IL293319B1 - Crystal structure of s)–7–(1–acryloylpiperidin–4–yl)–2–(4–)phenoxyphenyl)–4,5,6,7–tetra–hydropyrazolo(1,5–a)pyrimidine–3–carboxamide, methods of preparation and uses thereof - Google Patents

Crystal structure of s)–7–(1–acryloylpiperidin–4–yl)–2–(4–)phenoxyphenyl)–4,5,6,7–tetra–hydropyrazolo(1,5–a)pyrimidine–3–carboxamide, methods of preparation and uses thereof

Info

Publication number
IL293319B1
IL293319B1 IL293319A IL29331922A IL293319B1 IL 293319 B1 IL293319 B1 IL 293319B1 IL 293319 A IL293319 A IL 293319A IL 29331922 A IL29331922 A IL 29331922A IL 293319 B1 IL293319 B1 IL 293319B1
Authority
IL
Israel
Prior art keywords
compound
amorphous form
lymphoma
proliferative disease
cell proliferative
Prior art date
Application number
IL293319A
Other languages
English (en)
Hebrew (he)
Other versions
IL293319A (en
Original Assignee
Beone Medicines Ltd
Beone Medicines Gmbh
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=IL293319(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Beone Medicines Ltd, Beone Medicines Gmbh filed Critical Beone Medicines Ltd
Publication of IL293319A publication Critical patent/IL293319A/en
Publication of IL293319B1 publication Critical patent/IL293319B1/en

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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (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)
IL293319A 2016-08-16 2017-08-15 Crystal structure of s)–7–(1–acryloylpiperidin–4–yl)–2–(4–)phenoxyphenyl)–4,5,6,7–tetra–hydropyrazolo(1,5–a)pyrimidine–3–carboxamide, methods of preparation and uses thereof IL293319B1 (en)

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 (2)

Publication Number Publication Date
IL293319A IL293319A (en) 2022-07-01
IL293319B1 true IL293319B1 (en) 2026-01-01

Family

ID=61197220

Family Applications (3)

Application Number Title Priority Date Filing Date
IL293319A IL293319B1 (en) 2016-08-16 2017-08-15 Crystal structure of s)–7–(1–acryloylpiperidin–4–yl)–2–(4–)phenoxyphenyl)–4,5,6,7–tetra–hydropyrazolo(1,5–a)pyrimidine–3–carboxamide, methods of preparation and uses thereof
IL264784A IL264784B (en) 2016-08-16 2017-08-15 Crystal structure of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo(1,5-a)pyrimidine-3-carboxamide Preparation methods and its uses
IL325562A IL325562A (en) 2016-08-16 2025-12-23 Crystal structure of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, methods of preparation and uses thereof

Family Applications After (2)

Application Number Title Priority Date Filing Date
IL264784A IL264784B (en) 2016-08-16 2017-08-15 Crystal structure of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo(1,5-a)pyrimidine-3-carboxamide Preparation methods and its uses
IL325562A IL325562A (en) 2016-08-16 2025-12-23 Crystal structure of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, methods of preparation and uses thereof

Country Status (17)

