PARTICULATES OF A CRTH2 ANTAGONIST
    22.
    发明申请
    PARTICULATES OF A CRTH2 ANTAGONIST 有权
    CRTH2拮抗剂的颗粒

    公开(公告)号:US20110052701A1

    公开(公告)日:2011-03-03

    申请号:US12665706

    申请日:2008-06-18

    申请人: Tai Wei Ly Hui-Yin Li

    发明人: Tai Wei Ly Hui-Yin Li

    CPC分类号: C07D239/48 Y10T428/2982

    摘要: Provided herein are particulates of {4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)benzyl)pyrimidin-5-yl} acetic acid in amorphous or crystalline forms, processes for their preparation, pharmaceutical compositions comprising them, and methods of their use for treating, preventing, or ameliorating one or more symptoms of a CRTH2-mediated disorder or disease.

    摘要翻译: 本文提供了无定形或结晶形式的{4,6-双(二甲基氨基)-2-(4-(4-(三氟甲基)苯甲酰氨基)苄基)嘧啶-5-基}乙酸的颗粒,其制备方法,药物 包含它们的组合物及其用于治疗,预防或改善CRTH2介导的病症或疾病的一种或多种症状的方法。

    Imidazo[1,2-C]Pyrimidinylacetic Acid Derivatives
    24.
    发明申请
    Imidazo[1,2-C]Pyrimidinylacetic Acid Derivatives 有权
    咪唑并[1,2-C]嘧啶基乙酸衍生物

    公开(公告)号:US20090012102A1

    公开(公告)日:2009-01-08

    申请号:US10585429

    申请日:2005-01-19

    CPC分类号: C07D487/04

    摘要: The present invention relates to an imidazo[1,2-c]pyrimidinylacetic acid derivative and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The imidazo[1,2-c]pyrimidinylacetic acid derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis.

    摘要翻译: 本发明涉及可用作药物制剂活性成分的咪唑并[1,2-c]嘧啶基乙酸衍生物及其盐。 本发明的咪唑并[1,2-c]嘧啶基乙酸衍生物具有优异的CRTH2(G蛋白偶联化学引诱物受体,在Th2细胞上表达)拮抗活性,可用于预防和治疗与CRTH2活性相关的疾病 特别是用于治疗过敏性疾病如哮喘,过敏性鼻炎,特应性皮炎和过敏性结膜炎; 嗜酸性粒细胞相关疾病,如中华综合征和鼻窦炎; 嗜碱性粒细胞相关疾病,如嗜碱性白血病,慢性荨麻疹和人类和其他哺乳动物的嗜碱性白细胞增多症; 以T淋巴细胞为特征的炎性疾病和白血球浸润如银屑病,湿疹,炎性肠病,溃疡性结肠炎,克罗恩病,COPD(慢性阻塞性肺病)和关节炎等。

    Isotopically enriched arylsulfonamide CCR3 antagonists
    25.
    发明授权
    Isotopically enriched arylsulfonamide CCR3 antagonists 有权
    同位素富集的芳基磺酰胺CCR3拮抗剂

    公开(公告)号:US08999995B2

    公开(公告)日:2015-04-07

    申请号:US13038251

    申请日:2011-03-01

    CPC分类号: C07D295/26 C07B59/002

    摘要: Provided herein are isotopically enriched arylsulfonamides, for example, of Formula I, that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.

    摘要翻译: 本文提供了可用于调节CCR3活性的同位素富集的芳基磺酰胺,例如式I,以及其药物组合物。 本文还提供其用于治疗,预防或改善CCR3介导的病症,疾病或病症的一种或多种症状的方法。

    2-S-benzyl substituted pyrimidines as CRTH2 antagonists
    28.
    发明授权
    2-S-benzyl substituted pyrimidines as CRTH2 antagonists 有权
    2-S-苄基取代的嘧啶作为CRTH2拮抗剂

    公开(公告)号:US08314116B2

    公开(公告)日:2012-11-20

    申请号:US12679893

    申请日:2008-09-24

    IPC分类号: C07D239/47 A61K31/505

    CPC分类号: C07D239/47

    摘要: Provided herein are 2-S-benzyl pyrimidine compounds having CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity, useful for the prophylaxis and treatment of diseases associated with CRTH2 activity, including the treatment of allergic diseases, eosinophil-related diseases and basophil-related diseases.

