EA201290515A1 - Аминопиримидины в качестве syk ингибиторов - Google Patents

Аминопиримидины в качестве syk ингибиторов

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Publication number
EA201290515A1
EA201290515A1 EA201290515A EA201290515A EA201290515A1 EA 201290515 A1 EA201290515 A1 EA 201290515A1 EA 201290515 A EA201290515 A EA 201290515A EA 201290515 A EA201290515 A EA 201290515A EA 201290515 A1 EA201290515 A1 EA 201290515A1
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EA
Eurasian Patent Office
Prior art keywords
aminopyrimidines
syk inhibitors
pyrimidinamines
copd
asthma
Prior art date
Application number
EA201290515A
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English (en)
Other versions
EA022790B1 (ru
Inventor
Майкл Д. Алтман
Брайан М. Андресен
Кеннет Л. Аррингтон
Калин Конрад Чайлдерс
Мария Эмилия Ди Франческо
Энтони Донофрио
Джон Майкл Эллис
Кристиан Фишер
Дэвид Джозеф Герин
Эндрю М. Хайдл
Соломон Каттар
Сандра Ли Ноулес
Чаоминь Ли
Чжонгвон Лим
Мишелль Р. Машасек
Алан Б. Нортруп
Брендан М. О'Бойл
Райан Д. Отте
Алессия Петрокки
Майкл Х. Ройтершан
Эрик Ромео
Тони Сиу
Брендон М. Таока
Б. Уэсли Троттер
Хуа Чжоу
Джейсон Берч
Бернар Коте
Кристина Дюпон-Годе
Жан-Франсуа Фурнье
Жак Ив Готье
Даниель Гуэй
Жоэль С. Робишо
Original Assignee
Мерк Шарп Энд Домэ Корп.
Мерк Кэнэда Инк.
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43502894&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201290515(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Мерк Шарп Энд Домэ Корп., Мерк Кэнэда Инк. filed Critical Мерк Шарп Энд Домэ Корп.
Publication of EA201290515A1 publication Critical patent/EA201290515A1/ru
Publication of EA022790B1 publication Critical patent/EA022790B1/ru

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Abstract

Настоящее изобретение относится к новым пиримидинаминам формулы (I), которые являются потенциальными ингибиторами тирозинкиназы селезенки и являются пригодными для лечения и предотвращения заболеваний, опосредованных упомянутым ферментом, таких как астма, ХОБЛ и ревматоидный артрит.
EA201290515A 2009-12-17 2010-12-15 Аминопиримидины в качестве syk ингибиторов EA022790B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US28726709P 2009-12-17 2009-12-17
PCT/US2010/060463 WO2011075517A1 (en) 2009-12-17 2010-12-15 Aminopyrimidines as syk inhibitors

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EA201290515A1 true EA201290515A1 (ru) 2013-01-30
EA022790B1 EA022790B1 (ru) 2016-03-31

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US (3) US8759366B2 (ru)
EP (1) EP2513098B1 (ru)
JP (2) JP5242857B2 (ru)
KR (1) KR101445012B1 (ru)
CN (1) CN102858767B (ru)
AR (1) AR080672A1 (ru)
AU (1) AU2010331927B2 (ru)
BR (1) BR112012014703B1 (ru)
CA (1) CA2782889C (ru)
CL (1) CL2012001627A1 (ru)
CO (1) CO6551728A2 (ru)
CR (1) CR20120331A (ru)
DO (1) DOP2012000166A (ru)
EA (1) EA022790B1 (ru)
EC (1) ECSP12011982A (ru)
ES (1) ES2609040T3 (ru)
GE (1) GEP20146125B (ru)
GT (1) GT201200202A (ru)
MA (1) MA33926B1 (ru)
MX (1) MX2012007154A (ru)
NI (1) NI201200108A (ru)
NZ (1) NZ600673A (ru)
PE (1) PE20121480A1 (ru)
SG (1) SG181803A1 (ru)
TN (1) TN2012000288A1 (ru)
TW (1) TW201132637A (ru)
WO (2) WO2011075517A1 (ru)

