276872-81-2Relevant academic research and scientific papers
The development of HEC-866 and its analogues for the treatment of idiopathic pulmonary fibrosis
Cao, Shengtian,Li, Jing,Lin, Runfeng,Wang, Xiaojun,Xu, Juan,Yang, Wen,Yang, Xinye,Zhang, Jiancun,Zhang, Zheng,Zuo, Yinglin
, p. 1222 - 1231 (2021/11/02)
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, th
COMPOUNDS AND USES THEREOF
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Page/Page column 71, (2020/08/13)
The present invention features compounds useful in the treatment of neurological disorders and primary brain cancer. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders and primary brain cancer.
NITROGENOUS HETEROCYCLIC DERIVATIVES AND THEIR APPLICATION IN DRUGS
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Paragraph 00186; 00214, (2015/07/07)
The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, IPF, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.
Synthesis, evaluation and metabolic studies of radiotracers containing a 4-(4-[18F]-fluorobenzyl)piperidin-1-yl moiety for the PET imaging of NR2B NMDA receptors
Labas, Romain,Gilbert, Gwéna?lle,Nicole, Olivier,Dhilly, Martine,Abbas, Ahmed,Tirel, Olivier,Buisson, Alain,Henry, Jo?l,Barré, Louisa,Debruyne, Danièle,Sobrio, Franck
supporting information; experimental part, p. 2295 - 2309 (2011/06/21)
In this study, novel specific PET radioligands containing the 4-(4-fluorobenzyl)piperidine moiety and selectively antagonistic for the NR2B subunit containing NMDA receptors were developed. Two antagonists, RGH-896 (1a) and 4-(4-fluorobenzyl)piperidinyl-1
Piperidine-based heterocyclic oxalyl amides as potent p38α MAP kinase inhibitors
Mavunkel, Babu J.,Perumattam, John J.,Tan, Xuefei,Luedtke, Gregory R.,Lu, Qing,Lim, Don,Kizer, Darin,Dugar, Sundeep,Chakravarty, Sarvajit,Xu, Yong-jin,Jung, Joon,Liclican, Albert,Levy, Daniel E.,Tabora, Jocelyn
scheme or table, p. 1059 - 1062 (2010/06/14)
The design and synthesis of a new class of p38α MAP kinase inhibitors based on 4-fluorobenzylpiperidine heterocyclic oxalyl amides are described. Many of these compounds showed low-nanomolar activities in p38α enzymatic and cell-based cytokine TNFα produc
The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists
Ting, Pauline C.,Lee, Joe F.,Wu, Jie,Umland, Shelby P.,Aslanian, Robert,Cao, Jianhua,Dong, Youhao,Garlisi, Charles G.,Gilbert, Eric J.,Huang, Ying,Jakway, James,Kelly, Joseph,Liu, Zhidan,McCombie, Stuart,Shah, Himanshu,Tian, Fang,Wan, Yuntao,Shih, Neng-Yang
, p. 1375 - 1378 (2007/10/03)
Bipiperidine amide 1 has been identified as a CC chemokine receptor 3 (CCR3) antagonist. Optimization of its structure-activity relationship has resulted in the identification of cis (R,R)-4-[(3,4-dichlorophenyl)methyl]-3- hydroxymethyl-1′(6-quinolinylcar
CCR5 antagonists as anti-HIV-1 agents. Part 3: Synthesis and biological evaluation of piperidine-4-carboxamide derivatives
Imamura, Shinichi,Nishikawa, Youichi,Ichikawa, Takashi,Hattori, Taeko,Matsushita, Yoshihiro,Hashiguchi, Shohei,Kanzaki, Naoyuki,Iizawa, Yuji,Baba, Masanori,Sugihara, Yoshihiro
, p. 397 - 416 (2007/10/03)
Replacement of the 5-oxopyrrolidin-3-yl fragment in the previously reported lead structure with a 1-acetylpiperidin-4-yl group led to the discovery of a novel series of potent CCR5 antagonists. Introduction of small hydrophobic substituents on the central phenyl ring increased the binding affinity, providing low to sub-nanomolar CCR5 antagonists. The selected compound 11f showed excellent antiviral activity against CCR5-using HIV-1 replication in human peripheral blood mononuclear cells (EC50 = 0.59 nM) and an acceptable pharmacokinetic profile in dogs.
Cyclic amine compounds as CCR5 antagonists
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, (2008/06/13)
A compound of formula (I) (wherein R1is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1and R2may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Y?(R5is a hydrocarbon group; Y?is a counter anion); R3is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; R4is a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; G1is a bond, CO or SO2; G2is CO, SO2, NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent C1-3aliphatic hydrocarbon which may be substituted; provided that J is methine when G2is OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when G1is a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).
UREA COMPOUNDS, PROCESS FOR PRODUCING THE SAME AND USE THEREOF
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, (2008/06/13)
A compound of the formula: [whereinR1 is a hydrocarbon group which may be substituted;R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted;R3 is halogen atoms, a carbam
Heterocycyclic piperidines as modulators of chemokine receptor activity
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, (2008/06/13)
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
