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The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 9889124 B1

PDFFull Text
Date of Patent:
Feb. 13, 2018

Filed:

Aug. 31, 2015

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 pharmaceutical formulations

Applicant:

Aicuris Anti-infective Cures Gmbh, Wuppertal, DE;

Inventors:

Wilfried Schwab, Werder, DE;

Alexander Birkmann, Wuppertal, DE;

Kerstin Paulus, Ratingen, DE;

Kurt Vogtli, Oberhofen AG, CH;

Dieter Haag, Ramlingsburg BL, CH;

Stephan Maas, Krefeld, DE;

Kristian Ruepp, Berlin, DE;

Assignee:

AICURIS ANTI-INFECTIVE CURES GMBH, Wuppertal, DE;

Attorneys:

Millen White Zelano and Branigan, PC

Csaba Henter

John Sopp

Primary Examiner:

Daniel R Carcanague

Int. Cl.
CPC ...
A61K 45/06 (2006.01); A61K 9/14 (2006.01); A61K 31/4439 (2006.01); C07D 417/12 (2006.01); A61K 31/10 (2006.01); A61K 9/16 (2006.01);
U.S. Cl.
CPC ...
A61K 31/4439 (2013.01); A61K 9/145 (2013.01); A61K 9/16 (2013.01); A61K 31/10 (2013.01); A61K 45/06 (2013.01); C07D 417/12 (2013.01); Y10T 428/2982 (2015.01);
Abstract

The present invention relates to the crystalline mono mesylate monohydrate salt of N-[5 -(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide in a definite particle size range, particle size distribution and a specific surface area range, which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions, as well as to pharmaceutical compositions containing said crystalline N-[5-(amino sulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2 -pyridinyl)phenyl]acetamide mono mesylate monohydrate having the afore-mentioned particle size range, particle size distribution and specific surface area range. Moreover, the present invention relates to the pharmacokinetic and pharmacodynamic in vivo profiles of the resultant free base of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4 -(2-pyridinyl)phenyl]-acetamide after administration of the afore-mentioned crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]-acetamide mono mesylate monohydrate salt to a subject in need thereof.

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