4-ethyl-2-phenylthiazole | 158555-01-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-ethyl-2-phenylthiazole
• 英文别名: 4-ethyl-2-phenyl-thiazole；4-Aethyl-2-phenyl-thiazol；4-Ethyl-2-phenylthiazol；4-Ethyl-2-phenyl-1,3-thiazole
• CAS: 158555-01-2
• 化学式: C₁₁H₁₁NS
• 分子量: 189.281
• InChiKey: OIDMRPOGFLSDCK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  41.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-ethyl-2-phenylthiazole 生成 4-ethyl-2-(4-nitro-phenyl)-thiazole
  参考文献：
  名称：

  Aminophenyl Oxazoles and Thiazoles

  摘要：

  DOI：

  10.1021/ja01290a045
• 作为产物：
  描述：

  (4R)-4-ethyl-2-phenyl-4,5-dihydro-1,3-thiazole 在 sulfur 作用下， 以81%的产率得到4-ethyl-2-phenylthiazole
  参考文献：
  名称：

  Aitken, R. Alan; Armstrong, David P.; Galt, Ronald H. B., Journal of the Chemical Society. Perkin transactions I, 1997, # 6, p. 935 - 943

  摘要：

  DOI：

文献信息

• [EN] IMIDAZOTHIADIAZOLE AND IMIDAZOPYRAZINE DERIVATIVES AS PROTEASE ACTIVATED RECEPTOR 4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION<br/>[FR] DÉRIVÉS D'IMIDAZOTHIADIAZOLE ET D'IMIDAZOPYRAZINE UTILISÉS COMME INHIBITEURS DU RÉCEPTEUR 4 ACTIVÉ PAR UNE PROTÉASE (PAR4) POUR LE TRAITEMENT DE L'AGRÉGATION PLAQUETTAIRE
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2013163279A1

  公开（公告）日：2013-10-31

  The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R5, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.

  本发明提供了式I的噻唑化合物，其中W、Y、R0、R2、R4、R5、R6、R7、X1、X2、X3和X4如本文所定义，或其立体异构体、互变异构体、药学上可接受的盐、前药酯或溶剂化合物形式，其中所有变量均如本文所定义。这些化合物是血小板聚集抑制剂，因此可用作治疗或预防血栓栓塞性疾病的药物。
• DIARYLETHER DERIVATIVES AS ANTITUMOR AGENTS
  申请人：Matsuyama Hironori

  公开号：US20100004438A1

  公开（公告）日：2010-01-07

  An object of the present invention is to provide a medicinal drug much improved in anti tumor activity and excellent in safety. According to the present invention, there is provided a medicinal drug containing a compound represented by the following general formula (1) or a salt thereof as an active ingredient: [Formula 1] wherein X 1 represents a nitrogen atom or a group —CH═, R 1 represents a group -Z-R 6 , in which Z represents a group —CO—, a group —CH(OH)— or the like, R 6 represents a 5- to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R 2 represents a hydrogen atom or a halogen atom, Y represents a group —O—, a group —CO—, a group —CH(OH)— or a lower alkylene group, and A represents [Formula 2] wherein R 3 represents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, R 4 represents an imidazolyl lower alkyl group or the like.

  本发明的一个目的是提供一种在抗肿瘤活性方面大大改进且安全性优异的药物。根据本发明，提供了一种包含以下一般式（1）所表示的化合物或其盐作为活性成分的药物：[式1]其中X1代表氮原子或基团—CH═，R1代表一个基团-Z-R6，其中Z代表基团—CO—，基团—CH(OH)—或类似的基团，R6代表一个含有1至4个氮原子、氧原子或硫原子的5至15个成员的单环、双环或三环饱和或不饱和杂环基团，R2代表氢原子或卤原子，Y代表基团—O—，基团—CO—，基团—CH(OH)—或低碳烷基基团，A代表[式2]其中R3代表氢原子、低碳氧基基团或类似基团，p代表1或2，R4代表咪唑基低碳基团或类似基团。
• [EN] END CAPPED NUCLEIC ACID MOLECULES<br/>[FR] MOLÉCULES D'ACIDE NUCLÉIQUE À EXTRÉMITÉ COIFFÉE
  申请人：NOVARTIS AG

  公开号：WO2016098028A1

  公开（公告）日：2016-06-23

  The disclosure relates to nucleic acids that contain modifications at the 5'-end, 3'-end or 5'-end and 3'-ends, and compounds that can be used to make the modified nucleic acids are disclosed. The modified nucleic acids have improved expression, lower immunogenicity and improved stability compared to unmodified nucleic acids.

  该披露涉及在5'-末端、3'-末端或5'-末端和3'-末端上含有修饰的核酸，以及可用于制备修饰核酸的化合物。与未经修饰的核酸相比，修饰核酸具有更好的表达、更低的免疫原性和更好的稳定性。
• COMPOUNDS FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISEASE
  申请人：SHY Therapeutics LLC

  公开号：US20170174699A1

  公开（公告）日：2017-06-22

  Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease.

  本文提供了抑制MAPK磷酸化的化合物，因此可用于治疗癌症和炎症性疾病的组合物和方法。
• [EN] TRICYCLIC INDOLE-DERIVED SPIRO DERIVATIVES AS CRTH2 MODULATORS<br/>[FR] DÉRIVÉS SPIRO ISSUS D'INDOLE TRICYCLIQUE COMME MODULATEURS DE CRTH2
  申请人：MERCK SERONO SA

  公开号：WO2011006936A1

  公开（公告）日：2011-01-20

  The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases. The compounds according to Formula (I) are suitable as modulators of CRTH2. The invention provides spiro derivatives according to Formula (I) and related formulae that are useful in the treatment and/or prevention of diseases selected from allergic diseases such as allergic asthma, allergic rhinitis, allergic conjunctivitis, and inflammatory dermatoses such as atopic dermatitis, contact hypersensitivity, allergic contact dermatitis, chronic urticaria/chronic idiopathic/autoimmune urticaria, drag-induced exanthems (e.g. toxic epidermal necrolysis or Lyell's syndrome/Stevens-Johnson syndrome/drug hypersensitivity syndrome), photodermatosis or polymorphous light eruption (e.g. photo-irritant contact dermatitis, photoallergy contact dermatitis, chronic actinic dermatitis), and myositis neurodegenerative disorders such as neuropatic pain and other diseases with an inflammatory component such as rheumatoid arthritis, multiple sclerosis, osteoarthritis, and inflammatory bowel disease (IBD).

  本发明涉及式（I）的化合物作为药用活性化合物的用途，以及含有该化合物的药物配方，用于治疗过敏性疾病。根据式（I）的化合物适用作为CRTH2的调节剂。本发明提供了根据式（I)的螺环衍生物及相关公式，可用于治疗和/或预防选择自过敏性疾病的疾病，如过敏性哮喘、过敏性鼻炎、过敏性结膜炎和炎症性皮肤病，如特应性皮炎、接触性过敏性皮炎、慢性荨麻疹/慢性特发性/自身免疫性荨麻疹、药物诱发性皮疹（如毒性表皮坏死松解症或李尔综合征/史蒂文斯-约翰逊综合征/药物过敏综合征）、光敏性皮炎或多形性光疹（如光致刺激性接触性皮炎、光过敏接触性皮炎、慢性日光性皮炎）和肌炎神经退行性疾病，如神经性疼痛和其他具有炎症成分的疾病，如类风湿性关节炎、多发性硬化、骨关节炎和炎症性肠病（IBD）。

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