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71. 发明申请

WO2021173598A1 COMBINATION DECITABINE AND CEDAZURIDINE SOLID ORAL DOSAGE FORMS 审中-公开
公开(公告)号：WO2021173598A1
公开(公告)日：2021-09-02
申请号：PCT/US2021/019310
申请日：2021-02-24
申请人： OTSUKA PHARMACEUTICAL CO., LTD.
发明人： OGANESIAN, Aram , DAVAR, Nipun , KOU, Jim Hwaicher
IPC分类号： A61K31/706 , A61K31/7068
摘要： Embodiments of the present invention provide solid oral dosage forms that upon daily administration to a subject provide plasma levels of decitabine with a 5-day AUC for decitabine that is equivalent to the 5-day AUC for a daily IV dose of decitabine of 20 mg/m2 administered as a one hour (1 h) infusion. Also provided according to embodiments of the present invention are solid oral dosage forms wherein upon daily administration to a subject provides a pharmacodynamic effect that is equivalent to the pharmacodynamic effect for a daily intravenous dose of decitabine of 20 mg/m2 administered as a one hour (1 h) infusion. Also provided are methods of treatment using a solid oral dosage form according to an embodiment of the invention.

72. 发明申请

WO2021149817A1 Enhancement of anti-tumor activity of SHP2 inhibitor pyrimidinone in combination with novel cancer medicines in cancers 审中-公开
公开(公告)号：WO2021149817A1
公开(公告)日：2021-07-29
申请号：PCT/JP2021/002318
申请日：2021-01-22
申请人： TAIHO PHARMACEUTICAL CO., LTD. , OTSUKA PHARMACEUTICAL CO., LTD.
发明人： HOSHINO, Takuya , KOMIYA, Yu , NAKATSURU, Yoko , WALLIS, Nicola Gail
IPC分类号： A61K31/519 , A61K31/506 , A61K39/395 , A61K45/00 , A61P35/00
摘要： The present invention provides a combination drug for the treatment of a malignant tumor comprising 2-((1R,2R,4S)-2-amino-7-azabicyclo[2.2.1]heptan-7-yl)-5-(3,4-dichloro-2-methyl-2H-indazol-5-yl)-3-methyl-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one or a pharmaceutically acceptable salt thereof, and at least one additional compound having an antitumor effect or at least one pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising both the active ingredients.

73. 发明申请

WO2021071890A1 2'-DEOXY-2',2'-DIFLUOROTETRAHYDROURIDINES WITH HIGH PURITY AND METHODS OF MAKING THE SAME 审中-公开
公开(公告)号：WO2021071890A1
公开(公告)日：2021-04-15
申请号：PCT/US2020/054500
申请日：2020-10-07
申请人： OTSUKA PHARMACEUTICAL CO., LTD. , ZUEND, Gemma , SCOTT, Ian , DAVAR, Nipun , ANNAKA, Kimiyoshi , MIYAKE, Masahiro , MATSUI, Motoshi
发明人： ZUEND, Gemma , SCOTT, Ian , DAVAR, Nipun , ANNAKA, Kimiyoshi , MIYAKE, Masahiro , MATSUI, Motoshi
IPC分类号： C07H19/04 , C07H1/00 , B01J31/02
摘要： The invention relates to methods of synthesizing 2'-deoxy-2',2'-difluorotetrahydrouridine with increased purity and uniform particle size distribution. In particular, methods of the invention include crystallization and isolation procedures rendering synthetic reaction intermediates. The invention further includes compositions comprising the final compound in highly pure form, including lower number of impurities and lower levels of individual and total impurities.

74. 发明申请

WO2020050409A1 HETEROCYCLIC COMPOUND 审中-公开
公开(公告)号：WO2020050409A1
公开(公告)日：2020-03-12
申请号：PCT/JP2019/035233
申请日：2019-09-06
申请人： OTSUKA PHARMACEUTICAL CO., LTD.
发明人： OHDACHI, Kazuhiro , FUJIMORI, Yusuke , MAKITA, Naoya , KOSEKI, Noritaka , HAYASHI, Hideki , SAKAMOTO, Yuki , MINENO, Kurumi , TAGA, Ryosuke
IPC分类号： C07D498/14 , C07D513/14 , A61P7/04 , A61K31/519
摘要： Provided is a novel heterocyclic compound having an aryl hydrocarbon receptor antagonist activity and useful for the promotion of platelet production, the compound being represented by the general formula [I]: wherein ring A, ring B, R 1 , R 2 , R 3 , R 4 , n, and X are as defined above, or a salt thereof.

