CA2939529A1 - N-[5-(aminosulfonyle)-4-methyle-1,3-thiazol-2-yl]-n-methyle-2-[4-(2-pyridine yl)phenyle]acetamide mesylate monohydrate - Google Patents

N-[5-(aminosulfonyle)-4-methyle-1,3-thiazol-2-yl]-n-methyle-2-[4-(2-pyridine yl)phenyle]acetamide mesylate monohydrate Download PDF

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Publication number
CA2939529A1
CA2939529A1 CA2939529A CA2939529A CA2939529A1 CA 2939529 A1 CA2939529 A1 CA 2939529A1 CA 2939529 A CA2939529 A CA 2939529A CA 2939529 A CA2939529 A CA 2939529A CA 2939529 A1 CA2939529 A1 CA 2939529A1
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Prior art keywords
methyl
thiazol
phenyl
pyridinyl
acetamide
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Granted
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CA2939529A
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English (en)
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CA2939529C (fr
Inventor
Alexander Birkmann
Alfons Grunenberg
Dieter Haag
Birgit D.I. Keil
Andreas Lender
Stephan Mass
Kerstin Paulus
Joachim Rehse
Kristian Ruepp
Wilfried Schwab
Kurt Vogtli
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AIC316 GmbH
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Aicuris GmbH and Co KG
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Filing date
Publication date
Priority claimed from EP11007803A external-priority patent/EP2573085A1/fr
Priority claimed from EP11007823A external-priority patent/EP2573086A1/fr
Application filed by Aicuris GmbH and Co KG filed Critical Aicuris GmbH and Co KG
Publication of CA2939529A1 publication Critical patent/CA2939529A1/fr
Application granted granted Critical
Publication of CA2939529C publication Critical patent/CA2939529C/fr
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Abstract

La présente invention porte sur une synthèse améliorée et raccourcie de N -[5-aminosulfonyI)-4-méthyl-1 ,3-thiazol-2-yl]-N-méthyl-2-[4-(2- pyridinyl)phényl] acétamide et de sont sel monohydrate mésylate en utilisant des dérivés dacide borique et des réactifs de borolane tout en évitant les composés de fer organiques toxiques et le sel monohydrate de mésylate de N-[5-(aminosulfonyl)-4-méthyl-1,3-thiazol-2-yl] -N-méthyl-2-[4-(2-pyridinyl)phényl]acétamide qui a démontré une stabilité accrue à long terme et des propriétés cinétiques de libération des compositions pharmaceutiques. La présente invention porte également sur le sel monohydrate de mésylate cristallin de N-[5-(aminosulfonyl)-4-méthyl-1, 3-thiazol-2-yl]-N-méthyl-2-[4-(2- pyridinyl)phényl] acétamide dans une distribution de tailles de particules définie et une plage de zone de surface spécifique, qui a démonté une stabilité à long terme accrue et des propriétés cinétiques de libération des compositions pharmaceutiques renfermant ledit monohydrate de mésylate N-[5-(aminosulfonyl)-4-méthyl-1,3-thiazol-2-yl]-N-méthyl-2-[4- (2-pyridinyl) phényl]acétamide ayant la distribution de tailles de particules et la plage de zone de surface spécifique mentionnées.
CA2939529A 2011-09-26 2012-09-26 N-[5-(aminosulfonyle)-4-methyle-1,3-thiazol-2-yl]-n-methyle-2-[4-(2-pyridine yl)phenyle]acetamide mesylate monohydrate Active CA2939529C (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP11007803A EP2573085A1 (fr) 2011-09-26 2011-09-26 Monohydrate de mesylate acétamide N-[5-(aminosulfonyl)-4méthyl-1,3-thiazol-2-yl]-N-méthyl-2-[4-(2-pyridinyl)phényl] disposant d'une gamme de distribution de taille de particules spécifiques et portée de surface spécifique
EP11007803.7 2011-09-26
EP11007823A EP2573086A1 (fr) 2011-09-26 2011-09-26 Monohydrate de mesylate acétamide N-[5-(Aminosulfonyl)-4-méthyl-1,3-thiazol-2-yl]-N-méthyl-2-[4-(2-pyridinyl)phényl]
EP11007823.5 2011-09-26
CA2791142A CA2791142C (fr) 2011-09-26 2012-09-26 N-[5-(aminosulfonyle)-4-methyle-1,3-thiazol-2-yl]-n-methyle-2-[4-(2-pyridine yl)phenyle]acetamide mesylate monohydrate

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CA2791142A Division CA2791142C (fr) 2011-09-26 2012-09-26 N-[5-(aminosulfonyle)-4-methyle-1,3-thiazol-2-yl]-n-methyle-2-[4-(2-pyridine yl)phenyle]acetamide mesylate monohydrate

Publications (2)

Publication Number Publication Date
CA2939529A1 true CA2939529A1 (fr) 2013-03-26
CA2939529C CA2939529C (fr) 2018-07-03

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CA2939529A Active CA2939529C (fr) 2011-09-26 2012-09-26 N-[5-(aminosulfonyle)-4-methyle-1,3-thiazol-2-yl]-n-methyle-2-[4-(2-pyridine yl)phenyle]acetamide mesylate monohydrate

Country Status (1)

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CA (1) CA2939529C (fr)

Also Published As

Publication number Publication date
CA2939529C (fr) 2018-07-03

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Publication Publication Date Title
CA2791142C (fr) N-[5-(aminosulfonyle)-4-methyle-1,3-thiazol-2-yl]-n-methyle-2-[4-(2-pyridine yl)phenyle]acetamide mesylate monohydrate
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EP2598502B1 (fr) Monohydrate de mesylate acétamide n-[5-(aminosulfonyl)-4méthyl-1,3-thiazol-2-yl]-n-méthyl-2-[4-(2-pyridinyl)phényl] disposant d'une gamme de distribution de taille de particules spécifiques et portée de surface spécifique
CA2939529A1 (fr) N-[5-(aminosulfonyle)-4-methyle-1,3-thiazol-2-yl]-n-methyle-2-[4-(2-pyridine yl)phenyle]acetamide mesylate monohydrate
HK1196017A (en) N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-n-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate having a specific particle size distribution range and a specific surface area range for use in pharmaceutical formulations
HK1196017B (en) N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-n-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate having a specific particle size distribution range and a specific surface area range for use in pharmaceutical formulations
NZ621615B2 (en) N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-n-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate

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