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公开(公告)号：US08658642B2
公开(公告)日：2014-02-25
申请号：US13841705
申请日：2013-03-15
申请人： Tai Wei Ly , Jared Andrew Forrester
发明人： Tai Wei Ly , Jared Andrew Forrester
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/497 , A61K31/495
CPC分类号： A61K31/5377 , A61K31/495 , A61K31/496 , A61K31/497 , C07D213/50 , C07D231/12 , C07D241/12 , C07D261/08 , C07D285/06 , C07D295/26 , C07D333/22
摘要： Provided herein are arylsulfonamides 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活性的芳基磺酰胺及其药物组合物。 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。
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公开(公告)号：US08420639B2
公开(公告)日：2013-04-16
申请号：US12764894
申请日：2010-04-21
申请人： Tai Wei Ly , Jared Andrew Forrester
发明人： Tai Wei Ly , Jared Andrew Forrester
IPC分类号： A61K31/5377 , A61K31/495 , A61K31/496 , C07D241/04 , C07D413/06 , C07D401/06
CPC分类号： A61K31/5377 , A61K31/495 , A61K31/496 , A61K31/497 , C07D213/50 , C07D231/12 , C07D241/12 , C07D261/08 , C07D285/06 , C07D295/26 , C07D333/22
摘要： Provided herein are arylsulfonamides 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活性的芳基磺酰胺及其药物组合物。 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。
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公开(公告)号：US20100273785A1
公开(公告)日：2010-10-28
申请号：US12764249
申请日：2010-04-21
申请人： Tai Wei Ly , Garrett Thomas Potter
发明人： Tai Wei Ly , Garrett Thomas Potter
IPC分类号： A61K31/54 , A61K31/5375 , A61K31/495 , A61K31/4453 , C07D295/26 , C07D241/18 , C07D211/96 , A61P11/06 , A61P29/00 , A61P37/02 , A61P31/18 , A61P25/28 , A61P11/00 , A61P37/08
CPC分类号： C07D295/26 , A61K31/445 , A61K31/4453 , A61K31/495 , A61K31/5375 , A61K31/54 , A61K45/06 , C07D211/96 , C07D241/04 , C07D241/08 , C07D265/30
摘要： Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists of Formula I or II, and pharmaceutical compositions thereof: wherein X, Y, Z, and R1-R5 are as defined herein. 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： 本文提供式I或II的2,5-二取代芳基磺酰胺CCR3拮抗剂及其药物组合物：其中X，Y，Z和R 1 -R 5如本文所定义。 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。
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公开(公告)号：US20100273782A1
公开(公告)日：2010-10-28
申请号：US12764900
申请日：2010-04-21
IPC分类号： A61K31/445 , C07D211/58 , C07D295/14 , C07D243/08 , C07D401/04 , C07D487/04 , A61K31/495 , A61K31/551 , A61K31/5375 , A61K31/4468 , A61K31/454 , A61K31/277 , A61K31/54 , A61P11/06 , A61P29/00 , A61P11/00 , A61P19/02 , A61P9/00
CPC分类号： C07D487/04 , C07C311/29 , C07C323/67 , C07D211/96 , C07D241/04 , C07D243/08 , C07D295/26 , C07D403/04
摘要： Provided herein are 2,5-disubstituted arylsulfonamides 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2,5-二取代的芳基磺酰胺及其药物组合物。 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。
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公开(公告)号：US20100240685A1
公开(公告)日：2010-09-23
申请号：US12679893
申请日：2008-09-24
IPC分类号： A61K31/505 , C07D239/38 , A61P27/14 , A61P29/00 , A61P35/02 , A61P19/02 , A61P1/00 , A61P11/06
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。
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6.发明申请Pyrimidine derivatives useful for the treatment of diseases mediated by crth2 有权可用于治疗由crth2介导的疾病的嘧啶衍生物公开(公告)号：US20070129355A1
公开(公告)日：2007-06-07
申请号：US10554668
申请日：2004-04-14
申请人： Tai-wei Ly , Yuji Koriyama , Takashi Yoshino , Hiroki Sato , Kazuho Tanaka , Hiromi Sugimoto , Yoshihisa Manabe , Kevin Bacon , Klaus Urbahns , Masanori Seki , Takuya Shintani
