(2S,5R,6R)-6-[[3-(2-chlorophenyl)-5-methyl-1,2-oxazole-4-carbonyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid;(2S,5R,6R)-6-[[3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazole-4-carbonyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: (2S,5R,6R)-6-[[3-(2-chlorophenyl)-5-methyl-1,2-oxazole-4-carbonyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid;(2S,5R,6R)-6-[[3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazole-4-carbonyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
• 化学式: C38H35Cl3N6O10S2
• 分子量: 906.2
• InChiKey: APKJMUSDFLXNCE-BGCGJMPHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.75
• 重原子数：
  59
• 可旋转键数：
  8
• 环数：
  8.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  276
• 氢给体数：
  4
• 氢受体数：
  14

文献信息

• Cholestosome vesicles for incorporation of molecules into chylomicrons
  申请人：TheraSyn Sensors, Inc.

  公开号：US10369114B2

  公开（公告）日：2019-08-06

  The present invention is directed to a cargo-loaded cholesteryl ester nanoparticle with a hollow compartment (“cholestosome”) consisting essentially of at least one non-ionic cholesteryl ester and one or more encapsulated active molecules which cannot appreciably pass through an enterocyte membrane in the absence of said molecule being loaded into said cholestosome, the cholestosome having a neutral surface and having the ability to pass into enterocytes in the manner of orally absorbed nutrient lipids using cell pathways to reach the golgi apparatus. Pursuant to the present invention, the novel cargo loaded cholestosomes according to the present invention are capable of depositing active molecules within cells of a patient or subject and effecting therapy or diagnosis of the patient or subject.

  本发明涉及一种装载货物的胆固醇酯纳米粒子，该粒子具有中空隔室（"胆固醇体"），主要由至少一种非离子胆固醇酯和一种或多种封装的活性分子组成，在没有将所述分子装载到所述胆固醇体中的情况下，活性分子不能明显地通过肠细胞膜、胆甾体具有中性表面，能够像口服吸收的营养脂质一样通过细胞通路进入肠细胞，到达高尔基体。根据本发明，本发明的新型载货胆甾体能够将活性分子沉积在患者或受试者的细胞内，并对患者或受试者进行治疗或诊断。
• Medicament for treatment of diabetic foot infections
  申请人：Debiopharm International S.A.

  公开号：US10751351B2

  公开（公告）日：2020-08-25

  The present invention provides means and methods for treating diabetic foot infections. In particular, drug compounds are provided that combine a high therapeutic activity against Staphylococcus Spp. bacteria with a high degree of bone penetration and vasodilatory effects. This unique combination of properties allows to accomplish high local concentrations of the drug at the site of infection even in diabetic foot patients typically having poor blood perfusion at the site of infection.

  本发明提供了治疗糖尿病足感染的手段和方法。特别是，本发明提供的药物化合物结合了对葡萄球菌属细菌的高治疗活性、高骨穿透性和血管扩张作用。这种独特的特性组合可以使药物在感染部位达到较高的局部浓度，即使是感染部位血液灌流较差的糖尿病足患者也不例外。
• Expanded pore particles and delivery methods thereof
  申请人：National Technology & Engineering Solutions of Sandia, LLC

  公开号：US10933027B1

  公开（公告）日：2021-03-02

  The present invention relates to a construct including a porous core, a cargo, and a spacer disposed between the core and the cargo. In some examples, the construct further includes an outer layer composed of a lipid, a polymer, or a combination thereof. Methods of making and employing such constructs are also described herein.

  本发明涉及一种构造物，包括多孔内核、货物以及设置在内核和货物之间的间隔物。在某些实例中，该结构体还包括由脂质、聚合物或其组合构成的外层。本文还描述了制造和使用这种构造物的方法。
• Envenomation therapies and related pharmaceutical compositions, systems and kits
  申请人：OPHIREX, INC

  公开号：US11000506B2

  公开（公告）日：2021-05-11

  The invention provides methods of treatment, pharmaceutical compositions, systems and kits appropriate for first line and/or adjunct therapy with antivenom using at least one active component, in some instances at least two active components and in other instances no more than two active components selected from the group consisting of a selective secretory PLA2 inhibitor (sPLA2 or PLA2 inhibitor), a metalloproteinase inhibitor, a serine protease inhibitor, antivenom, one or more acetylcholinesterase inhibitors or a nAChR agonist paired with a mAChR antagonist, a NMDA receptor antagonist and a spreading factor inhibitor to treat a subject who suffers from an envenomation, preferably at the time of envenomation and often within a period of less than about an hour after an envenomation or 6 hours after an envenomation and throughout the course of treatment at time with or without antivenom as an adjunct therapy after an envenomation by, for example, a snake or invertebrate.

  本发明提供了适用于一线和/或辅助治疗的抗蛇毒血清的治疗方法、药物组合物、系统和试剂盒，这些药物组合物、系统和试剂盒使用至少一种活性成分，在某些情况下至少两种活性成分，在其他情况下不超过两种活性成分，这些活性成分选自选择性分泌型PLA2抑制剂（sPLA2或PLA2抑制剂）、金属蛋白酶抑制剂、丝氨酸蛋白酶抑制剂、抗蛇毒血清、一种或多种乙酰胆碱酯酶抑制剂或与mAChR拮抗剂配对的nAChR激动剂、NMDA受体拮抗剂和扩散因子抑制剂组成的组、一种或多种乙酰胆碱酯酶抑制剂或 nAChR 激动剂与 mAChR 拮抗剂、NMDA 受体拮抗剂和扩散因子抑制剂配伍，用于治疗被毒蛇咬伤的患者、优选在被毒蛇或无脊椎动物等毒害后，在毒害发生时，通常在毒害发生后不到一小时或6小时的时间内，以及在整个治疗过程中，随时使用或不使用抗蛇毒血清作为辅助治疗。
• Active targeting of cells by monosized protocells
  申请人：Brinker Charles Jeffrey

  公开号：US11344629B2

  公开（公告）日：2022-05-31

  In one aspect, the disclosure provides mesoporous silica nanoparticles (MSNPs), monodisperse populations of MSNPs and related protocells which exhibit cell binding specificity. For example, MSNPs and protocells of the disclosure may be used to target specific delivery of therapeutic agents to CD19 or EGFR expressing cancer cells, or target specific delivery of therapeutic agents to other cell types. Related protocells, pharmaceutical compositions and therapeutic and diagnostic methods are also provided.

  在一个方面，本公开提供了介孔二氧化硅纳米颗粒（MSNPs）、MSNPs的单分散群和相关的原细胞，它们表现出细胞结合特异性。例如，本公开的 MSNPs 和原细胞可用于向表达 CD19 或表皮生长因子受体的癌细胞靶向特异性递送治疗剂，或向其他细胞类型靶向特异性递送治疗剂。还提供了相关的原细胞、药物组合物以及治疗和诊断方法。