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1. 发明申请

WO2008039882A1 A COMBINATION OF NIACIN AND A PROSTAGLANDIN D2 RECEPTOR ANTAGONIST 审中-公开
标题翻译： NIACIN和PROSTAGLANDIN D2受体拮抗剂的组合
公开(公告)号：WO2008039882A1
公开(公告)日：2008-04-03
申请号：PCT/US2007/079614
申请日：2007-09-27
申请人： SANOFI-AVENTIS U.S. LLC , HARRIS, Keith John
发明人： HARRIS, Keith John
IPC分类号： A61K31/505 , A61K31/455 , A61P3/00
CPC分类号： A61K31/455 , A61K31/505 , A61K2300/00
摘要： The present invention is directed to a pharmaceutical composition comprising Niacin or a pharmaceutically acceptable salt, solvate or N-oxide thereof, or a nicotinic acid receptor agonist, and a compound of formula (I) as defined herein, or an N-oxide thereof, or an ester prodrug thereof, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and its use for treating atherosclerosis, dyslipidemia, diabetes or a related condition while reducing substantial flushing.
摘要翻译：本发明涉及包含烟酸或其药学上可接受的盐，溶剂化物或N-氧化物或烟酸受体激动剂和本文定义的式（I）化合物或其N-氧化物的药物组合物，或其酯前体药物或其药学上可接受的盐，水合物或溶剂合物，以及其用于治疗动脉粥样硬化，血脂异常，糖尿病或相关病症同时减少实质性潮红的用途。

2. 发明申请

WO2006044732A2 2, 6-SUBSTITUTED-4-MONOSUBSTITUTEDAMINO-PYRIDIMIDINE AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2，6-取代的4-单核苷酸氨基嘧啶作为PROSTAGLANDIN D2受体拮抗剂
公开(公告)号：WO2006044732A2
公开(公告)日：2006-04-27
申请号：PCT/US2005/037148
申请日：2005-10-14
申请人： AVENTIS PHARMACEUTICALS INC. , LIM, Sungtaek , HARRIS, Keith, John , STEFANY, David , GARDNER, Charles, J. , CAO, Bin , BOFFEY, Ray , GILLESPY, Timothy, A. , AGUIAR, Joacy, C. , HUNT, Hazel, J. , DECHAUX, Elsa, A.
发明人： LIM, Sungtaek , HARRIS, Keith, John , STEFANY, David , GARDNER, Charles, J. , CAO, Bin , BOFFEY, Ray , GILLESPY, Timothy, A. , AGUIAR, Joacy, C. , HUNT, Hazel, J. , DECHAUX, Elsa, A.
IPC分类号： C07D239/46 , C07D409/04 , C07D413/04 , C07D403/04
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The present invention is directed a compound of Formula (I) as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (I) in admixture with a pharmaceutically acceptable carrier, and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, discorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like by administering to said patient a pharmaceutically effective amount of a compound according to Formula (I).
摘要翻译：本发明涉及如本文所定义的式（I）化合物，药物组合物，其包含药学上有效量的一种或多种根据式（I）的化合物与药学上可接受的载体的混合物，以及治疗患者的方法患有PGD2介导的障碍，包括但不限于过敏性疾病（如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），系统性肥大细胞增多症，伴有系统性肥大细胞活化的失调者，过敏性休克，支气管收缩，支气管炎，荨麻疹，湿疹，伴有瘙痒的疾病（如特应性皮炎和荨麻疹），伴随瘙痒的行为而产生的疾病（如白内障，视网膜脱离，炎症，感染和睡眠障碍）（如作为搔抓和殴打），炎症，慢性阻塞性肺疾病，缺血再灌注损伤 ry，脑血管意外，慢性类风湿性关节炎，胸膜炎，溃疡性结肠炎等，通过向所述患者施用药学有效量的根据式（I）的化合物。

3. 发明申请

WO2007121280A1 2,6-SUBSTITUTED-4-MONOSUBSTITUTED AMINO-PYRIMIDINE AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为前列腺素D2受体拮抗剂的2,6-取代的4-单核苷酸氨基嘧啶
公开(公告)号：WO2007121280A1
公开(公告)日：2007-10-25
申请号：PCT/US2007/066481
申请日：2007-04-12
申请人： SANOFI-AVENTIS , STEFANY, David , HARRIS, Keith John , GILLESPY, Timothy, Alan , GARDNER, Charles J. , AGUIAR, Joacy C.
发明人： STEFANY, David , HARRIS, Keith John , GILLESPY, Timothy, Alan , GARDNER, Charles J. , AGUIAR, Joacy C.
IPC分类号： C07D239/46 , C07D403/04 , C07D409/04 , A61K31/505 , A61P11/00
CPC分类号： C07D403/04 , C07D239/47 , C07D409/04
摘要： The present invention is directed to a compound of formula (I) wherein R 1 and R 2 are as defined herein, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, a pharmaceutically acceptable prodrug thereof, or a pharmaceutically acceptable salt, hydrate or solvate of the prodrug, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds of the invention in admixture with a pharmaceutically acceptable carrier, a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which are generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like by administering to said patient a pharmaceutically effective amount of a compound of the invention.
摘要翻译：本发明涉及其中R 1和R 2如本文所定义的式（I）化合物或其药学上可接受的盐，水合物或溶剂化物，其药学上可接受的前药，或其药学上可接受的盐，水合物或溶剂化物，药物组合物，其包含药学上有效量的一种或多种本发明化合物与药学上可接受的载体的混合物，治疗患者的方法来自PGD2介导的障碍，包括但不限于过敏性疾病（例如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），全身肥大细胞增多症，伴有全身性肥大细胞活化的病症，过敏性休克，支气管收缩，支气管炎，荨麻疹，湿疹，伴有瘙痒的疾病（如特应性皮炎和荨麻疹），疾病（如白内障，视网膜脱离，炎症，感染和睡眠障碍），其由伴随瘙痒的行为（例如搔抓和殴打），炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，慢性类风湿性关节炎，胸膜炎，溃疡性结肠炎等引起。通过向所述患者施用药学有效量的本发明化合物。

