5-Methyldibenzazocin-6-on | 33486-34-9

• 分子结构分类: 有机化合物 - 苯类化合物
• 英文名称: 5-Methyldibenzazocin-6-on
• 英文别名: (11Z)-5-methylbenzo[c][1]benzazocin-6-one
• CAS: 33486-34-9
• 化学式: C₁₆H₁₃NO
• 分子量: 235.285
• InChiKey: VITDVNJGCZNHEF-KHPPLWFESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  18
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• [EN] LYMPHATIC SYSTEM-DIRECTING LIPID PRODRUGS<br/>[FR] PROMÉDICAMENTS LIPIDIQUES ORIENTANT VERS LE SYSTÈME LYMPHATIQUE
  申请人：ARIYA THERAPEUTICS INC

  公开号：WO2019046491A1

  公开（公告）日：2019-03-07

  The present invention provides lymphatic system-directing lipid prodrugs, pharmaceutical compositions thereof, methods of producing such prodrugs and compositions, as well as methods of improving the bioavailability or other properties of a therapeutic agent that comprises part of the lipid prodrug. The present invention also provides methods of treating a disease, disorder, or condition such as those disclosed herein, comprising administering to a patient in need thereof a provided lipid prodrug or a pharmaceutical composition thereof.

  本发明提供了淋巴系统定向脂质前药，其制药组合物，制备这种前药和组合物的方法，以及改善作为脂质前药一部分的治疗剂的生物利用度或其他性质的方法。本发明还提供了治疗疾病、紊乱或症状的方法，包括向需要的患者施用所提供的脂质前药或其制药组合物。
• [EN] BIOCONJUGATES CONTAINING SULFAMIDE LINKERS FOR USE IN TREATMENT<br/>[FR] BIOCONJUGUÉS CONTENANT DES SÉQUENCES DE LIAISON SULFAMIDE POUR UTILISATION À DES FINS THÉRAPEUTIQUES
  申请人：SYNAFFIX BV

  公开号：WO2017137456A1

  公开（公告）日：2017-08-17

  The present invention is based on the surprising finding that the linker employed in a bioconjugate, such as an anti-body-drug conjugate, is not therapeutically inert but has an effect on the therapeutic index of the bioconjugate. The present invention thus concerns a method for increasing the therapeutic index of a bioconjugate and the bioconjugates for use in treatment, in particular cancer. The bioconjugates according to the invention have a sulfamide linker comprising a group according to formula (1).

  本发明基于一个令人惊讶的发现，即生物结合物中使用的连接剂，如抗体药物结合物，不是治疗惰性的，而是对生物结合物的治疗指数产生影响。因此，本发明涉及一种增加生物结合物的治疗指数的方法，以及用于治疗，特别是癌症的生物结合物。根据本发明的生物结合物具有包含符合式（1）的基团的磺酰胺连接剂。
• N-Acylated lipophilic amino acid derivatives
  申请人：Funamizu HIdenori

  公开号：US20080027038A1

  公开（公告）日：2008-01-31

  Compounds of structural formula (I) where A is a lipophilic group including an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group and R is hydrogen, alkyl or cycloalkyl, and pharmaceutically acceptable salts and individual isomers thereof, which have growth hormone releasing activity in humans or animals.

  结构式(I)中，A是一个包括脂溶性桥接基团的亲脂基团，B是一个亲脂基团，D是一个至少有一个氨基或取代氨基的基团，R是氢、烷基或环烷基，以及其药学上可接受的盐和单体异构体，具有在人或动物体内释放生长激素的活性的化合物。
• D-amino acid derivative-modified peptidoglycan and methods of use thereof
  申请人：The Regents of the University of California

  公开号：US10016498B2

  公开（公告）日：2018-07-10

  The present disclosure provides modified bacteria and modified peptidoglycan comprising modified D-amino acids; compositions comprising the modified bacteria or peptidoglycan; and methods of using the modified bacteria or peptidoglycan. The modified D-amino acids include a bioorthogonal functional group such as an azide, an alkyne or a norbornene group. Also provided are modified peptidoglycans conjugated to a molecule of interest via a linker.

  本公开提供了包含改性 D-氨基酸的改性细菌和改性肽聚糖；包含改性细菌或肽聚糖的组合物；以及使用改性细菌或肽聚糖的方法。改性 D-氨基酸包括生物正交官能团，如叠氮基、炔基或降冰片烯基。还提供了通过连接体与相关分子共轭的改性肽聚糖。
• Process for the cycloaddition of a halogenated 1,3-dipole compound with a (hetero)cycloalkyne
  申请人：SynAffix B.V.

  公开号：US10266502B2

  公开（公告）日：2019-04-23

  The present invention relates to a cycloaddition process comprising the step of reacting a halogenated aliphatic 1,3-dipole compound with a (hetero)cycloalkyne according to Formula (1): Preferably, the (hetero)cycloalkyne according to Formula (1) is a (hetero)cyclooctyne. The invention also relates to the cycloaddition products obtainable by the process according to the invention. The invention further relates to halogenated aliphatic 1,3-dipole compounds, in particular to halogenated aliphatic 1,3-dipole compounds comprising N-acetylgalactosamine-UDP (GalNAc-UDP), and to halogenated 1,3-dipole compounds comprising (peracylated) N-acetylglucosamine (GlcNAc), N-acetylgalactosamine (GalNAc), N-acetylmannosamine (ManNAc) and N-acetyl neuraminic acid (NeuNAc).

  本发明涉及一种环加成工艺，包括卤代脂肪族 1,3-二极化合物与符合式（1）的（杂）环炔反应的步骤：根据式（1）的（杂）环炔最好是（杂）环辛炔。本发明还涉及根据本发明的工艺可获得的环加成产物。本发明还涉及卤代脂肪族 1，3-二极化合物，特别是包含 N-乙酰半乳糖胺-UDP（GalNAc-UDP）的卤代脂肪族 1，3-二极化合物、以及由（过酰化）N-乙酰葡糖胺（GlcNAc）、N-乙酰半乳糖胺（GalNAc）、N-乙酰甘露糖胺（ManNAc）和 N-乙酰神经氨酸（NeuNAc）组成的卤代 1，3-二极化合物。