Composition for treating respiratory and skin diseases, comprising at least one leukotriene antagonist and at least one antihistamine

A technology of leukotriene antagonists and antihistamines, which can be used in drug combinations, skin diseases, respiratory diseases, etc., and can solve problems such as ineffective treatments

Inactive Publication Date: 2001-02-07
SCHERING AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although leukotriene antagonists are effective in themselves, they are not very effective in the treatment of a variety of symptoms associated with

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0014] antihistamines

[0015] Descarboethoxyloratidine (DCL) is a non-sedative antihistamine, its chemical name is 8-chloro-6,11-dihydro-11-(4-piperidinylidene)-5H-benzo[5,6] Cyclohepta[1,2]pyridine. This compound is described in Quercia, et al., Hosp. Formul., 28:137-53 (1993), U.S. Patent 4,659,716 and WO96 / 20708. DCL is an antagonist of the H-1 histamine receptor protein. H-1 receptors are those that are counteracted by commonly used antihistamines to induce responses. H-1 receptors are present, for example, in the intestine, skin and bronchial smooth muscle of humans and other mammals. The amount of DCL used in a unit (ie single) dosage form of the composition of the present invention may be about 2.5 to about 20 mg, and about 5 to about 10 mg, preferably about 5 or 7.5 mg.

[0016] Cetirizine is an antihistamine whose chemical name is (±)-[2-[4-(p-chloro-α-phenylbenzyl)-1-piperazinyl]ethoxy] acetic acid. The pharmaceutically acceptable salt is preferably a hydrochl...

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PUM

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Abstract

A pharmaceutical composition useful in the treatment of sneezing, itching runny nose, nasal congestion, redness of the eye, tearing, itching of the ears or palate, shortness of breath, inflammation of the bronchial mucosa, reduced Forced Expiratory Volume In One Second (FEV1), coughs, rash, itchy skin, headaches, and aches and pains associated with seasonal allergic rhinitis, perennial allergic rhinitis, common colds, otitis, sinusitus, allergy, asthma, allergic asthma and/or inflammation, in a mammalian organism in need of such treatment. The composition comprises: i) an effective amount of at least one leukotriene antagonist selected from a) montelukast, b) 1-(((R)- (3-(2-(6,7- difluoro-2- quinolinyl)ethenyl) phenyl)-3-(2- (2-hydroxy-2- propyl)phenyl) thio)methylcyclopropaneacetic acid; c) 1-(((1(R)-3 (3-(2-(2,3- dichlorothieno[3, 2-b]pyridin-5-yl) -(E)-ethenyl)phenyl) -3-(2-(1-hydroxy-1- methylethyl) phenyl)propyl) thio)methyl) cyclopropaneacetic acid; d) pranlukast; or f) [2-[[2-(4-tert -butyl-2-thiazolyl) -5-benzofuranyl] oxymethyl]phenyl] acetic acid; or a pharmaceutically acceptable salt thereof; in admixture with ii) an effective amount of at least one antihistamine which is descarboethoxyloratidine, cetirizine, fexofenadine, ebastine, astemizole, norastemizole, epinastine, efletirizine or a pharmaceutically acceptable salt thereof.

Description

Background of the invention [0001] The present invention relates to compositions for treating allergic rhinitis and other allergic diseases. Products of the 5-lipoxygenase pathway of eicosatetraenoic acid metabolism, particularly leukotrienes, can lead to bronchoconstriction, mucus secretion, edema of the tracheal mucosa, chemotaxis and migration of cells into the inflamed trachea that occurs in asthma. Although leukotriene antagonists are effective in themselves, they are not very effective in the treatment of a variety of symptoms associated with respiratory diseases, such as seasonal allergic rhinitis, non-seasonal allergic rhinitis, common cold, sinusitis, and allergic asthma. complication. Symptoms of these disorders include sneezing, itching, runny nose, nasal congestion, bloodshot eyes, watery eyes, itchy ears or palate, and cough associated with postnasal drip. It is ideal for enhancing the effects of leukotriene antagonists, increasing their overall effectiveness. ...

Claims

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Application Information

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IPC IPC(8): A61K31/47A61KA61K31/327A61K31/352A61K31/404A61K31/4184A61K31/4365A61K31/445A61K31/4468A61K31/454A61K31/495A61K31/55A61P11/00A61P11/02A61P11/06A61P17/00A61P17/04A61P27/16A61P37/08A61P43/00
CPCA61K31/495A61K31/47A61K31/445A61K45/06A61K31/55A61P11/00A61P11/02A61P11/06A61P11/10A61P11/12A61P11/14A61P17/00A61P17/04A61P17/06A61P25/06A61P27/00A61P27/16A61P29/00A61P37/00A61P37/08A61P43/00A61K2300/00
Inventor P·K·詹森R·R·罗贝尔M·R·丹兹格P·T·梅代洛斯
Owner SCHERING AG
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