EA201990519A1 - КРИСТАЛЛИЧЕСКАЯ ФОРМА (S)-7-(1-АКРИЛОИЛПИПЕРИДИН-4-ИЛ)-2-(4-ФЕНОКСИФЕНИЛ)-4,5,6,7-ТЕТРАГИДРОПИРАЗОЛО[1,5-a]ПИРИМИДИН-3-КАРБОКСАМИДА, ЕЕ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЯ - Google Patents

КРИСТАЛЛИЧЕСКАЯ ФОРМА (S)-7-(1-АКРИЛОИЛПИПЕРИДИН-4-ИЛ)-2-(4-ФЕНОКСИФЕНИЛ)-4,5,6,7-ТЕТРАГИДРОПИРАЗОЛО[1,5-a]ПИРИМИДИН-3-КАРБОКСАМИДА, ЕЕ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЯ

Info

Publication number
EA201990519A1
EA201990519A1 EA201990519A EA201990519A EA201990519A1 EA 201990519 A1 EA201990519 A1 EA 201990519A1 EA 201990519 A EA201990519 A EA 201990519A EA 201990519 A EA201990519 A EA 201990519A EA 201990519 A1 EA201990519 A1 EA 201990519A1
Authority
EA
Eurasian Patent Office
Prior art keywords
crystalline form
acryloylpiperidin
phenoxyphenyl
pyrimidin
carboxamide
Prior art date
Application number
EA201990519A
Other languages
English (en)
Russian (ru)
Inventor
Чживэй Ван
Юньхан Го
Гунинь Ши
Original Assignee
Бейджин, Лтд.
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.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=61197220&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201990519(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Бейджин, Лтд. filed Critical Бейджин, Лтд.
Publication of EA201990519A1 publication Critical patent/EA201990519A1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
EA201990519A 2016-08-16 2017-08-15 КРИСТАЛЛИЧЕСКАЯ ФОРМА (S)-7-(1-АКРИЛОИЛПИПЕРИДИН-4-ИЛ)-2-(4-ФЕНОКСИФЕНИЛ)-4,5,6,7-ТЕТРАГИДРОПИРАЗОЛО[1,5-a]ПИРИМИДИН-3-КАРБОКСАМИДА, ЕЕ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЯ EA201990519A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2016095510 2016-08-16
PCT/IB2017/054955 WO2018033853A2 (en) 2016-08-16 2017-08-15 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

Publications (1)

Publication Number Publication Date
EA201990519A1 true EA201990519A1 (ru) 2019-08-30

Family

ID=61197220

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201990519A EA201990519A1 (ru) 2016-08-16 2017-08-15 КРИСТАЛЛИЧЕСКАЯ ФОРМА (S)-7-(1-АКРИЛОИЛПИПЕРИДИН-4-ИЛ)-2-(4-ФЕНОКСИФЕНИЛ)-4,5,6,7-ТЕТРАГИДРОПИРАЗОЛО[1,5-a]ПИРИМИДИН-3-КАРБОКСАМИДА, ЕЕ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЯ

Country Status (15)

