JP6670756B2 - ブルトン型チロシンキナーゼ（ｂｔｋ）インヒビターとしての多フルオロ置換化合物 - Google Patents

ブルトン型チロシンキナーゼ（ｂｔｋ）インヒビターとしての多フルオロ置換化合物 Download PDF

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JP6670756B2
JP6670756B2 JP2016565402A JP2016565402A JP6670756B2 JP 6670756 B2 JP6670756 B2 JP 6670756B2 JP 2016565402 A JP2016565402 A JP 2016565402A JP 2016565402 A JP2016565402 A JP 2016565402A JP 6670756 B2 JP6670756 B2 JP 6670756B2
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フー，ウェイ
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チョーチアン ディーティーアールエム バイオファーマ コーポレーション リミテッド
チョーチアン ディーティーアールエム バイオファーマ コーポレーション リミテッド
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JP2016565402A 2014-04-29 2015-04-27 ブルトン型チロシンキナーゼ（ｂｔｋ）インヒビターとしての多フルオロ置換化合物 Active JP6670756B2 (ja)

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CN201410175783.7 2014-04-29
CN201410175783.7A CN105017256A (zh) 2014-04-29 2014-04-29 多氟化合物作为布鲁顿酪氨酸激酶抑制剂
PCT/CN2015/000290 WO2015165279A1 (zh) 2014-04-29 2015-04-27 多氟化合物作为布鲁顿酪氨酸激酶抑制剂

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US (3) US9532990B2 (https=)
EP (1) EP3138842B1 (https=)
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KR (2) KR20160144378A (https=)
CN (3) CN105017256A (https=)
AU (1) AU2015252654C1 (https=)
BR (1) BR112016025132A2 (https=)
CA (1) CA2947338C (https=)
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JP2020040989A (ja) * 2014-04-29 2020-03-19 チョーチアン ディーティーアールエム バイオファーマ コーポレーション リミテッド ブルトン型チロシンキナーゼ（ｂｔｋ）インヒビターとしての多フルオロ置換化合物

