73792-08-2Relevant academic research and scientific papers
DIARYLTHIOHYDANTOIN COMPOUND AS ANDROGEN RECEPTOR ANTAGONIST
-
Paragraph 0192-0194, (2020/07/07)
The present application belongs to the field of medicine. In particular, the present application relates to a diarylthiohydantoin compound as an androgen receptor antagonist or a pharmaceutically acceptable salt thereof, a preparation method of the same, a pharmaceutical composition comprising the compound, and a use thereof in treating a cell proliferative disease mediated by androgen. The compound of the present application has good antagonistic effect on androgen receptor and exhibits excellent antitumor effect.
INDOLE DERIVATIVE USED AS CRTH2 INHIBITOR
-
Paragraph 0384-0385, (2019/06/07)
The present application discloses an indole as represented by formula (I) used as a CRTH2 inhibitor, and a pharmaceutically acceptable salt or tautomer of the indole, and an application of same in treating a disease related to a CRTH2 receptor.
Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist
Clarke, Earl,Jarvis, Christopher I.,Goncalves, Maria B.,Kalindjian, S. Barret,Adams, David R.,Brown, Jane T.,Shiers, Jason J.,Taddei, David M.A.,Ravier, Elodie,Barlow, Stephanie,Miller, Iain,Smith, Vanessa,Borthwick, Alan D.,Corcoran, Jonathan P.T.
supporting information, p. 798 - 814 (2018/01/01)
A ligand-based virtual screening exercise examining likely bioactive conformations of AM 580 (2) and AGN 193836 (3) was used to identify the novel, less lipophilic RARα agonist 4-(3,5-dichloro-4-ethoxybenzamido)benzoic acid 5, which has good selectivity over the RARβ and RARγ receptors. Analysis of the medicinal chemistry parameters of the 3,5-substituents of derivatives of template 5 enabled us to design a class of drug-like molecules with lower intrinsic clearance and higher oral bioavailability which led to the novel RARα agonist 4-(3-chloro-4-ethoxy-5-isopropoxybenzamido)-2-methylbenzoic acid 56 that has high RARα potency and excellent selectivity versus RARβ (2 orders of magnitude) and RARγ (4 orders of magnitude) at both the human and mouse RAR receptors with improved drug-like properties. This RARα specific agonist 56 has high oral bioavailability (>80%) in both mice and dogs with a good PK profile and was shown to be inactive in cytotoxicity and genotoxicity screens.
Compound and composition as well as application thereof to drugs preparation
-
Paragraph 0109; 0112-0114, (2019/01/08)
The present invention relates to a compound having a structure of formula I or a pharmaceutically acceptable salt of the compound. Regarding the compound, R1 is selected from hydrogen, fluorine, and chlorine; R2 and R3 are independently selected from hydr
Mechanistic Evaluation of Bioorthogonal Decaging with trans-Cyclooctene: The Effect of Fluorine Substituents on Aryl Azide Reactivity and Decaging from the 1,2,3-Triazoline
Matikonda, Siddharth S.,Fairhall, Jessica M.,Fiedler, Franziska,Sanhajariya, Suchaya,Tucker, Robert A. J.,Hook, Sarah,Garden, Anna L.,Gamble, Allan B.
, p. 324 - 334 (2018/02/28)
Bioorthogonal prodrug activation/decaging strategies need to be selective, rapid and release the drug from the masking group upon activation. The rates of the 1,3-dipolar cycloaddition between a trans-cyclooctene (TCO) and a series of fluorine-substituted
As CRTH2 inhibitor of indole compounds (by machine translation)
-
Paragraph 0237; 0238; 0239, (2018/05/16)
The application discloses a formula (I) as shown in CRTH2 inhibitor of indole compound or its pharmaceutically acceptable salt, and their use in the treatment with the CRTH2 receptor-related diseases in the application. (by machine translation)
THIAZOLIDINONE COMPOUNDS AND USE THEREOF
-
Paragraph 0133-0134, (2017/09/21)
A pharmaceutical composition containing a compound of Formula (I) for treating an opioid receptor-associated condition. Also disclosed is a method for treating an opioid receptor-associated condition using such a compound. Further disclosed are two sets of thiazolidinone compounds of formula (I): (i) compounds each having an enantiomeric excess greater than 90% and (ii) compounds each being substituted with deuterium.
SUBSTITUTED PYRAZOLYL-BASED CARBOXAMIDE AND UREA DERIVATIVES BEARING A PHENYL MOIETY SUBSTITUTED WITH A CO-CONTAINING GROUP AS VANILLOID RECEPTOR LIGANDS
-
, (2013/05/23)
The invention relates to substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with a CO-containing group as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
THERAPEUTIC ARYL-AM I DO-ARYL COMPOUNDS AND THEIR USE
-
Page/Page column 76, (2011/04/14)
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as "AAA compounds"), which, inter alia, a
The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators
Takahashi, Keiji,Hashimoto, Noriaki,Nakama, Chisato,Kamata, Kenji,Sasaki, Kaori,Yoshimoto, Riki,Ohyama, Sumika,Hosaka, Hideka,Maruki, Hiroko,Nagata, Yasufumi,Eiki, Jun-ichi,Nishimura, Teruyuki
experimental part, p. 7042 - 7051 (2010/01/06)
The optimization of a series of benzimidazole glucokinase activators is described. We identified a novel and potent achiral benzimidazole derivative as an allosteric GK activator. This activator was designed and synthesized via removal of the chiral center of the lead compound, 6-(N-acylpyrrolidin-2-yl)benzimidazole. The activator exhibited good PK profiles in rats and dogs, and significant hypoglycemic efficacy at 1 mg/kg po dosing in a rat OGTT model. The binding site and binding mode of the benzimidazole class of GKA with GK protein was confirmed by X-ray crystallographic analysis.
