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US 2014/0371209 A1Published application
S1P Modulating Agents
AssigneeBiogen MA Inc.
InventorsJermaine Thomas, Sha Mi, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin Guckian, Gnanasambandam Kumaravel
Life of this patent
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Abstract
Compounds of formula (I) or (II) can modulate the activity of SIP receptors.
Claims32
A compound of formula (I):
- wherein:
- A1 is —CH═ or —N═;
- A2 is —CH═ or —N═;
- A3 is —CH2—, —CH═, or —N═;
- A4 is —CH2—, —CH═, or —N═;
- A5 is —CH2—, —CH═, or —N—;
- A6 is —CH═ or —N═;
- W is —O—, ═CR5—, or —CHR5—;
- R5 is hydrogen, halo, alkyl, or haloalkyl;
- Cy is a 4- to 7-membered cycloalkyl group, a 4- to 7-membered cycloalkenyl group, or Cy is a 4- to 7-membered heterocycloalkyl group having 1 heteroatom which is O;
- wherein Cy is optionally substituted by one to four R1;
- each R1, independently, is halo, alkyl, haloalkyl, hydroxyalkyl, cycloalkyl, trialkylsilyl, alkoxy, cycloalkoxy, alkoxyalkyl, cycloalkoxyalkyl, or aryl, or two R1, taken together, are C1 to C5 alkylene;
- L1 is —C(O)— or —C(R3)2—;
- each R3, independently, is hydrogen, alkyl, or haloalkyl;
- x is 0, 1, 2, 3, 4, or 5;
- y is 0, 1, 2, 3, 4, or 5;
- wherein the sum of x and y is 4 or 5;
- each Ra and each R1), independently, is hydrogen, halo, hydroxy, —CO2Rc, alkyl, or aryl;
- R2 is —(CH2)nCO2Rc, wherein n is 0 or 1;
- R1 is hydrogen, alkyl, haloalkyl, cycloalkyl, or aryl;
- provided that the compound is not 1-((2-(trans-4-tert-butylcyclohexyloxy)naphthalen-6-yl)methyl)piperidine-4-carboxylic acid, 1-((2-(trans-4-tert-butylcyclohexyloxy)naphthalen-6-yl)methyl)piperidine-3R-carboxylic acid, or 1-((2-(trans-4-tert-butylcyclohexyloxy)naphthalen-6-yl)methyl)piperidine-3S-carboxylic acid;
- or a pharmaceutically acceptable salt thereof.
19 more elements
Dependencies are inferred from the claim text.