The development of HEC-866 and its analogues for the treatment of idiopathic pulmonary fibrosis
Literature Information
Publication Date
2021-06-02
DOI
10.1039/D1MD00023C
Impact Factor
0
Authors
Runfeng Lin, Zheng Zhang, Shengtian Cao, Wen Yang, Yinglin Zuo, Xinye Yang, Jiancun Zhang, Juan Xu, Jing Li, Xiaojun Wang
View Original
Abstract
Idiopathic pulmonary fibrosis (IPF) is a chronic progressive lung disease with a typical survival time between three to five years. Two drugs, pirfenidone and nintedanib have been approved for the treatment of IPF, but they have limited efficacy. Thus, the development of new drugs to treat IPF is an urgent medical need. In this paper we report the discovery of a series of orally active pyrimidin-4(3H)-one analogs which exhibit potent activity in in vitro assays. Among them, HEC-866 showed promising efficacy in rat IPF models. Since HEC-866 also had good oral bioavailability, a long half-life and favorable long-term safety profiles, it was selected for further clinical evaluation.
Related Literature
Generalized approximate spin projection calculations of effective exchange integrals of the CaMn4O5 cluster in the S1 and S3 states of the oxygen evolving complex of photosystem II
H. Isobe, M. Shoji, S. Yamanaka, H. Mino, Y. Umena, K. Kawakami, N. Kamiya, J.-R. Shen
2014-02-21
Paper
DOI: 10.1039/C4CP00282B
Superbasicity of silylene derivatives achieved via non-covalent intramolecular cation⋯π interactions and exploited as molecular containers for CO2
Rabindranath Lo, Mrinal Kanti Si
2014-05-07
Paper
DOI: 10.1039/C4CP01394H
Dissolution of NaCl nanocrystals: an ab initio molecular dynamics study
Nico Holmberg
2014-03-26
Paper
DOI: 10.1039/C4CP00635F
Triplet–triplet annihilation photon-upconversion: towards solar energy applications
Victor Gray, Damir Dzebo, Maria Abrahamsson, Bo Albinsson, Kasper Moth-Poulsen
2014-04-08
Perspective
DOI: 10.1039/C4CP00744A
Photoluminescence of cerium fluoride and cerium-doped lanthanum fluoride nanoparticles and investigation of energy transfer to photosensitizer molecules
Daniel R. Cooper, Konstantin Kudinov, Pooja Tyagi, Colin K. Hill, Stephen E. Bradforth, Jay L. Nadeau
2014-05-08
Paper
DOI: 10.1039/C4CP01044B
New studies on molecular chirality in the gas phase: enantiomer differentiation and determination of enantiomeric excess
David Patterson
2014-04-10
Perspective
DOI: 10.1039/C4CP00417E
Why genetic modification of lignin leads to low-recalcitrance biomass
Paul Langan, Loukas Petridis
2014-11-11
Paper
DOI: 10.1039/C4CP05004E
Electrochemical conversion of CO2 to fuels: tuning of the reaction zone using suitable functional groups in a solid polymer electrolyte
Leela Manohar Aeshala, Ramagopal Uppaluri, Anil Verma
2014-06-09
Paper
DOI: 10.1039/C4CP02389G
Investigation of molecular partitioning between non polar oil droplets and aqueous solution using double potential step chronoamperometry
Jonathan C. Newland, Patrick R. Unwin, Julie V. Macpherson
2014-03-06
Paper
DOI: 10.1039/C4CP00231H
You might also like
Compound Q&A
What are the main uses of 1-(3-Aminophenyl)-3-[(3R)-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-(2-pyridinyl)-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]urea (CAS: 155412-88-7)?
This compound is mainly used as an intermediate in the synthesis of antipsychoti...
155412-88-71-(3-Aminophenyl)-3-...
Compound Q&A
How should waste containing 1-(D-Ribofuranosyl)-1,4-dihydro-3-pyridinecarboxamide (CAS: 19132-12-8) be handled?
