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61. 发明公开

EP1767521A4 L-ORNITHINE-CITRIC ACID SALT CRYSTAL 有权
标题翻译： L-鸟氨酸，CITRONENSÄURESALZKRISTALL
公开(公告)号：EP1767521A4
公开(公告)日：2008-03-19
申请号：EP05765086
申请日：2005-06-24
申请人： KYOWA HAKKO KOGYO KK
发明人： MURATA HIDEKI , YAMAMOTO YU
IPC分类号： C07C229/26 , C07C51/41 , C07C51/43 , C07C59/265 , C07C227/16 , C07C227/42 , C07C229/36
CPC分类号： C07C229/26 , C07C51/412 , C07C59/265
摘要： Disclosed are a crystal of a salt composed of L-ornithine and citric acid, a crystal of a salt composed of L-ornithine and citric acid whose 5 weight% aqueous solution has a pH of 3-6, a crystal of a salt composed of L-ornithine and citric acid wherein the composition ratio (molar ratio) between L-ornithine and citric acid is 2:1, a method for producing a crystal of a salt composed of L-ornithine and citric acid which is characterized in that L-ornithine and citric acid are dissolved in water and a crystal is separated from the thus-obtained aqueous solution, and such a method for producing a crystal of a salt composed of L-ornithine and citric acid wherein the aqueous solution has a pH of 3-6.
摘要翻译：本发明公开了L-鸟氨酸和柠檬酸构成的盐的晶体，L-鸟氨酸和柠檬酸，其5重量％的水溶液构成的盐的结晶的pH为3-6，构成的盐的结晶 L-鸟氨酸和柠檬酸，其中间L-鸟氨酸和柠檬酸的组成比（摩尔比）为2：1，一种生产L-鸟氨酸和柠檬酸构成的盐，其特征在于的结晶的方法L- 鸟氨酸和柠檬酸溶解在水中并结晶从由此得到的水溶液中分离，并用于产生L-鸟氨酸和柠檬酸构成的盐的晶体，其中所述水溶液的pH为3-这样的方法 6。

62. 发明授权

EP1334964B1 PROCESS FOR PRODUCING B-FORM NATEGLINIDE CRYSTAL 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG DER B-FORM VON NATEGLINID-KRISTALLEN
公开(公告)号：EP1334964B1
公开(公告)日：2007-08-15
申请号：EP01976819.1
申请日：2001-10-23
申请人： Ajinomoto Co., Inc.
发明人： SUMIKAWA, Michito c/o Tokai Plant , MARUO, Makoto c/o Tokai Plant , MIYAZAKI, Kazuo c/o Tokai Plant , NISHINA, Shigehiro c/o Tokai Plant , MATSUZAWA, Yukiko c/o Tokai Plant
IPC分类号： C07C233/63 , C07C227/42
CPC分类号： C07C231/24 , C07C2601/14 , C07C233/63
摘要： A process for producing B-form nateglinide crystals containing substantially no H-form crystals, which comprises the steps of drying wet crystals of a nateglinide solvate at a low temperature until the solvent disappears and then causing them to undergo a crystal transition. By this process, nateglinide crystals in the B-form only can be produced on an industrial scale.
摘要翻译：提供了一种生产基本不含H型晶体的那格列奈B型晶体的方法，其包括在低温下干燥那格列奈的溶剂化湿的晶体，直到没有溶剂残留并进行晶体转化。根据该方法，可以以工业规模生产那格列奈的B型晶体，而不允许其他形式的结晶多晶型共存。

63. 发明公开

EP1603863A1 PROCESS FOR THE PREPARATION OF AMINO METHYL CYCLO ALKANE ACETIC ACIDS 有权
标题翻译：用于生产AMINOMETHYLCYCLOALKAN乙酸
公开(公告)号：EP1603863A1
公开(公告)日：2005-12-14
申请号：EP02808152.9
申请日：2002-11-20
申请人： Hikal Ltd.
发明人： KUPPUSWAMY, Nagarajan,Hikal R & D centre , HARIHARAN, Sivaramakrishnan,Hikal R & D centre , MARIADAS, Arulselvan,Hikal R & D centre
IPC分类号： C07C227/42 , C07C229/28
CPC分类号： C07C227/18 , C07C227/38 , C07C2601/14 , C07C229/28
摘要： This invention relates to an improved process for the preparation of amino methyl cyclo alkane acetic acids. This invention particularly relates to an improved process for the preparation of gabapentin (which is chemically known as 1-aminomethyl-1-cyclohexaneacetic acid), which is a very well known agent useful for the treatment of epilepsy and other cerebral disorders. In the chemical series of 1-amino methyl cyclo alkane-1-acetic acids, Gabapentin, which is 1-amino methyl cyclo hexane -1-acetic acid has been developed as a drug having anti convulsive properties.