75. 发明申请

WO2019163738A1 METHOD OF 4-BORONOPHENYLALANINE PRODUCTION 审中-公开
公开(公告)号：WO2019163738A1
公开(公告)日：2019-08-29
申请号：PCT/JP2019/005984
申请日：2019-02-19
申请人： OTSUKA PHARMACEUTICAL CO., LTD.
发明人： ZAHRADNIK, Petr , STURC, Antonin , MALINAK, Jiri , KOCI, Jan
IPC分类号： C07B47/00 , C07B49/00 , C07B51/00 , C07B63/02 , C07F5/02
摘要： The present invention relates to a method of production of 4-boronophenylalanine (BPA) from 4-iodophenylalanine, in which all the functional groups of the amino acid are protected by benzyl protection method, and which uses isopropyl magnesium halogenide stabilized by a complexation base, and subsequent condensation of the resulting Grignard reagent with a boric acid ester. The final reaction step, catalytic hydrogenolysis or transfer hydrogenolysis of protecting groups on the amino acid, occurs after hydrolysis of the boronate ester groups.

76. 发明申请

WO2017111123A1 DRUG COMPRISING ARIPIPRAZOLE AND CILOSTAZOL 审中-公开
标题翻译：包含ARIPIPRAZOLE和CILOSTAZOL的药物
公开(公告)号：WO2017111123A1
公开(公告)日：2017-06-29
申请号：PCT/JP2016/088554
申请日：2016-12-22
申请人： OTSUKA PHARMACEUTICAL CO., LTD.
发明人： SHIN, Hwa Kyoung , CHOI, Byung Tae , HONG, Ki Whan
IPC分类号： A61K31/496 , A61K31/4709 , A61P9/10 , A61P25/14 , A61P25/16 , A61P25/24 , A61P25/28
CPC分类号： A61K31/4709 , A61K31/496 , A61K2300/00
摘要： The present invention enables treatment and/or prevention of dementia, cognitive impairment, and vascular depression by a combination of aripiprazole and cilostazol, or the like. The combination contains aripiprazole and cilostazol, and is used for the treatment and/or prevention of at least one member selected from the group consisting of dementia, cognitive impairment, and vascular depression.
摘要翻译：本发明能够通过阿立哌唑和西洛他唑等的组合来治疗和/或预防痴呆，认知障碍和血管性抑郁症。该组合含有阿立哌唑和西洛他唑，并用于治疗和/或预防选自痴呆，认知障碍和血管性抑郁症中的至少一种。

