N-亚硝基脲 | 13010-20-3

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机碳酸及其衍生物
• 中文名称: N-亚硝基脲
• 英文名称: nitrosourea
• 英文别名: N-nitrosourea
• CAS: 13010-20-3
• 化学式: CH₃N₃O₂
• 分子量: 89.0537
• InChiKey: OSTGTTZJOCZWJG-UHFFFAOYSA-N

物化性质

• 熔点：
  111-111.3 °C (decomp)
• 沸点：
  165.09°C (rough estimate)
• 密度：
  1.82±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.8
• 重原子数：
  6
• 可旋转键数：
  0
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  84.6
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-亚硝基脲 在 氢氧化钾 作用下， 以 乙醚 、 水 为溶剂， 反应 1.0h， 生成 重氮甲烷
  参考文献：
  名称：

  HETEROCYCLIC ANTIVIRAL COMPOUNDS

  摘要：

  式I化合物，其中R1、R2、R3、X1、X2和Ar如本文所定义，或其药学上可接受的盐，抑制HIV-1逆转录酶，并提供预防和治疗HIV-1感染以及治疗艾滋病和/或艾滋病相关复合征（ARC）的方法。本发明还涉及含有式I化合物的组合物，这些组合物对于预防和治疗HIV-1感染以及治疗艾滋病和/或ARC是有用的。

  公开号：

  US20090170856A1

文献信息

• Non-nucleoside reverse transcriptase inhibitors
  申请人：Kennedy-Smith Joshua

  公开号：US20080045511A1

  公开（公告）日：2008-02-21

  The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R 1 , R 2 , R 3 , R 4a , R 4b , R 5 , R 6 , Ar, X 1 , X 2 , X 4 , X 4 and X 5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.

  本发明提供了用于治疗HIV感染、预防HIV感染、治疗艾滋病或AIDS相关复合征（ARC）的有用化合物。本发明的化合物具有式I的结构，其中A为A1、A2、A3或A4，且R1、R2、R3、R4a、R4b、R5、R6、Ar、X1、X2、X4、X4和X5如本文所定义。本发明还公开了使用本文定义的化合物治疗HIV感染的方法以及含有这些化合物的药物组合物。
• Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes
  作者：Chutian Shu、Hu Ge、Michael Song、Jyun-hong Chen、Huimin Zhou、Qu Qi、Feng Wang、Xifeng Ma、Xiaolei Yang、Genyan Zhang、Yanwei Ding、Dapeng Zhou、Peng Peng、Cheng-kon Shih、Jun Xu、Frank Wu

  DOI：10.1021/ml5001905

  日期：2014.8.14

  We report our discovery of a novel series of potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. Starting from a lead identified by scaffold-hopping approach, our discovery and development efforts were focused on exploring structure-activity relationships, optimizing pharmacokinetic profile, improving in vitro and in vivo efficacy, and evaluating safety profile. The selected candidate

  我们报告了我们发现的一系列新型的有效和选择性二肽基肽酶IV（DPP-4）抑制剂。从通过脚手架跳跃方法确定的线索开始，我们的发现和开发工作集中在探索结构与活性之间的关系，优化药代动力学特征，改善体外和体内功效以及评估安全性特征。选定的候选人伊米列汀目前正在接受临床试验。
• Sulfonic acid ester derivatives useful as antilipemic agents
  申请人：Taiho Pharmaceutical Company, Limited

  公开号：US04675428A1

  公开（公告）日：1987-06-23

  A sulfonic acid ester derivative represented by the general formula ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms, A is a group represented by the general formula ##STR2## (wherein R.sub.2 and R.sub.3 are each alkyl having 1 to 4 carbon atoms) or by the general formula ##STR3## (wherein R.sub.4 and R.sub.5 are each alkyl having 1 to 4 carbon atoms or, when taken together with the cabon atom to which they are attached, form cycloalkyl having 4 to 6 carbon atoms), and l is an integer of from 1 to 3, and a process for preparing the derivative.

  一种磺酸酯衍生物，其通式表示为 ##STR1## 其中R.sub.1为氢原子，具有1至4个碳原子的烷基或1至4个碳原子的烷氧基，A是由通式##STR2##（其中R.sub.2和R.sub.3均为具有1至4个碳原子的烷基）或由通式##STR3##（其中R.sub.4和R.sub.5均为具有1至4个碳原子的烷基或与它们所连接的碳原子一起形成具有4至6个碳原子的环烷基），l为1至3的整数，以及制备该衍生物的方法。
• Sulfonic acid ester derivatives and process for preparing same
  申请人：Taiho Pharmaceutical Company Limited

  公开号：US04797502A1

  公开（公告）日：1989-01-10

  A sulfonic acid ester derivative represented by the general formula ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms, A is a group represented by the general formula ##STR2## (wherein R.sub.2 and R.sub.3 are each alkyl having 1 to 4 carbon atoms) or by the general formula ##STR3## (wherein R.sub.4 and R.sub.5 are each alkyl having 1 to 4 carbon atoms or, when taken together with the carbon atom to which they are attached, form cycloalkyl having 4 to 6 carbon atoms), and l is an integer of from 1 to 3, and a process for preparing the derivative.

  一种磺酸酯衍生物，其通式表示为##STR1##其中R.sub.1是氢原子，具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基，A是由通式##STR2## (其中R.sub.2和R.sub.3均为具有1至4个碳原子的烷基)或由通式##STR3## (其中R.sub.4和R.sub.5均为具有1至4个碳原子的烷基或与它们附着的碳原子一起形成具有4至6个碳原子的环烷基)表示的基团，l为1至3的整数，并提供了制备该衍生物的方法。
• Silver halide photographic light-sensitive element
  申请人：Fuji Photo Film Co., Ltd.

  公开号：US04334010A1

  公开（公告）日：1982-06-08

  A silver halide photographic light-sensitive element is described comprising a support having thereon at least one silver halide emulsion layer, wherein at least one compound represented by formula (I) is incorporated in the silver halide emulsion layer or in another hydrophilic colloid layer: ##STR1## wherein X represents a hydroxy group or a group represented by ##STR2## wherein R.sup.2 and R.sup.3 (which may be the same or different) each reprsents hydrogen, an alkyl group, or an aryl group; R.sup.1 represents a sulfur-containing saturated heterocyclic group or a group represented by -A-S-B, wherein A represents an alkylene group and B represents hydrogen, an alkyl group, or an aryl group; and Z represents an atomic group forming a 5-membered or 6-membered unsubstituted or substituted carbocyclic ring. In the silver halide photographic light-sensitive element, the so-called "latent image fading" phenomenon is prevented without accompanying degradation of other photograhic properties.

  本文描述了一种含有至少一层银卤素乳剂层的支撑体的银卤素摄影感光元件，其中在银卤素乳剂层或其他亲水性胶体层中包含至少一种由式(I)表示的化合物：##STR1## 其中X表示羟基或由##STR2##表示的基团，其中R.sup.2和R.sup.3（可以相同也可以不同）分别表示氢、烷基或芳基；R.sup.1表示含硫饱和杂环基或由-A-S-B表示的基团，其中A表示烷基，B表示氢、烷基或芳基；Z表示形成5元环或6元环未取代或取代的碳环的原子基团。在银卤素摄影感光元件中，可以防止所谓的“潜影褪色”现象，而不伴随其他摄影性质的降解。