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    A PLURALITY OF TASQUINIMOD PARTICLES AND USE THEREOF
    1.
    发明公开
    A PLURALITY OF TASQUINIMOD PARTICLES AND USE THEREOF 审中-公开

    公开(公告)号：US20240285532A1

    公开(公告)日：2024-08-29

    申请号：US18289738

    申请日：2022-05-23

    申请人： ACTIVE BIOTECH AB

    发明人： Hans Wännman

    IPC分类号： A61K9/14 ,  A61K31/4704

    CPC分类号： A61K9/14 ,  A61K31/4704

    摘要： A plurality of particles of tasquinimod in free base form or as a pharmaceutically acceptable salt, said particles having a D(v, 0.9) of at most 30 pm and a D(v, 0.5) of at most 15 μm. A pharmaceutical composition comprising said particles and preferably one or more pharmaceutically acceptable excipients. A pharmaceutical dosage unit. The particles, composition and dosage unit are useful in the treatment of cancer.

    DEUTERIUM-ENRICHED 4-HYDROXY-5-METHOXY-N,1-DIMETHYL-2-OXO-N-[(4-TRIFLUORO-METHYL)PHENYL]-1,2-DIHYDROQUINOLINE-3-CARBOXAMIDE
    7.
    发明申请
    DEUTERIUM-ENRICHED 4-HYDROXY-5-METHOXY-N,1-DIMETHYL-2-OXO-N-[(4-TRIFLUORO-METHYL)PHENYL]-1,2-DIHYDROQUINOLINE-3-CARBOXAMIDE 有权
    异恶唑-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-羧酰胺

    公开(公告)号：US20140112946A1

    公开(公告)日：2014-04-24

    申请号：US14125666

    申请日：2012-06-22

    申请人： ACTIVE BIOTECH AB

    发明人： Leif Svensson

    IPC分类号： C07D215/56

    CPC分类号： C07D215/56 ,  A61K31/4704

    摘要： 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.

    摘要翻译： 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。

    Immunomodulatory compounds
    8.
    发明申请
    Immunomodulatory compounds 有权
    免疫调节化合物

    公开(公告)号：US20040116461A1

    公开(公告)日：2004-06-17

    申请号：US10717519

    申请日：2003-11-21

    申请人： ACTIVE BIOTECH AB

    发明人： Ian Richard Matthews ,  Thomas Stephen Coulter ,  Chiara Ghiron ,  Chris James Brennan ,  Muhammed Kamal Uddin ,  Lars Olof Goran Pettersson ,  Dorthe da Graca Thrige ,  Philip Huxley

    IPC分类号： A61K031/4745 ,  A61K031/4162

    CPC分类号： C07D519/00 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04

    摘要： The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.

    摘要翻译： 本发明涉及新的杂环化合物，其制备方法，含有它们的组合物，以及用于临床治疗可能受益于免疫调节的医学病症的方法和用途，所述免疫调节包括类风湿性关节炎，多发性硬化，糖尿病，哮喘，移植， 系统性红斑狼疮和牛皮癣。 更具体地说，本发明涉及能够抑制CD80和CD28之间相互作用的CD80拮抗剂的新型杂环化合物。

    Process for the manufacture of quinoline derivatives
    9.
    发明申请
    Process for the manufacture of quinoline derivatives 有权
    制备喹啉衍生物的方法

    公开(公告)号：US20040034227A1

    公开(公告)日：2004-02-19

    申请号：US10459718

    申请日：2003-06-12

    申请人： ACTIVE BIOTECH AB

    发明人： Karl Jansson

    IPC分类号： C07D215/36

    CPC分类号： C07D215/56

    摘要： A process for the preparation of the compounds of general formula (I) 1 wherein R is selected from methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, sec.-butyl and allyl; R5 is selected from the methyl, ethyl, n-propyl, iso-propyl, methoxy, ethoxy, methylthio, ethylthio, n-propylthio, methylsulphinyl, ethylsulphinyl, fluoro, chloro, bromo, trifluoromethyl, and OCHxFy; wherein xnull0null2, ynull1null3 with the proviso that xnullynull3; R6 is hydrogen; or R5 and R6 taken together are methylenedioxy; Rnull is selected from methyl, methoxy, fluoro, chloro, bromo, trifluoromethyl, and OCHxFy, wherein xnull0null2, ynull1null3 with the proviso that xnullynull3; Rnull is selected form hydrogen, fluoro and chloro, with the proviso that Rnull is selected from fluoro and chloro only when Rnull is selected from fluoro and chloro; by reacting a quinoline-3-carboxylic acid ester derivative of formula A with an aniline derivative of formula B 2 in a solvent selected from straight or branched alkanes and cycloalkanes or mixtures thereof with a boiling point between 80 and 200null C.

    摘要翻译： 制备通式（I）的化合物的方法，其中R选自甲基，乙基，正丙基，异丙基，正丁基，异丁基，仲丁基和烯丙基; R5选自甲基，乙基，正丙基，异丙基，甲氧基，乙氧基，甲硫基，乙硫基，正丙硫基，甲基亚磺酰基，乙基亚磺酰基，氟，氯，溴，三氟甲基和OCH x Fy; 其中x = 0-2，y = 1-3，条件是x + y = 3; R6是氢; 或R5和R6一起是亚甲二氧基; R'选自甲基，甲氧基，氟，氯，溴，三氟甲基和OCH x Fy，其中x = 0-2，y = 1-3，条件是x + y = 3; R“选自氢，氟和氯，条件是当R'选自氟和氯时，R”选自氟和氯; 通过使式A的喹啉-3-羧酸酯衍生物与式B的苯胺衍生物在选自直链或支链烷烃和环烷烃的溶剂或其混合物中沸点在80-200℃之间进行反应。

    Quinoline derivatives
    10.
    发明申请
    Quinoline derivatives 有权
    喹啉衍生物

    公开(公告)号：US20020173519A1

    公开(公告)日：2002-11-21

    申请号：US10131176

    申请日：2002-04-25

    申请人： Active Biotech AB

    发明人： Anders Bjork ,  Stig Jonsson ,  Tomas Fex ,  Gunnar Hedlund

    IPC分类号： A61K031/47 ,  C07D215/36

    CPC分类号： C07D215/56

    摘要： Compounds of formula (I) 1 and tautomers thereof are effective for the treatment of mammals suffering from diseases resulting from autoimmunity and pathological inflammation.

    摘要翻译： 式（I）化合物及其互变异构体对于治疗患有由自身免疫和病理性炎症引起的疾病的哺乳动物是有效的。