2-methyl-2,3,4,9-tetrahydro-1H-indeno[2,1-c]pyridine | 110605-92-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚和异茚
• 英文名称: 2-methyl-2,3,4,9-tetrahydro-1H-indeno[2,1-c]pyridine
• 英文别名: 2-Methyl-2,3,4,9-tetrahydro-1H-indeno[2,1-c]pyridine；2-methyl-1,3,4,9-tetrahydroindeno[2,1-c]pyridine
• CAS: 110605-92-0
• 化学式: C₁₃H₁₅N
• 分子量: 185.269
• InChiKey: BPGPBEYOYLIMCC-UHFFFAOYSA-N

物化性质

• 沸点：
  311.9±41.0 °C(Predicted)
• 密度：
  1.11±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  2-methyl-2,3,4,9-tetrahydro-1H-indeno[2,1-c]pyridine 在 palladium on activated charcoal 双氧水 、 sodium carbonate 作用下， 以 乙醇 、 二氯甲烷 、 水 为溶剂， 反应 35.83h， 生成 2-methyl-1,3,4,9-tetrahydroindeno[2,1-c]pyridine-1-carbonitrile
  参考文献：
  名称：

  黑纹状体毒素1-甲基-4-苯基-1,2,3,6-四氢吡啶的半刚性三环类似物的研究。

  摘要：

  N-甲基色胺和甲醛的缩合反应生成的四氢-β-咔啉是一种1-甲基-4-苯基-1,2,3,6-四氢吡啶（MPTP）tha的半刚性三环类似物。在单胺氧化酶B（MAO-B）催化的反应中，正常实验大鼠以约0.5％的MPTP速率生物转化为相应的二氢化合物。其中与氮原子的双键β，γ保持烯丙基特性的相应的四氢茚并吡啶是稍好的MAO-B底物。从这些类型的三环结构衍生的所提出的以碳为中心的自由基中间体中，除了存在环应变外，氮和亚甲基桥的空间位阻还可能导致其相对较差的MAO-B底物性能。

  DOI：

  10.1021/jm00122a031
• 作为产物：
  描述：

  cis-1,2,3,4,4a,9a-hexahydro-2-methyl-9H-indeno<2,1-c>pyridin-9-one 在 lithium aluminium tetrahydride 、 氯化亚砜 、 potassium tert-butylate 作用下， 以 乙醚 为溶剂， 反应 21.25h， 生成 2-methyl-2,3,4,9-tetrahydro-1H-indeno[2,1-c]pyridine
  参考文献：
  名称：

  黑纹状体毒素1-甲基-4-苯基-1,2,3,6-四氢吡啶的半刚性三环类似物的研究。

  摘要：

  N-甲基色胺和甲醛的缩合反应生成的四氢-β-咔啉是一种1-甲基-4-苯基-1,2,3,6-四氢吡啶（MPTP）tha的半刚性三环类似物。在单胺氧化酶B（MAO-B）催化的反应中，正常实验大鼠以约0.5％的MPTP速率生物转化为相应的二氢化合物。其中与氮原子的双键β，γ保持烯丙基特性的相应的四氢茚并吡啶是稍好的MAO-B底物。从这些类型的三环结构衍生的所提出的以碳为中心的自由基中间体中，除了存在环应变外，氮和亚甲基桥的空间位阻还可能导致其相对较差的MAO-B底物性能。

  DOI：

  10.1021/jm00122a031

文献信息

• Therapeutic agent for intestinal diseases and visceral pain
  申请人：Tokumasu Munetaka

  公开号：US20090270455A1

  公开（公告）日：2009-10-29

  The present invention relates to a therapeutic agent for irritable bowel syndrome of diarrhea type, ulcerative colitis, visceral pain or abdominal pain, which contains a compound of the following formula and which has 5-HT7 receptor antagonistic effect or an analogue thereof; and this therapeutic agent has an excellent therapeutic effect and a high safety:

  本发明涉及一种治疗腹泻型肠易激综合症、溃疡性结肠炎、内脏疼痛或腹痛的治疗剂，该治疗剂包含以下公式的化合物或其类似物，具有5-HT7受体拮抗作用；该治疗剂具有优异的治疗效果和高安全性：
• IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
  申请人：Trabanco-Suarez Andres Avelino

  公开号：US20110009441A1

  公开（公告）日：2011-01-13

  The present invention relates to novel compounds, in particular novel imidazo[1,2-a]piridine derivatives according to Formula (I). The compounds according to the invention are positive allosteric modulators of metabotropic receptors-sub-type 2 (‘mGluR2’) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新型化合物，特别是公式（I）中的新型咪唑并[1,2-a]吡啶衍生物。本发明的化合物是代谢型受体亚型2（“mGluR2”）的阳性变构调节剂，可用于治疗或预防与谷氨酸功能障碍有关的神经和精神障碍以及涉及代谢型受体亚型mGluR2的疾病。特别是，这些疾病是来自焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统疾病的群体。本发明还涉及制备这些化合物和组合物的制药组合物和制备过程，以及将这些化合物用于预防和治疗涉及mGluR2的这些疾病的用途。
• HAHNE H.; ZYMALKOWSKI F., ARCH. PHARM., 1979, 312, NO 6, 472-477
  作者：HAHNE H.、 ZYMALKOWSKI F.

  DOI：——

  日期：——
• HYPERGLYCOSYLATED POLYPEPTIDE VARIANTS AND METHODS OF USE
  申请人：BLATT LAWRENCE M.

  公开号：US20110008289A1

  公开（公告）日：2011-01-13

  The present invention provides synthetic Type I interferon receptor polypeptide agonists comprising consensus or hybrid Type I interferon receptor polypeptide agonists, containing one or more native or non-native glycosylation sites. The present invention provides synthetic Type I interferon receptor polypeptide agonists comprising consensus or hybrid Type I interferon receptor polypeptide agonists, containing one or more native or non-native glycosylation sites, as well as erythropoietin and darbepoetin alfa, each of which are linked to a penetrating peptide that facilitates translocation of a substance across a biological barrier as well as pharmaceutical compositions, including oral formulations, of the same. The present invention further provides oral formulations of hyperglycosylated or protease-resistant, hyperglycosylated polypeptide variants, which polypeptide variants lack at least one protease cleavage site found in a parent polypeptide, and thus exhibit increased protease resistance compared to the parent polypeptide, which polypeptide variants further include (1) a carbohydrate moiety covalently linked to at least one non-native glycosylation site not found in the parent protein therapeutic or (2) a carbohydrate moiety covalently linked to at least one native glycosylation site found but not glycosylated in the parent protein therapeutic. The present invention further provides compositions, including oral pharmaceutical compositions, comprising the synthetic Type I interferon receptor polypeptide agonist, the hyperglycosylated polypeptide variant, or the hyperglycosylated, protease-resistant polypeptide variant. The present invention further provides containers, devices, and kits comprising the synthetic Type I interferon receptor polypeptide agonist, the hyperglycosylated polypeptide variant, or the hyperglycosylated, protease-resistant polypeptide variant. The present invention further provides therapeutic methods involving administering an effective amount of an oral pharmaceutical composition comprising a synthetic Type I interferon receptor polypeptide agonist, a hyperglycosylated polypeptide variant, or a hyperglycosylated, protease-resistant polypeptide variant to an individual in need thereof.
• US8785486B2
  申请人：——

  公开号：US8785486B2

  公开（公告）日：2014-07-22