BR112012033253A2 - novos derivados de pirimidina fundidos para inibição da atividade de tirosina quinase - Google Patents

novos derivados de pirimidina fundidos para inibição da atividade de tirosina quinase

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Publication number
BR112012033253A2
BR112012033253A2 BR112012033253A BR112012033253A BR112012033253A2 BR 112012033253 A2 BR112012033253 A2 BR 112012033253A2 BR 112012033253 A BR112012033253 A BR 112012033253A BR 112012033253 A BR112012033253 A BR 112012033253A BR 112012033253 A2 BR112012033253 A2 BR 112012033253A2
Authority
BR
Brazil
Prior art keywords
inhibition
tyrosine kinase
kinase activity
pyrimidine derivatives
fused pyrimidine
Prior art date
Application number
BR112012033253A
Other languages
English (en)
Inventor
Eun Joo Kwak
Ji Young Jeon
Ju Yeon Lee
Kwang Ok Lee
Kwee Hyun Suh
Maeng Sup Kim
Mi Ra Kim
Mi Young Cha
Myoung Gi Jo
Seok Jong Kang
Tae Hee Ha
Original Assignee
Hanmi Science Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45371929&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR112012033253(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hanmi Science Co Ltd filed Critical Hanmi Science Co Ltd
Priority to BR122014012788-0A priority Critical patent/BR122014012788B1/pt
Publication of BR112012033253A2 publication Critical patent/BR112012033253A2/pt

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    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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    • 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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Abstract

novos derivados de pirimidina fundidos para inibição da atividade de tirosina quinase. a presente invenção refere-se a um novo derivado de pirimidina contendo uma atividade e inibitória para tirosinas quinases, e uma composição farmacêutica para prevenir ou tratar cânceres, tumores, doenças inflamatórias, doenças autoimunes, ou doenças mediadas imunologicamente compreendendo o mesmo como um lingrediente ativo.
BR112012033253A 2010-06-23 2011-06-20 novos derivados de pirimidina fundidos para inibição da atividade de tirosina quinase BR112012033253A2 (pt)

Priority Applications (1)

Application Number Priority Date Filing Date Title
BR122014012788-0A BR122014012788B1 (pt) 2010-06-23 2011-06-20 Derivados de pirimidina fundidos, seus usos, e composição farmacêutica para inibição da atividade de tirosina quinase

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR20100059686 2010-06-23
PCT/KR2011/004482 WO2011162515A2 (en) 2010-06-23 2011-06-20 Novel fused pyrimidine derivatives for inhd3ition of tyrosine kinase activity

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Families Citing this family (120)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0622054B8 (pt) 2006-09-22 2021-05-25 Oxford Amherst Llc composto e composição farmacêutica
US20120101113A1 (en) 2007-03-28 2012-04-26 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
DK2300013T3 (en) 2008-05-21 2017-12-04 Ariad Pharma Inc PHOSPHORUS DERIVATIVES AS KINASE INHIBITORS
MX2011000661A (es) 2008-07-16 2011-05-25 Pharmacyclics Inc Inhibidores de tirosina cinasa de bruton para el tratamiento de tumores solidos.
IL300955A (en) 2010-06-03 2023-04-01 Pharmacyclics Llc (R)-1-(3-(4-amino-3-(4-phenoxyphenyl)-H1-pyrazolo[4,3-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1- Indicated for use as a drug to treat chronic lymphocytic leukemia or small lymphocytic lymphoma
LT2975042T (lt) * 2010-06-23 2019-01-25 Hanmi Science Co., Ltd. Naujieji kondensuoti pirimidino dariniai, skirti tirozino kinazės aktyvumo slopinimui
MX2013003913A (es) * 2010-10-08 2013-09-26 Abbvie Inc Compuestos de furo [3, 2-d] pirimidina.
