1-[(4-Methoxyphenyl)sulfonyl]-4-piperidinecarboxylic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-[(4-Methoxyphenyl)sulfonyl]-4-piperidinecarboxylic acid
• 英文别名: 1-(4-methoxyphenyl)sulfonylpiperidine-4-carboxylic acid
• 化学式: C₁₃H₁₇NO₅S
• mdl: MFCD02331441
• 分子量: 299.34
• InChiKey: XCSWWTGQHOOLAE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.461
• 拓扑面积：
  92.3
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• NEW HSL INHIBITORS USEFUL IN THE TREATMENT OF DIABETES
  申请人：Ackermann Jean

  公开号：US20110065707A1

  公开（公告）日：2011-03-17

  The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof, wherein A 1 , A 2 , R 1 , R 2 , R 3 , R 4 , R 5 and R 6 have the significance given herein.

  本发明涉及式(I)的化合物以及其药学上可接受的盐，其中A1、A2、R1、R2、R3、R4、R5和R6具有本文中给出的含义。
• [EN] HSL INHIBITORS USEFUL IN THE TREATMENT OF DIABETES<br/>[FR] INHIBITEURS DE HSL UTILES DANS LE TRAITEMENT DU DIABÈTE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2011029808A1

  公开（公告）日：2011-03-17

  Compounds of formula (I), as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A1, A2, R1,R2 R3,R4 R5 and R6 have the significance given in claim 1. Objects of the present invention are the compounds of formula (I) and their aforementioned salts and esters and their use as therapeutically active substances, a process for the manufacture of the said compounds, intermediates, pharmaceutical compositions, medicaments containing the said compounds, their pharmaceutically acceptable salts or esters, the use of the said compounds, salts or esters for the treatment or prophylaxis of illnesses, especially in the treatment or prophylaxis of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis or obesity and the use of the said compounds, salts or esters for the production of medicaments for the treatment or prophylaxis of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis or obesity.

  化合物的化学式（I），以及其药学上可接受的盐可以用作药物组合物的形式，其中A1，A2，R1，R2，R3，R4，R5和R6具有权利要求1中给定的含义。本发明的目的是化学式（I）的化合物及其上述的盐和酯，以及它们作为治疗活性物质的用途，制造所述化合物的方法，中间体，含有所述化合物的药物组合物，含有所述化合物、其药学上可接受的盐或酯的药物，所述化合物、盐或酯的用途用于治疗或预防疾病，特别是用于治疗或预防糖尿病、代谢综合征、血脂异常、动脉粥样硬化或肥胖症，以及所述化合物、盐或酯的用途用于生产用于治疗或预防糖尿病、代谢综合征、血脂异常、动脉粥样硬化或肥胖症的药物。
• N-hydroxy-2-(alkyl, aryl, or heteroaryl sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors
  申请人：American Cyanamid Company

  公开号：US20020006922A1

  公开（公告）日：2002-01-17

  Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (is) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection having the formula 1 wherein R 2 and R 3 form a heterocyclic ring and A is S, S(O), or S(O)2, and R 1 and R 4 are defined herein.

  基质金属蛋白酶（MMPs）是一组酶，已被认为参与了结缔组织和基底膜的病理性破坏。这些含锌内切肽酶包括胶原酶、基质金属蛋白酶和明胶酶等几个亚组。TNF转化酶（TACE）是一种促炎细胞因子，催化膜结合型TNF-α前体蛋白形成TNF-α。预计基质金属蛋白酶和TACE的小分子抑制剂具有治疗多种疾病的潜力。本发明提供了用于治疗关节炎、肿瘤转移、组织溃疡、异常伤口愈合、牙周病、骨病、糖尿病（胰岛素抵抗）和HIV感染的基质金属蛋白酶（is）和TNF-α转化酶（TACE）的低分子量、非肽抑制剂，其化学式为1，其中R2和R3形成杂环环，A为S、S（O）或S（O）2，R1和R4如本文所定义。
• Inhibitors of cathepsin S
  申请人：IRM LLC

  公开号：US20040248887A1

  公开（公告）日：2004-12-09

  The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

  本发明提供了化合物、组合物和方法，用于选择性抑制蛋白酶S。在首选方面，当存在至少一种其他蛋白酶同工酶时，选择性抑制蛋白酶S。本发明还提供了通过选择性抑制蛋白酶S治疗受试者的疾病状态的方法。
• INHIBITORS OF CATHEPSIN S
  申请人：Liu Hong

  公开号：US20080242671A1

  公开（公告）日：2008-10-02

  The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

  本发明提供了化合物、组合物和方法，用于选择性抑制蛋白酶S。在首选方面，当存在至少一种其他蛋白酶同工酶时，选择性地抑制蛋白酶S。本发明还提供了通过选择性抑制蛋白酶S治疗受试者疾病状态的方法。