2-(Morpholin-2-yl)acetamide | 135072-28-5

• 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: 2-(Morpholin-2-yl)acetamide
• 英文别名: 2-morpholin-2-ylacetamide
• CAS: 135072-28-5
• 化学式: C₆H₁₂N₂O₂
• 分子量: 144.17
• InChiKey: XLZZCQLWBSKIMI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.7
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  64.4
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• [EN] INHIBITORS OF PI3 KINASE<br/>[FR] INHIBITEURS DE LA PI3 KINASE
  申请人：CT NAC INVESTIGACIONES ONCOLOGICAS CNIO

  公开号：WO2011089400A1

  公开（公告）日：2011-07-28

  There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.

  提供了式（I）的化合物，其中A1、A4、A4a、A5、B1、B1a、B2、B2a、B3、B3a、B4、B4a和R3的含义如描述中所给，并且其药学上可接受的酯、酰胺、溶剂合物或盐，这些化合物在治疗需要或期望抑制蛋白激酶或脂质激酶（例如PI3-K和/或mTOR）的疾病中非常有用，特别是在癌症或增生性疾病的治疗中。
• PYRAZOLE DERIVATIVES
  申请人：DAIICHI PHARMACEUTICAL CO., LTD.

  公开号：EP1762568A1

  公开（公告）日：2007-03-14

  A compound represented by formula (I): (wherein Ar1 represents a phenyl group which may have 1 to 3 substituents, or a non-substituted 5- or 6-membered aromatic heterocyclic group; Ar2 represents (i) a non-substituted phenyl group, (ii) a phenyl group which has been substituted by a lower alkyl group having 1 to 3 groups or atoms selected from among a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom, or (iii) a 5- or 6-membered nitrogen-containing aromatic heterocyclic group which has been substituted by 1 to 3 groups or atoms selected from among a lower alkyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group, a cyano group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom; and X represents a group represented by formula (II): (wherein the ring structure represents a 4- to 7-membered heterocyclic group which may have, in addition to the nitrogen atom shown in formula (II), one heteroatom selected from among nitrogen, oxygen, and sulfur, and which may be substituted by 1 to 4 groups or atoms selected from among a lower alkyl group, a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, an oxo group, a lower alkanoyl group, a lower alkylsulfonyl group, and a halogen atom)), a salt thereof, a solvate of the compound or the salt, and a drug.

  由式(I)表示的化合物： （其中Ar1代表可能具有1到3个取代基的苯基，或者是非取代的5-或6-成员芳香杂环基团；Ar2代表（i）非取代的苯基团，（ii）已被1到3个来自羰胺基、氨基、羟基、低烷氧基和卤原子的群或原子取代的较低烷基基团取代的苯基团，或者（iii）已被1到3个来自低烷基基团、低炔基基团、低烷酰基团、羰胺基、氰基、氨基、羟基、低烷氧基和卤原子的群或原子取代的5-或6-成员含氮芳香杂环基团；X代表由式(II)表示的基团： （其中环结构表示可能具有除了式(II)中显示的氮原子之外，从氮、氧和硫中选择的一个杂原子的4-到7-成员杂环基团，并且可能被1到4个来自低烷基基团、羰胺基、氨基、羟基、低烷氧基、氧基、低烷酰基团、低烷基磺酰基团和卤原子的群或原子取代）），其盐，该化合物或其盐的溶剂化合物，以及药物。
• [EN] SPIROCYCLIC COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS AND DIAGNOSTIC PROBES<br/>[FR] COMPOSÉS SPIROCYCLIQUES ET LEUR UTILISATION COMME AGENTS THÉRAPEUTIQUES ET SONDES DE DIAGNOSTIC
  申请人：UNIV BASEL

  公开号：WO2011114275A1

  公开（公告）日：2011-09-22

  The invention relates to new triazines (G = Q = U are N), pyrimidines (two out of G, Q and U are N), and pyridopyrimidines (one of G and U together with R2 forms an anullated pyridine ring) of formula (I) carrying a spirocyclic substituent, wherein E1 is CR4 or N; X1 is CHR4, CH2CH2, NR4, NR4→0, or O; and the other substituents are as defined in the specification. The compounds inhibit phosphoinositide 3-kinase (PI3K), mammalian target of rapamycin (mTOR), DNA-PK and ATM kinase, and may be used as therapeutic agents or diagnostic probes. The invention also relates to methods of using the compounds for treatment of associated pathological conditions.

  本发明涉及新的三嗪类化合物（其中G = Q = U为N）、嘧啶类化合物（其中G、Q和U中的两个为N）和吡啶嘧啶类化合物（其中G和U中的一个与R2共同形成一个环状吡啶环），它们都带有一个螺环取代基，化学式为（I）。其中，E1为CR4或N；X1为CHR4、CH2CH2、NR4、NR4→0或O；其他取代基如规范中所定义。这些化合物能够抑制磷脂酰肌醇3-激酶（PI3K）、哺乳动物雷帕霉素靶蛋白酶（mTOR）、DNA-PK和ATM激酶，并可用作治疗剂或诊断探针。本发明还涉及使用这些化合物治疗相关病理条件的方法。
• SPIROCYCLIC COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS AND DIAGNOSTIC PROBES
  申请人：Cmiljanovic Vladimir

  公开号：US20130040934A1

  公开（公告）日：2013-02-14

  The invention relates to new triazines (G=Q=U are N), pyrimidines (two out of G, Q and U are N), and pyridopyrimidines (one of G and U together with R2 forms an anullated pyridine ring) of formula (I) carrying a spirocyclic substituent, wherein E 1 is CR 4 or N; X 1 is CHR 4 , CH 2 CH 2 , NR 4 , NR4→0, or O; and the other substituents are as defined in the specification. The compounds inhibit phosphoinositide 3-kinase (PI3K), mammalian target of rapamycin (mTOR), DNA-PK and ATM kinase, and may be used as therapeutic agents or diagnostic probes. The invention also relates to methods of using the compounds for treatment of associated pathological conditions.

  该发明涉及具有螺环取代基的新三嗪类化合物（其中G=Q=U为N）、嘧啶类化合物（其中G、Q和U中的两个为N）和吡啶嘧啶类化合物（其中G和U中的一个与R2一起形成一个环状吡啶环）的化学式（I），其中E1为CR4或N；X1为CHR4、CH2CH2、NR4、NR4→0或O；其他取代基如规范中定义。这些化合物抑制磷脂酰肌醇3-激酶（PI3K）、哺乳动物雷帕霉素靶蛋白（mTOR）、DNA-PK和ATM激酶，并可用作治疗剂或诊断探针。该发明还涉及使用这些化合物治疗相关病理条件的方法。
• Aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives
  申请人：Buettelmann Bernd

  公开号：US20070179178A1

  公开（公告）日：2007-08-02

  The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives of formula I: wherein R 1 to R 5 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

  本发明涉及式I的芳基异噁唑-4-基-咪唑并[1,2-a]吡啶衍生物： 在此式中，R1至R5如规范中所定义，并且其药用可接受的酸盐。这类化合物具有高亲和力和选择性，适用于GABA A α5受体结合位点，并可能用作认知增强剂或治疗认知障碍，如阿尔茨海默病。