Abstract: Quinolonecarboxylic esters of the general formula (II) are hydrolyzed to quinolonecarboxylic acids of the general formula (I): The method comprises the step A): A) reacting compounds of the formula (II) with a mixture comprising acetic acid, sulfuric acid and water In step A), ?30 to ?40 mol of acetic acid, ?0.3 to ?1 mol of sulfuric acid and ?0.9 to ?2.5 mol of water are used per mole of compounds of the formula (II). The method is particularly suitable for the synthesis of the intermediate (I) in the synthesis of pradofloxacin.

Abstract: Quinolonecarboxylic esters of the general formula (II) are hydrolyzed to quinolonecarboxylic acids of the general formula (I): The method comprises the step A): A) reacting compounds of the formula (II) with a mixture comprising acetic acid, sulfuric acid and water In step A), ?30 to ?40 mol of acetic acid, ?0.3 to ?1 mol of sulfuric acid and ?0.9 to ?2.5 mol of water are used per mole of compounds of the formula (II). The method is particularly suitable for the synthesis of the intermediate (I) in the synthesis of pradofloxacin.

Abstract: The present invention provides for amorphous Letermovir and orally administrable solid pharmaceutical formulations thereof (immediate release formulation). Said amorphous Letermovir is suitable for immediate release formulations when isolated out of an organic solution by either roller-drying said organic solution in a volatile organic solvent, in particular acetone, at a temperature of 30° C. to 60° C., and subsequently drying the amorphous Letermovir obtained, or isolating said amorphous Letermovir by precipitation from water miscible solvents selected from acetone or acetonitrile into excess water as anti-solvent, and subsequently filtrating or centrifuging the amorphous Letermovir obtained. The immediate release formulations of amorphous Letermovir are intended for use in methods of prophylaxis or methods of treatment of diseases associated with the group of Herpesviridae, preferably associated with cytomegalovirus (CMV), even more preferably associated with human cytomegalovirus (HCMV).

Abstract: The invention relates to sodium and calcium salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid and solvates thereof, to the use thereof in a method of treatment and/or prophylaxis of virus infections and to the use thereof for producing drugs for use in methods of treatment and/or prophylaxis of diseases, more particularly the use thereof as antiviral agents, more particularly against cytomegaloviruses.

Abstract: The present invention provides for amorphous Letermovir and orally administrable solid pharmaceutical formulations thereof (immediate release formulation). Said amorphous Letermovir is suitable for immediate release formulations when isolated out of an organic solution by either roller-drying said organic solution in a volatile organic solvent, in particular acetone, at a temperature of 30° C. to 60° C., and subsequently drying the amorphous Letermovir obtained, or isolating said amorphous Letermovir by precipitation from water miscible solvents selected from acetone or acetonitrile into excess water as anti-solvent, and subsequently filtrating or centrifuging the amorphous Letermovir obtained. The immediate release formulations of amorphous Letermovir are intended for use in methods of prophylaxis or methods of treatment of diseases associated with the group of Herpesviridae, preferably associated with cytomegalovirus (CMV), even more preferably associated with human cytomegalovirus (HCMV).

Abstract: The invention relates to sodium and calcium salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid and solvates thereof, to the use thereof in a method of treatment and/or prophylaxis of virus infections and to the use thereof for producing drugs for use in methods of treatment and/or prophylaxis of diseases, more particularly the use thereof as antiviral agents, more particularly against cytomegaloviruses.

Abstract: Dihydroquinazolines of the formula: The dihydroquinalzolines are useful as antiviral agents in particular against cytomegaloviruses.

Abstract: The present invention relates to a process for the preparation of dihydroquinazolines, which are used for the production of medicaments.

Abstract: The present invention relates to a process for the preparation of dihydroquinazolines, for example, methyl (S)-{8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoro -methyl)-phenyl]-3,4-dihydroquinazolin-4-yl}acetate (2S,3S)-2,3-bis[(4-methylbenzoyl) -oxy]succinic acid salt, which are used for the production of antiviral medicaments.

Abstract: A method is described for the manufacture of pure 2-fluoro-ara-adenine of Formula (I) from 2-fluoro-ara-adenine triacetate using potassium carbonate (K2CO3), wherein the 2-fluoro-ara-adenine has a reduced dimer contents, as well as the compound 2-fluoro-ara-adenine having a dimer contents of ?0.3%.

Abstract: The present invention relates to a process for the preparation of dihydroquinazolines, which are used for the production of medicaments.

Abstract: The present invention relates to a process for preparing 4-{4-[({[4-chloro-3-(trifluoro-methyl)phenyl]amino}carbonyl)amino]phenoxy}-N-methylpyridine-2-carboxamide and its tosylate salt.

Abstract: The present invention relates to a process for the preparation of dihydroquinazolines, for example {8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-4-yl}acetic acid, which are used as antiviral agents in the production of medicaments.

Abstract: The present invention relates to a process for preparing 4-(4-aminophenyl)-3-morpholinone by reacting 4-(4-nitrophenyl)-3-morpholinone with hydrogen in the presence of a hydrogenation catalyst, characterized in that the reaction is effected in an aliphatic alcohol.

Abstract: The present invention relates to a process for the preparation of dihydroquinazolines, which are used for the production of medicaments.

Abstract: The present invention relates to a process for preparing 4-{4-[({[4-chloro-3-(trifluoro-methyl)phenyl]amino}carbonyl)amino]phenoxy}-N-methylpyridine-2-carboxamide and its tosylate salt.

Abstract: The present invention relates to a process for preparing 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide starting from 2-[(2S)-2-oxiranylmethyl]-1H-isoindole-1,3(2H)-dione, 4-(4-aminophenyl)-3-morpholinone and 5-chlorothiophene-2-carbonyl chloride.

Abstract: The present invention relates to a process for preparing 4-(4-aminophenyl)-3-morpholinone by reacting 4-(4-nitrophenyl)-3-morpholinone with hydrogen in the presence of a hydrogenation catalyst, characterized in that the reaction is effected in an aliphatic alcohol.

Abstract: The present invention relates to a process for preparing 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide starting from 2-[(2S)-2-oxiranylmethyl]-1H-isoindole-1,3(2H)-dione, 4-(4-aminophenyl)-3-morpholinone and 5-chlorothiophene-2-carbonyl chloride.

Abstract: The invention relates to a process for the preparation of nifedipine by the reaction of methyl 2-(2-nitrobenzylidene)acetoacetate and methyl 3-aminocrotonate and the use of the nifedipine thus prepared for the production of a medicament.