TWI818985B - 作為類視色素相關孤兒受體γ（ＲＯＲγ）調節劑之苯并咪唑衍生物及其醫藥用途 - Google Patents

作為類視色素相關孤兒受體γ（ＲＯＲγ）調節劑之苯并咪唑衍生物及其醫藥用途 Download PDF

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TWI818985B
TWI818985B TW108115438A TW108115438A TWI818985B TW I818985 B TWI818985 B TW I818985B TW 108115438 A TW108115438 A TW 108115438A TW 108115438 A TW108115438 A TW 108115438A TW I818985 B TWI818985 B TW I818985B
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alkyl
cycloalkyl
heterocyclyl
aryl
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TW108115438A
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TW202014185A (zh
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銀發 燕
民生 張
東 劉
鳳岐 張
蘇星 劉
儒民 張
峰 賀
維康 陶
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中國大陸商江蘇恒瑞醫藥股份有限公司
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TW108115438A 2018-05-03 2019-05-03 作為類視色素相關孤兒受體γ（ＲＯＲγ）調節劑之苯并咪唑衍生物及其醫藥用途 TWI818985B (zh)

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SMT202300212T1 (it) * 2018-05-03 2023-09-06 Shanghai hengrui pharmaceutical co ltd Derivati di benzimidazolo come modulatori del recettore gamma orfano correlato al retinoide (rory) e usi farmaceutici di essi
BR112022008293A2 (pt) * 2019-10-31 2022-07-26 Jiangsu Hengrui Medicine Co Sal de adição de ácido de regulador de ror?, composições farmacêuticas, uso dos mesmos e métodos para preparar forma cristalina e composição farmacêutica
CN112745268B (zh) * 2019-10-31 2022-09-16 江苏恒瑞医药股份有限公司 苯并咪唑衍生物的晶型及制备方法
TW202136238A (zh) * 2020-01-06 2021-10-01 大陸商廣東東陽光藥業有限公司 RORγt抑制劑及其製備方法和用途
TW202136237A (zh) * 2020-01-06 2021-10-01 大陸商廣東東陽光藥業有限公司 RORγt抑制劑及其製備方法和用途
CN111269126B (zh) * 2020-03-12 2023-04-07 北京理工大学重庆创新中心 一种熔铸载体1,2-二氟-4,5-二硝基苯的制备方法
CN115702024A (zh) 2020-04-07 2023-02-14 Ucb生物制药有限责任公司 用作il-17调节剂的二氟环己基衍生物
TW202146381A (zh) * 2020-05-15 2021-12-16 大陸商上海輝启生物醫藥科技有限公司 可用作RORγ調節劑的聯芳基類化合物
WO2022245067A1 (ko) * 2021-05-17 2022-11-24 서울대학교 산학협력단 RORα의 활성자 JC1-40을 포함하는 근감소증 예방, 개선, 또는 치료를 위한 약학적 조성물
CN121045325A (zh) * 2024-05-31 2025-12-02 中国科学院广州生物医药与健康研究院 磺酰胺基乙酰胺类化合物及其制备方法和应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110190364A1 (en) * 2006-05-03 2011-08-04 Player Mark R Benzimidazole modulators of vr1
US20130065896A1 (en) * 2010-05-24 2013-03-14 Toa Eiyo Ltd. Fused imidazole derivative

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3075991A (en) * 1960-01-20 1963-01-29 Dow Chemical Co Benzimidazolylalkylbenzene-sulfonamide compounds
DE60023920T2 (de) * 1999-08-27 2006-07-20 Sugen, Inc., South San Francisco Phosphatmimetika und Verfahren zur Behandlung mit Phosphataseinhibitoren HIBITOREN
WO2012027965A1 (en) 2010-09-01 2012-03-08 Glaxo Group Limited Novel compounds
CN102060780B (zh) * 2010-12-27 2014-11-05 雅本化学股份有限公司 2-(n-取代)-氨基苯并咪唑衍生物的制备方法
WO2013029338A1 (en) 2011-09-01 2013-03-07 Glaxo Group Limited Novel compounds
CA2874303C (en) 2012-06-11 2020-10-13 Ucb Biopharma Sprl Tnf -alpha modulating benz imidazoles
EP3089963A1 (en) * 2013-10-30 2016-11-09 Novartis AG 2-benzyl-benzimidazole complement factor b inhibitors and uses thereof
BR122020020657B1 (pt) 2014-04-14 2022-12-20 Boehringer Ingelheim International Gmbh Compostos, composição farmacêutica e seus usos como moduladores de ror gama
CA2940264A1 (en) 2014-04-16 2015-10-22 Glenmark Pharmaceuticals S.A. Aryl and heteroaryl ether compounds as ror gamma modulators
WO2015196335A1 (en) * 2014-06-23 2015-12-30 Tocopherx, Inc. Pyrazole compounds as modulators of fshr and uses thereof
US9771374B2 (en) * 2014-07-25 2017-09-26 Innov17 Llc Benzimidazole retinoic acid receptor-related orphan receptor modulators and uses thereof
FR3030516B1 (fr) * 2014-12-19 2019-12-27 Galderma Research & Development Derives sulfonamides bicycles en tant qu'agonistes inverses du recepteur gamma orphelin associe aux retinoides ror gamma (t)
TWI757266B (zh) * 2016-01-29 2022-03-11 美商維它藥物有限責任公司 ＲＯＲ－γ調節劑
SMT202300212T1 (it) * 2018-05-03 2023-09-06 Shanghai hengrui pharmaceutical co ltd Derivati di benzimidazolo come modulatori del recettore gamma orfano correlato al retinoide (rory) e usi farmaceutici di essi

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110190364A1 (en) * 2006-05-03 2011-08-04 Player Mark R Benzimidazole modulators of vr1
US20130065896A1 (en) * 2010-05-24 2013-03-14 Toa Eiyo Ltd. Fused imidazole derivative

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