4-(2,5-dimethyl-furan-3-ylmethyl)-morpholine | 14497-40-6

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 4-(2,5-dimethyl-furan-3-ylmethyl)-morpholine
• 英文别名: 4-[(2,5-Dimethylfuran-3-yl)methyl]morpholine
• CAS: 14497-40-6
• 化学式: C₁₁H₁₇NO₂
• 分子量: 195.261
• InChiKey: SFKRSMJGFCGONJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.64
• 拓扑面积：
  25.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  吗啉 、 3-chloromethyl-2,5-dimethyl-furan 在 氢氧化钾 作用下， 生成 4-(2,5-dimethyl-furan-3-ylmethyl)-morpholine
  参考文献：
  名称：

  Researches on furans

  摘要：

  DOI：

  10.1007/bf00664821

文献信息

• [EN] 3,4-DISUBSTITUTED PYRAZOLES AS CYCLIN DEPENDENT KINASES (CDK) OR AURORA KINASE OR GLYCOGEN SYNTHASE 3 (GSK-3) INHIBITORS<br/>[FR] PYRAZOLES 3,4-DISUBSTITUTES SERVANT D'INHIBITEURS DE KINASES CYCLINES DEPENDANTES (CDK), OU DE KINASES AURORA OU DE GLYCOGENE SYNTASES 3 (GSK-3)
  申请人：ASTEX TECHNOLOGY LTD

  公开号：WO2006003440A1

  公开（公告）日：2006-01-12

  The invention provides compounds of the formula (I); or salts or solvates or N-oxides thereof; wherein: Rq is selected from groups (a), (b) and (c); the asterisk denoting the point of attachment to the pyrazole ring; X is N or CR5; X' is NR4', O, S or S(O); A is a bond or -(CH2)m-(B)n-; B is C=O, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R0 is hydrogen or, together with NRg when present, forms a group -(CH2)p- wherein p is 2 to 4; and R1 to R6b are as defined in the description. Compounds of the formula (I) have activity as inhibitors of CDK, aurora and GSK-3 kinases are useful in treating or preventing diseases such as cancers that are mediated by the said kinases.

  本发明提供式(I)的化合物；或其盐、溶剂化物或N-氧化物；其中：Rq选自基团(a)、(b)和(c)；星号表示与吡唑环的连接点；X为N或CR5；X'为NR4'、O、S或S(O)；A为键或-(CH2)m-(B)n-；B为C=O、NRg(C=O)或O(C=O)，其中Rg为氢或C1-4烃基，可选择性地被羟基或C1-4烷氧基取代；m为0、1或2；n为0或1；R0为氢，或与存在的NRg一起形成基团-( )p-，其中p为2至4；R1至R6b如说明书中所定义。式(I)的化合物作为CDK、aurora和GSK-3激酶的抑制剂，对于治疗或预防由所述激酶介导的疾病，如癌症，具有用途。
• Benzimidazole derivatives and their use as protein kinases inhibitors
  申请人：Berdini Valerio

  公开号：US20070135477A1

  公开（公告）日：2007-06-14

  The invention provides compounds of the formula (1): The compounds have activity against cyclin depdenent kinases, glycogen synthase kinase and Auroa kinases and are therefore useful to treat cancer and viral diseases.

  该发明提供了式（1）的化合物： 这些化合物具有对环素依赖性激酶、糖原合成酶激酶和Auroa激酶的活性，因此可用于治疗癌症和病毒性疾病。
• 3,4-Disubstituted Pyrazoles as Cyclin Dependent Kinases (Cdk) or Aurora Kinase or Glycogen Synthase 3 (Gsk-3) Inhibitors
  申请人：Gill Liam Adrian

  公开号：US20080004270A1

  公开（公告）日：2008-01-03

  The invention provides compounds of the formula (I); or salts or solvates or N-oxides thereof; wherein: R q is selected from groups (a), (b) and (c); the asterisk denoting the point of attachment to the pyrazole ring; X is N or CR 5 ; X″ is NR 4 ; O, S or S(O); A is a bond or —(CH 2 ) m —(B) n —; B is C═O, NR g (C═O) or O(C═O) wherein R g is hydrogen or C 1-4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R 0 is hydrogen or, together with NR g when present, forms a group —(CH 2 ) p — wherein p is 2 to 4; and R 1 to R 6b are as defined in the description. Compounds of the formula (I) have activity as inhibitors of CDK, aurora and GSK-3 kinases are useful in treating or preventing diseases such as cancers that are mediated by the said kinases.

