Back to results
US 6,605,742 B2Granted
Cyclo azaphospha hydrocarbons
AssigneeLeo Pharma A/S
InventorsThomas Høyer, Morten Dahl Sørensen
Life of this patent
Estimating the term…
Abstract
Novel cyclo azaphospha hydrocarbons according to formula I are provided. The compounds are useful as metalloprotease inhibitors.
Claims9
A compound of the general formula I
- wherein bonds denoted a, b and c independently represents single or double bonds;
- m and n are independently 0, 1, 2 or 3, provided that m and n are not both 0;
- X is S or O;
- R1 is
- wherein E, when present represents a bond, methylene or ethylene optionally substituted with halogen, hydroxy, cyano, nitro, C1-4 alkyl, haloalkyl, hydroxyalkyl, alkoxy or alkylcarbonyl;
- s and t are independently 0, 1, 2 or 3;
- A and A′ independently represent a bond, or a saturated or unsaturated, optionally substituted cyclic or heterocyclic hydrocarbon di- or triradical;
- Y represents a bond, O, S, C(O)NR10, NR10C(O) or NR10, wherein R10 is hydrogen, hydroxy, branched or straight, saturated or unsaturated hydrocarbon diradical, optionally substituted with halogen, nitro, cyano, hydroxyl, alkoxy, alkylcarbonyl or alkylamino;
- R8 represents a bond, hydrogen, alkan or alken diradical, one or more ether diradicals (R′—O—R″) or amine diradicals (R′—N—R″), wherein R′ and R″ independently represent alkyl or alkenyl with a C-content from 0 to 3;
- R9 represents hydrogen, hydroxy, halogen, cyano, nitro, branched or straight, saturated or unsaturated hydrocarbon radical, optionally substituted with halogen, cyano, hydroxyl, alkoxy, alkylcarbonyl or alkylamino;
- NR11R12, C(O)NR11R12, C(O)R11R12, CO(O)R11R12, S(O)2R11, wherein each R11 and R12 independently represent hydrogen, halogen, a branched or straight, saturated or unsaturated hydrocarbon radical, optionally substituted with halogen, cyano, hydroxyl, alkoxy, alkylcarbonyl or alkylamino;
- R2 represents hydroxamic acid, carboxylic acid, phosphonic acid or a mercaptomethyl group;
- R3 and R4 each independently represent hydrogen, halogen, cyano, hydroxy, nitro, branched or straight, saturated or unsaturated alkane or alkene radical, optionally substituted with halogen, cyano, nitro, hydroxyl, alkoxy, alkylcarbonyl or alkylamino;
- or R3 and R4 together with the carbon atoms to which they are attached and the connecting nitrogen atom form a hetero cyclic ring;
- each R5, R6, and R7 independently represents hydrogen, hydroxy, nitro, cyano, halogen, branched or straight, saturated or unsaturated hydrocarbon radical, optionally substituted with halogen, cyano, nitro, hydroxyl, alkoxy, alkylcarbonyl or alkylamino;
- or R4 and R5, R5 and R6 or R6 and R7, together with the carbon atom to which they are attached form a saturated or unsaturated, optionally substituted cyclic or heterocyclic ring;
- and pharmaceutically acceptable salts thereof.
14 more elements
Dependencies are inferred from the claim text.