乳酸米力农 | 100286-97-3

• 物质功能分类: 原料药 - 循环系统用药 - 抗充血性心力衰竭药
• 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: 乳酸米力农
• 英文名称: 2-hydroxypropanoate;6-methyl-2-oxo-5-pyridin-4-yl-1H-pyridine-3-carbonitrilium
• CAS: 100286-97-3
• 化学式: C15H15N3O4
• 分子量: 301.3
• InChiKey: VWUPWEAFIOQCGF-UHFFFAOYSA-N

物化性质

• 熔点：
  >120°C (dec.)
• 溶解度：
  可溶于氯仿（轻微、加热）、甲醇（轻微、加热、超声处理）

计算性质

• 辛醇/水分配系数(LogP)：
  1.07
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  123
• 氢给体数：
  3
• 氢受体数：
  6

制备方法与用途

概述

乳酸米力农的活性是氨力农的10～75倍。它主要适用于充血性心力衰竭的短期静脉内给药。新近研究显示，乳酸米力农还可用于心外科体外循环后低心排综合征、解除搭桥血管痉挛、改善心脏原位移植病人心功能及抗炎症反应、改善内脏血流灌注等。

用途

乳酸米力农（Milrinone Lactate）是一种非强心甙、非儿茶酚胺类的新型强心药，由美国Sterling公司开发。它是氨力农(Amrinone)的双毗啶衍生物，属于磷酸二酯酶III(PDE III)抑制剂。乳酸米力农具有正性肌力和外周血管扩张作用。

文献信息

• NOVEL PYRROLOÝ2,3-d¨PYRIMIDINE COMPOUND
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：EP2390254A1

  公开（公告）日：2011-11-30

  Disclosed is a novel pyrrolo[2,3-d]pyrimidine compound represented by formula [I] or a pharmacologically acceptable salt thereof, which has a GPR119 receptor agonistic activity and is useful for a pharmaceutical. In formula [I], E represents a group represented by formula: -NH-, or the like; ring A represents a 6-membered aromatic ring which may contain 1 to 2 nitrogen atoms as heteroatoms (the aromatic ring may be substituted by a halogen atom, a group represented by formula: -CONRaRb, or the like; Ra and Rb are the same or different and independently represent hydrogen, alkyl, hydroxyalkyl, or the like); R1 represents an acyl group or the like; and R2 represents a halogen atom or a cyano group.

  揭示了一种新型吡咯并[2,3-d]嘧啶化合物，其表示为式[I]或其药理学上可接受的盐，具有GPR119受体激动活性，并且对制药有用。在式[I]中，E代表由式表示的基团：-NH-，或类似基团；环A代表可能含有1至2个氮原子作为杂原子的6元芳香环（芳香环可能被卤素原子、由式表示的基团：-CONRaRb，或类似基团取代；Ra和Rb相同或不同且独立地代表氢、烷基、羟基烷基，或类似基团）；R1代表酰基团或类似基团；R2代表卤素原子或氰基。
• [EN] POLYMERIC HYPERBRANCHED CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À DES EXCIPIENTS POLYMÉRIQUES HYPERBRANCHÉS
  申请人：ASCENDIS PHARMA AS

  公开号：WO2013024048A1

  公开（公告）日：2013-02-21

  The present invention relates to water-soluble carrier-linked prodrugs of formula (I),wherein POL is a polymeric moiety,each Hyp is independently a hyperbranched moiety,each moiety SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, m is 0 or 1, each n is independently an integer from 2 to 200 and each x is independently 0 or 1. It further relates to pharmaceutical compositions comprising said water- soluble carrier-linked prodrugs and methods of treatment.

  本发明涉及水溶性载体连接的前药，其化学式为（I），其中POL是聚合物基团，每个Hyp是独立的超支化基团，每个基团SP是独立的间隔基团，每个L是独立的可逆前药连接基团，m为0或1，每个n是独立的整数，范围从2到200，每个x是独立的0或1。此外，还涉及包含所述水溶性载体连接的前药的药物组合物和治疗方法。
• [EN] HIGH-LOADING WATER-SOLUBLE CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À DES EXCIPIENTS HYDROSOLUBLES DE FORTE CHARGE
  申请人：ASCENDIS PHARMA AS

  公开号：WO2013024047A1

  公开（公告）日：2013-02-21

  The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein B, A and Hyp form the carrier, B is a branching core, each A is independently a poly(ethylene glycol)-based polymeric chain, each Hyp is independently a branched moiety, each SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, each D is independendly a biologically active moiety, each x is independently 0 or 1, each m is independently an integer of from 2 to 64, n is an integer from 3 to 32; or the pharmaceutically acceptable salt thereof. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs, their use asmedicament or diagnostic, and methods of treatment.

  本发明涉及水溶性载体连接的前药，其化学式为(I)，其中B、A和Hyp形成载体，B是一个分支核心，每个A独立地是一条聚乙二醇基聚合链，每个Hyp独立地是一个分支基团，每个SP独立地是一个间隔基团，每个L独立地是一个可逆前药连接基团，每个D独立地是一个生物活性基团，每个x独立地为0或1，每个m独立地是从2到64的整数，n是从3到32的整数；或其药学上可接受的盐。进一步涉及包括所述水溶性载体连接的前药的药物组合物，其用作药物或诊断，以及治疗方法。
• Particles with improved solubilization capacity
  申请人：——

  公开号：US20030022242A1

  公开（公告）日：2003-01-30

  A particle is disclosed that comprises a first volume of hydrophobe-rich material with tunable dissolution and solubilization characteristics and a distinct second volume of nanostructured nonlamellar liquid crystalline material, said second volume containing said first domain and being capable of being in equilibrium with said first volume. Preferably, the nanostructured nonlamellar liquid crystalline material is capable of being in equilibrium with a polar solvent or a water-immiscible solvent or both.

  揭示了一种颗粒，包括具有可调溶解和溶解特性的第一体积的疏水基质材料和独特的第二体积的纳米结构非层状液晶材料，所述第二体积包含所述第一领域，并能够与所述第一体积处于平衡状态。优选，所述纳米结构非层状液晶材料能够与极性溶剂或水不相溶溶剂或两者同时处于平衡状态。
• [EN] RELEASABLE CONJUGATES<br/>[FR] CONJUGUÉS LIBÉRABLES
  申请人：QUIAPEG PHARMACEUTICALS AB

  公开号：WO2018163131A1

  公开（公告）日：2018-09-13

  The present application provides compounds of Formula (B), or pharmaceutically acceptable salts thereof, wherein D is a residue of a biologically active drug, which underdo hydrolysis under physiological conditions to release the biologically active drug and which are useful in the treatment of disorders that could be beneficially treated with the drug.

  本申请提供了化合物的公式（B），或其药用盐，其中D是生物活性药物的残留物，在生理条件下经过水解释放出生物活性药物，并且对可能受益于该药物治疗的疾病具有用处。