Aicuris Gmbh + Co. Kg.

Aicuris Anti-infective Cures Gmbh

Aicuris Anti-infective Cures Ag

Alexander Birkmann

Wilfried Schwab

Kerstin Paulus

Alfons Grunenberg

Holger Zimmermann

Dieter Haag

Kristian Ruepp

Stephan Maas

Yogeshwar Bachhav

Kurt Vogtli

Susanne Bonsmann

Kurt Voegtli

Thomas Goldner

Andreas Lender

Birgit Keil

Joachim Rehse

Karl Malcolm

Tamara Pfaff

Daniela Paulsen

Kurt Vögtli

Wilfried Dr Schwab

Stephan Mass

Anti-viral active agents, particularly the free base hemihydrate form of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide, as well as methods for the manufacture thereof. Also the use of the above compound in the treatment of human herpes virus infections and in the preparation of pharmaceuticals comprising said compound.

N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide free base hemihydrate, methods of manufacture and uses thereof

The present invention relates to the field of anti-viral active agents, particularly to salts, more particularly to a maleate salt of the free base of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide, to pharmaceutical formulations thereof as well as to methods for the production of these salts. The present invention also relates to the use of theses salts and of respective pharmaceutical formulations thereof in methods of treatment and/or prevention of human herpes simplex virus infections, particulary infections caused by HSV-1 and HSV-2.

Sulfate salt of the free base of n-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-n-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide, pharmaceutical formulations, methods of manufacture and uses thereof

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-(aminosulfonyl)-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.

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

The present invention relates to the field of anti-viral active agents, particularly to salts, more particularly to a maleate salt of the free base of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide, to pharmaceutical formulations thereof as well as to methods for the production of these salts. The present invention also relates to the use of theses salts and of respective pharmaceutical formulations thereof in methods of treatment and/or prevention of human herpes simplex virus infections, particularly infections caused by HSV-1 and HSV-2.

Maleate salt of the free base of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide, pharmaceutical formulations, methods of manufacture and uses thereof for the treatment of herpes viruses

The present invention relates to field of intravaginally applicable devices that release antiviral compounds. In particular, the present invention relates to vaginal rings comprising a matrix releasing at least one antivirally active compound, in particular anti-herpetic compound N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide (in the following also referred to as 'Pritelivir') or salts thereof. The present invention therefore relates to the treatment and prevention of herpes infections.

Intravaginally applicable devices comprising antiviral compounds

The present invention relates to the field of anti-viral active agents, particularly the free base hemihydrate form of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide as well as methods for the manufacture thereof. The present invention relates also to the use of the above compound in the treatment of human herpes virus infections and in the preparation of pharmaceuticals comprising said compound.

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

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.

The present invention relates to an improved and shortened synthesis of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide and the mesylate monohydrate salt thereof by using boronic acid derivatives or borolane reagents while avoiding toxic organic tin compounds and to the mesylate monohydrate salt of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions.

N-[5-(Aminosulfony1)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate

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Wuppertal, Germany

Alexander Birkmann