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S1P and/or ATX modulating agents
专利权人:
BIOGEN MA INC.
发明人:
Hairuo Peng,Edward Yin-Shiang Lin,Jianhua Chao,Zhili Xin,Bin Ma,Kevin Guckian,Timothy Chan,Gnanasambandam Kumaravel,Arthur G. Taveras
申请号:
US14443912
公开号:
US09850206B2
申请日:
2013.11.20
申请国别(地区):
US
年份:
2017
代理人:
摘要:
Compounds of formula (I) wherein: X is —O—, —S(O)r—, —CH2—, or —NR—, wherein r is 0, 1, or 2; X1, X2, and X5 are each independently CR7 or N; one of X3 or X4 is C and is attached by a single bond to -L-, and the other is CR7 or N, provided that no more than three of X1, X2, X3, X or X5 are N; Ring A is monocyclic C5-6scycloalkyl or a 5- to 6-membered monocyclic heterocyclyl comprising from 1 to 5 heteroatoms independently selected from N, S, or O; wherein Ring A is further optionally substituted with from 1 to 3 R4; provided that Ring A is not morpholinyl, thiomorpholinyl or tetrahydro-2H-pyranyl; L is a bond, —O—, —NR—, —S(O)n—, —CH2—, or —C(O)—, wherein n is 0, 1, or 2; 1 2 L1 is an C1-8alkylene, C3-scycloalkylene, —CH2-L2-, or a 3- to 8-membered heterocyclylene comprising 1 to 5; R1 is C6-20alkyl or a monocyclic C3-8cycloalkyl; wherein said C3-8cycloalkyl is substituted with at least one R6 and may be optionally substituted with from 1 to 5 additional R6 substituents, wherein R6 for each occurrence is independently selected; and R2 is —C(O)OR3, —C(O)N(R3)—S(O)2R3, —S(O)2OR3, —C(O)NHC(O)R3, —Si(O)OH, —B(OH)2, —N(R3)S(O)2R3, —S(O)2N(R3)2, —O—P(O)(OR3)2, or —P(O)(OR3)2, —CN, —S(O)2NHC(O)R3, —C(O)NHS(O)2R3, —C(O)NHOH, —C(O)NHCN, —CH(CF3)OH, —C(CF3)2OH, or a selected heteroaryl or heterocyclyl; and pharmaceutically acceptable salts thereof, can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).
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