(1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-Dihydroxy-12-[(E)-1-[(3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone;hydrate

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 大环内酯内酰胺
• 英文名称: (1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-Dihydroxy-12-[(E)-1-[(3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone;hydrate
• 化学式: C44H71NO13
• 分子量: 822.0
• InChiKey: NWJQLQGQZSIBAF-HZXKVGIDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.81
• 重原子数：
  58
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.77
• 拓扑面积：
  179
• 氢给体数：
  4
• 氢受体数：
  13

文献信息

• Separation And Manipulation Of A Chiral Object
  申请人：Kibar Osman

  公开号：US20080262240A1

  公开（公告）日：2008-10-23

  Among other things, to cause directional motion of chiral objects in a mixture in a chamber, a field is rotated relative, to a chamber to cause rotation of the chiral objects. The rotation of the objects causes them to move directionally based on their chirality.

  在混合物室中，为了使手性物体产生定向运动，需要旋转一个场，相对于室内旋转手性物体。物体的旋转会根据它们的手性定向移动。
• ARYLTHIOACETAMIDE CARBOXYLATE DERIVATIVES AS FKBP INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL DISEASES
  申请人：Pellecchia Maurizio

  公开号：US20080293721A1

  公开（公告）日：2008-11-27

  The present invention provides compounds having the general structure I, or a pharmaceutically acceptable salt thereof: wherein Z is selected from a group consisting of O, C, N, and S; each of Ar 1 , Ar 2 , and Ar 3 is a moiety selected from a group consisting of an aryl and a substituted aryl; Y is selected from a group consisting of S, O, CH 2 and SO 2 ; K is selected from a group consisting CH 2 , CF 2 , O, NH, and SO 2 ; each of n 1 and n 2 is an integer selected from a group consisting of 0, 1, 2, 3, and 4; and each of x, y, m 1 and m 2 is an integer selected from a group consisting of 0 and 1. Pharmaceutical compositions based on compounds I are also provided for treatment of a neurological disorders, diseases, or pathologies, and for treatment of infectious diseases.

  本发明提供具有一般结构I或其药学上可接受的盐的化合物：其中Z从O、C、N和S的群中选择；Ar1、Ar2和Ar3中的每一个是从芳基和取代芳基的群中选择的基团；Y从S、O、CH2和SO2的群中选择；K从 、CF2、O、NH和SO2的群中选择；n1和n2中的每一个是从0、1、2、3和4的群中选择的整数；x、y、m1和m2中的每一个是从0和1的群中选择的整数。还提供基于化合物I的药物组合物，用于治疗神经系统疾病、疾病或病理以及感染性疾病的治疗。
• INDWELLING STENT
  申请人：KANEKA CORPORATION

  公开号：EP1586346A1

  公开（公告）日：2005-10-19

  As a therapy for angiostenosis, angioplasty (PTA, PTCA), in which a small balloon is inflated in a blood vessel to expand the vessel, has been widely practiced as a minimally invasive treatment. In this therapy, however, repeated stenosis (restenosis) occurs at a high incidence. In order to reduce the restenosis rate, procedures that use indwelling stents have gained popularity in recent years. However, restenosis has been reported in about 20% to 30% of stent placement cases. Although attempts have been made to coat the stent with a drug that regulates occlusion, stenosis still occurs at a high frequency. At least two layers including an immunosuppressant-containing layer and an antiinflammatory agent-containing layer are provided on the surface of an indwelling stent.

  血管成形术（PTA，PTCA）是一种治疗血管狭窄的微创疗法，通过在血管中充入一个小球囊来扩张血管。然而，在这种疗法中，反复狭窄（再狭窄）的发生率很高。为了降低再狭窄率，近年来使用留置支架的手术越来越受欢迎。 然而，据报道，约 20% 至 30% 的支架置入病例会发生再狭窄。尽管已尝试在支架上涂抹调节闭塞的药物，但支架狭窄的发生率仍然很高。 留置支架表面至少有两层，包括含免疫抑制剂层和含抗炎剂层。
• STENT
  申请人：KANEKA CORPORATION

  公开号：EP1611920A1

  公开（公告）日：2006-01-04

  A stent that can further reduce the incidence of repeated stenosis (restenosis) that has been experienced in conventional stents is provided. Onto the outer surface of a stent body, a structure for cutting body tissues and the like is disposed so that during stent expansion in the outward radial direction and placement, the body tissues, such as blood vessels, are cut. Thus, the stress and unrestricted damage applied to body tissues such as blood vessels can be reduced, and restenosis can be suppressed. By coating the stent with a drug, a stent having enhanced effects can be provided.

  本发明提供了一种可进一步降低传统支架反复狭窄（再狭窄）发生率的支架。在支架体的外表面，设置了用于切割人体组织等的结构，以便在支架向外径向扩张和放置时，切割人体组织（如血管）。因此，可以减少对血管等人体组织施加的应力和无限制的损伤，抑制再狭窄。通过在支架上涂敷药物，可以提供效果更佳的支架。
• STENT TO BE PLACED IN VIVO
  申请人：KANEKA CORPORATION

  公开号：EP1652550A1

  公开（公告）日：2006-05-03

  As a treatment for angiostenosis, angioplasty (PTA or PTCA) of expanding a small-sized balloon in a vessel has been commonly conducted. However, this treatment easily causes repeated stenosis (restenosis) after the treatment. Placement of a stent in a vessel is also effective in decreasing restenosis, but this treatment may also cause restenosis. The present invention provides a stent containing a poly (lactide-co-glycolide) or both a poly (lactide-co-glycolide) and an immunosuppressive agent in at least a portion of a surface of the stent, and further containing a material nondegradable in vivo.

  作为治疗血管狭窄的一种方法，血管成形术（PTA 或 PTCA）通常是在血管内扩张一个小尺寸的球囊。然而，这种治疗方法很容易在治疗后导致血管反复狭窄（再狭窄）。在血管中放置支架也能有效减少再狭窄，但这种治疗方法也可能导致再狭窄。本发明提供了一种支架，在支架表面的至少一部分含有聚（乳酸-共聚乙二醇）或聚（乳酸-共聚乙二醇）和免疫抑制剂，并进一步含有一种在体内不可降解的材料。