(R)-(+)-3-二甲氨基吡咯烷双盐酸盐 | 864448-61-3

• 物质功能分类: 有机原料 - 杂环化合物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 中文名称: (R)-(+)-3-二甲氨基吡咯烷双盐酸盐
• 中文别名: (R)-(+)-3-二甲氨基吡咯烷二盐酸盐；(3R)-(+)-3-二甲氨基吡咯烷二盐酸盐；(R)-3-(二甲基氨基)吡咯烷双盐酸盐
• 英文名称: (R)-(+)-3-(Dimethylamino)pyrrolidine dihydrochloride
• 英文别名: (3R)-N,N-dimethylpyrrolidin-3-amine;dihydrochloride
• CAS: 864448-61-3
• 化学式: C6H16Cl2N2
• 分子量: 187.11
• InChiKey: LCPKWRSLMCUOOZ-QYCVXMPOSA-N

物化性质

• 熔点：
  194-197℃

计算性质

• 辛醇/水分配系数(LogP)：
  0.75
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  15.3
• 氢给体数：
  3
• 氢受体数：
  2

安全信息

• 海关编码：
  2933990090
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H315,H319,H335

反应信息

• 作为反应物：
  描述：

  (R)-(+)-3-二甲氨基吡咯烷双盐酸盐 、 5-chloro-N-(4-fluoro-2-methoxy-5-nitrophenyl)-4-(pyrazolo[1,5-a]pyridin-3-yl)pyrimidin-2-amine 、 N,N-二异丙基乙胺 在 甲醇 、 氨 、 二氯甲烷 作用下， 以 N,N-二甲基乙酰胺 、 甲醇 为溶剂， 反应 0.5h， 以gave the title compound (149 mg, 61%) as an orange foam的产率得到5-Chloro-N-[4-[(3R)-3-dimethylaminopyrrolidin-1-yl]-2-methoxy-5-nitrophenyl]-4-pyrazolo[1,5-a]pyridin-3-ylpyrimidin-2-amine
  参考文献：
  名称：

  2-(2,4,5-substituted-anilino) pyrimidine compounds

  摘要：

  本发明涉及某些2-(2,4,5-取代苯胺基)嘧啶化合物及其药学上可接受的盐，可用于治疗或预防经由某些突变表皮生长因子受体介导的疾病或医疗状况（例如L858R激活突变体、Exon19缺失激活突变体和T790M耐药突变体）。这些化合物及其盐可用于治疗或预防多种不同的癌症。本发明还涉及包含所述化合物及其盐的药物组合物，特别是这些化合物及其盐的有用多晶形式、制造这些化合物的中间体以及使用这些化合物及其盐治疗不同形式的EGFR介导疾病的方法。

  公开号：

  US08946235B2

文献信息

• [EN] 1,3,4-OXADIAZOLE SULFONAMIDE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME<br/>[FR] COMPOSÉS DÉRIVÉS DE 1,3,4-OXADIAZOLE SULFONAMIDE SERVANT D'INHIBITEUR DE L'HISTONE DÉSACÉTYLASE 6, ET COMPOSITION PHARMACEUTIQUE COMPRENANT CEUX-CI
  申请人：CHONG KUN DANG PHARMACEUTICAL CORP

  公开号：WO2017018803A1

  公开（公告）日：2017-02-02

  The present invention relates to novel compounds represented by the formula I having histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel compounds. (I) The novel compounds, stereoisomers thereof or pharmaceutically acceptable salts thereof according to the present invention have histone deacetylase (HDAC) inhibitory activity and are effective for the prevention or treatment of HDAC6-mediated diseases.

