1,4,4-Trimethyl-1,4,5,6-tetrahydropyridin | 35079-50-6

• 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
• 英文名称: 1,4,4-Trimethyl-1,4,5,6-tetrahydropyridin
• 英文别名: 1,4,4-Trimethyl-1,2,3,4-tetrahydropyridine；1,4,4-trimethyl-2,3-dihydropyridine
• CAS: 35079-50-6
• 化学式: C₈H₁₅N
• 分子量: 125.214
• InChiKey: OBNANVWKTAVJEL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.75
• 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：

  1,4,4-Trimethylpiperidin 在 mercury(II) diacetate 、 溶剂黄146 作用下， 生成 1,4,4-Trimethyl-1,4,5,6-tetrahydropyridin
  参考文献：
  名称：

  Unsaturated Amines. X. The Mercuric Acetate Route to Substituted Piperidines, Δ²-Tetrahydropyridines and Δ²-Tetrahydroanabasines

  摘要：

  DOI：

  10.1021/ja01576a056

文献信息

• [EN] PROGRANULIN MODULATORS AND METHODS OF USING THE SAME<br/>[FR] MODULATEURS DE LA PROGRANULINE ET LEURS PROCÉDÉS D'UTILISATION
  申请人：ARKUDA THERAPEUTICS

  公开号：WO2021081272A1

  公开（公告）日：2021-04-29

  Provided herein are compounds of formula (I) that modulate progranulin and methods of using the compounds in progranulin- associated disorders, such as Frontotemperal lobe dementia (FTLD).

  本文提供了化合物的公式(I)，这些化合物可以调节前蛋白颗粒素，并且可以用于治疗与前蛋白颗粒素相关的疾病，如额颞叶痴呆症（FTLD）。
• [EN] A MEDICAMENT FOR TREATING MYCOBACTERIAL INFECTION CHARACTERIZED BY COMBINING A CYTOCHROME BC1 INHIBITOR WITH CLARITHROMYCIN OR AZITHROMYCIN<br/>[FR] MÉDICAMENT DESTINÉ AU TRAITEMENT D'UNE INFECTION MYCOBACTÉRIENNE, CARACTÉRISÉ PAR LA COMBINAISON D'UN INHIBITEUR DE CYTOCHROME BC1 AVEC DE LA CLARITHROMYCINE OU DE L'AZITHROMYCINE
  申请人：SHIONOGI & CO

  公开号：WO2022119899A1

  公开（公告）日：2022-06-09

  A medicament characterized in that (A) a compound represented by formula (I):, or its pharmaceutically acceptable salt, wherein R1, R2, R3and R4are each independently hydrogen atom, halogen, hydroxy, cyano, substituted or unsubstituted alkyl or the like; R5is a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like; R6, R7, R8and R9are each independently hydrogen atom, halogen or the like; X is CH or N; Y is CH or N; R10is each independently halogen, hydroxy, cyano, substituted or unsubstituted alkyl or the like; m is 0, 1, 2, 3 or 4; R11is halogen, hydroxy, cyano, substituted or unsubstituted alkyl or the like; R12is each independently halogen, hydroxy, cyano or the like; n is 0, 1, 2, 3 or 4; is combined with (B) clarithromycin or its pharmaceutically acceptable salt, or azithromycin or its pharmaceutically acceptable salt; and (C) clofazimine, or its pharmaceutically acceptable salt.

  一种药物，其特点在于(A)化合物由式(I)表示，或其药学上可接受的盐，其中R1、R2、R3和R4分别独立地为氢原子，卤素，羟基，氰基，取代或未取代的烷基或类似物；R5为氢原子，卤素，氰基，取代或未取代的烷基或类似物；R6、R7、R8和R9分别独立地为氢原子，卤素或类似物；X为CH或N；Y为CH或N；R10分别独立地为卤素，羟基，氰基，取代或未取代的烷基或类似物；m为0，1，2，3或4；R11为卤素，羟基，氰基，取代或未取代的烷基或类似物；R12分别独立地为卤素，羟基，氰基或类似物；n为0，1，2，3或4；与(B)克拉霉素或其药学上可接受的盐，或阿奇霉素或其药学上可接受的盐结合；以及(C)克罗法齐明或其药学上可接受的盐。
• SUSTAINED HIV PROTEASE INHIBITOR
  申请人：Shionogi & Co., Ltd.

  公开号：EP3192794A1

  公开（公告）日：2017-07-19

  The present invention provides useful compounds for HIV protease inhibitor. A compound represented by formula or its pharmaceutically acceptable salt Formula: wherein ring A is R4 is -Y-Z, hydrogen atom, halogen, hydroxy and the like, R5 is hydrogen atom, halogen, hydroxy and the like, R6 is each independently halogen, hydroxy, carboxy and the like, ring A may be substituted with said R6 at any substitutable position(s), a is an integer of 0 to 7, ring B is substituted or unsubstituted aromatic carbocyclyl, or substituted or unsubstituted aromatic heterocyclyl, ring C is substituted or unsubstituted aromatic carbocyclyl, substituted or unsubstituted non-aromatic carbocyclyl, substituted or unsubstituted aromatic heterocyclyl, or substituted or unsubstituted non-aromatic heterocyclyl, R1 is -Y-Z, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl and the like, R2 and R3 are each independently -Y-Z or hydrogen atom, provided that at least one of R1, R2, R3 and R4 is a group represented by formula: -Y-Z, Y is a bond, or a spacer of any combination selected from the group consisting of -O-, -S-, -NR7-, -C(=O)-, -SO-, -SO2-, -NR7-C(=O)-, -C(=O)-NR7-, -NR7-C(=O)-NR7-, -NR7-C(=O)-O-, -SO2-NR7-, -NR7-SO2-, substituted or unsubstituted alkylene, substituted or unsubstituted alkenylene, substituted or unsubstituted alkynylene, substituted or unsubstituted aromatic carbocyclediyl, substituted or unsubstituted non-aromatic carbocyclediyl, substituted or unsubstituted aromatic heterocyclediyl and substituted or unsubstituted non-aromatic heterocyclediyl, R7 are each independently hydrogen atom, hydroxy, carboxy and the like, and Z is substituted aromatic carbocyclyl, substituted non-aromatic carbocyclyl, substituted aromatic heterocyclyl or substituted non-aromatic heterocyclyl.

