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    LURASIDONE NOVEL DOSAGE REGIMENS AND USE THEREOF FOR THE TREATMENT, PREVENTION, AND/OR MANAGEMENT OF AT LEAST ONE CNS DISORDER
    1.
    发明申请
    LURASIDONE NOVEL DOSAGE REGIMENS AND USE THEREOF FOR THE TREATMENT, PREVENTION, AND/OR MANAGEMENT OF AT LEAST ONE CNS DISORDER 审中-公开
    LURASIDONE新剂量方案及其用于治疗，预防和/或管理至少一例CNS病症

    公开(公告)号：US20140350029A1

    公开(公告)日：2014-11-27

    申请号：US14361536

    申请日：2012-11-30

    申请人： DAINIPPON SUMITOMO PHARMA CO., LTD.

    发明人： Antony D Loebel

    IPC分类号： A61K31/496 ,  B65D77/08

    CPC分类号： A61K31/496 ,  B65D77/08

    摘要： Dosage regimens for at least one compound chosen from Iurasidone and pharmaceutically acceptable salts, solvates, clathrates, and stereoisomers thereof are disclosed as are kits and methods for treatment and/or prevention of at least one CNS disorder such as, for example, mixed depression and bipolar disorder, and management of at least one CNS disorder, such as improving quality of life and reversing impairment in learning and memory associated with schizophrenia, comprising administering to a patient a therapeutically or prophylactically effective amount of at least one compound chosen from lurasidone and pharmaceutically acceptable salts, solvates, clathrates, and stereoisomers thereof.

    摘要翻译： 至少一种选自碘尿嘧啶酮和其药学上可接受的盐，溶剂合物，包合物和立体异构体的化合物的剂量方案公开如下：用于治疗和/或预防至少一种CNS病症的试剂盒和方法，例如混合抑郁症和 包括给予患者治疗或预防有效量的至少一种选自卢拉西酮和药学上的化合物的化合物 可接受的盐，溶剂合物，包合物和立体异构体。

    Pyrazole compound
    2.
    发明授权
    Pyrazole compound 有权
    吡唑化合物

    公开(公告)号：US08809383B2

    公开(公告)日：2014-08-19

    申请号：US14041246

    申请日：2013-09-30

    申请人： Dainippon Sumitomo Pharma Co., Ltd.

    发明人： Izumi Sasaki ,  Tomohiro Toyoda ,  Hidefumi Yoshinaga ,  Itaru Natsutani ,  Yoko Takahashi

    IPC分类号： A61K31/415 ,  C07D405/06 ,  C07D231/22

    CPC分类号： C07D231/20 ,  C07D231/18 ,  C07D231/22 ,  C07D231/38 ,  C07D231/44 ,  C07D405/06 ,  C07D493/08

    摘要： The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.

    摘要翻译： 本发明涉及还显示5-HT 2C拮抗作用（抗抑郁和抗焦虑作用）的5-羟色胺再摄取抑制剂，特别是包含化合物（1）：或其药学上可接受的盐的5-HT 2C反向激动作用其中R1，R2 ，R3和R4独立地是氢或C1-6烷基等; R5是C4-7烷基或 - （CR8R9）r-E; R6，R7，R8和R9独立地是氢，氟或C1-6烷基; A为C6-10芳基或杂芳基等; r为1,2,3或4; E为C3-8环烷基或C6-10芳基等; L是氧，硫或-NR10-; n为1,2或3; R 10是氢或C 1-6烷基等; X为氢或卤素等。

    TREATMENT AND MANAGEMENT OF CNS DISORDERS
    4.
    发明申请
    TREATMENT AND MANAGEMENT OF CNS DISORDERS 审中-公开
    中枢神经系统疾病的治疗与治疗

    公开(公告)号：US20140113912A1

    公开(公告)日：2014-04-24

    申请号：US14116396

    申请日：2012-05-11

    申请人： Antony D. Loebel ,  Robert M. Silva

    发明人： Antony D. Loebel ,  Robert M. Silva

    IPC分类号： A61K31/496 ,  G01N33/483

    CPC分类号： A61K31/496 ,  G01N33/483

    摘要： The present disclosure relates to methods of treating certain CNS disorders. The present disclosure also relates to biomarkers for monitoring or predicting the efficacy of a treatment for a CNS disorder by lurasidone, or a pharmaceutically acceptable salt, solvate, clathrate or stereoisomer thereof.

