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    Deuterium-enriched 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[(4-trifluoro-methyl)phenyl]-1,2-dihydroquinoline-3-carboxamide
    21.
    发明授权
    Deuterium-enriched 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[(4-trifluoro-methyl)phenyl]-1,2-dihydroquinoline-3-carboxamide 有权
    富含氘的4-羟基-5-甲氧基-N，1-二甲基-2-氧代-N - [（4-三氟 - 甲基）苯基] -1,2-二氢喹啉-3-甲酰胺

    公开(公告)号：US09216956B2

    公开(公告)日：2015-12-22

    申请号：US14125666

    申请日：2012-06-20

    Applicant: Leif Svensson

    Inventor： Leif Svensson

    IPC: C07D215/00 ,  C07D215/56 ,  A61K31/4704

    CPC classification number: C07D215/56 ,  A61K31/4704

    Abstract: Deuterium-enriched 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[(4-trifluoromethyl) -phenyl]-1,2-dihydroquinoline-3-carboxamide, having a deuterium enrichment in the amide-N methyl group of at least 70%; or a salt thereof with a pharmaceutically acceptable organic or inorganic cation; and a method of preparing said compounds. The compounds are useful in therapy, e.g. for the treatment of a malignant hyperproliferative disorder or an autoimmune disease.

    Abstract translation: 富含氘的4-羟基-5-甲氧基-N，1-二甲基-2-氧代-N - [（4-三氟甲基） - 苯基] -1,2-二氢喹啉-3-甲酰胺在酰胺中具有氘浓缩 -N甲基至少70％; 或其盐与药学上可接受的有机或无机阳离子; 以及制备所述化合物的方法。 这些化合物可用于治疗，例如 用于治疗恶性过度增殖性疾病或自身免疫性疾病。

    HETEROCYCLIC COMPOUND AND USE THEREFOR
    24.
    发明申请
    HETEROCYCLIC COMPOUND AND USE THEREFOR 有权
    杂环化合物及其用途

    公开(公告)号：US20150126487A1

    公开(公告)日：2015-05-07

    申请号：US14382390

    申请日：2013-02-28

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： Hiroki Sakamoto ,  Takahiro Sugimoto

    IPC: C07D405/12 ,  C07D401/10 ,  C07D401/12 ,  C07D401/06 ,  C07D237/28 ,  C07D215/56 ,  C07D403/10

    CPC classification number: C07D405/12 ,  C07D215/56 ,  C07D237/28 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10

    Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, a sleep disorder and the like. The present invention relates to a compound represented by the formula (I): wherein R1 is an optionally substituted amino group or an optionally substituted cyclic amino group, R2 and R3 are each independently a hydrogen atom or a substituent, X is —CH═ or —N═, and ring A is an optionally substituted 5- to 10-membered ring, or a salt thereof.

    Abstract translation: 本发明提供具有胆碱能毒蕈碱M1受体阳性变构调节剂活性的化合物，可用作阿尔茨海默氏病，精神分裂症，疼痛，睡眠障碍等的预防或治疗药物。 本发明涉及由式（I）表示的化合物：其中R 1为任选取代的氨基或任意取代的环状氨基，R 2和R 3各自独立地为氢原子或取代基，X为-CH =或 -N =，环A为任选取代的5至10元环或其盐。

    Bifunctional metnase/intnase inhibitors and related compositions and methods of treatment of cancer
    27.
    发明授权
    Bifunctional metnase/intnase inhibitors and related compositions and methods of treatment of cancer 有权
    双功能metnase / intnase抑制剂和相关的治疗癌症的组合物和方法

    公开(公告)号：US08889689B2

    公开(公告)日：2014-11-18

    申请号：US13574941

    申请日：2011-01-26

    Applicant: Robert Hromas ,  Andrei Leitao ,  Tudor I. Oprea ,  Larry A. Sklar ,  Elizabeth A. Williamson ,  Justin Wray ,  Wei Wang