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015008844A1 (ja) 2013-07-18 2015-01-22 大鵬薬品工業株式会社 Ｆｇｆｒ阻害剤耐性癌の治療薬
TR201907147T4 (tr) 2013-07-18 2019-06-21 Taiho Pharmaceutical Co Ltd Fgfr inhibitörünün aralıklı uygulanmasına yönelik anti-tümör ilaç.
EP3221320A4 (en) * 2014-11-19 2018-04-25 Sun Pharmaceutical Industries Ltd A process for the preparation of ibrutinib
US10214532B2 (en) 2015-02-12 2019-02-26 Shanghai Dude Medical Science and Technology Co., Ltd. Process for preparing ibrutinib
CN106146508A (zh) * 2015-03-19 2016-11-23 浙江导明医药科技有限公司 优化的联合用药及其治疗癌症和自身免疫疾病的用途
US9717745B2 (en) 2015-03-19 2017-08-01 Zhejiang DTRM Biopharma Co. Ltd. Pharmaceutical compositions and their use for treatment of cancer and autoimmune diseases
CN106146511A (zh) * 2015-04-03 2016-11-23 安润医药科技（苏州）有限公司 吡唑并嘧啶衍生物、制备方法、药物组合物及用途
CN106146512B (zh) * 2015-04-09 2018-07-17 北京睿创康泰医药研究院有限公司 依鲁替尼的制备方法
CA2981886A1 (en) 2015-04-16 2016-10-20 Icahn School Of Medicine At Mount Sinai Ksr antagonists
EP3424505A4 (en) 2016-03-04 2019-10-16 Taiho Pharmaceutical Co., Ltd. PREPARATION AND COMPOSITION FOR THE TREATMENT OF MALIGNANT TUMORS
US11883404B2 (en) 2016-03-04 2024-01-30 Taiho Pharmaceuticals Co., Ltd. Preparation and composition for treatment of malignant tumors
JP6959252B2 (ja) 2016-03-24 2021-11-02 ミッション セラピューティクス リミティド Ｄｕｂ阻害剤としての１−シアノピロリジン誘導体
WO2018002958A1 (en) 2016-06-30 2018-01-04 Sun Pharma Advanced Research Company Limited Novel hydrazide containing compounds as btk inhibitors
CN106146518A (zh) * 2016-06-30 2016-11-23 苏州爱玛特生物科技有限公司 一种布鲁顿酪氨酸激酶抑制剂中间体及其制备方法
GB201616511D0 (en) 2016-09-29 2016-11-16 Mission Therapeutics Limited Novel compounds
JP6782855B2 (ja) * 2016-11-15 2020-11-11 杭州和正医薬有限公司 選択性ブルトン型チロシンキナーゼ阻害剤及びその使用
MA46995A (fr) 2016-12-03 2019-10-09 Acerta Pharma Bv Méthodes et compositions pour l'utilisation de lymphocytes t thérapeutiques en association avec des inhibiteurs de kinase
CN106831788B (zh) * 2017-01-22 2020-10-30 鲁南制药集团股份有限公司 伊布替尼精制方法
KR102627756B1 (ko) 2017-03-22 2024-01-23 쑤저우 바이지부공 파마수티컬 테크널러지 컴퍼니 리미티드 브루톤 타이로신 키나제 억제제
CN107501270B (zh) * 2017-09-01 2019-06-28 宏腾建设集团有限公司 一种含有磺酰吖丙啶结构的化合物、药物组合物以及其应用
TW201922256A (zh) 2017-10-27 2019-06-16 中國大陸商浙江導明醫藥科技有限公司 治療淋巴樣惡性疾病之方法
CN109970740A (zh) * 2017-12-27 2019-07-05 广东众生药业股份有限公司 4-氨基-嘧啶并氮杂环衍生物及其制备方法和用途
SG11202008435SA (en) 2018-03-19 2020-10-29 Taiho Pharmaceutical Co Ltd Pharmaceutical composition including sodium alkyl sulfate
CN110964016B (zh) 2018-09-29 2021-05-28 南京药捷安康生物科技有限公司 氨基降茨烷衍生物及其制备方法与应用
CN113260618A (zh) * 2018-11-09 2021-08-13 大鹏药品工业株式会社 二甲氧基苯化合物类似物、分析所述化合物的方法和所述化合物的标准品
CN111171035B (zh) * 2018-11-13 2021-03-30 山东大学 4-苯氧基苯基吡唑并嘧啶酰胺衍生物的制备方法和应用
CN111454268B (zh) * 2019-01-18 2023-09-08 明慧医药（上海）有限公司 作为布鲁顿酪氨酸激酶抑制剂的环状分子
CA3133184A1 (en) 2019-03-15 2020-09-24 Bayer Aktiengesellschaft Specifically substituted 3-phenyl-5-spirocyclopentyl-3-pyrrolin-2-ones and their use as herbicides
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
CA3139285A1 (en) * 2019-06-27 2020-12-30 Hangzhou Healzen Therapeutics Co., Ltd. Casein kinase 1e inhibitor, pharmaceutical composition and application thereof
WO2021038540A1 (en) 2019-08-31 2021-03-04 Sun Pharma Advanced Research Company Limited Cycloalkylidene carboxylic acids and derivatives as btk inhibitors
HUE065965T2 (hu) * 2019-09-26 2024-06-28 Jumbo Drug Bank Co Ltd 4-fluor-1H-pyrazolo[3,4-C]piridin-származékok mint szelektív bruton-tirozinkináz (BTK) inhibitorok a B-sejtes limfóma és autoimmun betegségek kezelésére
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
TW202144465A (zh) 2020-02-11 2021-12-01 瑞士商諾和席卓股份有限公司 合成聚葡萄胺糖衍生物之新方法及其用途
EP3865535A1 (en) 2020-02-11 2021-08-18 Bosti Trading Ltd. New method of synthesis of chitosan derivatives and uses thereof
AU2020436612A1 (en) * 2020-03-16 2022-09-01 Flash Therapeutics, Llc Compounds for treating or inhibiting recurrence of acute myeloid leukemia
MX2022015495A (es) 2020-06-08 2023-03-14 Halia Therapeutics Inc Inhibidores de cinasa relacionada con el gen a nunca en mitosis (nek7).
CN113943294A (zh) * 2020-07-15 2022-01-18 成都海博为药业有限公司 一种作为btk抑制剂的化合物及其制备方法与用途
WO2022081512A1 (en) * 2020-10-12 2022-04-21 Synubi Pharmaceuticals Llc Compositions and methods of treatment of neuroinflammatory diseases with bruton's tyrosine kinase inhibitors
CN112574046A (zh) * 2020-12-17 2021-03-30 深圳市华先医药科技有限公司 一种制备(1r,3s)-3-氨基环戊醇盐酸盐的方法
US20240100172A1 (en) 2020-12-21 2024-03-28 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
WO2022137240A1 (en) * 2020-12-23 2022-06-30 Yeda Research And Development Co. Ltd. Methacrylamides protein binders and uses thereof
ES3010513T3 (en) * 2021-02-03 2025-04-03 Accutar Biotechnology Inc Substituted pyrrolopyrimidine and pyrazolopyrimidine as bruton's tyrosine kinase (btk) degraders
AR126678A1 (es) 2021-08-06 2023-11-01 Novochizol Sa Composiciones para el cuidado de las plantas y usos de las mismas
US12403221B2 (en) 2021-08-06 2025-09-02 Novochizol Sa Preparation of composite gels, polymer scaffolds, aggregates and films comprising soluble cross-linked chitosan and uses thereof
CN114605418B (zh) * 2022-03-15 2023-09-05 广东医科大学附属医院 一类具有抗肿瘤活性的依鲁替尼丙烯酰胺类衍生物及其合成方法与应用
CN117430610A (zh) * 2023-10-11 2024-01-23 宁夏医科大学 一种氘代稠合杂环化合物及其制备方法和应用
CN117903141B (zh) * 2023-12-19 2024-11-05 江苏长泰药业股份有限公司 一种化合物及其盐、在制备治疗癌症药物和激酶抑制剂中的用途、治疗癌症的药物
WO2025202889A1 (en) * 2024-03-28 2025-10-02 Array Biopharma Inc. Her2 mutation inhibitors

