RU2677653C2 - Производные пиримидина в качестве ингибиторов киназы - Google Patents

Производные пиримидина в качестве ингибиторов киназы Download PDF

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RU2677653C2
RU2677653C2 RU2016104388A RU2016104388A RU2677653C2 RU 2677653 C2 RU2677653 C2 RU 2677653C2 RU 2016104388 A RU2016104388 A RU 2016104388A RU 2016104388 A RU2016104388 A RU 2016104388A RU 2677653 C2 RU2677653 C2 RU 2677653C2
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alkyl
cancer
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Сяо СЮЙ
Сяобо ВАН
Лун МАО
Ли ЧЖАО
Бяо СИ
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Ацея Байосайенсиз Инк.
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
RU2016104388A 2013-07-11 2014-07-11 Производные пиримидина в качестве ингибиторов киназы RU2677653C2 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361845342P 2013-07-11 2013-07-11
US61/845,342 2013-07-11
US201461923179P 2014-01-02 2014-01-02
US61/923,179 2014-01-02
PCT/US2014/046442 WO2015006754A2 (en) 2013-07-11 2014-07-11 Heterocyclic compounds and uses thereof

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RU2016104388A RU2016104388A (ru) 2017-08-16
RU2016104388A3 RU2016104388A3 (https=) 2018-04-27
RU2677653C2 true RU2677653C2 (ru) 2019-01-18

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US (1) US10562918B2 (https=)
EP (1) EP3019496B1 (https=)
JP (1) JP6564771B2 (https=)
KR (1) KR102173433B1 (https=)
CN (3) CN112592334B (https=)
AU (1) AU2014287016B2 (https=)
BR (1) BR112016000195A8 (https=)
CA (1) CA2917364C (https=)
DK (1) DK3019496T3 (https=)
ES (1) ES2761572T3 (https=)
IL (1) IL243420A0 (https=)
MX (1) MX368491B (https=)
NZ (1) NZ715687A (https=)
RU (1) RU2677653C2 (https=)
SG (1) SG11201600062RA (https=)
WO (1) WO2015006754A2 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2702631C2 (ru) * 2014-10-11 2019-10-09 Шанхай Хэнсох Биомедикал Ко., Лтд. Ингибитор egfr и его получение и применение
RU2743040C2 (ru) * 2015-07-09 2021-02-12 Мерк Патент Гмбх Производные пиримидина в качестве btk ингибиторов и их применение