EA201390550A1 (ru) * 2010-10-14 2013-08-30 Ариад Фармасьютикалз, Инк. Способы ингибирования пролиферации клеток в egfr-стимулируемых злокачественных опухолях
AU2012250517B2 (en) * 2011-05-04 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
KR20140048968A (ko) 2011-07-13 2014-04-24 파마시클릭스, 인코포레이티드 브루톤형 티로신 키나제의 억제제
PL3686194T3 (pl) 2011-07-27 2022-01-17 Astrazeneca Ab Związki 2-(2,4,5-podstawione-anilino)pirymidynowe
KR20130076046A (ko) * 2011-12-28 2013-07-08 한미약품 주식회사 타이로신 카이네이즈 억제 활성을 갖는 신규 이미다조피리딘 유도체
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
EP2802568A1 (en) 2012-01-13 2014-11-19 Acea Biosciences, Inc. Heterocyclic compounds and uses as anticancer agents.
US9586965B2 (en) 2012-01-13 2017-03-07 Acea Biosciences Inc. Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases
KR20130091464A (ko) * 2012-02-08 2013-08-19 한미약품 주식회사 타이로신 카이네이즈 억제 활성을 갖는 트리아졸로피리딘 유도체
ES2580530T3 (es) * 2012-02-23 2016-08-24 Taiho Pharmaceutical Co., Ltd. Compuesto con anillo fusionado de quinolilpirrolopirimidilo o sal del mismo
AU2013204563B2 (en) 2012-05-05 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
UA114421C2 (uk) 2012-06-04 2017-06-12 Фармасайклікс Ллс Кристалічна форма інгібітору тирозинкінази брутона
WO2013184766A1 (en) * 2012-06-06 2013-12-12 Irm Llc Compounds and compositions for modulating egfr activity
CN104704129A (zh) 2012-07-24 2015-06-10 药品循环公司 与对布鲁顿酪氨酸激酶(btk)抑制剂的抗性相关的突变
MX2015006168A (es) 2012-11-15 2015-08-10 Pharmacyclics Inc Compuestos de pirrolopirimidina como inhibidores de quinasas.
KR20150119401A (ko) 2013-02-22 2015-10-23 다이호야쿠힌고교 가부시키가이샤 3환성 화합물의 제조 방법 및 상기 제조 방법에 의해 얻을 수 있는 3환성 화합물
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
CN103242341B (zh) * 2013-04-19 2015-12-09 中国科学院广州生物医药与健康研究院 噻吩并2，4取代嘧啶类化合物及其药物组合物与应用
CA2902686C (en) 2013-04-25 2017-01-24 Beigene, Ltd. Fused heterocyclic compounds as protein kinase inhibitors
WO2014175370A1 (ja) * 2013-04-25 2014-10-30 塩野義製薬株式会社 ピロリジン誘導体およびそれらを含有する医薬組成物
JP6564771B2 (ja) * 2013-07-11 2019-08-21 エイシア バイオサイエンシーズ インコーポレイテッド キナーゼ阻害剤としてのピリミジン誘導体
EP2832358A1 (en) 2013-08-02 2015-02-04 Bionsil S.r.l. Pharmaceutical kit for use in the treatment of colon and colorectal cancer
TWI649081B (zh) 2013-08-02 2019-02-01 製藥公司 治療固態腫瘤之方法
US9415050B2 (en) 2013-08-12 2016-08-16 Pharmacyclics Llc Methods for the treatment of HER2 amplified cancer
AU2013400609B9 (en) 2013-09-13 2020-03-05 Beigene Switzerland Gmbh Anti-PD1 antibodies and their use as therapeutics and diagnostics
RU2650512C2 (ru) 2013-09-18 2018-04-16 Бейджин Ханми Фармасьютикал Ко., Лтд. Соединение, ингибирующее активности киназ ВТК и/или JAK3
MA38961A1 (fr) 2013-09-30 2018-05-31 Pharmacyclics Llc Composés 3-phenyl-1h-pyrazolo[3,4-d]pyrimidin-4-ylamine substitués inhibiteurs de la tyrosine kinase de bruton utilisés pour traiter par exemple les maladies auto-immunes, respiratoires et inflammatoires, cancer, mastocytose et osteoporose
