US Patent No. 9,592,225

CRYSTALLINE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONO MESYLATE MONOHYDRATE HAVING A SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND A SPECIFIC SURFACE AREA RANGE FOR USE IN PHARM


Patent No. 9,592,225
Issue Date March 14, 2017
Title Crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-n-methyl-2-[4-(2-pyridinyl)phenyl]acetamide Mono Mesylate Monohydrate Having A Specific Particle Size Distribution Range And A Specific Surface Area Range For Use In Pharm
Inventorship Wilfried Schwab, Werder (DE)
Alexander Birkmann, Wuppertal (DE)
Kerstin Paulus, Ratingen (DE)
Kurt Vogtli, Oberhofen (CH)
Dieter Haag, Ramlinsburg (CH)
Stephan Maas, Krefeld (DE)
Kristian Ruepp, Berlin (DE)
Assignee AICURIS ANTI-INFECTIVE CURES GMBH, Wuppertal (DE)

Claim of US Patent No. 9,592,225

1. A composition of crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]acetamide
mono methanesulfonic acid monohydrate particles of the following formula

having a purity of >99%,
wherein said particles in the composition have a particle size range from 1 to 500 ?m, a particle size distribution which
is defined by d(0.1) from 2 to 100 ?m, d(0.5) from 30 to 210 ?m and d(0.9) from 70 to 400 ?m and a specific surface area of
less than 1.0 m2/g.