2-tert-Butyl-5-nitrofuran | 841243-44-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 呋喃
• 英文名称: 2-tert-Butyl-5-nitrofuran
• CAS: 841243-44-5
• 化学式: C8H11NO3
• 分子量: 169.18
• InChiKey: XLERQSNLKOUOIP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  59
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• QUINOLONE COMPOUND
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：US20140179675A1

  公开（公告）日：2014-06-26

  The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R 1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R 2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R 3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile -associated diarrhea.

  本发明提供了一种由式(I)表示的化合物 其中X是氢原子或氟原子；R是氢原子或烷基；R 1 是(1)环丙基，可选地取代1至3个卤素原子，或(2)苯基，可选地取代1至3个卤素原子；R 2 是烷基，烷氧基，卤代烷氧基，卤素原子，氰基等；R 3 是7-氧代-7,8-二氢-1,8-萘啉基，3-吡啶基等，或其盐。本发明的化合物对 艰难梭菌 具有优异的抗菌活性，并可用于预防或治疗肠道感染，如 艰难梭菌 相关性腹泻。
• PEPTIDE AND PEPTIDE MIMETIC BINDING ANTAGONISTS OF POLO-LIKE KINASE 1 POLO BOX DOMAIN AND METHODS OF USE
  申请人：THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH & HUMAN SERVIC

  公开号：US20160039872A1

  公开（公告）日：2016-02-11

  The invention provides novel compounds that may serve as anticancer therapeutics. The compounds of the invention bind to polo-like kinases through the polo-box domain. In certain embodiments, the compounds of the invention are POM-protected peptide derivatives. The use of cationic bis-alkyl his residues in combination with a mono POM-protected pho-phoryl group results in a peptide possessing an overall neutral charge. The peptide derivatives of the invention have achieved both good efficacy and an enhanced bioavailability. The invention also provides methods of use, compositions, and kits thereof. Further, the invention provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.

  该发明提供了可能用作抗癌治疗的新化合物。该发明的化合物通过波洛盒结构结合到波洛样激酶。在某些实施方式中，该发明的化合物是POM保护的肽衍生物。在结合了阳离子双烷基组氨酸残基和单个POM保护的磷酸化基团的情况下，得到的肽具有整体中性电荷。该发明的肽衍生物既具有良好的疗效又具有增强的生物利用度。该发明还提供了使用方法、组合物和相关试剂盒。此外，该发明提供了一种新的设计和/或合成磷酸化肽衍生物的方法，这些衍生物可用作治疗剂。
• PEPTIDE MIMETIC LIGANDS OF POLO-LIKE KINASE 1 POLO BOX DOMAIN AND METHODS OF USE
  申请人：Burke, JR. Terrence R.

  公开号：US20120065146A1

  公开（公告）日：2012-03-15

  Found in various eukaryotic organisms, polo-like kinases (collectively, Plks) are a conserved subfamily of Ser/Thr protein kinases that play critical roles in cell proliferation. Provided herein are compounds that specifically inhibit the activity of Plks, specifically Plk1. Further provided herein are methods for use of the compounds for the treatment of hyperproliferative disorders, particularly cancer. Also provided are uses of the compounds for the preparation of a medicament.

  在各种真核生物中发现的波罗样激酶（Plks）是一类保守的Ser / Thr蛋白激酶亚家族，它们在细胞增殖中发挥关键作用。本文提供了特异性抑制Plks，特别是Plk1活性的化合物。本文还提供了使用这些化合物治疗高增殖性疾病，特别是癌症的方法。此外，还提供了使用这些化合物制备药物的用途。
• Hypoxia Activated Drugs Of Nitrogen Mustard Alkylators
  申请人：Lewis Jason

  公开号：US20110190310A1

  公开（公告）日：2011-08-04

  Hypoxia activated drug compounds having a structure of formula (I) are useful in the treatment of cancer and other hyperproliferative diseases.

  具有公式（I）结构的缺氧激活药物化合物在癌症和其他过度增生性疾病的治疗中是有用的。
• PHOSPHORAMIDATE ALKYLATOR PRODRUGS
  申请人：Matteucci Mark

  公开号：US20100137254A1

  公开（公告）日：2010-06-03

  Phosphoramidate alkylator prodrugs can be used to treat cancer when administered along or in combination with one or more anti-neoplastic agents.

  磷酰胺酰化烷基化剂前药可以在单独或与一个或多个抗肿瘤剂联合使用时用于治疗癌症。