Country Link
US (12) US10927117B2 (enExample)
EP (3) EP4353322A3 (enExample)
JP (6) JP7402685B2 (enExample)
KR (3) KR102793825B1 (enExample)
CN (3) CN116478166A (enExample)
AU (4) AU2017314178B2 (enExample)
CA (3) CA3258471A1 (enExample)
EA (1) EA201990519A1 (enExample)
ES (1) ES3060138T3 (enExample)
IL (3) IL293319B1 (enExample)
MX (1) MX384627B (enExample)
NZ (1) NZ751418A (enExample)
PL (1) PL3500575T3 (enExample)
SG (1) SG11201901141WA (enExample)
TW (3) TWI884890B (enExample)
WO (1) WO2018033853A2 (enExample)
ZA (1) ZA201900919B (enExample)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2902686C (en) 2013-04-25 2017-01-24 Beigene, Ltd. Fused heterocyclic compounds as protein kinase inhibitors
CN112552401B (zh) 2013-09-13 2023-08-25 广州百济神州生物制药有限公司 抗pd1抗体及其作为治疗剂与诊断剂的用途
CN106604742B (zh) 2014-07-03 2019-01-11 百济神州有限公司 抗pd-l1抗体及其作为治疗剂及诊断剂的用途
US10864203B2 (en) 2016-07-05 2020-12-15 Beigene, Ltd. Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer
WO2018033853A2 (en) 2016-08-16 2018-02-22 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
WO2018033135A1 (en) 2016-08-19 2018-02-22 Beigene, Ltd. Use of a combination comprising a btk inhibitor for treating cancers
US11555038B2 (en) 2017-01-25 2023-01-17 Beigene, Ltd. Crystalline forms of (S)-7-(1-(but-2-ynoyl)piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
EP3645569A4 (en) 2017-06-26 2021-03-24 BeiGene, Ltd. IMMUNOTHERAPY FOR LIVER CELL CARCINOMA
US11377449B2 (en) 2017-08-12 2022-07-05 Beigene, Ltd. BTK inhibitors with improved dual 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
JP2021530253A (ja) * 2018-03-29 2021-11-11 マティ セラピューティクス,インク. 眼科用徐放性製剤およびドライアイ症候群治療のための使用
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
CN117820311A (zh) * 2019-05-08 2024-04-05 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
CN113544130B (zh) 2019-05-31 2024-01-09 西藏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
CN113950327A (zh) * 2019-06-10 2022-01-18 百济神州瑞士有限责任公司 口服胶囊剂及其制备方法
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
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
KR102801205B1 (ko) * 2019-12-04 2025-04-29 허난 즈웨이 바이오메디슨 씨오., 엘티디. 브루톤 티로신 키나제 억제제인 이미다졸 카복사마이드 유도체
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
US20230089557A1 (en) * 2020-02-27 2023-03-23 Beigene Switzerland Gmbh Methods of treating dlbcl using btk inhibitors and combinations thereof
WO2021259732A1 (en) 2020-06-24 2021-12-30 Sandoz Ag Multi-component compounds comprising zanubrutinib and a benzoic acid derivative
TW202216715A (zh) 2020-07-07 2022-05-01 大陸商四川海思科製藥有限公司 降解btk激酶的化合物、製造方法及其應用
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
KR20230107866A (ko) * 2020-11-20 2023-07-18 베이진 스위찰랜드 게엠베하 Btk 억제제를 사용한 전신성 홍반성 루푸스의 치료 방법
EP4259633A1 (en) 2020-12-11 2023-10-18 Teva Pharmaceuticals International GmbH Processes for the preparation of zanubrutinib and intermediates thereof
US20240100172A1 (en) 2020-12-21 2024-03-28 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
CN117886822A (zh) * 2023-12-24 2024-04-16 神隆医药(常熟)有限公司 一种高收率且适于工业化推广的泽布替尼中间体的制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014173289A1 (en) * 2013-04-25 2014-10-30 Beigene, Ltd. Fused heterocyclic compounds as protein kinase inhibitors
WO2016100914A1 (en) * 2014-12-18 2016-06-23 Gourlay Steven Treatment of pemphigus
WO2016105582A1 (en) * 2014-12-24 2016-06-30 Nunn Philip A Compositions for ileo-jejunal drug delivery

Family Cites Families (115)

