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1. (WO2000029383) CRYSTALLINE FORMS OF 3-(2,4-DICHLOROBENZYL)-2-METHYL-N-(PENTYLSULFONYL)-3H-BENZIMIDAZOLE-5-CARBOXAMIDE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2000/029383    International Application No.:    PCT/JP1999/006296
Publication Date: 25.05.2000 International Filing Date: 11.11.1999
Chapter 2 Demand Filed:    18.05.2000    
IPC:
A61K 31/404 (2006.01), A61K 31/415 (2006.01), C07D 209/08 (2006.01), C07D 209/10 (2006.01), C07D 235/08 (2006.01)
Applicants: FUJISAWA PHARMACEUTICAL CO., LTD. [JP/JP]; 4-7, Dosho-machi 3-chome Chuo-ku Osaka-shi Osaka 541-8514 (JP) (For All Designated States Except US).
DAICEL CHEMICAL INDUSTRIES, LTD. [JP/JP]; 1, Teppo-cho Sakai-shi Osaka 590-0905 (JP) (For All Designated States Except US).
MURAI, Yoshiyuki [JP/JP]; (JP) (For US Only).
YAMASAKI, Noritsugu [JP/JP]; (JP) (For US Only).
IMOTO, Takafumi [JP/JP]; (JP) (For US Only).
NISHIKAWA, Masahiro [JP/JP]; (JP) (For US Only).
MITITSU, Kunihiko [JP/JP]; (JP) (For US Only)
Inventors: MURAI, Yoshiyuki; (JP).
YAMASAKI, Noritsugu; (JP).
IMOTO, Takafumi; (JP).
NISHIKAWA, Masahiro; (JP).
MITITSU, Kunihiko; (JP)
Agent: SHIMIZU, Hatsushi; Kantetsu Tsukuba Building 6F 1-1-1, Oroshi-machi Tsuchiura-shi Ibaraki 300-0847 (JP)
Priority Data:
10/324026 13.11.1998 JP
Title (EN) CRYSTALLINE FORMS OF 3-(2,4-DICHLOROBENZYL)-2-METHYL-N-(PENTYLSULFONYL)-3H-BENZIMIDAZOLE-5-CARBOXAMIDE
(FR) FORMES CRISTALLINES DU 3-(2,4-DICHLOROBENZYL)-2-METHYL-N-(PENTYLSULFONYL)-3H-BENZIMIDAZOLE-5-CARBOXAMIDE
Abstract: front page image
(EN)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.
(FR)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.
Designated States: AE, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CR, CU, CZ, DE, DK, DM, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, ZW.
African Regional Intellectual Property Organization (GH, GM, KE, LS, MW, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG).
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)