  本发明涉及具有组蛋白去乙酰化酶6（HDAC6）抑制活性的新化合物，其立体异构体或药学上可接受的盐，其用于制备治疗药物，含有相同化合物的药物组合物，使用该组合物治疗疾病的方法，以及制备新化合物的方法。根据本发明，这些新化合物、其立体异构体或药学上可接受的盐具有组蛋白去乙酰化酶（HDAC）抑制活性，并且对于预防或治疗HDAC6介导的疾病有效。
• 2-(2,4,5-SUBSTITUTED-ANILINO) PYRIMIDINE COMPOUNDS
  申请人：BUTTERWORTH Sam

  公开号：US20130053409A1

  公开（公告）日：2013-02-28

  The present invention relates to certain 2-(2,4,5-substituted-anilino)pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exon19 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.

  本发明涉及某些2-(2,4,5-取代苯胺基)嘧啶化合物及其药学上可接受的盐，这些化合物可能对通过某些突变表皮生长因子受体介导的疾病或医疗状况（例如L858R激活突变体、Exon19缺失激活突变体和T790M耐药突变体）的治疗或预防有用。这些化合物及其盐可能对多种不同的癌症的治疗或预防有用。本发明还涉及包含这些化合物及其盐的药物组合物，特别是这些化合物及其盐的有用多形式，以及用于制造这些化合物的中间体和使用这些化合物及其盐治疗通过不同形式的EGFR介导的疾病的方法。
• 2-(2,4,5-substituted-anilino) pyrimidine compounds
  申请人：Butterworth Sam

  公开号：US08946235B2

  公开（公告）日：2015-02-03

  The present invention relates to certain 2-(2,4,5-substituted-anilino)pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exon19 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using such compounds and salts thereof.

  本发明涉及某些2-(2,4,5-取代苯胺基)嘧啶化合物及其药学上可接受的盐，可用于治疗或预防经由某些突变表皮生长因子受体介导的疾病或医疗状况（例如L858R激活突变体、Exon19缺失激活突变体和T790M耐药突变体）。这些化合物及其盐可用于治疗或预防多种不同的癌症。本发明还涉及包含所述化合物及其盐的药物组合物，特别是这些化合物及其盐的有用多晶形式、制造这些化合物的中间体以及使用这些化合物及其盐治疗不同形式的EGFR介导疾病的方法。
• 2-(2,4,5-SUBSTITUTED-ANILINO)PYRIMIDINE DERIVATIVES AS EGFR MODULATORS USEFUL FOR TREATING CANCER
  申请人：Astrazeneca AB

  公开号：EP3009431A1

  公开（公告）日：2016-04-20

  The present invention relates to certain 2-(2,4,5-substituted-anilino)pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.

  本发明涉及某些2-(2,4,5-取代-苯胺基)嘧啶化合物及其药学上可接受的盐类，它们可用于治疗或预防通过某些突变形式的表皮生长因子受体（例如L858R激活突变体、Exonl9缺失激活突变体和T790M抗性突变体）介导的疾病或医疗状况。此类化合物及其盐类可用于治疗或预防多种不同的癌症。本发明还涉及包含上述化合物及其盐类的药物组合物、特别有用的这些化合物及其盐类的多态形式、用于制造上述化合物的中间体，以及使用上述化合物及其盐类治疗由各种不同形式的表皮生长因子受体介导的疾病的方法。
• 2-(2,4,5-substituted-anilino)pyrimidine compounds
  申请人：AstraZeneca AB

  公开号：US10017493B2

  公开（公告）日：2018-07-10

  The present invention relates to certain 2-(2,4,5-substituted-anilino)pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exon19 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.

  本发明涉及某些2-(2,4,5-取代-苯胺基)嘧啶化合物及其药学上可接受的盐类，它们可用于治疗或预防通过某些突变形式的表皮生长因子受体（例如L858R激活突变体、Exon19缺失激活突变体和T790M抗性突变体）介导的疾病或医疗状况。此类化合物及其盐类可用于治疗或预防多种不同的癌症。本发明还涉及包含上述化合物及其盐类的药物组合物、特别有用的这些化合物及其盐类的多态形式、用于制造上述化合物的中间体，以及使用上述化合物及其盐类治疗由各种不同形式的表皮生长因子受体介导的疾病的方法。