* 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
JP2003508401A (ja) 1999-08-27 2003-03-04 アボット・ラボラトリーズ Cox−2阻害薬として有用なスルホニルフェニルピラゾール化合物
JP2003509428A (ja) * 1999-09-17 2003-03-11 アボツト・ゲー・エム・ベー・ハー・ウント・コンパニー・カーゲー 治療薬としてのピラゾロピリミジン
WO2002020740A2 (en) 2000-09-08 2002-03-14 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
MXPA03004652A (es) * 2000-12-21 2003-09-05 Warner Lambert Co Derivados de piperidina como antagonistas selectivos de subtipo de n-metil-d-aspartato.
WO2002050071A1 (en) 2000-12-21 2002-06-27 Bristol-Myers Squibb Company Thiazolyl inhibitors of tec family tyrosine kinases
AP2002002460A0 (en) 2001-03-09 2002-06-30 Pfizer Prod Inc Novel benzimidazole anti-inflammatory compounds.
WO2003004497A1 (en) 2001-07-05 2003-01-16 Sumitomo Pharmaceuticals Company, Limited Novel heterocyclic compound
US20040132101A1 (en) 2002-09-27 2004-07-08 Xencor Optimized Fc variants and methods for their generation
EP1572113B1 (en) 2002-08-26 2017-05-17 Takeda Pharmaceutical Company Limited Calcium receptor modulating compound and use thereof
CN1771231B (zh) 2002-08-26 2011-05-25 武田药品工业株式会社 钙受体调节性化合物及其用途
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
US7405295B2 (en) 2003-06-04 2008-07-29 Cgi Pharmaceuticals, Inc. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
WO2005005429A1 (en) 2003-06-30 2005-01-20 Cellular Genomics, Inc. Certain heterocyclic substituted imidazo[1,2-a]pyrazin-8-ylamines and methods of inhibition of bruton’s tyrosine kinase by such compounds
WO2005011597A2 (en) 2003-07-29 2005-02-10 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2005047290A2 (en) 2003-11-11 2005-05-26 Cellular Genomics Inc. Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors
AU2005304473A1 (en) 2004-11-10 2006-05-18 Cgi Pharmaceuticals, Inc. Imidazo[1 , 2-a] pyrazin-8-ylamines useful as modulators of kinase activity
US8101770B2 (en) 2004-12-16 2012-01-24 Vertex Pharmaceuticals Incorporated Pyridones useful as inhibitors of kinases
MX2007011041A (es) 2005-03-10 2008-02-22 Cgi Pharmaceuticals Inc Ciertas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas.
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
EP1919906B1 (en) 2005-08-29 2011-10-12 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
WO2007026950A1 (en) 2005-09-01 2007-03-08 Astellas Pharma Inc. Pyridazinone derivatives used for the treatment of pain
KR20080098490A (ko) 2006-01-13 2008-11-10 파마시클릭스, 인코포레이티드 티로신 키나제 억제제 및 이의 용도
WO2007136790A2 (en) 2006-05-18 2007-11-29 Mannkind Corporation Intracellular kinase inhibitors
TWI398252B (zh) 2006-05-26 2013-06-11 諾華公司 吡咯并嘧啶化合物及其用途
WO2008033858A2 (en) 2006-09-11 2008-03-20 Cgi Pharmaceuticals, Inc. Kinase inhibitors, and methods of using and identifying kinase inhibitors
PE20081370A1 (es) 2006-09-11 2008-11-28 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas
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.
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.
DK2526933T3 (en) 2006-09-22 2015-05-18 Pharmacyclics Inc Inhibitors of Bruton's tyrosine kinase
JP2010505859A (ja) 2006-10-06 2010-02-25 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤およびそれを使用するための方法
CA2668286C (en) 2006-11-03 2014-09-16 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
CN101730699A (zh) 2007-03-21 2010-06-09 百时美施贵宝公司 可用于治疗增殖性、变应性、自身免疫性和炎症性疾病的稠合杂环化合物
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
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
TWI552752B (zh) 2007-10-19 2016-10-11 賽基艾維洛米斯研究股份有限公司 雜芳基化合物及其用途
CN101835755B (zh) 2007-10-23 2013-12-11 霍夫曼-拉罗奇有限公司 激酶抑制剂
