公开(公告)号：US20240083900A1

公开(公告)日：2024-03-14

申请号：US18036853

申请日：2021-11-12

Applicant: BIOGEN MA INC.

Inventor： Brian T. Hopkins ,  Bin Ma ,  Isaac Marx ,  Jürgen Schulz ,  George Vandeveer ,  Robin Prince ,  Marta Nevalainen ,  TeYu Chen ,  Zain Yousaf ,  Martin Himmelbauer ,  Vatee Pattaropong ,  John Howard Jones ,  Edward Yin-Shiang Lin ,  Felix Gonzalez Lopez de Turiso ,  Thomas Purgett ,  Andrew George Capacci ,  Simone Sciabola

IPC: C07D487/04 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D519/00

Abstract: Provided are compounds of Formula (I′): or pharmaceutically acceptable salts thereof, wherein the variables in the formula are as defined herein; and methods for their use and production.

公开(公告)号：US20210340135A1

公开(公告)日：2021-11-04

申请号：US17183702

申请日：2021-02-24

Applicant: BIOGEN MA INC.

Inventor： Brian T. Hopkins ,  Bin Ma ,  Robin Prince ,  Isaac Marx ,  Joseph P. Lyssikatos ,  Fengmei Zheng ,  Matthew Peterson ,  Daniel B. Patience

IPC: C07D417/14 ,  C07D403/14 ,  C07D413/14 ,  A61P43/00 ,  C07D405/14 ,  C07D471/04 ,  A61P1/16

Abstract: Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, and methods for their use and production.

公开(公告)号：US10406144B2

公开(公告)日：2019-09-10

申请号：US16020696

申请日：2018-06-27

Applicant: BIOGEN MA INC.

Inventor： Jermaine Thomas ,  Sha Mi ,  Edward Yin-Shiang Lin ,  Guo Zhu Zheng ,  Bin Ma ,  Richard D. Caldwell ,  Kevin M. Guckian ,  Gnanasambandam Kumaravel

IPC: A61K31/445 ,  A61K31/225 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/517 ,  A61K31/55 ,  A61K31/695 ,  A61K39/395 ,  A61K38/21 ,  C07D211/34 ,  C07D211/60 ,  C07D211/62 ,  C07D401/06 ,  C07D405/12 ,  C07D215/20 ,  C07K16/28

Abstract: Compounds of formula (I) or (II) can modulate the activity of S1P receptors.

公开(公告)号：US20180369215A1

公开(公告)日：2018-12-27

申请号：US16020696

申请日：2018-06-27

Applicant: BIOGEN MA INC.

Inventor： Jermaine Thomas ,  Sha Mi ,  Edward Yin-Shiang Lin ,  Guo Zhu Zheng ,  Bin Ma ,  Richard D. Caldwell ,  Kevin M. Guckian ,  Gnanasambandam Kumaravel

IPC: A61K31/445 ,  A61K31/517 ,  C07D211/34 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/55 ,  A61K31/225 ,  A61K31/695 ,  C07K16/28 ,  A61K38/21 ,  A61K39/395 ,  C07D215/20 ,  C07D405/12 ,  C07D401/06 ,  C07D211/62 ,  C07D211/60

CPC classification number: A61K31/445 ,  A61K31/225 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/517 ,  A61K31/55 ,  A61K31/695 ,  A61K38/21 ,  A61K39/3955 ,  C07D211/34 ,  C07D211/60 ,  C07D211/62 ,  C07D215/20 ,  C07D401/06 ,  C07D405/12 ,  C07K16/2842

Abstract: Compounds of formula (I) or (II) can modulate the activity of S1P receptors.

公开(公告)号：US20180362522A1

公开(公告)日：2018-12-20

申请号：US16113455

申请日：2018-08-27

Applicant: BIOGEN MA INC.

Inventor： Brian T. Hopkins ,  Bin Ma ,  Robin Prince ,  Isaac Marx ,  Joseph P. Lyssikatos ,  Fengmei Zheng ,  Matthew Peterson ,  Daniel B. Patience

IPC: C07D417/14 ,  A61P43/00 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

CPC classification number: C07D417/14 ,  A61K31/44 ,  A61K31/443 ,  A61K31/506 ,  A61P43/00 ,  C07B2200/13 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

Abstract: Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, and methods for their use and production.

公开(公告)号：US20180002356A1

公开(公告)日：2018-01-04

申请号：US15621665

申请日：2017-06-13

Applicant: BIOGEN MA INC.

Inventor： Richard D. Caldwell ,  Kevin M. Guckian ,  Gnanasambandam Kumaravel ,  Wen-Cherng Lee ,  Edward Yin-Shiang Lin ,  Xiaogao Liu ,  Bin Ma ,  Daniel M. Scott ,  Zhan Shi ,  Jermaine Thomas ,  Arthur G. Taveras ,  Guo Zhu Zheng

IPC: C07F9/6512 ,  C07D263/24 ,  C07D215/20 ,  C07C217/58 ,  C07C233/47 ,  C07C229/36 ,  C07F9/60 ,  C07D239/80

CPC classification number: C07F9/6512 ,  C07C217/58 ,  C07C217/74 ,  C07C229/36 ,  C07C233/47 ,  C07C2602/10 ,  C07D215/06 ,  C07D215/20 ,  C07D215/227 ,  C07D233/32 ,  C07D239/74 ,  C07D239/80 ,  C07D263/24 ,  C07D277/64 ,  C07D401/04 ,  C07F9/091 ,  C07F9/60 ,  C07F9/65744

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

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).

