公开(公告)号：US09522889B2

公开(公告)日：2016-12-20

申请号：US14417300

申请日：2013-07-26

Applicant: BIOGEN MA INC.

Inventor： Kevin Guckian ,  Gnanasambandam Kumaravel ,  Bin Ma ,  Sha Mi ,  Hairuo Peng ,  Zhaohui Shao ,  Lihong Sun ,  Arthur Taveras ,  Deping Wang ,  Zhili Xin ,  Lei Zhang

IPC: A61K31/015 ,  A61K31/44 ,  A61K31/4375 ,  C07D295/096 ,  C07D223/06 ,  A61K45/06 ,  C07D217/22 ,  C07D471/08 ,  C07D211/34 ,  C07D211/62 ,  C07C255/59 ,  C07C229/46 ,  C07C229/48 ,  A61K31/136 ,  A61K31/196 ,  A61K31/439 ,  A61K31/445 ,  A61K31/46 ,  A61K31/5375 ,  A61K31/55 ,  C07C217/22 ,  C07D209/52 ,  C07D221/22

CPC classification number: C07D451/02 ,  A61K31/136 ,  A61K31/196 ,  A61K31/439 ,  A61K31/445 ,  A61K31/46 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/5375 ,  A61K31/55 ,  A61K45/06 ,  C07B2200/07 ,  C07C217/22 ,  C07C229/46 ,  C07C229/48 ,  C07C255/59 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/42 ,  C07D209/52 ,  C07D211/34 ,  C07D211/62 ,  C07D217/22 ,  C07D221/22 ,  C07D223/06 ,  C07D295/096 ,  C07D401/06 ,  C07D471/08 ,  Y02A50/401

Abstract: Disclosed are bicyclic aryl compounds of formula (I), that can modulate the activity of the autotaxin (ATX) enzyme. This invention further relates to compounds that are ATX inhibitors, and methods of making and using such compounds in the treatment of demyelination due to injury or disease, as well as for treating proliferative disorders such as cancer.

Abstract translation: 公开了式（I）的双环芳基化合物，其可以调节自分泌素（ATX）酶的活性。 本发明还涉及作为ATX抑制剂的化合物，以及制备和使用这些化合物治疗由于损伤或疾病引起的脱髓鞘以及治疗增殖性疾病如癌症的方法。

公开(公告)号：US20160039825A1

公开(公告)日：2016-02-11

申请号：US14772481

申请日：2014-03-14

Applicant: BIOGEN MA INC.

Inventor： Hairuo Peng ,  Zhili Xin ,  Lei Zhang ,  Lihong Sun ,  Gnanasambandam Kumaravel ,  Art Taveras ,  Deping Wang

IPC: C07D487/04 ,  C07D519/00

CPC classification number: A61K31/198 ,  A61K36/9068 ,  C07D487/04 ,  C07D519/00

Abstract: Compounds of formula (I), 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：US20240308995A1

公开(公告)日：2024-09-19

申请号：US18673619

申请日：2024-05-24

Applicant: BIOGEN MA INC.

Inventor： Nathan Genung ,  Kevin M. Guckian ,  Jeffrey Vessels ,  Lei Zhang ,  Ryan Gianatassio ,  Edward Yin Shiang Lin ,  Zhili Xin

IPC: C07D417/14 ,  A61P25/28 ,  C07D417/06

CPC classification number: C07D417/14 ,  A61P25/28 ,  C07D417/06

Abstract: Described herein are compounds represented by formulas (IA) or (IB)




or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables R1, R3, R4, Y1, Y2, Ar, Z and n are as defined herein.

公开(公告)号：US20210340107A1

公开(公告)日：2021-11-04

申请号：US17221358

申请日：2021-04-02

Applicant: BIOGEN MA INC.

Inventor： Brian Stuart Lucas ,  Edward Yin Shiang Lin ,  Andrew George Capacci ,  Zhili Xin ,  Istvan Enyedy ,  TeYu Chen ,  John H. Jones ,  Kurt D. van Vloten

IPC: C07D217/04 ,  C07D217/08 ,  C07D217/20 ,  C07D217/22 ,  C07D223/14 ,  C07D311/74 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D413/06 ,  C07D498/04

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

公开(公告)号：US20210317103A1

公开(公告)日：2021-10-14

申请号：US17267631

申请日：2019-08-13

Applicant: BIOGEN MA INC.

Inventor： Felix Gonzalez Lopez de Turiso ,  Zhili Xin ,  Martin Himmelbauer ,  John H. Jones

IPC: C07D401/14 ,  C07D405/14

Abstract: Provided are compounds of Formula (I): Formula (I), including compounds of Formulas (II), (III), (IV), (V) and (VI), wherein X, R1, R2, R3, R4 and n are as defined herein, and pharmaceutically acceptable salts thereof, and methods for their use and production. These compounds can be useful, e.g., in the treatment of disorders responsive to the inhibition of apoptosis signal-regulating kinase 1 (ASK1).

公开(公告)号：US10968181B2

公开(公告)日：2021-04-06

申请号：US16473667

申请日：2017-12-27

Applicant: BIOGEN MA INC.

Inventor： Brian Stuart Lucas ,  Edward Yin-Shiang Lin ,  Andrew George Capacci ,  Zhili Xin ,  Istvan Enyedy ,  TeYu Chen ,  John H. Jones ,  Kurt D. van Vloten

IPC: C07D311/76 ,  C07D217/04 ,  C07D217/08 ,  C07D223/16 ,  C07D498/14 ,  A61K31/352 ,  A61K31/47 ,  C07D217/20 ,  C07D217/22 ,  C07D223/14 ,  C07D311/74 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D413/06 ,  C07D498/04

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

公开(公告)号：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).