3-Methylindoxazene

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并异恶唑
• 英文名称: 3-Methylindoxazene
• 英文别名: 4-methyl-1,2-benzoxazole
• 化学式: C₈H₇NO
• 分子量: 133.15
• InChiKey: JZQZYXDKEKPSPS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  26
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] COMPOSITIONS AND METHODS FOR INHIBITING PROTEIN EMBRYONIC ECTODERM DEVELOPMENT ACTIVITY AND TREATING DISEASE<br/>[FR] COMPOSITIONS ET PROCÉDÉS POUR L'INHIBITION DE L'ACTIVITÉ DE DÉVELOPPEMENT D'ECTODERME EMBRYONNAIRE DE PROTÉINE ET DE TRAITEMENT D'UNE MALADIE
  申请人：EXO THERAPEUTICS INC

  公开号：WO2021195183A1

  公开（公告）日：2021-09-30

  The invention provides compounds that are inhibitors of the protein embryonic ectoderm development (EED), pharmaceutical compositions, their use in modulating the activity of EED, and their use in the treatment of medical disorders, such as cancer. The invention further provides methods of treating medical disorders, such as cancer, and covalently modifying and/or modulating the activity of EED, using an agent that reacts with, and forms a covalent bond to, cysteine324 of EED.

  这项发明提供了抑制蛋白胚胎外胚层发育（EED）的化合物，药物组合物，它们在调节EED活性中的应用，以及它们在治疗癌症等医学疾病中的应用。该发明还提供了治疗医学疾病（如癌症）的方法，并利用一种与EED的半胱氨酸324发生反应并形成共价键的试剂，对EED进行共价修饰和/或调节活性。
• [EN] 3-AZA-BICYCLO[3.3.0]OCTANE COMPOUNDS<br/>[FR] COMPOSÉS 3-AZA-BICYCLO[3.3.0]OCTANE
  申请人：ACTELION PHARMACEUTICALS LTD

  公开号：WO2009004584A1

  公开（公告）日：2009-01-08

  The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as orexin receptor antagonists.

  这项发明涉及式(I)的3-aza-bicyclo[3.3.0]辛烷衍生物，其中R1、R2、R3和A如描述中所述，并且它们作为促进睡眠的受体拮抗剂的用途。
• Fused heterocyclic derivatives and methods of use
  申请人：Albrecht Brian K.

  公开号：US20090318436A1

  公开（公告）日：2009-12-24

  Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  所选化合物对于预防和治疗疾病，例如HGF介导的疾病具有有效性。该发明包括新颖的化合物、类似物、前药和其药学上可接受的盐，以及预防和治疗涉及癌症等疾病和其他不适或状况的药物组合物和方法。该发明还涉及制备这种化合物的过程，以及在这种过程中有用的中间体。
• Aryl sulfonamides useful as inhibitors of chemokine receptor activity
  申请人：Dai Mingshi

  公开号：US20090275556A1

  公开（公告）日：2009-11-05

  The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein R 1 , X, Z, R 2 , X 1 , Ar, n, R 3 and R 4 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR 8 and accordingly are useful for the treatment of a variety of inflammatory and allergic disorders.

  本发明提供了一般式I的化合物：或其药学上可接受的盐，其中R1、X、Z、R2、X1、Ar、n、R3和R4在此处通常定义和子集中定义。本发明的化合物是CCR8的抑制剂，因此对于治疗各种炎症和过敏性疾病是有用的。
• Selective Ligands for the Dopamine 3 (D3) Receptor and Methods of using the Same
  申请人：Wang Shaomeng

  公开号：US20110184033A1

  公开（公告）日：2011-07-28

  Potent and selective ligands for the dopamine 3 (D 3 ) receptor are disclosed. The D3 receptor ligands have a structural formula (I) wherein X is C═O or SO 2 , R 1 is C 1-6 alkyl, R 2 is aryl, heteroaryl, aryl, —(CH 2 ) 1-3 aryl, or —(CH 2 ) 1-3 heteroaryl, and n is 0 or 1. Methods of using the D 3 receptor ligands in the treatment of diseases and conditions wherein modulation of the D 3 receptor provides a benefit also are disclosed.

  揭示了对多巴胺3（D3）受体具有强效和选择性的配体。D3受体配体具有结构式（I），其中X是C═O或SO2，R1是C1-6烷基，R2是芳基，杂环芳基，芳基，—（CH2）1-3芳基或—（CH2）1-3杂环芳基，n为0或1。还揭示了在调节D3受体提供益处的疾病和病况的治疗中使用D3受体配体的方法。