diethyl ([1,1'-biphenyl]-2-ylmethyl)phosphonate | 127218-04-6

• 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: diethyl ([1,1'-biphenyl]-2-ylmethyl)phosphonate
• 英文别名: 2-Phenyl-benzyl-phosphonsaeure-diaethylester；diethyl (4-biphenylmethyl)phosphonate；Diethyl [([1,1'-biphenyl]-2-yl)methyl]phosphonate；1-(diethoxyphosphorylmethyl)-2-phenylbenzene
• CAS: 127218-04-6
• 化学式: C₁₇H₂₁O₃P
• 分子量: 304.326
• InChiKey: MNRIYVANSCJUHM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  21
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  35.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  diethyl ([1,1'-biphenyl]-2-ylmethyl)phosphonate 在 盐酸 、 五氯化磷 作用下， 生成 2-Phenyl-benzylphosphonsaeure-dianilid
  参考文献：
  名称：

  723. 9,10-二氢-9-羟基-9-磷菲9氧化物，一种新的环状次膦酸

  摘要：

  DOI：

  10.1039/jr9620003729
• 作为产物：
  描述：

  2-联苯基甲醇 在 氯化亚砜 作用下， 生成 diethyl ([1,1'-biphenyl]-2-ylmethyl)phosphonate
  参考文献：
  名称：

  723. 9,10-二氢-9-羟基-9-磷菲9氧化物，一种新的环状次膦酸

  摘要：

  DOI：

  10.1039/jr9620003729

文献信息

• [EN] NITROGENOUS HETEROCYCLIC DERIVATIVES AND THEIR APPLICATION IN DRUGS<br/>[FR] DÉRIVÉS HÉTÉROCYCLIQUES AZOTÉS ET LEUR APPLICATION DANS DES MÉDICAMENTS
  申请人：SUNSHINE LAKE PHARMA CO LTD

  公开号：WO2015090232A1

  公开（公告）日：2015-06-25

  The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, IPF, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.

  本发明涉及医学领域，提供了新颖的含氮杂环化合物，其制备方法以及作为药物的用途，特别是用于治疗和预防组织纤维化。本文还提供了包含这些含氮杂环化合物的药用可接受组合物，以及这些组合物在治疗人类或动物组织纤维化方面的用途，特别是用于人类或动物肾间质纤维化、肾小球硬化、肝纤维化、肺纤维化、IPF、腹膜纤维化、心肌纤维化、皮肤纤维化、术后粘连、良性前列腺增生、骨骼肌纤维化、硬皮病、多发性硬化、胰腺纤维化、肝硬化、肌肉肉瘤、神经纤维瘤、肺间质纤维化、糖尿病肾病、阿尔茨海默病或血管纤维化。
• The development of HEC-866 and its analogues for the treatment of idiopathic pulmonary fibrosis
  作者：Runfeng Lin、Zheng Zhang、Shengtian Cao、Wen Yang、Yinglin Zuo、Xinye Yang、Jiancun Zhang、Juan Xu、Jing Li、Xiaojun Wang

  DOI：10.1039/d1md00023c

  日期：——

  Idiopathic pulmonary fibrosis (IPF) is a chronic progressive lung disease with a typical survival time between three to five years. Two drugs, pirfenidone and nintedanib have been approved for the treatment of IPF, but they have limited efficacy. Thus, the development of new drugs to treat IPF is an urgent medical need. In this paper we report the discovery of a series of orally active pyrimidin-4(3H)-one

  特发性肺纤维化 (IPF) 是一种慢性进行性肺病，典型的生存时间在三到五年之间。两种药物吡非尼酮和尼达尼布已被批准用于治疗 IPF，但疗效有限。因此，开发治疗IPF的新药是迫切的医疗需求。在本文中，我们报告了一系列口服活性 pyrimidin-4(3 H )-one 类似物的发现，这些类似物在体外试验中表现出有效的活性。其中，HEC-866 在大鼠 IPF 模型中显示出良好的疗效。由于 HEC-866 还具有良好的口服生物利用度、较长的半衰期和良好的长期安全性，因此被选中进行进一步的临床评估。
• Heterocyclic compounds
  申请人：Zeneca Limited

  公开号：US05612352A1

  公开（公告）日：1997-03-18

  Biphenylylquinuclidine derivatives of formula I, Q--Ar.sup.1 --Ar.sup.2, in which Q is of formula Ia or Ib, ##STR1## in which R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halogeno and hydroxy; or R.sup.1 and R.sup.2 when taken together define an oxo group; Xb is selected from --CH.sub.2 --, .dbd.CH-- and --CH(OH); Xa is selected from --CH.sub.2 --, .dbd.CH--, CO, --O--, and --S(O)n (wherein n=0, 1 or 2); Ar.sup.1 is a phenylene moiety; Ar.sup.2 is phenyl; and wherein one or both of Ar.sup.1 and Ar.sup.2 is optionally unsubstituted or substituted by one or more substituents independently selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-carbamoyl, N,N-di-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogeno-alkyl, alkanoyl and alkanoylamino; and their pharamaceutically acceptable salts are inhibitors of squalene synthase and hence useful in treating diseases and medical conditions in which a lowering of cholesterol is desirable. The use of these derivatives in medicine is disclosed tohether with novel compounds, processes for their preparation and pharmaceutical composition containing them.