FR3015483B1 (fr) * 2013-12-23 2016-01-01 Servier Lab Nouveaux derives de thienopyrimidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
WO2015143400A1 (en) 2014-03-20 2015-09-24 Pharmacyclics, Inc. Phospholipase c gamma 2 and resistance associated mutations
WO2015148904A1 (en) * 2014-03-28 2015-10-01 Driver Group Methods for predicting egfr tyrosine kinase inhibitor efficacy
CN106659765B (zh) 2014-04-04 2021-08-13 德玛医药 二脱水半乳糖醇及其类似物或衍生物用于治疗非小细胞肺癌和卵巢癌的用途
KR20160144399A (ko) 2014-05-01 2016-12-16 노파르티스 아게 톨-유사 수용체 7 효능제로서의 화합물 및 조성물
KR102139847B1 (ko) 2014-05-01 2020-07-31 노파르티스 아게 톨-유사 수용체 7 효능제로서의 화합물 및 조성물
MA39908A (fr) * 2014-05-28 2015-12-03 Astellas Pharma Inc Composition médicinale comprenant un composé pyrazine carboxamide utilisé comme principe actif
WO2016000619A1 (en) 2014-07-03 2016-01-07 Beigene, Ltd. Anti-pd-l1 antibodies and their use as therapeutics and diagnostics
EP2974729A1 (en) * 2014-07-17 2016-01-20 Abivax Quinoline derivatives for use in the treatment of inflammatory diseases
CA2959602A1 (en) 2014-08-01 2016-02-04 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
BR112017002231A2 (pt) 2014-08-07 2018-07-17 Pharmacyclics Llc novas formulações de um inibidor de tirosina cinase de bruton
AR101476A1 (es) 2014-08-07 2016-12-21 Acerta Pharma Bv Métodos para tratar cánceres, enfermedades inmunes y autoinmunes, y enfermedades inflamatorias en base a la tasa de ocupación de la tirosin quinasa de bruton (btk) y a la tasa de resíntesis de la tirosin quinasa de bruton (btk)
US10040801B2 (en) 2014-12-30 2018-08-07 Hanmi Pharm. Co., Ltd. Method for preparing thienopyrimidine compound and intermediates used therein
KR20160082062A (ko) 2014-12-30 2016-07-08 한미약품 주식회사 싸이옥소 퓨로피리미디논 유도체의 제조방법 및 이에 사용되는 중간체
CN105837572B (zh) * 2015-02-02 2019-04-19 四川大学 N-取代苯基酰胺衍生物及其制备方法和用途
RU2572709C1 (ru) * 2015-03-03 2016-01-20 Государственное бюджетное образовательное учреждение высшего профессионального образования "Курский государственный медицинский университет" Министерства здравоохранения Российской Федерации Способ коррекции структурно-функциональных нарушений артериального русла у больных ревматоидным артритом
SG11201707122QA (en) 2015-03-03 2017-09-28 Pharmacyclics Llc Pharmaceutical formulations of bruton's tyrosine kinase inhibtor
EP3312179B1 (en) 2015-04-29 2019-07-10 Nanjing Sanhome Pharmaceutical Co., Ltd. Fused-ring or tricyclic aryl pyrimidine compound used as kinase inhibitor
CA2992161A1 (en) 2015-07-17 2017-01-26 Institut Pasteur 5-hydroxytryptamine 1b receptor-stimulating agent for use as a promoter of satellite cells self-renewal and/or differentiation
MA44909A (fr) 2015-09-15 2018-07-25 Acerta Pharma Bv Association thérapeutique d'un inhibiteur du cd19 et d'un inhibiteur de la btk
