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Title:
PHTHALAZONE HYDROXAMIC ACID DERIVATIVE, PREPARATION THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/177126
Kind Code:
A1
Abstract:
A phthalazone hydroxamic acid compound, a preparation method therefor and an application thereof. A structural formula of the compound is represented by formula I: (I), wherein R1 and R2 are hydrogen atoms or halogen, Y is an oxygen atom, methylene, or difluorine-substituted methylene, Z is -NHCH2-, or (II) is a chemical bond, methylene, fluoro-methylene, or a double bond. The compound can be prepared by enabling carboxylic ester and carboxylic acid to react with hydroxylamine, or performing a deprotection reaction on protected hydroxamic acid, and has inhibitory activity on poly(ADP-ribose)polymerase and/or histone deacetylase.

Inventors:
JIANG YUYANG (CN)
YUAN ZIGAO (CN)
GAO CHUNMEI (CN)
CHEN SHAOPENG (CN)
Application Number:
CN2018/079106
Publication Date:
October 04, 2018
Filing Date:
March 15, 2018
Export Citation:
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Assignee:
SHENZHEN KIVITA INNOVATIVE DRUG INST (CN)
International Classes:
C07D237/32; A61K31/50; A61K31/501; A61P35/00
Foreign References:
CN106946792A2017-07-14
CN102898378A2013-01-30
CN102898377A2013-01-30
CN104003940A2014-08-27
Other References:
DAE-KEE KIM: "Synthesis and Biological Evaluation of 3-(4-Substitu- ted-phenyl)-N-hydroxy-2-propenamides, a New Class of Histone Deacetylase In- hibitors", J. MED. CHEM., vol. 46, no. 26, 22 November 2003 (2003-11-22), pages 5745 - 5751, XP002350854, DOI: 10.1021/jm030377q
XIAO-LING COCKCROFT: "Phthalazinones 2:0ptimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 16, no. 4, 15 November 2005 (2005-11-15), pages 1040 - 1044, XP027965805, DOI: 10.1016/j.bmcl.2005.10.081
TAN, YUMEI.: "The study on the design, synthesis and structure function relationship of novel histone deacetylase inhibitors", CHINESE MASTER'S THESES FULL-TEXT DATABASE (MEDICAL AND HEALTH SCIENCES) (NON-OFFICIAL TRANSLATION), 15 March 2011 (2011-03-15)
Attorney, Agent or Firm:
BEIJING SICHUANG DACHENG INTELLECTUAL PROPERTY AGENCY CO., LTD. (CN)
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