吡替尼定 | 103923-27-9

• 物质功能分类: 原料药 - 抗肿瘤药 - 替尼类抗肿瘤药
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 吡替尼定
• 英文名称: Pirtenidine
• 英文别名: N,1-dioctylpyridin-4-imine
• CAS: 103923-27-9
• 化学式: C₂₁H₃₈N₂
• 分子量: 318.5
• InChiKey: RGTPDNXJDCPXAB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.2
• 重原子数：
  23
• 可旋转键数：
  14
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.76
• 拓扑面积：
  15.6
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] OCTENIDINE BASED COMPOUNDS<br/>[FR] COMPOSÉS À BASE D'OCTÉNIDINE
  申请人：DISHMAN CARBOGEN AMCIS LTD

  公开号：WO2019038669A1

  公开（公告）日：2019-02-28

  The present invention discloses Octenidine based compounds of formula (A) or formula (B) and formula(C) where in, n=1,2,3,4 and R'=un-substituted or substituted aryl or alkyl group; R is hydroxy or hydrogen, X is chlorine, bromine and iodine. The present invention also relates to a process for the preparation thereof.

  本发明披露了基于八亚甲基-4,5-二氮杂-2-丙醇（Octenidine）的化合物，其化学式为（A）或（B）和（C），其中n=1,2,3,4，R'=未取代或取代的芳基或烷基；R为羟基或氢，X为氯、溴和碘。本发明还涉及一种制备该化合物的方法。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Anti-microbial N-(1-(alkyl or arylmethyl)-4(1H)-pyridinylidine)alkanamines and acid addition salts thereof and process for preparation, methods of use and compositions thereof
  申请人：STERLING DRUG INC.

  公开号：EP0174632A1

  公开（公告）日：1986-03-19

  N-[1-(alkyl or arylmethyl)-4(1H)-pyridinylidine]alkanamine and pharmaceutically acceptable acid addition salts thereof, for example, N-(1-octyl-4(1H)-pyridinylidinel-octan- amine monohydrochloride salt, which are useful as antimicrobial agents, especially on living tissues and non-living surfaces and most especially against pathogenic dental microbes, and a process for preparation, methods of use and compositions thereof are disclosed.

  本发明公开了 N-[1-(烷基或芳基甲基)-4(1H)-吡啶基]烷胺及其药学上可接受的酸加成盐，例如 N-(1-辛基-4(1H)-吡啶基)辛胺单盐酸盐，它们可用作抗菌剂，特别是在生物组织和非生物表面上，尤其是针对牙科病原微生物，并公开了其制备工艺、使用方法和组合物。
• 8-ARM POLYETHYLENE GLYCOL DERIVATIVE, MANUFACTURING METHOD AND MODIFIED BIO-RELATED SUBSTANCE THEREBY
  申请人：Xiamen Sinopeg Biotech Co., Ltd.

  公开号：EP3315531A1

  公开（公告）日：2018-05-02

  Disclosed are an 8-arm polyethylene glycol (PEG) derivative (formula 1), manufacturing method and modified bio-related substance thereby, wherein a tetravalent group U and four trivalent groups Ec form a highly symmetric octavalent central structure CORE0 together, Lc connects the octavalent center to eight PEG arms having polydiversity or monodiversity and having n1-n8 as the degrees of polymerization thereof. The terminal of one PEG chain is connected to at least one functional group F (k ≥ 1), and said PEG chain and F can be directly connected (g = 0) or connected with a divalent linking group L0 connected with a terminal branched group G (g = 1) therebetween. The latter provides more reacting sites to combine more pharmaceutical molecules, thereby increasing the drug loading capacity. The near-center symmetric structure of the derivative allows more precise control over the molecular weight during large-scale production, thereby facilitating acquisition of a product having a narrower molecular weight distribution. A bio-related substance modified thereby has a more uniform and controllable performance.

  本发明公开了一种 8 臂聚乙二醇（PEG）衍生物（式 1）、其制造方法和改性生物相关物质，其中一个四价基团 U 和四个三价基团 Ec 共同形成一个高度对称的八价中心结构 CORE0，Lc 将八价中心连接到八个 PEG 臂上，这些 PEG 臂具有多元性或单元性，其聚合度为 n1-n8。一条 PEG 链的末端与至少一个官能团 F（k ≥ 1）相连，所述 PEG 链和 F 可以直接相连（g = 0），也可以通过二价连接基 L0 与中间的末端支化基 G（g = 1）相连。后者提供了更多的反应位点，可以结合更多的药物分子，从而提高药物负载能力。衍生物的近中心对称结构可以在大规模生产过程中更精确地控制分子量，从而有利于获得分子量分布更窄的产品。由此改性的生物相关物质具有更均匀、更可控的性能。
• Eight-arm polyethylene glycol derivative, production method therefor, and modified bio-related substance thereof
  申请人：XIAMEN SINOPEG BIOTECH CO., LTD.

  公开号：US10434182B2

  公开（公告）日：2019-10-08

  Disclosed are an eight-arm polyethylene glycol (PEG) derivative (formula I), production method therefor and modified bio-related substance thereby. Wherein, one tetravalent group U together with four trivalent groups Ec form a highly symmetrical octavalent group CORE0; Lc connects the octavalent group to eight PEG chains having polydispersity or monodispersity and having n1 to n8 as the degree of polymerization thereof; the terminal of one PEG chain is connected to at least one functional group F (k≥1); said PEG chain and F therebetween can be directly connected (g=0) or be indirectly connected via a linking group L0 to a terminal end-branching group G (g=1); the latter provides more reactive sites for binding more drug molecules and increases the drug loading. The eight-arm polyethylene glycol derivative has a centrosymmetric or approximately centrosymmetric structure, and leads to more precise control of the molecular weight in large-scale production and much narrower distribution of molecular weight for products. The modified bio-related substance thereby has a more uniform and controllable performance.

  本发明公开了一种八臂聚乙二醇（PEG）衍生物（式 I）、其生产方法及其改性生物相关物质。其中，一个四价基团 U 与四个三价基团 Ec 形成一个高度对称的八价基团 CORE0；Lc 将八价基团连接到八条具有多分散性或单分散性且聚合度为 n1 至 n8 的 PEG 链上；一条 PEG 链的末端与至少一个官能团 F 连接（k≥1）；所述 PEG 链和 F 之间可以直接连接（g=0），也可以通过连接基团 L0 与末端支化基团 G 间接连接（g=1）；后者提供了更多的反应位点，可以结合更多的药物分子，增加药物负载量。八臂聚乙二醇衍生物具有中心对称或近似中心对称结构，因此在大规模生产中可以更精确地控制分子量，产品的分子量分布也更窄。因此，改性生物相关物质的性能更均匀、更可控。