64. 发明授权

EP1033362B1 CRYSTALS OF [S,S]-ETHYLENEDIAMINE-N,N'-DISUCCINIC ACID WITH HIGH BULK DENSITY AND METHOD OF OBTAINING THE SAME 有权
标题翻译： [S，S] - 乙二胺-N，具有高堆积密度和用于生产过程N'-二琥珀酸晶体
公开(公告)号：EP1033362B1
公开(公告)日：2005-05-11
申请号：EP98954716.1
申请日：1998-11-18
申请人： Mitsubishi Rayon Co., Ltd.
发明人： BAMBA, Hiroyasu Mitsubishi Rayon Co., Ltd. Chem. , TANAKA, Shigeho Mitsubishi Rayon Co., Ltd. Chem. , NIWA, Kiyonobu Mitsubishi Rayon Co., Ltd. Chem. , ENDO, Takakazu Mitsubishi Rayon Co., Ltd. Chem.
IPC分类号： C07C229/24 , C07C227/42
CPC分类号： C07C229/24 , C07C227/42
摘要： A method of crystallizing [S,S]-ethylenediamine-N,N'-disuccinic acid, characterized by regulating an aqueous solution of a metal salt of [S,S]-ethylenediamine-N,N'-disuccinic acid so as to have a temperature of 40 to 80 °C and pH of 1.9 to 4.5 and cooling the solution to 40 °C or lower over 0.2 to 10 hours while feeding a mineral acid so as to maintain the pH at 1.9 to 4.5 to thereby crystallize [S,S]-ethylenediamine-N,N'-disuccinic acid. By this method, crystals of [S,S]-ethylenediamine-N,N'-disuccinic acid which have a bulk density of 0.45 to 1.2 g/cm3 can be obtained in a high yield while inhibiting cyclization during the crystallization.

65. 发明公开

EP1468985A1 A process for the preparation of gabapentin free from inorganic acids anions 有权转让
标题翻译：一种用于从无机酸阴离子游离制备加巴喷丁的方法
公开(公告)号：EP1468985A1
公开(公告)日：2004-10-20
申请号：EP04008806.4
申请日：2004-04-14
申请人： FARCHEMIA S.r.l. , ZAMBON GROUP S.p.A.
发明人： Breviglieri, Gabriele , Contrini, Sergio , Assanelli, Cinzia
IPC分类号： C07C229/28 , C07C227/42
CPC分类号： C07C227/40 , C07C65/03 , C07C65/10 , C07C2601/14 , C07C229/28
摘要： Gabapentin free from mineral acids anions is obtained by precipitating from a gabapentin aqueous solution a corresponding hydroxybenzoate, from which pure gabapentin is subsequently obtained by dissolution in a lower alcohol and treatment with a tertiary base.

66. 发明公开

EP1384473A1 Stable gabapentin containing more than 20 ppm of chlorine ion 审中-公开
标题翻译：稳定的加巴喷丁含有超过20 ppm的氯离子
公开(公告)号：EP1384473A1
公开(公告)日：2004-01-28
申请号：EP03022372.1
申请日：2001-06-15
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD.
发明人： Singer, Claude , Pilarski, Gideon , Pesachovich, Michael , Schwarz, Edi
IPC分类号： A61K31/195 , C07C227/42 , C07C229/28
CPC分类号： A61K31/195 , A61K9/2054 , A61K9/2059
摘要： Pharmaceutical compositions containing substantially pure and stable gabapentin are disclosed wherein gabapentin contains an anion of a mineral acid, such as chloride, in amounts greater than 20 ppm.
摘要翻译：公开了含有基本上纯且稳定的加巴喷丁的药物组合物，其中加巴喷丁含有大于20ppm量的无机酸阴离子如氯化物。

67. 发明授权

EP1289364B1 STABLE GABAPENTIN CONTAINING MORE THAN 2O PPM OF CHLORINE ION 无效
标题翻译：稳定的GABAPENTIN含有超过2O ppm的氯离子
公开(公告)号：EP1289364B1
公开(公告)日：2003-12-10
申请号：EP01946364.5
申请日：2001-06-15
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD.
发明人： SINGER, Claude , PILARSKI, Gideon , PESACHOVICH, Michael , SCHWARTZ, Edi
IPC分类号： A61K31/195 , C07C227/42 , C07C229/28
CPC分类号： A61K31/195 , A61K9/2054 , A61K9/2059
摘要： Pharmaceutical compositions containing substantially pure and stable gabapentin are disclosed wherein gabapentin contains an anion of a mineral acid, such as chloride, in amounts greater than 20 ppm.
摘要翻译：公开了含有基本上纯且稳定的加巴喷丁的药物组合物，其中加巴喷丁含有大于20ppm量的无机酸阴离子如氯化物。

