N-[(5-chlorofuran-2-yl)methyl]-N'-(1-chloronaphthalen-2-yl)ethane-1,2-diamine | 1391027-10-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并呋喃
• 英文名称: N-[(5-chlorofuran-2-yl)methyl]-N'-(1-chloronaphthalen-2-yl)ethane-1,2-diamine
• CAS: 1391027-10-3
• 化学式: C₁₇H₁₆Cl₂N₂O
• 分子量: 335.233
• InChiKey: MBCJPHGQNWUMJI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  22
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  37.2
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-[(1-chloronaphthalen-2-yl)amino]ethanaminium chloride 、 5-氯-2-糠醛 生成 N-[(5-chlorofuran-2-yl)methyl]-N'-(1-chloronaphthalen-2-yl)ethane-1,2-diamine
  参考文献：
  名称：

  TRPM8 receptor antagonists

  摘要：

  作为瞬时受体电位阳离子通道亚家族M成员8 (以下简称TRPM8) 的选择性拮抗剂的化合物，其化学式为：其中，R选择自：H、Br、CN、NO2、SO2NH2、SO2NHR′ 和SO2NR′2，其中R′选择自线性或支链的C1-C4烷基；X选择自：F、Cl、C1-C3烷基、NH2 和OH；Y选择自：O、CH2、NH 和SO2；R1和R2，独立于彼此，选择自：H、F 和线性或支链的C1-C4烷基；R3和R4，独立于彼此，选择自：H 和线性或支链的C1-C4烷基；Z选择自：NR6 和R6R7N+，其中R6和R7独立于彼此，选择自：H 和线性或支链的C1-C4烷基；R5是选择自：H 和线性或支链的C1-C4烷基的残基；Het是选择自：取代或不取代的吡咯基、取代或不取代的N-甲基吡咯基、取代或不取代的噻吩基、取代或不取代的呋喃基和取代或不取代的吡啶基的杂环基团。所述化合物在预防和治疗依赖于TRPM8活性的病理情况，如疼痛、炎症、缺血、神经退行性疾病、中风、精神障碍、炎症性疾病和泌尿系疾病中有用。

  公开号：

  US08906946B2

文献信息

• [EN] DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE FOR TREATING PAIN<br/>[FR] DÉRIVÉS DE TYPE AZA-INDAZOLE OU DIAZA-INDAZOLE POUR LE TRAITEMENT DE LA DOULEUR
  申请人：PF MEDICAMENT

  公开号：WO2014016433A1

  公开（公告）日：2014-01-30

  The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; for use in the treatment of pain.

  本发明涉及如下式(I)的化合物：或其药用可接受的盐或溶剂化物，其构象异构体，或其立体异构体或立体异构体混合物，以任何比例，例如对映体混合物，尤其是外消旋混合物；用于治疗疼痛。
• [EN] DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE FOR TREATING A CANCER OVEREXPRESSING TRK<br/>[FR] DÉRIVÉS DE TYPE AZA-INDAZOLE OU DIAZA-INDAZOLE POUR LE TRAITEMENT D'UN CANCER SUREXPRIMANT LA TRK
  申请人：PF MEDICAMENT

  公开号：WO2014016434A1

  公开（公告）日：2014-01-30

  The present invention relates to a compound of following formula (I) or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture, as well as pharmaceutical composition comprising such a compound, for use in the treatment of a cancer associated with the overexpression of at least one Trk protein.

  本发明涉及式(I)所示的化合物，或其药用可接受的盐或溶剂化物，其同分异构体，或其立体异构体或立体异构体混合物，以任何比例，例如对映体混合物，尤其是外消旋混合物，以及包含该化合物的药物组合物，用于治疗与至少一种Trk蛋白过表达相关的癌症。
• [EN] DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT<br/>[FR] DÉRIVÉS DE TYPE AZAINDAZOLE OU DIAZAINDAZOLE UTILISÉS COMME MÉDICAMENTS
  申请人：PF MEDICAMENT

  公开号：WO2012101239A1

  公开（公告）日：2012-08-02

  The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.

