(2,2-dimethyl-propyl)-thiazol-2-yl-amine | 69212-68-6

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (2,2-dimethyl-propyl)-thiazol-2-yl-amine
• 英文别名: N-(2,2-dimethylpropyl)-1,3-thiazol-2-amine
• CAS: 69212-68-6
• 化学式: C₈H₁₄N₂S
• 分子量: 170.279
• InChiKey: KGXVGHWSHCMEHV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  11
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  53.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (2,2-dimethyl-propyl)-thiazol-2-yl-amine 、 2,4,6-三氯苯基马来酸二酯 生成 8-(2,2-dimethyl-propyl)-5,7-dioxo-5,6,7,8-tetrahydro-thiazolo[3,2-a]pyrimidinylium betaine
  参考文献：
  名称：

  中性黄嘌呤类似物作为环状AMP磷酸二酯酶的抑制剂。

  摘要：

  合成了两种中离子黄嘌呤类似物的几种衍生物，即中离子噻唑并[3,2-α嘧啶-5,7-二酮]和1,3,4-噻二唑并[3,2-α嘧啶-5,7-二酮]。并被评估为环状AMP磷酸二酯酶的抑制剂。这些化合物中大量显示出茶碱样活性。

  DOI：

  10.1002/jps.2600671236
• 作为产物：
  描述：

  2,2-dimethyl-N-thiazol-2-ylpropionamide 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 生成 (2,2-dimethyl-propyl)-thiazol-2-yl-amine
  参考文献：
  名称：

  中性黄嘌呤类似物作为环状AMP磷酸二酯酶的抑制剂。

  摘要：

  合成了两种中离子黄嘌呤类似物的几种衍生物，即中离子噻唑并[3,2-α嘧啶-5,7-二酮]和1,3,4-噻二唑并[3,2-α嘧啶-5,7-二酮]。并被评估为环状AMP磷酸二酯酶的抑制剂。这些化合物中大量显示出茶碱样活性。

  DOI：

  10.1002/jps.2600671236

文献信息

• [EN] PYRIDINE-2-AMIDES USEFUL AS CB2 AGONISTS<br/>[FR] PYRIDINE-2-AMIDES UTILES COMME AGONISTES DE CB2
  申请人：HOFFMANN LA ROCHE

  公开号：WO2014086805A1

  公开（公告）日：2014-06-12

  The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) is a CB2 agonist and can be used as an active ingredient in a medicament.

  这项发明涉及一种化合物，其化学式为（I），其中R1至R4的定义如描述和索赔中所述。化合物的化学式（I）是一种CB2激动剂，可用作药物的活性成分。
• MACROCYCLIC ANTAGONISTS OF THE MOTILIN RECEPTOR FOR TREATMENT OF GASTROINTESTINAL DYSMOTILITY DISORDERS
  申请人：Marsault Eric

  公开号：US20100093720A1

  公开（公告）日：2010-04-15

  The present invention provides conformationally-defined macrocyclic compounds that bind to and/or are functional modulators of the motilin receptor including subtypes, isoforms and/or variants thereof. These macrocyclic compounds, at a minimum, possess adequate pharmacological properties to be useful as therapeutics for a range of disease indications. In particular, these compounds are useful for treatment and prevention of disorders characterized by hypermotilinemia and/or gastrointestinal hypermotility, including, but not limited to, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, C. difficile associated diarrhea, traveller's diarrhea, diarrhea induced by graph versus host disease, other types of diarrhea, dyspepsia, irritable bowel syndrome, chemotherapy-induced nausea and vomiting (emesis) and post-operative nausea and vomiting and functional gastrointestinal disorders. In addition, the compounds possess utility for the treatment of diseases and disorders characterized by poor stomach or intestinal absorption, such as short bowel syndrome, celiac disease and cachexia. The compounds also have use for the treatment of inflammatory diseases and disorders of the gastrointestinal tract, such as inflammatory bowel disease, ulcerative colitis, Crohn's disease and pancreatitis. Accordingly, methods of treating such disorders and pharmaceutical compositions including compounds of the present invention are also provided.

  本发明提供了与胃动素受体及其亚型、异构体和/或变体结合和/或是功能调节剂的构象定义明确的大环化合物。这些大环化合物至少具有足够的药理特性，可用作治疗一系列疾病指示的治疗药物。特别是，这些化合物对于治疗和预防以高胃动素血症和/或胃肠道高蠕动性为特征的疾病非常有用，包括但不限于腹泻、癌症治疗相关腹泻、癌症诱导腹泻、化疗诱导腹泻、放射性肠炎、放射性腹泻、压力诱导腹泻、慢性腹泻、艾滋病相关腹泻、C. difficile相关腹泻、旅行者腹泻、移植物宿主病引起的腹泻、其他类型的腹泻、消化不良、肠易激综合征、化疗诱导的恶心和呕吐（呕吐）以及术后恶心和呕吐和功能性胃肠道疾病。此外，这些化合物对于治疗以胃或肠道吸收不良为特征的疾病和疾病也具有用途，例如短肠综合征、乳糜泻和虚弱。这些化合物还可用于治疗胃肠道炎症性疾病和疾病，如炎症性肠病、溃疡性结肠炎、克罗恩病和胰腺炎。因此，本发明还提供了治疗此类疾病的方法和包括本发明化合物的药物组合物。
• Antimicrobial compounds and methods of making and using the same
  申请人：BIOVERSYS AG

  公开号：US10947237B2

  公开（公告）日：2021-03-16

  The present disclosure relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, reducing the risk of, and delaying the onset of microbial infections in humans and animals.

  本公开内容一般涉及抗微生物化合物领域及其制造和使用方法。这些化合物可用于治疗、预防、降低微生物感染的风险并延缓人类和动物微生物感染的发生。
• PYRIDINE-2-AMIDES USEFUL AS CB2 AGONISTS
  申请人：F.Hoffmann-La Roche AG

  公开号：EP2928867A1

  公开（公告）日：2015-10-14
• MACROCYCLIC ANTAGONISTS OF THE MOTILIN RECEPTOR FOR MODULATION OF THE MIGRATING MOTOR COMPLEX
  申请人：Fraser Graeme L.

  公开号：US20080287371A1

  公开（公告）日：2008-11-20

  The present invention relates to novel conformationally-defined macrocyclic compounds that bind to and/or are functional modulators of the motilin receptor including subtypes, isoforms and/or variants thereof. These macrocyclic compounds are useful as therapeutics for a range of gastrointestinal disorders, in particular those in which suppression or inhibition of the migrating motor complex (MMC) is effective or malfunction of gastric motility or increased motilin secretion is observed, such as hypermotilinemia, imitable bowel syndrome, dyspepsia, including gallbladder dyspepsia, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, C. difficile associated diarrhea, traveller's diarrhea, acute infectious diarrhea, diarrhea induced by graph versus host disease, other types of diarrhea, functional gastrointestinal disorders, chemotherapy-induced nausea and vomiting (emesis), post-operative nausea and vomiting, cyclic vomiting syndrome and functional vomiting. Accordingly, methods of treating such disorders with such macrocyclic compounds and pharmaceutical compositions thereof are also provided in addition to methods of modulating the migrating motor complex.