Patent DE-102006003697-A1 (DE)
Title: 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
Inventor: MUELLER STEPHAN
IPC: A61P13/10
Filed: 2006-01-26
Abstract: 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 7>R 13>, -OR 14>, NR 13>R 15>, 1-10C alkyl, 3-8C cycloalkyl, -NR 16>CX-R 17>, -NR 18>CX-OR 19>, -NR 20>SO mR 21>, SO pNR 22>R 23>or -SO qR 24>(all optionally substituted), H, halo, CN, NO 2or -NHCXNH 2; R 3>1-10C 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 5>H, halo or 1-10 alkyl (all optionally substituted); or R 4>R 5>3-8C alkyl bridge; R 6>heterocyclic compounds of formula (a)-(i); R 25>-R 28>T, heteroaryl, -CX-R 17>, -OR 14>, NR 13>R 15>, 2-8C cycloalkyl, -NR 20>SO mR 21>, -SO pNR 22>R 23>, -SO qR 24>, -NR 18>CX-R 19>, -NR 18>CXOR 17>(all optionally substituted), H, OH, halo, CN or NO 2(where R 25>and R 26>cannot simultaneously represent H); T : 1-10C alkyl, 6-18C aryl or heterocyclyl; R 8>T, -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 9>1-10C alkyl, 6-14C aryl, heteroaryl, 3-8C cycloalkyl, heterocycloalkyl (all optionally substituted) or H; R 12>benzyl, 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 23>1-10C alkyl, 6-14C aryl, heterocyclyl, 3-8C cycloalkyl (all optionally substituted) or H; R 14>, R 19>, R 29>1-10C alkyl, 6-14C aryl, 3-8C cycloalkyl, heteroaryl, heterocyclyl, -CXNR 13>R 15>, -CXR 7>(all optionally substituted) or H; R 17>1-10C alkyl, 6-14C aryl, heterocyclyl, heteroaryl or 3-8C cycloalkyl; R 21>, R 24>N(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 29>and n : 0-3; In formula (II) R 1>aryl or heteroaryl (both optionally substituted); R 2>heteroaryl or heterocyclyl (both optionally substituted), where R 2>contains at least one nitrogen atom; either R 3>, R 4>1-5C alkyl, 3-6C cycloalkyl, heterocyclyl, aryl or heteroaryl (all optionally substituted) or H; or R 3>R 4>2-7 membered alkylene bridge; R 5>-R 7>1-10C alkyl, alkenyl, alkynyl, 6-10C aryl, heterocyclyl, 3-8C cycloalkyl, -NR 8>-1-5C-alkyl, -NR 8>-aryl, halo, CN, -NR 8>CO-(1-5C alkyl), -NR 8>CO-aryl, -NR 8>SO 2-(1-5C alkyl), -NR 8>SO 2-aryl, -CO 2R 8>, -SO 2R 8>, -CONHR 8>, -SO 2NHR 8>or -OR 8>(all optionally substituted), while the above-mentioned alkyl groups may each be substituted; and R 8>H 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.