20896-27-9Relevant academic research and scientific papers
Copper-mediated etherification of arenes with alkoxysilanes directed by an (2-aminophenyl)pyrazole group
Selvakumar, Jayaraman,Grandhi, Gowri Sankar,Sahoo, Harekrishna,Baidya, Mahiuddin
, p. 79361 - 79365 (2016)
An efficient copper-mediated etherification of inert C-H bonds of (hetero)arenes with reagent-amounts of alkoxysilanes and alkanols has been developed using (2-aminophenyl)pyrazole (2-APP) as a removable directing group. The reaction is scalable, rapidly proceeds under an open atmosphere, and tolerates diverse functional groups to provide alkyl aryl ethers in high yields (up to 87%). As an application, the formal synthesis of anti-emetic drug metoclopramide is accomplished.
BICYCLIC HETEROARYL DERIVATIVES AS ECTONUCLEOTIDE PYROPHOSPHATASE PHOSPHODIESTERASE 1 INHIBITORS
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Paragraph 0325, (2020/10/21)
The present disclosure provides certain bicyclic heteroaryl compounds that inhibit ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) enzymatic activity and are therefore useful for the treatment of diseases and conditions modulated at least in part by ENPP1. In some embodiments, the bicyclic heteroaryl compounds includes those of Formula (I). Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Novel multitarget-directed ligands targeting acetylcholinesterase and σ1 receptors as lead compounds for treatment of Alzheimer's disease: Synthesis, evaluation, and structural characterization of their complexes with acetylcholinesterase
Lalut, Julien,Santoni, Gianluca,Karila, Delphine,Lecoutey, Cédric,Davis, Audrey,Nachon, Florian,Silman, Israel,Sussman, Joel,Weik, Martin,Maurice, Tangui,Dallemagne, Patrick,Rochais, Christophe
supporting information, p. 234 - 248 (2018/11/24)
Pleiotropic intervention may be a requirement for effective limitation of the progression of multifactorial diseases such as Alzheimer's Disease. One approach to such intervention is to design a single chemical entity capable of acting on two or more targets of interest, which are accordingly known as Multi-Target Directed Ligands (MTDLs). We recently described donecopride, the first MTDL able to simultaneously inhibit acetylcholinesterase and act as an agonist of the 5-HT4 receptor, which displays promising activities in vivo. Pharmacomodulation of donecopride allowed us to develop a novel series of indole derivatives possessing interesting in vitro activities toward AChE and the σ1 receptor. The crystal structures of complexes of the most promising compounds with Torpedo californica AChE were solved in order to further understand their mode of inhibition.
As neuroprotective agents of pharmaceutical compounds
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Paragraph 0694; 0695; 0696; 0697, (2019/06/26)
The invention discloses a medicinal compound as a neuroprotective agent. The medicinal compound is a neuronal nitric oxide synthase-postsynaptic density protein 95 (nNOS-PSD95) decoupling agent. The medicinal compound is a benzene ring derivative shown in the general formula (I) or its pharmaceutically acceptable salt. The invention further discloses a preparation method of the medicinal compound and a use of the medicinal compound in prevention and treatment on neuronal damage influence-caused diseases.
Synthetic method of 4-amino-5-chloro-2-methoxyl benzoic acid
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Paragraph 0025, (2016/10/27)
The invention discloses a synthetic method of 4-amino-5-chloro-2-methoxyl benzoic acid, wherein the synthetic method includes the steps of dimethyl sulphate methylation, N-chloro-succinimide chlorination, alkaline hydrolysis de-esterification and hydrochloric acid acidification to prepare an intermediate product, wherein aminosalicylic acid, which is low in cost and easy to obtain, is employed as a raw material. The synthetic method is reasonable and simple in process route design, is mild in reaction conditions, is easy to industrially operate, is low in costs of raw material and devices, is high in yield and product quality, and is effectively reduced in production cost.
HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
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Page/Page column 59, (2012/11/08)
Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
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Page/Page column 66, (2010/07/08)
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators.
Compounds having beta adrenergic receptor agonist and muscarinic receptor antagonist activity
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Page/Page column 30-31, (2008/06/13)
This invention provides compounds of formula I: wherein R1, R2, R4, R5, R6, R7, R8a, R8b, W, a, b, c and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both β2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Accordingly, such compounds are expected to be useful as therapeutic agents for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
COMPOUNDS HAVING β2 ADRENERGIC RECEPTOR AGONIST AND MUSCARINIC RECEPTOR ANTAGONIST ACTIVITY
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Page/Page column 76, (2008/06/13)
This invention provides compounds of formula I wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, W, a and b are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both β2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Accordingly, such compounds are expected to be useful as therapeutic agents for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
Crystalline form of a biphenyl compound
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Page/Page column 12, (2008/06/13)
The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.
