2-(Methylamino)-5-oxohexanoic acid

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 2-(Methylamino)-5-oxohexanoic acid
• 化学式: C₇H₁₃NO₃
• 分子量: 159.18
• InChiKey: QBAOJDDQEIVZJA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.8
• 重原子数：
  11
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  66.4
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Acylated Exendin-4 Compounds
  申请人：Lau Jesper

  公开号：US20090318353A1

  公开（公告）日：2009-12-24

  This invention provides new therapeutic peptides, i.e. new protracted Exendin-4 compounds, pharmaceutical compositions and the use of such.

  本发明提供了新的治疗性肽，即新的长效Exendin-4化合物、药物组合物及其用途。
• SELECTIVE PYY COMPOUNDS AND USES THEREOF
  申请人：NOVO NORDISK A/S

  公开号：US20160289283A1

  公开（公告）日：2016-10-06

  The invention relates to PYY compounds having the amino acid in the position corresponding to position 30 of hPYY(1-36) substituted with tryptophan and derivatives thereof with a modifying group attached to the position corresponding to position 7 of hPYY(1-36). The compounds of the invention are selective Y2 receptor agonists. The invention also relates to pharmaceutical compositions comprising such PYY compounds and pharmaceutically acceptable excipients, as well as the medical use of the PYY compounds.

  该发明涉及PYY化合物，其氨基酸在与hPYY(1-36)中位置30对应的位置被色氨酸及其衍生物取代，并且在与hPYY(1-36)中位置7对应的位置附着有修饰基团。该发明的化合物是选择性Y2受体激动剂。该发明还涉及含有这种PYY化合物和药用可接受的辅料的药物组合物，以及PYY化合物的医药用途。
• [EN] EGF(A) ANALOGUES WITH FATTY ACID SUBSTITUENTS<br/>[FR] ANALOGUES D'EGF(A) AVEC SUBSTITUANTS ACIDES GRAS
  申请人：NOVO NORDISK AS

  公开号：WO2017121850A1

  公开（公告）日：2017-07-20

  The invention relates to compounds derived from the EGF(A) domain of LDL-R, in particular compounds comprising a peptide analogue of the wild-type EGF(A) (LDL-R(293- 332)) sequence and at least one substituent comprising at least one fatty acid group. The invention also relates to a pharmaceutical composition thereof and use a medicament. The novel EGF(A) compounds of the invention are useful as treatment e.g. in the field of cholesterol lowering, dyslipidaemia and cardiovascular disease.

  该发明涉及从LDL-R的EGF(A)结构域衍生的化合物，特别是包括野生型EGF(A)(LDL-R(293-332))序列的肽类类似物和至少一个含有至少一个脂肪酸基团的取代基的化合物。该发明还涉及其制药组合物和药物的使用。该发明的新型EGF(A)化合物可用于治疗，例如在降低胆固醇、脂质代谢异常和心血管疾病领域。
• [EN] GLP-1 DERIVATIVES AND USES THEREOF<br/>[FR] DÉRIVÉS DE GLP-1 ET LEURS UTILISATIONS
  申请人：NOVO NORDISK AS

  公开号：WO2016083499A1

  公开（公告）日：2016-06-02

  The invention relates to a derivative of a GLP-1 analogue of a general Formula I, which derivative comprises a side chain attached to a Lys residue at position 34, 35, 36, 37, or 38 of the GLP-1 analogue, which side chain comprises a Branched linker, a 1st and a 2nd Protractor selected from C18 diacid, C20 diacid, and sulfonic acid C16, and at least one Linker element-1 incorporating ethylene glycol units. Linker element-1 may be incorporated in an optional Pre-linker, and/or in a 1st or 2nd Post-linker. The invention also relates to novel GLP-1 analogues, novel side chain intermediate products and their manufacture and use to prepare derivatives of biologically active peptides and proteins, as well as pharmaceutical compositions and medical uses of the analogues and derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.

  这项发明涉及通用公式I的GLP-1类似物的衍生物，该衍生物包括连接到GLP-1类似物的第34、35、36、37或38位的Lys残基的侧链，该侧链包括一个分支连接物、从C18二酸、C20二酸和磺酸C16中选择的第一和第二伸缩剂，以及至少一个包含乙二醇单元的连接元素-1。连接元素-1可以被合并到一个可选的前连接物中，和/或第一或第二后连接物中。该发明还涉及新型GLP-1类似物、新型侧链中间体产品及其制备和用于制备生物活性肽和蛋白质衍生物的用途，以及类似物和衍生物的药物组合物和医疗用途。这些衍生物具有非常长的半衰期，同时保持令人满意的效力，因此它们有潜在适用于每月一次的给药。
• HPYY(1-36) Having a Beta-Homoarginine Substitution at Position 35
  申请人：NOVON NORDISK A/S

  公开号：US20160263197A1

  公开（公告）日：2016-09-15

  The invention relates to PYY compounds having the amino acid in the position corresponding to position 35 of hPYY(1-36) substituted with beta-homoarginine and derivatives thereof with a modifying group attached to the position corresponding to position 7 of hPYY(1-36). The compounds of the invention are selective Y2 receptor agonists. The invention also relates to pharmaceutical compositions comprising such PYY compounds and pharmaceutically acceptable excipients, as well as the medical use of the PYY compounds.

  该发明涉及PYY化合物，其中该氨基酸位于与hPYY(1-36)的第35位对应的位置上，被β-同型精氨酸及其衍生物取代，并且在与hPYY(1-36)的第7位对应的位置上连接有修饰基团。该发明的化合物是选择性Y2受体激动剂。该发明还涉及包括这种PYY化合物和药用可接受的赋形剂的药物组合物，以及PYY化合物的医药用途。