公开(公告)号：US09421273B2

公开(公告)日：2016-08-23

申请号：US14363546

申请日：2012-12-14

Applicant: Biogen Idec MA Inc.

Inventor： Jianhua Chao

IPC: C07F7/04 ,  A61K47/48 ,  C07F7/08 ,  C07F7/18

CPC classification number: A61K47/48023 ,  A61K47/54 ,  C07F7/0836 ,  C07F7/1804 ,  C07F7/1896

Abstract: The present invention is directed to silicon-containing fumaric acid esters of the Formulae I-IV. The silicon-containing fumaric acid esters of Formulae I-IV are useful in transplantation medicine and for the treatment of autoimmune diseases and autoimmune-related diseases. (I), (II), (III) & (IV).

Abstract translation: 本发明涉及式I-Ⅳ的含硅富马酸酯。 式I-IV的含硅富马酸酯可用于移植医学和用于治疗自身免疫疾病和自身免疫相关疾病。 （I），（II），（III）和（IV）。

公开(公告)号：US20150274663A1

公开(公告)日：2015-10-01

申请号：US14443912

申请日：2013-11-20

Applicant: BIOGEN IDEC MA INC.

Inventor： Hairuo Peng ,  Edward Yin-Shiang Lin ,  Jianhua Chao ,  Zhili Xin ,  Bin Ma ,  Kevin Guckian ,  Timothy Chan ,  Gnanasambandam Kumaravel ,  Arthur G. Taveras

IPC: C07D211/22 ,  C07D401/12 ,  A61K31/4545 ,  C07D295/15 ,  A61K45/06 ,  C07D403/04 ,  A61K31/501 ,  A61K31/506 ,  C07D401/04 ,  A61K31/451 ,  A61K31/495

CPC classification number: C07D211/22 ,  A61K31/451 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  C07D207/08 ,  C07D211/56 ,  C07D211/62 ,  C07D211/70 ,  C07D213/74 ,  C07D237/22 ,  C07D239/47 ,  C07D295/15 ,  C07D295/155 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04

Abstract: 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).

公开(公告)号：US20140336151A1

公开(公告)日：2014-11-13

申请号：US14363546

申请日：2012-12-14

Applicant: Biogen Idec MA Inc.

Inventor： Jianhua Chao

IPC: A61K47/48 ,  C07F7/08 ,  C07F7/18

CPC classification number: A61K47/48023 ,  A61K47/54 ,  C07F7/0836 ,  C07F7/1804 ,  C07F7/1896

Abstract: The present invention is directed to silicon-containing fumaric acid esters of the Formulae I-IV. The silicon-containing fumaric acid esters of Formulae I-IV are useful in transplantation medicine and for the treatment of autoimmune diseases and autoimmune-related diseases. (I), (II), (III) & (IV)

Abstract translation: 本发明涉及式I-IV的含硅富马酸酯。 式I-IV的含硅富马酸酯可用于移植医学和用于治疗自身免疫疾病和自身免疫相关疾病。 （I），（II），（III）和（IV）