Substituted cycloalkyl derivatives for the treatment of respiratory diseases

摘要

N-(Phenyl-substituted cycloalkyl or cycloalkylmethyl)-phenylethanolamine derivatives (I) (including benzo-heterocyclic analogs) are new. Also new are cyclopropylamine or cyclopropylmethylamine derivative intermediates (II). Phenylethanolamine derivatives of formula (I) (including optical isomers, enantiomer mixtures and racemates) and their salts, solvates and hydrates are new. n : 0 or 1; m : 1-4; X : direct bond, 2-6C alkenylene, -O-Q-, -NH-Q-, -S-Q- or -Q-; Q : 1-6C alkylene; R 1>H; and R 3>hydroxyalkyl or halo; or R 1> + R 2>OCH 2CONH, CH 2CH 2CONH, CH=CHCONH, NHCH 2CONH, SCH 2CONH, OCONH, SCONH, NHCONH or OCH 2SO 2NH (all optionally substituted (os) by 1 or 2 of alkyl, OH or halo); R 3>, R 4>H, OH, halo, 1-6C alkyl, 1-6C haloalkyl, 1-6C hydroxyalkyl, NH 2 or mono- or dialkylamino; R 5> - R 8>H, OR 9>, halo, 1-6C alkyl, 1-6C haloalkyl, 1-6C hydroxyalkyl, 3-6C cycloalkyl, 3-6C hydroxycycloalkyl, CN, NO 2, COR 9>, COOR 9>, CONR 10>R 11>, NR 10>R 11>, NR 10>COR 9>, NR 10>SO 2R 12>, SR 12>, SOR 12>, SO 2R 12>, SO 2NR 10>R 11> or halo; or two vicinal groups R 6> - R 8> together= 2-6C alkylene, 2-6C alkenylene or O-Q-O (all os by 1 or 2 of alkyl, alkoxy, OH or halo); R 9> - R 11>H, alkyl, aryl or arylalkyl; R 12>alkyl, aryl or arylalkyl; unless specified otherwise alkyl moieties have 1-4C and aryl moieties 6-10C. An independent claim is included for cycloalkylamine or cycloalkylalkylamine derivative intermediates of formula (II) as new compounds, provided that m= 1. [Image] [Image] ACTIVITY : Antiinflammatory; antiasthmatic; antiallergic; virucide; antibacterial; fungicide; protozoacide; anthelmintic; cardiant; dermatological; immunosuppressive; tocolytic; antiarrhythmic; vasotropic; antipruritic. MECHANISM OF ACTION : beta -Mimetic.