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公开(公告)号：US12275728B2
公开(公告)日：2025-04-15
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
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.
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公开(公告)号：US20240343733A1
公开(公告)日：2024-10-17
申请号：US18576940
申请日：2022-07-07
Applicant: BIOGEN MA INC. , C4 THRAPEUTICS, INC.
Inventor： Kevin M. Guckian , Emily Anne Peterson , Fang Gao , Ryan Evans , Eric Stefan , Jeremy L. Yap , Corey Don Anderson , Morgan Welzel O'Shea , Jae Young M. Ahn , Christopher G. Nasveschuk , James A. Henderson
IPC: C07D487/04 , A61K31/4545 , A61K31/513 , A61K31/519 , C07D401/14 , C07D471/04 , C07D487/10 , C07D519/00
CPC classification number: C07D487/04 , A61K31/4545 , A61K31/513 , A61K31/519 , C07D401/14 , C07D471/04 , C07D487/10 , C07D519/00
Abstract: This disclosure relates to compounds of Formula (A): IRAK-L-DSM (A), or a pharmaceutically acceptable salt thereof, wherein DSM is a degradation signaling moiety that is covalently attached to the linker L, L is a linker that covalently attaches IRAK to DSM; and IRAK is an IRAK4 binding moiety represented by Formula (I) that is covalently attached to linker L; in which all of the variables are as defined in the application. Compounds or pharmaceutically acceptable salts thereof as described herein are capable of activating the selective ubiqitination of IRAK4 proteins via the ubiquitin-proteasome pathways (UPP) and cause degradation of IRAK4 proteins. The present disclosure also provides methods of treating disorders responsive to modulation of IRAK4 activity and/or degradation of IRAK4 with at least one compound described herein.
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公开(公告)号：US11459324B2
公开(公告)日：2022-10-04
申请号：US16978550
申请日：2019-03-13
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 , C07D417/06 , C07D471/04
Abstract: Described herein are compounds represented by formula (I″) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables Ar, Ra, Rb, m, n, Y1, Y2, R3 and R4 are defined herein.
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公开(公告)号：US10081646B2
公开(公告)日：2018-09-25
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: C07D239/80 , C07F9/6512 , C07F9/60 , C07C217/58 , C07C229/36 , C07C233/47 , C07D215/20 , C07D263/24
CPC classification number: C07D215/20 , C07C217/58 , C07C217/74 , C07C229/36 , C07C233/47 , C07C2602/10 , C07D215/06 , C07D215/14 , C07D215/227 , C07D233/32 , C07D239/74 , C07D239/80 , C07D263/24 , C07D277/64 , C07D401/04 , C07F7/0836 , C07F9/091 , C07F9/60 , C07F9/6512 , 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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公开(公告)号：US10034869B2
公开(公告)日：2018-07-31
申请号：US15644352
申请日：2017-07-07
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 , A61K38/21 , C07D211/62 , C07D401/06 , C07D405/12 , C07D215/20 , A61K31/225 , A61K39/395 , A61K31/517 , A61K31/695 , A61K31/55 , C07K16/28 , A61K31/498 , A61K31/4709 , C07D211/34 , C07D211/60 , A61K31/4545
Abstract: The present invention provides compounds of formula (I) or (II) or a pharmaceutically acceptable salt thereof and their use in modulating the activity of S1P receptors. Also provided is a pharmaceutical composition comprising the compounds of formula (I) or (II) or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient or carrier.
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Patent Agency Ranking
公开(公告)号：US09944666B2
公开(公告)日：2018-04-17
申请号：US15368454
申请日：2016-12-02
Applicant: BIOGEN MA INC.
