2-甲基-2-丙基(3S)-3-(叠氮基甲基)-1-哌啶羧酸酯 | 140645-22-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 2-甲基-2-丙基(3S)-3-(叠氮基甲基)-1-哌啶羧酸酯
• 中文别名: II3,3'-(1,2-环己二基二次氮基&lt三价氮基&gt)-二(2-甲基丙烷-2-硫醇酸根)锌
• 英文名称: (3S)-3-azidomethyl-1-(tert-butoxycarbonyl)-piperidine
• 英文别名: (S)-3-(az-domethyl)piperidine-1-carboxylic acid tert-butyl ester；(S)-tert-butyl 3-(azidomethyl)piperidine-1-carboxylate；t-butyl (S)-3-azidomethyl-1-piperidinecarboxylate；tert-butyl (3S)-3-(azidomethyl)piperidine-1-carboxylate
• CAS: 140645-22-3
• 化学式: C₁₁H₂₀N₄O₂
• 分子量: 240.305
• InChiKey: BAEVCCYGRQSYIU-SECBINFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  17
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.91
• 拓扑面积：
  43.9
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-甲基-2-丙基(3S)-3-(叠氮基甲基)-1-哌啶羧酸酯 在 钯 氢气 作用下， 以 甲醇 为溶剂， 反应 9.0h， 生成 (R)-1-Boc-3-氨甲基哌啶
  参考文献：
  名称：

  NOVEL TRIAZOLOPYRAZINE DERIVATIVE AND USE THEREOF

  摘要：

  本发明涉及一种新型的三唑并吡嗪衍生物或其药学上可接受的盐，以及包含其作为活性成分的制备用于预防或治疗高增殖障碍的药物组合物。本发明可以作为治疗与异常激酶活性引起的过度细胞增殖和生长相关的各种高增殖障碍的治疗剂，如癌症、银屑病、类风湿性关节炎和糖尿病视网膜病变，通过有效抑制c-Met酪氨酸激酶活性。

  公开号：

  US20150259350A1
• 作为产物：
  描述：

  (S)-3-哌啶甲酸乙酯 在 4-二甲氨基吡啶 、 lithium aluminium tetrahydride 、 sodium azide 、 三乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 13.0h， 生成 2-甲基-2-丙基(3S)-3-(叠氮基甲基)-1-哌啶羧酸酯
  参考文献：
  名称：

  신규한 트리아졸로 피라진 유도체 및 그의 용도

  摘要：

  该专利涉及一种新型的三唑基吡啶衍生物或其药学上可接受的盐，以及包含它们作为有效成分的用于抑制c-Met酪氨酸激酶活性的药学组合物，以及用于预防或治疗过度增殖性疾病（过度增殖性疾病）的药学组合物。该发明通过有效地抑制c-Met酪氨酸激酶的活性，可以有效地用于治疗与异常激酶活性导致的过度细胞增殖和生长有关的各种过度增殖性疾病，例如癌症、银屑病、类风湿关节炎、糖尿病性视网膜病变等。

  公开号：

  KR101745741B1

文献信息

• [EN] INDOLE DERIVATIVES AND USES THEREOF FOR TREATING A CANCER<br/>[FR] DÉRIVÉS D'INDOLE ET LEURS UTILISATIONS POUR LE TRAITEMENT D'UN CANCER
  申请人：UNIV CLAUDE BERNARD LYON

  公开号：WO2022008475A1

  公开（公告）日：2022-01-13

  The present invention relates to indole derivatives of formula (I') as CK2 inhibitor and pharmaceutical compositions comprising the same. The present invention further relates to the use of such compounds of formula (I) for use for preventing and/or treating a cancer.

  本发明涉及一种具有如下式（I'）的吲哚衍生物作为CK2抑制剂，以及包含该衍生物的药物组合物。本发明还涉及利用该式（I）化合物用于预防和/或治疗癌症的用途。
• Novel amide derivatives
  申请人：——

  公开号：US20040204369A1

  公开（公告）日：2004-10-14

  This invention relates to compounds which are represented by the general formula [I] 1 [in which A stands for a group of the following formula [a o ] or [b o ] 2 Ar 1 , Ar 2 and Ar 3 stand for optionally substituted phenyl; k stands for 0 or 1; m, n and s stand for 0, 1 or 2; R 1 stands for hydrogen or optionally substituted lower alkyl; R 2 , R 3 , R 4 and R 5 either stand for hydrogen or optionally substituted lower alkyl, or R 2 and R 3 , or R 4 and R 5 together stand for trimethylene and the like; R 60 stands for hydrogen, alkyl, or the like; R 61 and R 71 either stand for alkyl and the like, or together stand for trimethylene and the like; X stands for carbonyl or methylene; Y stands for nitrogen or methine; and Q − stands for anion], and the like. The compounds of the invention exhibit selective antagonism to muscarinic M 3 receptors, and therefore are useful as safe and effective agents showing little side effect, for treating diseases of the respiratory, urinary and digestive systems.

