Zaklady Farmaceutyczne Polpharma S.a.

Marcin Szulc

Robert Rynkiewicz

Roman Szramka

Przemyslaw Skoczen

Mariusz Krzyzanowski

Monika Oracz

Arkadiusz Majewski

Dominika Podwysocka

Piotr Garczarek

Jerzy Drygas

Barbara Piotrkowska

The invention particularly relates to crystalline (solid) forms of N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]acetamide), i.e. Form N, Form M, Form O and Form P. It also refers to a pharmaceutical composition or dosage form comprising said crystalline forms. The invention also concerns said pharmaceutical composition or dosage form for use in a method of treating a disease or disorder defined in the claims. Finally, the invention pertains to the use of said novel crystalline forms for the preparation of a pharmaceutical composition or dosage form.

Crystalline forms of apremilast

The method of synthesizing vardenafil base, in anhydrous conditions, by chlorosulfonation of 2-(2-etoxy-phenyl)-5 -methyl-7-propyl-iH-imidazo[5,1-fJ[1,2,4]triazin-4-one in a mixture of thionyl chloride and sulfurochloridic acid followed by amidation of the product, 4-etoxy-3-(5-methyl-4-oxo-7-propyl-3,4-dihydroimidazo[5,1-f][1,2,4]triazin-2-yl)benzene-sulfonic acid chloride with N-ethylpiperazine, in an aprotic solvent, in the presence of an inorganic base and the method of conversion the product, vardenafil base, to yield vardenafil monohydrochloride trihydrate having a melting point of 234&#xb0; C. by contacting with water of the anhydrous modification V of vardenafil monohydrochloride in an organic solvent. The subject of the invention is also the anhydrous modification V of vardenafil monohydrochloride and its use in the preparation of vardenafil monohydrochloride trihydrate having a melting point of 234&#xb0; C.

Method for manufacturing of vardenafil and its salts

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Starogard Gdanski, Poland

Marcin Szulc