New formamide derivatives are beta2-receptor agonists, useful to treat e.g. asthma, chronic obstructive pulmonary disease, bronchitis, chronic or acute bronchoconstriction and adult respiratory distress syndrome

摘要

Formamide derivatives (I) and their salts and solvates are new. Formamide derivatives of formula (I) and their salts and solvates are new. R 1, R 2H or 1-4C alkyl; n : 0-2; Q 1phenyl compounds of formula (Ia) (where the group is optionally bridged by one carbon atom), indane compound of formula (Ib), *-piperidine or amine compound (If) of formula (*-NR 8-Q 2-A); p, q : 1-2; A : pyridyl, 3-10C cycloalkyl, 2-3 carbon atoms of the cycloalkyl (optionally bridged by 1-4 (1-4C alkyl), where alkylene bridge is optionally branched), tetrahydropyranyl, piperidinyl or tetrahydrothiopyranyl or phenyl compounds of formula (Ic) or (Id); R 3-R 7H, 1-4C alkyl, OR 9, SR 9, SOR 9, SO 2R 9, halo, CO 2R 9, CF 3, CN, OCF 3, SO 2NR 9R 10, CONR 9R 10, NR 9R 10, NHCOR 10 or phenyl (optionally substituted with 1-3 OR 9, halo or 1-4C alkyl; R 9, R 10H or 1-4C alkyl; and * : attachment point to the carbonyl group. Provided that the (CH 2) n-C(=O)Q 1 group is in meta or para position. [Image] ACTIVITY : Antiasthmatic; Antiallergic; Antiinflammatory; Respiratory-Gen.; Antibacterial; Fungicide; Protozoacide; Virucide; Tocolytic; Cardiovascular-Gen.; Antidepressant; Antipsoriatic; Cytostatic; Ophthalmological. MECHANISM OF ACTION : beta 2-Receptor agonist. The ability of (I) to agonize beta 2-receptor was tested using biological assays. The results showed that N-benzyl-2-(3-{2-[(2R)-2-(3-formylamino-4-hydroxyphenyl)-2-hydroxyethylamino]-2-methylpropyl}phenyl)acetamide exhibited a median effective concentration value of 5 nM.