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Methods and compositions using norastemizole in combination with leukotriene inhibitors

a technology of leukotriene inhibitors and norastemizole, which is applied in the field of antihistamines and leukotriene inhibitors, can solve the problems of causing headache, nausea, headache, nausea, and zileuton, and achieves the effects of reducing or avoiding adverse effects, improving overall therapy, and potent antihistaminic activity

Inactive Publication Date: 2002-07-04
SEPACOR INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010] The compositions of the invention can be used to treat, prevent, or manage the disorders described herein while reducing or avoiding adverse effects associated with administration of other non-sedating antihistamines, such as astemizole.

Problems solved by technology

), however, the use of astemizole is believed to have a potential for serious cardiotoxicity in certain patients.
In some patients, zileuton was reported to cause headache, pain, asthenia, dyspepsia, nausea, and myalgia.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

5.1 Example 1

Preparation of Norastemizole

[0049] Norastemizole may be synthesized, for example, by the methods disclosed in U.S. Pat. Nos. 4,219,559 and 4,835,161, which are hereby incorporated herein by express reference thereto. Norastemizole may also be prepared by the reaction steps disclosed in WO 94 / 07495, published Apr. 14, 1994. Reaction of an isothiocyanate with phenylenediamine gives a corresponding thiourea. N-Alkylation with p-fluorobenzylbromide gives a secondary amine which, upon cyclization, yields a substituted benzimidazole. Treatment of the benzimidazole with base hydrolyzes the urethane moiety to give norastemizole. N-Alkylation of norastemizole with p-methoxyphenethyl bromide yields astemizole. Astemizole can be converted to desmethylastemizole by demethylation using, for example, a Lewis acid, such as boron trifluoride, boron trichloride, aluminum trichloride, and the like.

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Abstract

Methods and pharmaceutical compositions employing norastemizole and a leukotriene inhibitor for the treatment or prevention of inflammation or allergic disorders, such as asthma or the symptoms thereof. Also included are methods and compositions employing norastemizole and a decongestant for the treatment or prevention of inflammation or allergic disorders, such as asthma or the symptoms thereof.

Description

1. FIELD OF THE INVENTION[0001] The invention relates to methods of treating asthma, inflammation, and allergic conditions. In another aspect, this invention relates to the use of antihistamines and leukotriene inhibitors, and compositions containing them.2. BACKGROUND OF THE INVENTION[0002] Astemizole is an antagonist of the H-1 histamine receptor protein, which mediates the response antagonized by conventional antihistamines. Astemizole is well absorbed but is extensively metabolized. See Uchiyama et al., Pharmacometrics, 40:7793 (1990). Three main metabolites have been identified, all of which are reported to have some antihistaminic activity. See Kamei et al., Arzneimittel-Forschung / Drug Research, 41:932-36 (1991).[0003] Weintraub et al., Hosp. Formul., 22:918-27 (1987) describes clinical efficacy of astemizole in the treatment of both seasonal and perennial allergies. It has also been suggested that astemizole would be useful for the treatment of asthma.[0004] Astemizole is sol...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/454A61K45/06A61K9/00A61P11/06A61P17/00A61P27/16A61P29/00A61P37/08
CPCA61K45/06A61K31/445Y10S514/826A61P11/06A61P17/00A61P27/16A61P29/00A61P37/08
Inventor RUBIN, PAUL D.
Owner SEPACOR INC
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