530084-74-3Relevant academic research and scientific papers
Discovery of a novel class of inhaled dual pharmacology muscarinic antagonist and β2 agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD)
Rancati, Fabio,Linney, Ian D.,Rizzi, Andrea,Delcanale, Maurizio,Knight, Chris K.,Schmidt, Wolfgang,Pastore, Fiorella,Riccardi, Benedetta,Mileo, Valentina,Carnini, Chiara,Cesari, Nicola,Blackaby, Wesley P.,Patacchini, Riccardo,Carzaniga, Laura
supporting information, (2021/04/12)
The targeting of both the muscarinic and β-adrenergic pathways is a well validated therapeutic approach for the treatment of chronic obstructive pulmonary disease (COPD). In this communication we report our effort to incorporate two pharmacologies into a single chemical entity, whose characteristic must be suitable for a once daily inhaled administration. Contextually, we aimed at a locally acting therapy with limited systemic absorption to minimize side effects. Our lung-tailored design of bifunctional compounds that combine the muscarinic and β-adrenergic pharmacologies by the elaboration of the muscarinic inhibitor 7, successfully led to the potent, pharmacologically balanced muscarinic antagonist and β2 agonist (MABA) 13.
Carbamide derivative and preparation method thereof
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Paragraph 0203-0208, (2020/07/28)
The invention discloses a carbamide derivative and a preparation method thereof. The present invention relates to a compound represented by a general formula (I) or a stereoisomer, a hydrate, a metabolite, a solvate, a pharmaceutically acceptable salt, a co-crystal or a prodrug thereof, a preparation method and applications of the derivative in preparation of drugs for treatment of airway obstructive diseases; the compound represented by the general formula (I) is shown in the specification, and wherein definitions of substituents are consistent with those in the specification.
Muscarinic receptor m3 antagonist/beta2-adrenergic receptor stimulant bridge ring derivatives
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Paragraph 0521-0526, (2020/09/09)
The invention relates to bridged ring compounds shown in a general formula (III) and having dual activities of muscarinic receptor M3 antagonism and beta2-adrenergic receptor stimulation, or stereoisomers, hydrates, metabolites, solvates, pharmaceutically acceptable salts, eutectic crystals or prodrugs thereof. The invention also relates to a preparation method and application of the compounds inpreparation of drugs for treating airway obstruction diseases. Each substituent in the general formula (III) is as defined in the specification.
IMPROVED PROCESS FOR THE PREPARATION OF INDACATEROL MALEATE
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Page/Page column 9, (2020/10/19)
An improved process for the preparation of Indacaterol Maleate having the structural formula (I). The present invention also relates to an improved process for the preparation of benzyl intermediate of Formula IV. The present invention provides improved p
Synthesis method of indacaterol and salt derivatives thereof and intermediate for the synthesis
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Paragraph 0030-0032, (2019/10/01)
The invention belongs to the technical field of drug synthesis, and particularly relates to a synthesis method of indacaterol and salt derivatives thereof and intermediate for the synthesis. The synthesis method of indacaterol comprises the following steps: carrying out amine alkylation and deprotection reaction, in a one-pot manner, on a compound shown as a general formula IV and a compound shownas a formula V serving as raw materials to obtain a compound shown as a formula I, wherein the reaction equation is shown as the specification; wherein R is a silane protecting group. According to the technical scheme provided by the invention, by carrying out Boc protection on the amino group, polyalkylation on the amino group is ingeniously avoided, so that under the condition that both the hydroxyl group and the amino group have proper protection, the alkylation reaction effectively avoids the generation of by-products; after the alkylation reaction, hydroxyl and amino deprotection can bedirectly carried out, so that the multi-step reaction is completed in one reactor; according to the method, the intermediate purification and separation process is omitted, the reaction yield is increased to the maximum extent, and the production cost is reduced.
COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY
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Page/Page column 28; 30; 31, (2017/07/19)
The present invention relates to compounds acting both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists, to processes for their preparation, to compositions comprising them, to therapeutic uses and combinations with other pharmace
COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY
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Paragraph 0361; 0362; 0363, (2016/09/12)
Compounds of formula I, defined herein, act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for treating broncho-obstructive and inflammatory diseases.
COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY
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Page/Page column 39-40, (2016/12/22)
The present invention relates to compounds acting both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists, to processes for their preparation, to compositions comprising them, to therapeutic uses and combinations with other pharmaceutical active ingredients.
Novel Process for Preparation of Indacaterol or Its Pharmaceutically Acceptable Salts
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Paragraph 0069; 0070, (2016/11/28)
A novel process the for preparation of Indacaterol or its pharmaceutically acceptable salts and novel intermediates employed in the preparation thereof that is economically significant for large scale.
COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY
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Paragraph 0215-0217, (2014/06/24)
Compounds of formula (I) defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
