4-Methylidene-1-propan-2-ylpiperidine | 135522-04-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 4-Methylidene-1-propan-2-ylpiperidine
• CAS: 135522-04-2
• 化学式: C₉H₁₇N
• 分子量: 139.241
• InChiKey: FAMIXDVXNZZMRF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.78
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  聚合甲醛 、 3-三甲基硅基-2-三甲基硅基甲基丙烯 、 异丙胺 在 三氟乙酸 作用下， 以 乙腈 为溶剂， 反应 2.0h， 以67%的产率得到4-Methylidene-1-propan-2-ylpiperidine
  参考文献：
  名称：

  Le 2-trimethylsilylmethyl allyltrimethylsilane, precurseur de carbocycles et heterocycles a groupe methylenique

  摘要：

  2-Trimethylsilylmethyl allyltrimethylsilane, easily prepared from isobutene, allows a convenient one-pot synthesis of functional methylene cycloalcanes from bis-acetals and of 4-methylene N-alkyl piperidines from primary amines and polyoxymethylene.

  DOI：

  10.1016/s0040-4020(01)86438-3

文献信息

• NOVEL TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
  申请人：Kim Myung-Hwa

  公开号：US20110218193A1

  公开（公告）日：2011-09-08

  The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases.

  本发明涉及一种新型三环衍生物，具有高效的抑制聚(ADP-核糖)聚合酶（PARP）或其药用可接受盐的活性，以及其制备方法和含有该衍生物的药物组合物。本发明的三环衍生物通过抑制聚(ADP-核糖)聚合酶的活性，对于预防或治疗由过度PARP活性引起的疾病特别有效，包括神经病痛、神经退行性疾病、心血管疾病、糖尿病肾病、炎症性疾病、骨质疏松症和癌症。
• NOVEL AZABICYCLOHEXANES
  申请人：Jain Rajseh

  公开号：US20120165320A1

  公开（公告）日：2012-06-28

  The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.

  本发明涉及公式I的新化合物，其药学上可接受的衍生物，互变异构体，立体异构体包括R和S异构体，多晶型，前药，代谢物，盐或溶剂的形式。该发明还涉及用于合成公式I的新化合物，其药学上可接受的衍生物，互变异构体，立体异构体，多晶型，前药，代谢物，盐或溶剂的过程。
• Cannabinoid receptor ligands and uses thereof
  申请人：Pfizer Inc

  公开号：US20040214855A1

  公开（公告）日：2004-10-28

  Compounds of Formula (I) and (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein. 1

  本文描述了作为大麻素受体配体的化合物(I)和(II)的公式，以及它们在治疗与动物大麻素受体介导相关疾病中的用途。
• COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
  申请人：Charrier Jean-Damien

  公开号：US20120040020A1

  公开（公告）日：2012-02-16

  The present disclosure relates to pyrazine compounds of formula I: wherein L, n, R 1 , and R 2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.

  本公开涉及式I的吡嗪化合物：其中L、n、R1和R2如规范所述。这些化合物可用作ATR蛋白激酶的抑制剂。本公开还涉及包含本公开化合物的药学上可接受的组合物；使用本公开化合物治疗各种疾病、障碍和病况的方法；制备本公开化合物的过程；制备本公开化合物的中间体；以及在体外应用中使用这些化合物的方法，例如研究生物和病理现象中的激酶、这些激酶介导的细胞内信号传导途径的研究以及新的激酶抑制剂的比较评估。
• ACETIC ACID AMIDE DERIVATIVE HAVING INHIBITORY ACTIVITY ON ENDOTHELIAL LIPASE
  申请人：Masuda Koji

  公开号：US20110251386A1

  公开（公告）日：2011-10-13

  Disclosed is a compound which is useful as an endothelial lipase inhibitor. A pharmaceutical composition having inhibitory activity on endothelial lipase comprising a compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein Ring A is nitrogen-containing hetero ring, Ring A may be substituted with a substituent other than a group represented by the formula: —C(R 1 R 2 )—C(═O)—NR 3 R 4 and a group represented by the formula: —R 5 , a broken line represents the presence or the absence of a bond, Z is —NR 6 —, ═N—, —O—, or —S—, R 6 is halogen, substituted or unsubstituted alkyl or the like, R 1 and R 2 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy or substituted or unsubstituted alkyl, R 3 is hydrogen or substituted or unsubstituted alkyl, R 4 is hydrogen, substituted or unsubstituted alkyl or the like, R 3 and R 4 taken together with the adjacent nitrogen atom to which they are attached may form a substituted or unsubstituted ring, R 5 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or the like.

  公开了一种作为内皮酯酶抑制剂有用的化合物。一种具有内皮酯酶抑制活性的药物组合物，包括下式所示的化合物：其药学上可接受的盐或其溶剂合物，其中，环A是含氮杂环，环A可以被除了由下式表示的基团：—C(R1R2)—C(═O)—NR3R4和由下式表示的基团：—R5以外的基团取代，其中，一条虚线表示键的存在或不存在，Z为—NR6—，═N—，—O—或—S—，R6为卤素，取代或未取代的烷基或类似物，R1和R2各自独立地为氢、卤素、羟基、氰基、硝基、羧基或取代或未取代的烷基，R3为氢或取代或未取代的烷基，R4为氢、取代或未取代的烷基或类似物，R3和R4与它们所连接的相邻氮原子一起可以形成取代或未取代的环，R5为氢、卤素、羟基、氰基、硝基、羧基、取代或未取代的烷基、取代或未取代的烯基、取代或未取代的炔基或类似物。