(6-吡咯烷-1-基吡啶-2-基)甲胺 | 868755-49-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: (6-吡咯烷-1-基吡啶-2-基)甲胺
• 英文名称: (6-(pyrrolidin-1-yl)pyridin-2-yl)methanamine
• 英文别名: (6-Pyrrolidin-1-ylpyrid-2-yl)methylamine；(6-pyrrolidin-1-ylpyridin-2-yl)methanamine
• CAS: 868755-49-1
• 化学式: C₁₀H₁₅N₃
• 分子量: 177.249
• InChiKey: HBEJFAYJKXYWKS-UHFFFAOYSA-N

物化性质

• 沸点：
  130-135/0.2mm
• 密度：
  1.127±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  42.2
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 危险品标志：
  C
• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  (6-吡咯烷-1-基吡啶-2-基)甲胺 、 6-溴-4-氯-1(2H)-酞嗪酮 在 tris-(dibenzylideneacetone)dipalladium(0) 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 sodium t-butanolate 作用下， 以 异丁酰胺 为溶剂， 反应 1.5h， 生成 4-chloro-6-[(6-pyrrolidin-1-yl-pyridin-2-ylmethyl)-amino]-2H-phthalazin-1-one
  参考文献：
  名称：

  WO2008/61108

  摘要：

  公开号：
• 作为产物：
  描述：

  6-(吡咯烷-1-基)吡啶-2-甲醛 在 吡啶 、 盐酸羟胺 、 溶剂黄146 、 锌 作用下， 以 乙醇 为溶剂， 反应 4.0h， 生成 (6-吡咯烷-1-基吡啶-2-基)甲胺
  参考文献：
  名称：

  [EN] PYRROLIDINO HETEROCYCLES
  [FR] HÉTÉROCYCLES PYRROLIDINO

  摘要：

  这项发明涉及公式I的化合物，其中A1、A2、A3、B、R1、R2、R3和R4如描述和索赔中所定义，并且其生理上可接受的盐。这些化合物抑制PDE10A，可用作药物。

  公开号：

  WO2013178569A1

文献信息

• [EN] PYRROLIDINO HETEROCYCLES<br/>[FR] HÉTÉROCYCLES PYRROLIDINO
  申请人：HOFFMANN LA ROCHE

  公开号：WO2013178569A1

  公开（公告）日：2013-12-05

  The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.

  这项发明涉及公式I的化合物，其中A1、A2、A3、B、R1、R2、R3和R4如描述和索赔中所定义，并且其生理上可接受的盐。这些化合物抑制PDE10A，可用作药物。
• COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
  申请人：Ibrahim Prabha N.

  公开号：US20090286782A1

  公开（公告）日：2009-11-19

  Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one of Fms protein kinase or Kit protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinases and/or Kit protein kinases, including rheumatoid arthritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, myelopreparation for autologous transplantation, transplant rejection, nephritis, nephropathy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastomas, neurofibromatosis, osteolytic bone metastases, and giant cell tumors.

  描述了化合物及其盐，配方，共轭物，衍生物，形式和用途。在某些方面和实施例中，所述的化合物或其盐，配方，共轭物，衍生物，形式对Fms蛋白激酶或Kit蛋白激酶至少有一种活性。还描述了使用这些方法来治疗疾病和症状，包括与Fms蛋白激酶和/或Kit蛋白激酶活性相关的疾病和症状，包括类风湿关节炎，骨关节炎，骨质疏松症，周围假体周围骨溶解，系统性硬化症，脱髓鞘疾病，多发性硬化症，沙科特-玛丽-屈特综合症，肌萎缩侧索硬化症，阿尔茨海默病，帕金森病，溃疡性结肠炎，克罗恩病，免疫性血小板减少性紫癜，自体移植的骨髓准备，移植排斥反应，肾炎，肾病，I型糖尿病，急性疼痛，炎症性疼痛，神经病性疼痛，乳腺癌，前列腺癌，胰腺癌，肺癌，卵巢癌，神经胶质瘤，胶质母细胞瘤，神经纤维瘤病，骨转移性溶骨病和巨细胞瘤。
• PHTHALAZINE DERIVATIVES
  申请人：Araldi Gian-Luca

  公开号：US20080146547A1

  公开（公告）日：2008-06-19

  The present invention relates to novel phthalazine derivatives and, more particularly, to phthalazine derivatives that are useful as protein kinase inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and methods of treatment using the compounds.

  本发明涉及新的邻苯二酸嗪衍生物，更具体地，涉及可用作蛋白激酶抑制剂的邻苯二酸嗪衍生物。本发明还涉及制备这些化合物的方法，含有这些化合物的组合物，以及使用这些化合物的治疗方法。
• ARYL SUBSTITUTED CARBOXAMIDE DERIVATIVES AS CALCIUM OR SODIUM CHANNEL BLOCKERS
  申请人：Inoue Tadashi

  公开号：US20120101105A1

  公开（公告）日：2012-04-26

  The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Na v1.3 and Na v1.7 , and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.

  本发明涉及公式(I)或其药学上可接受的盐的芳基取代羧酰胺衍生物，其具有T型钙通道或电压门控钠通道的阻滞活性，如Nav1.3和Nav1.7等Tetrodotoxin敏感(TTX-S)阻滞剂，并且在涉及T型钙通道或电压门控钠通道的疾病或疾病的治疗或预防中有用。本发明还涉及包含这些化合物的制药组合物以及在涉及T型钙通道或电压门控钠通道的疾病或疾病的预防或治疗中使用这些化合物和组合物的用途。
• CANNABINOID RECEPTOR MODULATORS
  申请人：Jones Robert M.

  公开号：US20120214766A1

  公开（公告）日：2012-08-23

  The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.

  本发明涉及公式Ia的某些化合物及其制药组合物，其调节大麻素CB2受体的活性。本发明还涉及公式Ia的某些化合物及其制药组合物，其调节CB1受体和CB2受体的活性。本发明的化合物和制药组合物适用于治疗以下疾病的方法：疼痛，例如骨骼和关节疼痛，肌肉疼痛，牙痛，偏头痛和其他头痛，炎性疼痛，神经痛，由治疗副作用引起的疼痛和与骨关节炎相关的疼痛；过敏症；炎性过敏症；神经病性过敏症；急性疼痛感受；骨质疏松症；多发性硬化症相关痉挛；自身免疫疾病；过敏反应；中枢神经系统炎症；动脉粥样硬化；不良的免疫细胞活动和炎症；年龄相关的黄斑变性；咳嗽；白血病；淋巴瘤；中枢神经系统肿瘤；前列腺癌；阿尔茨海默病；中风引起的损伤；痴呆症；肌萎缩性侧索硬化症和帕金森病。