Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF56 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although corticosteroid therapy can yield important benefits, the efficacy of these agents is often far from satisfactory, especially in the treatment of COPD

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Novel combinations
  • Novel combinations
  • Novel combinations

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 ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com