    摘要翻译： 本公开涉及治疗某些CNS疾病的方法。 本公开还涉及用于监测或预测由卢卡西酮或其药学上可接受的盐，溶剂化物，包合物或立体异构体治疗CNS病症的功效的生物标志物。

    Tablet having improved elution properties
    6.
    发明授权
    Tablet having improved elution properties 有权
    片剂具有改善的洗脱性能

    公开(公告)号：US08673353B2

    公开(公告)日：2014-03-18

    申请号：US12866999

    申请日：2009-02-10

    申请人： Makiko Yanagida ,  Hiroyuki Nishii ,  Masayuki Nakazono

    发明人： Makiko Yanagida ,  Hiroyuki Nishii ,  Masayuki Nakazono

    IPC分类号： A61K9/20 ,  A61K9/30

    CPC分类号： A61K9/2054 ,  A61K9/2018 ,  A61K9/284 ,  A61K9/2866 ,  A61K31/517

    摘要： The present invention provides a tablet having improved dissolution property, which comprises (+)-3-{1-[3-(trifluoromethoxy)benzyl]piperidin-4-yl}-4-phenyl-3,4-dihydro-2(1H)-quinazolinone or a pharmaceutically acceptable salt thereof as an active component, and a production method thereof.A film-coated tablet obtained by mixing granulated particles obtained by granulating a mixture containing (a) the aforementioned active component, (b) one or more kinds of fillers selected from lactose, D-mannitol, erythritol and crystalline cellulose, (c) a cellulose-based disintegrant and (d) a water-soluble binder with a later powder containing (e) one or more kinds of fillers selected from lactose, D-mannitol and crystalline cellulose and/or (f) a cellulose-based disintegrant, forming the mixture, and applying film coating. A production method of a film-coated tablet, including a step of producing the granulated particles, a step of producing a tablet by mixing with the later powder and forming the mixture, and a step of applying a film coating to the obtained tablet.

    摘要翻译： 本发明提供具有改善的溶解性的片剂，其包含（+） - 3- {1- [3-（三氟甲氧基）苄基]哌啶-4-基} -4-苯基-3,4-二氢-2（1H ） - 喹唑啉酮或其药学上可接受的盐作为活性成分，及其制备方法。 （a）上述活性成分，（b）一种或多种选自乳糖，D-甘露糖醇，赤藓糖醇和结晶纤维素的填料的混合物混合制粒颗粒而得到的薄膜包衣片，（c） 纤维素类崩解剂和（d）具有以下粉末的水溶性粘合剂，所述粉末含有（e）一种或多种选自乳糖，D-甘露糖醇和结晶纤维素的填料和/或（f）纤维素类崩解剂，形成 混合物，并涂覆薄膜涂层。 一种薄膜包衣片的制造方法，包括制造造粒颗粒的步骤，通过与后来的粉末混合制备片剂并形成混合物的步骤，以及将膜包衣涂布在所得片剂上的步骤。

    9-Substituted 8-Oxoadenine Compound
    7.
    发明申请
    9-Substituted 8-Oxoadenine Compound 有权
    9-取代的8-氧基腺嘌呤化合物

    公开(公告)号：US20140045837A1

    公开(公告)日：2014-02-13

    申请号：US14058064

    申请日：2013-10-21

    申请人： Ayumu Kurimoto ,  Kazuki Hashimoto ,  Yoshiaki Isobe ,  Stephen Brough ,  Ian Millichip ,  Hiroki Wada ,  Roger Bonnert ,  Thomas Mcinally

    发明人： Ayumu Kurimoto ,  Kazuki Hashimoto ,  Yoshiaki Isobe ,  Stephen Brough ,  Ian Millichip ,  Hiroki Wada ,  Roger Bonnert ,  Thomas Mcinally

    IPC分类号： C07D473/18

    CPC分类号： C07D473/18 ,  A61K31/522 ,  A61K31/5377

    摘要： The present invention provides an 8-oxoadenine compound having immunomodulating activities such as an interferon inducing activity and useful as an antiviral agent and antiallergic agent, which is represented by the following formula (1): [wherein the ring A represents a 6-10 membered aromatic carbocyclic ring and the like, R represents a halogen atom, an alkyl group and the like, n represents an integer of 0-2, Z1 represents alkylene, X2 represents oxygen atom, sulfur atom, SO2, NR5, CO, CONR5, NR5CO and the like, Y1, Y2 and Y3 represent independently a single bond or an alkylene group, X1 represents oxygen atom, sulfur atom, NR4 (R4 is hydrogen atom or an alkyl group) or a single bond, R2 represents a substituted or unsubstituted alkyl group, R1 represents hydrogen atom, hydroxy group, an alkoxy group, an alkoxycarbonyl group or a haloalkyl group] or its pharmaceutically acceptable salt.

