KR101623997B1 - syk 또는 JAK 키나제 억제제로서의 2,6-디아미노-피리미딘-5-일-카르복스아미드 - Google Patents

syk 또는 JAK 키나제 억제제로서의 2,6-디아미노-피리미딘-5-일-카르복스아미드 Download PDF

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KR101623997B1
KR101623997B1 KR1020107025540A KR20107025540A KR101623997B1 KR 101623997 B1 KR101623997 B1 KR 101623997B1 KR 1020107025540 A KR1020107025540 A KR 1020107025540A KR 20107025540 A KR20107025540 A KR 20107025540A KR 101623997 B1 KR101623997 B1 KR 101623997B1
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pyrimidine
phenylamino
carboxamide
cyclopropylamino
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KR20100126863A (ko
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쇼운 엠. 바우어
쟈오종 제이. 지아
용홍 송
칭 슈
무쿤드 메로트라
잭 더블유. 로즈
월린 후앙
찬드라세카 벤카타라마니
안젤리 팬데이
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포톨라 파마슈티컬스, 인코포레이티드
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KR1020107025540A 2008-04-16 2009-04-16 syk 또는 JAK 키나제 억제제로서의 2,6-디아미노-피리미딘-5-일-카르복스아미드 Active KR101623997B1 (ko)

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US4541708P 2008-04-16 2008-04-16
US4540608P 2008-04-16 2008-04-16
US61/045,406 2008-04-16
US61/045,417 2008-04-16
US12034808P 2008-12-05 2008-12-05
US12034408P 2008-12-05 2008-12-05
US61/120,344 2008-12-05
US61/120,348 2008-12-05

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KR20100126863A KR20100126863A (ko) 2010-12-02
KR101623997B1 true KR101623997B1 (ko) 2016-05-24

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EP (1) EP2321283B1 (enExample)
JP (2) JP5705720B2 (enExample)
KR (1) KR101623997B1 (enExample)
CN (1) CN102066340B (enExample)
CA (2) CA2960692C (enExample)
DO (1) DOP2010000310A (enExample)
EA (1) EA024109B1 (enExample)
HN (1) HN2010002119A (enExample)
HR (1) HRP20161310T1 (enExample)
MA (1) MA32280B1 (enExample)
MY (1) MY155639A (enExample)
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024107017A1 (ko) * 2022-11-18 2024-05-23 가톨릭대학교 산학협력단 Stat6 억제제를 이용한 전신경화증 비멘틴 변이 단백질 활성 억제 치료 조성물

