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1. 发明专利

JP2008163016A Method for producing cyclohexanediamine monoamide derivative, and intermediate 审中-公开
标题翻译：生产环己烷氨基甲酰胺衍生物的方法和中间体
公开(公告)号：JP2008163016A
公开(公告)日：2008-07-17
申请号：JP2007315975
申请日：2007-12-06
申请人： Arena Pharmaceuticals Inc , Taisho Pharmaceutical Co Ltd , アリーナファーマシューチカルズインコーポレーテッド , 大正製薬株式会社
发明人： MANNAKA AKIRA , ISHII TAKAAKI , SAKUTE TARO , SHIKANUMA KOSUKE , OMODERA KATSUNORI
IPC分类号： C07C231/02 , A61K31/44 , A61P25/22 , A61P25/24 , A61P43/00 , C07C233/74 , C07C233/79 , C07C233/81 , C07C247/14 , C07C309/66 , C07D213/44
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a cis-1,4-cyclohexanediamine monoamide derivative useful as MCH (melanin-concentrating hormone) 1 receptor antagonist, being inexpensive and suitable for mass production and to provide an efficient dimetylamination method of chloropyrimidine and to provide a new intermediate compound produced in those production processes.
SOLUTION: The method for producing a compound represented by formula (I) (wherein R
1 are same or different and they are each a phenyl group which may have one to five substituents selected from the group consisting of a hydrogen atom, a halogen atom, a 1-6C alkyl group, a 1-6C alkoxy group, a 2-7C alkoxycarbonyl group, an acetyl group and a cyano group) comprises the steps amidating a compound represented by formula (II) and further converting a carboxy group to an amino group.
COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供可用作MCH（黑色素浓缩激素）1受体拮抗剂的顺式-1,4-环己烷二胺单酰胺衍生物的方法，其成本低廉并且适于批量生产并提供有效的二甲基胺并提供在这些生产工艺中生产的新的中间体化合物。解决方案：由式（I）表示的化合物（其中R 1和R 2相同或不同）的制备方法，它们各自为可以具有一至五个选自下列基团的取代基的苯基：由氢原子，卤素原子，1-6C烷基，1-6C烷氧基，2-7C烷氧基羰基，乙酰基和氰基组成）包括将由式（II）表示的化合物）并进一步将羧基转化为氨基。版权所有（C）2008，JPO＆INPIT

2. 发明专利

JP2009107997A Crystal of (1s)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-d-glucitol, and method for preparing the same 审中-公开
标题翻译：（1S）-1,5-壬基-1- [5-（4-乙氧基苄基）-2-甲氧基-4-甲基苯基] -1-硫代-D-葡萄糖醇的晶体及其制备方法
公开(公告)号：JP2009107997A
公开(公告)日：2009-05-21
申请号：JP2007283982
申请日：2007-10-31
申请人： Taisho Pharmaceutical Co Ltd , 大正製薬株式会社
发明人： OGINO NARUMI , NISHIMURA CHIENO , SAKUTE TARO , MANNAKA AKIRA
IPC分类号： C07D335/02 , A61K31/382 , A61P3/10
摘要： PROBLEM TO BE SOLVED: To provide a method of preparing a crystal of (1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol which is stable in an environment wherein the compound is used as a medicine, and a crystal of (1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol having a specific crystal structure that enables the rapid elution thereof as a solid pharmaceutical preparation, and a method for preparing the same.
SOLUTION: Disclosed is a method of preparing a crystal having at least one of the following physical properties (a) to (c) as described below, which method is characterized by comprising a process of dissolving a (1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol into a liquid mixture of water and an organic solvent having characteristics of intermingling with water, a process of subsequently crystallizing the same at a temperature of 5 to 70°C, and a process of drying the resulting crystal at a temperature of not higher than 50°C. (a) Its powder X-ray diffraction spectrum (Cu-Kα) has peaks at diffraction angles 2θ=3.2°, 9.6°, 11.1°, and 15.5°; (b) its infrared absorption spectrum has characteristic absorption bands at 2,977 cm
-1 , 1,510 cm
-1 , 1,244 cm
-1 , 1,091 cm
-1 , 1,053 cm
-1 and 773 cm
-1 ; and (c) its melting point is 156 to 160°C.
COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供制备（1S）-1,5-脱水-1- [5-（4-乙氧基苄基）-2-甲氧基-4-甲基苯基] -1-硫基的晶体的方法（1S）-1,5-脱水-1- [5-（4-乙氧基苄基）-2-甲氧基-4-三氟甲磺酸的结晶，其在化合物用作药物的环境中是稳定的，具有能够作为固体药物制剂快速洗脱的特定结晶结构的甲基苯基] -1-硫代-D-葡萄糖醇及其制备方法。解决方案：公开了一种制备具有如下所述的以下物理性质（a）至（c）中的至少一种的晶体的方法，该方法的特征在于包括将（1S）-1， 5-脱水-1- [5-（4-乙氧基苄基）-2-甲氧基-4-甲基苯基] -1-硫代-D-葡萄糖醇转化为具有与水混合的特性的水和有机溶剂的液体混合物，随后在5至70℃的温度下使其结晶，以及在不高于50℃的温度下干燥所得晶体的方法。（a）其粉末X射线衍射光谱（Cu-Kα）在衍射角2θ= 3.2°，9.6°，11.1°和15.5°处具有峰值; （b）其红外吸收光谱在2,977厘米 -1 ，1,510厘米 -1 ，1,244厘米 -1 ，1,091厘米 -1 ，1,053厘米 -1 和773厘米 -1 ; 和（c）其熔点为156〜160℃。版权所有（C）2009，JPO＆INPIT

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