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    • 4. 发明申请
    • SPIROPIPERIDINE BENZYLAMINES AS BETA-TRYPTASE INHIBITORS
    • 螺吡啶苯甲酰胺作为β-酪氨酸酶抑制剂
    • WO2011079103A1
    • 2011-06-30
    • PCT/US2010/061464
    • 2010-12-21
    • SANOFICHOI-SLEDESKI, Yong MiLIANG, GuyanPOLI, Gregory B.
    • CHOI-SLEDESKI, Yong MiLIANG, GuyanPOLI, Gregory B.
    • C07D491/107A61K31/438A61P19/02A61P11/06A61P17/00
    • C07D491/107
    • The present invention discloses and claims a series of substituted spiropiperidine benzylamines of formula (I) wherein R is as described herein. More specifically, the compounds of this invention are inhibitors of β-tryptase and are, therefore, useful as pharmaceutical agents for treating joint inflammation, including arthritis, rheumatoid arthritisand other arthritic condition such as rheumatoid spondylitis, gouty arthπtis, traumatic arthritis, rubella arthritis, psoriatic arthritis, osteoarthritis or other chronic inflammatory joint disease, or diseases of joint cartilage destruction, ocular conjunctivitis, vernal conjunctivitis, inflammatory bowel disease, asthma, allergic rhinitis, interstitial lung diseases, fibrosis, sceleroderma, pulmonary fibrosis, liver cirrhosis, myocardial fibrosis, neurofibromas, hypertrophic scars, various dermatological conditions, for example, atopic dermatitis and psoriasis, myocardial infarction, stroke, angina or other consequences of atherosclerotic plaque rupture, as well as periodontal disease, diabetic retinopathy, macular degeneration, acute macular degeneration, wet macular degeneration, tumour growth, anaphylaxis, multiple sclerosis, peptic ulcers, or a syncytial viral infection.
    • 本发明公开并要求一系列取代的式(I)的哌啶哌啶苄胺,其中R如本文所述。 更具体地说,本发明的化合物是β-胰蛋白酶抑制剂,因此可用作治疗关节炎的药剂,包括关节炎,类风湿性关节炎和其它关节炎病症如类风湿性脊椎炎,痛风性关节炎,创伤性关节炎,风疹性关节炎, 牛皮癣关节炎,骨关节炎或其他慢性炎性关节疾病,关节软骨破坏性疾病,眼结膜炎,春季结膜炎,炎性肠病,哮喘,过敏性鼻炎,间质性肺病,纤维化,强迫症,肺纤维化,肝硬化,心肌纤维化, 神经纤维瘤,肥厚性瘢痕,各种皮肤病学条件,例如特应性皮炎和牛皮癣,心肌梗死,中风,心绞痛或动脉粥样硬化斑块破裂的其他后果,以及牙周病,糖尿病性视网膜病变,黄斑变性,急性黄斑变性,湿性黄斑变性 ,肿瘤生长,过敏反应,多发性硬化,消化性溃疡或合胞病毒感染。