Families Citing this family (104)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ589315A (en) 2008-04-16 2012-11-30 Portola Pharm Inc 2,6-diamino-pyrimidin-5-yl-carboxamides as Spleen tryosine kinase (syk) or Janus kinase (JAK) inhibitors
CN102066339B (zh) * 2008-04-16 2014-09-24 波托拉医药品公司 作为syk或jak蛋白激酶抑制剂的2,6-二氨基-嘧啶-5-基甲酰胺类化合物
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
EP2361242B1 (en) 2008-10-17 2018-08-01 Oryzon Genomics, S.A. Oxidase inhibitors and their use
US8993808B2 (en) 2009-01-21 2015-03-31 Oryzon Genomics, S.A. Phenylcyclopropylamine derivatives and their medical use
US8367689B2 (en) 2009-05-06 2013-02-05 Portola Pharmaceuticals, Inc. Inhibitors of JAK
DK2428508T3 (en) * 2009-05-08 2016-02-01 Astellas Pharma Inc Diamino heterocyclic carboxamide COMPOUND
US8859555B2 (en) 2009-09-25 2014-10-14 Oryzon Genomics S.A. Lysine Specific Demethylase-1 inhibitors and their use
US8946296B2 (en) 2009-10-09 2015-02-03 Oryzon Genomics S.A. Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use
WO2011075560A1 (en) 2009-12-17 2011-06-23 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
US8551984B2 (en) 2009-12-17 2013-10-08 Merck Sharp & Dohme Corp. Aminopyrimidines as SYK inhibitors
PL2516434T3 (pl) 2009-12-23 2015-11-30 Takeda Pharmaceuticals Co Skondensowane heteroaromatyczne pirolidynony jako inhibitory SYK
WO2011106105A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
US9186337B2 (en) 2010-02-24 2015-11-17 Oryzon Genomics S.A. Lysine demethylase inhibitors for diseases and disorders associated with Hepadnaviridae
JP2011182847A (ja) 2010-03-05 2011-09-22 Three M Innovative Properties Co 医療用粘着剤組成物
RU2599248C2 (ru) 2010-04-19 2016-10-10 Оризон Дженомикс С.А. Лизинспецифические ингибиторы деметилазы-1 и их применение
CN102958918B (zh) 2010-06-30 2015-12-09 富士胶片株式会社 新型烟酰胺衍生物或其盐
CA2801781C (en) * 2010-07-21 2018-02-27 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
ME03085B (me) 2010-07-29 2019-01-20 Oryzon Genomics Sa Demetilaza inhibitori lsd1 zasnovani na arilciklopropilaminu i njihova medicinska primjena
US9006449B2 (en) 2010-07-29 2015-04-14 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as LSD1 inhibitors
WO2012045010A1 (en) * 2010-09-30 2012-04-05 Portola Pharmaceuticals, Inc. Combinations of 4-(3-(2h-1,2,3-triazo-2-yl) phenylamino)-2-((1r,2s)-2-aminocyclohexylamino) pyrimidine-5-carboxamide and fludarabine
US9061966B2 (en) 2010-10-08 2015-06-23 Oryzon Genomics S.A. Cyclopropylamine inhibitors of oxidases
WO2012072713A2 (en) 2010-11-30 2012-06-07 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae
US20140163041A1 (en) * 2011-02-08 2014-06-12 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders
EP3981395A1 (en) 2011-02-08 2022-04-13 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative disorders
EP2489663A1 (en) 2011-02-16 2012-08-22 Almirall, S.A. Compounds as syk kinase inhibitors
SG194086A1 (en) * 2011-04-22 2013-11-29 Signal Pharm Llc Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith
US9120785B2 (en) 2011-05-10 2015-09-01 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as Syk inhibitors
EP2706852B1 (en) 2011-05-10 2018-08-22 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors
WO2012154519A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
US20140296255A1 (en) * 2011-05-19 2014-10-02 Oryzong Genomics, S.A. Lysine demethylase inhibitors for thrombosis and cardiovascular diseases
US20140329833A1 (en) * 2011-05-19 2014-11-06 Oryzon Genomics, S.A Lysine demethylase inhibitors for inflammatory diseases or conditions
KR101255939B1 (ko) * 2011-05-31 2013-04-23 동화약품주식회사 4-(1h-인다졸-6-일아미노)-n-아이소프로필-2-(메틸티오)피리미딘-5-카르복스아미드 화합물 또는 이의 약학적으로 허용가능한 염을 포함하는 당뇨병 예방 또는 치료용 조성물
US9056873B2 (en) 2011-06-22 2015-06-16 Takeda Pharmaceutical Company Limited Substituted 6-aza-isoindolin-1-one derivatives
WO2013054351A1 (en) * 2011-08-08 2013-04-18 Cadila Healthcare Limited Heterocyclic compounds