JP5643105B2 (ja) 2007-12-14 2014-12-17 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 新規イミダゾ[1,2−a]ピリジン及びイミダゾ[1,2−b]ピリダジン誘導体
PL2242749T3 (pl) 2008-02-05 2013-09-30 Hoffmann La Roche Nowe pirydynony i pirydazynony
CA2723237A1 (en) 2008-05-06 2009-11-12 Peter A. Blomgren Substituted amides, method of making, and use as btk inhibitors
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
PE20110164A1 (es) 2008-07-02 2011-03-28 Hoffmann La Roche Nuevas fenilpirazinonas como inhibidores de quinasa
WO2010006947A1 (en) 2008-07-15 2010-01-21 F. Hoffmann-La Roche Ag Novel phenyl-imidazopyridines and pyridazines
CA2730930C (en) 2008-07-16 2015-01-13 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
ES2461494T3 (es) 2008-07-18 2014-05-20 F. Hoffmann-La Roche Ag Nuevas fenilimidazopirazinas
US8476430B2 (en) 2008-07-24 2013-07-02 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
JP2012501654A (ja) 2008-09-05 2012-01-26 アビラ セラピューティクス, インコーポレイテッド 不可逆的インヒビターの設計のためのアルゴリズム
EP2348860B1 (en) 2008-10-31 2015-05-27 Genentech, Inc. Pyrazolopyrimidine jak inhibitor compounds and methods
US20120028981A1 (en) 2008-11-05 2012-02-02 Principia Biopharma Inc. Kinase Knockdown Via Electrophilically Enhanced Inhibitors
US8598174B2 (en) 2008-11-12 2013-12-03 Genetech, Inc. Pyridazinones, method of making, and method of use thereof
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
US8084620B2 (en) 2008-12-19 2011-12-27 Bristol-Myers Squibb Company Carbazole carboxamide compounds useful as kinase inhibitors
EP3828185B1 (en) 2009-01-06 2024-11-20 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
US8299077B2 (en) 2009-03-02 2012-10-30 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
WO2010122038A1 (en) 2009-04-24 2010-10-28 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
US8765754B2 (en) 2009-04-29 2014-07-01 Locus Pharmaceuticals, Inc. Pyrrolotriazine compounds
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
NZ598985A (en) 2009-09-04 2013-07-26 Biogen Idec Inc Bruton's tyrosine kinase inhibitors
EP2485589A4 (en) 2009-09-04 2013-02-06 Biogen Idec Inc HETEROARYL-BTK INHIBITORS
US7718662B1 (en) 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
EP2566869B1 (en) 2010-05-07 2016-03-02 Gilead Connecticut, Inc. Pyridone and aza-pyridone compounds and methods of use
TWI500617B (zh) 2010-05-31 2015-09-21 Ono Pharmaceutical Co Purine ketone derivatives
CA3007787C (en) 2010-06-03 2020-03-10 Pharmacyclics Llc The use of inhibitors of bruton's tyrosine kinase (btk)
WO2011159857A1 (en) 2010-06-16 2011-12-22 Bristol-Myers Squibb Company Carboline carboxamide compounds useful as kinase inhibitors
MX342164B (es) 2010-06-23 2016-09-19 Hanmi Science Co Ltd Derivados de pirimidina fusionados novedosos para la inhibicion de la actividad de tirosina cinasa.
US20120053189A1 (en) 2010-06-28 2012-03-01 Pharmacyclics, Inc. Btk inhibitors for the treatment of immune mediated conditions
MX336875B (es) 2010-08-10 2016-02-04 Celgene Avilomics Res Inc Sal de besilato de un inhibidor de tirosina cinasa de bruton (btk).
AR082590A1 (es) 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
US8975260B2 (en) 2010-09-01 2015-03-10 Genetech, Inc Pyridazinones, method of making, and method of use thereof
CA2809836C (en) 2010-09-01 2019-01-15 Gilead Connecticut, Inc. Pyridinones/pyrazinones, method of making, and method of use thereof for the treatment of disorders mediated by bruton's tyrosine kinase
JP6147727B2 (ja) 2011-04-01 2017-06-14 ユニヴァーシティー オブ ユタ リサーチ ファウンデーション チロシン受容体キナーゼbtk阻害剤としての置換n−(3−(ピリミジン−4−イル)フェニル)アクリルアミド類似体
CA2760174A1 (en) 2011-12-01 2013-06-01 Pharmascience Inc. Protein kinase inhibitors and uses thereof