Families Citing this family (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA33926B1 (fr) 2009-12-17 2013-01-02 Merck Sharp & Dohme Aminopyrimidines en tant qu'inhibiteurs de la syk
EP2512246B1 (en) 2009-12-17 2015-09-30 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
SI2516434T1 (sl) 2009-12-23 2015-10-30 Takeda Pharmaceutical Company Limited Zliti heteroaromatski pirolidinoni kot inhibitorji SYK
WO2011086085A1 (en) 2010-01-12 2011-07-21 Ab Science Thiazole and oxazole kinase inhibitors
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
KR20140025500A (ko) * 2011-05-04 2014-03-04 머크 샤프 앤드 돔 코포레이션 아미노-피리딘-함유 비장 티로신 키나제 (Syk) 억제제
KR20140028062A (ko) * 2011-05-10 2014-03-07 머크 샤프 앤드 돔 코포레이션 Syk 억제제로서의 아미노피리미딘
EP2706852B1 (en) 2011-05-10 2018-08-22 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors
AU2012253886A1 (en) 2011-05-10 2013-10-31 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as Syk inhibitors
JP2014159375A (ja) * 2011-06-15 2014-09-04 Takeda Chem Ind Ltd アゼパン化合物
JP6026525B2 (ja) 2011-06-22 2016-11-16 武田薬品工業株式会社 置換6−アザ−イソインドリン−1−オン誘導体
WO2013092512A1 (en) * 2011-12-21 2013-06-27 Bayer Intellectual Property Gmbh Substituted benzylpyrazoles
US8906889B2 (en) 2012-02-15 2014-12-09 Bristol-Myers Squibb Company C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory activity
US9096579B2 (en) 2012-04-20 2015-08-04 Boehringer Ingelheim International Gmbh Amino-indolyl-substituted imidazolyl-pyrimidines and their use as medicaments
US8889854B2 (en) 2012-05-07 2014-11-18 Bristol-Myers Squibb Company C-17 bicyclic amines of triterpenoids with HIV maturation inhibitory activity
EP3822273B1 (en) 2012-06-13 2024-04-10 Incyte Holdings Corporation Substituted tricyclic compounds as fgfr inhibitors
EP2863914B1 (en) 2012-06-20 2018-10-03 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors
EP2863913B1 (en) 2012-06-20 2018-09-12 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
EP2863916B1 (en) * 2012-06-22 2018-07-18 Merck Sharp & Dohme Corp. Substituted pyridine spleen tyrosine kinase (syk) inhibitors
US9416111B2 (en) 2012-06-22 2016-08-16 Merck Sharp & Dohme Corp. Substituted diazine and triazine spleen tyrosine kinease (Syk) inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
WO2014031438A2 (en) * 2012-08-20 2014-02-27 Merck Sharp & Dohme Corp. SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS
US9586931B2 (en) 2012-09-28 2017-03-07 Merck Sharp & Dohme Corp. Triazolyl derivatives as Syk inhibitors
HUE040126T2 (hu) 2012-11-01 2019-02-28 Infinity Pharmaceuticals Inc Rákok kezelése PI3 kináz izoform modulátorok alkalmazásával
EP2916837A4 (en) * 2012-11-07 2016-07-20 Merck Sharp & Dohme BIPYRIDYLAMINOPYRIDINE PRODRUCE AS SYK INHIBITORS
US20150284381A1 (en) * 2012-11-07 2015-10-08 Merck Sharp & Dohme Corp. Amino-pyridine-containing spleen tyrosine kinase (syk) inhibitors
EP2931281B1 (en) 2012-12-12 2018-01-17 Merck Sharp & Dohme Corp. Amino-pyrimidine-containing spleen tyrosine kinase inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
WO2014100314A1 (en) * 2012-12-21 2014-06-26 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
NZ629037A (en) 2013-03-15 2017-04-28 Infinity Pharmaceuticals Inc Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
SG10201708520YA (en) 2013-04-19 2017-12-28 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US9499534B2 (en) * 2013-04-26 2016-11-22 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors
US9745295B2 (en) 2013-04-26 2017-08-29 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US20140377258A1 (en) 2013-05-30 2014-12-25 Infinity Pharmaceuticals, Inc. Treatment Of Cancers Using PI3 Kinase Isoform Modulators
