2-phenyl-4-propylthiazole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-phenyl-4-propylthiazole
• 英文别名: 2-Phenyl-4-propyl-1,3-thiazole
• 化学式: C₁₂H₁₃NS
• 分子量: 203.308
• InChiKey: XUSXIZNFBSTXBB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  41.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  1-戊炔 、 硫代苯甲酰胺 在 9-mesityl-10-methylacridinium tetrafluoroborate 作用下， 以 1,2-二氯乙烷 为溶剂， 反应 9.0h， 以35%的产率得到2-phenyl-4-propylthiazole
  参考文献：
  名称：

  可见光诱导的炔烃双官能化：噻唑和1,1-Dibromo-1-en-3-ynes的合成。

  摘要：

  可见光诱导的硫代酰胺与炔的级联环化反应合成了1,3-噻唑。硫酰胺通过单电子转移（SET）途径生成的硫自由基通过光催化作为该反应的关键中间体而得到促进。当使用溴炔作为底物时，以中等收率获得自偶联产物1,1-dibromo-1-en-3-ynes，并提出了可见光光催化促进该转化的能量转移途径。

  DOI：

  10.1021/acs.joc.9b02300

文献信息

• Nicotinamide Derivatives
  申请人：Blake Tanisha D.

  公开号：US20080146569A1

  公开（公告）日：2008-06-19

  The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds for the treatment of various diseases and conditions such as asthma.

  本发明涉及公式（I）的化合物及其药用可接受的盐和溶剂化合物，其中取代基如本文所定义，包含这种化合物的组合物以及这种化合物用于治疗各种疾病和状况，如哮喘。
• NOVEL TRIAZINEDIONE DERIVATIVES AS GABAB RECEPTOR MODULATORS
  申请人：Riguet Eric

  公开号：US20100004246A1

  公开（公告）日：2010-01-07

  The present invention provides novel compounds of formula I wherein W 1 , W 2 , W 3 , W 4 , W 5 , B, X 1 , X 2 , X 3 , X 4 , X 5 , E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B (“GABA B ”) positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome.

  本发明提供了式I的新化合物，其中W1、W2、W3、W4、W5、B、X1、X2、X3、X4、X5、E和L的定义如本文所述；发明的化合物是γ-氨基丁酸受体亚型B（“GABAB”）正向变构调节剂（增强剂），可用于提供治疗或预防疾病或疾病的方法，包括焦虑、抑郁、癫痫、精神分裂症、认知障碍、痉挛和骨骼肌肌紧张、脊髓损伤、多发性硬化、肌萎缩性侧索硬化、脑瘫、神经痛和与可卡因和尼古丁相关的渴望、惊恐障碍、创伤后应激障碍、急迫性尿失禁、胃食管反流病、暂时性下食管括约肌松弛、功能性胃肠疾病和肠易激综合征的治疗。
• N-HYDROXY-NAPHTHALENE DICARBOXAMIDE AND N-HYDROXY-BIPHENYL-DICARBOXAMIDE COMPOUNDS AS HISTONE DEACETYLASE INHIBITORS
  申请人：Kattar Solomon

  公开号：US20100216796A1

  公开（公告）日：2010-08-26

  The present invention relates to a novel class of N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives. The N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide compounds can be used to treat cancer. The N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives in vivo.

  本发明涉及一种新的N-羟基萘二甲酰胺和N-羟基联苯二甲酰胺衍生物。N-羟基萘二甲酰胺和N-羟基联苯二甲酰胺化合物可用于治疗癌症。N-羟基萘二甲酰胺和N-羟基联苯二甲酰胺化合物还可抑制组蛋白去乙酰化酶，并适用于选择性诱导末端分化，抑制肿瘤细胞的增殖和/或凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物适用于治疗具有肿瘤细胞增殖特征的患者。本发明的化合物也可用于预防和治疗TRX介导的疾病，如自身免疫、过敏和炎症性疾病，以及中枢神经系统（CNS）疾病的预防和/或治疗，如神经退行性疾病。本发明还提供了包含N-羟基萘二甲酰胺和N-羟基联苯二甲酰胺衍生物的药物组合物和这些药物组合物的安全给药方案，易于遵循，并在体内产生治疗有效量的N-羟基萘二甲酰胺和N-羟基联苯二甲酰胺衍生物。
• TRICYCLIC INDOLE-DERIVED SPIRO DERIVATIVES AS CRTH2 MODULATORS
  申请人：Crosignani Stefano

  公开号：US20120115895A1

  公开（公告）日：2012-05-10

  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 emption (e.g., photoirritant 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）的化合物作为药物活性化合物的用途，以及含有该化合物的药物制剂，用于治疗过敏性疾病。根据式（I）的化合物适用于CRTH2的调节剂。本发明提供了根据式（I）及相关式的螺环衍生物，其在过敏性疾病（如过敏性哮喘、过敏性鼻炎、过敏性结膜炎）以及炎症皮肤病（如特应性皮炎、接触性超敏性、过敏性接触性皮炎、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（如毒性表皮坏死症或Lyell综合征/史蒂文斯-约翰逊综合征/药物过敏综合征）、光敏皮肤病或多形性光敏反应（如光致刺激性接触性皮炎、光致过敏接触性皮炎、慢性光性皮炎））以及肌炎神经退行性疾病（如神经病性疼痛）和其他具有炎症成分的疾病（如类风湿性关节炎、多发性硬化症、骨关节炎和炎症性肠病（IBD））的治疗和/或预防中有用。
• Inhibitors of ADAMTS4 or ADAMTS5 for use in preventing or treating cardiac remodeling and chronic heart failure
  申请人：Universitetet i Oslo

  公开号：US10322143B2

  公开（公告）日：2019-06-18

  The present invention provides an inhibitor of an ADAMTS proteoglycanase for use in treating or preventing cardiac remodeling or for use in treating or preventing heart failure in a subject. In particular, the present invention provides an inhibitor of ADAMTS4 or ADAMTS5 for use in treating or preventing cardiac remodeling or chronic heart failure in a subject with cardiac remodeling or with chronic heart failure, or with a condition that may lead to cardiac remodeling and/or chronic heart failure. Also provided is a method of treating or preventing cardiac remodeling or treating or preventing heart failure which method comprises administering to a subject in need thereof a therapeutically effective amount of an inhibitor of an ADAMTS proteoglycanase. Also provided is the use of an inhibitor of an ADAMTS proteoglycanase in the manufacture of a medicament for treating or preventing cardiac remodeling or treating or preventing heart failure.

  本发明提供了一种ADAMTS蛋白聚糖酶抑制剂，用于治疗或预防心脏重塑或用于治疗或预防受试者的心力衰竭。特别是，本发明提供了一种ADAMTS4或ADAMTS5的抑制剂，用于治疗或预防患有心脏重塑或慢性心力衰竭或可能导致心脏重塑和/或慢性心力衰竭的病症的受试者的心脏重塑或慢性心力衰竭。还提供了一种治疗或预防心脏重塑或治疗或预防心衰的方法，该方法包括向有需要的受试者施用治疗有效量的 ADAMTS 蛋白聚糖酶抑制剂。还提供了一种ADAMTS蛋白聚糖酶抑制剂在制造治疗或预防心脏重塑或治疗或预防心衰的药物中的用途。