CN107949388B (zh) 2015-10-09 2021-10-26 艾森医药公司 吡咯并嘧啶激酶抑制剂的药用盐、物理形态和组合物及其制备方法
MA44334A (fr) 2015-10-29 2018-09-05 Novartis Ag Conjugués d'anticorps comprenant un agoniste du récepteur de type toll
KR20170050453A (ko) * 2015-10-30 2017-05-11 한미약품 주식회사 싸이에노피리미딘 화합물의 신규 제조방법 및 이에 사용되는 중간체
CN108137614B (zh) * 2015-12-02 2021-01-05 深圳市塔吉瑞生物医药有限公司 一种稠合嘧啶化合物及包含该化合物的组合物及其用途
EP3383401B1 (en) * 2015-12-03 2020-05-20 Zheijiang Jianfreng-Yien Biotechnology Co., Ltd. Thieno-pyrimidine derivatives and uses thereof
US10844074B2 (en) 2015-12-03 2020-11-24 Zhejiang Jianfeng-Yien Biotechnology Co., Ltd. Heterocycle compounds and uses thereof
AU2016382385A1 (en) 2015-12-31 2018-07-12 Hanmi Pharm. Co., Ltd. Crystalline forms of thienopyrimidine compound
RU2018122050A (ru) * 2015-12-31 2020-01-31 Ханми Фарм. Ко., Лтд. Кристаллические формы гидрохлоридных солей тиенопиримидинового соединения
PL3402503T3 (pl) 2016-01-13 2021-04-19 Acerta Pharma B.V. Kombinacje terapeutyczne antyfolianu oraz inhibitora btk
WO2017198602A1 (en) * 2016-05-18 2017-11-23 Boehringer Ingelheim International Gmbh Anticancer combination therapy
WO2017204582A1 (en) * 2016-05-27 2017-11-30 Hanmi Pharm. Co., Ltd. Pharmaceutical composition comprising an amide derivative or a pharmaceutically acceptable salt thereof inhibiting growth of cancer cells and a stabilizer having low melting point
JP2019519579A (ja) 2016-06-30 2019-07-11 デウン ファーマシューティカル カンパニー リミテッド キナーゼ阻害剤としてのピラゾロピリミジン誘導体
CN109475536B (zh) 2016-07-05 2022-05-27 百济神州有限公司 用于治疗癌症的PD-l拮抗剂和RAF抑制剂的组合
BR112019000706A8 (pt) 2016-07-15 2022-12-06 Pasteur Institut Agente de estímulo do receptor 1b de 5-hidroxitriptamina para reparo de pele e/ou cabelo
CN107698603B (zh) 2016-08-09 2022-04-08 南京红云生物科技有限公司 噻吩并嘧啶类化合物、其制备方法、药用组合物及其应用
AU2017314178B2 (en) 2016-08-16 2021-11-18 Beigene Switzerland Gmbh Crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
EP4353747A2 (en) 2016-08-19 2024-04-17 BeiGene Switzerland GmbH Combination of zanubrutinib with an anti-cd20 or an anti-pd-1 antibody for use in treating cancer
US20190201409A1 (en) 2016-09-19 2019-07-04 Mei Pharma, Inc. Combination therapy
CN106565612B (zh) * 2016-10-25 2018-10-16 大连医科大学 二苯乙烯基嘧啶类化合物，组合物及其用途
CN110545826A (zh) 2016-12-03 2019-12-06 朱诺治疗学股份有限公司 用于与激酶抑制剂组合使用治疗性t细胞的方法和组合物
KR20180075228A (ko) * 2016-12-26 2018-07-04 한미약품 주식회사 싸이에노피리미딘 화합물의 신규 제조방법 및 중간체
WO2018134786A1 (en) 2017-01-19 2018-07-26 Acerta Pharma B.V. Compositions and methods for the assessment of drug target occupancy for bruton's tyrosine kinase
WO2018137681A1 (en) 2017-01-25 2018-08-02 Beigene, Ltd. Crystalline forms of (s) -7- (1- (but-2-ynoyl) piperidin-4-yl) -2- (4-phenoxyphenyl) -4, 5, 6, 7-tetrahy dropyrazolo [1, 5-a] pyrimidine-3-carboxamide, preparation, and uses thereof