  公式I的二苯基喹啉衍生物，Q--Ar.sup.1 --Ar.sup.2，其中Q为公式Ia或Ib，##STR1##其中R.sup.1和R.sup.2分别独立地选择自氢、烷基、卤代和羟基；或者当R.sup.1和R.sup.2一起定义一个氧代基时；Xb从--CH.sub.2 --、.dbd.CH--和--CH(OH)中选择；Xa从--CH.sub.2 --、.dbd.CH--、CO、--O--和--S(O)n（其中n=0、1或2）中选择；Ar.sup.1是苯基亚甲基；Ar.sup.2是苯基；其中Ar.sup.1和Ar.sup.2中的一个或两个是选择性地未取代或由一个或多个取代基独立地选择性取代，这些取代基来自卤代、羟基、氨基、硝基、氰基、羧基、氨基甲酰基、烷基、烯基、炔基、烷氧基、烷基氨基、二烷基氨基、N-氨基甲酰基、N,N-二烷基氨基甲酰基、烷氧羰基、烷基硫醚、烷基磺醇、烷基磺酰基、卤代烷基、烷酰基和烷酰氨基；它们的药学上可接受的盐是皂化酶的抑制剂，因此在治疗需要降低胆固醇的疾病和医疗状况中有用。在医学上披露了这些衍生物的用途，以及新颖化合物、其制备方法和含有它们的药物组合物。
• Process for Producing Polyester, Polyester Produced Using Said Process, and Polyester Molded Product
  申请人：Kageyama Katsuhiko

  公开号：US20080249280A1

  公开（公告）日：2008-10-09

  This invention provides a polyester and a polyester molded product, which, while maintaining color tone, transparency, and thermal stability, can realize a high polycondensation rate, are less likely to cause the production of polycondensation catalyst-derived undesired materials, and can simultaneously meet both quality and cost effectiveness requirements, which can exhibit the characteristic features, for example, in the fields of ultrafine fibers, high transparent films for optical use, or ultrahigh transparent molded products. These advantages can be realized by using, in the production of a polyester in the presence of an aluminum compound-containing polyester polycondensation catalyst, an aluminum compound having an absorbance of not more than 0.0132 as measured in the form of an aqueous aluminum compound solution, prepared by dissolving the aluminum compound in pure water to give a concentration of 2.7 g/liter in terms of the amount of aluminum element, under conditions of cell length 1 cm and wavelength 680 nm.

  本发明提供了一种聚酯和聚酯成型产品，可以在保持色调、透明度和热稳定性的同时，实现高聚酯化速率，不太可能引起聚酯化催化剂来源的不良材料的生产，并且可以同时满足质量和成本效益的要求，这些优点可以在超细纤维、用于光学的高透明薄膜或超高透明成型产品等领域展现出特征性能。通过在含有铝化合物聚酯聚合催化剂的聚酯生产中使用具有吸光度不超过0.0132的铝化合物，可以实现这些优点。该吸光度是在细胞长度为1厘米，波长为680纳米的条件下，将铝化合物溶解在纯水中以给定铝元素量浓度为2.7克/升形成的水溶性铝化合物溶液中测量得出的。
• PROCESS FOR PRODUCING POLYESTER, POLYESTER PRODUCED USING SAID PROCESS, AND POLYESTER MOLDED PRODUCT
  申请人：Toyo Boseki Kabushiki Kaisha

  公开号：EP1842868A1

  公开（公告）日：2007-10-10

  This invention provides a polyester and a polyester molded product, which, while maintaining color tone, transparency, and thermal stability, can realize a high polycondensation rate, are less likely to cause the production of polycondensation catalyst-derived undesired materials, and can simultaneously meet both quality and cost effectiveness requirements, which can exhibit the characteristic features, for example, in the fields of untrafine fibers, high transparent films for optical use, or ultrahigh transparent molded products. These advantages can be realized by using, in the production of a polyester in the presence of an aluminum compound-containing polyester polycondensation catalyst, an aluminum compound having an absorbance of not more than 0.0132 as measured in the form of an aqueous aluminum compound solution, prepared by dissolving the aluminum compound in pure water to give a concentration of 2.7 g/liter in terms of the amount of aluminum element, under conditions of cell length 1 cm and wavelength 680 nm.

  本发明提供了一种聚酯和聚酯模塑产品，在保持色调、透明度和热稳定性的同时，可实现较高的缩聚速率，不易产生由缩聚催化剂衍生的不良物质，并可同时满足质量和成本效益的要求，例如在非细化纤维、光学用高透明薄膜或超高透明模塑产品等领域可表现出特征特性。要实现这些优点，可以在有含铝化合物的聚酯缩聚催化剂存在的情况下生产聚酯时，使用吸光度不超过 0.0132 的铝化合物，这种铝化合物是以铝化合物水溶液的形式测量的，其制备方法是将铝化合物溶解在纯水中，使其在电池长度为 1 厘米、波长为 680 纳米的条件下，铝元素的用量浓度为 2.7 克/升。