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1. 发明专利

JP2010013369A Method for producing pyrazine derivative 审中-公开
标题翻译：生产吡嗪衍生物的方法
公开(公告)号：JP2010013369A
公开(公告)日：2010-01-21
申请号：JP2008172641
申请日：2008-07-01
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： ORII RYOKI , MATSUBARA HIROMASU , KIKUCHI TAKASHI , HASHIMOTO NORIO , GOSHIMA SHUNSUKE
IPC分类号： C07D403/04 , A61K31/497 , A61K31/501 , A61P9/10 , A61P25/04 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D401/04
摘要： PROBLEM TO BE SOLVED: To provide another method for more safely producing an 2-aminopyrazine derivative known as a medicine, especially an adenosine antagonist, in shortened total processes and in a higher total yield than those of known methods for producing the derivative; an intermediate thereof; and a method for producing the intermediate.
SOLUTION: The inventors have zealously examined another method for producing the 2-aminopyrazine derivative, and has consequently found that a pyrazine ring can safely and efficiently be constructed by reacting a pyridazinone derivative whose adjacent carbon atoms are diketone or its salt with a diaminopropionic acid derivative or its salt, and that the 2-aminopyrazine derivative can efficiently be produced by adopting the pyrazine compound obtained by the reaction or its salt as an intermediate. Thus, the present invention has been completed.
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供另一种更为安全地生产称为药物，特别是腺苷拮抗剂的2-氨基吡嗪衍生物的方法，其缩短的总方法和总产率高于已知制备衍生物的方法 ; 其中间体; 和中间体的制造方法。解决方案：本发明人热切地研究了用于制备2-氨基吡嗪衍生物的另一种方法，因此发现吡嗪环可以安全有效地通过使相邻的碳原子为二酮或其盐的哒嗪酮衍生物与二氨基丙酸衍生物或其盐，并且2-氨基吡嗪衍生物可以通过采用通过反应获得的吡嗪化合物或其盐作为中间体而有效地制备。因此，本发明已经完成。版权所有（C）2010，JPO＆INPIT

2. 发明专利

JP2010077031A MANUFACTURING METHOD OF 4-HALO-1H-PYRROLO[2,3-b]PYRIDINE-5-CARBOXYLIC ACID OR SALT THEREOF 审中-公开
标题翻译： 4-HALO-1H-吡咯并[2,3-b]吡啶-5-羧酸或其盐的制备方法
公开(公告)号：JP2010077031A
公开(公告)日：2010-04-08
申请号：JP2008244137
申请日：2008-09-24
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： KIKUCHI TAKASHI , KITAMURA TAKESHI
IPC分类号： C07D471/04 , C07F7/10
摘要： PROBLEM TO BE SOLVED: To provide a manufacturing method of a 4-halo-1H-pyrrolo[2,3-b]pyridine-5-carboxylic acid or a salt thereof that does not require repeated extraction operations at a post-treatment stage, hardly accompanies a side reaction, is excellently operable, increases the total yield and is efficient.
SOLUTION: In a reaction step, [1] a salt of pyrrolo[2,3-b]pyridine-7-oxide is isolated in a high yield; and [2] the 4-halo-1H-pyrrolo[2,3-b]pyridine-5-carboxylic acid or a salt thereof is obtained by causing a 4-halo-1H-pyrrolo[2,3-b]pyridine to react with carbon dioxide in the presence of a base thereby introducing in a high yield a carboxy group at the 5-position without by-producing a ketone compound.
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：为了提供在后期不需要重复提取操作的4-卤代-1H-吡咯并[2,3-b]吡啶-5-甲酸或其盐的制备方法，治疗阶段，几乎不伴随副反应，具有优异的可操作性，提高总产量并且效率高。解决方案：在反应步骤中，以高产率分离出[1]吡咯并[2,3-b]吡啶-7-氧化物的盐; 和[2] 4-卤代-1H-吡咯并[2,3-b]吡啶-5-甲酸或其盐是通过使4-卤代-1H-吡咯并[2,3-b]吡啶在碱的存在下与二氧化碳反应，从而高产率地引入5-位的羧基而不产生酮化合物。版权所有（C）2010，JPO＆INPIT

3. 发明公开

EP2420487A4 NOVEL METHOD FOR PRODUCING OPTICALLY ACTIVE PYRROLIDINE COMPOUND 审中-公开
标题翻译：新方法制造光学活性吡咯烷
公开(公告)号：EP2420487A4
公开(公告)日：2012-10-17
申请号：EP10764432
申请日：2010-04-13
申请人： ASTELLAS PHARMA INC
发明人： OHIGASHI ATSUSHI , KIKUCHI TAKASHI
IPC分类号： C07B53/00 , C07B61/00 , C07C253/30 , C07C255/24 , C07D207/16
CPC分类号： C07D207/12 , C07B53/00 , C07C253/30 , C07D207/16 , C07C255/24