US9751888B2 (en) 2013-10-04 2017-09-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
MX2021012208A (es) 2013-10-04 2023-01-19 Infinity Pharmaceuticals Inc Compuestos heterocíclicos y usos de los mismos.
US20160244452A1 (en) 2013-10-21 2016-08-25 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
EP3082807B1 (en) * 2013-12-20 2018-07-04 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
EP3083559B1 (en) 2013-12-20 2021-03-10 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
US9775839B2 (en) 2014-03-13 2017-10-03 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
CA2943075C (en) 2014-03-19 2023-02-28 Infinity Pharmaceuticals, Inc. Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
WO2015143712A1 (en) 2014-03-28 2015-10-01 Merck Sharp & Dohme Corp. 4'-substituted nucleoside reverse transcriptase inhibitors
US20150320754A1 (en) 2014-04-16 2015-11-12 Infinity Pharmaceuticals, Inc. Combination therapies
US9708348B2 (en) 2014-10-03 2017-07-18 Infinity Pharmaceuticals, Inc. Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MX2017010673A (es) 2015-02-20 2018-03-21 Incyte Corp Heterociclos biciclicos como inhibidores de receptores del factor de crecimiento fibroblastico (fgfr).
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
ES2893148T3 (es) 2015-04-02 2022-02-08 Intervet Int Bv Anticuerpos contra el receptor alfa de la interleucina 4 canina
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
JP7054681B2 (ja) 2016-06-24 2022-04-14 インフィニティー ファーマシューティカルズ, インコーポレイテッド 組合せ療法
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CN107573263B (zh) * 2017-08-14 2020-04-07 大连理工大学 一种ω-取代缩二脲类化合物的合成方法
EP4112616A1 (en) 2017-09-11 2023-01-04 Cyteir Therapeutics, Inc. Rad51 inhibitors
JP2020537678A (ja) 2017-10-19 2020-12-24 バイエル・アニマル・ヘルス・ゲーエムベーハー 動物における疾患の治療および予防のための縮合ヘテロ芳香族ピロリドンの使用
US11040975B2 (en) 2017-12-08 2021-06-22 Merck Sharp & Dohme Corp. Carbocyclic nucleoside reverse transcriptase inhibitors
CN112867716A (zh) 2018-05-04 2021-05-28 因赛特公司 Fgfr抑制剂的固体形式和其制备方法
CN112566912A (zh) 2018-05-04 2021-03-26 因赛特公司 Fgfr抑制剂的盐
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
JP2022519929A (ja) 2019-03-25 2022-03-25 サイティアー セラピューティクス,インコーポレイティド Rad51及びparp阻害薬の併用に関連した出願
ES2962852T3 (es) 2019-05-10 2024-03-21 Deciphera Pharmaceuticals Llc Inhibidores de la autofagia de heteroarilaminopirimidina amida y métodos de uso de los mismos
CN114258318A (zh) 2019-06-17 2022-03-29 德西费拉制药有限责任公司 氨基嘧啶酰胺自噬抑制剂及其使用方法
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AU2020366006A1 (en) 2019-10-14 2022-04-21 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
KR20220110241A (ko) 2019-11-29 2022-08-05 루핀 리미티드 치환된 트리사이클릭 화합물
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US20230250177A1 (en) 2019-12-20 2023-08-10 Intervet Inc. Bispecific Caninized Antibodies for Treating Atopic Dermatitis
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CA3194384A1 (en) 2020-10-15 2022-04-21 Intervet International B.V. Caninized rat antibodies to canine interleukin-31 receptor alpha
BR112023019388A2 (pt) 2021-03-23 2023-11-07 Halia Therapeutics Inc Derivados de pirimidina úteis como inibidores de quinase lrrk2
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
CA3227725A1 (en) 2021-08-20 2023-02-23 Mohamad Morsey Homodimer fusion proteins for treating atopic dermatitis
CN114105958B (zh) * 2021-12-03 2022-11-22 郑州大学第一附属医院 一组含羟肟酸的2-苯氨基嘧啶类衍生物及其应用
WO2023111148A1 (en) 2021-12-16 2023-06-22 Intervet International B.V. Caninized antibodies to canine interleukin-31 receptor alpha 1

