1-(7-fluoro-1-(2-methoxy-ethyl)-indole-3-yl)-carbonyl-5'-aminomethyl-spiro[piperidine-4,3'-(2H)-benzo[b]furan] hydrochloride | 1374881-75-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 1-(7-fluoro-1-(2-methoxy-ethyl)-indole-3-yl)-carbonyl-5'-aminomethyl-spiro[piperidine-4,3'-(2H)-benzo[b]furan] hydrochloride
• 英文别名: [5-(aminomethyl)spiro[2H-1-benzofuran-3,4'-piperidine]-1'-yl]-[7-fluoro-1-(2-methoxyethyl)indol-3-yl]methanone;hydrochloride
• CAS: 1374881-75-0
• 化学式: C₂₅H₂₈FN₃O₃*ClH
• 分子量: 473.975
• InChiKey: SWEPXYKHIZACIR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.87
• 重原子数：
  33
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  69.7
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] SPIROPIPERIDINE BENZYLAMINES AS BETA-TRYPTASE INHIBITORS<br/>[FR] SPIROPIPÉRIDINE BENZYLAMINESUTILES COMME INHIBITRICES DE LA BÊTA-TRYPTASE
  申请人：SANOFI SA

  公开号：WO2011079103A1

  公开（公告）日：2011-06-30

  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.

  本发明公开并声明了一系列式(I)的取代螺环哌啶苄胺化合物，其中R如本文所述。更具体地说，本发明的化合物是β-色胺酶的抑制剂，因此可用作治疗关节炎，包括关节炎、类风湿关节炎和其他关节炎症状，如类风湿脊柱炎、痛风性关节炎、创伤性关节炎、风疹性关节炎、银屑病性关节炎、骨关节炎或其他慢性炎症性关节疾病，或关节软骨破坏疾病、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、硬皮病、肺纤维化、肝硬化、心肌纤维化、神经纤维瘤、肥厚性瘢痕、各种皮肤病症，例如特应性皮炎和银屑病、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的药物。