4. 发明公开

EP2894152A4 METHOD FOR PRODUCING SULFONYL AMIDINE COMPOUND 审中-公开
标题翻译：生产磺酰胺脒化合物的方法
公开(公告)号：EP2894152A4
公开(公告)日：2016-03-09
申请号：EP13835562
申请日：2013-09-06
申请人： ASTELLAS PHARMA INC
发明人： KIKUCHI TAKASHI , YOSHIDA SHINYA , NAKAMURA ATSUSHI , AKIBA TAKAHIRO , YOSHINO TOSHITAKA , NAKAGAWA SHUICHI , SATO KIICHI
IPC分类号： C07D235/12 , C07D309/06 , C07D309/12 , C07D405/12
CPC分类号： C07D235/12 , C07B2200/13 , C07D235/14 , C07D309/06 , C07D309/12 , C07D405/12

5. 发明公开

EP2592080A4 CRYSTAL OF FUSED PYRIDINE COMPOUND SALT 有权
标题翻译：一种结晶的吡啶类化合物盐的晶体
公开(公告)号：EP2592080A4
公开(公告)日：2014-01-15
申请号：EP11798182
申请日：2011-06-22
申请人： ASTELLAS PHARMA INC
发明人： KIKUCHI TAKASHI , GATO KATSUHIKO , MUKOYOSHI KOICHIRO , KITAMURA TSUYOSHI , KAWAKAMI TAKESHI , YASUDA HIRONOBU
IPC分类号： C07D471/04 , A61K9/14 , A61K9/16 , A61K9/20 , A61K9/48 , A61K31/437 , A61P9/10 , A61P11/06 , A61P17/04 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00
CPC分类号： C07D471/04 , A61K31/437

6. 发明专利

CA2883126A1 METHOD FOR PRODUCING SULFONYL AMIDINE COMPOUND 未知
公开(公告)号：CA2883126A1
公开(公告)日：2014-03-13
申请号：CA2883126
申请日：2013-09-06
申请人： ASTELLAS PHARMA INC
发明人： KIKUCHI TAKASHI , YOSHIDA SHINYA , NAKAMURA ATSUSHI , AKIBA TAKAHIRO , YOSHINO TOSHITAKA , NAKAGAWA SHUICHI , SATO KIICHI
IPC分类号： C07D235/12 , C07D309/12 , C07D405/12
摘要： Provided are: a method for producing a sulfonyl amidine compound, which has an excellent gonadotropin releasing hormone receptor antagonism and is useful as a therapeutic agent for gonadotropin-dependent diseases (for example, prostate cancer, mammary cancer, endometriosis, uterine fibroid, prostatic hyperplasia, etc.) or a salt thereof; and a synthesis intermediate useful in the production method. The production method according to the present invention, whereby formation of a by-product, said by-product being hardly removed unless column purification is conducted, and racemization of the target compound are inhibited and therefore the target compound can be obtained at a high purity, is suitable for industrial production.

7. 发明专利

BR112021012657A2 Método para produzir nanopartícula com partícula de metal que contém óxido de ferro ao qual um ou mais ligantes hidrofílicos são ligados por coordenação 未知
公开(公告)号：BR112021012657A2
公开(公告)日：2021-09-08
申请号：BR112021012657
申请日：2019-12-27
申请人： ASTELLAS PHARMA INC
发明人： KURODA AKIO , TOYA HIROKI , HIRASAWA SHUN , KIKUCHI TAKASHI , SUGIMORI TOSHIYUKI , MIZUTANI TSUYOSHI , GOTO YOTA
IPC分类号： B01J31/02 , A61K49/06 , C01G49/00 , C01G49/02 , C01G49/06 , C01G49/08
摘要： método para produzir nanopartícula com partícula de metal que contém óxido de ferro ao qual um ou mais ligantes hidrofílicos são ligados por coordenação. problema: um novo método para produzir uma nanopartícula com uma partícula de metal que contém óxido de ferro ao qual um ou mais ligantes hidrofílicos são ligados por coordenação é fornecido, onde a nanopartícula é útil como um agente de contraste para imagem por ressonância magnética.meios para solução: como o novo método para a produção de uma nanopartícula com uma partícula de metal que contém óxido de ferro ao qual um ou mais ligantes hidrofílicos são ligados por coordenação, realizando a troca de ligante para um ligante hidrofílico a partir de uma nanopartícula de óxido de ferro com uma superfície para a qual um ligante hidrofóbico é a coordenação ligada em uma etapa usando um catalisador de transferência de fase, é possível esperar o encurtamento dos processos de produção e redução dos ligantes hidrofílicos usados. além disso, ao produzir uma nanopartícula de óxido de ferro com uma superfície à qual um ligante hidrofóbico é ligado por coordenação usando um método de adição gota a gota, é possível evitar um rápido aumento de temperatura e uma reação a uma alta temperatura de 200°c ou superior, que é mais vantajoso para a produção industrial.