CN103596958A (zh) 2011-04-20 2014-02-19 葛兰素集团有限公司 用作抗结核病化合物的四氢吡唑并[1,5-a]嘧啶
US20140107151A1 (en) 2011-05-17 2014-04-17 Principia Biophama Inc. Tyrosine kinase inhibitors
WO2012158795A1 (en) 2011-05-17 2012-11-22 Principia Biopharma Inc. Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors
AU2012257802A1 (en) 2011-05-17 2013-10-31 F. Hoffmann-La Roche Ag Inhibitors of Bruton's tyrosine kinase
PL2710005T3 (pl) 2011-05-17 2017-07-31 Principia Biopharma Inc. Inhibitory kinazy tyrozynowej
MX354412B (es) 2011-06-10 2018-03-05 Merck Patent Gmbh Composiciones y metodos para la produccion de compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton.
ES2548414T3 (es) 2011-07-08 2015-10-16 Novartis Ag Novedosos derivados de pirrolo pirimidina
CN112552401B (zh) 2013-09-13 2023-08-25 广州百济神州生物制药有限公司 抗pd1抗体及其作为治疗剂与诊断剂的用途
EA201690746A1 (ru) 2013-10-25 2016-12-30 Фармасайкликс Элэлси Лечение с применением ингибиторов тирозинкиназы брутона и иммунотерапии
CN106604742B (zh) 2014-07-03 2019-01-11 百济神州有限公司 抗pd-l1抗体及其作为治疗剂及诊断剂的用途
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
TW201618775A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 Btk抑制劑、pi3k抑制劑、jak-2抑制劑、pd-1抑制劑及/或pd-l1抑制劑之治療組合物
US10035802B2 (en) 2014-08-14 2018-07-31 Teva Pharmaceuticals Usa, Inc. 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
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
US20190054090A1 (en) 2015-10-01 2019-02-21 Gilead Sciences, Inc. Combination of a btk inhibitor and a checkpoint inhibitor for treating cancers
CA3014090A1 (en) 2016-02-19 2017-08-24 Jiangsu Hengrui Medicine Co., Ltd. Pharmaceutical composition containing jak kinase inhibitor or pharmaceutically acceptable salt thereof
WO2018033853A2 (en) 2016-08-16 2018-02-22 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
WO2018033135A1 (en) 2016-08-19 2018-02-22 Beigene, Ltd. Use of a combination comprising a btk inhibitor for treating cancers
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
US11555038B2 (en) 2017-01-25 2023-01-17 Beigene, Ltd. Crystalline forms of (S)-7-(1-(but-2-ynoyl)piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
EP3612839A1 (en) 2017-04-20 2020-02-26 ADC Therapeutics SA Combination therapy
EP3645569A4 (en) 2017-06-26 2021-03-24 BeiGene, Ltd. IMMUNOTHERAPY FOR LIVER CELL CARCINOMA
US11377449B2 (en) 2017-08-12 2022-07-05 Beigene, Ltd. BTK inhibitors with improved dual 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
CN112165939A (zh) 2018-03-21 2021-01-01 梅制药公司 联合疗法
US20220249491A1 (en) 2019-06-10 2022-08-11 Beigene Switzerland Gmbh Oral solid tablet comprising bruton's tyrosine kinase inhibitor and preparation method therefor
CN113950327A (zh) 2019-06-10 2022-01-18 百济神州瑞士有限责任公司 口服胶囊剂及其制备方法
CN114174299B (zh) 2019-07-26 2024-10-25 百济神州有限公司 通过btk抑制剂与e3连接酶配体缀合对布鲁顿氏酪氨酸激酶(btk)的降解以及使用方法
WO2021047623A1 (en) 2019-09-11 2021-03-18 Beigene, Ltd. Treatment of cancer using a combination comprising multi-tyrosine kinase inhibitor and immune checkpoint inhibitor
US20230011916A1 (en) 2019-11-21 2023-01-12 Beigene, Ltd. Methods of cancer treatment using anti-ox40 antibodies in combination with pi3 kinase delta inhibitors
US20230089557A1 (en) 2020-02-27 2023-03-23 Beigene Switzerland Gmbh Methods of treating dlbcl using btk inhibitors and combinations thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014173289A1 (en) * 2013-04-25 2014-10-30 Beigene, Ltd. Fused heterocyclic compounds as protein kinase inhibitors
WO2016100914A1 (en) * 2014-12-18 2016-06-23 Gourlay Steven Treatment of pemphigus
WO2016105582A1 (en) * 2014-12-24 2016-06-30 Nunn Philip A Compositions for ileo-jejunal drug delivery

