奎诺二甲基丙烯酯

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机磺酸及其衍生物
• 中文名称: 奎诺二甲基丙烯酯
• 中文别名: 3-[(1,1-二甲基-2-羟乙基氨基]-2-羟基丙磺酸；3-[(1,1-二甲基-2-羟乙基)氨基]-2-羟基-1-丙磺酸
• 英文名称: 2-hydroxy-3-[(1-hydroxy-2-methylpropan-2-yl)azaniumyl]propane-1-sulfonate
• 化学式: C7H17NO5S
• mdl: MFCD00041777
• 分子量: 227.28
• InChiKey: ACERFIHBIWMFOR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -4.3
• 重原子数：
  14
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  115
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• [EN] HINDERED DISULFIDE DRUG CONJUGATES<br/>[FR] CONJUGUÉS MÉDICAMENTEUX À PONT DISULFURE ENCOMBRÉ
  申请人：GENENTECH INC

  公开号：WO2017064675A1

  公开（公告）日：2017-04-20

  The invention relates generally to disulfide drug conjugates wherein a linker comprising a sulfur-bearing carbon atom substituted with at least one hydrocarbyl or substituted hydrocarbyl is conjugated by a disulfide bond to a cysteine sulfur atom of a targeting carrier, and wherein the linker is further conjugated to a drug moiety. The invention further relates to activated linker-drug conjugates suitable for conjugation to a targeting carrier by a disulfide bond. The invention further relates to methods for preparing hindered disulfide drug conjugates.

  该发明一般涉及二硫键药物偶联物，其中含有至少一个被至少一个碳氢化合物或取代碳氢化合物所取代的含硫碳原子的连接剂通过二硫键与靶向载体的半胱氨酸硫原子偶联，并且连接剂进一步与药物部分偶联。该发明进一步涉及适合通过二硫键与靶向载体偶联的活化连接剂-药物偶联物。该发明还进一步涉及制备受阻二硫键药物偶联物的方法。
• [EN] PROCESSES FOR PREPARING ACC INHIBITORS AND SOLID FORMS THEREOF<br/>[FR] PROCÉDÉS DE PRÉPARATION D'INHIBITEURS D'ACC ET FORMES SOLIDES CORRESPONDANTES
  申请人：GILEAD SCIENCES INC

  公开号：WO2018161022A1

  公开（公告）日：2018-09-07

  The present disclosure provides solid forms, including a salt or co-crystal, of Compound I which exhibits Acetyl-CoA carboxylase ("ACC") inhibitory activity and may be useful in treating ACC mediated diseases. Also provided herein are processes or steps for the preparation of a Compound I and intermediates useful for the processes or steps described herein.

  本公开提供了化合物I的固体形式，包括盐或共晶，该化合物表现出乙酰辅酶A羧化酶（"ACC"）抑制活性，并可能在治疗ACC介导的疾病中有用。本文还提供了用于制备化合物I的过程或步骤，以及对所述过程或步骤有用的中间体。
• [EN] NUCLEOTIDE CLEAVABLE LINKERS AND USES THEREOF<br/>[FR] LIEURS CLIVABLES NUCLÉOTIDIQUES ET LEURS UTILISATIONS
  申请人：SINGULAR GENOMICS SYSTEMS INC

  公开号：WO2020146397A1

  公开（公告）日：2020-07-16

  Disclosed herein, inter alia, are compounds, compositions, and methods of use thereof for sequencing a nucleic acid.

  在此披露的内容包括化合物、组合物以及它们的使用方法，用于测序核酸。
• Inhibitors of macrophage migration inhibitory factor and methods for identifying the same
  申请人：——

  公开号：US20030195194A1

  公开（公告）日：2003-10-16

  Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: 1 including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R 1 , R 2 , R 3 , R 4 , X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

  提供了MIF的抑制剂，对治疗各种疾病具有实用性，包括与MIF活性相关的病理条件的治疗。MIF的抑制剂具有以下结构：包括立体异构体、前药和其药用盐，其中n、R1、R2、R3、R4、X、Y和Z如本文所定义。还提供了含有MIF抑制剂的组合物，与药用载体结合，以及使用方法。
• Molecular Crystal of (4-(1,8-Naphthyridin-2-YL)Piperidin-1-YL)Pyrimidine Derivative
  申请人：Phillips Eric

  公开号：US20110237605A1

  公开（公告）日：2011-09-29

  A molecular crystal form of (S)-3-(2,5-dimethyl-6-(4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidin- 1 -yl)pyrimidin-4-ylamino)-2-(4-methoxyphenylsulfonamido)propanoic acid is characterized by an X-ray powder diffraction (“XRPD”) spectrum that comprises peaks at 2θ angles of 7.44, 14.80, 16.64, and 23.04±0.2°. The molecular crystal can be formulated into pharmaceutical composition for treating or controlling diseases resulting from pathological angiogenesis.

  (S)-3-(2,5-二甲基-6-(4-(5,6,7,8-四氢-1,8-萘啶基-2-基)哌啶-1-基)嘧啶-4-基氨基)-2-(4-甲氧基苯磺酰胺基)丙酸的分子晶体形式，其具有X射线粉末衍射（“XRPD”）谱，包括2θ角度为7.44、14.80、16.64和23.04±0.2°的峰。该分子晶体可以制成药物组合物，用于治疗或控制由病理性血管生成导致的疾病。