    摘要翻译: 本文提供了具有CRTH2(G蛋白偶联化学引诱物受体,Th2细胞表达)拮抗活性的2-S-苄基嘧啶化合物,可用于预防和治疗与CRTH2活性相关的疾病,包括治疗过敏性疾病,嗜酸性粒细胞 相关疾病和嗜碱性粒细胞相关疾病。

    ISOTOPICALLY ENRICHED PYRIMIDIN-5-YL ACETIC ACID DERIVATIVES AS CRTH2 ANTAGONISTS
    29.
    发明申请
    ISOTOPICALLY ENRICHED PYRIMIDIN-5-YL ACETIC ACID DERIVATIVES AS CRTH2 ANTAGONISTS 有权
    作为CRTH2拮抗剂的同位素富集的吡哩啶-5-YL乙酸衍生物

    公开(公告)号:US20110172250A1

    公开(公告)日:2011-07-14

    申请号:US13061921

    申请日:2009-09-01

    申请人: Tai Wei Ly

    发明人: Tai Wei Ly

    CPC分类号: C07D239/48

    摘要: Provided herein are 2H- and 13C-enriched compounds of formula (I) or (II); wherein R is as defined herein, and wherein at least one hydrogen atom, in certain embodiments, three or more hydrogen atoms, are deuterium atoms or at least one carbon atom is a carbon-13 atom. Also provided are pharmaceutical compositions and methods using the 2H- and 13C-enriched compounds, useful for treating CRTH2-related diseases or disorders such as, for example, asthma, allergic rhinitis, atopic dermatitis, allergic conjuvatitis, Churg-Strauss syndrome, sinusitis, basophilic leukemia, chronic urticaria or basophilic leukocytosis.

    摘要翻译: 本文提供了式(I)或(II)的富含2H-和13C的化合物; 其中R如本文所定义,并且其中至少一个氢原子(在某些实施方案中为三个或更多个氢原子)为氘原子或至少一个碳原子为碳-13原子。 还提供了使用富含2H和13C的化合物的药物组合物和方法,其可用于治疗CRTH2相关疾病或病症,例如哮喘,过敏性鼻炎,特应性皮炎,过敏性结膜炎,Churg-Strauss综合征,鼻窦炎, 嗜碱性白血病,慢性荨麻疹或嗜碱性白细胞增多症。

    AMINE SALTS OF A CRTH2 ANTAGONIST
    30.
    发明申请
    AMINE SALTS OF A CRTH2 ANTAGONIST 有权
    CRTH2 ANTAGONIST的胺盐

    公开(公告)号:US20110034482A1

    公开(公告)日:2011-02-10

    申请号:US12665705

    申请日:2008-06-18

    申请人: Tai Wei Ly

    发明人: Tai Wei Ly

    CPC分类号: C07D239/48

    摘要: Provided are amine salts of {4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)benzyl)pyrimidin-5-yl}-acetic acid, processes for their preparation, pharmaceutical compositions containing them, and their use for treating, preventing, or ameliorating one or more symptoms of a CRTH2-mediated disorder or disease.

    摘要翻译: 提供{4,6-双(二甲基氨基)-2-(4-(4-(三氟甲基)苯甲酰氨基)苄基)嘧啶-5-基} - 乙酸的胺盐,其制备方法,含有它们的药物组合物, 以及它们用于治疗,预防或改善CRTH2介导的病症或疾病的一种或多种症状的用途。