fluorophenyl)-4-[3-(2-chlorophenyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl]-5-fluorobenzamide and Compound (II), N-(2-chloro-6-fluorophenyl)-4-[4-ethyl-3-(hydroxymethyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl]-5-fluoro-2-{[(2S)-1,1,1-trifluoropropan-2-yl]oxy}benzamide, (II):and stereoisomers, tautomers, N-oxides, hydrates, solvates, and salts thereof, and mixtures of same, methods for the preparation of Compound (I) and Compound (II) and their use for the treatment of hyperproliferative diseases, particularly cancer.

5-oxo-4,5-dihydro-1h-1,2,4-triazol derivatives for the treatment of cancer

The present invention relates to : * combinations of : component A : one or more 2,3-dihydroimidazo[l,2-c]quinazoline compounds of general formula (Al) or (A2) as defined herein, or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; component B : one or more dihydroorotate dehydrogenase (DHODH)-inhibiting 2,4,5- trisubstituted 1,2,4-triazolone compounds of general formula (B-l) as defined herein, or a tautomer, an N-oxide, a salt, a salt of a tautomer or a salt of an N-oxide thereof; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially. dependently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route; * use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and * a kit comprising such a combination.

Combinations of copanlisib with triazolone derivatives and their use in the treatment of cancer

The present invention provides methods for the preparation of Compound (I): Compound (I), the use of intermediates for the preparation of said compound and its crystalline form A.

Method for the preparation of a 2,4,5-trisubstituted 1,2,4-triazolone

The present invention provides triazolone compounds compounds of general formula (I) : in which R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of DHODH

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2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of DHODH