57516-16-2Relevant articles and documents
PHD INHIBITOR COMPOUNDS, COMPOSITIONS, AND USE
-
Paragraph 0767-0768, (2021/09/26)
The present invention provides, in part, novel small molecule inhibitors of PHD, having a structure according to Formula (A), and sub-formulas thereof: or a pharmaceutically acceptable salt thereof. The compounds provided herein can be useful for treatment of diseases including heart ( e.g. ischemic heart disease, congestive heart failure, and valvular heart disease), lung (e.g., acute lung injury, pulmonary hypertension, pulmonary fibrosis, and chronic obstructive pulmonary disease), liver (e.g. acute liver failure and liver fibrosis and cirrhosis), and kidney (e.g. acute kidney injury and chronic kidney disease) disease.
Allosteric Inhibitors of SHP2 with Therapeutic Potential for Cancer Treatment
Xie, Jingjing,Si, Xiaojia,Gu, Shoulai,Wang, Mingliang,Shen, Jian,Li, Haoyan,Li, Dan,Fang, Yanjia,Liu, Cong,Zhu, Jidong
, p. 10205 - 10219 (2018/01/10)
SHP2, a cytoplasmic protein-tyrosine phosphatase encoded by the PTPN11 gene, is involved in multiple cell signaling processes including Ras/MAPK and Hippo/YAP pathways. SHP2 has been shown to contribute to the progression of a number of cancer types inclu
COMPOUNDS AND METHODS for the inhibition of HDAC
-
Paragraph 0696-0697, (2015/11/24)
Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.
Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors
Kono, Mitsunori,Matsumoto, Takahiro,Kawamura, Toru,Nishimura, Atsushi,Kiyota, Yoshihiro,Oki, Hideyuki,Miyazaki, Junichi,Igaki, Shigeru,Behnke, Craig A.,Shimojo, Masato,Kori, Masakuni
, p. 28 - 41 (2013/02/22)
A series of piperazine ureas was designed, synthesized, and evaluated for their potential as novel orally available fatty acid amide hydrolase (FAAH) inhibitors that are therapeutically effective against pain. We carried out an optimization study of the l
One-pot tandem copper-catalyzed library synthesis of 1-thiazolyl-1,2,3- triazoles as anticancer agents
Li, Wen-Tai,Wu, Wan-Hsun,Tang, Chien-Hsiang,Tai, Ready,Chen, Shui-Tein
, p. 72 - 78 (2011/04/17)
One-pot multicomponent synthesis to assemble compounds has been an efficient method for constructing a compound library. We have developed one-pot tandem copper-catalyzed azidation and CuAAC reactions that afford 1-thiazolyl-1,2,3-triazoles with anticancer activity. By utilizing this one-pot synthetic strategy, we constructed a library of 1-thiazolyl-1,2,3-triazoles in search of the potent lead compound. Furthermore, 1-thiazolyl-1,2,3-triazoles were evaluated for anticancer activity against the multidrug-resistant cancer cells MES-SA/Dx5. Most of the 1-thiazolyl-1,2,3-triazoles revealed cytotoxic effect against cancer cells at micromolar to low micromolar range. Testing some of the most potent compounds (5{4,2-4} and 5{5,1-3}) against the normal cell line Vero showed no significant toxicity (except 5{4,2}) to normal cells. This result indicates that compounds 5{4,3-4} and 5{5,1-3} possessed good potency and selectivity to cancer cells over normal cells.
Condensation reagents and a process for their preparation
-
, (2008/06/13)
The present invention relates to new bromo- and chlorothiazolium salts of the formula (I) in which R1, R2, R3, R4, n and X? have the meaning indicated in the disclosure, a process for their preparation, their use as condensation reagents, particularly as peptide coupling reagents, and intermediates for the preparation of these compounds.