2-amino-2-oxoethyl 3,5-bis(acetylamino)-2,4,6-triiodobenzoate | 153850-06-7

• 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: 2-amino-2-oxoethyl 3,5-bis(acetylamino)-2,4,6-triiodobenzoate
• 英文别名: 2-Amino-2-oxoethyl 3,5-diacetamido-2,4,6-triiodobenzoate；(2-amino-2-oxoethyl) 3,5-diacetamido-2,4,6-triiodobenzoate
• CAS: 153850-06-7
• 化学式: C₁₃H₁₂I₃N₃O₅
• 分子量: 670.969
• InChiKey: OTAOZPQJJOPPTI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  24
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  128
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• Composition of and method for preparing stable particles in a frozen aqueous matrix
  申请人：——

  公开号：US20030077329A1

  公开（公告）日：2003-04-24

  The present invention discloses a composition of a stable suspension of a poorly water soluble pharmaceutical agent or cosmetic in the form of particles of the pharmaceutical agent or cosmetic suspended in a frozen aqueous matrix and method for its preparation. The composition is stable for a prolonged period of time, preferably six months or longer and is suitable for parenteral, oral, or non-oral routes such as pulmonary (inhalation), ophthalmic, or topical administration.

  本发明揭示了一种稳定的悬浮液组合物，其包含一种难溶于水的药物或化妆品，以药物或化妆品的颗粒形式悬浮于冻结水基体中，并揭示了其制备方法。该组合物稳定性长时间，优选为六个月或更长时间，适用于静脉、口服或非口服途径，例如肺部（吸入）、眼科或局部给药。
• COMPOSITION OF AND METHOD FOR PREPARING STABLE PARTICLES IN A FROZEN AQUEOUS MATRIX
  申请人：Kipp E. James

  公开号：US20060222710A1

  公开（公告）日：2006-10-05

  The present invention discloses a composition of a stable suspension of a poorly water soluble pharmaceutical agent or cosmetic in the form of particles of the pharmaceutical agent or cosmetic suspended in a frozen aqueous matrix and method for its preparation. The composition is stable for a prolonged period of time, preferably six months or longer and is suitable for parenteral, oral, or non-oral routes such as pulmonary (inhalation), ophthalmic, or topical administration.

  本发明揭示了一种稳定的悬浮液组合物，该组合物以制药剂或化妆品的颗粒形式悬浮于冻结的水基基质中，并提供了其制备方法。该组合物稳定性能长时间保持，最好为六个月或更长时间，并适用于肠道内、口服或非口服途径，如肺部（吸入）、眼科或局部给药。
• (Polyalkoxy)sulfonate surface modifiers
  申请人：Kipp E. James

  公开号：US20060141048A1

  公开（公告）日：2006-06-29

  The present invention is directed to novel compounds, methods of manufacture and methods of use. The present invention is also directed to solid drug/active agent particles having one or more of the compounds of the present invention associated with the surface thereof. The compounds of the present invention are comprised of a non-polar polyether covalently linked to an anionic sulfonate group. The compounds have an amphipathic quality and preferably, are surface active. Such compounds are preferably useful as surface-active agents to coat and stabilize dispersions of particles in a continuous liquid medium. These surface-active agents may be applied in the stabilization of suspensions, emulsions, or liposome formulations intended for pharmaceutical, medical, cosmetic, or agricultural use. The particles that can be prepared by a variety of methods and will preferably comprise a pharmaceutical agent. Pharmaceutical compositions of the present invention can be used to treat a myriad of conditions and can be administered by many routes, including intravenous, intramuscular, subcutaneous, intrathecal, subdural, intracameral, intracerebral, intralesional, topical, oral, buccal, rectal, transcutaneous, pulmonary, and nasal.

  本发明涉及新型化合物、制造方法和使用方法。本发明还涉及具有本发明化合物中的一个或多个与其表面相关联的固体药物/活性剂颗粒。本发明化合物由非极性聚醚共价连接到阴离子磺酸基团上。该化合物具有两性性质，最好是表面活性。这样的化合物最好用作表面活性剂，用于包覆和稳定分散在连续液体介质中的颗粒。这些表面活性剂可用于稳定制药、医疗、化妆品或农业用途的悬浮液、乳液或脂质体制剂。可通过各种方法制备颗粒，颗粒最好包含一种药物。本发明的制药组合物可用于治疗多种疾病，并可通过许多途径给药，包括静脉、肌肉注射、皮下注射、蛛网膜下腔、硬膜外、眼前房、颅内、病变部位内、局部、口服、颊粘膜、直肠、经皮、肺和鼻腔。
• Iodinated aroyloxy carboxamides and contrast agents containing them
  申请人：NanoSystems L.L.C.

  公开号：EP0601616A1

  公开（公告）日：1994-06-15

  Compounds having the structure    wherein (Z)̵COO is the residue of an iodinated aromatic acid;    n is an integer from 0 to 20;    R¹ and R² are independently H, alkyl, fluoro-alkyl, cycloalkyl, aryl, aralkyl, alkoxy or aryloxy;    R³ and R⁴ are independently a substituent as defined for R¹ and R² above, halogen, hydroxy or an acylamino;    and R⁵ and R⁶ are independently H, alkyl, cycloalkyl, aryl, aralkyl, alkoxy, alkoxyalkyl, or acetamidoalkyl;    or R⁵ and R⁶, taken together with the nitrogen atom to which they are attached, represent a 4 to 7-membered nitrogen containing ring,    are useful as contrast agents in x-ray imaging compositions and methods for x-ray diagnostic imaging.

  具有以下结构的化合物 其中(Z)̵COO 是碘化芳香酸的残留物； n 是 0 至 20 的整数； R¹ 和 R² 独立地为 H、烷基、氟代烷基、环烷基、芳基、芳烷基、烷氧基或芳氧基； R³ 和 R⁴ 独立地为上文 R¹ 和 R² 所定义的取代基、卤素、羟基或酰氨基； 和 R⁵ 和 R⁶ 独立地为 H、烷基、环烷基、芳基、芳烷基、烷氧基、烷氧基烷基或乙酰胺基烷基； 或 R⁵ 和 R⁶ 与它们所连接的氮原子一起代表 4 至 7 元含氮环、 可用作 X 射线成像组合物和 X 射线诊断成像方法中的造影剂。
• Reduction of intravenously administered nanoparticulate-formulation-induced adverse physiological reactions
  申请人：Elan Pharma International Limited

  公开号：EP2275094A2

  公开（公告）日：2011-01-19

  Disclosed are methods of intravenous administration of nanoparticulate drug formulations to a mammal to avoid adverse hemodynamic effects: by reducing the rate and concentration of the nanoparticles in the formulations; or by pretreating the subject with histamine; or by pretreating the subject with a desensitizing amount of the nanoparticulate drug formulations.

  公开了向哺乳动物静脉注射纳米颗粒药物制剂以避免不良血液动力学效应的方法：通过降低制剂中纳米颗粒的速率和浓度；或通过用组胺预处理受试者；或通过用脱敏量的纳米颗粒药物制剂预处理受试者。