Country Link
US (12) US10927117B2 (enExample)
EP (3) EP3500575B1 (enExample)
JP (4) JP7402685B2 (enExample)
KR (3) KR102793825B1 (enExample)
CN (3) CN116478166A (enExample)
AU (3) AU2017314178B2 (enExample)
CA (1) CA3033827A1 (enExample)
EA (1) EA201990519A1 (enExample)
IL (2) IL264784B (enExample)
MX (1) MX384627B (enExample)
NZ (1) NZ751418A (enExample)
SG (1) SG11201901141WA (enExample)
TW (3) TWI884890B (enExample)
WO (1) WO2018033853A2 (enExample)
ZA (1) ZA201900919B (enExample)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA028756B1 (ru) 2013-04-25 2017-12-29 Бэйджин, Лтд. Конденсированные гетероциклические соединения в качестве ингибиторов протеинкиназы
PT3702373T (pt) 2013-09-13 2022-09-27 Beigene Switzerland Gmbh Anticorpos anti-pd1 e a sua utilização como agentes terapêuticos e de diagnóstico
JP6526189B2 (ja) 2014-07-03 2019-06-05 ベイジーン リミテッド 抗pd−l1抗体並びにその治療及び診断のための使用
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
SG11201901141WA (en) 2016-08-16 2019-03-28 Beigene Ltd 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
CN118252927A (zh) 2016-08-19 2024-06-28 百济神州有限公司 使用包含btk抑制剂的组合产品治疗癌症
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
JP2020525411A (ja) 2017-06-26 2020-08-27 ベイジーン リミテッド 肝細胞癌のための免疫療法
WO2019034009A1 (en) 2017-08-12 2019-02-21 Beigene, Ltd. BTK INHIBITOR WITH ENHANCED DOUBLE SELECTIVITY
WO2019108795A1 (en) 2017-11-29 2019-06-06 Beigene Switzerland Gmbh Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors
CN112312858A (zh) * 2018-03-29 2021-02-02 马缇医疗股份有限公司 眼科药物持续释放制剂及其用于干眼综合征治疗的用途
CN111675711A (zh) * 2019-03-11 2020-09-18 百济神州(苏州)生物科技有限公司 Btk抑制剂化合物的单晶及其制备方法
CN111909152B (zh) * 2019-05-08 2023-12-15 百济神州(苏州)生物科技有限公司 Btk抑制剂及其中间体的制备方法
WO2020239103A1 (zh) 2019-05-31 2020-12-03 四川海思科制药有限公司 一种btk抑制剂环衍生物及其制备方法和药学上的应用
CN112057427B (zh) * 2019-06-10 2024-09-03 百济神州(苏州)生物科技有限公司 一种含有布鲁顿氏酪氨酸激酶抑制剂的口服固体片剂及其制备方法
US20220249491A1 (en) * 2019-06-10 2022-08-11 Beigene Switzerland Gmbh Oral solid tablet comprising bruton's tyrosine kinase inhibitor and preparation method therefor
JP2022538215A (ja) * 2019-06-10 2022-09-01 ベイジーン スウィッツァーランド ゲーエムベーハー 経口カプセルおよびその調製方法
CN112057432A (zh) * 2019-06-10 2020-12-11 百济神州(苏州)生物科技有限公司 口服胶囊剂及其制备方法
CN110563733A (zh) * 2019-09-12 2019-12-13 安帝康(无锡)生物科技有限公司 作为选择性btk抑制剂的咪唑并吡嗪类化合物
CA3160368A1 (en) * 2019-12-04 2021-06-10 Henan Zhiwei Biomedicine Co., Ltd. Substituted imidazolecarboxamide as bruton's tyrosine kinase inhibitors
CN110922409A (zh) * 2019-12-19 2020-03-27 武汉九州钰民医药科技有限公司 制备btk抑制剂泽布替尼的方法
CN110845504A (zh) * 2019-12-19 2020-02-28 武汉九州钰民医药科技有限公司 合成赞布替尼的新方法
CN110938077B (zh) * 2019-12-25 2021-04-27 武汉九州钰民医药科技有限公司 合成Avapritinib的方法
CN115175678B (zh) * 2020-02-27 2024-12-27 百济神州瑞士有限责任公司 使用btk抑制剂及其组合治疗dlbcl的方法
WO2021259732A1 (en) 2020-06-24 2021-12-30 Sandoz Ag Multi-component compounds comprising zanubrutinib and a benzoic acid derivative
WO2022007824A1 (zh) 2020-07-07 2022-01-13 四川海思科制药有限公司 一种具有降解btk激酶的化合物及其制备方法和药学上的应用
WO2022101939A1 (en) * 2020-11-13 2022-05-19 Msn Laboratories Private Limited, R&D Center Novel process for the preparation of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide or its salts thereof
WO2022105870A1 (en) * 2020-11-20 2022-05-27 Beigene, Ltd. Methods of treating systemic lupus erythematosus using btk inhibitors
WO2022125862A1 (en) 2020-12-11 2022-06-16 Teva Pharmaceuticals International Gmbh Processes for the preparation of zanubrutinib and intermediates thereof
WO2022140246A1 (en) 2020-12-21 2022-06-30 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
WO2023014817A1 (en) 2021-08-03 2023-02-09 Syros Pharmaceuticals, Inc. Compositions and methods for treating lymphomas with a cdk7 inhibitor in combination with a btk inhibitor
IT202100025997A1 (it) * 2021-10-11 2023-04-11 Olon Spa Processo per la preparazione di zanubrutinib
IT202200009872A1 (it) * 2022-05-12 2023-11-12 Olon Spa Processo di preparazione di Zanubrutinib in forma amorfa.
IT202200024192A1 (it) * 2022-11-24 2024-05-24 Olon Spa Processo per la preparazione di Zanubrutinib.
CN118307541A (zh) * 2023-01-09 2024-07-09 天津济坤医药科技有限公司 氘代吡唑并嘧啶衍生物及其制备方法和药物组合物、结合物及应用
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