EP2763974B1 (en) 2011-10-05 2016-09-14 Merck Sharp & Dohme Corp. Phenyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
WO2013052393A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
EP2763976B1 (en) 2011-10-05 2016-05-18 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
BR112014009238B1 (pt) 2011-10-20 2022-08-09 Oryzon Genomics S.A. Compostos de (hetero)aril ciclopropilamina, seus usos e composições farmacêuticas
BR112014009306B1 (pt) 2011-10-20 2021-07-20 Oryzon Genomics S.A. Compostos de (hetero)aril ciclopropilamina como inibidores de lsd1
EP2782579B1 (en) * 2011-11-23 2019-01-02 Portola Pharmaceuticals, Inc. Pyrazine kinase inhibitors
US20140323418A1 (en) * 2011-11-23 2014-10-30 Portola Pharmaceuticals, Inc. Selective kinase inhibitors
WO2013092854A1 (en) 2011-12-23 2013-06-27 Cellzome Limited Pyrimidine-2,4-diamine derivatives as kinase inhibitors
BR112014016328A8 (pt) 2011-12-28 2017-07-04 Fujifilm Corp novo derivado de nicotinamida ou sal do mesmo
WO2013104573A1 (en) * 2012-01-10 2013-07-18 F. Hoffmann-La Roche Ag Pyridazine amide compounds and their use as syk inhibitors
UA111010C2 (uk) * 2012-01-17 2016-03-10 Астеллас Фарма Інк. Сполука піразинкарбоксаміду
LT2840080T (lt) * 2012-04-17 2018-02-12 Fujifilm Corporation Heterociklinis junginys, turintis azotą, arba jo druska
CN102731412A (zh) * 2012-06-13 2012-10-17 盛世泰科生物医药技术(苏州)有限公司 一种2,4-二氯-5-嘧啶甲醛的合成方法
WO2013192125A1 (en) 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors
CN102731375A (zh) * 2012-06-20 2012-10-17 盛世泰科生物医药技术(苏州)有限公司 4,6-二氯-5-嘧啶甲醛的合成
US9487504B2 (en) 2012-06-20 2016-11-08 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
EP2863915B1 (en) 2012-06-22 2017-12-06 Merck Sharp & Dohme Corp. SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS
WO2013192098A1 (en) 2012-06-22 2013-12-27 Merck Sharp & Dohme Corp. SUBSTITUTED PYRIDINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS
KR101446742B1 (ko) 2012-08-10 2014-10-01 한국화학연구원 N2,n4-비스(4-(피페라진-1-일)페닐)피리미딘-2,4-디아민 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
US9353066B2 (en) 2012-08-20 2016-05-31 Merck Sharp & Dohme Corp. Substituted phenyl-Spleen Tyrosine Kinase (Syk) inhibitors
CN104640863B (zh) * 2012-09-20 2016-06-08 山东亨利医药科技有限责任公司 嘧啶胺衍生物及其制备方法和应用
EP2900665B1 (en) 2012-09-28 2018-01-03 Merck Sharp & Dohme Corp. Triazolyl derivatives as syk inhibitors
JP2015534959A (ja) 2012-10-19 2015-12-07 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Sykの阻害剤
ES2648226T3 (es) * 2012-11-08 2017-12-29 Bristol-Myers Squibb Company Compuestos de pirimidina sustituidos con alquilamida útiles en la modulación de IL-12, IL-23 y/o IFN
EP2931281B1 (en) 2012-12-12 2018-01-17 Merck Sharp & Dohme Corp. Amino-pyrimidine-containing spleen tyrosine kinase inhibitors
US9598405B2 (en) 2012-12-21 2017-03-21 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
WO2014176210A1 (en) 2013-04-26 2014-10-30 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
WO2014176216A1 (en) 2013-04-26 2014-10-30 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors
PT3030561T (pt) 2013-08-07 2017-03-23 Cadila Healthcare Ltd N-cianometilamidas como inibidores de cinase janus
HUE044683T2 (hu) * 2013-10-21 2019-11-28 Merck Patent Gmbh Heteroaril vegyületek mint BTK inhibitorok és alkalmazásuk
AU2014360446A1 (en) 2013-12-05 2016-06-09 Pharmacyclics, Llc Inhibitors of Bruton's tyrosine kinase
US9783531B2 (en) 2013-12-20 2017-10-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US9822107B2 (en) 2013-12-20 2017-11-21 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
EP3083560B1 (en) 2013-12-20 2021-10-27 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
NZ715903A (en) 2014-01-30 2017-06-30 Signal Pharm Llc Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
WO2015138273A1 (en) 2014-03-13 2015-09-17 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
