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Biphenyl derivatives

A kind of technology of compound and solvate, applied in the field of new biphenyl derivatives, can solve undisclosed and other problems

Active Publication Date: 2006-04-12
THERAVANCE BIOPHARMA R&D IP LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although with β 2 Compounds with adrenergic receptor agonist or muscarinic receptor antagonist activity are known, but have not previously been disclosed as having beta 2 Compounds with dual activity as adrenergic receptor agonists and muscarinic receptor antagonists

Method used

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  • Biphenyl derivatives
  • Biphenyl derivatives
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Examples

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Embodiment approach

[0081] The following substituents and values ​​are intended to provide representative examples of aspects and embodiments of the invention. These representative values ​​are to further define and explain these aspects and embodiments, and not to eliminate the scope of other embodiments or restricting the scope of the invention. In this regard, the recitation of a preference for a particular value or substituent is not intended in any way to exclude other values ​​or substituents from the invention unless specifically stated otherwise.

[0082] In a particular embodiment of the compound of formula I, a and b are independently 0, 1 or 2; In one embodiment, both a and b are 0.

[0083] When present, R 1 Each can be at the 2, 3, 4, 5 or 6-position of the phenyl ring to which it is attached. In one embodiment, R 1 Each is independently selected from (1-4C)alkyl, halogen, -OR 1a and-NR 1f R 1g ; For example, methyl, fluorine, chlorine, bromine, hydroxyl, methoxy, amino, methy...

preparation Embodiment A

[0562] Dry powders for administration by inhalation are prepared as follows:

[0563] Ingredient Amount

[0564] Compound of the present invention 0.2mg

[0565] Lactose 25mg

[0566] representative method : The compound of the present invention is micronized and mixed with lactose. This blended mixture is filled into gelatin inhalation cartridges. Administer the contents of the cartridge with a powder inhaler.

preparation Embodiment B

[0568] Dry powder formulations for use in dry powder inhalation devices are prepared as follows:

[0569] representative method : Preparation of a pharmaceutical composition in which the ratio of the micronized compound of the present invention to a lactose mixed preparation is 1:200. The composition is filled into a dry powder inhaler device capable of delivering about 10 μg to 100 μg of a compound of the invention per dose.

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Abstract

This invention provides biphenyl derivatives of formula I: wherein R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Description

Background of the invention [0001] field of invention [0002] The present invention relates to novel biphenyl derivatives useful in the treatment of pulmonary diseases. The present invention also relates to pharmaceutical compositions containing such biphenyl derivatives, methods and intermediates for preparing such biphenyl derivatives, and methods of using such biphenyl derivatives for the treatment of pulmonary diseases. [0003] technical status [0004] Lung diseases such as asthma and chronic obstructive pulmonary disease (COPD) are often treated with bronchodilators. A widely used class of bronchodilators consists of the beta 2 Adrenergic receptor (adrenergic receptor) agonists such as albuterol, formoterol, and salmeterol. These compounds are usually administered by inhalation. Another class of bronchodilators consists of muscarinic receptor antagonists (anticholinergic compounds), such as ipratropium and tiotropium. These compounds are also usually administe...

Claims

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Application Information

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IPC IPC(8): C07D401/02A61K31/4709C07D211/46C07D211/48C07D211/58C07D401/14C07D405/14C07D409/14C07D453/02
Inventor M·玛曼S·邓纳姆A·休斯李泰源C·休斯菲尔德E·斯坦格兰德陈燕
Owner THERAVANCE BIOPHARMA R&D IP LLC
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