1-Methoxynaphthalene-2-sulfonyl chloride | 56875-52-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 1-Methoxynaphthalene-2-sulfonyl chloride
• CAS: 56875-52-6
• 化学式: C₁₁H₉ClO₃S
• 分子量: 256.71
• InChiKey: BPDGXUXLCACGBF-UHFFFAOYSA-N

物化性质

• 沸点：
  415.2±28.0 °C(Predicted)
• 密度：
  1.393±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  51.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-Methoxynaphthalene-2-sulfonyl chloride 在 4-二甲氨基吡啶 、 magnesium 作用下， 以 二氯甲烷 为溶剂， 反应 6.5h， 生成 1-(1-Propan-2-ylnaphthalen-2-yl)sulfonylpyrrolidine
  参考文献：
  名称：

  Hattori, Tetsutaro; Suzuki, Mikio; Tomita, Noriyuki, Journal of the Chemical Society. Perkin transactions I, 1997, # 8, p. 1117 - 1123

  摘要：

  DOI：
• 作为产物：
  描述：

  1-甲氧基萘 在 正丁基锂 、 磺酰氯 、 四甲基乙二胺 、 二氧化硫 作用下， 生成 1-Methoxynaphthalene-2-sulfonyl chloride
  参考文献：
  名称：

  Hattori, Tetsutaro; Suzuki, Mikio; Tomita, Noriyuki, Journal of the Chemical Society. Perkin transactions I, 1997, # 8, p. 1117 - 1123

  摘要：

  DOI：

文献信息

• Thrombin inhibitors. 2. Amide derivatives of N.alpha.-substituted L-arginine
  作者：Ryoji Kikumoto、Yoshikuni Tamao、Kazuo Ohkubo、Tohru Tezuka、Shinji Tonomura、Shosuke Okamoto、Yoshinori Funahara、Akiko Hijikata

  DOI：10.1021/jm00182a004

  日期：1980.8

  with tetralin or an oxygen-containing heterocyclic compound as a N alpha-substituent showed an inhibition with an I50 less than 10(-5) M. N-Monosubstituted derivatives of N alpha-dansyl-L-arginine amide were not hydrolyzed at all by thrombin and were hydrolyzed very slowly by trypsin, and N,N-disubstituted derivatives were not hydrolyzed at all by both enzymes.

  制备了一系列具有取代或未取代的萘和杂环化合物作为Nα取代基的Nα-（芳基磺酰基）-L-精氨酸酰胺衍生物，并测试了它们作为凝血酶凝血活性的抑制剂。Nα-丹磺酰基-L-精氨酸酰胺的Nn-丁基和Nn-丁基-N-甲基衍生物对Nα-丹磺酰基-L-精氨酸酰胺的N-烷基和N，N-二烷基衍生物的抑制作用最大。它们的抑制作用与I50为2 X 10（-6）M的Nα-丹磺酰基-L-精氨酸-正丁酯的抑制作用一样。Nα-取代的4-甲基萘他磺酰基-L-精氨酸酰胺衍生物-和4-乙基哌啶也显示出有效的抑制作用，I50为10（-7）至10（-6）M。在该研究中，最有效的抑制作用是1- [Nα-（4,6-二甲氧基萘-2-磺酰基]-精氨酰基] -4-甲基哌啶，I50为7。
• [EN] SELECTIVE HYDROXAMIC ACID BASED MMP-12 AND MMP-13 INHIBITORS<br/>[FR] INHIBITEURS SÉLECTIFS DE MMP-12 ET MMP-13 À BASE D'ACIDE HYDROXAMIQUE
  申请人：NOVARTIS AG

  公开号：WO2010007027A1

  公开（公告）日：2010-01-21

  The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP- 13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).

  本发明提供了一种具有化学式(I)的化合物，该化合物是MMP-12和/或MMP-13的抑制剂，因此可用于治疗由MMP-12和/或MMP-13异常活性特征的疾病或疾病。因此，化合物的化学式(I)可用于治疗由MMP-12和/或MMP-13介导的疾病或疾病。最后，本发明还提供了包括化学式(I)的化合物的药物组合物。
• SELECTIVE HYDROXAMIC ACID BASED MMP-12 AND MMP-13 INHIBITORS
  申请人：McQuire Leslie Wighton

  公开号：US20110112076A1

  公开（公告）日：2011-05-12

  The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).

  本发明提供了一种式子为(I)的化合物，该化合物是MMP-12和/或MMP-13的抑制剂，因此可用于治疗MMP-12和/或MMP-13活性异常引起的疾病或疾病。因此，式(I)的化合物可用于治疗由MMP-12和/或MMP-13介导的疾病或疾病。最后，本发明还提供了包括式(I)的化合物的药物组合物。
• US8841291B2
  申请人：——

  公开号：US8841291B2

  公开（公告）日：2014-09-23
• [EN] SULFONIC ACID OR SULFONYLAMINO N-(HETEROARALKYL)-AZAHETEROCYCLYLAMIDE COMPOUNDS<br/>[FR] COMPOSES A BASE D'ACIDE SULFONIQUE OU DE SULFONYL-AMINO N-(HETEROARALKYL)-AZAHETEROCYCLYLAMIDE
  申请人：AVENTIS PHARMA GMBH

  公开号：WO2001039759A2

  公开（公告）日：2001-06-07

  The compounds of formula (I) herein exhibit useful phamacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula (I), compositions containing compounds of formula (I), and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.