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
CA2861010A1 (en) 2012-01-13 2013-07-18 Xiao Xu Heterocyclic compounds and uses as anticancer agents
ES2704744T3 (es) 2012-06-13 2019-03-19 Incyte Holdings Corp Compuestos tricíclicos sustituidos como inhibidores de FGFR
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
EA035095B1 (ru) 2013-04-19 2020-04-27 Инсайт Холдингс Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
NZ715687A (en) 2013-07-11 2019-04-26 Acea Biosciences Inc Pyrimidine derivatives as kinase inhibitors
AU2014308616B2 (en) 2013-08-23 2018-12-06 Neupharma, Inc. Certain chemical entities, compositions, and methods
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
AU2015371251B2 (en) 2014-12-23 2020-06-11 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN105884695B (zh) * 2015-02-13 2019-02-26 山东轩竹医药科技有限公司 杂环衍生物类酪氨酸激酶抑制剂
MX373169B (es) 2015-02-20 2020-04-24 Incyte Holdings Corp Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr).
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
HK1246645A1 (zh) * 2015-03-27 2018-09-14 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
CN106146515B (zh) * 2015-04-17 2020-09-04 常州隆赛医药科技有限公司 新型激酶抑制剂的制备及应用
KR101778004B1 (ko) * 2015-06-22 2017-09-15 (주) 에빅스젠 이마티닙을 유효성분으로 포함하는 안구 건조 질환 예방 및 치료용 약학 조성물
KR20180067584A (ko) 2015-10-09 2018-06-20 아세아 테라퓨틱스 인코포레이티드 피롤로피리미딘 키나아제 억제제의 약학적 염, 물리적 형태 및 조성물, 및 이들의 제조 방법
CN106608868A (zh) * 2015-10-21 2017-05-03 复旦大学 5-(硫醚基)嘧啶类化合物及其药用组合物和应用
KR20170050453A (ko) * 2015-10-30 2017-05-11 한미약품 주식회사 싸이에노피리미딘 화합물의 신규 제조방법 및 이에 사용되는 중간체
CN108137544B (zh) * 2015-12-10 2022-01-04 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物
RU2714206C1 (ru) 2016-06-30 2020-02-13 Даевунг Фармасьютикал Ко., Лтд. Пиразолопиримидиновые производные в качестве ингибитора киназы
CN109843858B (zh) 2016-08-15 2023-05-05 润新生物公司 某些化学实体、组合物及方法
CN106749042B (zh) * 2016-11-16 2019-01-22 大连医科大学 磺酰胺基嘧啶类化合物，组合物及用途
KR20180075228A (ko) * 2016-12-26 2018-07-04 한미약품 주식회사 싸이에노피리미딘 화합물의 신규 제조방법 및 중간체
WO2018124001A1 (ja) 2016-12-27 2018-07-05 国立研究開発法人理化学研究所 Ｂｍｐシグナル阻害化合物
WO2018139883A1 (ko) * 2017-01-26 2018-08-02 부광약품 주식회사 다중 표적 키나아제 저해제로서 융합피리미딘 유도체
CN110072865B (zh) * 2017-02-08 2022-02-11 中国医药研究开发中心有限公司 吡咯并芳杂环类化合物及其制备方法和医药用途
AU2017408099A1 (en) 2017-04-07 2019-11-07 ACEA Therapeutics, Inc. Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
MA52493A (fr) 2018-05-04 2021-03-10 Incyte Corp Sels d'un inhibiteur de fgfr
CR20200590A (es) 2018-05-04 2021-04-26 Incyte Corp Formas sólidas de un inhibidor de fgfr y procesos para prepararlas
US12187701B2 (en) 2018-06-25 2025-01-07 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
JP7675647B2 (ja) * 2018-08-09 2025-05-13 エイシア セラピューティクス， インコーポレイテッド （ｓ）－ｎ－（３－（（２－（（４－（（１－アセチルピロリジン－３－イル）（メチル）アミノ）フェニル）アミノ）－５－メトキシピリミジン－４－イル）オキシ）フェニル）アクリルアミドの製造のためのプロセスおよびその製剤
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
JP7660063B2 (ja) 2018-12-28 2025-04-10 ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド サイクリン依存性キナーゼ７のインヒビターおよびそれらの使用
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
TWI891666B (zh) 2019-10-14 2025-08-01 美商英塞特公司 作為ｆｇｆｒ抑制劑之雙環雜環
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AU2020385513A1 (en) * 2019-11-22 2022-07-14 Medshine Discovery Inc. Pyrimidopyrrole spiro compounds and derivatives thereof as DNA-PK inhibitors
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN111018842B (zh) * 2019-12-04 2021-02-12 宜春市人民医院 一种唑代嘧啶衍生物、其药物组合物和在抗肿瘤中的应用
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN111848631B (zh) * 2020-08-28 2022-04-19 四川大学华西医院 一种靶向EGFR突变的吡咯并[2,3-d]嘧啶衍生物及其制备方法和用途
US20240100172A1 (en) 2020-12-21 2024-03-28 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN114184671B (zh) * 2021-12-09 2024-02-06 中国石油大学(北京) 用于确定表面活性剂在岩石表面的吸附层数的方法
CA3238851A1 (en) * 2021-12-21 2023-06-29 Yuli Xie Compound as fak inhibitor and use thereof
WO2024092047A1 (en) * 2022-10-26 2024-05-02 Sorrento Therapeutics, Inc. Administration of pyrrolopyrimidine-based kinase inhibitors for treatment of psoriasis
CN117586235B (zh) * 2023-11-27 2025-08-22 广东省人民医院 增强线粒体自噬的嵌合分子及其应用