公开(公告)号：US09809577B2

公开(公告)日：2017-11-07

申请号：US15103749

申请日：2014-12-11

Applicant: BIOGEN MA INC.

Inventor： Brian T. Hopkins ,  Bin Ma ,  Timothy Raymond Chan ,  Lihong Sun ,  Lei Zhang ,  Gnanasambandam Kumaravel ,  Joseph P. Lyssikatos ,  Kevin Koch ,  Hua Miao

IPC: C07D403/12 ,  C07D417/14 ,  C07D495/04 ,  C07D409/14 ,  C07D401/14 ,  C07D513/04 ,  C07D413/14 ,  C07D417/12 ,  C07D487/04

CPC classification number: C07D403/12 ,  A61K31/506 ,  C07D239/30 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  C07F5/027

Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.

公开(公告)号：US09808449B2

公开(公告)日：2017-11-07

申请号：US14757822

申请日：2015-12-23

Applicant: Biogen MA Inc.

Inventor： Jermaine Thomas ,  Sha Mi ,  Edward Yin-Shiang Lin ,  Guo Zhu Zheng ,  Bin Ma ,  Richard D. Caldwell ,  Kevin Guckian ,  Gnanasambandam Kumaravel

IPC: A61K31/445 ,  A61K38/21 ,  A61K31/225 ,  A61K39/395 ,  A61K31/517 ,  A61K31/695 ,  A61K31/4545 ,  C07K16/28 ,  A61K31/4709 ,  C07D215/20 ,  C07D405/12 ,  C07D211/34 ,  C07D211/60 ,  C07D211/62 ,  C07D401/06 ,  A61K31/498 ,  A61K31/55

CPC classification number: A61K31/445 ,  A61K31/225 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/517 ,  A61K31/55 ,  A61K31/695 ,  A61K38/21 ,  A61K39/3955 ,  C07D211/34 ,  C07D211/60 ,  C07D211/62 ,  C07D215/20 ,  C07D401/06 ,  C07D405/12 ,  C07K16/2842

Abstract: Compounds of formula (I) or (II) can modulate the activity of S1P receptors.

公开(公告)号：US20150361029A1

公开(公告)日：2015-12-17

申请号：US14763893

申请日：2014-01-29

Applicant: BIOGEN MA INC.

Inventor： Kevin Guckian ,  Gnanasambandam Kumaravel ,  Xiaogao Liu ,  Bin Ma ,  Hairuo Peng

IPC: C07C229/14 ,  C07D207/16 ,  C07D211/62 ,  C07C229/50 ,  C07C229/48 ,  C07D211/34 ,  C07F7/08 ,  A61K45/06 ,  A61K31/198 ,  A61K31/397 ,  A61K31/197 ,  A61K31/40 ,  A61K31/445 ,  A61K31/196 ,  A61K31/695 ,  C07D205/04

CPC classification number: C07C229/14 ,  A61K31/196 ,  A61K31/197 ,  A61K31/198 ,  A61K31/397 ,  A61K31/40 ,  A61K31/445 ,  A61K31/695 ,  A61K45/06 ,  C07C229/48 ,  C07C229/50 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/26 ,  C07C2602/44 ,  C07D205/04 ,  C07D207/08 ,  C07D207/16 ,  C07D211/34 ,  C07D211/62 ,  C07F7/0812 ,  Y02A50/401

Abstract: Compounds of formula (I) can modulate the activity of one or more S 1P receptors. Sphingosine 1-phosphate (S IP) is a lysophospholipid mediator that evokes a variety of cellular responses by stimulation of five members of the endothelial cell differentiation gene (EDG) receptor family, namely S1P1, S1P2, S1P3, S1P4, and S1P5 (formerly EDG1, EDG5, EDG3, EDG6 and EDG8). The EDG receptors are G-protein coupled receptors (GPCRs) and on stimulation propagate second messenger signals via activation of heterotrimeric G-protein alpha (Ga.) subunits and beta-gamma (G( )y) dimers.

Abstract translation: 式（I）化合物可调节一种或多种S 1 P受体的活性。 鞘氨醇1-磷酸（SIP）是一种溶血磷脂介质，通过刺激内皮细胞分化基因（EDG）受体家族的五个成员即S1P1，S1P2，S1P3，S1P4和S1P5（以前称为EDG1），诱发多种细胞反应 ，EDG5，EDG3，EDG6和EDG8）。 EDG受体是G蛋白偶联受体（GPCR），刺激通过激活异源三聚体G蛋白α（Ga。）亚基和β-gamma（G（）y）二聚体而传播第二信使信号。