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    • 6. 发明授权
    • 8-(biaryl)quinoline PDE4 inhibitors
    • 8-(联芳)喹啉PDE4抑制剂
    • US07153968B2
    • 2006-12-26
    • US10517416
    • 2003-06-23
    • Daniel DubeMichel GallantPatrick LacombeDenis DeschenesLaurence DubeYves GirardDwight Macdonald
    • Daniel DubeMichel GallantPatrick LacombeDenis DeschenesLaurence DubeYves GirardDwight Macdonald
    • C07D219/08C07D215/12A61K31/47
    • C07D215/04C07D215/06C07D215/12C07D215/14C07D401/04C07D401/10C07D401/12C07D403/10C07D405/10C07D407/10C07D409/10C07D413/10C07D413/14C07D417/10C07D417/12C07D471/04C07F7/0812C07F9/60
    • 8-(biaryl) quinolines wherein the bi-aryl group at the 8-position is in a meta relationship to the quinoline group, are PDE4 inhibitors useful in the treatment of asthma, chronic bronchitis, chronic obstructive pulmonary disease, eosinophilic granuloma, psoriasis and other benign or malignant proliferative skin diseases, endotoxic shock, laminitis in horses, colic in horses, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and brain, inflammatory arthritis, chronic glomerulonephritis, atopic dermatitis, urticaria, adult respiratory distress syndrome, chronic obstructive pulmonary disease in animals, diabetes insipidus, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, arterial restenosis, ortherosclerosis, atherosclerosis, neurogenic inflammation, pain, cough, rheumatoid arthritis, ankylosing spondylitis, transplant rejection, graft versus host disease, hypersecretion of gastric acid, bacterial, fungal induced sepsis, viral induced sepsis, fungal induced septic shock, viral induced septic shock, inflammation-mediated chronic tissue degeneration, cytokine-mediated chronic tissue degeneration, osteoarthritis, cancer, cachexia, muscle wasting, depression, memory impairment, tumour growth, or cancerous invasion of normal tissues. In another aspect, the present invention is directed to a method of enhancing cognition in a healthy subject comprising administering a safe cognition enhancing amount of phosphodiesterase-4 inhibitor. In particular, this invention is directed to a method of enhancing memory, learning, retention, recall, awareness and judgement in health subjects comprising administering a safe and cognition enhancing amount of a phosphodiesterase-4 inhibitor.
    • 8-(联芳)喹啉,其中8-位上的双芳基与喹啉基团呈元间关系,是可用于治疗哮喘,慢性支气管炎,慢性阻塞性肺疾病,嗜酸性肉芽肿,银屑病的PDE4抑制剂 其他良性或恶性增殖性皮肤疾病,内毒素性休克,马匹中的扁桃体炎,马蹄痛,败血性休克,溃疡性结肠炎,克罗恩病,心肌和脑的再灌注损伤,炎症性关节炎,慢性肾小球肾炎,特应性皮炎,荨麻疹,成人呼吸窘迫 综合征,动物慢性阻塞性肺病,尿崩症,过敏性鼻炎,过敏性结膜炎,春季结膜炎,动脉再狭窄或动脉粥样硬化,动脉粥样硬化,神经源性炎症,疼痛,咳嗽,类风湿关节炎,强直性脊柱炎,移植排斥反应,移植物抗宿主病,分泌过多 的胃酸,细菌,真菌诱导的败血症,病毒诱导 d败血症,真菌诱发的败血症休克,病毒诱导的败血性休克,炎症介导的慢性组织变性,细胞因子介导的慢性组织变性,骨关节炎,癌症,恶病质,肌肉消瘦,抑郁,记忆障碍,肿瘤生长或正常组织的癌性侵袭 。 另一方面,本发明涉及一种增强健康受试者认知的方法,其包括施用安全认知增加量的磷酸二酯酶-4抑制剂。 特别地,本发明涉及一种在健康受试者中增强记忆,学习,保留,召回,意识和判断的方法,包括施用安全和认知增加量的磷酸二酯酶-4抑制剂。
    • 7. 发明申请
    • 8-(Biaryl)quinoline pde4 inhibitors