4. 发明申请

WO2011115943A1 A SUBSTITUTED PYRIMIDINE AS A PROSTAGLANDIN D2 RECEPTOR ANTAGONIST 审中-公开
标题翻译：作为PROSTAGLANDIN D2受体拮抗剂的替代吡咯胺
公开(公告)号：WO2011115943A1
公开(公告)日：2011-09-22
申请号：PCT/US2011/028433
申请日：2011-03-15
申请人： AVENTIS PHARMACEUTICALS INC. , HARRIS, Keith John , AGUIAR, Joacy C. , SHUM, Patrick Wai-Kwok , ZHAO, Zhicheng , POLI, Gregory B. , STOKLOSA, Gregory T. , CHOI-SLEDESKI, Yong-Mi , REILING, Stephan
发明人： HARRIS, Keith John , AGUIAR, Joacy C. , SHUM, Patrick Wai-Kwok , ZHAO, Zhicheng , POLI, Gregory B. , STOKLOSA, Gregory T. , CHOI-SLEDESKI, Yong-Mi , REILING, Stephan
IPC分类号： C07D403/04 , A61K31/505 , A61P11/00
CPC分类号： C07D403/04
摘要： The present invention is directed to a 2,6-substituted-4-monosubstitutedamino-pyrinudine compound of formula (I) as set forth herein, or an enantiomer thereof, or an ester prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such a compound. The invention also includes a method of treatment of a patient by the administration of a pharmaceutically effective amount of such a compound.
摘要翻译：本发明涉及本文所述的式（I）的2,6-取代-4-单取代的氨基 - 嘧啶嘌呤化合物或其对映异构体或其酯前药或其药学上可接受的盐，或包含这样的化合物。本发明还包括通过施用药学有效量的这种化合物来治疗患者的方法。

5. 发明申请

WO2006044732A3 2, 6-SUBSTITUTED-4-MONOSUBSTITUTEDAMINO-PYRIMIDINE AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2，6-取代的4-单核苷酸氨基嘧啶作为PROSTAGLANDIN D2受体拮抗剂
公开(公告)号：WO2006044732A3
公开(公告)日：2006-11-23
申请号：PCT/US2005037148
申请日：2005-10-14
申请人： AVENTIS PHARMA INC , LIM SUNGTAEK , HARRIS KEITH JOHN , STEFANY DAVID , GARDNER CHARLES J , CAO BIN , BOFFEY RAY , GILLESPY TIMOTHY A , AGUIAR JOACY C , HUNT HAZEL J , DECHAUX ELSA A
发明人： LIM SUNGTAEK , HARRIS KEITH JOHN , STEFANY DAVID , GARDNER CHARLES J , CAO BIN , BOFFEY RAY , GILLESPY TIMOTHY A , AGUIAR JOACY C , HUNT HAZEL J , DECHAUX ELSA A
IPC分类号： C07D239/46 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/04 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The present invention is directed a compound of Formula (I) as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (I) in admixture with a pharmaceutically acceptable carrier, and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, discorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like by administering to said patient a pharmaceutically effective amount of a compound according to Formula (I).
摘要翻译：本发明涉及如本文所定义的式（I）化合物，药物组合物，其包含药学上有效量的一种或多种根据式（I）的化合物与药学上可接受的载体的混合物，以及治疗患者的方法患有PGD2介导的障碍，包括但不限于过敏性疾病（如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），系统性肥大细胞增多症，伴有系统性肥大细胞活化的失调者，过敏性休克，支气管收缩，支气管炎，荨麻疹，湿疹，伴有瘙痒的疾病（如特应性皮炎和荨麻疹），伴随瘙痒的行为而产生的疾病（如白内障，视网膜脱离，炎症，感染和睡眠障碍）（如作为搔抓和殴打），炎症，慢性阻塞性肺疾病，缺血再灌注损伤 ry，脑血管意外，慢性类风湿性关节炎，胸膜炎，溃疡性结肠炎等，通过向所述患者施用药学有效量的根据式（I）的化合物。

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