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009158571A1 (en) * 2008-06-27 2009-12-30 Avila Therapeutics And Uses Thereof Heteroaryl compounds and uses thereof
WO2010129053A2 (en) * 2009-05-05 2010-11-11 Dana Farber Cancer Institute Egfr inhibitors and methods of treating disorders
WO2011079231A1 (en) * 2009-12-23 2011-06-30 Gatekeeper Pharmaceutical, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
WO2012061303A1 (en) * 2010-11-01 2012-05-10 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof
WO2012064706A1 (en) * 2010-11-10 2012-05-18 Avila Therapeutics, Inc. Mutant-selective egfr inhibitors and uses thereof
WO2013106792A1 (en) * 2012-01-13 2013-07-18 Acea Biosciences Inc. Heterocyclic compounds and uses as anticancer agents.
RU2536586C2 (ru) * 2009-10-22 2014-12-27 Марсель Петер Герард МАЕС Система сигнализации с улучшенной контрастностью
RU2645672C2 (ru) * 2012-08-06 2018-02-27 Ацея Байосайенсиз Инк. Новые соединения пирролопиримидина в качестве ингибиторов протеинкиназ

Family Cites Families (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3974277A (en) 1974-09-06 1976-08-10 Diamond Shamrock Corporation 2-[2-(5-Nitro-2-furyl)vinyl]-4-(anilino)quinazolines as growth promotants and feed efficiency enhancing agents
EP1230225A2 (en) 1999-11-01 2002-08-14 Eli Lilly And Company Pharmaceutically active 4-substituted pyrimidine derivatives
EP1369418B1 (en) 2001-02-21 2010-07-28 Mitsubishi Tanabe Pharma Corporation Quinazoline derivatives
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
WO2003026664A1 (en) 2001-09-26 2003-04-03 Bayer Corporation 2-phenylamino-4- (5-pyrazolylamino) -pyramidine derivatives as kinase inhibitors, in particular, src kinase inhibitors
US7560269B2 (en) 2002-12-20 2009-07-14 Acea Biosciences, Inc. Real time electronic cell sensing system and applications for cytotoxicity profiling and compound assays
US7192752B2 (en) 2002-12-20 2007-03-20 Acea Biosciences Real time electronic cell sensing systems and applications for cell-based assays
US7732127B2 (en) 2002-12-20 2010-06-08 Acea Biosciences, Inc. Dynamic monitoring of cell adhesion and spreading using the RT-CES system
US7470533B2 (en) 2002-12-20 2008-12-30 Acea Biosciences Impedance based devices and methods for use in assays
US7468255B2 (en) 2002-12-20 2008-12-23 Acea Biosciences Method for assaying for natural killer, cytotoxic T-lymphocyte and neutrophil-mediated killing of target cells using real-time microelectronic cell sensing technology
WO2004010102A2 (en) 2002-07-20 2004-01-29 Acea Biosciences, Inc. Impedance based apparatuses and methods for analyzing cells and particles
AU2003265636A1 (en) 2002-09-06 2004-03-29 Smithkline Beecham Corporation Pyrrolo(2, 3-d)pyrimidine-4-yl and purin-6-yl urea compounds
TW200416034A (en) 2002-11-15 2004-09-01 Mitsubishi Pharma Corp Medicinal composition
CA2550361C (en) 2003-12-19 2014-04-29 Prabha Ibrahim Compounds and methods for development of ret modulators
NZ546058A (en) 2004-01-12 2010-09-30 Ym Biosciences Australia Pty Benzimidazole and other fused ring derivatives as selective janus kinase inhibitors
JP2007526339A (ja) 2004-03-02 2007-09-13 ニューロジェン・コーポレーション アリール置換プリン類縁体
CA2570817A1 (en) 2004-06-17 2006-01-26 Plexxikon, Inc. Azaindoles modulating c-kit activity and uses therefor
CA2572331A1 (en) 2004-07-02 2006-02-09 Exelixis, Inc. C-met modulators and method of use
BRPI0617167B8 (pt) 2005-09-21 2021-05-25 Nycomed Gmbh sulfonilpirróis como inibidores de hdac's, seu uso, composição farmacêutica e combinação
WO2007042298A1 (en) 2005-10-13 2007-04-19 Glaxo Group Limited Pyrrolopyrimidine derivatives as syk inhibitors
KR100832593B1 (ko) 2005-11-08 2008-05-27 한미약품 주식회사 신호전달 저해제로서의 퀴나졸린 유도체 및 이의 제조방법
GB0526246D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
CA2644494A1 (en) 2006-03-03 2007-09-13 Aveo Pharmaceuticals, Inc. Processes for synthesizing 7-alkynyl-4-aminoquinazolines and a related intermediate
CA2647543A1 (en) 2006-03-29 2007-11-08 Foldrx Pharmaceuticals, Inc. Inhibition of alpha-synuclein toxicity
WO2008039359A2 (en) 2006-09-25 2008-04-03 Janssen Pharmaceutica N.V. Bicyclic pyrimidine kinase inhibitors
