公开(公告)号：US08541459B2

公开(公告)日：2013-09-24

申请号：US12523067

申请日：2008-01-17

申请人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

发明人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

IPC分类号： A01N43/52 ,  A61K31/415 ,  C07D233/28 ,  C07D233/91

CPC分类号： A61K31/4168 ,  A61K9/0019 ,  A61K47/12 ,  A61K47/18 ,  A61K47/22

摘要： To provide a pharmaceutical composition which can enhance the storage stability of 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole without impairing the effect of the compound.The pharmaceutical composition includes 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole, which is represented by formula (1): and a compound having chelating ability.

公开(公告)号：US08450356B2

公开(公告)日：2013-05-28

申请号：US13362527

申请日：2012-01-31

申请人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

发明人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

IPC分类号： A01N43/52 ,  A61K31/415 ,  C07D233/28 ,  C07D233/91

CPC分类号： A61K31/4168 ,  A61K9/0019 ,  A61K47/12 ,  A61K47/18 ,  A61K47/22

摘要： To provide a pharmaceutical composition which can enhance the storage stability of 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole without impairing the effect of the compound.The pharmaceutical composition includes 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole, which is represented by formula (1): and a compound having chelating ability.

摘要翻译： 提供能够提高1-（1-羟甲基-2,3-二羟基丙氧基甲基）-2-硝基咪唑的保存稳定性的药物组合物，而不损害化合物的作用。 药物组合物包括由式（1）表示的1-（1-羟甲基-2,3-二羟基丙氧基甲基）-2-硝基咪唑：和具有螯合能力的化合物。

公开(公告)号：US08202898B1

公开(公告)日：2012-06-19

申请号：US13365785

申请日：2012-02-03

申请人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

发明人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

IPC分类号： A01N43/52 ,  A61K31/415 ,  C07D233/28 ,  C07D233/91

CPC分类号： A61K9/08 ,  A61K9/0019 ,  A61K31/4168 ,  A61K41/0038 ,  C07D233/91

摘要： To provide a pharmaceutical composition containing a 2-nitroimidazole derivative, which has high solubility in an aqueous carrier and high stability.The pharmaceutical composition is characterized by containing 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole and creatinine, and containing creatinine of 0.001 to 1 part by mass with respect to 1 part by mass of 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole.

摘要翻译： 提供含有在水性载体中具有高溶解度和高稳定性的2-硝基咪唑衍生物的药物组合物。 该药物组合物的特征在于含有1-（1-羟甲基-2,3-二羟丙基）氧甲基-2-硝基咪唑和肌酸酐，相对于1质量份的1-（1 - 羟基甲基-2,3-二羟丙基）氧基甲基-2-硝基咪唑。

公开(公告)号：US20120136160A1

公开(公告)日：2012-05-31

申请号：US13365785

申请日：2012-02-03

申请人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

发明人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

IPC分类号： C07D233/91

CPC分类号： A61K9/08 ,  A61K9/0019 ,  A61K31/4168 ,  A61K41/0038 ,  C07D233/91

摘要： To provide a pharmaceutical composition containing a 2-nitroimidazole derivative, which has high solubility in an aqueous carrier and high stability.The pharmaceutical composition is characterized by containing 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole and creatinine, and containing creatinine of 0.001 to 1 part by mass with respect to 1 part by mass of 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole.

公开(公告)号：US20100130576A1

公开(公告)日：2010-05-27

申请号：US12598044

申请日：2008-04-16

申请人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

发明人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

IPC分类号： A61K31/4168 ,  A61P35/00

CPC分类号： A61K9/08 ,  A61K9/0019 ,  A61K31/4168 ,  A61K41/0038 ,  C07D233/91

摘要： To provide a pharmaceutical composition containing a 2-nitroimidazole derivative, which has high solubility in an aqueous carrier and high stability.The pharmaceutical composition is characterized by containing 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole and creatinine, and containing creatinine of 0.001 to 1 part by mass with respect to 1 part by mass of 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole.

摘要翻译： 提供含有在水性载体中具有高溶解度和高稳定性的2-硝基咪唑衍生物的药物组合物。 该药物组合物的特征在于含有1-（1-羟甲基-2,3-二羟丙基）氧甲基-2-硝基咪唑和肌酸酐，相对于1质量份的1-（1 - 羟基甲基-2,3-二羟丙基）氧基甲基-2-硝基咪唑。

公开(公告)号：US20100076042A1

公开(公告)日：2010-03-25

申请号：US12523067

申请日：2008-01-17

申请人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

发明人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

IPC分类号： A61K31/417 ,  A61P35/00

CPC分类号： A61K31/4168 ,  A61K9/0019 ,  A61K47/12 ,  A61K47/18 ,  A61K47/22

摘要： To provide a pharmaceutical composition which can enhance the storage stability of 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole without impairing the effect of the compound.The pharmaceutical composition includes 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole, which is represented by formula (1): and a compound having chelating ability.

