Marcus, F.,Маркус Эф,Esther,Эстер,Enugurthi,Ингурти,Manisha,Маниша,Junko,Юнко,Liming,Лиминг,Adam, Richard,Адам Ричард
申请号：
EA201290329
公开号：
EA025672B1
申请日:
2010.11.15
申请国别(地区):
EA
年份:
2017
代理人:
摘要：
Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor, having the following structural formula:wherein a dashed line signifies that a single bond or a double bond can be present, provided that there are two double bonds and three single bonds in the ring comprising A1, A2 and A3 A1, A2 and A3 each independently is C or S or N provided that one of A1, A2 and A3 is S R1 is di-substituted phenyl where the phenyl substituents are each independently selected from the group consisting of halo, nitro, cyano, perfluromethyl, fluorinated methyl and C1-4-alkoxy provided that phenyl is para-substituted with C1-4-alkoxy R2 iswherein a wavy line indicates a point of attachment X is NRR" or -OR" R is H, C1-4-alkyl, n-hydroxy C1-4-alkyl, -SO2-R3 or -CO-R3 R" is H, -SO2-R5, C1-4-alkyl optionally substituted with 1 or more R4, or a ring moiety optionally substituted with R6, wherein such ring moiety is piperidinyl, cyclohexyl, morpholinyl, thiazolyl, pyrazolyl, pyrrolidinyl, imidazolyl or phenyl R" is H, C1-4-alkyl or -CO-R3 or R and R" taken together with the nitrogen atom to which they are bound form a 4-, 5- or 6-membered saturated heterocyclic ring containing 0 or 1 additional heteroatom, where such additional heteroatom is O or N, wherein such heterocycle is optionally singly or multiply substituted with substituents independently selected from the group consisting of -OH, oxo, -NH2, n-hydroxy- C1-4-alkyl, -COOH, -(CH2)m-COOH, -(CH2)m-COOR3, -N(R3R3) and -(CH2)m-CO-N(R7R7) each R3 is independently C1-4-alkyl or H each R4 is independently H, halo, OH, oxo, =NH, NH2, -COOH, F, -NHR3, -N(R7R7), -SO2-R3, -SO2-N(R7R7), -N(R3)-SO2-R3, -COOR3, -OCO-R3, -CO-N(R7R7), -N(R3)-COR3, C1-3-alkyl, C1-3-alkoxy and a ring moiety optionally substituted with R6, wherein such ring moiety is piperazinyl, piperidinyl, morpholinyl, pyrrolidinyl, pyrazolyl, imidazolyl, benzimidazolyl, azetidinyl, cyclobuti
