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1. WO2006101082 - PYRIMIDINE COMPOUND CRYSTAL OR AMORPHOUS FORM AND PROCESS FOR PRODUCING THE SAME

Publication Number WO/2006/101082
Publication Date 28.09.2006
International Application No. PCT/JP2006/305565
International Filing Date 20.03.2006
IPC
C07D 405/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14containing three or more hetero rings
C07D 405/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
CPC
A61P 1/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
10Laxatives
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
C07D 405/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14containing three or more hetero rings
Applicants
  • エーザイ・アール・アンド・ディー・マネジメント株式会社 Eisai R & D Management Co., Ltd. [JP]/[JP] (AllExceptUS)
  • 原田 均 HARADA, Hitoshi [JP]/[JP] (UsOnly)
  • 石原 比呂之 ISHIHARA, Hiroshi [JP]/[JP] (UsOnly)
  • 佐藤 義明 SATO, Yoshiaki [JP]/[JP] (UsOnly)
  • 千葉 博之 CHIBA, Hiroyuki [JP]/[JP] (UsOnly)
  • 小松 雄毅 KOMATSU, Yuki [JP]/[JP] (UsOnly)
  • 井上 晋 INOUE, Susumu [JP]/[JP] (UsOnly)
  • 尾関 直樹 OZEKI, Naoki [JP]/[JP] (UsOnly)
Inventors
  • 原田 均 HARADA, Hitoshi
  • 石原 比呂之 ISHIHARA, Hiroshi
  • 佐藤 義明 SATO, Yoshiaki
  • 千葉 博之 CHIBA, Hiroyuki
  • 小松 雄毅 KOMATSU, Yuki
  • 井上 晋 INOUE, Susumu
  • 尾関 直樹 OZEKI, Naoki
Agents
  • 長谷川 芳樹 HASEGAWA, Yoshiki
Priority Data
60/66358021.03.2005US
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) PYRIMIDINE COMPOUND CRYSTAL OR AMORPHOUS FORM AND PROCESS FOR PRODUCING THE SAME
(FR) CRISTAL OU FORME AMORPHE D’UN COMPOSE DE PYRIMIDINE ET PROCEDE POUR LES PRODUIRE
(JA) ピリミジン化合物の結晶、非晶質および製造方法
Abstract
(EN)
Crystal of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1- methylpyridin-2(1H)-one exhibiting, in powder X-ray diffractometry, diffraction peaks at diffraction angles (2&thetas;±0.2°) of 9.7° and/or 21.9°. This crystal is suitable for use as an active ingredient of preventive/therapeutic agents for diseases, such as costiveness. Further, a hydrate of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one and 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1- methylpyridin-2(1H)-one in amorphous form are also suitable for use as an active ingredient of preventive/therapeutic agents for diseases, such as costiveness.
(FR)
L’invention décrit un cristal de la 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-méthylpyridin-2(1H)-one présentant, lors d’une analyse par diffraction X sur poudre, des pics de diffraction aux angles de diffraction (2&thetas; ± 0,2°) 9,7° et/ou 21,9°. Ce cristal est approprié pour être utilisé en tant que principe actif dans des agents préventifs/thérapeutiques pour des troubles tel que la production de scybales. En outre, un hydrate de la 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-méthylpyridin-2(1H)-one et la 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-méthylpyridin-2(1H)-one sous sa forme amorphe sont également appropriés pour être utilisés en tant que principe actif dans des agents préventifs/thérapeutiques pour des maladies telles que la production de scybales.
(JA)
 粉末X線回折において、回折角度(2θ±0.2°)9.7°および/または21.9°に回折ピークを有する5-[2-アミノ-4-(2-フリル)ピリミジン-5-イル]-1-メチルピリジン-2(1H)-オンの結晶は、便秘症等の疾患の予防・治療剤の有効成分として適している。また、5-[2-アミノ-4-(2-フリル)ピリミジン-5-イル]-1-メチルピリジン-2(1H)-オン水和物および5-[2-アミノ-4-(2-フリル)ピリミジン-5-イル]-1-メチルピリジン-2(1H)-オンの非晶質も、便秘症等の疾患の予防・治療剤の有効成分として適している。
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