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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).
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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.
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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。
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公开(公告)号：US20200038385A1
公开(公告)日：2020-02-06
申请号：US16542746
申请日：2019-08-16
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 , C07K16/28 , A61K39/395 , A61K38/21 , A61K31/695 , A61K31/55 , A61K31/517 , A61K31/498 , A61K31/4709 , A61K31/4545 , A61K31/225 , C07D215/20 , C07D401/06 , C07D405/12 , C07D211/62 , C07D211/60 , C07D211/34
Abstract: Compounds of formula (I) or (II) can modulate the activity of S1P receptors.
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公开(公告)号：US10273234B2
公开(公告)日：2019-04-30
申请号：US14420020
申请日：2013-08-05
Applicant: BIOGEN MA INC.
Inventor： Kevin Guckian , Gnanasambandam Kumaravel , Bin Ma , Lihong Sun , Zhili Xin , Lei Zhang
IPC: C07D471/08 , A61K31/122 , C07C229/48 , C07D223/06 , C07D205/04 , C07D207/16 , C07D209/52 , C07D211/62 , A61K45/06 , A61K31/397 , A61K31/403 , A61K31/44 , A61K31/55 , A61K31/196 , A61K31/40 , A61K31/439 , A61K31/445 , C07C211/38 , C07D207/08
Abstract: Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).
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Patent Agency Ranking
6.发明授权公开(公告)号：US09499485B2
公开(公告)日：2016-11-22
申请号：US14420025
申请日：2013-08-05
Applicant: BIOGEN MA INC.
Inventor： Kevin Guckian , Gnanasambandam Kumaravel , Bin Ma , Lihong Sun , Zhili Xin , Lei Zhang
IPC: C07D451/02 , C07D211/62 , A61K31/122 , A61K45/06 , A61K31/192 , A61K31/216 , A61K31/439 , A61K31/445 , A61K31/45 , C07C229/14 , C07C229/48 , C07D211/60 , A61K31/196 , A61K31/197 , A61K31/198 , A61K31/46 , C07D211/34 , C07D451/14
CPC classification number: C07D211/62 , A61K31/122 , A61K31/192 , A61K31/196 , A61K31/197 , A61K31/198 , A61K31/216 , A61K31/439 , A61K31/445 , A61K31/45 , A61K31/46 , A61K45/06 , C07C229/14 , C07C229/48 , C07C2601/14 , C07D211/34 , C07D211/60 , C07D451/02 , C07D451/14 , A61K2300/00
Abstract: Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).
Abstract translation: 式（I）化合物可以调节一种或多种SIP受体的活性和/或自分泌素（ATX）的活性。
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公开(公告)号：US20210188809A1
公开(公告)日：2021-06-24
申请号：US16071200
申请日：2017-01-18
Applicant: BIOGEN MA INC.
Inventor： Timothy Chan , Kevin Guckian , Tracy Jenkins , Jermaine Thomas , Jeffrey Vessels , Gnanasambandam Kumaravel , Robert Meissner , Joseph P. Lyssikatos , Brian Lucas , Irina Leaf , Jeremy Duffield , Nathan Genung
IPC: C07D401/14 , A61K45/06
Abstract: Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production. Formula (I) The compounds are IRAK-4 inhibitors useful for treating an inflammatory disease, an autoimmune disease, cancer, a cardiovascular disease, a disease of the central nervous system, a disease of the skin, an ophthalmic disease and condition, and a bone disease.
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公开(公告)号：US10577367B2
公开(公告)日：2020-03-03
申请号：US16271497
申请日：2019-02-08
Applicant: BIOGEN MA INC.
Inventor： Timothy Chan , Kevin Guckian , Tracy Jenkins , Jermaine Thomas , Jeffery Vessels , Gnanasambandam Kumaravel , Robert Meissner , Joseph Lyssikatos , Brian Lucas , Irina Leaf , Jeremy Duffield
IPC: C07D401/14 , C07D487/04 , A61K31/416 , A61K31/437 , A61K31/44 , A61P13/12 , A61P19/02 , C07D471/04 , C07D405/14 , C07D413/14 , C07B59/00 , C07D401/12 , C07D417/14
Abstract: Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production.
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公开(公告)号：US20170204093A1
公开(公告)日：2017-07-20
申请号：US15326740
申请日：2015-07-17
Applicant: BIOGEN MA INC.
Inventor： Timothy Chan , Kevin Guckian , Tracy Jenkins , Jermaine Thomas , Jeffery Vessels , Gnanasambandam Kumaravel , Robert Meissner , Joseph Lyssikatos , Brian Lucas , Irina Leaf , Jeremy Duffield
IPC: C07D471/04 , C07D401/12 , C07D405/14 , C07D413/14 , C07B59/00 , C07D401/14 , C07D417/14
CPC classification number: C07D471/04 , A61K31/416 , A61P13/12 , C07B59/002 , C07B2200/05 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
Abstract: Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, and methods for their use and production.
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公开(公告)号：US09708353B2
公开(公告)日：2017-07-18
申请号：US14620700
申请日：2015-02-12
Applicant: BIOGEN MA INC.
Inventor： Richard D. Caldwell , Kevin 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: C07D263/24 , C07F9/6512 , C07C233/47 , C07C229/36 , C07C217/58 , C07D215/20 , 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.
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