Aureusidin | 480-70-6

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 橙酮类黄酮
• 英文名称: Aureusidin
• 英文别名: (2E)-2-[(3,4-dihydroxyphenyl)methylidene]-4,6-dihydroxy-1-benzofuran-3-one
• CAS: 480-70-6
• 化学式: C₁₅H₁₀O₆
• 分子量: 286.241
• InChiKey: WBEFUVAYFSOUEA-YIXHJXPBSA-N

物化性质

• 熔点：
  295-295 °C (decomp)
• 沸点：
  628.6±55.0 °C(Predicted)
• 密度：
  1.708±0.06 g/cm3(Predicted)
• 溶解度：
  可溶于DMSO（少许）、甲醇（少许）
• 物理描述：
  Solid

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  21
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  107
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• [EN] SELECTIVE FOXO INHIBITORS FOR TREATMENT OF DIABETES AND OTHER DISORDERS RELATED TO IMPAIRED PANCREATIC FUNCTION<br/>[FR] INHIBITEURS SÉLECTIFS DE FOXO POUR LE TRAITEMENT DU DIABÈTE ET D'AUTRES TROUBLES LIÉS À UNE FONCTION PANCRÉATIQUE ALTÉRÉE
  申请人：UNIV COLUMBIA

  公开号：WO2020198351A1

  公开（公告）日：2020-10-01

  Various embodiments relate to a compound (represented by Formula I) or a pharmaceutically acceptable salt or tautomer thereof. The compound may selectively inhibit a Forkhead Box O1 (FOXO1) transcription factor. Various embodiments relate to methods comprising administering to a mammal having a disease or disorder associated with impaired pancreatic endocrine function, a therapeutically effective amount of the compound or a pharmaceutically acceptable salt or tautomer thereof. Various embodiments relate to methods for producing enteroendocrine cells that make and secrete insulin in a mammal, comprising administering to the mammal an effective amount of the compound or a pharmaceutically acceptable salt or tautomer thereof.

  各种实施方式涉及一种化合物（由式I表示）或其药用可接受的盐或互变异构体。该化合物可能选择性地抑制Forkhead Box O1（FOXO1）转录因子。各种实施方式涉及方法，包括向患有与胰腺内分泌功能受损相关的疾病或疾病的哺乳动物施用该化合物或其药用可接受的盐或互变异构体的治疗有效量。各种实施方式涉及方法，用于在哺乳动物中产生能够制造和分泌胰岛素的肠内分泌细胞，包括向该哺乳动物施用该化合物或其药用可接受的盐或互变异构体的有效量。
• [EN] NOVEL COMPOUNDS AND METHODS OF USE TREATING FRUCTOSE-RELATED DISORDERS OR DISEASES<br/>[FR] NOUVEAUX COMPOSÉS ET MÉTHODES D'UTILISATION POUR LE TRAITEMENT DE TROUBLES OU DE MALADIES LIÉS AU FRUCTOSE
  申请人：COLORADO RES PARTNERS LLC

  公开号：WO2020215022A1

  公开（公告）日：2020-10-22

  Disclosed herein are novel compounds that inhibit fructokinase (KHK or ketohexokinase) and the downstream metabolic effects mediated by fructose metabolism. Fructokinase inhibitors specifically block the metabolism of both dietary and endogenous fructose metabolism and have a host of potential metabolic benefits.

  本文披露了一种新型化合物，可以抑制果糖激酶（KHK或酮己糖激酶）以及由果糖代谢介导的下游代谢效应。果糖激酶抑制剂可以特异性地阻断膳食和内源性果糖代谢的代谢，并具有一系列潜在的代谢益处。
• [EN] INDAZOLE INHIBITORS OF FRUCTOKINASE (KHK) AND METHODS OF USE IN TREATING KHK-MEDIATED DISORDERS OR DISEASES<br/>[FR] INHIBITEURS D'INDAZOLE DE LA FRUCTOKINASE (KHK) ET MÉTHODES D'UTILISATION DANS LE TRAITEMENT DE TROUBLES OU DE MALADIES À MÉDIATION PAR KHK
  申请人：REGENTS OF THE UNIV OF COLORADO A BODY CORPORATE