Family Cites Families (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE792533A (fr) 1971-12-09 1973-06-08 Int Chem & Nuclear Corp Nouvelles pyrazolo (1,5a) pyrimidines et leur procede de preparation
JP2778921B2 (ja) 1994-11-18 1998-07-23 三共株式会社 イミダゾピラゾール誘導体
PT1206474E (pt) 1999-08-27 2004-10-29 Abbott Lab Compostos de sulfonilfenilpirazole uteis como inibidores de cox-2
BR0014073A (pt) 1999-09-17 2002-07-16 Abbott Gmbh & Co Kg Pirazolopirimidinas como agentes terapêuticos
US7041298B2 (en) 2000-09-08 2006-05-09 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
US20020094989A1 (en) * 2000-10-11 2002-07-18 Hale Jeffrey J. Pyrrolidine modulators of CCR5 chemokine receptor activity
DE60117605T2 (de) 2000-12-21 2006-12-07 Bristol-Myers Squibb Co. Thiazolyl-inhibitoren von tyrosinkinasen der tec-familie
JP2004516295A (ja) * 2000-12-21 2004-06-03 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー サブタイプ選択的なn−メチル−d−アスパラギン酸拮抗薬としてのピペリジン誘導体
MXPA03008142A (es) 2001-03-09 2003-12-12 Pfizer Prod Inc Nuevos compuestos antiinflamatorios de bencimidazol.
JPWO2003004497A1 (ja) 2001-07-05 2004-10-28 住友製薬株式会社 新規複素環化合物
US20040132101A1 (en) 2002-09-27 2004-07-08 Xencor Optimized Fc variants and methods for their generation
ZA200500782B (en) 2002-08-26 2007-10-31 Takeda Pharmaceutical Calcium receptor modulating compound and use thereof
AU2003265585B2 (en) 2002-08-26 2008-07-03 Takeda Pharmaceutical Company Limited Calcium receptor modulating compound and use thereof
WO2005014599A1 (en) 2003-06-04 2005-02-17 Cellular Genomics, Inc. Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds
US20060183746A1 (en) 2003-06-04 2006-08-17 Currie Kevin S Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
US7393848B2 (en) 2003-06-30 2008-07-01 Cgi Pharmaceuticals, Inc. Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds
CN1860118A (zh) 2003-07-29 2006-11-08 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
WO2005047290A2 (en) 2003-11-11 2005-05-26 Cellular Genomics Inc. Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors
KR20070119606A (ko) 2004-11-10 2007-12-20 씨지아이 파마슈티칼스, 인크. 특정 이미다조[1,2-a]피라진-8-일아민, 그의 제조 방법및 용도
US8101770B2 (en) 2004-12-16 2012-01-24 Vertex Pharmaceuticals Incorporated Pyridones useful as inhibitors of kinases
TW200716551A (en) 2005-03-10 2007-05-01 Cgi Pharmaceuticals Inc Certain substituted amides, method of making, and method of use thereof
ATE548363T1 (de) 2005-08-29 2012-03-15 Vertex Pharma 3,5-disubstituierte pyrid-2-one, die sich als inhibitoren der tec-familie von nicht-rezeptor- tyrosinkinasen eignen
WO2007027729A1 (en) 2005-08-29 2007-03-08 Vertex Pharmaceuticals Incorporated 3, 5-disubstituted pyrid-2-ones useful as inhibitors of tec family of non-receptor tyrosine kinases
WO2007026720A1 (ja) * 2005-08-31 2007-03-08 Taisho Pharmaceutical Co., Ltd. 縮環ピラゾール誘導体
BRPI0617100A2 (pt) 2005-09-01 2011-07-12 Astellas Pharma Inc composto derivado de piridazinona, composição farmacêutica, método para previnir ou tratar uma doença e uso de um composto derivado de piridazinona
RU2008133161A (ru) 2006-01-13 2010-02-20 Фармасайкликс, Инк. (Us) Ингибиторы тирозин киназ и их применение
CA2651732C (en) 2006-05-18 2014-10-14 Mannkind Corporation Intracellular kinase inhibitors