Inventor： Kevin M. Guckian , Gnanasambandam Kumaravel , Bin Ma , Sha Mi , Hairuo Peng , Zhaohui Shao , Lihong Sun , Arthur G. Taveras , Zhili Xin , Lei Zhang
IPC: C07D401/04 , C07D215/38 , C07D217/12 , A61K31/47 , C07F7/08 , A61K45/06 , C07C229/50 , A61K31/196 , C07D215/12 , A61K31/4545 , A61K31/506 , C07D295/096 , A61K31/495 , C07D213/74 , A61K31/496 , A61K31/551 , C07D239/42 , C07D241/20 , A61K31/497 , C07D211/14 , A61K31/451 , C07D205/04 , A61K31/397 , C07D401/06 , A61K31/4709 , C07D491/107 , C07D209/52 , A61K31/403 , C07D451/02 , A61K31/439 , A61K31/695 , C07C233/60 , C07D451/14
CPC classification number: C07F7/081 , A61K31/195 , A61K31/196 , A61K31/397 , A61K31/403 , A61K31/41 , A61K31/439 , A61K31/451 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/551 , A61K31/5513 , A61K31/695 , A61K45/06 , C07C211/38 , C07C217/58 , C07C229/46 , C07C229/50 , C07C233/60 , C07C233/61 , C07C235/66 , C07C2102/10 , C07C2102/42 , C07C2102/44 , C07C2102/50 , C07C2103/62 , C07C2601/10 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07C2602/44 , C07C2602/46 , C07C2602/50 , C07C2603/62 , C07C2603/74 , C07D205/04 , C07D209/52 , C07D211/14 , C07D213/74 , C07D215/12 , C07D215/20 , C07D215/38 , C07D217/22 , C07D239/42 , C07D241/20 , C07D295/096 , C07D401/04 , C07D401/06 , C07D451/02 , C07D451/14 , C07D471/08 , C07D491/107 , C07F7/0805 , A61K2300/00
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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公开(公告)号：US09827258B2
公开(公告)日：2017-11-28
申请号：US15397421
申请日：2017-01-03
Applicant: BIOGEN MA INC.
Inventor： Jermaine Thomas , Xiaogao Liu , Edward Yin-Shiang Lin , Guo Zhu Zheng , Bin Ma , Richard D. Caldwell , Kevin M. Guckian , Gnanasambandam Kumaravel , Arthur G. Taveras
IPC: A61K31/695 , C07C229/14 , C07C229/22 , C07C229/46 , C07C229/48 , C07C237/08 , C07C237/52 , C07C309/14 , C07C311/51 , C07D205/04 , C07D207/16 , C07D209/08 , C07D211/60 , C07D211/62 , C07D215/20 , C07D217/24 , C07D257/04 , C07D305/08 , C07D403/06 , C07D417/06 , C07F9/38 , C07F9/40 , A61K31/085 , A61K31/11 , A61K31/18 , A61K31/197 , A61K31/216 , A61K31/277 , A61K31/337 , A61K31/397 , A61K31/40 , A61K31/404 , A61K31/41 , A61K31/428 , A61K31/445 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/517 , A61K31/662 , A61K31/683 , A61K45/06 , C07C43/247 , C07C47/575 , C07C255/54 , C07D215/227 , C07D217/04 , C07D239/74 , C07D277/64 , C07D401/06 , C07F7/08 , A61K31/137 , A61K31/165 , A61K31/185 , A61K31/198 , A61K31/222 , A61K31/223 , A61K31/235 , A61K31/401
CPC classification number: A61K31/695 , A61K31/085 , A61K31/11 , A61K31/137 , A61K31/165 , A61K31/18 , A61K31/185 , A61K31/197 , A61K31/198 , A61K31/216 , A61K31/222 , A61K31/223 , A61K31/235 , A61K31/277 , A61K31/337 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/404 , A61K31/41 , A61K31/428 , A61K31/445 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/517 , A61K31/662 , A61K31/683 , A61K45/06 , C07C43/247 , C07C47/575 , C07C229/14 , C07C229/22 , C07C229/46 , C07C229/48 , C07C237/08 , C07C237/52 , C07C255/54 , C07C309/14 , C07C311/51 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07D205/04 , C07D207/16 , C07D209/08 , C07D211/60 , C07D211/62 , C07D215/20 , C07D215/227 , C07D217/04 , C07D217/24 , C07D239/74 , C07D257/04 , C07D277/64 , C07D305/08 , C07D401/06 , C07D403/06 , C07D417/06 , C07F7/081 , C07F9/3808 , C07F9/3834 , C07F9/4006
Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
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公开(公告)号：US20170158687A1
公开(公告)日：2017-06-08
申请号：US15296601
申请日：2016-10-18
Applicant: BIOGEN MA INC.