  公开号：WO2018170517A1

  公开（公告）日：2018-09-20

  Disclosed herein are novel indazole-based compounds that inhibit fructokinase (aka ketohexokinase) and the downstream metabolic effects mediated by fructose metabolism. Fructokinase inhibitors specifically block the metabolism of both dietary and endogenous fructose metabolism and have a host of potential metabolic benefits. These benefits including blocking sugar craving and sugar induced metabolic syndrome and diabetes, but also blocking fructose metabolism can benefit the rare orphan disease Hereditary Fructose Intolerance, obesity, insulin resistance, metabolic syndrome, fatty liver, hypertension, cardiac injury from ischemia, certain cancers (including hepatocellular and pancreas), acute kidney injury from ischemia, heat stress, rhabdomyolysis or radiocontrast, and chronic diabetic and nondiabetic renal disease.

  本文披露了一种新型的基于吲唑的化合物，可以抑制果糖激酶（又称酮葡糖激酶）以及由果糖代谢介导的下游代谢效应。果糖激酶抑制剂特异性地阻断了膳食和内源性果糖代谢的代谢，具有一系列潜在的代谢益处。这些益处包括阻止对糖的渴望和糖诱导的代谢综合征和糖尿病，同时阻断果糖代谢也有助于罕见的孤儿病遗传性果糖不耐受症、肥胖、胰岛素抵抗、代谢综合征、脂肪肝、高血压、缺血所致心脏损伤、某些癌症（包括肝细胞和胰腺）、缺血所致急性肾损伤、热应激、横纹肌溶解症或放射造影剂引起的肌纤维溶解症，以及慢性糖尿病和非糖尿病肾病。
• [EN] THERAPEUTIC AURONES<br/>[FR] AURONES THÉRAPEUTIQUES
  申请人：MIDDLE TENNESSEE STATE UNIV

  公开号：WO2017180644A1

  公开（公告）日：2017-10-19

  Substituted aurones were found to have antitrypanosomal, antifungal and immunomodulatory activity. The invention provides novel aurone compounds, pharmaceutical compositions, and methods encompassing medical and veterinary applications.

  发现替代的金莲素具有抗锥虫、抗真菌和免疫调节活性。该发明提供了新型金莲素化合物、药物组合物和方法，涵盖医学和兽医应用。
• NICOTINYL RIBOSIDE COMPOUNDS AND THEIR USES
  申请人：MitoPower, LLC

  公开号：US20200397807A1

  公开（公告）日：2020-12-24

  The disclosure provides nicotinamide riboside (NR), the reduced form of NR (NRH), nicotinic acid riboside (NAR), the reduced form of NAR (NARH), derivatives thereof, compositions thereof and uses thereof. The NR and NAR derivatives have improved stability and bioavailability compared to NR and NAR. NR, NRH, NAR, NARH, and derivatives thereof can increase cellular NAD + levels and enhance mitochondrial and cellular function and cell viability. Therefore, NR, NRH, NAR, NARH, and derivatives thereof, whether alone or in combination with one or more additional therapeutic agents (e.g., a mitochondrial uncoupler or/and a PARP inhibitor), are useful for treating mitochondrial diseases, mitochondria-related diseases and conditions, metabolic disorders, and other disorders and conditions.

  该披露提供烟酰胺核糖苷（NR）、烟酰胺核糖苷的还原形式（NRH）、烟酸核糖苷（NAR）、烟酸核糖苷的还原形式（NARH）、以及它们的衍生物、组合物和用途。与NR和NAR相比，NR和NAR的衍生物具有更好的稳定性和生物利用度。NR、NRH、NAR、NARH和它们的衍生物可以增加细胞NAD+水平，增强线粒体和细胞功能以及细胞存活能力。因此，NR、NRH、NAR、NARH和它们的衍生物，无论是单独使用还是与一个或多个额外治疗剂（例如线粒体解耦蛋白抑制剂和/或PARP抑制剂）结合使用，都可用于治疗线粒体疾病、与线粒体相关的疾病和症状、代谢紊乱以及其他疾病和症状。