77. 发明申请

WO2014178334A1 ORAL SOLID PREPARATION COMPRISING ARIPIPRAZOLE AND METHOD FOR PRODUCING ORAL SOLID PREPARATION COMPRISING ARIPIPRAZOLE 审中-公开
标题翻译：包含阿维哌唑的口服固体制剂和生产包含阿维哌唑的口服固体制剂的方法
公开(公告)号：WO2014178334A1
公开(公告)日：2014-11-06
申请号：PCT/JP2014/061643
申请日：2014-04-18
申请人： OTSUKA PHARMACEUTICAL CO., LTD.
发明人： YOSHIDA, Haruka , TANIGUCHI, Toshiaki , MUKAI, Tadashi
IPC分类号： A61K9/14 , A61K9/20
CPC分类号： A61K9/14 , A61K9/2018
摘要： An object of the present invention is to provide an oral solid preparation that can be produced in a simpler manner than conventional methods, that exhibits high bioavailability and high dissolubility even in persons having low stomach acid, and that can also ensure dissolubility after being allowed to stand for a certain period of time. Another object is to provide a simple method for producing the oral solid preparation. The present invention relates to an oral solid preparation comprising, as an active ingredient, a finely milled crystal obtained by milling an aripiprazole hydrate crystal, and a pharmaceutically acceptable carrier, the finely milled crystal having a mean particle size of 15 μm or less; an oral solid preparation comprising, as an active ingredient, a finely milled powder obtained by milling a highly hygroscopic aripiprazole anhydrous crystal, and a pharmaceutically acceptable carrier, the finely milled crystal having a mean particle size of 10 μm or less; a method for producing an oral solid preparation comprising the steps of (1) milling an aripiprazole hydrate crystal into a finely milled crystal having a mean particle size of 15 μm or less, and (2) mixing the obtained finely milled crystal with a pharmaceutically acceptable carrier; and a method for producing an oral solid preparation comprising the steps of: (1') milling a highly hygroscopic aripiprazole anhydrous crystal into a finely milled powder having a mean particle size of 10 μm or less; and (2') mixing the obtained finely milled powder with a pharmaceutically acceptable carrier.
摘要翻译：本发明的目的是提供一种口服固体制剂，其可以比常规方法更简单地制备，即使在具有低胃酸的人中也显示出高生物利用度和高溶解性，并且还可以确保在允许代表一段时间。另一个目的是提供一种生产口服固体制剂的简单方法。本发明涉及一种口服固体制剂，其包含通过研磨阿立哌唑水合物晶体获得的精细研磨的晶体和药学上可接受的载体作为活性成分，所述精细研磨的晶体具有15μm或更小的平均粒径; 一种口服固体制剂，其包含通过研磨高吸湿性阿立哌唑无水晶体获得的细磨粉末作为活性成分和药学上可接受的载体，所述磨碎的平均粒径为10μm或更小的晶体; 一种制备口服固体制剂的方法，包括以下步骤：（1）将阿立哌唑水合物晶体研磨成平均粒度为15μm或更小的精细研磨的晶体，和（2）将得到的细磨结晶与药学上可接受的载体; 和口服固体制剂的制备方法，包括以下步骤：（1'）将高吸湿性阿立哌唑无水晶体研磨成平均粒径为10μm以下的细磨粉末; 和（2'）将获得的细磨粉末与药学上可接受的载体混合。

78. 发明申请

WO2014104412A1 INJECTABLE DEPOT FORMULATION COMPRISING OPTICALLY ACTIVE TOLVAPTAN AND PROCESS OF PRODUCING THE SAME 审中-公开
标题翻译：包含光学有效的TOLVAPTAN的注射剂配方及其生产方法
公开(公告)号：WO2014104412A1
公开(公告)日：2014-07-03
申请号：PCT/JP2013/085355
申请日：2013-12-27
申请人： OTSUKA PHARMACEUTICAL CO., LTD.
发明人： KANEKO, Daiki , MATSUDA, Takakuni , MIYATA, Kenichi , SUZUKI, Kai , FUJIKI, Hiroyuki , KINOSHITA, Shizuo , OHMOTO, Koji , AIHARA, Miki
IPC分类号： A61K9/00 , A61K9/16 , A61K31/55 , A61K9/14
CPC分类号： A61K9/0019 , A61K9/0024 , A61K9/10 , A61K9/14 , A61K9/1635 , A61K9/1647 , A61K9/1652 , A61K9/1688 , A61K9/1694 , A61K31/55 , A61K47/10 , A61K47/32 , A61K47/38
摘要： This invention provides an injectable formulation to be administered intramuscularly or subcutaneously that is used for the prevention or treatment of polycystic kidney disease, and that can maintain a therapeutically effective blood concentration of tolvaptan for a long period of time; and a process for producing the same. More specifically, this invention relates to an injectable depot formulation comprising (1) a particle containing optically active tolvaptan as an active ingredient and (2) a pharmaceutically acceptable carrier for injection, and a process for producing the same.
摘要翻译：本发明提供肌内或皮下施用的可注射制剂，其用于预防或治疗多囊肾病，并且可以长时间维持托伐普坦的治疗有效血药浓度; 及其制造方法。更具体地说，本发明涉及一种可注射贮库制剂，其包含（1）含光学活性托伐普坦作为活性成分的颗粒和（2）药学上可接受的注射用载体及其制备方法。

