[(E,1R)-1-[(2R,4Z,7S,8R)-7-溴-8-乙基-3,6,7,8-四氢-2H-氧杂环辛三烯-2-基]己-3-烯-5-炔基]乙酸酯 | 3442-58-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 奥昔康唑
• 中文名称: [(E,1R)-1-[(2R,4Z,7S,8R)-7-溴-8-乙基-3,6,7,8-四氢-2H-氧杂环辛三烯-2-基]己-3-烯-5-炔基]乙酸酯
• 英文名称: Laurencin
• 英文别名: [(E)-1-[(5Z)-3-bromo-2-ethyl-3,4,7,8-tetrahydro-2H-oxocin-8-yl]hex-3-en-5-ynyl] acetate
• CAS: 3442-58-8
• 化学式: C₁₇H₂₃BrO₃
• 分子量: 355.3
• InChiKey: ZFYWONYUPVGTQJ-MUIOLIGRSA-N

物化性质

• 熔点：
  73-74 °C
• 沸点：
  421.4±45.0 °C(Predicted)
• 密度：
  1.209±0.06 g/cm3(Predicted)
• 溶解度：
  CHCl3, Methanol

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  21
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  35.5
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• [EN] POLYGLYOXYLATES, MANUFACTURE AND USE THEREOF<br/>[FR] POLYGLYOXYLATES, LEUR PRODUCTION ET LEUR UTILISATION
  申请人：UNIV WESTERN ONTARIO

  公开号：WO2015168809A1

  公开（公告）日：2015-11-12

  Self-immolative polymers degrade by an end-to-end depolymerisation mechanism in response to the cleavage of a stabilizing end-cap from the polymer terminus. Examples include homopolymers, mixed polymers including block copolymers, suitable for a variety of applications. A polyglyoxylate can be end-capped or capped with a linker as in a block copolymer.

  自焚式聚合物通过从聚合物末端切割稳定端盖，以端到端解聚机制进行降解。例如包括均聚物、混合聚合物包括区块共聚物，适用于各种应用。聚乙二醇酸可以端接或与连接剂如区块共聚物一样封端。
• [EN] PROTEASOME INHIBITING ß-LACTAM PRODRUGS USEFUL FOR THE TREATMENT OF CANCER AND NEURODEGENERATIVE DISORDERS<br/>[FR] PROMÉDICAMENTS À BASE DE SS-LACTAME INHIBITEURS DU PROTÉASOME UTILES POUR LE TRAITEMENT DU CANCER ET DE TROUBLES NEURODÉGÉNÉRATIFS
  申请人：VITA API

  公开号：WO2018115497A1

  公开（公告）日：2018-06-28

  The present invention relates generally to proteasome inhibiting β-lactam compounds useful for the treatment of cancer and neurodegenerative disorders. The invention also provides pharmaceutical compositions and extended release formulations of said compounds, and medical uses of said compounds and/or pharmaceutical compositions to treat cancer and neurodegenerative disorders.

  本发明通常涉及抑制蛋白酶体的β-内酰胺化合物，用于治疗癌症和神经退行性疾病。该发明还提供了所述化合物的药物组合物和延长释放配方，以及利用所述化合物和/或药物组合物治疗癌症和神经退行性疾病的医疗用途。
• [EN] NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS<br/>[FR] NOUVEAUX COMPOSÉS ET COMPOSITIONS PHARMACEUTIQUES LES COMPRENANT POUR LE TRAITEMENT DE TROUBLES INFLAMMATOIRES
  申请人：GALAPAGOS NV

  公开号：WO2014202458A1

  公开（公告）日：2014-12-24

  The present invention discloses compounds according to Formula I: Wherein R 1a, R 1b, R 2, R 4, R5, R 6, R 7, R 8, W, X, Y, Z, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases,proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.

  本发明公开了根据式I的化合物：其中R 1a、R 1b、R 2、R 4、R5、R 6、R 7、R 8、W、X、Y、Z、Cy和下标a如本文所定义。本发明涉及抑制自体脂肪酶（NPP2或ENPP2）的化合物，其制备方法，包含其的药物组合物，以及使用该化合物进行预防和/或治疗涉及纤维化疾病、增殖性疾病、炎症性疾病、自身免疫疾病、呼吸系统疾病、心血管疾病、神经退行性疾病、皮肤病和/或与异常血管生成相关疾病的方法。
• [EN] COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS<br/>[FR] COMPOSÉS ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT DESTINÉS À TRAITER LES TROUBLES INFLAMMATOIRES
  申请人：GALAPAGOS NV

  公开号：WO2014139882A1

  公开（公告）日：2014-09-18

  The present invention discloses compounds according to Formula I: Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R7, R8, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseasesby administering the compound of the invention.

  本发明公开了根据式I的化合物：其中R1a、R1b、R2、R4、R5、R6a、R6b、R7、R8、W、X、Cy和下标a如本文所定义。本发明涉及抑制自体脂肪酶（NPP2或ENPP2）的化合物，其制备方法，包含其的药物组合物，以及使用该化合物进行预防和/或治疗涉及纤维化疾病、增生性疾病、炎症性疾病、自身免疫疾病、呼吸系统疾病、心血管疾病、神经退行性疾病、皮肤病和/或与异常血管生成相关疾病的方法。
• PLURIPOTENT EMBRYONIC-LIKE STEM CELLS, COMPOSITIONS, METHODS AND USES THEREOF
  申请人：Young Henry E.

  公开号：US20100239542A1

  公开（公告）日：2010-09-23

  The present invention relates to pluripotent stem cells, particularly to pluripotent embryonic-like stem cells. The invention further relates to methods of purifying pluripotent embryonic-like stem cells and to compositions, cultures and clones thereof. The present invention also relates to a method of transplanting the pluripotent stem cells of the present invention in a mammalian host, such as human, comprising introducing the stem cells, into the host. The invention further relates to methods of in vivo administration of a protein or gene of interest comprising transfecting a pluripotent stem cell with a construct comprising DNA which encodes a protein of interest and then introducing the stem cell into the host where the protein or gene of interest is expressed. The present also relates to methods of producing mesodermal, endodermal or ectodermal lineage-committed cells by culturing or transplantation of the pluripotent stem cells of the present invention.

  本发明涉及多能干细胞，特别是多能胚胎样干细胞。该发明还涉及纯化多能胚胎样干细胞的方法，以及相关的组成物、培养物和克隆体。本发明还涉及将本发明的多能干细胞移植到哺乳动物宿主（如人类）的方法，包括将干细胞引入宿主体内。该发明还涉及通过将编码感兴趣蛋白质的DNA构建转染多能干细胞，然后将干细胞引入宿主体内，在宿主体内表达感兴趣蛋白质或基因的体内给药方法。本发明还涉及通过培养或移植本发明的多能干细胞来产生中胚层、内胚层或外胚层定向分化的细胞的方法。