BRPI0720264B1 (pt) 2006-12-08 2022-03-03 Novartis Ag Compostos e composições como inibidores de proteína cinase
CN101622001A (zh) 2007-01-26 2010-01-06 Irm责任有限公司 作为激酶抑制剂用于治疗疟原虫相关疾病的嘌呤化合物和组合物
US8846704B2 (en) 2007-01-31 2014-09-30 YM Biosciences Austraila Pty Ltd Thiopyrimidine-based compounds and uses thereof
TWI377944B (en) 2007-06-05 2012-12-01 Hanmi Holdings Co Ltd Novel amide derivative for inhibiting the growth of cancer cells
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
US7981903B2 (en) 2007-08-08 2011-07-19 Glaxosmithkline Llc 2-[2-{phenylamino}-1H-pyrrolo[2,3-D]pyrimidin-4-yl)amino] benzamide derivatives as IGF-1R inhibitors for the treatment of cancer
WO2009032703A1 (en) 2007-08-28 2009-03-12 Irm Llc 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors
CN105367503A (zh) 2007-10-19 2016-03-02 阿维拉制药公司 杂芳基化合物和其用途
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
NZ588830A (en) 2008-04-22 2012-11-30 Portola Pharm Inc Inhibitors of protein kinases
PT2300013T (pt) 2008-05-21 2017-10-31 Ariad Pharma Inc Derivados de fósforo como inibidores de cinases
US8338439B2 (en) * 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
WO2010045451A1 (en) 2008-10-16 2010-04-22 Glaxosmithkline Llc Pyrrolopyrimidine compounds
US20100204221A1 (en) 2009-02-09 2010-08-12 Hariprasad Vankayalapati Pyrrolopyrimidinyl axl kinase inhibitors
CN102639936B (zh) 2009-12-28 2016-05-04 巴西石油公司 高性能燃烧设备和用于生产轻石蜡的流体催化裂化工艺
US20130137709A1 (en) 2010-05-05 2013-05-30 Nathanael S. Gray Compounds that modulate EGFR activity and methods for treating or preventing conditions therewith
PT2585470T (pt) * 2010-06-23 2017-03-06 Hanmi Science Co Ltd Novos derivados fundidos de pirimidina para inibição da actividade da tirosina cinase
MX382354B (es) * 2010-11-01 2025-03-13 Celgene Car Llc Compuestos heterocíclicos y usos de los mismos.
CN102583089B (zh) 2011-01-11 2015-11-25 山东新北洋信息技术股份有限公司 薄片类介质处理装置
JP2014511391A (ja) 2011-03-07 2014-05-15 フォンダッツィオーネ・テレソン Ｔｆｅｂリン酸化阻害剤およびその使用
EP2694486B1 (en) 2011-04-01 2018-01-10 University of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
US9834518B2 (en) * 2011-05-04 2017-12-05 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in EGFR-driven cancers
US8828391B2 (en) 2011-05-17 2014-09-09 Boehringer Ingelheim International Gmbh Method for EGFR directed combination treatment of non-small cell lung cancer
CA2836449C (en) * 2011-05-17 2021-04-27 The Regents Of The University Of California Kinase inhibitors
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
US9586965B2 (en) 2012-01-13 2017-03-07 Acea Biosciences Inc. Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases
NZ715687A (en) 2013-07-11 2019-04-26 Acea Biosciences Inc Pyrimidine derivatives as kinase inhibitors
CN104306348B (zh) 2014-09-30 2017-05-31 地奥集团成都药业股份有限公司 一种辛伐他汀片及其制备方法
KR20180067584A (ko) 2015-10-09 2018-06-20 아세아 테라퓨틱스 인코포레이티드 피롤로피리미딘 키나아제 억제제의 약학적 염, 물리적 형태 및 조성물, 및 이들의 제조 방법
AU2017408099A1 (en) 2017-04-07 2019-11-07 ACEA Therapeutics, Inc. Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009158571A1 (en) * 2008-06-27 2009-12-30 Avila Therapeutics And Uses Thereof Heteroaryl compounds and uses thereof
WO2010129053A2 (en) * 2009-05-05 2010-11-11 Dana Farber Cancer Institute Egfr inhibitors and methods of treating disorders
US20120094999A1 (en) * 2009-05-05 2012-04-19 Dana-Farber Cancer Institute, Inc. Egfr inhibitors and methods of treating disorders
RU2536586C2 (ru) * 2009-10-22 2014-12-27 Марсель Петер Герард МАЕС Система сигнализации с улучшенной контрастностью
WO2011079231A1 (en) * 2009-12-23 2011-06-30 Gatekeeper Pharmaceutical, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
WO2012061303A1 (en) * 2010-11-01 2012-05-10 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof
WO2012064706A1 (en) * 2010-11-10 2012-05-18 Avila Therapeutics, Inc. Mutant-selective egfr inhibitors and uses thereof
WO2013106792A1 (en) * 2012-01-13 2013-07-18 Acea Biosciences Inc. Heterocyclic compounds and uses as anticancer agents.
RU2645672C2 (ru) * 2012-08-06 2018-02-27 Ацея Байосайенсиз Инк. Новые соединения пирролопиримидина в качестве ингибиторов протеинкиназ