JO3235B1 (ar) 2006-05-26 2018-03-08 Astex Therapeutics Ltd مركبات بيررولوبيريميدين و استعمالاتها
AR063946A1 (es) 2006-09-11 2009-03-04 Cgi Pharmaceuticals Inc Determinadas pirimidinas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
US20100160292A1 (en) 2006-09-11 2010-06-24 Cgi Pharmaceuticals, Inc Kinase Inhibitors, and Methods of Using and Identifying Kinase Inhibitors
AR063706A1 (es) 2006-09-11 2009-02-11 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
AR063707A1 (es) 2006-09-11 2009-02-11 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmacéuticas que las comprenden.
EP2529621B1 (en) 2006-09-22 2016-10-05 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
AU2007308045A1 (en) 2006-10-06 2008-04-17 Irm Llc Protein kinase inhibitors and methods for using thereof
US8987233B2 (en) 2006-11-03 2015-03-24 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
US8188272B2 (en) 2007-03-21 2012-05-29 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
WO2008144253A1 (en) 2007-05-14 2008-11-27 Irm Llc Protein kinase inhibitors and methods for using thereof
CL2008002793A1 (es) 2007-09-20 2009-09-04 Cgi Pharmaceuticals Inc Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras
TWI475996B (zh) 2007-10-19 2015-03-11 Celgene Avilomics Res Inc 雜芳基化合物及其用途
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
EP2205564B1 (en) 2007-10-23 2014-07-30 F. Hoffmann-La Roche AG Novel kinase inhibitors
CN101952283B (zh) 2007-12-14 2013-04-17 霍夫曼-拉罗奇有限公司 咪唑并[1,2-a]吡啶和咪唑并[1,2-b]哒嗪衍生物
NZ586916A (en) 2008-02-05 2012-06-29 Hoffmann La Roche Novel pyridinones and pyridazinones
JP5529852B2 (ja) 2008-05-06 2014-06-25 ジリード コネティカット,インコーポレイティド 置換アミド、その製造法及びBtkインヒビターとしての使用
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8450335B2 (en) 2008-06-27 2013-05-28 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
PT2300459E (pt) 2008-07-02 2013-07-04 Hoffmann La Roche Novas fenilpirazinonas utilizadas como inibidores de cinase
ES2552681T3 (es) 2008-07-15 2015-12-01 F. Hoffmann-La Roche Ag Nuevas fenil-imidazopiridinas y piridazinas
EP3311818A3 (en) 2008-07-16 2018-07-18 Pharmacyclics, LLC Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
KR101358532B1 (ko) 2008-07-18 2014-02-05 에프. 호프만-라 로슈 아게 신규한 페닐이미다조피라진
CN102164604A (zh) 2008-07-24 2011-08-24 百时美施贵宝公司 用作激酶调节剂的稠合杂环化合物
MX2011002484A (es) 2008-09-05 2011-09-26 Avila Therapeutics Inc Algoritmo para diseñar inhibidores irreversibles.
BRPI0914404A2 (pt) 2008-10-31 2019-03-06 Genentech Inc "compostos, composição farmacêutica e método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak quinase em um paciente"
US20120028981A1 (en) 2008-11-05 2012-02-02 Principia Biopharma Inc. Kinase Knockdown Via Electrophilically Enhanced Inhibitors
EP2365970B1 (en) 2008-11-12 2018-03-21 Gilead Connecticut, Inc. Pyridazinones and their use as btk inhibitors
US8426428B2 (en) 2008-12-05 2013-04-23 Principia Biopharma, Inc. EGFR kinase knockdown via electrophilically enhanced inhibitors
WO2010068788A1 (en) 2008-12-10 2010-06-17 Cgi Pharmaceuticals, Inc. Heterocyclic amides as btk inhibitors
WO2010068806A1 (en) 2008-12-10 2010-06-17 Cgi Pharmaceuticals, Inc. Amide derivatives as btk inhibitors in the treatment of allergic, autoimmune and inflammatory disorders as well as cancer