JP6517319B2 (ja) * 2014-03-28 2019-05-22 キャリター・サイエンシーズ・リミテッド・ライアビリティ・カンパニーCalitor Sciences, Llc 置換されたヘテロアリール化合物および使用方法
JP6684780B2 (ja) 2014-08-25 2020-04-22 ソーク インスティテュート フォー バイオロジカル スタディーズ 新規ulk1阻害剤およびそれを使用する方法
WO2016060963A1 (en) * 2014-10-14 2016-04-21 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
WO2016100308A1 (en) * 2014-12-16 2016-06-23 Signal Pharmaceuticals, Llc Methods for measurement of inhibition of c-jun n-terminal kinase in skin
SG11201704827UA (en) 2014-12-16 2017-07-28 Signal Pharm Llc Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide
EP3250557B1 (en) 2015-01-29 2024-11-20 Signal Pharmaceuticals, LLC Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
EP3302485B1 (en) 2015-05-29 2023-07-12 Alexion Pharmaceuticals, Inc. Cerdulatinib for the treatment of b-cell malignancies
CN107922287B (zh) 2015-07-24 2021-04-09 细胞基因公司 合成(1r,2r,5r)-5-氨基-2-甲基环己醇盐酸盐的方法和其中可用的中间体
CN108348779A (zh) * 2015-08-02 2018-07-31 H·李·莫菲特癌症中心研究有限公司 Ack1/tnk2酪氨酸激酶的抑制剂
US20170042896A1 (en) 2015-08-12 2017-02-16 Portola Pharmaceuticals, Inc. Cerdulatinib for treating myeloma
AR106830A1 (es) 2015-12-04 2018-02-21 Asana Biosciences Llc Usos de piridazinonas para tratar el cáncer
CN108367006B (zh) 2015-12-04 2021-12-31 博尔托拉制药公司 用于治疗血液癌症的赛度替尼
KR101936054B1 (ko) 2017-06-23 2019-01-11 한국과학기술연구원 항염증 활성을 가지는 6-페녹시피리미딘 유도체, 이의 제조방법 및 이를 활성성분으로 하는 약학 조성물
CN111032630B (zh) * 2017-08-18 2022-12-16 北京韩美药品有限公司 一种化合物,其药物组合物及其用途及应用
EP3686197B1 (en) * 2017-09-21 2023-06-21 Beijing Scitech-MQ Pharmaceuticals Limited 2-substituted pyrazole amino-4-substituted amino-5-pyrimidine formamide compound, composition, and application thereof
KR20200073216A (ko) 2017-10-19 2020-06-23 바이엘 애니멀 헬스 게엠베하 동물에서의 질환의 치료 및 방지를 위한 융합된 헤테로방향족 피롤리돈의 용도
JP7167146B2 (ja) 2017-11-06 2022-11-08 ブリストル-マイヤーズ スクイブ カンパニー Hpk1阻害剤として有用なイソフラノン化合物
WO2019099311A1 (en) * 2017-11-19 2019-05-23 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
CN108299312B (zh) * 2018-03-29 2020-10-30 郑州大学第一附属医院 一组嘧啶类衍生物及其在制备抗肿瘤药物中的应用
JP7324778B2 (ja) * 2018-05-04 2023-08-10 ポートラ ファーマシューティカルズ, エルエルシー セルデュラチニブ(cerdulatinib)の固体形態
TWI805751B (zh) * 2018-05-04 2023-06-21 美商普托拉製藥有限公司 賽度替尼(cerdulatinib)之合成
WO2020187292A1 (zh) * 2019-03-19 2020-09-24 北京赛特明强医药科技有限公司 2-取代吡唑氨基-4-取代氨基-5-嘧啶甲酰胺类化合物、组合物及其应用
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2022078305A1 (zh) * 2020-10-12 2022-04-21 四川海思科制药有限公司 一种杂环衍生物及其在医药上的应用
JP2024509309A (ja) * 2021-03-09 2024-02-29 石薬集団中奇制薬技術(石家庄)有限公司 三環式ヘテロアリール基を有する化合物の用途
EP4401735A4 (en) * 2021-09-16 2025-07-16 Lomond Therapeutics Inc COMPOUNDS COMPRISING N-ARYLPYRIMIDIN-2-AMINE DERIVATIVES AS THERAPEUTIC AGENTS
WO2023108536A1 (en) * 2021-12-16 2023-06-22 Lynk Pharmaceuticals Co. Ltd. Tyk2 inhibitors and compositions and methods thereof
JP2025503448A (ja) 2021-12-16 2025-02-04 リンク ファーマシューティカルズ シーオー.エルティーディー. Tyk2阻害剤および組成物ならびにその方法
CN114621206B (zh) * 2022-03-24 2023-11-24 安徽医科大学 一种5-取代的嘧啶二胺类衍生物及其制备方法与应用
CN115304550A (zh) * 2022-07-25 2022-11-08 南通大学 哌嗪苯基氨基取代的嘧啶氨基酸衍生物及制备方法与应用
CN115141150B (zh) * 2022-07-25 2024-04-26 南通大学 2,4,5-三取代嘧啶羟胺酰衍生物及其制备方法与应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040029902A1 (en) * 2002-02-01 2004-02-12 Rajinder Singh 2,4-Pyrimidinediamine compounds and their uses
WO2008009458A1 (en) * 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999031073A1 (en) * 1997-12-15 1999-06-24 Yamanouchi Pharmaceutical Co., Ltd. Novel pyrimidine-5-carboxamide derivatives
CN1665789A (zh) * 2002-06-28 2005-09-07 山之内制药株式会社 二氨基嘧啶酰胺衍生物
US8367689B2 (en) * 2009-05-06 2013-02-05 Portola Pharmaceuticals, Inc. Inhibitors of JAK

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040029902A1 (en) * 2002-02-01 2004-02-12 Rajinder Singh 2,4-Pyrimidinediamine compounds and their uses
WO2008009458A1 (en) * 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024107017A1 (ko) * 2022-11-18 2024-05-23 가톨릭대학교 산학협력단 Stat6 억제제를 이용한 전신경화증 비멘틴 변이 단백질 활성 억제 치료 조성물

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