公开(公告)号：US20170354639A1

公开(公告)日：2017-12-14

申请号：US15521239

申请日：2015-10-23

Applicant: Biogen MA Inc.

Inventor： Jianhua Chao ,  Brian Lucas

IPC: A61K31/365 ,  C07D413/06 ,  A61K31/423 ,  C07D407/06 ,  C07D411/06 ,  A61K31/39 ,  C07D307/60

CPC classification number: A61K31/365 ,  A61K31/39 ,  A61K31/423 ,  C07D307/58 ,  C07D307/60 ,  C07D407/06 ,  C07D411/06 ,  C07D413/06

Abstract: Provided herein are compounds of formula (I) and compositions containing the compounds. The compounds and compositions are useful in the methods of treating, amelioration or prophylaxix of diseases associated with Nrf2/NF-κB pathways. The diseases associated include, but are not limited to a fibrotic disease such as lung fibrosis, liver fibrosis, kidney fibrosis, and scleroderma, or a neurodegenerative disease, such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, Huntington's disease, and Alzheimer's disease, and sickle cell disease.

公开(公告)号：US10399924B2

公开(公告)日：2019-09-03

申请号：US14201380

申请日：2014-03-07

Applicant: Biogen MA Inc.

Inventor： Jianhua Chao

IPC: A61K31/22 ,  C07C69/60 ,  C07C69/533 ,  A61K31/225 ,  A61K31/235 ,  A61K31/24 ,  A61K31/5375 ,  A61K45/06 ,  C07C69/76 ,  C07C229/36 ,  C07D295/145 ,  C07B59/00

Abstract: Provided herein are deuterium substituted fumarate derivatives and pharmaceutical compositions comprising deuterium substituted fumarate derivatives. Also provided is a method of treating, prophylaxis, or amelioration of a disease, comprising administering to a subject in need of treatment for the disease an effective amount of a deuterium substituted fumarate derivative or a pharmaceutical composition comprising a deuterium substituted fumarate derivative. In one embodiment, the method is a neurodegenerative disease, such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, Huntington's disease, or Alzheimer's disease.

公开(公告)号：US09850206B2

公开(公告)日：2017-12-26

申请号：US14443912

申请日：2013-11-20

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

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).