WO2010068810A2 (en) 2008-12-10 2010-06-17 Cgi Pharmaceuticals, Inc. Certain substituted amides, method of making, and method of use thereof
CN102325753B (zh) 2008-12-19 2014-09-10 百时美施贵宝公司 用作激酶抑制剂的咔唑甲酰胺化合物
EP3255047B1 (en) 2009-01-06 2021-06-30 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and uses in treating disorders
US8299077B2 (en) 2009-03-02 2012-10-30 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
SG175287A1 (en) 2009-04-24 2011-11-28 Hoffmann La Roche Inhibitors of bruton's tyrosine kinase
JP5656976B2 (ja) 2009-04-29 2015-01-21 ローカス ファーマシューティカルズ インコーポレイテッド ピロロトリアジン化合物
EP2440204B1 (en) 2009-06-12 2013-12-18 Bristol-Myers Squibb Company Nicotinamide compounds useful as kinase modulators
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
US8846673B2 (en) 2009-08-11 2014-09-30 Bristol-Myers Squibb Company Azaindazoles as kinase inhibitors and use thereof
EP3461824B1 (en) 2009-09-04 2021-08-25 Biogen MA Inc. Bruton's tyrosine kinase inhibitors
WO2011029043A1 (en) 2009-09-04 2011-03-10 Biogen Idec Ma Inc. Heteroaryl btk inhibitors
US7718662B1 (en) 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
ES2573716T3 (es) 2010-05-07 2016-06-09 Gilead Connecticut, Inc. Compuestos de piridona y aza-piridona y métodos de utilización
TWI500617B (zh) 2010-05-31 2015-09-21 Ono Pharmaceutical Co Purine ketone derivatives
EA031737B1 (ru) 2010-06-03 2019-02-28 Фармасайкликс, Инк. Применение ингибиторов тирозинкиназы брутона (btk) для лечения лейкоза и лимфомы
WO2011159857A1 (en) 2010-06-16 2011-12-22 Bristol-Myers Squibb Company Carboline carboxamide compounds useful as kinase inhibitors
BR112012033253A2 (pt) 2010-06-23 2016-11-22 Hanmi Science Co Ltd novos derivados de pirimidina fundidos para inibição da atividade de tirosina quinase
US20120053189A1 (en) 2010-06-28 2012-03-01 Pharmacyclics, Inc. Btk inhibitors for the treatment of immune mediated conditions
JP6068340B2 (ja) 2010-08-10 2017-01-25 セルジーン アヴィロミクス リサーチ, インコーポレイテッド Btk阻害剤のベシル酸塩
AR082590A1 (es) 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
ES2561277T3 (es) 2010-09-01 2016-02-25 Gilead Connecticut, Inc. Piridinonas/pirazinonas, procedimiento de preparación y procedimiento de utilización de las mismas
ES2537190T3 (es) 2010-09-01 2015-06-03 Gilead Connecticut, Inc. Piridazinonas, procedimiento de preparación y procedimientos de utilización de las mismas
WO2012135801A1 (en) 2011-04-01 2012-10-04 University Of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
CA2760174A1 (en) 2011-12-01 2013-06-01 Pharmascience Inc. Protein kinase inhibitors and uses thereof
EA201391558A1 (ru) 2011-04-20 2014-05-30 Глэксо Груп Лимитед Тетрагидропиразоло[1,5-а]пиримидины как противотуберкулезные соединения
WO2012158810A1 (en) 2011-05-17 2012-11-22 Principia Biopharma Inc. Tyrosine kinase inhibitors
SI2710005T1 (sl) 2011-05-17 2017-03-31 Principia Biopharma Inc. Zaviralci tirozinske kinaze
KR101585753B1 (ko) 2011-05-17 2016-01-14 에프. 호프만-라 로슈 아게 브루톤 티로신 키나아제의 억제제
US9376438B2 (en) 2011-05-17 2016-06-28 Principia Biopharma, Inc. Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors
LT2718270T (lt) 2011-06-10 2022-08-10 Merck Patent Gmbh Pirimidino ir piridino junginių, turinčių btk inhibitorinį aktyvumą, kompozicijos ir gamybos būdai
