64328-73-0Relevant academic research and scientific papers
(THIO)MORPHOLINE DERIVATIVES AS S1P MODULATORS
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Page/Page column 25, (2011/04/14)
The present invention relates to (thio)morpholine derivatives of the formula (I), wherein R1 is selected from cyano, (2-4C)alkynyl, (1-4C)alkyl, (3-6C)cycloalkyl, (4-6C)cycloalkenyl, (6-8C)bicycloalkyl, (8-10C)bicyclic group, each optionally substituted with (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkyloptionally substituted with one or more fluoro atoms, (2-4C)alkynyl, (1-4C)alkoxy optionally substituted with one or more fluoro atoms,amino, di(1-4C)alkylamino, -SO2-(1-4C)alkyl, -CO-(1-4C)alkyl, -CO-O-(1-4C)alkyl, -NH-CO-(1-4C)alkyl and (3-6C)cycloalkyl, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, monocyclic heterocycle optionally substituted with halogen, (1-4C)alkyl or with phenyl optionally substituted with (1-4C)alkyl, and bicyclic heterocycle optionally substituted with (1-4C)alkyl; A is selected from -CO-O-, -O-CO-, -NH-CO-, -CO-NH, -C=C-, -CCH3-O- and the linking group –Y-(CH2)n-X- wherein Y is attached to R1 and selected from a bond, -O-, -S-, -SO-, -SO2-, -CH2-O-, -CO-, -O-CO-, -CO-O-, -CO-NH-, -NH-CO-, -C=C-and -C≡C-; n is an integer from 1 to 10; and X is attached to the phenylene / pyridyl group and selected from a bond, -O-, -S-, -SO-, -SO2 -, -NH, -CO-, -C=C-and -C≡C-; ring structure B optionally contains one nitrogen atom; R2 is H, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, or halogen; and R3 is (1-4C)alkylene-R5 wherein the alkylene group may be substituted with (CH2)2 to form a cyclopropyl moiety or one or two halogen atoms, or R3 is is (3-6C)cycloalkylene-R5 or -CO-CH2-R5, wherein R5 is -OH, -PO3H2, -OPO3H2, -COOH, -COO(1-4C)alkyl or tetrazol-5-yl; R4 is H or (1-4C)alkyl; R6 is one or more substituents independently selected from H, (1-4C)alkyl or oxo; W is -O-, -S-, -SO- or -SO2-; or a pharmaceutically acceptable salt, a solvate or hydrate thereof; with the proviso that the derivative of formula (I) is not 2-(4-ethylphenyl)-4-morpholinoethanol or 4-[4-(2-hydroxyethyl)-2-morpholinyl]benzeneacetonitrile or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.
Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists
Evindar, Ghotas,Bernier, Sylvie G.,Kavarana, Malcolm J.,Doyle, Elisabeth,Lorusso, Jeanine,Kelley, Michael S.,Halley, Keith,Hutchings, Amy,Wright, Albion D.,Saha, Ashis K.,Hannig, Gerhard,Morgan, Barry A.,Westlin, William F.
, p. 369 - 372 (2011/03/18)
In the design of potent and selective sphingosine-1-phosphate receptor agonists, we were able to identify two series of molecules based on phenylamide and phenylimidazole analogs of FTY-720. Several designed molecules in these scaffolds have demonstrated selectivity for S1P receptor subtype 1 versus 3 and excellent in vivo activity in mouse. Two molecules PPI-4621 (4b) and PPI-4691 (10a), demonstrated dose responsive lymphopenia, when administered orally.
METHODS AND COMPOSITIONS FOR MODULATING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR ACTIVITY
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Page/Page column 59; 61, (2010/10/20)
The present invention relates to compounds which modulate the activity of the SI P1 receptor, the use of these compounds for treating conditions associated with signaling through the S1 P1 receptor, and pharmaceutical compositions comprising these compounds.
PHENACYL ESTERS - A NEW TYPE OF LUQUID-CRYSTALLINE COMPOUND
Torgova, S. I.,Karamysheva, L. A.,Agafonova, I. F.
, p. 1162 - 1168 (2007/10/02)
The reaction of aliphatic, alicyclic, and aromatic acids with 4-substituted α-bromoacetophenones gave a series of new liquid-crystalline phenacyl esters.Their mesomorphous characteristics are discussed in relation to the structures of the acid and ketone parts of the molecule.
Synthese de derives du tetrathiafulvalene a proprietes mesomorphogenes
Polycarpe, Catherine,Torreilles, Eliane,Giral, Louis,Babeau, Annick,Tinh, Nguyen-Hun,Gasparoux, Henri
, p. 1741 - 1745 (2007/10/02)
We report the synthesis of di(4-alkoxyphenyl)- and di(4-alkanoyloxyphenyl)tetrathiafulvalenes.Their polymorphism has been investigated.
Transitions de Phase en Series Mesogenes: Les di TTF et les diTTF
Chann, N. B.,Cotrait, M.,Gautlier, J.,Haget, Y.,Tinh, Nguyen Huu,et al.
, p. 129 - 142 (2007/10/02)
The polymorphism of the di(4-alkylphenyl) and di(4-alkoxyphenyl) tetrathiafulvalene (TTF) is investigated by optical, crystallographic and calorimetric methods.All the studied derivatives are mesomorphic.The first mesophase is always a smectic G phase; th
