公开(公告)号：EP2269982A4

公开(公告)日：2014-03-12

申请号：EP09724232

申请日：2009-03-18

申请人： KYORIN SEIYAKU KK

发明人： KOMATSU HIDETAKA ,  SATOH HIROYA

IPC分类号： C07C319/28 ,  C07C323/32

CPC分类号： C07C319/28 ,  C07B2200/13 ,  C07C323/32

摘要： The present invention herein provides a method for highly efficiently preparing high purity crystals of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-ethyl]-1,3-propanediol hydrochloride. The method comprises the following steps: (1) dissolving 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol in a mixed solvent comprising a solvent in which the compound in the form of the hydrochloride thereof is highly soluble and a solvent in which the compound in its hydrochloride is less soluble, to thus prepare a solution of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol; and then (2) adding hydrochloric acid to the resultant solution with stirring, to thus crystallize the hydrochloride of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol.

摘要翻译： 本发明提供了高效制备2-氨基-2- [2- [4-（3-苄氧基苯硫基）-2-氯苯基] - 乙基] -1,3-丙二醇盐酸盐的高纯度晶体的方法。 该方法包括以下步骤：（1）将2-氨基-2- [2-（4-（3-苄氧基苯硫基）-2-氯苯基]乙基] -1,3-丙二醇溶于包含其中的溶剂的混合溶剂中， 其盐酸盐形式的化合物是高度可溶的，其中其盐酸盐中的化合物较不溶解的溶剂，从而制备2-氨基-2- [2- [4-（3-苄氧基苯硫基） - 2-氯苯基]乙基] -1,3-丙二醇; 然后（2）在搅拌下向所得溶液中加入盐酸，从而使2-氨基-2- [2- [4-（3-苄氧基苯硫基）-2-氯苯基]乙基] -1,3- 丙二醇。

公开(公告)号：EP0881219A4

公开(公告)日：2000-01-26

申请号：EP96942555

申请日：1996-12-16

申请人： KYORIN SEIYAKU KK

发明人： MAEDA TOSHIO ,  NOMURA MASAHIRO ,  AWANO KATSUYA ,  KINOSHITA SUSUMU ,  SATOH HIROYA ,  MURAKAMI KOJI ,  TSUNODA MASAKI

IPC分类号： C07D277/20 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61P3/06 ,  A61P3/08 ,  A61P43/00 ,  C07D277/34 ,  C07D417/12

CPC分类号： C07D417/12 ,  C07D277/34

摘要： Novel N-substituted dioxothiazolidylbenzamide derivatives having an improved insulin resistance and potent hypoglycemic and hypolipidemic effects and represented by general formula (1), wherein R?1 and R2¿ may be the same or different and each represents hydrogen, C¿1-4? alkyl, C1-3 alkoxy, C1-3 haloalkyl, C1-3 haloalkoxy, halogeno, or hydroxy, or R?1 and R2¿ are bonded to each other to thereby form methylenedioxy; R3 represents hydrogen, C¿1-3? alkoxy, hydroxy, or halogeno; R?4¿ represents hydrogen or C¿1-3? alkyl; n represents an integer of 0 to 2; and X represents N or CH.

公开(公告)号：EP1219595A4

公开(公告)日：2004-08-18

申请号：EP00956871

申请日：2000-09-01

申请人： KYORIN SEIYAKU KK

发明人： SATOH HIROYA ,  KOMURO MASAKATSU ,  MURAKAMI KOJI ,  AWANO KATSUYA

IPC分类号： A61P3/06 ,  A61P3/10 ,  A61P43/00 ,  C07C235/60 ,  C07C317/46 ,  C07C323/60 ,  A61K31/166 ,  A61K31/192 ,  A61K31/235

CPC分类号： C07C317/46 ,  C07C235/60 ,  C07C323/60

摘要： o-Anisamide derivatives which serve as peroxisome proliferator-activated receptor (PPAR) agonists, in particular human PPAR agonists, and are efficacious in preventing and/or treating metabolic diseases in which they participate (hyperlipemia, diabetes, etc.), acid addition salts thereof and a process for producing the same. Namely, o-anisamide derivatives represented by general formula (1), pharmaceutically acceptable salts thereof and hydrates of the same, wherein R represents carboxy, carboxymethyl, CH2CHXCOY (wherein X represents mercapto or S(O)nMe wherein n is 0, 1 or 2; and Y represents amino or hydroxy).

公开(公告)号：EP0846693A4

公开(公告)日：1999-03-03

申请号：EP96920002

申请日：1996-05-30

申请人： KYORIN SEIYAKU KK

发明人： MAEDA TOSHIO ,  NOMURA MASAHIRO ,  AWANO KATSUYA ,  KINOSHITA SUSUMU ,  SATOH HIROYA ,  MURAKAMI KOJI ,  TSUNODA MASAKI

IPC分类号： C07D277/20 ,  A61K31/425 ,  A61K31/426 ,  A61P3/06 ,  A61P3/08 ,  A61P3/10 ,  C07C67/347 ,  C07C69/76 ,  C07C69/84 ,  C07C69/92 ,  C07D277/34 ,  C07D417/12

CPC分类号： C07D417/12 ,  C07D277/34

摘要： Novel N-benzyldioxothiazolidylbenzamide derivatives represented by general formula (1) which improve insulin resistance and have potent hypoglycemic and lipid-lowering effects, wherein R?1 and R2¿ are the same or different and each represents hydrogen, lower (C¿1-4?) alkyl, lower (C1-3) alkoxy, lower (C1-3) haloalkyl, lower (C1-3) haloalkoxy, halogeno, hydroxy, nitro, amino optionally substituted by lower (C1-3) alkyl or a heterocycle, or R?1 and R2¿ may be bonded to each other to thereby form methylenedioxy; R3 represents lower (C¿1-3?) alkoxy, hydroxy or halogeno; and --- represents a double or single bond.