BR112014000314A2 (pt) 2011-07-08 2017-01-10 Novartis Ag derivados de pirrolo pirimidina
EA028756B1 (ru) 2013-04-25 2017-12-29 Бэйджин, Лтд. Конденсированные гетероциклические соединения в качестве ингибиторов протеинкиназы
PT3702373T (pt) 2013-09-13 2022-09-27 Beigene Switzerland Gmbh Anticorpos anti-pd1 e a sua utilização como agentes terapêuticos e de diagnóstico
EP3060251A4 (en) 2013-10-25 2017-12-06 Pharmacyclics LLC Treatment using bruton's tyrosine kinase inhibitors and immunotherapy
JP6526189B2 (ja) 2014-07-03 2019-06-05 ベイジーン リミテッド 抗pd−l1抗体並びにその治療及び診断のための使用
CN106687446B (zh) * 2014-07-18 2020-04-28 百济神州(北京)生物科技有限公司 作为t790m/wt-egfr的选择性和不可逆的激酶抑制剂的5-氨基-4-氨甲酰基-吡唑化合物及其用途
SMT202200285T1 (it) 2014-08-11 2022-09-14 Acerta Pharma Bv Combinazioni terapeutiche di un inibitore di btk, un inibitore di pd-1 e/o un inibitore di pd-l1
WO2016025720A1 (en) 2014-08-14 2016-02-18 Assia Chemical Industries Ltd. Solid state forms of ibrutinib
WO2016087994A1 (en) 2014-12-05 2016-06-09 Acerta Pharma B.V. Btk inhibitors to treat solid tumors through modulation of the tumor microenvironment
PT3233103T (pt) 2014-12-18 2021-01-18 Principia Biopharma Inc Tratamento de pênfigo
WO2016105582A1 (en) * 2014-12-24 2016-06-30 Nunn Philip A Compositions for ileo-jejunal drug delivery
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
WO2017046746A1 (en) 2015-09-15 2017-03-23 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor and a gitr binding molecule, a 4-1bb agonist, or an ox40 agonist
WO2017059224A2 (en) 2015-10-01 2017-04-06 Gilead Sciences, Inc. Combination of a btk inhibitor and a checkpoint inhibitor for treating cancers
KR20180109992A (ko) 2016-02-19 2018-10-08 지앙수 헨그루이 메디슨 컴퍼니 리미티드 Jak 키나아제 억제제 또는 약학적으로 허용가능한 그의 염을 함유하는 약학적 조성물
SG11201901141WA (en) 2016-08-16 2019-03-28 Beigene Ltd 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
CN118252927A (zh) 2016-08-19 2024-06-28 百济神州有限公司 使用包含btk抑制剂的组合产品治疗癌症
WO2018095403A1 (zh) 2016-11-25 2018-05-31 江苏恒瑞医药股份有限公司 一种吡啶酮类衍生物药物组合物及其制备方法
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
CN110869765A (zh) 2017-04-20 2020-03-06 Adc治疗有限公司 组合疗法
JP2020525411A (ja) 2017-06-26 2020-08-27 ベイジーン リミテッド 肝細胞癌のための免疫療法
WO2019034009A1 (en) 2017-08-12 2019-02-21 Beigene, Ltd. BTK INHIBITOR WITH ENHANCED DOUBLE SELECTIVITY
WO2019108795A1 (en) 2017-11-29 2019-06-06 Beigene Switzerland Gmbh Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors
WO2019183226A1 (en) 2018-03-21 2019-09-26 Mei Pharma, Inc. Combination therapy
JP2022538215A (ja) 2019-06-10 2022-09-01 ベイジーン スウィッツァーランド ゲーエムベーハー 経口カプセルおよびその調製方法
US20220249491A1 (en) 2019-06-10 2022-08-11 Beigene Switzerland Gmbh Oral solid tablet comprising bruton's tyrosine kinase inhibitor and preparation method therefor
US20220281876A1 (en) 2019-07-26 2022-09-08 Beigene, Ltd. Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use
US20220387404A1 (en) 2019-09-11 2022-12-08 Beigene, Ltd. Treatment of cancer using a combination comprising multi-tyrosine kinase inhibitor and immune checkpoint inhibitor
WO2021098777A1 (en) 2019-11-21 2021-05-27 Beigene, Ltd. Methods of cancer treatment using anti-ox40 antibodies in combination with pi3 kinase delta inhibitors
CN115175678B (zh) 2020-02-27 2024-12-27 百济神州瑞士有限责任公司 使用btk抑制剂及其组合治疗dlbcl的方法