8. 发明专利

CA3124753A1 METHOD FOR PRODUCING NANOPARTICLE HAVING METAL PARTICLE WHICH CONTAINS IRON OXIDE TO WHICH ONE OR MORE HYDROPHILIC LIGANDS ARE COORDINATION BONDED 未知
公开(公告)号：CA3124753A1
公开(公告)日：2020-07-02
申请号：CA3124753
申请日：2019-12-27
申请人： ASTELLAS PHARMA INC
发明人： KIKUCHI TAKASHI , MIZUTANI TSUYOSHI , TOYA HIROKI , KURODA AKIO , GOTO YOTA , HIRASAWA SHUN , SUGIMORI TOSHIYUKI
IPC分类号： C01G49/00 , A61K49/06 , B01J31/02 , C01G49/02 , C01G49/06 , C01G49/08
摘要： [Problem] To provide a novel method for producing nanoparticles which include metal particles containing iron oxide having at least one hydrophilic ligand coordinated thereto, and are useful as a contrast agent for magnetic resonance imaging. [Solution] The present invention provides a novel method for producing nanoparticles which include metal particles containing iron oxide having at least one hydrophilic ligand coordinated thereto, wherein ligand exchange for a hydrophilic ligand from iron oxide nanoparticles having a hydrophobic ligand coordinated to the surface thereof is carried out in a single process by using a phase-transfer catalyst, and it is thus expected that the production steps and the amount of hydrophilic ligand used will be reduced. In addition, the iron oxide nanoparticles having a hydrophobic ligand coordinated to the surface thereof are produced using a dropping method, thereby making it possible to avoid a rapid temperature increase or a reaction at a high temperature of 200°C or higher. The present invention is thus more advantageous for industrial production.

9. 发明专利

ES2566671T3 Cristal de sal de un compuesto de piridina fusionado 未知
公开(公告)号：ES2566671T3
公开(公告)日：2016-04-14
申请号：ES11798182
申请日：2011-06-22
申请人： ASTELLAS PHARMA INC
发明人： KIKUCHI TAKASHI , GATO KATSUHIKO , MUKOYOSHI KOICHIRO , KITAMURA TSUYOSHI , KAWAKAMI TAKESHI , YASUDA HIRONOBU
IPC分类号： C07D471/04 , A61K9/14 , A61K9/16 , A61K9/20 , A61K9/48 , A61K31/437 , A61P9/10 , A61P11/06 , A61P17/04 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00
摘要： Un cristal de hidrobromuro de 4-{[(1R,2s,3S,5s,7s)-5-hidroxi-2-adamantil]amino}-1H-pirrolo[2,3-b]piridin-5- carboxamida.

10. 发明专利

MX2015002961A METODO PARA PRODUCIR EL COMPUESTO SULFONILAMIDINA. 未知
公开(公告)号：MX2015002961A
公开(公告)日：2015-09-24
申请号：MX2015002961
申请日：2013-09-06
申请人： ASTELLAS PHARMA INC
发明人： YOSHINO TOSHITAKA , KIKUCHI TAKASHI , YOSHIDA SHINYA , NAKAMURA ATSUSHI , AKIBA TAKAHIRO , SATO KIICHI , NAKAGAWA SHUICHI
IPC分类号： C07D235/12 , C07D309/12 , C07D405/12
摘要： Se proporcionan: un método para producir un compuesto sulfonilamidina, que tiene un excelente antagonismo del receptor de hormona liberadora de gonadotropina y es útil como un agente terapéutico para enfermedades dependientes de gonadotropina (por ejemplo, cáncer de próstata, cáncer de mama, endometriosis, fibroides uterinos, hiperplasia prostática, o similares) o una sal del mismo, y un intermediario de síntesis útil en el método de producción. El método de producción de acuerdo con la presente invención, mediante el cual se inhibe la formación de un subproducto, donde dicho subproducto difícilmente se elimina a menos que se conduzca la purificación de columna, y se inhibe la racemización de un compuesto objetivo y por lo tanto se obtiene el compuesto objetivo a una alta pureza, es adecuado para la producción industrial.

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