Use of aminoalcohol derivatives, for the treatment of overactive bladder e.g. urge incontinence, stress incontinence, mixed incontinence, overactive bladder in the forms of wet overactive bladder or dry overactive bladder and dysuria

摘要

Use of aminoalcohol derivatives (A) and their acid addition salts, optionally in the form of the tautomers, racemates, enantiomers, diastereomers, solvates, hydrates, prodrugs, double prodrugs and/or their salts, for preparing a medicament for the treatment of overactive bladder. Use of aminoalcohol derivatives (A) of formula (I) or (II) and their acid addition salts, optionally in the form of the tautomers, racemates, enantiomers, diastereomers, solvates, hydrates, prodrugs, double prodrugs and/or their salts, for preparing a medicament for the treatment of overactive bladder. In formula (I), R 1, R 2, R 10, R 11-COR 7, -COOR 7, -CONR 7R 13, -OR 14, NR 13R 15, 1-10C alkyl, 3-8C cycloalkyl, -NR 16CX-R 17, -NR 18CX-OR 19, -NR 20SO mR 21, SO pNR 22R 23or -SO qR 24(all optionally substituted), H, halo, CN, NO 2or -NHCXNH 2; R 31-10C alkyl, 6-10C aryl, heterocyclyl or 3-8C cycloalkyl (all optionally substituted), H, -CX-1-10C alkyl or -CX-6-14C aryl; either R 4, R 5H, halo or 1-10 alkyl (all optionally substituted); or R 4R 53-8C alkyl bridge; R 6heterocyclic compounds of formula (a)-(i); R 25-R 28T, heteroaryl, -CX-R 17, -OR 14, NR 13R 15, 2-8C cycloalkyl, -NR 20SO mR 21, -SO pNR 22R 23, -SO qR 24, -NR 18CX-R 19, -NR 18CXOR 17(all optionally substituted), H, OH, halo, CN or NO 2(where R 25and R 26cannot simultaneously represent H); T : 1-10C alkyl, 6-18C aryl or heterocyclyl; R 8T, -SO q-1-10C alkyl, -SO q-6-14C aryl, -CX-1-10C alkyl, -CX-6-14C aryl, 6-10C aryl, 3-8C cycloalkyl (all optionally substituted) or H; R 91-10C alkyl, 6-14C aryl, heteroaryl, 3-8C cycloalkyl, heterocycloalkyl (all optionally substituted) or H; R 12benzyl, 1-12C alkyl, 6-14C aryl (all optionally substituted) or H; R 7, R 13, R 15, R 16, R 18, R 20, R 22, R 231-10C alkyl, 6-14C aryl, heterocyclyl, 3-8C cycloalkyl (all optionally substituted) or H; R 14, R 19, R 291-10C alkyl, 6-14C aryl, 3-8C cycloalkyl, heteroaryl, heterocyclyl, -CXNR 13R 15, -CXR 7(all optionally substituted) or H; R 171-10C alkyl, 6-14C aryl, heterocyclyl, heteroaryl or 3-8C cycloalkyl; R 21, R 24N(1-10C alkyl) 2, N(3-8C cycloalkyl), 1-10C alkyl, 6-14C aryl, heterocyclyl, heteroaryl, 3-8C cycloalkyl (all optionally substituted), H or OH; l,k : 1-3; m, p, q : 0-2; X : O, S or NR 29and n : 0-3; In formula (II) R 1aryl or heteroaryl (both optionally substituted); R 2heteroaryl or heterocyclyl (both optionally substituted), where R 2contains at least one nitrogen atom; either R 3, R 41-5C alkyl, 3-6C cycloalkyl, heterocyclyl, aryl or heteroaryl (all optionally substituted) or H; or R 3R 42-7 membered alkylene bridge; R 5-R 71-10C alkyl, alkenyl, alkynyl, 6-10C aryl, heterocyclyl, 3-8C cycloalkyl, -NR 8-1-5C-alkyl, -NR 8-aryl, halo, CN, -NR 8CO-(1-5C alkyl), -NR 8CO-aryl, -NR 8SO 2-(1-5C alkyl), -NR 8SO 2-aryl, -CO 2R 8, -SO 2R 8, -CONHR 8, -SO 2NHR 8or -OR 8(all optionally substituted), while the above-mentioned alkyl groups may each be substituted; and R 8H or 1-5C alkyl. [Image] [Image] [Image] [Image] ACTIVITY : Uropathic; Analgesic; Cytostatic; Antiinflammatory; Antimicrobial; Antibacterial; Gastrointestinal-Gen; Antidiarrheic. MECHANISM OF ACTION : Beta-3 receptor agonists.