methyl-(3-morpholin-4-yl-phenyl)-amine | 84995-56-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: methyl-(3-morpholin-4-yl-phenyl)-amine
• 英文别名: N-methyl-3-morpholinoaniline；N-methyl-3-(4-morpholinyl)benzenamine；N-methyl-3-morpholin-4-ylaniline
• CAS: 84995-56-2
• 化学式: C₁₁H₁₆N₂O
• 分子量: 192.261
• InChiKey: MMXWMHKUMGONPM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  24.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-溴苯酚 、 methyl-(3-morpholin-4-yl-phenyl)-amine 、 生成 4-[methyl-(3-morpholin-4-yl-phenyl)-amino]-phenol
  参考文献：
  名称：

  HISTONE DEMETHYLASE INHIBITORS

  摘要：

  本发明涉及治疗癌症和肿瘤疾病的组合物和方法。本文提供了取代的吡啶并[3,4-d]嘧啶-4-酮衍生物化合物及包含该化合物的制药组合物。所述化合物和组合物对组蛋白去甲基化酶的抑制具有用途。此外，所述化合物和组合物对治疗癌症，如前列腺癌，乳腺癌，膀胱癌，肺癌，黑色素瘤等具有用途。

  公开号：

  US20160194323A1
• 作为产物：
  描述：

  吗啉 、 3-氯-N-甲基苯胺 在 bis[chloro(1,2,3-trihapto-allylbenzene)palladium(II)] 、 N-[2-二(1-金刚烷)磷苯基]吗啉 、 sodium t-butanolate 作用下， 反应 22.0h， 以88%的产率得到methyl-(3-morpholin-4-yl-phenyl)-amine
  参考文献：
  名称：

  Buchwald-Hartwig 在无水和无溶剂条件下使用 Mor-DalPhos 对（杂）芳基氯化物进行胺化

  摘要：

  我们报告了 [Pd(cinnamyl)Cl]2/Mor-DalPhos 催化剂体系在（杂）芳基氯化物与伯胺或仲胺的 Buchwald-Hartwig 胺化中的应用，该胺化反应在水性条件下进行，不使用共溶剂和/或表面活性剂或在无溶剂条件下（52 个例子）。We have established that reactions of this type can be conducted without the rigorous exclusion of air, and in the case of the solvent-free reactions, we have demonstrated that appropriately selected liquid and solid reagents can be employed successfully.

  DOI：

  10.1002/ejoc.201200510

文献信息

• [EN] COMPOUNDS<br/>[FR] COMPOSÉS
  申请人：MEDICAL RES COUNCIL TECHNOLOGY

  公开号：WO2010106333A1

  公开（公告）日：2010-09-23

  A compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; -NHR3; fused aryl-C4-7-heterocycloalkyI; -CONR4R5; -NHCOR6; -C3-7-cycloalkyl; -O-C3-7-cycloalkyl; -NR3R6; and optionally substituted -C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7 heterocycloalkyl and halogen, wherein said C1-6-alkyl, C2-6-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (I).

  一种具有式（I）的化合物，或其药学上可接受的盐或酯，其中R1选自：芳基；杂环芳基；-NHR3；融合芳基-C4-7-杂环烷基；-CONR4R5；-NHCOR6；-C3-7-环烷基；-O-C3-7-环烷基；-NR3R6；和可选择地取代的-C1-6烷基；其中所述的芳基、杂环芳基、融合芳基-C4-7-杂环烷基和C4-7-杂环烷基均可选择地取代；R2选自氢、芳基、C1-6-烷基、C2-6-烯基、C3-7-环烷基、杂环芳基、C4-7-杂环烷基和卤素，其中所述的C1-6-烷基、C2-6-烯基、芳基、杂环芳基和C4-7-杂环烷基均可选择地取代。进一步涉及制备具有式（I）的化合物的药物组合物、治疗用途和制备方法的其他方面。
• [EN] DIKETOPIPERAZINE DERIVATIVES AS P2X7 MODULATORS<br/>[FR] DÉRIVÉS DE DICÉTOPIPÉRAZINE COMME MODULATEURS DE P2X7
  申请人：GLAXO GROUP LTD

  公开号：WO2010125103A1

  公开（公告）日：2010-11-04

  The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein: A represents an aryl, heteroaryl or heterocyclyl group; and any ring or ring system of said aryl or heteroaryl is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of halogen, C1-6 alkyl, -CF3, - OCF3, cyano, C1-6 alkoxy, -NR10R11, -X-aryl, -X-heteroaryl and -X-heterocyclyl; R1, R2, R3, R4 and R5 independently represent hydrogen, fluorine, chlorine, -CF3, cyano or C1-6 alkyl, such that at least one of R1, R2, R3, R4 and R5 is other than hydrogen; R6, R7, R8, R9, R10 and R11 independently represent hydrogen or C1-6 alkyl; X represents a linker selected from a bond, -(CH2)n- and -O-(CH2)n-; and n represents an integer from 1 to 3. The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor ("P2X7 receptor antagonists").

