| 摘要 |
The present application relates to prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of cardiovascular disorders. |
| 主权项 |
1. A method of treatment of a cardiovascular disorder selected from the group consisting of: hypertension, peripheral and cardiac vascular disorders, coronary heart disease, coronary restenosis, myocardial infarction, acute coronary syndrome, acute coronary syndrome with ST elevation, acute coronary syndrome without ST elevation, stable and unstable angina pectoris, myocardial insufficiency, princemetal angina, persistent ischemic dysfunction, temporary postischemic dysfunction, heart failure, tachycardia, atrial tachycardia, arrhythmias, atrial and ventricular fibrillation, persistent atrial fibrillation, permanent atrial fibrillation, atrial fibrillation with normal left ventricular function, atrial fibrillation with impaired left ventricular function, Wolff-Parkinson-White syndrome, disturbances of peripheral blood flow, elevated levels of fibrinogen and of low density LDL, and elevated concentrations of plasminogen activator inhibitor 1 (PAI-1) comprising administering an effective amount of a compound of the formula (I) in which RA is a group of the formula in which * means the point of linkage to the O atom, L1 and L2 are independently of one another a bond or —CH2—, R1, R2 and R3 are independently of one another hydrogen or methyl, R4 and R6 are identical or different and are independently of one another hydrogen or the side group of a natural α-amino acid or its homologs or isomers, R5 and R7 are independently of one another hydrogen or methyl, L3 is straight-chain or branched (C2-C4)-alkanediyl which is additionally substituted by amino, R8, R9 and R10 are independently of one another hydrogen or methyl, m is the number 2, 3, 4, 5 or 6, L4 is straight-chain or branched (C2-C4)-alkanediyl, which is additionally substituted by carboxyl, R11 is hydrogen or methyl, and n is the number 1, 2, 3 or 4, or a salt thereof to a human or animal in need thereof. |
