（2S）-2-[[[9-丙-2-基-6-[（4-吡啶-2-基苯基）甲基氨基]嘌呤-2-基]氨基]丁-1-醇 | 1084893-56-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: （2S）-2-[[[9-丙-2-基-6-[（4-吡啶-2-基苯基）甲基氨基]嘌呤-2-基]氨基]丁-1-醇
• 英文名称: (2S)-2-[[9-propan-2-yl-6-[[4-(2-pyridinyl)phenyl]methylamino]-2-purinyl]amino]-1-butanol
• 英文别名: (2S)-2-[[9-propan-2-yl-6-[(4-pyridin-2-ylphenyl)methylamino]purin-2-yl]amino]butan-1-ol
• CAS: 1084893-56-0
• 化学式: C₂₄H₂₉N₇O
• 分子量: 431.5
• InChiKey: HOCBJBNQIQQQGT-IBGZPJMESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  32
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  101
• 氢给体数：
  3
• 氢受体数：
  7

文献信息

• [EN] 5-ALKYLTHIO-7-[(4-ARYLBENZYL)AMINO]-1(2)H-PYRAZOLO[4,3-D]PYRIMIDINES FOR TREATMENT OF LYMPHOMA<br/>[FR] 5-ALKYLTHIO-7-[(4-ARYLBENZYL) AMINO] -1 (2) H-PYRAZOLO [4,3-D] PYRIMIDINES POUR LE TRAITEMENT DU LYMPHOME
  申请人：UNIV PALACKEHO

  公开号：WO2019149295A1

  公开（公告）日：2019-08-08

  The present invention relates to 5-alkylthio-7-[(4-arylbenzyl)amino]-1(2)H-pyrazolo[4,3-d]pyrimidine derivatives of formula I which are effective inhibitors of kinases and exhibit strong antiproliferative and proapoptotic properties on lymphoma cells. This invention further relates to use of said derivatives in the treatment of blood hyperproliferative diseases, such as Non-Hodgkin lymphomas.

  本发明涉及式I的5-烷基硫基-7-[(4-芳基苄基)氨基]-1(2)H-吡唑并[4,3-d]嘧啶衍生物，它们是激酶的有效抑制剂，并在淋巴瘤细胞上表现出强烈的抗增殖和促凋亡特性。本发明还涉及利用这些衍生物治疗血液过度增殖性疾病，如非霍奇金淋巴瘤。
• Compounds for reducing c-Myc in c-Myc overexpressing cancers background
  申请人：The Trustees of Columbia University in the City of New York

  公开号：US10882863B2

  公开（公告）日：2021-01-05

  The invention relates to new compounds that reduce c-Myc expression and useful for cancer treatment, particularly hematological cancers such as aggressive B- and T-cell lymphomas. The new compounds may be combined with adjunct c-Myc inhibor agents such as a PI3K inhibitor, CK-1 inhibitor, Akt-inhibitor, proteasome inhibitor and/or mTor inhibitor. The c-Myc reducing agent may be provided as a lead-in treatment to reduce or initiate reduction of c-Myc prior to administration of the adjunct cancer therapeutic agent. Treatment with a c-Myc reducing agent modulates the disease state of the c-Myc overexpressing cancer making it less malignant and more susceptible to adjunctive cancer therapies.

  本发明涉及可降低 c-Myc 表达并可用于癌症治疗的新化合物，特别是血液肿瘤，如侵袭性 B 细胞和 T 细胞淋巴瘤。新化合物可与辅助性 c-Myc 抑制剂如 PI3K 抑制剂、CK-1 抑制剂、Akt-抑制剂、蛋白酶体抑制剂和/或 mTor 抑制剂结合使用。c-Myc还原剂可作为先导疗法，在使用辅助癌症治疗剂之前减少或开始减少c-Myc。使用c-Myc还原剂治疗可调节c-Myc过表达癌症的疾病状态，使其恶性程度降低，更容易接受辅助癌症疗法。
• UTILISATION DE DERIVES DE PURINE POUR LA FABRICATION D'UN MEDICAMENT
  申请人：Centre National de la Recherche Scientifique

  公开号：EP2187889B1

  公开（公告）日：2013-11-06
• 5-ALKYLTHIO-7-[(4-ARYLBENZYL)AMINO]-1(2)H-PYRAZOLO[4,3-D]PYRIMIDINES FOR TREATMENT OF LYMPHOMA
  申请人：Univerzita Palackeho v Olomouci

  公开号：EP3749670B1

  公开（公告）日：2021-10-06
• MODULATORS OF VIRAL TRANSCRIPTION, AND METHODS AND COMPOSITIONS THEREWITH
  申请人：KASHANCHI Fatah

  公开号：US20120149708A1

  公开（公告）日：2012-06-14

  The present invention is directed to a process for inhibiting the replication of human immunodeficiency virus-1 (HIV-1), by contacting a cell with at least one compound according to Formula I. The substituent groups R 1 , R 2 , R 3 , X, Y, Z, A and B are as defined above. Also contemplated is a method for treating or preventing a HIV-1 infection in a subject, by administering a therapeutically effective amount of at least one compound according to Formula I, as well as a method for modulating the activity of a cyclin dependent kinase (cdk) in a cell infected with HIV-1 using a Formula I compound.