79. 发明申请

WO2014038682A2 CANCER DIAGNOSTIC AND THERAPEUTIC METHOD TARGETING MOLECULES EXPRESSED IN CANCER STEM CELLS 审中-公开
标题翻译：癌症诊断和治疗方法指导癌症干细胞中表达的分子
公开(公告)号：WO2014038682A2
公开(公告)日：2014-03-13
申请号：PCT/JP2013/074172
申请日：2013-09-03
申请人： NIIGATA UNIVERSITY , OTSUKA PHARMACEUTICAL CO., LTD.
发明人： KAGAMU, Hiroshi , NARITA, Ichiei , GOTO, Yoshihiro , HAYASHI, Takashi
IPC分类号： G01N33/574
CPC分类号： A61K39/0011 , A61K31/17 , A61K31/404 , A61K31/4184 , A61K31/4412 , A61K31/551 , C12N9/14 , C12Y306/04013 , G01N33/57484 , G01N2333/54 , G01N2333/5406 , G01N2333/57 , G01N2333/914
摘要： The present invention provides a novel method for determining cancer malignancy, a novel cancer diagnostic method, a novel method for determining prognosis, a novel vaccine for cancer treatment, and a novel vaccine for suppressing cancer metastasis. Specifically, the invention provides a cancer malignancy evaluation method that comprises the step of measuring a DDX3X expression level in a cancer tissue, and the step of evaluating malignancy of the cancer tissue by using the DDX3X expression level.
摘要翻译：本发明提供了一种确定癌症恶性肿瘤的新方法，一种新的癌症诊断方法，一种预后判定方法，一种新型癌症治疗疫苗，以及一种抑制癌症转移的新型疫苗。具体地，本发明提供了癌症恶性肿瘤评价方法，其包括测定癌组织中DDX3X表达量的步骤，以及通过使用DDX3X表达水平评价癌组织的恶性的步骤。

80. 发明申请

WO2014036402A1 CONTAINER WITH CONCENTRATED SUBSTANCE AND METHOD OF USING THE SAME 审中-公开
标题翻译：具有浓缩物质的容器及其使用方法
公开(公告)号：WO2014036402A1
公开(公告)日：2014-03-06
申请号：PCT/US2013/057529
申请日：2013-08-30
申请人： OTSUKA PHARMACEUTICAL CO., LTD. , HOLLANDER, Scott Wayne , TIMBERLAKE, Joel Robert , KADASH, Marjory
发明人： HOLLANDER, Scott Wayne , TIMBERLAKE, Joel Robert , KADASH, Marjory
IPC分类号： A61J7/00 , A61K49/00 , B65D85/816 , G01N24/00 , G01F19/00
CPC分类号： A61J1/00 , A61J7/0046 , A61K49/0404 , A61K49/0438 , A61K49/0452 , A61K49/101 , A61K49/103 , A61K49/105 , A61K49/108 , A61K49/126 , A61K49/18 , A61K49/1818 , G01R33/5601
摘要： Apparatus and methods are described herein for a container with a unit dose of a concentrated substance that can be diluted and orally consumed using the container. In some embodiments, an apparatus includes a container body that defines an opening in fluid communication with an interior of the container body. A cap is coupled to the container body and encloses the opening. A unit dose of a concentrated medicament or a concentrated contrast agent is disposed within the interior of the container body. The unit dose of concentrated medicament or contrast agent can be diluted to a select dilution strength with a volume of a liquid receivable through the opening and within the interior of the container body. In some embodiments, the apparatus can include a barrier member in which the container body and cap can be disposed to protect the medicament or contrast agent from light and/or moisture.
摘要翻译：本文描述了具有可以使用容器稀释并口服消耗的浓缩物质的单位剂量的容器的装置和方法。在一些实施例中，一种装置包括容器主体，其限定与容器主体的内部流体连通的开口。盖子连接到容器主体并且封闭开口。浓缩药物或浓缩造影剂的单位剂量设置在容器体内。浓缩药物或造影剂的单位剂量可以稀释至选定的稀释强度，其中一定体积的液体可通过开口和容器主体的内部容纳。在一些实施例中，该装置可以包括阻挡构件，其中可以设置容器主体和盖以保护药物或造影剂免受光和/或湿气的影响。

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