913642-85-0Relevant academic research and scientific papers
BENZIMIDAZOLE DERIVATIVES, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
-
Page/Page column 36, (2022/02/24)
The present disclosure relates to benzimidazole derivatives, a preparation method therefor and a medical use thereof. Specifically, the present disclosure relates to a benzimidazole derivative represented by the general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and its use as a therapeutic agent, in particular its use for the treatment of diseases related to P2X3 activity.
HETEROCYCLIC COMPOUND INTERMEDIATE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
-
Paragraph 0395-0397, (2021/10/07)
Disclosed by the invention is a heterocyclic compound, an intermediate, and a preparation method therefor and an application thereof. Provided by the invention are a heterocyclic compound as shown in formula I, and a stereoisomer, a geometric isomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, an ester, a pharmaceutically acceptable salt or a prodrug thereof. The heterocyclic compound hasa high P2X3 antagonistic activity, and has good selectivity, low toxicity, good metabolic stability and little taste influence.
PREPARATION OF A P2X3 ANTAGONIST
-
Paragraph 00111; 00127, (2021/08/20)
Described herein are two processes for the preparation of methyl (5)-2-((2-(2,6-difLuoro-4-(methylcarbamol)phenyl)-7- methylimidaz[1,2-a]pyridine-3-yl)methyl)morpholine-4-carboxylate, a P2X3 antagonist, in a stepwise manner and chemical intermediates used in the synthetic processes.
IRAK DEGRADERS AND USES THEREOF
-
Paragraph 00962; 001229-001231; 001261-001263; 004941-004943, (2020/06/19)
The present invention provides compounds, compositions thereof, and methods of using the same.
IRAK DEGRADERS AND USES THEREOF
-
Paragraph 00920; 001806-001808, (2021/01/23)
The present invention provides compounds, compositions thereof, and methods of using the same. The compounds include an IRAK binding moiety capable of binding to IRAK4 and a degradation inducing moiety (DIM). The DIM could be DTM a ligase binding moiety (LBM) or lysine mimetic. The compounds could be useful as IRAK protein kinase inhibitors and applied to IRAK mediated disorders.
4 - Methyl dihydro pyrimidine compounds and their use in medicine
-
Paragraph 0426; 0428-0430, (2019/04/30)
The invention relates to a 4-methyl dihydropyrimidine compound and an application thereof as a drug, especially a drug used for treating and preventing hepatitis B, and in particular relates to a compound shown in a general formula (I) or general formula (Ia) in the specification or enantiomers, diastereoisomers, tautomers, hydrates, solvates or pharmaceutically acceptable salts of the compound. All the variables are defined in the specification. The invention also relates to an application of the compound shown in the general formula (I) or general formula (Ia) in the specification or the enantiomers, diastereoisomers, tautomers, hydrates, solvates or pharmaceutically acceptable salts of the compound as drugs, especially drugs used for treating and preventing hepatitis B.
IRAK DEGRADERS AND USES THEREOF
-
Paragraph 3709; 3710, (2019/07/10)
The present invention provides compounds, compositions thereof, and methods of using the same.
BENZO[B]FURANS AS BROMODOMAIN INHIBITORS
-
Page/Page column 73, (2017/11/06)
The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
IMIDAZOPYRIDINE COMPOUNDS AND USES THEREOF
-
Paragraph 218, (2014/08/19)
This invention generally relates to substituted imidazopyridine compounds, particularly substituted 4-(imidazo[1,2-a]pyridin-2-yl)benzamide compounds and salts thereof. This invention also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), processes for making such a compound, and intermediates used in such processes.
The design and synthesis of novel, potent and orally bioavailable N-aryl piperazine-1-carboxamide CCR2 antagonists with very high hERG selectivity
Cumming, John G.,Bower, Justin F.,Waterson, David,Faull, Alan,Poyser, Philip J.,Turner, Paul,McDermott, Benjamin,Campbell, Andrew D.,Hudson, Julian,James, Michael,Winter, Jon,Wood, Christine
scheme or table, p. 3895 - 3899 (2012/07/03)
A novel N-aryl piperazine-1-carboxamide series of human CCR2 chemokine receptor antagonists was discovered. Early analogues were potent at CCR2 but also inhibited the hERG cardiac ion channel. Structural modifications which decreased lipophilicity and basicity resulted in the identification of a sub-series with an improved margin over hERG. The pharmacological and pharmacokinetic properties of the lead compound from this series, N-(3,4-dichlorophenyl)-4-[(2R)-4-isopropylpiperazine-2-carbonyl] piperazine-1-carboxamide, are described.
