N-[(2R,3S,4S,5S,6S)-4,5-dihydroxy-6-(hydroxymethyl)-2-propan-2-yloxyoxan-3-yl]acetamide

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: N-[(2R,3S,4S,5S,6S)-4,5-dihydroxy-6-(hydroxymethyl)-2-propan-2-yloxyoxan-3-yl]acetamide
• 化学式: C₁₁H₂₁NO₆
• 分子量: 263.29
• InChiKey: CSHJQINNMOQHDM-QUARPLMYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.3
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.91
• 拓扑面积：
  108
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• Dual molecular delivery of oligonucleotides and peptide containing conjugates
  申请人：Merck Sharp & Dohme Corp.

  公开号：US10010562B2

  公开（公告）日：2018-07-03

  Disclosed herein is a method for inhibiting expression of a gene of a subject comprising administering (1) a composition comprising R-(L)a-(G)b; wherein R is an oligonucleotide selected from the group consisting of DNA, RNA, siRNA, and microRNA; L is a linker and each occurrence of L is independently selected from Table 3; G is a targeting ligand and each occurrence of G is independently selected from Table 4; each of a and b is independently 0, 1, 2, 3 or 4; and (2) a composition comprising (P)c-(L)d-(G)e; wherein P is a peptide and each occurrence of P is independently selected from Table 2; L is a linker and each occurrence of L is independently selected from Table 3; G is a targeting ligand and each occurrence of G is independently selected from Table 4; d is 0, 1, 2, 3, 4, 5 or 6; and each of c and e is independently 1, 2, 3, 4, 5 or 6. Compositions in (1) and (2) can be co-administered or sequentially administered.

  本文公开了一种抑制受试者基因表达的方法，包括施用(1)包含R-(L)a-(G)b的组合物；其中R是选自由DNA、RNA、siRNA和microRNA组成的组的寡核苷酸；L是连接子，且L的每个出现独立地选自表3；G是靶向配体，且G的每个出现独立地选自表4；a和b中的每一个独立地为0、1、2、3或4；和 (2)包含(P)c-(L)d-(G)e的组合物；其中P是多肽，且P的每一次出现独立地选自表2；L是连接体，L的每个出现独立地选自表3；G是靶向配体，G的每个出现独立地选自表4；d是0、1、2、3、4、5或6；c和e各自独立地为1、2、3、4、5或6。(1)和(2)中的组合物可以联合给药或顺序给药。
• Peptide containing conjugates for dual molecular delivery of oligonucleotides
  申请人：Merck Sharp & Dohme Corp.

  公开号：US10239957B2

  公开（公告）日：2019-03-26

  Disclosed herein is a peptide containing conjugate comprising (P)c-(L)d-(G)e, wherein P is a peptide and each occurance of P is independently selected from Table 2; L is an optional linker and each occurance of L, if present, is independently selected from Table 3; G is a targeting ligand and each occurance of G is independently selected from Table 4; d is 0, 1, 2, 3, 4, 5 or 6; and each of c and e is independently 1, 2, 3, 4, 5 or 6. The conjugate can be administered to a subject either alone or in combination with a composition comprising R-(L)a-(G)b, wherein R is an oligonucleotide as defined herein, to inhibit expression of a gene of the subject.

  本文公开了一种含有肽的共轭物，该共轭物包含(P)c-(L)d-(G)e，其中P是肽，且P的每个出现独立地选自表2；L是任选连接体，且L的每个出现（如果存在）独立地选自表3；G是靶向配体，且G的每个出现独立地选自表4；d是0、1、2、3、4、5或6；且c和e的每个出现独立地是1、2、3、4、5或6。该共轭物可单独或与包含 R-(L)a-(G)b（其中 R 是本文定义的寡核苷酸）的组合物结合施用给受试者，以抑制受试者基因的表达。
• PEPTIDE CONTAINING CONJUGATES FOR DUAL MOLECULAR DELIVERY OF OLIGONUCLEOTIDES
  申请人：Merck Sharp & Dohme Corp.

  公开号：US20170081425A1

  公开（公告）日：2017-03-23

  Disclosed herein is a peptide containing conjugate comprising (P) c -(L) d -(G) e , wherein P is a peptide and each occurance of P is independently selected from Table 2; L is an optional linker and each occurance of L, if present, is independently selected from Table 3; G is a targeting ligand and each occurance of G is independently selected from Table 4; d is 0, 1, 2, 3, 4, 5 or 6; and each of c and e is independently 1, 2, 3, 4, 5 or 6. The conjugate can be administered to a subject either alone or in combination with a composition comprising R-(L) a -(G) b , wherein R is an oligonucleotide as defined herein, to inhibit expression of a gene of the subject.
• DUAL MOLECULAR DELIVERY OF OLIGONUCLEOTIDES AND PEPTIDE CONTAINING CONJUGATES
  申请人：COLLETTI Steven L.

  公开号：US20170189441A1

  公开（公告）日：2017-07-06

  Disclosed herein is a method for inhibiting expression of a gene of a subject comprising administering (1) a composition comprising R-(L) a -(G) b ; wherein R is an oligonucleotide selected from the group consisting of DNA, RNA, siRNA, and microRNA; L is a linker and each occurrence of L is independently selected from Table 3; G is a targeting ligand and each occurrence of G is independently selected from Table 4; each of a and b is independently 0, 1, 2, 3 or 4; and (2) a composition comprising (P) c -(L) d -(G) e ; wherein P is a peptide and each occurrence of P is independently selected from Table 2; L is a linker and each occurrence of L is independently selected from Table 3; G is a targeting ligand and each occurrence of G is independently selected from Table 4; d is 0, 1, 2, 3, 4, 5 or 6; and each of c and e is independently 1, 2, 3, 4, 5 or 6. Compositions in (1) and (2) can be co-administered or sequentially administered.