WO2018139883A1 (ko) * 2017-01-26 2018-08-02 부광약품 주식회사 다중 표적 키나아제 저해제로서 융합피리미딘 유도체
CN106831814B (zh) * 2017-02-15 2018-11-23 山东大学 一种噻吩并[3,2-d]嘧啶类HIV-1逆转录酶抑制剂及其制备方法和应用
CN106916112B (zh) * 2017-03-02 2019-12-20 四川海思科制药有限公司 嘧啶衍生物及其制备方法和在医药上的应用
CN106866699B (zh) * 2017-03-29 2019-03-08 山东大学 一种二芳基噻吩并嘧啶类hiv-1逆转录酶抑制剂及其制备方法和应用
CN111212837A (zh) 2017-04-07 2020-05-29 艾森医药公司 吡咯并嘧啶激酶抑制剂的药用盐、物理形态和组合物及其制备方法
CN108727382B (zh) * 2017-04-19 2022-07-19 华东理工大学 作为btk抑制剂的杂环化合物及其应用
US11597768B2 (en) 2017-06-26 2023-03-07 Beigene, Ltd. Immunotherapy for hepatocellular carcinoma
CN109206435B (zh) * 2017-06-29 2020-09-08 中国医药研究开发中心有限公司 噻吩并[3,2-d]嘧啶类化合物及其制备方法和医药用途
CN110997677A (zh) 2017-08-12 2020-04-10 百济神州有限公司 具有改进的双重选择性的Btk抑制剂
US20200172529A1 (en) * 2017-08-18 2020-06-04 Beijing Hanmi Pharm. Co., Ltd. Chemical Compound, Pharmaceutical Composition Thereof, and Use and Application Thereof
CN109575045B (zh) * 2017-09-28 2021-02-12 南京红云生物科技有限公司 噻吩并嘧啶类化合物、其制备方法、药用组合物及其应用
KR102613433B1 (ko) * 2017-10-11 2023-12-13 주식회사 대웅제약 신규한 페닐피리딘 유도체 및 이를 포함하는 약학 조성물
SG11202004019SA (en) 2017-11-17 2020-05-28 Cellix Bio Private Ltd Compositions and methods for the treatment of eye disorders
CN111801334B (zh) 2017-11-29 2023-06-09 百济神州瑞士有限责任公司 使用包含btk抑制剂的组合治疗惰性或侵袭性b-细胞淋巴瘤
JP7043098B2 (ja) * 2017-12-21 2022-03-29 深▲チェン▼市塔吉瑞生物医薬有限公司 キナーゼ活性を阻害するためのジアニリノピリミジン系化合物
KR102577241B1 (ko) * 2017-12-28 2023-09-11 주식회사 대웅제약 카이네이즈 저해제로서의 아미노-플루오로피페리딘 유도체
RS63515B1 (sr) 2017-12-28 2022-09-30 Daewoong Pharmaceutical Co Ltd Derivat oksi-fluoropiperidina kao inhibitor kinaze
KR102577242B1 (ko) * 2017-12-28 2023-09-11 주식회사 대웅제약 카이네이즈 저해제로서의 아미노-메틸피페리딘 유도체
LT3784663T (lt) * 2018-04-23 2023-10-25 Celgene Corporation Pakeistieji 4-aminoizoindolin-1,3-diono junginiai ir jų naudojimas limfomos gydymui
WO2019208805A1 (ja) 2018-04-27 2019-10-31 小野薬品工業株式会社 Ｂｔｋ阻害活性を有する化合物を有効成分として含む自己免疫疾患の予防および／または治療剤
US20210308140A1 (en) 2018-07-25 2021-10-07 Novartis Ag Nlrp3 inflammasome inhibitors
KR101954370B1 (ko) * 2018-07-25 2019-03-05 한미약품 주식회사 피리미딘 화합물 및 이를 포함하는 암의 예방 또는 치료용 약학 조성물
US20220362357A1 (en) 2018-08-31 2022-11-17 Stichting Radboud Universitair Medisch Centrum Synergistic Combinations of Amino Acid Depletion Agent Sensitizers (AADAS) and Amino Acid Depletion Agents (AADA), and Therapeutic Methods of Use Thereof
CN109265469A (zh) * 2018-11-12 2019-01-25 大连医科大学附属第医院 嘧啶并噻唑类杂环化合物，组合物及其治疗淋巴细胞白血病的用途
KR20200114776A (ko) * 2019-03-29 2020-10-07 한미약품 주식회사 퓨로피리미딘 화합물의 산 부가염의 결정형
CN111747931A (zh) * 2019-03-29 2020-10-09 深圳福沃药业有限公司 用于治疗癌症的氮杂芳环酰胺衍生物
CN111909101B (zh) * 2019-05-10 2022-07-19 浙江大学 一种egfr激酶抑制剂及其在制备抗癌药物方面的应用
AR119731A1 (es) 2019-05-17 2022-01-05 Novartis Ag Inhibidores del inflamasoma nlrp3
JP2022534650A (ja) * 2019-05-31 2022-08-03 海思科医▲薬▼有限公司 Ｂｔｋ阻害薬環誘導体、その調製方法及びその医薬品適用