  本发明涉及由一般公式[I]1表示的化合物，其中A代表以下式[ao]或[bo]2Ar1的基团，Ar2和Ar3代表可选取代的苯基；k代表0或1；m、n和s代表0、1或2；R1代表氢或可选取代的低碳基；R2、R3、R4和R5要么代表氢或可选取代的低碳基，要么R2和R3，或者R4和R5一起代表三亚甲基等；R60代表氢、烷基或类似物；R61和R71要么代表烷基等，要么一起代表三亚甲基等；X代表羰基或亚甲基；Y代表氮或亚甲基；Q^-代表阴离子等。本发明的化合物表现出选择性的M3胆碱能受体拮抗作用，因此可用作治疗呼吸、泌尿和消化系统疾病的安全有效药物，副作用小。
• Amide derivatives
  申请人：Banyu Pharmaceutical Co., Ltd.

  公开号：US06809108B1

  公开（公告）日：2004-10-26

  This invention relates to compounds which are represented by the general formula [I] [in which A stands for a group of the following formula [a0] or [b0] Ar1, Ar2 and Ar3 stand for optionally substituted phenyl; k stands for 0 or 1; m, n and a stand for 0, 1 or 2; R1 stands for hydrogen or optionally substituted lower alkyl; R2, R3, R4 and R5 either stand for hydrogen or optionally substituted lower alkyl, or R2 and R3, or R4 and R5 together stand for trimethylene and the like; R60 stands for hydrogen, alkyl, or the like; R61 and R71 either stand for alkyl and the like, or together stand for trimethylene and the like; X stands for carbonyl or methylene; Y stands for nitrogen or methine; and Q− stands for anion], and the like. The compounds of the invention exhibit selective antagonism to muscarinic M3 receptors, and therefore are useful as safe and effective agents showing little side effect, for treating diseases of the respiratory, urinary and digestive systems.

  本发明涉及化合物，其由一般式[I]表示，其中A代表以下式[a0]或[b0]的基团，Ar1、Ar2和Ar3代表可选取代的苯基；k代表0或1；m、n和a代表0、1或2；R1代表氢或可选取代的低碳基；R2、R3、R4和R5要么代表氢或可选取代的低碳基，要么R2和R3，或R4和R5一起代表三亚甲基等；R60代表氢、烷基或类似物；R61和R71要么代表烷基等，要么一起代表三亚甲基等；X代表羰基或亚甲基；Y代表氮或甲烷基；Q−代表阴离子等。本发明的化合物表现出对肌动蛋白M3受体的选择性拮抗作用，因此可用作治疗呼吸、泌尿和消化系统疾病的安全有效药物，副作用小。
• Triazolopyrazine derivative and use thereof
  申请人：KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

  公开号：US09403831B2

  公开（公告）日：2016-08-02

  The present invention relates to a novel triazolopyrazine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as an active ingredient for preventing or treating hyper proliferative disorder. The present invention can be useful as a therapeutic agent for various hyper proliferative disorders associated with excessive cell proliferation and growth caused by abnormal kinase activity, such as cancer, psoriasis, rheumatoid arthritis, and diabetic retinopathy, by efficiently inhibiting c-Met tyrosine kinase activity.

  本发明涉及一种新型的三唑并吡嗪衍生物或其药学上可接受的盐，以及一种含有其作为活性成分的药物组合物，用于预防或治疗过度增殖性疾病。本发明可作为治疗各种与异常激酶活性引起的细胞增殖和生长过度有关的过度增殖性疾病的治疗剂，例如癌症、银屑病、类风湿性关节炎和糖尿病视网膜病变，通过有效抑制c-Met酪氨酸激酶活性。
• Design and Synthesis of Potent and Highly Selective Thrombin Inhibitors
  作者：Kurt Hilpert、Jean Ackermann、David W. Banner、Alain Gast、Klaus Gubernator、Paul Hadvary、Ludvik Labler、Klaus Mueller、Gerard Schmid、Thomas B. Tschopp、Han van de Waterbeemd

  DOI：10.1021/jm00049a008

  日期：1994.11.1

  Thrombin, a serine protease, plays a central role in the initiation and propagation of thrombotic events. An extensive search for new thrombin inhibitors was performed, using an unconventional approach. Screening of small basic molecules for binding in the recognition pocket of thrombin led to the discovery of (aminoiminomethyl)piperidine (amidinopiperidine) as a weak, but intrinsically selective, thrombin inhibitor. Elaboration of this molecule provided compounds which inhibit thrombin with K-i's in the range of 20-50 nM and with selectivities of 1000-4000 against trypsin. These inhibitor compounds show a new and unexpected, binding mode to thrombin. Modification of the central building block and then of one of the hydrophobic substituents led to the discovery of a new family of thrombin inhibitors which has reverted td the former binding mode to thrombin. This last class of compounds shows inhibitory activities in the picomolar range; low toxicity; and a short plasma half life which favors its use for an intravenous application. From this series of thrombin;inhibitors, 19f (Ro 46-6240) was selected for clinical development as an antithrombotic agent for intravenous administration.