Also Published As

Publication number Publication date
US20220340583A1 (en) 2022-10-27
US20240059699A1 (en) 2024-02-22
US10927117B2 (en) 2021-02-23
TWI865873B (zh) 2024-12-11
AU2022200278B2 (en) 2023-10-12
US12103931B2 (en) 2024-10-01
WO2018033853A3 (en) 2018-11-01
TWI884890B (zh) 2025-05-21
EP4353322A3 (en) 2024-07-31
EP3500575A2 (en) 2019-06-26
JP7402685B2 (ja) 2023-12-21
NZ751418A (en) 2023-04-28
US20220281881A1 (en) 2022-09-08
KR20250052473A (ko) 2025-04-18
WO2018033853A2 (en) 2018-02-22
CN109563099B (zh) 2023-02-03
KR102793825B1 (ko) 2025-04-11
JP2024026550A (ja) 2024-02-28
IL264784B (en) 2022-07-01
EP3500575B1 (en) 2025-11-05
JP7637459B2 (ja) 2025-02-28
TW201811794A (zh) 2018-04-01
BR112019003205A2 (pt) 2019-06-18
AU2022200278A1 (en) 2022-02-10
AU2017314178B2 (en) 2021-11-18
BR112019003205A8 (pt) 2023-01-17
US11884674B2 (en) 2024-01-30
US20210130363A1 (en) 2021-05-06
KR20190032613A (ko) 2019-03-27
SG11201901141WA (en) 2019-03-28
CA3033827A1 (en) 2018-02-22
JP2019528276A (ja) 2019-10-10
IL293319A (en) 2022-07-01
ZA201900919B (en) 2020-10-28
IL264784A (enExample) 2019-03-31
KR102604975B1 (ko) 2023-11-24
KR20230162137A (ko) 2023-11-28
JP2022071072A (ja) 2022-05-13
EP3500575A4 (en) 2020-04-08
US11591340B2 (en) 2023-02-28
MX2019001900A (es) 2019-07-01
AU2024200030A1 (en) 2024-01-25
US20190169201A1 (en) 2019-06-06
US11814389B2 (en) 2023-11-14
CN116478165A (zh) 2023-07-25
EP4509183A3 (en) 2025-05-21
US11851437B2 (en) 2023-12-26
AU2017314178A1 (en) 2019-04-04
US20240116940A1 (en) 2024-04-11
MX384627B (es) 2025-03-14
CN116478166A (zh) 2023-07-25
TWI760356B (zh) 2022-04-11
US11999743B2 (en) 2024-06-04
TW202233628A (zh) 2022-09-01
JP7413419B2 (ja) 2024-01-15
US20220274994A1 (en) 2022-09-01
US20220340584A1 (en) 2022-10-27
US20230242542A1 (en) 2023-08-03
TW202511264A (zh) 2025-03-16
EP4353322A2 (en) 2024-04-17
CN109563099A (zh) 2019-04-02
US20230057716A1 (en) 2023-02-23
US20240409546A1 (en) 2024-12-12
US20240092786A1 (en) 2024-03-21
EP4509183A2 (en) 2025-02-19
US11970500B1 (en) 2024-04-30
JP2025081429A (ja) 2025-05-27
NZ791292A (en) 2025-05-02