摘要翻译： 提供能够提高1-（1-羟甲基-2,3-二羟基丙氧基甲基）-2-硝基咪唑的保存稳定性的药物组合物，而不损害化合物的作用。 药物组合物包括由式（1）表示的1-（1-羟甲基-2,3-二羟基丙氧基甲基）-2-硝基咪唑：和具有螯合能力的化合物。

公开(公告)号：US20100004460A1

公开(公告)日：2010-01-07

申请号：US12522926

申请日：2008-01-17

申请人： Azuma Nishio

发明人： Azuma Nishio

IPC分类号： C07D233/91

CPC分类号： C07D233/91 ,  A61K51/0453

摘要： It is an object to provide a method for producing a 2-nitroimidazole derivative having an acyclic sugar chain in a side chain, which is suitable for production of a derivative having a radioisotope.A method for producing 1-(1-benzoyloxymethyl-2-hydroxyethyl)oxymethyl-2-nitroimidazole, characterized by reacting glycerin with a benzoylating agent to obtain 1-O-benzoylglycerin, reacting 1-O-benzoylglycerin with dimethoxymethane in the presence of a dehydrating agent to obtain 4-benzoyloxymethyl-1,3-dioxolane, and then reacting this product with 2-nitroimidazole or 2-nitro-1-trialkylsilylimidazole in the presence of a Lewis acid.

摘要翻译： 本发明的目的是提供一种用于制备侧链中具有无环糖链的2-硝基咪唑衍生物的方法，其适用于制备具有放射性同位素的衍生物。 1-（1-苯甲酰氧基甲基-2-羟乙基）氧基甲基-2-硝基咪唑的制备方法，其特征在于使甘油与苯甲酰化试剂反应，得到1-O-苯甲酰甘油，使1-O-苯甲酰甘油与二甲氧基甲烷在 脱水剂，得到4-苯甲酰氧基甲基-1,3-二氧戊环，然后在路易斯酸存在下使该产物与2-硝基咪唑或2-硝基-1-三烷基甲硅烷基咪唑反应。

公开(公告)号：US08258165B2

公开(公告)日：2012-09-04

申请号：US12598044

申请日：2008-04-16

申请人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

发明人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

IPC分类号： A01N43/52 ,  A61K31/415 ,  C07D233/28 ,  C07D233/91

CPC分类号： A61K9/08 ,  A61K9/0019 ,  A61K31/4168 ,  A61K41/0038 ,  C07D233/91

摘要： To provide a pharmaceutical composition containing a 2-nitroimidazole derivative, which has high solubility in an aqueous carrier and high stability.The pharmaceutical composition is characterized by containing 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole and creatinine, and containing creatinine of 0.001 to 1 part by mass with respect to 1 part by mass of 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole.

公开(公告)号：US20120136295A1

公开(公告)日：2012-05-31

申请号：US13365723

申请日：2012-02-03

申请人： Yasushi MURAKAMI ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

发明人： Yasushi MURAKAMI ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

IPC分类号： A61M37/00

CPC分类号： A61K9/08 ,  A61K9/0019 ,  A61K31/4168 ,  A61K41/0038 ,  C07D233/91

摘要： To provide a pharmaceutical composition containing a 2-nitroimidazole derivative, which has high solubility in an aqueous carrier and high stability.The pharmaceutical composition is characterized by containing 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole and creatinine, and containing creatinine of 0.001 to 1 part by mass with respect to 1 part by mass of 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole.

摘要翻译： 提供含有在水性载体中具有高溶解度和高稳定性的2-硝基咪唑衍生物的药物组合物。 该药物组合物的特征在于含有1-（1-羟甲基-2,3-二羟丙基）氧甲基-2-硝基咪唑和肌酸酐，相对于1质量份的1-（1 - 羟基甲基-2,3-二羟丙基）氧基甲基-2-硝基咪唑。

公开(公告)号：US20120130148A1

公开(公告)日：2012-05-24

申请号：US13362545

申请日：2012-01-31

申请人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

发明人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

IPC分类号： A61N5/00

CPC分类号： A61K31/4168 ,  A61K9/0019 ,  A61K47/12 ,  A61K47/18 ,  A61K47/22

摘要： To provide a pharmaceutical composition which can enhance the storage stability of 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole without impairing the effect of the compound.The pharmaceutical composition includes 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole, which is represented by formula (1): and a compound having chelating ability.