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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, pharmaceutical formulations, methods of manufacture and uses thereof for the treatment of herpes viruses

A technology for maleate salts and pharmaceutical preparations, used in drug delivery, antiviral agents, pharmaceutical formulations, etc., to achieve the effects of high therapeutically effective concentration, high purity, and significant photostability

Active Publication Date: 2019-07-26
AICURIS GMBH & CO KG
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although the physicochemical stability of the compound prelimovir has been quite good, the compound also exhibits UV absorption

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  • 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, pharmaceutical formulations, methods of manufacture and uses thereof for the treatment of herpes viruses
  • 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, pharmaceutical formulations, methods of manufacture and uses thereof for the treatment of herpes viruses
  • 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, pharmaceutical formulations, methods of manufacture and uses thereof for the treatment of herpes viruses

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Embodiment Construction

[0055] Before describing the invention in detail, it is considered advantageous to provide definitions for certain technical terms used throughout the description. While the invention will be described with respect to particular embodiments, such description should not be construed in a limiting sense. Before describing the exemplary embodiments of the present invention in detail, definitions important for understanding the present invention are given.

[0056] definition

[0057] In the context of the present invention, the term "prelavir" refers to the compound N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2 -[4-(2-Pyridyl)-phenyl]acetamide itself. That is, expressions such as "free base of prelavivir" or similar expressions refer to the compound N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N - The free base of methyl-2-[4-(2-pyridyl)-phenyl]acetamide. Similarly, the mesylate salt of Prelivir refers to the compound N-[5-(aminosulfonyl)-4-methyl-1,3-thiazo...

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Abstract

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.

Description

technical field [0001] The present invention relates to the field of antiviral active agents, in particular to N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4- (2-pyridyl)-phenyl]acetamide (this acetamide compound may also be referred to as "prelavivir" hereinafter) free base salt, more particularly the maleate salt, pharmaceutical preparations thereof and Methods of production of these salts. The present invention also relates to the use of said salt, especially said maleate and its corresponding pharmaceutical preparations in the treatment and / or prevention of human herpes simplex virus infection. Background technique [0002] N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridyl)-phenyl]acetamide ( "Prellivir"), its free base and mesylate salt are known antiviral compounds used in the treatment of herpes simplex virus (herpes simplex virus 1 and 2, respectively; hereinafter abbreviated as HSV-1 and HSV-2), as disclosed in WO2006 / 103011A...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/12A61K31/4427A61P31/22
CPCA61P31/22C07D417/12A61K9/0014A61K31/4439A61K45/06
Inventor 约戈什瓦尔·巴克哈夫维尔弗里德·施瓦布亚历山大·比克曼苏珊娜·邦斯曼托马斯·戈德纳
Owner AICURIS GMBH & CO KG
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