Similar Documents

Publication Publication Date Title
EA201990519A1 (ru) КРИСТАЛЛИЧЕСКАЯ ФОРМА (S)-7-(1-АКРИЛОИЛПИПЕРИДИН-4-ИЛ)-2-(4-ФЕНОКСИФЕНИЛ)-4,5,6,7-ТЕТРАГИДРОПИРАЗОЛО[1,5-a]ПИРИМИДИН-3-КАРБОКСАМИДА, ЕЕ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЯ
EA201690093A1 (ru) Производные пирроло[3,2-d]пиримидина для лечения вирусных инфекций и других заболеваний
EA201590663A1 (ru) ПРОИЗВОДНЫЕ ПИРРОЛО[3,2-d]ПИРИМИДИНА ДЛЯ ЛЕЧЕНИЯ ВИРУСНЫХ ИНФЕКЦИЙ И ДРУГИХ ЗАБОЛЕВАНИЙ
MX388457B (es) Inhibidores de imidazopirazina de la tirosina cinasa de bruton.
BR112017010141A2 (pt) Forma cristalina de hidrogenossulfato de (s)-n-(5- ((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5- a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
MX2019003605A (es) Formas solidas de un inhibidor de cdk4/6 selectivo.
MX380147B (es) Formas de dosificacion de ruxolitinib de liberacion sostenida.
SG10201804306VA (en) THIENO[3,2-d]PYRIMIDINES DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS
EA201692095A1 (ru) Имидазо[4,5-c]хинолин-2-оновые соединения и их применение в лечении рака
CY1119615T1 (el) Διπλα εκλεκτικοι αναστολεις ρι3 δελτα και γαμμα κινασης
EA201591541A1 (ru) Ингибиторы бета-секретазы 1 (bace 1)
EA201391440A1 (ru) Производные пиразолопиримидина
WO2016010869A3 (en) FUSED QUINOLINE COMPUNDS AS PI3K, mTOR INHIBITORS
EA201692111A1 (ru) Фармацевтические композиции, содержащие данириксин, для лечения инфекционных заболеваний
CY1120602T1 (el) [1,2,4]τριαζολο[4,3-β]πυριδαζινες για χρηση στη θεραπευτικη αντιμετωπιση πολλαπλασιαστικων ασθενειων
EA201890412A1 (ru) АНТИБАКТЕРИАЛЬНЫЕ АГЕНТЫ, СОДЕРЖАЩИЕ ПИРАЗИНО[2,3-b][1,4]ОКСАЗИН-3-ОН ИЛИ РОДСТВЕННУЮ КОЛЬЦЕВУЮ СИСТЕМУ
WO2017168454A3 (en) Novel compounds as btk inhibitors
EA201790140A1 (ru) Фармацевтические лекарственные формы
EA201990834A1 (ru) Пиримидиновые пролекарства для лечения вирусных инфекций и других заболеваний
EA201790795A1 (ru) СОЕДИНЕНИЯ 4Н-ПИРИДО[1,2-a]ПИРИМИДИН-4-ОНА