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 incre...

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Hauptverfasser:	VOGTLI KURT, PAULUS KERSTIN, SCHWAB WILFRIED, MAAS STEPHAN, BIRKMANN ALEXANDER, HAAG DIETER, RUEPP KRISTIAN
Format:	Patent
Sprache:	eng
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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creator	VOGTLI KURT PAULUS KERSTIN SCHWAB WILFRIED MAAS STEPHAN BIRKMANN ALEXANDER HAAG DIETER RUEPP KRISTIAN
description	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.
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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.</description><language>eng</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><creationdate>2015</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20150901&DB=EPODOC&CC=US&NR=9119786B2$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20150901&DB=EPODOC&CC=US&NR=9119786B2$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>VOGTLI KURT</creatorcontrib><creatorcontrib>PAULUS KERSTIN</creatorcontrib><creatorcontrib>SCHWAB WILFRIED</creatorcontrib><creatorcontrib>MAAS STEPHAN</creatorcontrib><creatorcontrib>BIRKMANN ALEXANDER</creatorcontrib><creatorcontrib>HAAG DIETER</creatorcontrib><creatorcontrib>RUEPP KRISTIAN</creatorcontrib><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 pharmaceutical formulations</title><description>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.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2015</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNjjtPA0EMhNNQIOA_uAwSLu4SHmmJQFRpgCqKInPny1ral9Z7SJv_jsSeCBIl1dj6ZsY-n32tU9FM1opn2OD2FufkxAcd7RB8sde4RMfZFIvNzQKzEToGiy0Wu8PNL2pxu8R5i7Ek6WWKRcNVdtRxrn09gws-gGMtlvLPZkqfptnQp_gDEGjkTgbpIFLK0lkGlSNDL5qTfIxZgodE_sBAvv_r1zEN9RJQYjo5hpBgVAbxEA0lV3Et6MhOxI31idqml7Ozgazy1UkvZvD89LZ-QY5hzxprynPev7-ummZ1_3D32C7-YfkGvvZ2gQ</recordid><startdate>20150901</startdate><enddate>20150901</enddate><creator>VOGTLI KURT</creator><creator>PAULUS KERSTIN</creator><creator>SCHWAB WILFRIED</creator><creator>MAAS STEPHAN</creator><creator>BIRKMANN ALEXANDER</creator><creator>HAAG DIETER</creator><creator>RUEPP KRISTIAN</creator><scope>EVB</scope></search><sort><creationdate>20150901</creationdate><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 pharmaceutical formulations</title><author>VOGTLI KURT ; PAULUS KERSTIN ; SCHWAB WILFRIED ; MAAS STEPHAN ; BIRKMANN ALEXANDER ; HAAG DIETER ; RUEPP KRISTIAN</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_US9119786B23</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2015</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><toplevel>online_resources</toplevel><creatorcontrib>VOGTLI KURT</creatorcontrib><creatorcontrib>PAULUS KERSTIN</creatorcontrib><creatorcontrib>SCHWAB WILFRIED</creatorcontrib><creatorcontrib>MAAS STEPHAN</creatorcontrib><creatorcontrib>BIRKMANN ALEXANDER</creatorcontrib><creatorcontrib>HAAG DIETER</creatorcontrib><creatorcontrib>RUEPP KRISTIAN</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>VOGTLI KURT</au><au>PAULUS KERSTIN</au><au>SCHWAB WILFRIED</au><au>MAAS STEPHAN</au><au>BIRKMANN ALEXANDER</au><au>HAAG DIETER</au><au>RUEPP KRISTIAN</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><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 pharmaceutical formulations</title><date>2015-09-01</date><risdate>2015</risdate><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-(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. 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subjects	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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 pharmaceutical formulations
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