IP Library › Granted Patent US 8,933,195
Granted Patent B2
US 8,933,195 · App. 13/980,308 · Granted Jan 13, 2015

Histone deacetylase inhibitors and synthetic method thereof and use thereof in manufacture of medicaments

Inventors: Sheng Jiang (Nanjing, CN); Shang Li (Nanjing, CN); Zhiyi Yao (Nanjing, CN); Yiwu Yao (Nanjing, CN); Feng Zhang (Nanjing, CN); Yang Chao (Nanjing, CN); Hai Ye (Nanjing, CN); Min Chen (Nanjing, CN)
Assignees: Nanjing Yoko Biomedical R & D Ltd.; Nanjing Xingang Medical Co., Ltd.; Nanjing Yoko Pharmaceutical Co., Ltd.
C07K5/0821C07F7/10C07F7/1852C07F7/1856A61K38/06
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Quick Facts
Patent No.
US 8,933,195
App. No.
13/980,308
Granted
Jan 13, 2015
Kind
B2
Abstract

The invention provides histone deacetylase (HDAC) inhibitors shown as Formula I, where R 1 to R 8 are as defined in the specification. The invention also provides methods for synthesis of these compounds and applications of these compounds in preparing pharmaceuticals for preventing or treating mammal diseases related to the dysregulation of HDAC.

Claims (13)

1. A cyclopeptide compound with a chemical structure shown as Formula I:

wherein,

R 1 is selected from the group consisting of hydrogen, C 1-12 alkyl, —CH 2 —O—(C 1-12 alkyl), —CH 2 —NH—(C 1-12 alkyl), —CH 2 —S—(C 1-12 alkyl), C 6-12 aryl, heteroaryl, —CH 2 —(C 6-12 aryl) and —CH 2 -heteroaryl;

wherein the C 6-12 aryl, the heteroaryl, the —CH 2 —C 6-12 aryl or the —CH 2 -heteroaryl optionally contains one or more substituents selected from the group consisting of halogen, amino, hydroxyl, nitro, cyano, C 1-12 alkyl, C 1-12 alkoxy, amino C 1-12 alkyl, acyl, acyloxy, thio C 1-12 alkyl, carboxyl and phenyl;

R 2 is hydrogen;

R 3 is methyl;

*** is a double bond;

R 4 is hydrogen or C 1-12 alkyl;

R 5 is hydrogen, C 1-12 alkyl or C 3-12 cycloalkyl;

R 6 , R 7 , and R 8 are hydrogen;

X is selected from the group consisting of,

wherein R 9 is hydrogen.

2. The cyclopeptide compound according to claim 1 , wherein the compound is selected from the following compounds:

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 7, 2016
From: NANJING YOKO BIOMEDICAL R & D LTD; NANJING XINGANG MEDICAL CO., LTD.; NANJING YOKO PHARMACEUTICAL CO., LTD.
To: NANJING YOKO BIOMEDICAL R&D LTD.; NANJING YOKO PHARMACEUTICAL CO., LTD.; NANJING YOKO PHARMACEUTICAL GROUP CO., LTD
Reel/Frame 037426/0087 →
Priority Claims (1)
CN 2011 1 0364545 · Nov 17, 2011 · national
Continuity (1)
Related Publication 20140243501A1 · Aug 28, 2014