Factor VII -binding reagent
AssigneeNovo Nordisk A/S
InventorsLars Christian Petersen, Ole Hvilsted Olsen, Stefan Lutz Richter, Palle Jakobsen
Life of this patent
Estimating the term…
Abstract
The invention relates to novel compounds that potentiate zinc ion inhibition of the activity of factor VIIa or tissue factor--factor VIIa complex having the formula Ia and Ib and pharmaceutical salts thereof as well as pharmaceutical compositions comprising said novel compounds. The invention is further related to the use of said compositions for inhibiting clotting activity, tissue factor activity and factor VIIa activity.
Claims20
A compound of the general formula Ia ##STR27## Wherein M' is quinoxaline or a group of the formula ##STR28## or a group of the formula, ##STR29## M.sup.2 is quinoxaline or a group of the formula ##STR30## or a group of the formula ##STR31## Z.sup.1, Z.sup.2, Z.sup.3, and Z.sup.4, independently of each other are hydrogen, with the proviso that Z.sup.1 and Z.sup.3, and Z.sup.2 and Z.sup.4,respectively are not both hydrogen;
- C.sub.1-4 alkyl, hydroxy, or a valence bond attached to A,
- Z.sup.5 and Z.sup.6 represent a >C.dbd.O, which is attached to A,
- Y.sup.1 and Y.sup.2 independently of each other are a group of the formula --X.sup.1 .about.X.sup.2 .about.X.sup.3 --,
- wherein.about.independently of each other means a single or double bond, and X.sup.1 represents >C.dbd.O, >CHR.sup.5, >CH.sub.2, >CH-- or a valence bond, wherein R.sup.5 is hydrogen, C.sub.1-4 alkyl, amino,, C.sub.1-4 alkyl-amino, or di(C.sub.1-4 alkyl)amino, X.sup.2 represents --NH--, >N--, >CH.sub.2 or >CH-- and X.sup.3 represents --S--, >CH.sub.2, >CH-- or a valence bond,
- A is aryl or quinoxaline,
- p, a and s independently of each other are 0 or 1;
- with the provisos that a+p+s is at least 1 and pharmaceutically acceptable salts thereof.
A compound of the general formula Ib ##STR32## Wherein X is a chain, aliphatic or comprising hetero atoms as chain members;
- and R1 is hydrogen, a substituted or nonsubstituted amino group, or a methyl group;
- and R2 is hydrogen, or a methyl group;
- or X, in combination with C2, R1, R2, N1, and C3, forms a carbocyclic system;
- and
- wherein the distance between C1and C3 is from about 0.37 nm to about 0.77 nm;
- and pharmaceutically acceptable salts thereof;
- with the proviso that the compound is not L-cystine dihydroxamate.
Dependencies are inferred from the claim text.