    摘要翻译： 本发明提供具有免疫调节活性的8-氧代腺嘌呤化合物，例如干扰素诱导活性，可用作抗病毒剂和抗变应性剂，其由下式（1）表示：[其中环A表示6-10元 芳香族碳环等，R表示卤素原子，烷基等，n表示0-2的整数，Z1表示亚烷基，X2表示氧原子，硫原子，SO2，NR5，CO，CONR5，NR5CO 等等，Y1，Y2和Y3独立地表示单键或亚烷基，X1表示氧原子，硫原子，NR4（R4是氢原子或烷基）或单键，R2表示取代或未取代的烷基 基团，R 1表示氢原子，羟基，烷氧基，烷氧基羰基或卤代烷基]或其​​药学上可接受的盐。

    MOLECULAR MARKER FOR CANCER STEM CELL
    8.
    发明申请
    MOLECULAR MARKER FOR CANCER STEM CELL 有权
    癌症干细胞分子标记

    公开(公告)号：US20140044686A1

    公开(公告)日：2014-02-13

    申请号：US13967410

    申请日：2013-08-15

    申请人： Dainippon Sumitomo Pharma Co. Ltd. ,  Sapporo Medical University

    发明人： Toshihiko Torigoe ,  Yoshihiko Hirohashi ,  Noriyuki Satoh ,  Kenjiro Kamiguchi ,  Rena Morita ,  Satoshi Nishizawa ,  Akari Takahashi

    IPC分类号： C12N5/0783 ,  C07K7/06

    CPC分类号： A61K38/177 ,  C07K7/06 ,  C12N5/0638 ,  C12N15/113 ,  C12N15/1138 ,  C12N2310/14 ,  C12Q1/6886 ,  C12Q2600/112 ,  C12Q2600/118 ,  C12Q2600/136 ,  C12Q2600/158 ,  G01N33/5017 ,  G01N33/574 ,  G01N33/57492 ,  G01N2333/705

    摘要： A molecular marker for detecting a cancer stem cell in a cell mass which is a subject of interest, wherein the molecular marker can be detected in a cancer stem cell contained in the subject of interest but cannot be detected in a normal cell and a cancer cell that is different from a cancer stem cell; a method for determining the presence or absence of a cancer stem cell in a subject of interest by using the molecular marker as an measure; a kit for determining the presence or absence of a cancer stem cell, which comprises at least a reagent for detecting the molecular marker; a polypeptide encoded by the molecular marker; an antibody capable of recognizing an epitope of an expression product of a gene derived from the molecular marker; a nucleic acid capable of inhibiting the expression of the molecular marker; and a nucleic acid vaccine comprising a gene derived from the molecular marker.

    摘要翻译： 用于检测作为感兴趣的受试者的细胞块中的癌干细胞的分子标记，其中可以在感兴趣的受试者所含的癌干细胞中检测分子标记，但在正常细胞和癌细胞中不能检测到 这与癌症干细胞不同; 通过使用分子标记作为测量来确定感兴趣对象中癌干细胞的存在或不存在的方法; 用于确定癌干细胞的存在或不存在的试剂盒，其包含至少一种用于检测分子标记的试剂; 由分子标记编码的多肽; 能够识别来自分子标记物的基因的表达产物的表位的抗体; 能够抑制分子标记物的表达的核酸; 和包含衍生自分子标记的基因的核酸疫苗。

    PYRAZOLE COMPOUND
    9.
    发明申请
    PYRAZOLE COMPOUND 有权
    吡唑化合物

    公开(公告)号：US20140031406A1

    公开(公告)日：2014-01-30

    申请号：US14041246

    申请日：2013-09-30

    申请人： Dainippon Sumitomo Pharma Co., Ltd.

    发明人： Izumi SASAKI ,  Tomohiro TOYODA ,  Hidefumi YOSHINAGA ,  Itaru NATSUTANI ,  Yoko TAKAHASHI

    IPC分类号： C07D493/08 ,  C07D405/06 ,  C07D231/20

    CPC分类号： C07D231/20 ,  C07D231/18 ,  C07D231/22 ,  C07D231/38 ,  C07D231/44 ,  C07D405/06 ,  C07D493/08

    摘要： The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.

    摘要翻译： 本发明涉及还显示5-HT 2C拮抗作用（抗抑郁和抗焦虑作用）的5-羟色胺再摄取抑制剂，特别是包含化合物（1）：或其药学上可接受的盐的5-HT 2C反向激动作用其中R1，R2 ，R3和R4独立地是氢或C1-6烷基等; R5是C4-7烷基或 - （CR8R9）r-E; R6，R7，R8和R9独立地是氢，氟或C1-6烷基; A为C6-10芳基或杂芳基等; r为1,2,3或4; E为C3-8环烷基或C6-10芳基等; L是氧，硫或-NR10-; n为1,2或3; R 10是氢或C 1-6烷基等; X为氢或卤素等。