Back to results
US 7,582,656 B2Granted
Guanidine derivatives and therapeutic uses thereof
AssigneeMerck Patent Gesellschaft
InventorsDidier Roche, Bruno Roux, Isabelle Berard
Life of this patent
Estimating the term…
Abstract
Compounds of the formula (I): in which the radicals R and R1 to R10 are as defined in the description, processes for the preparation of them, use thereof for the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.
Claims26
A compound of formula (I):
- wherein:
- R1 is in each case hydrogen, or (C1-C6)alkyl, or alternatively the two radicals R1 form, together with the carbon atom that bears them, (C3-C10)cycloalkyl;
- R2 is (C1-C10)alkyl, (C2-C10)alkenyl, (C6-C18)aryl(C1-C10)alkyl, (C1-C6)alkyl-O—(C1-C10)alkyl, or (C3-C10)cycloalkyl(C1-C10)alkyl;
- R3 and R4, which may be identical or different, are each, independently, hydrogen, (C1-C10)alkyl, (C2-C10)alkenyl, (C6-C18)aryl(C1-C10)alkyl, (C1-C6)alkyl-O—(C1-C10)alkyl, or (C3-C10)cycloalkyl(C1-C10)alkyl, or alternatively
- R3 and R4 form, together with the nitrogen atom that bears them, a 3- to 9-membered heterocycle;
- R5, R6, R7 and R8, which may be identical or different, are each, independently, hydrogen, (C1-C10)alkyl, a (C1-C10)alkenyl, (C1-C6)alkyl-O—;
- and
- R9 is hydrogen, and R10 is hydrogen or (C1-C6)alkyl, or alternatively
- R9 and R10 form, together with the nitrogen atom that bears them, a 3- to 7-membered heterocycle;
- wherein alkyl, aryl, and heterocyclic groups listed above are in each case unsubstituted or substituted one or more times by G;
- G is trifluoromethyl, styryl, halogen, Het which is unsubstituted or substituted one or more times by T, Het-CO— which is unsubstituted substituted one or more times by T, nitro, cyano, (C1-C10)alkyl, (C1-C10)alkylcarbonyl, (C1-C10)alkoxycarbonyl-A-, (C3-C10)cycloalkyl, trifluoromethoxy, di(C1-C10)alkylamino, (C1-C10)alkoxy(C1-C10)alkyl, (C1-C10)alkoxy, (C6-C18)aryl which is unsubstituted or substituted one or more times by T, (C6-C18)aryl(C1-C10)alkoxy-(CO)n— which is unsubstituted or substituted one or more times by T, (C6-C18)aryloxy(CO)n— which is unsubstituted or substituted one or more times by T, (C6-C18)arylthio in which aryl is unsubstituted or substituted one or more times by T, (C6-C18)aryloxy-(C1-C10)alkyl(CO)n— in which aryl is unsubstituted or substituted one or more times by T, monocyclic 5- to 8-membered heterocycle containing one or more hetero atoms chosen from O, N and S and which is unsubstituted or substituted one or more times by T, (C6-C18)aryl-carbonyl which is unsubstituted or substituted one or more times by T, (C6-C18)arylcarbonyl-B—(CO)n—, (C6-C18)aryl-C′—(CO)n— wherein aryl is unsubstituted or substituted one or more times by T, (C6-C18)aryl which is fused to a saturated or unsaturated heterocycle and which is unsubstituted or substituted one or more times by T, or (C2-C10)alkynyl;
- T is halogen, (C6-C18)aryl, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkoxy-(C6-C18)aryl, nitro, carboxyl, (C1-C6)alkoxycarboxyl, (C1-C6)alkoxy-carbonyl(C1-C6)alkyl, or (C1-C6)alkylcarbonyl((C1-C6)alkyl)n—, or T can also be oxo in the case where it substitutes a saturated or unsaturated heterocycle, or if two vicinal carbon atoms are substituted, T can also be a C1-C6 alkylenediyl chain or a C1-C6 alkylenedioxy chain;
- Het is a monocyclic, bicyclic or tricyclic aromatic heterocyclic radical containing one or more hetero atoms chosen from O, N and S;
- A is (C1-C6)alkylene, (C2-C6)alkenylene or a bond;
- n is 0 or 1;
- B represents (C1-C6)alkylene or (C2-C6)alkenylene and aryl is optionally substituted by one or more radicals T;
- and
- C′ represents (C1-C6)alkylene or (C2-C6)alkenylene;
- or
- an optical or geometrical isomer thereof, an oxide form thereof, a tautomeric form thereof;
- or a pharmaceutically acceptable addition salt thereof.
18 more elements
Dependencies are inferred from the claim text.