Back to results
US 8,044,076 B2Granted
Phenyl derivatives and their use as immunomodulators
AssigneeActelion Pharmaceuticals Ltd.
InventorsMartin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jorg Velker
Life of this patent
Estimating the term…
Abstract
The invention relates to phenyl derivatives of formula (I), their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
Claims19
A compound of the Formula (I),
- wherein the symbol # indicates the two carbon atoms of the phenyl ring bearing R1, R2 and R3 to either of which the group A may be attached;
- and wherein
- A represents
- wherein the asterisks indicate the bond that is linked to the phenyl ring of Formula (I) bearing R1, R2, and R3;
- R1 represents hydrogen, C1-3-alkyl, fluoro, chloro, methoxy, or cyano;
- R2 represents C2-5-alkyl or C1-4-alkoxy;
- R3 represents hydrogen, and if group A is attached to the para-position with respect to R2 of the phenyl ring of the Formula (I) bearing R1, R2, R3, then R3 is a H or methyl;
- R4 represents hydrogen;
- R5 represents methyl, ethyl or methoxy;
- R6 represents —(CH2—(CH2)k—NR61R62, —(CH2)nCH(OH)—CH2—NR61R62, —CH2(CH2)nNHSO2R63, —(CH2)nCH(OH)—CH2—NHSO2R63, —CH2—(CH2)n—NHCOR64, —(CH2)nCH(OH)—CH2—NHCOR64, hydroxy, hydroxy-C2-5-alkoxy, di-(hydroxy-C1-4-alkyl)-C1-4-alkoxy, 2,3-dihydroxypropoxy, 2-hydroxy-3-methoxy-propoxy, —OCH2—(CH2)m—NR61R62, —OCH2—CH(OH)—CH2—NR61R62, —OCH2—(CH2)mNHSO2R63, —OCH2—CH(OH)—CH2—NHSO2R63, —OCH2—(CH2)m—NHCOR64, or —OCH2—CH(OH)—CH2—NHCOR64;
- R61 represents hydrogen, C1-3-alkyl, 2-hydroxyethyl, 2-hydroxy-1-hydroxymethyl-ethyl, 2,3-dihydroxypropyl, carboxymethyl, 1-(C1-5-alkylcarboxy)methyl, 2-carboxyethyl, or 2-(C1-5-alkylcarboxy)ethyl;
- R62 represents hydrogen, methyl, or ethyl;
- R63 represents C1-3-alkyl, methylamino, ethylamino, or dimethylamino;
- R64 represents hydroxymethyl, 2-hydroxyethyl, 2-hydroxy-1-hydroxymethyl-ethyl, or 2,3-dihydroxypropyl;
- k represents the integer 1, 2, or 3;
- m represents the integer 1 or 2;
- n represents 0, 1, or 2;
- and
- R7 represents methyl, ethyl or halogen;
- in free or salt form.
17 more elements
Dependencies are inferred from the claim text.