Abstract: The present invention relates to a process for the preparation of a N-(N?-substituted glycyl)-2-cyanopyrrolidine comprising at least (a) reacting, in the presence of dimethylformamide, a compound of formula (V) ?wherein, independently of each other, X1 and X3 are halogen; X2 is halogen, OH, O—C(?O)—CH2X3, —O—SO2—(C1-8)alkyl or 13 O—SO2-(aryl), ?with L-prolinamide, followed by (b) reacting the resultant compound without isolation with a dehydration agent, optionally followed by (c) reacting, in the presence of a base, the resultant compound without isolation with an appropriate amine and (d) recovering the resultant compound in free form or in acid addition salt form.
Abstract: Compounds of the formula (I) provide pharmacological agents which are inhibitors of the P450 enzyme, aldosterone synthase, and thus may be employed for the treatment of aldosterone mediated conditions. Accordingly, the compounds of formula (I) may be employed for prevention, delay of progression, or treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, fibrosis and remodeling following hypertension and endothelial dysfunction. Preferred are the compounds of formula (I) which are selective inhibitors of aldosterone synthase devoid of undesirable side effects due to general inhibition of cytochrome P450 enzymes.
Abstract: Compounds of the formula (I), wherein R1, R1–R7 and alk have meaning as defined, pharmaceutical compositions thereof, and use thereof for the treatment and/or prevention of cardiovascular disorders responsive to ACE and NEP inhibition and/or ECE inhibition.
Abstract: The present invention relates to a pharmaceutical composition, comprising (a) a phosphodiesterase 5 inhibitor or a pharmaceutically acceptable salt thereof and (b) at least one of the active ingredients selected from the group consisting of (i) an anti-diabetic agent; (ii) HMG-Co-A reductase inhibitors; (iii) an anti-hypertensive agent; and (iv) a serotonin reuptake inhibitor (SSRI) or, in each case, or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.