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Pharmaceutical product comprising a muscarinic receptor antagonist and a beta2-adrenoceptor agonist

A technology of receptor agonists and pharmaceutical products, applied in the direction of medical preparations containing active ingredients, drug combinations, pharmaceutical formulations, etc., can solve problems such as unsatisfactory drug efficacy

Inactive Publication Date: 2011-06-08
ASTRAZENECA AB +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Although using beta 2 Treatment with adrenoceptor agonists or muscarinic antagonists can yield important benefits, but efficacy of these drugs is often far from satisfactory

Method used

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  • Pharmaceutical product comprising a muscarinic receptor antagonist and a beta2-adrenoceptor agonist
  • Pharmaceutical product comprising a muscarinic receptor antagonist and a beta2-adrenoceptor agonist
  • Pharmaceutical product comprising a muscarinic receptor antagonist and a beta2-adrenoceptor agonist

Examples

Experimental program
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Effect test

preparation example Construction

[0164] Preparation of muscarinic antagonists

[0165] The muscarinic antagonists of the present invention can be prepared as follows. Alternative salts to those described in this application can be prepared by conventional chemistry using methods analogous to those described.

[0166] General Experimental Details for the Preparation of Muscarinic Antagonists

[0167] Unless specifically stated otherwise, the following general conditions were used in the preparation of muscarinic antagonists.

[0168] All reactions were performed under nitrogen atmosphere unless otherwise specified.

[0169] In the examples, NMR spectra were measured on a Varian Unity Inova spectrometer at a proton frequency of 300 or 400 or 500 MHz, or on a Bruker DRX spectrometer at a proton frequency of 400 or 500 MHz, or on a Bruker Avance spectrometer at a proton frequency of 600 MHz The measurements were made at a proton frequency of 300 MHz or on a Bruker Avance DPX 300 spectrometer. MS spectra wer...

Embodiment 1

[0199] Example 1: (R)-3-(1-phenyl-cycloheptanecarbonyloxy)-1-(pyrazin-2-ylcarbamoylmethyl)-1-nitrogen - Bicyclo[2.2.2]octane bromide

[0200] a) 1-Phenyl-cycloheptanol

[0201]

[0202] To a solution of magnesium (1.2 g) in anhydrous tetrahydrofuran (60 mL) was added crystals of iodine followed by bromobenzene (7.85 g) under nitrogen at such a rate that the reaction maintained a steady reflux. The reaction mixture was stirred for 20 minutes then cycloheptanone (4.48g) was added carefully. After stirring for 10 minutes, saturated aqueous ammonium chloride (10 mL) was added and the reaction mixture was partitioned between water (100 mL) and isohexane (100 mL). The organic layer was dried (MgSO 4 ) and evaporated to give the subtitle compound (7.6 g) as an oil.

[0203] 1 H NMR (299.946MHz, CDCl 3 )δ7.53-7.47(m, 2H), 7.36-7.29(m, 2H), 7.26-7.19(m, 1H), 2.07(ddd, 2H), 1.97-1.50(m, 11H).

[0204] b) 1-methoxy-1-phenyl-cycloheptane

[0205]

[0206] 1-Phenyl-cyclohept...

Embodiment 1

[0230] For Example 1: (R)-3-(1-phenyl-cycloheptanecarbonyloxy)-1-(pyrazin-2-ylcarbamoylmethyl)-1-nitrogen -Analysis of bicyclo[2.2.2]octane bromide crystal form A

[0231] The samples of crystal form A of Example 1 obtained by the above operation were analyzed by XRPD (PANalytical X'Pert or CubiX system), DSC and TGA.

[0232] The melting temperature (melting temperature) of bromide crystal form A of Example 1 determined by DSC was measured to be 202°C (initial) (±2°C). The observed weight loss by TGA prior to melting was 2.7%. GVS was determined to give a 3% weight gain (% w / w) at 80% RH (±0.2%).

[0233] The XRPD spectrum of embodiment 1 bromide crystal form A is in figure 1 displayed in .

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Abstract

The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a selected muscarinic receptor antagonist, and a second active ingredient which is a Beta2-adrenoceptor agonist, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.

Description

technical field [0001] The present invention relates to combinations of pharmaceutically active substances for the treatment of respiratory diseases, in particular chronic obstructive pulmonary disease (COPD) and asthma. Background technique [0002] The essential function of the lung requires a delicate structure to be exposed extensively to the environment including pollutants, microorganisms, allergens and carcinogens. Host factors arising from the interplay of lifestyle choices and genetic makeup influence the response to this exposure. Injury or infection to the lungs can produce a wide range of respiratory disorders (or respiratory diseases). Many of these diseases are of enormous public health importance. Respiratory diseases include acute lung injury, acute respiratory distress syndrome (ARDS), occupational lung disease, lung cancer, tuberculosis, fibrosis, pneumoconiosis, pneumonia, emphysema, chronic obstructive pulmonary disease (COPD), and asthma . [0003] T...

Claims

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Application Information

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IPC IPC(8): A61K31/439A61P11/06A61P11/08A61K31/428
CPCA61K45/06A61K31/439A61K31/428A61P11/00A61P11/06A61P11/08A61P43/00A61K2300/00
Inventor 理查德·布尔罗南·福特安德鲁·马瑟安东尼奥·梅特凯瑟琳·威利
Owner ASTRAZENECA AB
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