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Compounds as s1p modulators and/or atx modulators
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A compound, R11 technology, applied in the field of compounds as S1P regulators and/or ATX regulators
Inactive Publication Date: 2018-08-17
BIOGEN MA INC
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However, this approach usually only delays rather than prevents the onset of disability in these patients
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Embodiment 1
[0914] Example 1: 4-(((6-(cyclohexyloxy)naphthalen-2-yl)methyl)amino)bicyclo[2.2.2]octane-1-carboxylic acid
[0917] Dissolve 6-hydroxy-2-naphthaldehyde (520mg, 3.02mmol, 1.0eq) and methyl 4-aminobicyclo[2.2.2]octane-1-carboxylate (663mg, 3.62mmol, 1.2eq) in toluene (100mL )middle. Magnesium sulfate (72 mg, 0.60 mmol, 0.2 equiv) was added to the solution and refluxed for 48 hours. Solvent was removed in vacuo. The residue was dissolved in THF (150 mL) and sodium cyanoborohydride (571 mg, 9.06 mmol, 3.0 equiv) was added. The mixture was refluxed for 24 hours. Solvent was removed in vacuo. Water (50 mL) was added to the residue and extracted with EtOAc (2 x 150 mL). The combined organic phases were washed with brine and washed with Na 2 SO 4 dry. The organic phase was concentrated to give methyl 4-(((6-hydroxynaphthalen-2-yl)methyl)amino)bicyclo[2.2.2]octane-1-car...
Embodiment 2
[0921] Example 2: 4-(((6-((trans-4-methylcyclohexyl)oxy)naphthalene-2-yl)methyl)amino)bicyclo[2.2.2]octane-1-carboxylic acid
[0922]
[0923] 4-(((6-((trans-4-methylcyclohexyl)oxy)naphthalene-2-yl)methyl)amino)bicyclo[2.2.2]octane-1-carboxylic acid and 4-( The preparation of ((6-(cyclohexyloxy)naphthalen-2-yl)methyl)amino)bicyclo[2.2.2]octane-1-carboxylic acid was the same. 34 mg, white solid, yield: 27% (two steps). ESI-MS(M+H) + :422.3. 1 H NMR (400MHz, CD 3 OD)δ:7.78(s,1H),7.74(d,J=8.8Hz,1H),7.69(d,J=9.2Hz,1H),7.37(dd,J=8.4,2.0Hz,1H),7.17 (d,J=2.0Hz,1H),7.07(dd,J=9.2,2.4Hz,1H),4.32-4.25(m,1H),4.14(s,2H),2.11-2.07(m,2H), 1.94-1.88 (m, 12H), 1.74-1.71 (m, 2H), 1.41-1.39 (m, 3H), 1.09-1.06 (m, 2H), 0.86 (d, J=6.8Hz, 3H).
Embodiment 3
[0924] Example 3: 4-(((6-((trans-4-ethylcyclohexyl)oxy)naphthalene-2-yl)methyl)amino)bicyclo[2.2.2]octane-1-carboxylic acid
[0925]
[0926] 4-(((6-((trans-4-ethylcyclohexyl)oxy)naphthalene-2-yl)methyl)amino)bicyclo[2.2.2]octane-1-carboxylic acid and 4-( The preparation of ((6-(cyclohexyloxy)naphthalen-2-yl)methyl)amino)bicyclo[2.2.2]octane-1-carboxylic acid was the same. 36 mg, white solid, yield: 28% (two steps). ESI-MS(M+H) + :436.2. 1 H NMR (400MHz, CD 3 OD)δ:7.89(s,1H),7.85(d,J=8.4Hz,1H),7.80(d,J=9.2Hz,1H),7.48(dd,J=8.8,2.0Hz,1H),7.28 (d,J=2.8Hz,1H),7.18(dd,J=8.8,2.4Hz,1H),4.43-4.39(m,1H),4.26(s,2H),2.25-2.21(m,2H), 2.05-1.99(m,12H),1.92-1.89(m,2H),1.48-1.45(m,2H),1.33-1.28(m,3H),1.19-1.13(m,2H),0.95(t,J =7.2Hz, 3H).
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Abstract
Compounds of formula (I) can modulate the activity of one or more S1P receptors and / or the activity of autotaxin (ATX).
Description
[0001] priority claim [0002] This application claims priority to US Provisional Application Serial No. 61 / 676,692, filed July 27, 2012, which is hereby incorporated by reference in its entirety. technical field [0003] The present invention relates to compounds that are S1P modulators and / or ATX modulators and methods of making and using such compounds. Background technique [0004] Sphingosine-1-phosphate (S1P) is a lysophospholipid mediator that elicits a variety of cellular responses by stimulating five members of the endothelial differentiation gene (EDG) receptor family. EDG receptors are G protein-coupled receptors (GPCRs) and upon stimulation by activation of heterotrimeric G protein α (G α ) subunit and β-γ (G βγ ) dimers to propagate second messenger signals. Ultimately, this S1P-driven signaling leads to cell survival, increased cell migration and generally mitosis. The recent development of agonists targeting the S1P receptor has provided an understanding o...
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