  本发明涉及式(I)所示的化合物：或其药用可接受的盐或溶剂化物，其构象异构体，或其立体异构体或立体异构体混合物，以任何比例，例如对映异构体的混合物，尤其是外消旋混合物；以及将上述化合物作为药物的使用，尤其是用于治疗癌症、炎症和神经退行性疾病如阿尔茨海默病；作为激酶抑制剂的使用；包含它们的药物组合物；以及制造它们的方法。
• [EN] TRPM8 RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES DES RÉCEPTEURS TRPM8
  申请人：DOMPE SPA

  公开号：WO2012101244A1

  公开（公告）日：2012-08-02

  Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula (I), wherein R is selected from: - H, Br, CN, NO2, SO2NH2, SO2NHR' and SO2NR'2, where R' is selected from linear or branched C1-C4 alkyl; X is selected from: - F, C1, C1-C3 alkyl, NH2 and OH Y is selected from: - O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from - H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from - H and linear or branched C1-C4 alkyl; Z is selected from: - NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: • H and linear or branched C1-C4 alkyl R5 is a residue selected from: - H and linear or branched C1-C4 alkyl Het is a heteroaryl group selected from - a substituted or not substituted pyrrolyl, a substituted or not substituted N- methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted or not substituted furyl and a substituted or not substituted pyridinyl. Said compounds are useful in the prevention and treatment of pathologies depending on TRPM8 activity such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, inflammatory conditions and urological disorders.

  作为Transient Receptor Potential阳离子通道亚家族M成员8（以下简称为TRPM8）的选择性拮抗剂的化合物，具有以下式（I），其中R选自：- H、Br、CN、NO2、SO2NH2、SO2NHR'和SO2NR'2，其中R'选自线性或支链的C1-C4烷基；X选自：- F、C1、C1-C3烷基、NH2和OH；Y选自：- O、CH2、NH和SO2；R1和R2，彼此独立地选自- H、F和线性或支链的C1-C4烷基；R3和R4，彼此独立地选自- H和线性或支链的C1-C4烷基；Z选自：- NR6和R6R7N+，其中R6和R7彼此独立地选自：• H和线性或支链的C1-C4烷基；R5是从- H和线性或支链的C1-C4烷基中选出的残基；Het是从- 取代或未取代的吡咯基、取代或未取代的N-甲基吡咯基、取代或未取代的噻吩基、取代或未取代的呋喃基和取代或未取代的吡啶基中选出的杂环芳基团。所述化合物在预防和治疗依赖于TRPM8活性的病理病变中具有用途，如疼痛、炎症、缺血、神经退行性、中风、精神障碍、炎症性疾病和泌尿系统疾病。
• TRPM8 RECEPTOR ANTAGONISTS
  申请人：Moriconi Alessio

  公开号：US20140031398A1

  公开（公告）日：2014-01-30

  Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO 2 , SO 2 NH 2 , SO 2 NHR′ and SO 2 NR′ 2 , where R′ is selected from linear or branched C 1 -C 4 alkyl; X is selected from: F, Cl, C 1 -C 3 alkyl, NH 2 and OH Y is selected from: O, CH 2 , NH and SO 2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C 1 -C 4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C 1 -C 4 alkyl; Z is selected from: NR6 and R6R7N + , where R6 and R7 independently one from the other, are selected from: H and linear or branched C 1 -C 4 alkyl R5 is a residue selected from: H and linear or branched C 1 -C 4 alkyl Het is a heteroaryl group selected from a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted or not substituted furyl and a substituted or not substituted pyridinyl. Said compounds are useful in the prevention and treatment of pathologies depending on TRPM8 activity such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, inflammatory conditions and urological disorders.

  具有以下式子的化合物作为瞬时受体电位阳离子通道亚家族M成员8（以下简称TRPM8）的选择性拮抗剂： 其中， R从以下选项中选择：H、Br、CN、NO2、SO2NH2、SO2NHR′和SO2NR′2，其中R′从线性或支链C1-C4烷基中选择； X从以下选项中选择：F、Cl、C1-C3烷基、NH2和OH； Y从以下选项中选择：O、CH2、NH和SO2； R1和R2各自独立地从H、F和线性或支链C1-C4烷基中选择； R3和R4各自独立地从H和线性或支链C1-C4烷基中选择； Z从以下选项中选择：NR6和R6R7N+，其中R6和R7各自独立地从H和线性或支链C1-C4烷基中选择； R5是从H和线性或支链C1-C4烷基中选择的残基； Het是从以下异芳基基团中选择的杂环基团：取代或未取代的吡咯基、取代或未取代的N-甲基吡咯基、取代或未取代的噻吩基、取代或未取代的呋喃基和取代或未取代的吡啶基。 所述化合物可用于预防和治疗依赖于TRPM8活性的病理状况，如疼痛、炎症、缺血、神经退行性疾病、中风、精神障碍、炎症性疾病和泌尿系统疾病。