  本发明提供了一种式(I)化合物或其药学上可接受的盐：(I)其中：A代表芳基、杂芳基或杂环基团；上述芳基或杂芳基的任何环或环系可选地被1至3个取代基取代，这些取代基可以相同或不同，选自卤素、C1-6烷基、-CF3、-OCF3、氰基、C1-6烷氧基、-NR10R11、-X-芳基、-X-杂芳基和-X-杂环基；R1、R2、R3、R4和R5各自独立地代表氢、氟、氯、-CF3、氰基或C1-6烷基，使得R1、R2、R3、R4和R5中至少有一个不是氢；R6、R7、R8、R9、R10和R11各自独立地代表氢或C1-6烷基；X代表连接子，选自键、-(CH2)n-和-O-(CH2)n-；n代表1至3的整数。这些化合物或盐能够调节P2X7受体功能，并能拮抗ATP在P2X7受体上的效应（“P2X7受体拮抗剂”）。
• [EN] NOVEL COMPOUND, PREPARATION METHOD THEREOF, AND USE THEREOF<br/>[FR] NOUVEAU COMPOSÉ, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
  申请人：DAEGU GYEONGBUK MEDICAL INNOVATION FOUND

  公开号：WO2021145729A1

  公开（公告）日：2021-07-22

  The present invention relates to a method for preparing a biomaterial having selectively functionalized tyrosine, a biomaterial having selectively functionalized tyrosine, and a pharmaceutical composition containing the same as an active ingredient. The method for preparing a biomaterial to which a compound represented by formula 2 is coupled, of the present invention, allows the compound represented by formula 2 to be selectively coupled, in a high yield in a biomaterial, to tyrosine, which is present on the surface of an aqueous solution such that the coupling thereof to amino acids other than tyrosine does not occur and, when only one tyrosine is present, heterogeneous mixtures are not present and the inherent activity of the biomaterial is maintained, and thus the compound can be effectively used as a pharmaceutical composition containing a biomaterial drug as an active ingredient. In addition, the method can selectively functionalize tyrosine, and thus can be effectively used for tyrosine functionalization in a biomaterial.

  本发明涉及一种制备具有选择性功能化酪氨酸的生物材料的方法，具有选择性功能化酪氨酸的生物材料，以及含有该生物材料作为活性成分的药物组合物。本发明的一种制备生物材料的方法，其中将由式2表示的化合物偶联到生物材料，使得该化合物能够选择性地偶联到酪氨酸，且在生物材料中的产率较高，酪氨酸位于水溶液表面，使得其与酪氨酸以外的氨基酸不发生偶联，当只有一个酪氨酸存在时，不会出现异质混合物，同时保持生物材料的固有活性，因此该化合物可以有效地用作含有生物材料药物的药物组合物的活性成分。此外，该方法可以选择性功能化酪氨酸，因此可以有效地用于生物材料中的酪氨酸功能化。
• [EN] QUINOLINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS<br/>[FR] DERIVES DE QUINOLEINE UTILISES EN TANT QU'INHIBITEURS DE LA PHOSPHODIESTERASE
  申请人：GLAXO GROUP LTD

  公开号：WO2004103998A1

  公开（公告）日：2004-12-02

  There are provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R19, R20 and R34 are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.

  根据本发明提供了化合物的新结构，其化学式为（I）或其药用盐，其中R1、R2、R19、R20和R34如规范中所述，以及制备这些化合物的方法、含有它们的配方和它们在治疗炎症性疾病中的用途。
• [EN] HISTONE DEMETHYLASE INHIBITORS<br/>[FR] INHIBITEURS DE L'HISTONE DÉMÉTHYLASE
  申请人：QUANTICEL PHARMACEUTICALS INC

  公开号：WO2016044429A1

  公开（公告）日：2016-03-24

  The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

  本发明通常涉及治疗癌症和肿瘤性疾病的组合物和方法。本文提供了替代的吡啶并[3,4-d]嘧啶-4-酮衍生物化合物和包含该化合物的药物组合物。所述化合物和组合物对组蛋白去甲基化酶的抑制有用。此外，所述化合物和组合物对于治疗癌症，如前列腺癌、乳腺癌、膀胱癌、肺癌和/或黑色素瘤等方面是有用的。