5-Methyl-2,3-dihydro-1-benzothiophene | 14450-23-8

• 分子结构分类: 有机化合物 - 有机硫化合物 - 硫醚类
• 英文名称: 5-Methyl-2,3-dihydro-1-benzothiophene
• CAS: 14450-23-8
• 化学式: C₉H₁₀S
• 分子量: 150.24
• InChiKey: UKWBFMJSVMQSPA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  25.3
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• GLUCOSYLCERAMIDE SYNTHASE INHIBITORS AND THERAPEUTIC METHODS USING THE SAME
  申请人：The Regents of The University of Michigan

  公开号：US20130095089A1

  公开（公告）日：2013-04-18

  Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.

  葡糖基鞘氨醇合成酶抑制剂和含有该抑制剂的组合物被揭示。还揭示了在治疗疾病和病况中使用葡糖基鞘氨醇合成酶抑制剂的方法，其中抑制葡糖基鞘氨醇合成酶提供益处，如高雪氏病和法布瑞氏病。
• C-ARYL GLUCOSIDE DERIVATIVE, PREPARATION METHODS THEREOF, AND MEDICAL APPLICATIONS THEREOF
  申请人：JIANGSU HANSOH PHARMACEUTICAL GROUP CO., LTD.

  公开号：US20160222047A1

  公开（公告）日：2016-08-04

  C-aryl glucoside derivatives, preparation methods thereof, and medical applications thereof are described. Specifically, compounds represented by formula I, and, tautomers, enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts of the compounds, preparation methods thereof, pharmaceutical compositions containing the compounds, and applications thereof are described. Compounds of formula (I) are useful as therapeutic agents, and particularly as sodium-dependent glucose contransporter protein (SGLT) inhibitors.

  本文描述了C-芳基葡萄糖苷衍生物，其制备方法以及医药应用。具体而言，描述了由式I表示的化合物，以及该化合物的互变异构体、对映体、非对映体、拉卡酯和药学上可接受的盐，其制备方法，含有该化合物的药物组合物以及其应用。式(I)的化合物可用作治疗剂，特别是作为钠依赖葡萄糖共转运蛋白（SGLT）抑制剂。
• [EN] INHIBITORS OF NO PRODUCTION<br/>[FR] INHIBITEURS DE LA PRODUCTION DE NO
  申请人：MAX DELBRUECK CENTRUM FUER MOLEKULARE MEDIZIN HELMHOLTZ GEMEINSCHAFT

  公开号：WO2022043465A1

  公开（公告）日：2022-03-03

  The invention relates to compounds useful as inhibitors of NO production, especially inhibitors of the inducible NO synthase iNOS expressed by microglia and macrophages. The invention also relates to pharmaceutical compositions comprising these compounds and to therapeutic uses of these compounds, especially in the prophylaxis or treatment of conditions characterized by excess NO production, such as ischemic stroke and retinopathies.

  本发明涉及一种化合物，其可用作NO产生的抑制剂，特别是可抑制由微胶质细胞和巨噬细胞表达的诱导型NO合酶iNOS的抑制剂。本发明还涉及含有这些化合物的药物组合物，以及这些化合物的治疗用途，特别是在预防或治疗由过量NO产生所表征的疾病中，如缺血性卒中和视网膜病。
• [EN] METHOD FOR PRODUCING DIPHENYLMETHANE DERIVATIVE<br/>[FR] PROCÉDÉ DE PRODUCTION D'UN DÉRIVÉ DE DIPHÉNYLMÉTHANE<br/>[KO] 다이페닐메탄 유도체의 제조방법
  申请人：DAE WOONG PHARMA

  公开号：WO2017217792A1

  公开（公告）日：2017-12-21

  본 발명은 나트륨-의존성 글루코스 공수송체(SGLT)의 억제제로서 유용한 다이페닐메탄 유도체를 제조하는 개선된 방법에 관한 것으로서, 주요 그룹별로 개별적으로 합성한 뒤 커플링시키는 수렴 합성(convergent synthesis) 방식으로 수행되므로, 종래문헌에 개시된 순차 합성(linear synthesis) 방식에 비해 합성 경로가 간결하고 수율을 높일 수 있으며, 순차 합성 경로가 내재하고 있는 위험요소를 줄일 수 있다. 또한, 상기 방법에 의해 제조된 화합물의 결정형은 물리화학적 특성이 우수하여, 약제 제조 등의 분야에서 유용하게 활용될 수 있다.

  本发明涉及一种改进的方法，用于制备对钠依赖性葡萄糖共运输体（SGLT）具有抑制作用的有用二苯甲烷衍生物。该方法采用汇合合成法，即先分别合成主要基团，然后将它们耦合，与传统文献中的线性合成法相比，合成路径更为简洁，可以提高收率，并降低线性合成路径所固有的风险因素。此外，通过该方法制备的化合物的晶体形态具有优异的物理化学特性，可在药物制造等领域中得到有益利用。
• NOVEL ANTHRANILIC ACID DERIVATIVE OR SALT THEREOF
  申请人：Yokotani Junichi

  公开号：US20090240052A1

  公开（公告）日：2009-09-24

  An anthranilic acid derivative represented by the general formula (X) [wherein R 1 represents hydrogen or a carboxy-protecting group; R 2 represents optionally substituted phenyl, a heterocyclic group, etc.; R 3 represents optionally substituted phenyl, a monocyclic heterocyclic group, etc.; X 1 represents carbonyl, etc.; X 2 represents optionally substituted alkylene group, a bond, etc.; X 3 represents oxygen, a bond, etc.; and X 4 represents a group represented by the general formula -X 5 -X 6 - or -X 6 -X 5 - (wherein X 5 means oxygen, a bond, etc.; and X 6 means optionally substituted alkylene, a bond, etc.)] or a salt of the derivative. The derivative or salt has the inhibitory activity of MMP- 13 production and is hence useful as a therapeutic agent for articular rheumatism, osteoarthritis, cancer, etc.

  一种由通式（X）表示的蒽酸衍生物[其中R1表示氢或羧基保护基；R2表示可选取代的苯基，杂环基等；R3表示可选取代的苯基，单环杂环基等；X1表示羰基等；X2表示可选取代的烷基，键等；X3表示氧原子，键等；X4表示由通式-X5-X6-或-X6-X5-表示的基团（其中X5表示氧原子，键等；X6表示可选取代的烷基，键等）]或其盐。该衍生物或盐具有MMP-13的抑制活性，因此可用作关节风湿病，骨关节炎，癌症等的治疗剂。