Novel combinations

A technology for active ingredients, pharmaceutical products, applied in new combination fields, which can solve problems such as unsatisfactory efficacy

Inactive Publication Date: 2013-08-14
ASTRAZENECA AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although corticosteroid therapy can yield important benefits, the efficacy of t

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0309] Methoxyacetic acid (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluoromethyl)thio]carbonyl}-7-(6-fluoropyridine-3 -yl)-11-hydroxyl-2,10a,12a-trimethyl-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetrahydrocyclo Penta[5,6]naphtho[1,2-f]indazol-1-ester (Compound A)

[0310]

[0311] In a 250 mL round bottom flask Intermediate 5 (8.8 g, 17.07 mmol) was dissolved in DCM (80 mL) and triethylamine (5.91 mL, 42.67 mmol) was added. To the stirred mixture was added 2-methoxyacetyl chloride (3.89 g, 35.84 mmol) while cooling in a water bath, and the mixture was stirred for 10 minutes. Add N 1 -Ethyl-N 2 ,N 2 - Dimethylethane-1,2-diamine (3.48 mL, 22.19 mmol) and the mixture was stirred for another 10 minutes. A 60% solution of bromofluoromethane (4.82 g, 25.60 mmol) in DMF was added followed by triethylamine (2 ml) and the reaction mixture was stirred for a further 30 minutes. The resulting mixture was concentrated in vacuo and partitioned between EtOAc (150ml) and 1M H...

Embodiment 2

[0316] Inhibition of lipopolysaccharide (LPS)-induced TNFα production in human peripheral blood mononuclear cells

[0317] Peripheral blood mononuclear cells (PBMC) isolated from humans were treated with a range of concentrations of the GR agonist methoxyacetic acid (1R, 2R, 3aS, 3bS, 10aS, 10bR, 11S, 12aS)-10b-fluoro-1-{[( Fluoromethyl)thio]carbonyl}-7-(6-fluoropyridin-3-yl)-11-hydroxy-2,10a,12a-trimethyl-1,2,3,3a,3b,4,5 ,7,10,10a,10b,11,12,12a-tetrahydrocyclopenta[5,6]naphtho[1,2-f]indazole-1-ester (compound A) (alone or in a In the presence of a series of concentrations of a second compound with different pharmacological activity) pre-incubated at 37°C for 45 minutes. The second compound is selected from β 2 Adrenoceptor agonists, double beta 2 Adrenergic receptor agonists / M3 receptor antagonists (hereinafter referred to as "MABA compounds"), muscarinic antagonists or p38 kinase inhibitors. After a pre-incubation period, cells were then incubated with LPS (5 ng / mL) for ...

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Abstract

The invention provides a pharmaceutical product comprising, in combination, (1) a named glucocorticosteroid receptor agonist and (2) a beta2 adrenoreceptor agonist, a dual beta 2 adrenoreceptor agonist/M3 receptor antagonist, a muscarinic antagonist, a p38 kinase inhibitor, a neutrophil elastase inhibitor, a phosphodiesterase PDE4 inhibitor, an IKK2 kinase inhibitor or a non-steroidal glucocorticoid receptor agonist, and the use of said product in treating respiratory diseases.

Description

technical field [0001] The present invention relates to combinations of two or more pharmaceutically active substances for use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease (COPD) or asthma. Background technique [0002] The primary function of the lung requires extensive exposure of a fragile structure to an environment including pollutants, microorganisms, allergens, and carcinogens. Host factors stemming from the interaction of lifestyle choices and genetic makeup influence responses to the above exposures. Lung injury or infection can lead to many respiratory diseases (or respiratory diseases). Many of these diseases are of great 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] The most common ...

Claims

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Application Information

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IPC IPC(8): A61K31/58A61K31/44
CPCA61K45/06A61K9/0075A61K31/58A61K31/44A61P11/00A61P11/02A61P11/06A61K2300/00
Inventor P.R.汉森S.伊万诺娃F.伯坎普
Owner ASTRAZENECA AB
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