    Inventor： Robert Hromas ,  Andrei Leitao ,  Tudor I. Oprea ,  Larry A. Sklar ,  Elizabeth A. Williamson ,  Justin Wray ,  Wei Wang

    IPC: A61K31/497 ,  A61K45/06 ,  C07D401/12 ,  C07D215/56 ,  A61K31/4709 ,  A61K31/47

    CPC classification number: C07D215/56 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/475 ,  A61K31/496 ,  A61K31/7048 ,  A61K45/06 ,  A61N5/1001 ,  A61N5/1045 ,  A61N2005/1087 ,  A61N2005/1098 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  A61K2300/00

    Abstract: This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical bifunctional inhibitors of DNA replication and repair proteins Metnase and/or Intnase (also termed Gypsy Integrase, Gypsy Integrease-1, Gypsy Retransposon Integrase 1, or GIN-I) that simultaneously damage DNA, and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols, including radiation therapy. In preferred embodiments, compounds, compositions and methods of treatment of the invention are used to treat a patient suffering from leukemia (e.g. acute myeloid leukemia (AML) and related cancers. In certain aspects of such treatments, compounds, compositions and methods of treatment of the invention are administered as a monotherapy (in some cases, to patients who have exhibited resistance to Topo IIalpha inhibitors such as VP-16), or are co-administered with a Topo IIalpha inhibitor or other anti-cancer agents as otherwise described herein or in combination with radiation therapy.

    Abstract translation: 本发明涉及新的癌症治疗组合物和相关的治疗方法。 更具体地说，本发明部分涉及同时损伤DNA的DNA复制和修复蛋白质Metnase和/或Intnase（也称为Gypsy整合酶，Gypsy Integrease-1，Gypsy Retransposon Integrase 1或GIN-1）的小型化学双功能抑制剂， 以及利用抑制剂增加包括放射治疗在内的癌症治疗方案的有效性的治疗方法。 在优选的实施方案中，本发明的化合物，组合物和治疗方法用于治疗患有白血病的患者（例如急性骨髓性白血病（AML）和相关的癌症）。在这些治疗的某些方面，化合物，组合物和治疗方法 本发明作为单一疗法（在某些情况下，对已显示出对Topo IIalpha抑制剂如VP-16具有抗性的患者）施用，或者与本文另有描述的Topo IIal抑制剂或其它抗癌剂共同施用，或 结合放射治疗。

    N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl)amino)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide
    30.
    发明授权
    N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl)amino)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide 有权
    N-乙基-4-羟基-1-甲基-5-（甲基（2,3,4,5,6-五羟基己基）氨基）-2-氧-N-苯基-1,2-二氢喹啉-3-甲酰胺

    公开(公告)号：US08809537B2

    公开(公告)日：2014-08-19

    申请号：US13888709

    申请日：2013-05-07

    Applicant: Avital Laxer ,  Konstantin Ulanenko

    Inventor： Avital Laxer ,  Konstantin Ulanenko

    IPC: A61K31/47 ,  C07D215/00

    CPC classification number: C07D215/56 ,  A61K31/4704 ,  A61K2300/00

    Abstract: The subject invention provides pharmaceutical compositions containing laquinimod or a pharmaceutically acceptable salt thereof, an isolated compound of N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl)amino)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide or a salt thereof, compositions containing N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl)amino)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide and methods of preparing the same.

    Abstract translation: 本发明提供含有拉喹莫德或其药学上可接受的盐，N-乙基-4-羟基-1-甲基-5-（甲基（2,3,4,5,6-五羟基己基）氨基）的分离化合物的药物组合物， -2-氧代-N-苯基-1,2-二氢喹啉-3-甲酰胺或其盐包含N-乙基-4-羟基-1-甲基-5-（甲基（2,3,4,5， 6-五羟基己基）氨基）-2-氧代-N-苯基-1,2-二氢喹啉-3-甲酰胺及其制备方法。

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