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1440973A3 (de) 1995-11-17 2004-10-20 Gesellschaft für biotechnologische Forschung mbH (GBF) Epothilonderivate, Herstellung und Mittel
AU756699B2 (en) 1996-12-03 2003-01-23 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
GB9918035D0 (en) * 1999-07-30 1999-09-29 Novartis Ag Organic compounds
US6960584B2 (en) 2001-04-10 2005-11-01 Merck & Co., Inc. Inhibitors of Akt activity
WO2002083140A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
EP1379251B1 (en) 2001-04-10 2008-07-09 Merck & Co., Inc. Inhibitors of akt activity
WO2002096905A1 (en) 2001-06-01 2002-12-05 Vertex Pharmaceuticals Incorporated Thiazole compounds useful as inhibitors of protein kinases
JP2005500294A (ja) 2001-06-19 2005-01-06 ブリストル−マイヤーズ スクイブ カンパニー ホスホジエステラーゼ7に対するピリミジン阻害剤
GB0123951D0 (en) 2001-10-05 2001-11-28 Glaxo Group Ltd Therapies for treating respiratory diseases
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US20050182256A1 (en) 2002-04-08 2005-08-18 Duggan Mark E. Inhibitors of akt activity
JP4451136B2 (ja) 2002-04-08 2010-04-14 メルク エンド カムパニー インコーポレーテッド Akt活性阻害薬
JP4394960B2 (ja) 2002-04-08 2010-01-06 メルク エンド カムパニー インコーポレーテッド Akt活性阻害薬
US7273869B2 (en) 2002-04-08 2007-09-25 Merck & Co., Inc. Inhibitors of Akt activity
US7361665B2 (en) 2002-07-09 2008-04-22 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
ATE396731T1 (de) 2003-03-25 2008-06-15 Vertex Pharma Thiazole zur verwendung als inhibitoren von protein-kinasen
US20040235834A1 (en) 2003-03-25 2004-11-25 Farmer Luc J. Thiazoles useful as inhibitors of protein kinases
WO2005044354A1 (en) 2003-11-03 2005-05-19 Glaxo Group Limited A fluid dispensing device
US7345043B2 (en) 2004-04-01 2008-03-18 Miikana Therapeutics Inhibitors of histone deacetylase
BRPI0606318B8 (pt) 2005-01-19 2021-05-25 Rigel Pharmaceuticals Inc composto, composição, e, uso de um composto
ZA200707227B (en) * 2005-02-28 2009-08-26 Japan Tobacco Inc Novel aminopyridine compound with syk inhibitory activity
WO2006093247A1 (ja) * 2005-02-28 2006-09-08 Japan Tobacco Inc. Syk阻害活性を有する新規なアミノピリジン化合物
WO2006129100A1 (en) 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
GB0520838D0 (en) * 2005-10-13 2005-11-23 Glaxo Group Ltd Novel compounds
EP2007732B1 (en) 2006-04-11 2011-11-23 Vertex Pharmaceuticals, Inc. Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases
WO2008024634A1 (en) 2006-08-25 2008-02-28 Smithkline Beecham Corporation Pyrimdine compounds useful as kinase inhibitors
PL2091918T3 (pl) 2006-12-08 2015-02-27 Novartis Ag Związki i kompozycje jako inhibitory kinazy białkowej
TW200840581A (en) 2007-02-28 2008-10-16 Astrazeneca Ab Novel pyrimidine derivatives
ES2381318T3 (es) 2007-05-04 2012-05-25 Irm Llc Derivados de pirimidina y composiciones útiles como inhibidores de cinasas C-KIT y PDGFR
BRPI0814432A2 (pt) 2007-07-17 2017-05-09 Rigel Pharmaceuticals Inc pirimidinadiaminas substituídas por amina cíclica como inibidores de pkc
CA2698511C (en) 2007-09-04 2016-10-11 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
PL2265607T3 (pl) 2008-02-15 2017-07-31 Rigel Pharmaceuticals, Inc. Związki pirymidyno-2-aminowe i ich zastosowanie jako inhibitory kinaz JAK
WO2009122180A1 (en) * 2008-04-02 2009-10-08 Medical Research Council Pyrimidine derivatives capable of inhibiting one or more kinases
JP5705720B2 (ja) 2008-04-16 2015-04-22 ポートラ ファーマシューティカルズ, インコーポレイテッド Sykまたはjakキナーゼ阻害剤としての2,6−ジアミノ−ピリミジン−5−イル−カルボキサミド
MA33926B1 (fr) * 2009-12-17 2013-01-02 Merck Sharp & Dohme Aminopyrimidines en tant qu'inhibiteurs de la syk
WO2011086085A1 (en) * 2010-01-12 2011-07-21 Ab Science Thiazole and oxazole kinase inhibitors
DE102010000842A1 (de) * 2010-01-13 2011-07-14 Robert Bosch GmbH, 70469 Batterie, Batteriesystem und Verfahren zur Verbindung einer Mehrzahl von Batterien

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