Inventor： Kevin M. Guckian , Gnanasambandam Kumaravel , Bin Ma , Sha Mi , Hairuo Peng , Zhaohui Shao , Lihong Sun , Arthur G. Taveras , Deping Wang , Zhili Xin , Lei Zhang
IPC: C07D451/02 , C07D401/06 , A61K45/06 , A61K31/4725 , C07D217/22 , A61K31/472
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.
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公开(公告)号：US20160129023A1
公开(公告)日：2016-05-12
申请号：US14874600
申请日：2015-10-05
Applicant: Biogen MA Inc.
Inventor： Jermaine Thomas , Xiaogao Liu , Edward Yin-Shiang Lin , Guo Zhu Zheng , Bin Ma , Richard D. Caldwell , Kevin M. Guckian , Gnanasambandam Kumaravel , Arthur G. Taveras
IPC: A61K31/695 , A61K31/11 , A61K31/18 , A61K31/216 , A61K31/197 , A61K31/397 , A61K31/40 , A61K31/445 , A61K31/683 , A61K31/662 , A61K31/47 , A61K31/277 , A61K31/41 , A61K31/4709 , A61K31/472 , A61K31/337 , A61K31/517 , A61K31/428 , A61K31/404 , A61K45/06 , A61K31/085
CPC classification number: A61K31/695 , A61K31/085 , A61K31/11 , A61K31/137 , A61K31/165 , A61K31/18 , A61K31/185 , A61K31/197 , A61K31/198 , A61K31/216 , A61K31/222 , A61K31/223 , A61K31/235 , A61K31/277 , A61K31/337 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/404 , A61K31/41 , A61K31/428 , A61K31/445 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/517 , A61K31/662 , A61K31/683 , A61K45/06 , C07C43/247 , C07C47/575 , C07C229/14 , C07C229/22 , C07C229/46 , C07C229/48 , C07C237/08 , C07C237/52 , C07C255/54 , C07C309/14 , C07C311/51 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07D205/04 , C07D207/16 , C07D209/08 , C07D211/60 , C07D211/62 , C07D215/20 , C07D215/227 , C07D217/04 , C07D217/24 , C07D239/74 , C07D257/04 , C07D277/64 , C07D305/08 , C07D401/06 , C07D403/06 , C07D417/06 , C07F7/081 , C07F9/3808 , C07F9/3834 , C07F9/4006
Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
Abstract translation: 提供了在一种或多种S1P受体上具有激动剂活性的化合物。 化合物是肌氨酸 - 甙类似物，磷酸化后，可以作为S1P受体的激动剂。
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公开(公告)号：US20250018046A1
公开(公告)日：2025-01-16
申请号：US18576933
申请日：2022-07-07
Applicant: BIOGEN MA INC , C4 THERAPEUTICS, INC.
Inventor： Kevin M. Guckian , Emily Anne Peterson , Fang Gao , Ryan Evans , Eric Stefan , Jeremy L. Yap , Corey Don Anderson , Morgan Weizel O'Shea , Jae Young M. Ahn , Christopher G. Nasveschuk , James A. Henderson
Abstract: This disclosure relates to compounds of Formula (A): Formula (A), or a pharmaceutically acceptable salt thereof, wherein DSM is a degradation signaling moiety that is covalently attached to the linker L, L is a linker that covalently attaches IRAK to DSM; and IRAK is an IRAK4 binding moiety represented by Formula (I) that is covalently attached to linker L; Formula (I) in which all of the variables are as defined in the application. Compounds or pharmaceutically acceptable salts thereof as described herein are capable of activating the selective ubiqitination of IRAK4 proteins via the ubiquitin-proteasome pathways (UPP) and cause degradation of IRAK4 proteins. The present disclosure also provides methods of treating disorders responsive to modulation of IRAK4 activity and/or degradation of IRAK4 with at least one compound described herein.
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