AZ10565259 | 485391-80-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: AZ10565259
• 英文别名: N-[[4-(3,4-dichlorophenoxy)[1,4'-bipiperidin]-1'-yl]carbonyl]-4-methylbenzenesulfonamide；4-[4-(3,4-dichlorophenoxy)piperidin-1-yl]-N-(4-methylphenyl)sulfonylpiperidine-1-carboxamide
• CAS: 485391-80-8
• 化学式: C₂₄H₂₉Cl₂N₃O₄S
• 分子量: 526.484
• InChiKey: QVLZVRFIGXNZMN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.1
• 重原子数：
  34
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  87.3
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  AZ10565259 、 三甲基硅烷化重氮甲烷 以 甲醇 、 二氯甲烷 为溶剂， 反应 12.0h， 生成 4-[4-(3,4-dichlorophenoxy)piperidin-1-yl]-N-methyl-N-(4-methylphenyl)sulfonylpiperidine-1-carboxamide
  参考文献：
  名称：

  The discovery of CCR3/H1 dual antagonists with reduced hERG risk

  摘要：

  A series of dual CCR3/H-1 antagonists based on a bispiperidine scaffold were discovered. Introduction of an acidic group overcame hERG liability. Bioavailability was optimised by modulation of physico-chemical properties and physical form to deliver a compound suitable for clinical evaluation. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.08.124
• 作为产物：
  描述：

  4-(3,4-dichloro-phenoxy)-[1,4']bipiperidine 、 对甲基苯磺酰异氰酸酯 以 二氯甲烷 为溶剂， 反应 1.0h， 生成 AZ10565259
  参考文献：
  名称：

  [EN] PREPARATION OF PHARMACEUTICAL SALTS OF [1, 4] - BIPIPERIDINE
  [FR] PREPARATION DE SELS PHARMACEUTIQUES DE [1,4]-BIPIPERIDINE

  摘要：

  本发明提供了无水和水合钠盐形式的N-[[4-(3,4-二氯苯氧)[1,4'-联吡哌啉]-1'-基]羰基]-4-甲基苯磺酰胺和结晶形式的N-[[4-(3,4-二氯苯氧)[1,4'-联吡哌啉]-1'-基]羰基]-4-甲基苯磺酰胺；这些化合物是趋化因子（特别是CCR3）活性的调节剂，特别适用于治疗哮喘和/或鼻炎。

  公开号：

  WO2005044268A1

文献信息

• Piperidine derivatives useful as modulators of chemokine receptor activity
  申请人：——

  公开号：US20040235894A1

  公开（公告）日：2004-11-25

  The invention provides a compound of formula (I), wherein: T is C(O) or S(O) 2 ; W is C(O) or S(O) 2 ; X is CH 2 , O or NH; Y is CR 5 or N; R 1 is optionally substituted aryl or optionally substituted heterocyclyl; R 2 is hydrogen or C 1-6 alkyl; R 3 is hydrogen or optionally substituted C 1-6 alkyl; and R 4 is alkyl, optionally substituted aryl, optionally substituted aralkyl or optionally substituted heterocyclyl; that are modulators of chemokine (especially CCR3) activity and are especially useful for treating asthma and/or rhinitis. 1

  该发明提供了一个化合物的公式（I），其中：T为C（O）或S（O）2；W为C（O）或S（O）2；X为CH2，O或NH；Y为CR5或N；R1为可选择替代芳基或可选择替代杂环基；R2为氢或C1-6烷基；R3为氢或可选择替代C1-6烷基；R4为烷基，可选择替代芳基，可选择替代芳基烷基或可选择替代杂环基；这些化合物是趋化因子（尤其是CCR3）活性的调节剂，特别适用于治疗哮喘和/或鼻炎。
• Preparation of Pharmaceutical Salts of [1,4] - Bipiperidine
  申请人：Else Howard

  公开号：US20070276141A1

  公开（公告）日：2007-11-29

  The invention provides anhydrous and hydrated forms of sodium salt of N-[[4-(3,4-dichlorophenoxy)[1,4′-bipiperidin]-1′-yl]carbonyl]-4-methyl-benzenesulfonamide and crystalline forms of N-[[4-(3,4-dichlorophenoxy)[1,4′-bipiperidin]-1′-yl]carbonyl]-4-methyl-benzenesulfonamide; and such compounds are modulators of chemokine (especially CCR3) activity and are especially useful for treating asthma and/or rhinitis.

  本发明提供了N-[[4-(3,4-二氯苯氧)[1,4'-双哌啶]-1'-基]羰基]-4-甲基苯磺酰胺的无水和水合物形式以及N-[[4-(3,4-二氯苯氧)[1,4'-双哌啶]-1'-基]羰基]-4-甲基苯磺酰胺的晶体形式；这些化合物是趋化因子（特别是CCR3）活性的调节剂，特别适用于治疗哮喘和/或鼻炎。
• INTERMEDIATES FOR THE PREPARATION OF PIPERIDINE DERIVATIVES USEFUL AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
  申请人：AstraZeneca AB

  公开号：EP1604982A1

  公开（公告）日：2005-12-14

  The invention provides a compound of formula (X) or (XVIII): wherein: R1 is optionally substituted aryl or optionally substituted heterocyclyl; and R2 is hydrogen or C1-6 alkyl; said compounds can be used for preparing modulators of chemokine (especially CCR3) activity.

  本发明提供了一种式 (X) 或 (XVIII) 的化合物： 其中R1是任选取代的芳基或任选取代的杂环基；R2是氢或C1-6烷基；所述化合物可用于制备趋化因子（尤其是CCR3）活性调节剂。
• Inhibition of chemokine CCL7 or receptor CCR3 of same for the treatment and diagnosis of prostate cancer
  申请人：Universite Paul Sabatier (Toulouse III)

  公开号：US10401365B2

  公开（公告）日：2019-09-03

  The invention concerns an inhibitor of the expression of chemokine CCL7 or an inhibitor of the expression of the receptor CCR3 or an inhibitor of CCL7/CCR3 interaction for the use of same to prevent or treat the extension of prostate cancer outside the prostatic capsule in a subject. The invention also concerns a method for determining the degree of aggressiveness of a prostate cancer tumor in a subject suffering from prostate cancer, comprising a step of determining the concentration or level of expression of the receptor CCR3 in a sample of prostate tumor cells obtained from said subject.

  本发明涉及一种趋化因子CCL7表达抑制剂或受体CCR3表达抑制剂或CCL7/CCR3相互作用抑制剂，用于预防或治疗受试者的前列腺癌向前列腺囊外延伸。本发明还涉及一种确定前列腺癌患者前列腺癌肿瘤侵袭程度的方法，该方法包括一个步骤，即确定从所述患者处获得的前列腺肿瘤细胞样本中受体CCR3的浓度或表达水平。
• Composition including glycosaminoglycan derivative and chemokine receptor activity regulator
  申请人：Seikagaku Corporation

  公开号：US11253540B2

  公开（公告）日：2022-02-22

  Provided are a composition comprising a GAG derivative and a chemokine receptor activity regulator, and a pharmaceutical composition comprising said composition.

  本文提供了一种包含凝胶体衍生物和趋化因子受体活性调节剂的组合物，以及一种包含所述组合物的药物组合物。