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    • 6. 发明申请
    • COMBINATION 408
    • 组合408
    • US20100144606A1
    • 2010-06-10
    • US12488027
    • 2009-06-19
    • Stephen ConnollyAdrian FisherAlexander HumphriesAndrew WattsKatherine Wiley
    • Stephen ConnollyAdrian FisherAlexander HumphriesAndrew WattsKatherine Wiley
    • A61K38/12C07C229/28A61P11/06
    • A61K45/06A61K31/428A61K2300/00
    • The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is N-Cyclohexyl-N3-[2-(3-fluorophenyl)ethyl]-N-(2-{[2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)-β-alaninamide or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DP1 antagonist; an Histone Deacetylase Inducer; an IKK2 inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; an MPO inhibitor; a muscarinic antagonist; a p38 inhibitor; a PDE inhibitor; a PPARγ agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease (for example chronic obstructive pulmonary disease (COPD) or asthma); to certain salts of N-Cyclohexyl-N3-[2-(3-fluorophenyl)ethyl]-N-(2-{[2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)-β-alaninamide and to an intermediate useful in the manufacture of this pharmaceutically active substance and salts thereof.
    • 本发明提供了包含N-环己基-N3- [2-(3-氟苯基)乙基] -N-(2 - {[2-(4-羟基-2- -2-氧代-2,3-二氢-1,3-苯并噻唑-7-基)乙基]氨基}乙基) - 丙氨酰胺或其盐,和第二活性成分,选自:非甾体糖皮质激素受体(GR 受体)激动剂; 抗氧化剂 CCR1拮抗剂; 趋化因子拮抗剂(不是CCR1); 皮质类固醇 CRTh2拮抗剂; DP1拮抗剂; 组蛋白脱乙酰酶诱导剂; IKK2抑制剂; COX抑制剂; 脂氧合酶抑制剂; 白细胞三烯受体拮抗剂; MPO抑制剂; 毒蕈碱拮抗剂 一种p38抑制剂; PDE抑制剂; PPARγ激动剂; 蛋白酶抑制剂; 他汀类 血栓素拮抗剂; 血管扩张剂 或ENAC阻断剂(上皮钠通道阻断剂); 及其用于治疗呼吸系统疾病(如慢性阻塞性肺疾病(COPD)或哮喘)); 对于N-环己基-N3- [2-(3-氟苯基)乙基] -N-(2 - {[2-(4-羟基-2-氧代-2,3-二氢-1,3-苯并噻唑) -7-基)乙基]氨基}乙基) - 乙酰氨基脲和可用于制备该药物活性物质及其盐的中间体。