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
Chun Han; et al., Novel Hybrids of (phenylsulfonyl)furoxan and Anilinopyrimidine as Potent and Selective Epidermal Growth Factor Receptor Inhibitors for intervention of Non-Small-Gell Lung Cancer, Journal of Medicinal Chemistry, 13.05.2013, vol.56,p.4738-4748. RU 2645672 C2, 27.02.2018, приоритеты 06.08.2012, 15.03.2013, 19.04.2013, 13.06.2013. Cortot, Alexis B.; et al., Resistance to Irreversible EGF Receptor Tyrosine Kinase Inhibitors through a Multistep Mechanism Involving the IGF1R Pathway. Cancer Research, 2013, 73(2),834-843. *
Wenjun Zhou et al. Discovery of selective irreversible inhibitors for EGFR T790M, bioorganic & Medicinal Chemistry Letters, 2011,vol.21, p.638-643. *
Wenjun Zhou et al., Novel mutant-selective EGFR kinase inhibitorsagainst EGFR T790M, NATURE, 2009, vol.462, no.24, p. 1070-1074. *
Wenjun Zhou et al., Novel mutant-selective EGFR kinase inhibitorsagainst EGFR T790M, NATURE, 2009, vol.462, no.24, p. 1070-1074. Wenjun Zhou et al. Discovery of selective irreversible inhibitors for EGFR T790M, bioorganic & Medicinal Chemistry Letters, 2011,vol.21, p.638-643. Chun Han; et al., Novel Hybrids of (phenylsulfonyl)furoxan and Anilinopyrimidine as Potent and Selective Epidermal Growth Factor Receptor Inhibitors for intervention of Non-Small-Gell Lung Cancer, Journal of Medicinal Chemistry, 13.05.2013, vol.56,p.4738-4748. *
приоритеты 06.08.2012, 15.03.2013, 19.04.2013, 13.06.2013. Cortot, Alexis B.; et al., Resistance to Irreversible EGF Receptor Tyrosine Kinase Inhibitors through a Multistep Mechanism Involving the IGF1R Pathway. Cancer Research, 2013, 73(2),834-843. *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2702631C2 (ru) * 2014-10-11 2019-10-09 Шанхай Хэнсох Биомедикал Ко., Лтд. Ингибитор egfr и его получение и применение
RU2743040C2 (ru) * 2015-07-09 2021-02-12 Мерк Патент Гмбх Производные пиримидина в качестве btk ингибиторов и их применение

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