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Sphingosine 1-phosphate receptor modulators and chiral synthesis methods
专利权人:
Celgene International II Sàrl
发明人:
MARTINBOROUGH, Esther,BOEHM, Marcus,YEAGER, Adam,TAMIYA, Junko,HUANG, Liming,BRAHMACHARY, Enugurthi,MOORJANI, Manisha
申请号:
ES10830877
公开号:
ES2665461T3
申请日:
2010.11.15
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound having the structure of the IR or IS Formulas or a pharmaceutically acceptable salt, hydrate or solvate thereof: ** (See formula) ** in which X is -NR'R "or -OR '' ' ; Y is -CN, -Cl, -CF3, I, -COOH or -COOR1; R 'is H, C1-4 alkyl, n-hydroxy C1-4 alkyl, -SO2-R1 or -CO-R1; R "is H, -SO2-R3, C1-4 alkyl optionally substituted with 1 or more R2, or a ring moiety optionally substituted with R4 wherein said ring moiety is piperidinyl, cyclohexyl, morpholinyl, thiazolyl, pyrazolyl, pyrrolidinyl, imidazolyl or phenyl ; or R 'and R "taken together with the nitrogen atom to which they are attached form a saturated 4, 5 or 6-membered heterocyclic ring containing 0 or 1 additional heteroatoms where said additional heteroatom is O or N where said heterocycle is optionally individually or multiple substituted with substituents independently selected from the group consisting of -OH, oxo, -NH2, n-hydroxy C1-4 alkyl, - COOH, - (CH2) m-COOH, - (CH2) m-COOR1, -N (R1R1) and - (CH2) m-CO-N (R5R5); R "'is H, C1-4 alkyl or -CO-R1; each R1 is independently C1-4 alkyl or H; each R2 is independently H, halo, OH, oxo,>; = NH, NH2, -COOH, F, -NHR1, -N (R5R5), - SO2-R1, -SO2- N (R5R5), -N (R1) -SO2-R1, -COOR1, -OCO-R1, -CO-N (R5R5), -N (R1) -COR1, C1-3alkyl, C1-3alkoxy and a ring moiety optionally substituted with R4 wherein said ring moiety is piperazinyl, piperidinyl, morpholinyl, pyrrolidinyl, pyrazolyl, imidazolyl, benzoimidazolyl, azetidinyl, cyclobutinyl or phenyl; each R3 is independently R2, C1-4 alkyl, C3-6 cycloalkyl or C1-4 alkyl optionally substituted with 1 or more R2; each R4 is independently halo, OH, -NH2, -NHR1, -N (R1R1), -COOH, -COOR1, -NHCO-R1; each R5 is independently C1-4 or H alkyl, or two R5 taken together with the nitrogen atom to which they are attached form a saturated 4, 5 or 6 membered heterocyclic ring containing 0 or 1 additional heteroatoms where said additional heteroatom is O or N wherein said heterocycle is optionally substituted with -OH, -NH2, -N
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