AB530 | 852670-21-4

• 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: AB530
• 英文别名: N-[4-[3-(5-tert-butyl-1,2-oxazol-3-yl)ureido]phenyl]imidazo[2,1-b]benzothiazole-2-carboxamide；ABS530；Benzo[d]imidazo[2,1-b]thiazole-2-carboxylic acid {4-[3-(5-tert-butyl-isoxazol-3-yl)-ureido]-phenyl}-amide；N-[4-[(5-tert-butyl-1,2-oxazol-3-yl)carbamoylamino]phenyl]imidazo[2,1-b][1,3]benzothiazole-2-carboxamide
• CAS: 852670-21-4
• 化学式: C₂₄H₂₂N₆O₃S
• 分子量: 474.543
• InChiKey: OEUMLQMTMOCCGW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  34
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  142
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  1-(4-aminophenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea 、 咪唑并[2,1-b]苯并噻唑-2-羧酸 在 N,N'-羰基二咪唑 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 AB530
  参考文献：
  名称：

  Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors

  摘要：

  A series of diaryl ureas with an amide substitution at the 4-position was prepared and found to be potent and selective FLT3 inhibitors with good oral bioavailability and efficacy in a tumor xenograft model. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.07.024

文献信息

• UREA DERIVATIVES AS ABL MODULATORS
  申请人：Grotzfeld Robert M.

  公开号：US20100173917A1

  公开（公告）日：2010-07-08

  The invention provides methods and compositions for treating conditions mediated by Bcr-Abl. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.

  本发明提供了治疗由Bcr-Abl介导的疾病的方法和组合物。本发明还提供了使用这些化合物和/或组合物治疗受试者的各种疾病和不良情况的方法。
• Co-therapy comprising a small molecule CSF-1R inhibitor and an agonistic antibody that specifically binds CD40 for the treatment of cancer
  申请人：Janssen Biotech, Inc.

  公开号：US10857230B2

  公开（公告）日：2020-12-08

  The present invention is directed to methods for treating cancer, preferably a solid tumor or hematological malignancy, including for example pancreatic cancer, lung cancer (including but not limited to non-small cell lung cancer (NSCLC)), prostate cancer, colorectal cancer, breast cancer, melanoma or non-Hodgkin's lymphoma, comprising administering to a subject in need thereof a therapeutically effective amount of co-therapy comprising, consisting or consisting essentially of (a) a small molecule CSF-1R inhibitor and (b) an agonistic antibody that binds CD40.

  本发明涉及治疗癌症的方法，优选实体瘤或血液恶性肿瘤，例如包括胰腺癌、肺癌（包括但不限于非小细胞肺癌（NSCLC））、前列腺癌、结直肠癌、乳腺癌、黑素瘤或非霍奇金淋巴瘤、或非霍奇金淋巴瘤，包括向有需要的受试者施用治疗有效量的联合疗法，该联合疗法包括或主要包括(a) 小分子 CSF-1R 抑制剂和(b) 结合 CD40 的激动抗体。
• CO-THERAPY COMPRISING A SMALL MOLECULE CSF-1R INHIBITOR AND AN AGONISTIC ANTIBODY THAT SPECIFICALLY BINDS CD40 FOR THE TREATMENT OF CANCER
  申请人：Janssen Biotech, Inc.

  公开号：US20180250398A1

  公开（公告）日：2018-09-06

  The present invention is directed to methods for treating cancer, preferably a solid tumor or hematological malignancy, including for example pancreatic cancer, lung cancer (including but not limited to non-small cell lung cancer (NSCLC)), prostate cancer, colorectal cancer, breast cancer, melanoma or non-Hodgkin's lymphoma, comprising administering to a subject in need thereof a therapeutically effective amount of co-therapy comprising, consisting or consisting essentially of (a) a small molecule CSF-1R inhibitor and (b) an agonistic antibody that binds CD40.
• Co-Therapy Comprising A Small Molecule CSF-1R Inhibitor And An Agonistic Antibody That Specifically Binds CD40 For The Treatment Of Cancer
  申请人：Janssen Biotech, Inc.

  公开号：US20210093719A1

  公开（公告）日：2021-04-01

  The present invention is directed to methods for treating cancer, preferably a solid tumor or hematological malignancy, including for example pancreatic cancer, lung cancer (including but not limited to non-small cell lung cancer (NSCLC)), prostate cancer, colorectal cancer, breast cancer, melanoma or non-Hodgkin's lymphoma, comprising administering to a subject in need thereof a therapeutically effective amount of co-therapy comprising, consisting or consisting essentially of (a) a small molecule CSF-1R inhibitor and (b) an agonistic antibody that binds CD40.
• METHODS AND COMPOSITIONS OF INHIBITING CSF1R FOR TREATING ALLERGIC INFLAMMATION
  申请人：THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS

  公开号：US20210145983A1

  公开（公告）日：2021-05-20

  In one aspect, the disclosure relates to methods of treating a disease or condition characterized by allergic inflammation, including, but not limited to, asthma, allergic conjunctivitis, allergic dermatitis, allergic esophagitis, allergic rhinitis, allergen-specific serum IgE production, allergic lung and airway inflammation and airway hyper-responsiveness (AHR) with minimal pulmonary adverse reaction, by administration of at least one CSF1R inhibitor and optionally a further therapeutic agent that is an anti-inflammatory drug and/or respiratory drug. In some aspects, the disclosed CSF1R inhibitors useful in the treatment of characterized by allergic inflammation can be administered using a disclosed pharmaceutical composition. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.