WO2020257385A1 (en) * 2019-06-20 2020-12-24 Dana-Farber Cancer Institute, Inc. Small molecule inhibitors of src tyrosine kinase
CN110372529B (zh) * 2019-08-08 2022-05-24 黄河水利职业技术学院 N-[(3,4,5-三氟)苯基]丙烯酰胺及其制备方法
CN110511994B (zh) * 2019-09-09 2023-05-26 中南大学湘雅二医院 miRNA-4769-3p及其同源物的应用
EP4077316A1 (en) * 2019-12-20 2022-10-26 Pfizer Inc. Benzimidazole derivatives
BR112022024729A2 (pt) 2020-06-05 2023-02-28 Kinnate Biopharma Inc Inibidores de quinases do receptor do fator de crescimento de fibroblastos
CN116239603A (zh) * 2020-06-20 2023-06-09 江西科技师范大学 一种2-氨基嘧啶杂环类化合物及其应用
UY39377A (es) 2020-08-14 2022-03-31 Novartis Ag Derivados de espiropiperidinilo sustituidos con heteroarilo y usos farmacéuticos de los mismos
JP2023547220A (ja) * 2020-10-29 2023-11-09 蘇州亜宝薬物研発有限公司 置換ジアリールアミン化合物及びその医薬組成物、製造方法と用途
WO2022212893A1 (en) 2021-04-02 2022-10-06 Biogen Ma Inc. Combination treatment methods of multiple sclerosis
US11786531B1 (en) 2022-06-08 2023-10-17 Beigene Switzerland Gmbh Methods of treating B-cell proliferative disorder
TW202406550A (zh) 2022-08-03 2024-02-16 瑞士商諾華公司 Ｎｌｒｐ３炎性小體抑制劑

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP970371A2 (en) * 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
MXPA06001590A (es) * 2003-08-19 2006-05-19 Wyeth Corp Proceso para la preparacion de 4-amino-3-quinolincarbonitrilos.
BRPI0706747A2 (pt) 2006-01-30 2011-04-05 Exelixis Inc 4-aril-2-amino-pirimidinas ou 4-aril-2-aminoalquil-pirimidinas como moduladores jak-2 e composições farmacêuticas que os contenham
JP2008013527A (ja) * 2006-07-10 2008-01-24 Sankyo Co Ltd チエノ［３，２−ｄ］ピリミジン−２，４−ジアミン誘導体
KR101507182B1 (ko) * 2006-12-07 2015-03-30 제넨테크, 인크. 포스포이노시타이드 3-키나제 억제제 화합물 및 그의 사용 방법
WO2008152394A1 (en) * 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Pharmaceutical compounds
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
CA2703600C (en) * 2007-11-15 2017-04-25 Ym Biosciences Australia Pty Ltd Fused thieno or pyrrolo pyrimidine heterocyclic compounds and use thereof as jak1, jak2, and/or jak3 inhibitors
CA2720946C (en) 2008-04-07 2013-05-28 Irm Llc Compounds and compositions as protein kinase inhibitors
ES2711249T3 (es) * 2008-06-27 2019-04-30 Celgene Car Llc Compuestos de heteroarilo y usos de los mismos
TWI385174B (zh) * 2008-11-10 2013-02-11 Nat Health Research Institutes 作為酪胺酸激酶抑制劑之稠合雙環及多環嘧啶化合物
WO2010129053A2 (en) 2009-05-05 2010-11-11 Dana Farber Cancer Institute Egfr inhibitors and methods of treating disorders
US20110207736A1 (en) 2009-12-23 2011-08-25 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
LT2975042T (lt) * 2010-06-23 2019-01-25 Hanmi Science Co., Ltd. Naujieji kondensuoti pirimidino dariniai, skirti tirozino kinazės aktyvumo slopinimui
JP5914667B2 (ja) * 2011-09-22 2016-05-11 ファイザー・インク ピロロピリミジンおよびプリン誘導体

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