http://rdf.ncbi.nlm.nih.gov/pubchem/patent/JP-2013503141-A

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filingDate 2010-08-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2013-01-31-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-2013503141-A
titleOfInvention (Thio) morpholine derivatives as S1P modulators
abstract [Chemical 1] The present invention provides compounds of formula (I) wherein R1 is cyano, (2-4C) alkynyl, (1-4C) alkyl, (3-6C) cycloalkyl, (4-6C) cycloalkenyl, each optionally. Is (6-8C) bicycloalkyl substituted with (1-4C) alkyl, (8-10C) bicyclic group, halogen, optionally substituted with one or more fluoro atoms (1- 4C) alkyl, (2-4C) alkynyl, (1-4C) alkoxy, amino, di (1-4C) alkylamino, optionally substituted with one or more fluoro atoms, —SO 2 — ( 1-4C) alkyl, -CO- (1-4C) alkyl, -CO-O- (1-4C) alkyl, -NH-CO- (1-4C) alkyl and (3-6C) cycloalkyl. Phenoxy, benzyl, benzyloxy each substituted with phenyl, biphenyl, naphthyl, optionally substituted with (1-4C) alkyl, each optionally substituted with one or more substituents independently selected from Phenyl, substituted with phenylethyl or monocyclic heterocycle, halogen, (1-4C) alkyl, or (1-4C) alkyl optionally substituted with phenyl optionally substituted mono Selected from cyclic heterocycles, as well as bicyclic heterocycles optionally substituted with (1-4C) alkyl; A is —CO—O—, —O—CO—, —NH—CO—, Selected from —CO—NH, —C═C—, —CCH 3 —O— and the linking group —Y— (CH 2 ) n —X—, wherein Y is bound to R 1. And a bond, —O—, —S—, —SO—, —SO 2 —, —CH 2 —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 bonded to and bonded to a phenylene / pyridyl group, -O-, -S -, - SO -, - SO 2 -, - NH, -CO -, - C = C- and -C≡C- are selected from; ring structure B contains one nitrogen atom optionally R2 is H (1-4C) alkyl optionally substituted with one or more fluoro atoms, optionally substituted with one or more fluoro atoms (1-4C); Alkoxy, or halogen; and R3 is (1-4C) alkylene-R5 Ri, where the alkylene group (CH 2) 2 is substituted with either may form a cyclopropyl moiety, or one or two or may be substituted with a halogen atom, or R3 is (3-6C) cycloalkylene -R5 or a -CO-CH 2 -R5, where R5 is -OH, -PO 3 H 2, -OPO 3 H 2, -COOH, -COO (1-4C) an 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 -SO 2 - in which] the (thio) morpholine derivatives; or acceptable salts thereof as pharmaceutically relate to solvate or hydrate; however, the formula (I Is a derivative of 2- (4-ethylphenyl) -4-morpholinoethanol or 4- [4- (2-hydroxyethyl) -2-morpholinyl] benzeneacetonitrile or a pharmaceutically acceptable salt or solvate thereof. Or it is not a hydrate. The compounds of the present invention have affinity for the S1P receptor and can be used in the treatment, alleviation or prevention of diseases and conditions mediated by the S1P receptor.
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Total number of triples: 1462.