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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 (1104-1106, Silver Star Hi-tech Industrial Park No. 1301, Guanguang Rd., Guanlan St., Longhua Dis, Shenzhen Guangdong 0, 518000, CN)
YUAN, Zigao (1104-1106, Silver Star Hi-tech Industrial Park No. 1301, Guanguang Rd., Guanlan St., Longhua Dis, Shenzhen Guangdong 0, 518000, CN)
GAO, Chunmei (1104-1106, Silver Star Hi-tech Industrial Park No. 1301, Guanguang Rd., Guanlan St., Longhua Dis, Shenzhen Guangdong 0, 518000, CN)
CHEN, Shaopeng (1104-1106, Silver Star Hi-tech Industrial Park No. 1301, Guanguang Rd., Guanlan St., Longhua Dis, Shenzhen Guangdong 0, 518000, 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 INSTITUTE (1104-1106, Silver Star Hi-tech Industrial Park No. 1301, Guanguang Rd., Guanlan St., Longhua Dis, Shenzhen Guangdong 0, 518000, 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. (GAO Shuang, Room 408 Building B, Kingsway International Center, Building No. 1, Courtyard No. 8, Longyu North Street, Huilongguan Town, Changping District, Beijing 0, 102200, CN)
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