    • 8-(双芳基)喹啉pde4抑制剂
    • US20050234238A1
    • 2005-10-20
    • US10517416
    • 2003-06-23
    • Daniel DubeMichel GallantPatrick LacombeDenis DeschenesLaurence DubeYves GirardDwight Macdonald
    • Daniel DubeMichel GallantPatrick LacombeDenis DeschenesLaurence DubeYves GirardDwight Macdonald
    • A61P29/00C07D215/04C07D215/12C07D401/04C07D401/10C07D403/10C07D407/10C07D409/10C07D413/10C07D413/14C07D417/10C07D471/02C07D471/04C07F7/08C07F9/60C07D41/02C07D43/14
    • C07D215/04C07D215/06C07D215/12C07D215/14C07D401/04C07D401/10C07D401/12C07D403/10C07D405/10C07D407/10C07D409/10C07D413/10C07D413/14C07D417/10C07D417/12C07D471/04C07F7/0812C07F9/60
    • 8-(biaryl) quinolines wherein the bi-aryl group at the 8-position is in a meta relationship to the quinoline group, are PDE4 inhibitors useful in the treatment of asthma, chronic bronchitis, chronic obstructive pulmonary disease, eosinophilic granuloma, psoriasis and other benign or malignant proliferative skin diseases, endotoxic shock, laminitis in horses, colic in horses, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and brain, inflammatory arthritis, chronic glomerulonephritis, atopic dermatitis, urticaria, adult respiratory distress syndrome, chronic obstructive pulmonary disease in animals, diabetes insipidus, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, arterial restenosis, ortherosclerosis, atherosclerosis, neurogenic inflammation, pain, cough, rheumatoid arthritis, ankylosing spondylitis, transplant rejection, graft versus host disease, hypersecretion of gastric acid, bacterial, fungal induced sepsis, viral induced sepsis, fungal induced septic shock, viral induced septic shock, inflammation-mediated chronic tissue degeneration, cytokine-mediated chronic tissue degeneration, osteoarthritis, cancer, cachexia, muscle wasting, depression, memory impairment, tumour growth, or cancerous invasion of normal tissues. In another aspect, the present invention is directed to a method of enhancing cognition in a healthy subject comprising administering a safe cognition enhancing amount of phosphodiesterase-4 inhibitor. In particular, this invention is directed to a method of enhancing memory, learning, retention, recall, awareness and judgement in health subjects comprising administering a safe and cognition enhancing amount of a phosphodiesterase-4 inhibitor.
    • 8-(联芳)喹啉,其中8-位上的双芳基与喹啉基团呈元间关系,是可用于治疗哮喘,慢性支气管炎,慢性阻塞性肺疾病,嗜酸性肉芽肿,银屑病的PDE4抑制剂 其他良性或恶性增殖性皮肤疾病,内毒素性休克,马匹中的扁桃体炎,马蹄痛,败血性休克,溃疡性结肠炎,克罗恩病,心肌和脑的再灌注损伤,炎症性关节炎,慢性肾小球肾炎,特应性皮炎,荨麻疹,成人呼吸窘迫 综合征,动物慢性阻塞性肺病,尿崩症,过敏性鼻炎,过敏性结膜炎,春季结膜炎,动脉再狭窄或动脉粥样硬化,动脉粥样硬化,神经源性炎症,疼痛,咳嗽,类风湿关节炎,强直性脊柱炎,移植排斥反应,移植物抗宿主病,分泌过多 的胃酸,细菌,真菌诱导的败血症,病毒诱导 d败血症,真菌诱发的败血症休克,病毒诱导的败血性休克,炎症介导的慢性组织变性,细胞因子介导的慢性组织变性,骨关节炎,癌症,恶病质,肌肉消瘦,抑郁,记忆障碍,肿瘤生长或正常组织的癌性侵袭 。 另一方面,本发明涉及一种增强健康受试者认知的方法,其包括施用安全认知增加量的磷酸二酯酶-4抑制剂。 特别地,本发明涉及一种在健康受试者中增强记忆,学习,保留,召回,意识和判断的方法,包括施用安全和认知增加量的磷酸二酯酶-4抑制剂。