((S)-piperidin-2-yl)methanone | 1046140-29-7

• 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: ((S)-piperidin-2-yl)methanone
• 英文别名: (2S)-piperidine-2-carbaldehyde
• CAS: 1046140-29-7
• 化学式: C₆H₁₁NO
• 分子量: 113.159
• InChiKey: XHLCYFVJQKWNRH-LURJTMIESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  8
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  ((S)-piperidin-2-yl)methanone 、 N-[2-Amino-5-[(diethylamino)carbonyl]phenyl]-4-ethoxy-benzeneacetamide 在 borane pyridine complex 作用下， 以 DCE 、 溶剂黄146 为溶剂， 反应 1.0h， 生成
  参考文献：
  名称：

  Novel benzimidazole derivatives as selective CB2 agonists

  摘要：

  The preparation and evaluation of a novel class of CB2 agonists based on a benzimidazole moiety are reported. They showed binding affinities up to 1 nM towards the CB2 receptor with partial to full agonist potencies. They also demonstrated good to excellent selectivity (> 1000-fold) over the CB1 receptor. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.05.073

文献信息

• Thio-containing inhibitors of aminopeptidase P, compositions thereof and method of use
  申请人：Simmons H. William

  公开号：US20070060525A1

  公开（公告）日：2007-03-15

  The present invention is directed to an α thio-containing compound that is capable of inhibiting the enzyme, membrane aminopeptidase P (mAPP or APP), whose natural substrate is bradykinin. The compound is useful as a pharmaceutical agent because by inhibiting bradykinin degradation, the compound allows bradykinin to exert its beneficial effects on the cardiovascular system, to improve renal function, and to improve glucose tolerance and insulin-sensitivity. The present invention is also directed to a pharmaceutical composition comprising the mAPP inhibitor of the present invention and a pharmaceutically acceptable carrier. In another aspect, the present invention is directed to a method of inhibiting bradykinin degradation in a mammalian patient, preferably human, in need of treatment comprising administering to the patient a therapeutically effective amount of an α thio-containing compound of the present invention. The method of the present invention also contemplates the further step of administering to the mammalian patient in need of treatment a therapeutically effective amount of an inhibitor of angiotensin converting enzyme (ACE).

  本发明涉及一种含α硫基的化合物，能够抑制酶、膜氨肽酶P（mAPP或APP），其天然底物为激肽。该化合物可用作药物代理，因为通过抑制激肽降解，使激肽能够在心血管系统上发挥其有益作用，改善肾功能，并改善葡萄糖耐量和胰岛素敏感性。本发明还涉及一种含有本发明mAPP抑制剂和药用可接受载体的药物组合物。另一方面，本发明涉及一种在需要治疗的哺乳动物患者，优选为人类，中抑制激肽降解的方法，包括向患者投予本发明的α硫基化合物的治疗有效量。本发明的方法还包括向需要治疗的哺乳动物患者投予抑制肾素转化酶（ACE）的治疗有效量的进一步步骤。
• Protease inhibitors
  申请人：——

  公开号：US20040157828A1

  公开（公告）日：2004-08-12

  The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

  本发明提供了4-氨基-氮杂辛酮类蛋白酶抑制剂及其药学上可接受的盐、水合物和溶剂化物，其可以抑制蛋白酶，包括卡他蛋白K，以及这些化合物的制药组合物、这些化合物的新中间体和治疗过度骨质流失或软骨或基质降解疾病的方法，包括骨质疏松症；牙龈疾病，包括牙龈炎和牙周炎；关节炎，更具体地说是骨关节炎和类风湿性关节炎；帕吉特病；恶性高钙血症；以及代谢性骨病，通过向需要治疗的患者给予本发明化合物来抑制骨质流失或过度软骨或基质降解。
• In vivo incorporation of unnatural amino acids
  申请人：Schultz Peter

  公开号：US20080227152A1

  公开（公告）日：2008-09-18

  The invention provides methods and compositions for in vivo incorporation of unnatural amino acids. Also provided are compositions including proteins with unnatural amino acids.

  本发明提供了体内合成非天然氨基酸的方法和组合物。还提供了包含非天然氨基酸蛋白质的组合物。
• IN Vivo Incorporation of Unnatural Amino Acids
  申请人：SCHULTZ PETER G.

  公开号：US20120202243A1

  公开（公告）日：2012-08-09

  The invention provides methods and compositions for in vivo incorporation of unnatural amino acids. Also provided are compositions including proteins with unnatural amino acids.

  该发明提供了体内合成非天然氨基酸的方法和组合物。还提供了含有非天然氨基酸蛋白质的组合物。
• MORPHINAN DERIVATIVE
  申请人：Nippon Chemiphar Co., Ltd.

  公开号：EP3498711A1

  公开（公告）日：2019-06-19

  A compound represented by the following general formula (I), wherein R1 represents hydrogen, C1-10 alkyl, cycloalkylalkyl where the cycloalkyl moiety has 3 to 6 carbon atoms and the alkylene moiety has 1 to 5 carbon atoms, or the like, R2 represents a 4- to 7-membered saturated heterocycle containing one or two heteroatoms which may be the same or different and are selected from N, O, and S, and two or more carbon atoms as ring-constituting atoms, the heterocycle may be substituted with a substituent such as an oxo group, R2 binds to Y via a carbon atom as a ring-constituting atom of R2, R3, R4, and R5, which are the same or different, represent hydrogen; hydroxy; or the like, R6a and R6b, which are the same or different, represent hydrogen or the like, R7 and R8, which are the same or different, represent hydrogen or the like, R9 and R10, which are the same or different, represent hydrogen or the like, X represents O or CH2, and Y represents C(= O) or the like), a tautomer of the compound, a stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an anxiolytic, an antidepressant, or the like.

  由以下通式 (I) 代表的化合物、 其中 R1 代表氢、C1-10 烷基、环烷基（其中环烷基有 3-6 个碳原子，亚烷基有 1-5 个碳原子）或类似物、 R2 代表含有一个或两个杂原子的 4 至 7 元饱和杂环，杂原子可以相同或不同，选自 N、O 和 S，以及两个或多个碳原子作为构环原子、 杂环可被氧代基等取代基取代、 R2 通过一个碳原子作为 R2 的构环原子与 Y 结合、 相同或不同的 R3、R4 和 R5 代表氢、羟基或类似物、 相同或不同的 R6a 和 R6b 代表氢或类似物、 相同或不同的 R7 和 R8 代表氢或类似物质、 相同或不同的 R9 和 R10 代表氢或类似物、 X 代表 O 或 CH2，以及 Y 代表 C(= O) 或类似物）、 该化合物的同分异构体、该化合物的立体异构体、其药学上可接受的盐或其溶解物可用作抗焦虑药、抗抑郁药或类似药物。