A method of treating an individual at risk of developing type 2 diabetes, or in the early stages thereof, so as to delay the onset and progression of the disease, which comprises the administration to the individual of repeated doses of an inhibitor of dipeptidyl peptidase IV or a prodrug thereof.
...
Compounds according to general formulae (1 and 2), wherein G<1> is an azepine derivative and G<2> is a group according to genera! formulae (9-11) are new. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.
...
Compounds according to general formula 1, wherein A1 - A3 are selected from A5 and A6 where A5 is either =CR13- or =N- and A6 is -NR14-, -O- or -S-; A4 is either a covalent bond or A5, provided that when A4 is a covalent bond one of A1 - A3 must be A6 and the other two must be A5 and when A4 is A5 then all of A1 - A...
This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V?1¿ and V?2¿ are both H, OMe or F, or one of V?1¿ and V?2¿ is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N¿3?, NH¿2?, NHBn or NH-acyl and the other is H, or V?1¿ and V?2¿ together are =O, -O(...
Compounds according to general formula (1), wherein G1 is NR5R6 or a fused polycyclic group are novel. They are selective and potent oxylocin agonists. Pharmaceutical compositions of such compounds are useful in the treatment of, inter alia, erectile dysfunction.
The present invention relates to a series of prodrugs of inhibitors of DP-IV with improved properties. The compounds can be used for the treatment of a number of human diseases, including impaired glucose tolerance and type II diabetes. The compounds of the invention are described by general formula (1); wherein R1 ...
. Compounds which are l-(2'-aminoacyl)-2-cyanopyrrolidine derivatives according to general formula (1) are DP-IV inhibitors for treatment of impaired glucose tolerance or type 2 diabetes; wherein A is selected from groups (2,3 and 4); X is selected from aminoacyl groups corresponding to the natural amino acids, acyl...
A compound of general formula 1 or a pharmaceutically acceptable salt thereof:
(Figure Removed)
wherein:
V is a covalent bond or NH,
X is selected from CH2, O and N-alkyl,
Z is either S or -CH=CH-,
R1 and R2 are independently selected from H, F, Cl, Br and alkyl,
R3 is selected from OH, O-alkyl and NR4R5
...
Inhibitors of dipeptidyl peptidase IV and pharmaceutical compositions comprising these inhibitors are useful in the treatment of short stature due to Growth Hormone deficiency and for promoting GH-dependent dssue growth or regrowth.
Compounds which are l-(2'-aminoacyl)-2-cyanopyrrolidine derivatives according to general formula (1) are DP-IV inhibitors for treatment of impaired glucose tolerance or type 2 diabetes; wherein A is selected from groups (2, 3 and 4); X is selected from aminoacyl groups corresponding to the natural amino acids, acyl...
Compounds according to formula (1), wherein R1 is H or CN, X1 is S,
O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing hetero-
cycle and n is 1-5 are new. The compounds of the invention are inhibitors of dipeptidyl
peptidase IV. Pharmaceutical compositions of the compounds of the invent...
Compounds according to general formula 1, wherein G1 is NR6R7or a group according to genera] formula 3 and G 2 is NR 24R25 or a fused polycyclic group are novel. They are selective and potent oxytocin agonists. Pharmaceutical compositions of such compounds are useful in the treatment of, inter alia, erectile dysfu...
Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R1 is H or CN, X1 is O, S, CH2, CHF, CF2, CH(CH3), C(CH3)2 or CH(CN), and b is 1 or 2. G1 is H or a group according to the formula -CH2-X2-(CH2)a-G3 and G2 is H or a gro...
The present invention concerns a new method of preparing granules comprising 5-aminosalicyclic acid and a new method of preparing an oral pharmaceutical composition for the treatment of ulcerative colitis or Crohn's disease comprising as active ingredient 5-aminosalicyclic acid, the method comprising granulation wit...
ABSTRACT OF THE DISCLOSURPeptides are provided which have improved duration of GnRH antagonistic properties. These antagonists may be used to regulate fertility and to treat steroid-dependent tumors and for other short-term and long-term treatment indications. These antagonists have a derivative of a...
Methods using and compositions including FSH for use in the treatment of infertility are described, wherein the dose is selected based on the patient's age to optimise cumulative efficiency and/or reduce OHSS risk.