  本发明提供了式（I）的化合物；或其盐、溶剂或N-氧化物；其中：Rq选择自组（a）、（b）和（c）；星号表示与吡唑环的连接点；X为N或CR5；X″为NR4；O、S或S（O）；A为键或—（CH2）m—（B）n—；B为C═O、NRg（C═O）或O（C═O），其中Rg为氢或C1-4烃基，可选地被羟基或C1-4烷氧基取代；m为0、1或2；n为0或1；R0为氢或与NRg一起，形成—（ ）p—基团，其中p为2至4；R1至R6如描述中所定义。式（I）的化合物具有作为CDK、极光激酶和GSK-3激酶抑制剂的活性，可用于治疗或预防由该激酶介导的癌症等疾病。
• Thiazole And Isothiazole Derivatives That Modulate The Activity Of CDK, GSK And Aurora Kinases
  申请人：Berdini Valerio

  公开号：US20080312223A1

  公开（公告）日：2008-12-18

  The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR 5 or N; each of Q 1 and Q 2 is a carbon atom; Q 3 is selected from S and CH; Q 4 is selected from CR 2 and S; provided that one of Q 3 and Q 4 is S and the other of Q 3 and Q 4 is not S; wherein when Q 3 is S, there is a double bond between Q 1 and Q 4 and a double bond between Q 2 and the adjacent ring nitrogen atom N; and when Q 4 is S, there is a double bond between Q 1 and Q 2 , and a double bond between Q 3 and the adjacent ring nitrogen atom N; A is a bond or —(CH 2 ) m —(B) n —; B is C═O, NR 8 (C═O) or O(C═O) wherein R 1 is hydrogen or C1_4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R o is hydrogen or, together with NR g when present, forms a group —(CH 2 ) p — wherein p is 2 to 4; R 1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C 1-8 hydrocarbyl group; R 2 is hydrogen, halogen, methoxy, or a C 1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or methoxy; R 3 and R 4 together with the carbon atoms to which they are attached form an optionally substituted fused carbocyclic or heterocyclic ring having from 5 to 7 ring members of which up to 3 can be heteroatoms selected from N, O and S; and R 5 is hydrogen, a group R 2 or a group R 10 wherein R 10 is as defined in the claims. The compounds have activity as inhibitors of cyclin dependent kinases, glycogen synthase kinases and Aurora kinases.

  本发明提供一种化合物，其化学式为（I）或其盐，N-氧化物，互变异构体或溶剂化物，其中X为CR5或N; Q1和Q2中的每一个都是碳原子; Q3从S和CH中选择; Q4从CR2和S中选择; 假设Q3和Q4中的一个是S，而另一个不是S; 当Q3为S时，Q1和Q4之间有一个双键，Q2和相邻的环氮原子N之间有一个双键; 当Q4为S时，Q1和Q2之间有一个双键，并且Q3和相邻的环氮原子N之间有一个双键; A是键或-(CH2)m-(B)n-; B为C═O，NR8（C═O）或O（C═O），其中R1为氢或C1_4烃基，可选择地被羟基或C1-4烷氧基取代; m为0、1或2; n为0或1; Ro为氢或与NRg一起形成一个群体-( )p-，其中p为2至4; R1为氢，具有3至12个环成员的碳环或杂环基，或可选择地被取代的C1-8烃基基团; R2为氢、卤素、甲氧基或可选择地被卤素、羟基或甲氧基取代的C1-4烃基基团; R3和R4与它们所连接的碳原子一起形成一个可选择地取代的融合碳环或杂环环，其具有5至7个环成员，其中最多可有3个异原子，选择自N、O和S; R5为氢、R2基团或R10基团，其中R10如权利要求所定义。该化合物具有作为细胞周期依赖性激酶、糖原合成酶激酶和极化子激酶的抑制剂的活性。
• Imine Compound
  申请人：Saito Shiuji

  公开号：US20080312435A1

  公开（公告）日：2008-12-18

  An imine compound represented by the formula: wherein A represents a heterocyclic group; R 1 , R 2 , an R 3 each represent a hydrogen atom, a halogen atom, a C 1-10 alkyl group optionally substituted with an aryl group(s) substituted with a halogen atom(s), a C 3-10 cycloalkyl group, a C 1-6 haloalkyl group, a C 1-10 alkoxy group, etc.; R 4 represents an optionally substituted C 1-10 alkyl, C 2-6 alkenyl, or aryl group; R 5 represents a hydrogen atom, a C 1-10 alkoxy group, a C 1-6 haloalkyl group, an optionally substituted C 1-10 alkyl or C 2-6 alkenyl group, an optionally substituted aryl or heterocyclic group, etc.; W represents —CO—, —CO—CO—, —CO—NH—, —CS—NH—, or —SO 2 —, or a cannabinoid-receptor agonist comprising said imine compound as an active ingredient. The imine compound of the present invention has a cannabinoid-receptor agonist effect, and is useful as a therapeutic or prophylactic drug for pains and autoimmune diseases.

  一种以以下式表示的亚胺化合物：其中A代表杂环基团；R1、R2和R3分别表示氢原子、卤素原子、C1-10烷基，该烷基可选地取代有芳基，所述芳基取代有卤素原子，C3-10环烷基，C1-6卤代烷基，C1-10烷氧基等；R4表示可选地取代的C1-10烷基，C2-6烯基或芳基；R5表示氢原子，C1-10烷氧基，C1-6卤代烷基，可选地取代的C1-10烷基或C2-6烯基，可选地取代的芳基或杂环基团等；W表示—CO—，—CO—CO—，—CO—NH—，—CS—NH—或—SO2—，或以该亚胺化合物为活性成分的大麻素受体激动剂。本发明的亚胺化合物具有大麻素受体激动剂作用，可用作治疗或预防疼痛和自身免疫性疾病的药物。