1H-pyrrolo[3,2-d]pyrimidin-2-ol

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并嘧啶类
• 英文名称: 1H-pyrrolo[3,2-d]pyrimidin-2-ol
• 化学式: C6H5N3O
• InChiKey: NXWVEGMKKAVOQL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.62
• 重原子数：
  10.0
• 可旋转键数：
  0.0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  61.8
• 氢给体数：
  2.0
• 氢受体数：
  3.0

文献信息

• [EN] ECTONUCLEOTIDE PYROPHOSPHATASE-PHOSPHODIESTERASE 1 (ENPP-1) INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE L'ECTONUCLÉOTIDE PYROPHOSPHATASE-PHOSPHODIESTÉRASE (ENPP-1) ET UTILISATIONS DE CES DERNIERS
  申请人：MAVUPHARMA INC

  公开号：WO2019046778A1

  公开（公告）日：2019-03-07

  Disclosed herein are methods and compounds of augmenting and enhancing the production of type I IFNs in vivo. In some embodiments, the compounds disclosed herein are ENPP-1 inhibitors, pharmaceutical compositions, and methods for the treatment of cancer or a viral infection.

  本文揭示了一种增强和促进体内I型干扰素产生的方法和化合物。在某些实施例中，本文所披露的化合物是ENPP-1抑制剂，药物组合物，以及用于治疗癌症或病毒感染的方法。
• [EN] FUSED HETEROARYL PYRIDYL AND PHENYL BENZENESUFLONAMIDES AS CCR2 MODULATORS FOR THE TREAMENT OF INFLAMMATION<br/>[FR] HÉTÉROARYL-PYRIDYL- ET PHÉNYL-BENZÈNESULFONAMIDES CONDENSÉS EN TANT QUE MODULATEURS DU CCR2 POUR LE TRAITEMENT DE L'INFLAMMATION
  申请人：CHEMOCENTRYX INC

  公开号：WO2009009740A1

  公开（公告）日：2009-01-15

  Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2- mediated diseases and as controls in assays for the identification of CCR2 antagonists. A compound of the formula (I) or a salt thereof: where: R1 and R2 are each independently hydrogen, halogen, C1-8alkyl, -CN. or C1-8 haloalkyl, provided that at least one of R11or R2 is other than hydrogen; each R3 is independently hydrogen; R4 is hydrogen; R5 is halogen or C1-8 alkyl; R6 is hydrogen; X1 is CR7, N or NO; X2 and X4 are N or NO; X3 is CR7; X6 and X7 are each independently selected from CR7, N, and NO; each R7 is independently selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C2-8 alkyl, substituted or unsubstituted C2-8 alkeπyl, substituted or unsubstituted C2-8 alkynyl, -CN. =O, -NO2, -OR6, -OC(O)R8, -CO2R8, -C(O)R8, -C(O)NR0R8, -OC(O)NR9R8, -NR10C(O)R8, -NR10C(O)NR9R8, -NR9R8, -NR10CO2R8, -SR8, -S(O)R8, -S(O)2R8, -S(O)2NR9R8, -NR10S(O)2R8, substituted or unsubstituted C6-10 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl and substituted or unsubstituted 3- to 10-membered heterocyclyl;

  提供的化合物作为CCR2受体的有效拮抗剂。这些化合物通常是芳基磺酰胺衍生物，可用于制药组合物、治疗CCR2介导疾病的方法以及作为鉴定CCR2拮抗剂的测定中的对照物。具有以下式（I）或其盐的化合物：其中：R1和R2各自独立地是氢、卤素、C1-8烷基、-CN或C1-8卤代烷基，但至少其中一个是氢以外的；每个R3独立地是氢；R4是氢；R5是卤素或C1-8烷基；R6是氢；X1是CR7、N或NO；X2和X4是N或NO；X3是CR7；X6和X7各自独立地选自CR7、N和NO；每个R7独立地选自氢、卤素、取代或未取代的C2-8烷基、取代或未取代的C2-8烯基、取代或未取代的C2-8炔基、-CN、=O、-NO2、-OR6、-OC（O）R8、-CO2R8、-C（O）R8、-C（O）NR0R8、-OC（O）NR9R8、-NR10C（O）R8、-NR10C（O）NR9R8、-NR9R8、-NR10CO2R8、-SR8、-S（O）R8、-S（O）2R8、-S（O）2NR9R8、-NR10S（O）2R8、取代或未取代的C6-10芳基、取代或未取代的5-至10-成员杂芳基和取代或未取代的3-至10-成员杂环烷基。
• [EN] A SIK INHIBITOR FOR USE IN A METHOD OF TREATING AN INFLAMMATORY AND/OR IMMUNE DISORDER<br/>[FR] INHIBITEUR DE SIK POUR L'UTILISATION DANS UNE MÉTHODE DE TRAITEMENT D'UN TROUBLE INFLAMMATOIRE ET/OU IMMUNITAIRE
  申请人：UNIV DUNDEE

  公开号：WO2013136070A1

  公开（公告）日：2013-09-19

  The present invention relates to the discovery that salt inducible kinases (SIKs) suppress the formation of anti-inflammatory molecules such as IL-10, which are important for the resolution of inflammation and identifies SIK inhibitors that may be used to treat disorders associated with undesirable inflammation, such as inflammatory bowel disease and/or autoimmune disorders.

  本发明涉及到一个发现，即盐诱导激酶（SIKs）抑制抗炎分子的形成，例如IL-10，这些分子对于炎症的解决非常重要，并且鉴定出可能用于治疗与不良炎症相关的疾病的SIK抑制剂，例如炎症性肠病和/或自身免疫性疾病。
• SIK INHIBITOR FOR USE IN A METHOD OF TREATING AN INFLAMMATORY AND/OR IMMUNE DISORDER
  申请人：UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEE

  公开号：US20150045370A1

  公开（公告）日：2015-02-12

  The present invention relates to the discovery that salt inducible kinases (SIKs) suppress the formation of anti-inflammatory molecules such as IL-10, which are important for the resolution of inflammation and identifies SIK inhibitors that may be used to treat disorders associated with undesirable inflammation, such as inflammatory bowel disease and/or autoimmune disorders.

  本发明涉及到一个发现：盐诱导激酶（SIKs）可以抑制抗炎分子的形成，例如重要的解决炎症的分子IL-10，并且鉴定出了SIK抑制剂，可以用于治疗与不良炎症有关的疾病，例如炎症性肠病和/或自身免疫性疾病。
• FUSED HETEROARYL PYRIDYL AND PHENYL BENZENESUFLONAMIDES AS CCR2 MODULATORS FOR THE TREATMENT OF INFLAMMATION
  申请人：Krasinski Antoni

  公开号：US20090233946A1

  公开（公告）日：2009-09-17

  Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the identification of CCR2 antagonists.

  提供了一些作为CCR2受体激动剂的有效拮抗剂的化合物。这些化合物通常是芳基磺酰胺衍生物，并可用于制备药物组合物，治疗CCR2介导的疾病的方法以及用作CCR2拮抗剂鉴定的实验控制。