  本发明提供了用于 HIV 蛋白酶抑制剂的有用化合物。由式或其药学上可接受的盐代表的化合物 式： 其中环 A 是 R4为-Y-Z、氢原子、卤素、羟基等、 R5 是氢原子、卤素、羟基等、 R6 各自独立地为卤素、羟基、羧基等、 环 A 可在任何可取代的位置被所述 R6 取代、 a 是 0 至 7 的整数、 环 B 是取代或未取代的芳香族碳环，或取代或未取代的芳香族杂环、 环 C 是取代或未取代的芳香族碳环，取代或未取代的非芳香族碳环，取代或未取代的芳香族杂环，或取代或未取代的非芳香族杂环、 R1 是-Y-Z、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等、 R2 和 R3 各自独立地为-Y-Z 或氢原子、 条件是 R1、R2、R3 和 R4 中至少有一个是由式表示的基团：-Y-Z、 Y 是键，或选自以下组别的任意组合的间隔物：-O-、-S-、-NR7-、-C(=O)-、-SO-、-SO2-、-NR7-C(=O)-、-C(=O)-NR7-、-NR7-C(=O)-NR7-、-NR7-C(=O)-O-、-SO2-、-NR7-SO2-、取代或未取代的亚烷基、取代或未取代的烯基、取代或未取代的炔基、取代或未取代的芳香族碳环基、取代或未取代的非芳香族碳环基、取代或未取代的芳香族杂环基和取代或未取代的非芳香族杂环基、 R7 各自独立地为氢原子、羟基、羧基等，以及 Z 是取代的芳香族碳环基、取代的非芳香族碳环基、取代的芳香族杂环基或取代的非芳香族杂环基。
• HETEROCYCLIC DERIVATIVE HAVING AMPK ACTIVATING EFFECT
  申请人：Shionogi & Co., Ltd.

  公开号：EP3214076A1

  公开（公告）日：2017-09-06

  A compound represented by formula: or its pharmaceutically acceptable salt, wherein L is NR2R3, SR7, SO2R8, substituted or unsubstituted alkyl, or substituted or unsubstituted alkenyl; R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like; R3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like; R7 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like; R8 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like, provided that R8 is not unsubstituted methyl or trifluoromethyl; Y is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, or the like, provided that Y is not unsubstituted methyl or unsubstituted ethyl; Z is -CR6=, or -N=; R1 is hydrogen, or substituted or unsubstituted alkyl; R4, R5 and R6 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like.

  由式表示的化合物： 或其药学上可接受的盐、 其中 L 是 NR2R3、SR7、SO2R8、取代或未取代的烷基，或取代或未取代的烯基； R2 是氢、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等； R3 是氢、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； R7 是氢、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； R8 是氢、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，但 R8 不是未取代的甲基或三氟甲基； Y 是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、取代或未 取代的芳基或类似物，条件是 Y 不是未取代的甲基或未取代的乙基； Z 是-CR6=，或-N=； R1 是氢、或取代或未取代的烷基； R4、R5 和 R6 各自独立地是氢、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。
• SUBSTITUTED POLYCYCLIC PYRIDONE DERIVATIVE AND PRODRUG THEREOF
  申请人：Shionogi & Co., Ltd

  公开号：EP3290424A1

  公开（公告）日：2018-03-07

  The present inventon provides the following compounds having anti-viral activity. A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is CR4AR4B, S or O; the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A1, is 1 or 2; R1A and R1B are each independently hydrogen, halogen, alkyl, or the like; R2A and R2B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B are each independently hydrogen, halogen, alkyl, or the like; R4A and R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together to form non-aromatic carbocycle or non-aromatic heterocycle; X is CH2, S or O; R1 is each independently halogen, hydroxy, or the like; m is any integer of 0 to 2; and n is any integer of 1 to 2.

  本发明提供了以下具有抗病毒活性的化合物。 A1 是 CR1AR1B，S 或 O； A2 是 CR2AR2B，S 或 O； A3 是 CR3AR3B，S 或 O； A4 是 CR4AR4B、S 或 O； 由 A1、A2、A3、A4、与 A1 相邻的氮原子和与 A1 相邻的碳原子构成的环的原子中杂原子的数目为 1 或 2； R1A 和 R1B 各自独立地为氢、卤素、烷基或类似物； R2A 和 R2B 各自独立地为氢、卤素、烷基或类似物； R3A 和 R3B 各自独立地为氢、卤素、烷基或类似物； R4A 和 R4B 各自独立地为氢、卤素、烷基或类似物； R3A 和 R3B 可结合在一起形成非芳香族碳环或非芳香族杂环； X 是 CH2、S 或 O； R1各自独立地为卤素、羟基或类似物； m 是 0 至 2 的任意整数；以及 n 是 1 到 2 的任意整数。