发明人： Tai-wei Ly , Yuji Koriyama , Takashi Yoshino , Hiroki Sato , Kazuho Tanaka , Hiromi Sugimoto , Yoshihisa Manabe , Kevin Bacon , Klaus Urbahns , Masanori Seki , Takuya Shintani
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/506 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D239/42 , C07D239/30 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12
摘要： The present invention relates to a pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine 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： 本发明涉及式（I）的嘧啶衍生物及其盐，其可用作药物制剂的活性成分。 本发明的嘧啶衍生物具有优异的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。
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公开(公告)号：US20130274227A1
公开(公告)日：2013-10-17
申请号：US13830712
申请日：2013-03-14
IPC分类号： C07D231/38 , A61K31/4439 , C07D401/12 , C07D405/12 , A61K31/4155 , C07D417/12 , A61K31/427 , C07D403/12 , A61K45/06 , A61K31/506 , C07D409/14 , A61K31/4184 , A61K31/4178 , A61K31/496 , A61K31/5377 , A61K31/454 , C07D409/12 , C07F5/02 , A61K31/69 , A61K31/415
CPC分类号： C07D413/12 , A61K31/415 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4184 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/69 , A61K45/06 , C07D231/38 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07F5/025
摘要： Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
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公开(公告)号：US08324229B2
公开(公告)日：2012-12-04
申请号：US12679895
申请日：2008-09-24
IPC分类号： C07D239/38 , C07D239/47 , A61K31/505
CPC分类号： C07D239/38 , C07D239/47 , C07D239/58 , C07D403/12
摘要： Provided herein are alkylthio substituted pyrimidine compounds having CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity, useful for the treatment or prophylaxis 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（在Th2细胞上表达的G蛋白偶联化学引诱物受体）拮抗活性的烷硫基取代的嘧啶化合物，其可用于治疗或预防与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。
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9.发明授权Pyrimidine derivatives useful for the treatment of diseases mediated by CRTH2 有权可用于治疗由CRTH2介导的疾病的嘧啶衍生物公开(公告)号：US07812160B2
公开(公告)日：2010-10-12
申请号：US10554668
申请日：2004-04-14
申请人： Tai-wei Ly , Yuji Koriyama , Takashi Yoshino , Hiroki Sato , Kazuho Tanaka , Hiromi Sugimoto , Yoshihisa Manabe , Kevin Bacon , Klaus Urbahns , Masanori Seki , Takuya Shintani
发明人： Tai-wei Ly , Yuji Koriyama , Takashi Yoshino , Hiroki Sato , Kazuho Tanaka , Hiromi Sugimoto , Yoshihisa Manabe , Kevin Bacon , Klaus Urbahns , Masanori Seki , Takuya Shintani
IPC分类号： C07D239/42 , C07D239/34 , C07D239/48 , C07D401/12 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D407/12 , A61K31/505 , A61K31/506 , A61P11/06
CPC分类号： C07D239/42 , C07D239/30 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12
摘要： The present invention relates to a pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine 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： 本发明涉及式（I）的嘧啶衍生物及其盐，其可用作药物制剂的活性成分。 本发明的嘧啶衍生物具有优异的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。
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10.发明授权Isotopically enriched pyrimidin-5-yl acetic acid derivatives as CRTH2 antagonists 有权同位素富集的嘧啶-5-基乙酸衍生物作为CRTH2拮抗剂公开(公告)号：US08541419B2
公开(公告)日：2013-09-24
申请号：US13061921
申请日：2009-09-01
申请人： Tai Wei Ly
发明人： Tai Wei Ly
IPC分类号： A01N43/54 , C07D239/42 , C07D239/02 , C07D401/04
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。
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