.alpha.-hydroxy thioethers

C - Chemistry – Metallurgy – 07 – K

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C07K 5/06 (2006.01) A61K 31/19 (2006.01) A61K 31/215 (2006.01) C07C 323/51 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1303294

- 1 - 21489-7051 4-15653/+/ZFO .alpha.-Hydroxy thioethers Abstract Novel asymmetric thioethers of the formula Image (I) in which the general symbols have the following meanings: a is an integer of from 1 to 7, R0 represents hydrogen or C1-7-alkanoyl, R1 represents C1-3-alkyl which may be substituted at the terminal carbon atom by hydroxy, by benzoyloxy, or by lower alkanoyl, by a halogen atom having an atomic number of at most 17, or by methoxy, or represents C1-3-perfluoroalkyl, R2 represents an aliphatic radical having from 5 to 15 carbon atoms, A represents ethylene or alternatively, is R1 represents a halogenated radical and/or B repre- sents phenylene or ethenylene, a single bond or vinylene, B represents a single bond, ethynylene or phenylene, R3 represents hydroxy, C1-7-alkoxy or an optionally substituted amino group of the formula Image (R?) wherein R? denotes hydrogen or C1-5-alkyl group, R? is hydroxy, C1-7-alkoxy or amino, and - 2 - 21489-7051 -X- represents a single bond, a methylene group or an optionally N-acylated primary aminomethylene group of the formula R4-NH-CH- (-X0-) wherein R4 is hydrogen, lower alkanoyl or not more than 7 carbon atoms or trifluoroacetyl, and salts of such compounds having salt-forming properties, are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by laucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.

524509

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