68. 发明公开

EP1347951A1 A PROCESS FOR THE PREPARATION OF 1-(AMINOMETHYL) CYCLOHEXANEACETIC ACID 有权
标题翻译：用于生产1-（氨基甲基）cyclohexaneacetic
公开(公告)号：EP1347951A1
公开(公告)日：2003-10-01
申请号：EP01990454.9
申请日：2001-11-29
申请人： ERREGIERRE S.p.A.
发明人： FERRARI, Massimo , GHEZZI, Marcello , BELOTTI, Paolo
IPC分类号： C07C227/42 , C07C227/18
CPC分类号： C07C227/42 , C07C227/18 , C07C2601/14 , C07C229/28
摘要： A conversion process of gabapentin hydrochloride into gabapentin comprising: a) dissolution of gabapentin hydrochloride in a solvent in which the gabapentin hydrochloride and the gabapentin are completely soluble; and b) subsequent addition of an amine that allows the removal of the chloride ion from the solution containing gabapentin hydrochloride, by precipitation of the hydrochloride of the same amine, leaving the gabapentin in solution in free amino acid form.

69. 发明公开

EP1289364A4 STABLE GABAPENTIN CONTAINING MORE THAN 2O PPM OF CHLORINE ION 无效
标题翻译：加巴喷丁STABLE大于20ppm的氯
公开(公告)号：EP1289364A4
公开(公告)日：2003-08-06
申请号：EP01946364
申请日：2001-06-15
申请人： TEVA PHARMA
发明人： SINGER CLAUDE , PILARSKI GIDEON , PESACHOVICH MICHAEL
IPC分类号： A61K9/20 , A61K31/195 , C07C227/42 , C07C229/28
CPC分类号： A61K31/195 , A61K9/2054 , A61K9/2059
摘要： Pharmaceutical compositions containing substantially pure and stable gabapentin are disclosed wherein gabapentin contains an anion of a mineral acid, such as chloride, in amounts greater than 20 ppm.

70. 发明公开

EP0903337A4 PROCESS FOR THE PREPARATION OF 1-ALKOXYCARBONYL-3-PHENYLPROPYL DERIVATIVES 失效
标题翻译： VERFAHREN ZUR HERSTELLUNG VON 1-ALKOXYCARBONY-3-PHENYLPROPYLDERIVATEN
公开(公告)号：EP0903337A4
公开(公告)日：2001-02-28
申请号：EP97918383
申请日：1997-05-08
申请人： KANEKA CORP
发明人： UEDA YASUYOSHI , MATSUMOTO AKIRA , MANABE HAJIME
IPC分类号： C07D233/36 , B01J23/44 , C07B61/00 , C07C227/16 , C07C227/42 , C07C229/36 , C07C237/12 , C07D209/42 , C07D209/52 , C07D215/48 , C07D217/26 , C07D223/16 , C07D285/12 , C07D453/02 , C07D495/10 , C07K1/113 , C07K5/02 , C07K5/062 , C07K5/078 , C07K5/068
CPC分类号： C07C227/42 , C07C227/16 , C07K5/022 , C07K5/0222 , C07K5/06139 , Y02P20/55 , C07C229/36
摘要： A simple, efficient and high-productivity process for preparing high-quality 1-alkoxycarbonyl-3-phenylpropyl derivatives containing few impurities by catalytic reduction of 1-alkoxycarbonyl-3-oxo-3-phenylpropyl derivatives.
摘要翻译：式（II）的1-烷氧基羰基-3-苯基丙基衍生物的制备包括在3当量的强酸存在下催化还原式（I）的1-烷氧基 - 羰基-3-氧代-3-苯基丙基衍生物，任选地在包含醇或醇中的0.4-0.5N酸的溶剂中。制备式（III）的1-烷氧基羰基-3-苯基丙基副产物被抑制。 R =烷基; X = Ala，Gly，Leu，Ile，Val或Hly（sic），Orn（sic）或任选通过酰基保护在ω-氨基上的Lys; Y = OH，Ala，Gly，Leu，Ile，Val，Pro或式（i） - （iv）的基团; 或X + Y =式（xi）或（xii）的基团。

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