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US 2011/0212998 A1Published application
Pyridine derivatives as s1p1/edg1 receptor modulators
AssigneeActelion Pharmaceuticals Ltd.
InventorsMartin Bolli, Cyrille Lescop, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jorg Velker
Life of this patent
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Abstract
The invention relates to novel pyridine derivatives of formula (D, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I) wherein A represents and the other substituents are as defined in the claims.
Claims17
A compound of Formula (I).
- Pyridine1-A-Pyridine2 Formula (I)
- wherein
- Pyridine1 represents
- wherein the asterisks mark the bond with which the Pyridine1 ring is bound to A;
- R1 represents C1-5-alkyl, C1-4-alkoxy, C3-6-cycloalkyl, hydroxymethyl, or NR1aR1b;
- R1a represents C1-4-alkyl;
- R1b represents hydrogen, or C1-3-alkyl;
- or R1a and R1b, together with the nitrogen that is attached to the pyridine, form a pyrrolidine ring;
- R2 represents hydrogen, or C1-4-alkyl, or in case R1 represents C1-5-alkyl or C3-6-cycloalkyl, R2 may in addition represent methoxy;
- R3 represents C1-5-alkyl, C1-4-alkoxy, C3-6-cycloalkyl, or NR3aR3b;
- R3a represents C1-4-alkyl;
- R3b represents hydrogen, or C1-3-alkyl;
- R4 represents C1-4-alkyl, or hydrogen;
- R5 represents C1-5-alkyl, methoxy, or NR5aR5b;
- and R6 represents C1-2-alkyl;
- R5a represents C1-4-alkyl;
- R5b represents hydrogen, or C1-3-alkyl;
- or
- R5 represents C1-2-alkyl, or methoxy;
- and R6 represents C1-5-alkyl, or NR6aR6b;
- R6a represents C1-4-alkyl;
- R6b represents hydrogen, or C1-3-alkyl;
- R7 represents C1-5-alkyl;
- R8 represents C1-2-alkyl, or methoxy;
- R9 represents C1-5-alkyl;
- R10 represents C1-2-alkyl;
- A represents
- wherein the asterisks indicate the bond that is linked to the Pyridine1 ring;
- Pyridine2 represents
- wherein the asterisks mark the bond with which the Pyridine2 ring is bound to A;
- R11 represents C1-4-alkyl, C1-3-alkoxy, hydroxymethyl, or NR11aR11b;
- R11a represents C1-3-alkyl;
- R11b represents hydrogen, or C1-2-alkyl;
- R12 represents hydrogen, or C1-2-alkyl;
- R13 represents C1-4-alkyl, or NR13aR13b;
- R13a represents C1-3-alkyl;
- R13b represents hydrogen, or C1-2-alkyl;
- R14 represents C1-2-alkyl;
- R15 represents C1-2-alkyl, or NR15aR15b;
- and R16 represents C1-2-alkyl;
- R15a represents C1-3-alkyl;
- R15b represents hydrogen, or C1-3-alkyl;
- or
- R15 represents C1-2-alkyl;
- and R16 represents C1-4-alkyl, or NR16aR16b;
- R16a represents C1-3-alkyl;
- R16b represents hydrogen, or C1-2-alkyl;
- R17 represents C1-4-alkyl;
- R18 represents C1-2-alkyl, or methoxy;
- R19 represents C1-4-alkyl;
- and
- R20 represents C1-2-alkyl;
- with the exception of 3-(2-ethyl-4-pyridyl)-5-(2-ethyl-4-pyridyl)-1,2,4-oxadiazole;
- in free or salt form.
51 more elements
(canceled)
Dependencies are inferred from the claim text.