2(R), 4(R)-dihydroxypyrrolidine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 2(R), 4(R)-dihydroxypyrrolidine
• 英文别名: 2,5-bis(hydroxymethyl)pyrrolidine-3,4-diol
• 化学式: C₆H₁₃NO₄
• 分子量: 163.17
• InChiKey: PFYHYHZGDNWFIF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.8
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  93
• 氢给体数：
  5
• 氢受体数：
  5

文献信息

• [EN] METHODS OF USE FOR OPSIN BINDING LIGANDS<br/>[FR] PROCÉDÉS D'UTILISATION DE LIGANDS DE LIAISON DE L'OPSINE
  申请人：BIKAM PHARMACEUTICALS INC

  公开号：WO2010074746A1

  公开（公告）日：2010-07-01

  Methods of use of compounds of the Formula I1 II, III, IV and/or V are disclosed for treating ophthalmic conditions related to the production of toxic visual cycle products that accumulate in the eye, and are associated with reactions of the visual cycle during medical procedures that expose the eye to light, most commonly the various forms of ophthalmic surgery and stabilize the proper folding of mutant opsins. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described, along with methods of screening for new agents useful in said treatments.

  公开了利用公式I1 II、III、IV和/或V的化合物治疗与在眼睛中积聚的有毒视觉循环产物有关的眼科疾病的方法，这些产物与暴露于光线的医疗程序期间的视觉循环反应有关，最常见的是各种形式的眼科手术，并稳定突变视蛋白的正确折叠。还描述了在这些方法中有用的化合物和组合物，无论是单独使用还是与其他治疗剂结合使用，以及筛选用于上述治疗的新药物的方法。
• [EN] SYNTHESIS OF LACTONE DERIVATIVES AND THEIR USE IN THE MODIFICATION OF PROTEINS<br/>[FR] SYNTHÈSE DE DÉRIVÉS DE LACTONE ET LEUR UTILISATION DANS LA MODIFICATION DE PROTÉINES
  申请人：GENIE BIOTECH UK LTD

  公开号：WO2021123229A1

  公开（公告）日：2021-06-24

  Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.

  蛋白质的位点特异性修饰在生物技术应用中是可取的，例如生物制药、免疫疗法、疫苗，并且在化学生物学中也非常有用。葡萄糖酸化是一种非酶促的共价后翻译修饰，常见于带有N-末端His-标签的蛋白质上。我们合成了葡萄糖酸-1,5-内酯衍生物，包括用于选择性酰化的叠氮化衍生物。只需将衍生物与目标蛋白质混合在不同的温度、水溶液缓冲剂、辅料或复杂的细胞裂解液条件下，即可实现高产酰化。
• IMMUNOMODULATORY ALKALOIDS
  申请人：Nash Robert James

  公开号：US20090117083A1

  公开（公告）日：2009-05-07

  Immunotherapy comprises administration of an alkaloid at a dose sufficient to induce IL-2 production in dendritic cells in a patient. The alkaloid induces the production of IL-2 in dendritic cells. The alkaloids need not be naturally occurring, and may be synthetic analogues or derivatives of naturally occurring counterparts. Such analogues or derivatives are preferably pharmaceutically acceptable analogues, salts, isomers or derivatives as herein defined. However, preferred alkaloids are phytochemicals. Such phytochemicals may be isolated from natural sources or synthesised in vitro. Particularly preferred are alkaloids is selected from piperidine alkaloids; pyrrolin alkaloids; pyrrolidine alkaloids; pyrolizidine alkaloids: indolizidine alkaloids and nortropane alkaloids.

  免疫疗法包括在患者体内以足够剂量给予一种生物碱，以诱导树突状细胞产生IL-2。这种生物碱会引起树突状细胞产生IL-2。这些生物碱不一定是天然存在的，也可以是天然存在的衍生物或合成类似物。这些类似物或衍生物最好是药学上可接受的类似物、盐、异构体或衍生物，如本文所定义。然而，最好的生物碱是植物化学物质。这些植物化学物质可以从天然来源中分离出来，也可以在体外合成。特别优选的生物碱包括吡啶生物碱、吡咯烷生物碱、吡咯烷生物碱、吡咯菊烷生物碱、吲哚菊烷生物碱和诺滕烷生物碱。
• Opsin-Binding Ligands, Compositions and Methods of Use
  申请人：Bikam Pharmaceuticals, Inc.

  公开号：US20150038574A1

  公开（公告）日：2015-02-05

  Compounds and compositions are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.

  本文披露了一些化合物和组合物，用于治疗由于或与眼睛中毒性视觉循环产物积累有关的眼科疾病，如干性成人黄斑变性，以及由突变视蛋白的错误折叠和/或视蛋白的错误定位引起或有关的疾病。描述了这些化合物单独或与其他治疗剂组合的组合物，以及使用这些化合物和/或组合物的治疗方法。还披露了合成这些药剂的方法。
• Opsin-binding ligands, compositions and methods of use
  申请人：Garvey David S.

  公开号：US20110003784A1

  公开（公告）日：2011-01-06

  Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.

  本文披露了用于治疗与视蛋白蛋白质错位、突变视蛋白蛋白质的错折和在眼中积累有毒视觉循环产物相关的眼科疾病的化合物和该化合物的组合物以及使用该化合物的方法。本文还描述了用于这些方法的化合物和组合物，可以单独使用或与其他治疗药物联合使用。