Waste containing 1-(D-Ribofuranosyl)-1,4-dihydro-3-pyridinecarboxamide (CAS: 191...
19132-12-81-(D-Ribofuranosyl)-...
Compound Q&A
What regulatory guidelines apply to 2-Methyl-2-propanyl 3-bromo-3-(hydroxymethyl)-1-azetidinecarboxylate (CAS: 2007919-81-3)?
2-Methyl-2-propanyl 3-bromo-3-(hydroxymethyl)-1-azetidinecarboxylate (CAS: 20079...
2007919-81-32-Methyl-2-propanyl ...
Compound Q&A
What is N-(4-Chloro-2-pyridinyl)acetamide (CAS: 245056-66-0)?
N-(4-Chloro-2-pyridinyl)acetamide (CAS: 245056-66-0) is a chemical compound with...
245056-66-0N-(4-Chloro-2-pyridi...
Compound Q&A
What is 5-Chloro-2-hydroxybenzoic acid (CAS: 321-14-2)?
5-Chloro-2-hydroxybenzoic acid, also known as 5-chlorosalicylic acid, is an arom...
321-14-25-Chloro-2-hydroxybe...
Compound Q&A
What precautions should be taken when handling 1,1-Dichloro-1-fluoroethane (CAS: 1717-00-6)?
When handling 1,1-Dichloro-1-fluoroethane (CAS: 1717-00-6), it is important to u...
1717-00-61,1-Dichloro-1-fluor...
Compound Q&A
What are the physical and chemical properties of Fmoc-(2S,3R)-3-phenylpyrrolidine-2-carboxylic acid (CAS: 281655-32-1)?
Fmoc-(2S,3R)-3-phenylpyrrolidine-2-carboxylic acid is a white crystalline solid ...
281655-32-1Fmoc-(2S,3R)-3-pheny...
Compound Q&A
What are the main uses of 4-Amino-5-bromo-2-pyridinecarboxylic acid (CAS: 1363381-01-4)?
4-Amino-5-bromo-2-pyridinecarboxylic acid is primarily used as a precursor in th...
1363381-01-44-Amino-5-bromo-2-py...
Compound Q&A
What precautions should be taken when handling (S)-tert-butyl 2-((2-(4-bromophenyl)-2-oxoethyl)carbamoyl)pyrrolidine-1-carboxylate (CAS: 1007881-98-2)?
Handling this compound should be done with personal protective equipment (PPE) i...
1007881-98-2(S)-tert-butyl 2-((2...
Compound Q&A
What precautions should be taken when handling 8-bromo-2,2-dimethyl-3,4-dihydro-2H-1,4-benzoxazin-3-one (CAS: 688363-73-7)?
When handling 8-bromo-2,2-dimethyl-3,4-dihydro-2H-1,4-benzoxazin-3-one, use prop...
688363-73-78-bromo-2,2-dimethyl...
Source Journal
Recommended Compounds
![2,6-Bis({(2R)-2-[hydroxy(diphenyl)methyl]-1-pyrrolidinyl}methyl)-4-methylphenol structure](https://static.chemtradehub.com/structs/877/877395-58-9-70bf.webp "2,6-Bis({(2R)-2-[hydroxy(diphenyl)methyl]-1-pyrrolidinyl}methyl)-4-methylphenol structure")
2,6-Bis({(2R)-2-[hydroxy(diphenyl)methyl]-1-pyrrolidinyl}methyl)-4-methylphenol
CAS Number:
877395-58-9
Molecular Formula:
C43H46N2O3
2-(4-Chlorophenyl)-4-(dimethylamino)-2-(2-(dimethylamino)ethyl)butanenitrile
CAS Number:
1246816-57-8
Molecular Formula:
C16H24ClN3
Recommended Suppliers
Disclaimer
This page provides academic journal information for reference and research purposes only. We are not affiliated with any journal publishers and do not handle publication submissions. For publication-related inquiries, please contact the respective journal publishers directly.
If you notice any inaccuracies in the information displayed, please contact us at support@chemtradehub.com. We will promptly review and address your concerns.