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040127470A1 (en) * 1998-12-23 2004-07-01 Pharmacia Corporation Methods and compositions for the prevention or treatment of neoplasia comprising a Cox-2 inhibitor in combination with an epidermal growth factor receptor antagonist
GB0402143D0 (en) * 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
BRPI0622054B8 (pt) * 2006-09-22 2021-05-25 Oxford Amherst Llc composto e composição farmacêutica
EP1921149A1 (en) 2006-11-13 2008-05-14 AEterna Zentaris GmbH Microorganisms as carriers of nucleotide sequences coding for antigens and protein toxins, process of manufacturing and uses thereof
IL295053A (en) 2007-03-28 2022-09-01 Pharmacyclics Llc Broton tyrosine kinase inhibitors
ES2660418T3 (es) * 2008-07-16 2018-03-22 Pharmacyclics Llc Inhibidores de la tirosina quinasa de Bruton para el tratamiento de tumores sólidos
US7718662B1 (en) 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
CN102115476A (zh) * 2011-03-23 2011-07-06 常州大学 一种2H-吡唑并[3,4-d]嘧啶衍生物及合成方法
US9376438B2 (en) * 2011-05-17 2016-06-28 Principia Biopharma, Inc. Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors
EA025496B1 (ru) * 2011-05-17 2016-12-30 Принсипиа Биофарма Инк. Ингибиторы тирозинкиназы
US9138436B2 (en) * 2011-07-13 2015-09-22 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
CN104487441B (zh) * 2012-06-18 2018-06-01 普林斯匹亚生物制药公司 有用于治疗癌症和自身免疫性疾病的可逆的共价吡咯并嘧啶或吡唑并嘧啶
CN104507946A (zh) * 2012-07-30 2015-04-08 康塞特医药品有限公司 氘代依鲁替尼
AU2013296509B2 (en) * 2012-07-31 2017-12-21 Orthovita Inc. Depth controlled Jamshidi needle
WO2014022569A1 (en) * 2012-08-03 2014-02-06 Principia Biopharma Inc. Treatment of dry eye
ME03455B (me) 2012-09-10 2020-01-20 Principia Biopharma Inc Jedinjenja pirazolopirimidina kao inhibitori kinaze
US9479134B2 (en) * 2013-03-04 2016-10-25 Texas Instruments Incorporated Position detecting system
WO2014143807A2 (en) 2013-03-15 2014-09-18 Stromatt Scott Anti-cd37 antibody and bcr pathway antagonist combination therapy for treatment of b-cell malignancies and disorders
MX2015014171A (es) 2013-04-08 2015-12-16 Bayer Pharma AG Uso de 2,3-dihidroimidazo[1,2-c]quinazolinas sustituidas.
HK1215374A1 (zh) 2013-04-08 2016-08-26 Pharmacyclics Llc 依鲁替尼联合疗法
US8957080B2 (en) * 2013-04-09 2015-02-17 Principia Biopharma Inc. Tyrosine kinase inhibitors
WO2014187319A1 (en) * 2013-05-21 2014-11-27 Jiangsu Medolution Ltd Substituted pyrazolopyrimidines as kinases inhibitors
CN105017256A (zh) * 2014-04-29 2015-11-04 浙江导明医药科技有限公司 多氟化合物作为布鲁顿酪氨酸激酶抑制剂
CN106146508A (zh) * 2015-03-19 2016-11-23 浙江导明医药科技有限公司 优化的联合用药及其治疗癌症和自身免疫疾病的用途

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020040989A (ja) * 2014-04-29 2020-03-19 チョーチアン ディーティーアールエム バイオファーマ コーポレーション リミテッド ブルトン型チロシンキナーゼ（ｂｔｋ）インヒビターとしての多フルオロ置換化合物
JP7005582B2 (ja) 2014-04-29 2022-01-21 チョーチアン ディーティーアールエム バイオファーマ コーポレーション リミテッド ブルトン型チロシンキナーゼ（ｂｔｋ）インヒビターとしての多フルオロ置換化合物

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