2-ethyl-N-methylcyclohexan-1-amine | 252854-42-5

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 2-ethyl-N-methylcyclohexan-1-amine
• CAS: 252854-42-5
• 化学式: C₉H₁₉N
• 分子量: 141.257
• InChiKey: JXVOCMMENPUMMV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  12
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  2-ethyl-N-methylcyclohexan-1-amine 、 4-氯吡咯并嘧啶 在 N,N-二异丙基乙胺 作用下， 以 四氢呋喃 、 叔丁醇 为溶剂， 生成 N-(2-Isopropyl-5-methylcyclohexyl)-N-methyl-7H-pyrrolo[2,3-d]-pyrimidin-4-amin
  参考文献：
  名称：

  Discovery of CP-690,550: A Potent and Selective Janus Kinase (JAK) Inhibitor for the Treatment of Autoimmune Diseases and Organ Transplant Rejection

  摘要：

  There is a critical need for safer and more convenient treatments for organ transplant rejection and autoimmune disorders such as rheumatoid arthritis. Janus tyrosine kinases (JAK1, JAK3) are expressed in lymphoid cells and are involved in the signaling of multiple cytokines important for various T cell functions. Blockade of the JAK1/JAK3-STAT pathway with a small molecule was anticipated to provide therapeutic immunosuppression/immunomodulation. The Pfizer compound library was screened against the catalytic domain of JAK3 resulting in the identification of a pyrrolopyrimidine-based series of inhibitors represented by CP-352,664 (2a). Synthetic analogues of 2a were screened against the JAK enzymes and evaluated in an IL-2 induced T cell blast proliferation assay. Select compounds were evaluated in rodent efficacy models of allograft rejection and destructive inflammatory arthritis. Optimization within this chemical series led to identification of CP-690,550 1, a potential first-in-class JAK inhibitor for treatment of autoimmune diseases and organ transplant rejection.

  DOI：

  10.1021/jm1004286
• 作为产物：
  描述：

  2-乙基环己酮 、 甲胺 在 溶剂黄146 作用下， 以 甲醇 、 1,2-二氯乙烷 为溶剂， 反应 18.0h， 生成 2-ethyl-N-methylcyclohexan-1-amine
  参考文献：
  名称：

  Discovery of CP-690,550: A Potent and Selective Janus Kinase (JAK) Inhibitor for the Treatment of Autoimmune Diseases and Organ Transplant Rejection

  摘要：

  There is a critical need for safer and more convenient treatments for organ transplant rejection and autoimmune disorders such as rheumatoid arthritis. Janus tyrosine kinases (JAK1, JAK3) are expressed in lymphoid cells and are involved in the signaling of multiple cytokines important for various T cell functions. Blockade of the JAK1/JAK3-STAT pathway with a small molecule was anticipated to provide therapeutic immunosuppression/immunomodulation. The Pfizer compound library was screened against the catalytic domain of JAK3 resulting in the identification of a pyrrolopyrimidine-based series of inhibitors represented by CP-352,664 (2a). Synthetic analogues of 2a were screened against the JAK enzymes and evaluated in an IL-2 induced T cell blast proliferation assay. Select compounds were evaluated in rodent efficacy models of allograft rejection and destructive inflammatory arthritis. Optimization within this chemical series led to identification of CP-690,550 1, a potential first-in-class JAK inhibitor for treatment of autoimmune diseases and organ transplant rejection.

  DOI：

  10.1021/jm1004286

文献信息

• [EN] CELLULAR SIGNALLING INHIBITORS, THEIR FORMULATIONS AND METHODS THEREOF<br/>[FR] INHIBITEURS DE SIGNALISATION CELLULAIRE, LEURS FORMULES ET LEURS PROCÉDÉS
  申请人：INVICTUS ONCOLOGY PVT LTD

  公开号：WO2017137958A1

  公开（公告）日：2017-08-17

  The present disclosure relates generally to Cellular Signalling inhibitors of compound of Formula (I), compositions and formulations comprising the same, methods, processes, and uses thereof. In particular, the present disclosure provides CSF-1R inhibitors demonstrating sustained inhibition of CSF/CSF1R signalling pathway with decreased toxicity. The present disclosure also provides supramolecular combinatorial therapeutics, wherein a CSF-1R inhibitor is combined with one or more of a chemotherapeutic agent, a kinase inhibitor, and an immunoregulator, each of which is optionally conjugated with a lipid. The present disclosure also provides a method for treating cancer, allergy, Systemic lupus erythematosus, nephritis, Chronic Obstructive Pulmonary Disease, and abnormal macrophage functions or any combinations thereof.

  本公开涉及一般细胞信号传导抑制剂，涉及式(I)的化合物、包含该化合物的组合物和制剂、以及它们的方法、过程和使用。特别是，本公开提供了CSF-1R抑制剂，它们表现出对CSF/CSF1R信号通路的持续抑制，并且毒性降低。本公开还提供了超分子组合疗法，其中CSF-1R抑制剂与一个或多个化疗剂、激酶抑制剂和免疫调节剂结合，其中每个可选地与脂质偶联。本公开还提供了一种治疗癌症、过敏、系统性红斑狼疮、肾炎、慢性阻塞性肺病和异常巨噬细胞功能或其任何组合的方法。
• CONTROLLED RELEASE PREPARATION
  申请人：Akiyama Yohko

  公开号：US20100285120A1

  公开（公告）日：2010-11-11

  A controlled release preparation wherein the release of active ingredient is controlled, which releases an active ingredient for an extended period of time by staying or slowly migrating in the gastrointestinal tract, is provided by means such as capsulating a tablet, granule or fine granule wherein the release of active ingredient is controlled and a gel-forming polymer. Said tablet, granule or fine granule has a release-controlled coating-layer formed on a core particle containing an active ingredient.

  提供了一种控制释放制剂，其中活性成分的释放受控制，通过将其包裹在一个控制释放的涂层中，使其在胃肠道内停留或缓慢迁移，从而延长活性成分的释放时间。该制剂可以通过将活性成分包裹在一个控制释放的涂层中，并添加一种凝胶形成聚合物，制成胶囊、颗粒或细颗粒。所述胶囊、颗粒或细颗粒具有一个包含活性成分的核心颗粒，并在其上形成一个控制释放的涂层层。
• COMPOUNDS FOR USE IN TREATING ACUTE CORONARY SYNDROME AND RELATED CONDITIONS
  申请人：Vitae Pharmaceuticals, Inc.

  公开号：US20170231992A1

  公开（公告）日：2017-08-17

  Provided herein are compounds and pharmaceutically acceptable salts thereof that are useful therapeutics for acute coronary syndrome and related disorders.
• COMPOUNDS FOR THE TREATMENT OF PARAMYXOVIRUS VIRAL INFECTIONS
  申请人：Alios BioPharma, Inc.

  公开号：US20170283429A1

  公开（公告）日：2017-10-05

  Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
• INDAZOLE COMPOUNDS AS FGFR KINASE INHIBITOR, PREPARATION AND USE THEREOF
  申请人：Shanghai Haihe Pharmaceutical Co., Ltd.

  公开号：US20170275291A1

  公开（公告）日：2017-09-28

  The present invention provides an indazole compound as a FGFR kinase inhibitor, preparation and use thereof. Specifically, the present invention provides a compound represented by formula (I), wherein the definitions of each group are described in the specification. The compound of the present invention has good FGFR kinase-inhibiting activity, and can be used in preparing a series of medicines for treating FGFR kinase activity related diseases.