C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 235/08 (2006.01) A61K 31/404 (2006.01) A61K 31/415 (2006.01) A61K 31/4184 (2006.01) C07D 209/08 (2006.01) C07D 209/10 (2006.01)
Patent
CA 2350520
3-(2,4-Dichlorobenzyl)-2-methyl-N-(pentylsulfonyl)-3H-benzimidazole-5- carboxamide having a hypoglycemic activity or a PDE5 inhibitory effect occurs as three crystalline forms which are distinguishable from each other based on the powdery X-ray diffraction data. The most stable crystalline form thereof is useful as a bulk powder for drugs. Other crystalline forms comprise larger crystals, which can be very easily isolated by filtration and efficiently purified by crystallization, are useful in purifying 3-(2,4-dichlorobenzyl)-2- methyl-N-(pentylsulfonyl)-3H-benzimidazole-5-carboxamide.
L'invention concerne un 3-(2,4-dichlorobenzyl)-2-méthyl-N-(pentylsulfonyl)-3H-benzimidazole-5-carboxamide possédant une activité hypoglycémique ou un effet d'inhibition de la phosphodiestérase 5 (PDE5), et se présentant sous trois formes cristallines se distinguant les unes des autres en fonction des données de diffraction des rayons X sur la matière pulvérulente. La forme cristalline la plus stable de ce carboxamide est utile en tant que poudre en vrac destinée à des médicaments. D'autres formes cristallines comprenant des cristaux plus grands, que l'on peut très facilement isoler par filtration et purifier de manière efficace par cristallisation, sont utiles pour purifier du 3-(2,4-dichlorobenzyl)-2-méthyl-N-(pentylsulfonyl)-3H-benzimidazole-5-carboxamide.
Dohtsu Kunihiko
Imoto Takafumi
Murai Yoshiyuki
Nishikawa Masahiro
Yamasaki Noritsugu
Astellas Pharma Inc.
Daicel Chemical Industries Ltd.
Fujisawa Pharmaceutical Co. Ltd.
Smart & Biggar
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