Also Published As

Publication number Publication date
WO2018033853A2 (en) 2018-02-22
CA3033827A1 (en) 2018-02-22
JP7413419B2 (ja) 2024-01-15
MX384627B (es) 2025-03-14
NZ791292A (en) 2025-05-02
CA3258471A1 (en) 2026-03-02
CN109563099A (zh) 2019-04-02
JP7402685B2 (ja) 2023-12-21
US20240116940A1 (en) 2024-04-11
CN116478166A (zh) 2023-07-25
AU2024200030B2 (en) 2026-02-19
AU2024200030A1 (en) 2024-01-25
US20220340583A1 (en) 2022-10-27
US20240059699A1 (en) 2024-02-22
IL293319A (en) 2022-07-01
AU2022200278A1 (en) 2022-02-10
IL264784B (en) 2022-07-01
BR112019003205A2 (pt) 2019-06-18
AU2022200278B2 (en) 2023-10-12
ES3060138T3 (en) 2026-03-25
TWI760356B (zh) 2022-04-11
EP3500575A2 (en) 2019-06-26
US12103931B2 (en) 2024-10-01
US20220281881A1 (en) 2022-09-08
CA3258473A1 (en) 2026-03-02
KR20250052473A (ko) 2025-04-18
US11814389B2 (en) 2023-11-14
KR20230162137A (ko) 2023-11-28
JP2026068011A (ja) 2026-04-21
JP2022071072A (ja) 2022-05-13
EP3500575C0 (en) 2025-11-05
SG11201901141WA (en) 2019-03-28
KR20190032613A (ko) 2019-03-27
US20190169201A1 (en) 2019-06-06
EP4353322A3 (en) 2024-07-31
US11970500B1 (en) 2024-04-30
WO2018033853A3 (en) 2018-11-01
MX2019001900A (es) 2019-07-01
US10927117B2 (en) 2021-02-23
JP2026048913A (ja) 2026-03-17
US20230057716A1 (en) 2023-02-23
EP3500575B1 (en) 2025-11-05
EP3500575B8 (en) 2026-02-25
IL325562A (en) 2026-02-01
JP2019528276A (ja) 2019-10-10
NZ751418A (en) 2023-04-28
US11851437B2 (en) 2023-12-26
EP4509183A2 (en) 2025-02-19
AU2026202253A1 (en) 2026-04-09
JP7637459B2 (ja) 2025-02-28
TW202233628A (zh) 2022-09-01
PL3500575T3 (pl) 2026-04-27
US20220274994A1 (en) 2022-09-01
EP3500575A4 (en) 2020-04-08
TW201811794A (zh) 2018-04-01
US20240409546A1 (en) 2024-12-12
TW202511264A (zh) 2025-03-16
US11884674B2 (en) 2024-01-30
CN109563099B (zh) 2023-02-03
US20230242542A1 (en) 2023-08-03
TWI884890B (zh) 2025-05-21
US11591340B2 (en) 2023-02-28
US20220340584A1 (en) 2022-10-27
AU2017314178B2 (en) 2021-11-18
EP4353322A2 (en) 2024-04-17
KR102793825B1 (ko) 2025-04-11
EA201990519A1 (ru) 2019-08-30
EP4509183A3 (en) 2025-05-21
BR112019003205A8 (pt) 2023-01-17
US11999743B2 (en) 2024-06-04
AU2017314178A1 (en) 2019-04-04
KR102604975B1 (ko) 2023-11-24
US20240092786A1 (en) 2024-03-21
JP2025081429A (ja) 2025-05-27
ZA201900919B (en) 2020-10-28
TWI865873B (zh) 2024-12-11
IL264784A (enExample) 2019-03-31
CN116478165A (zh) 2023-07-25
JP2024026550A (ja) 2024-02-28
US20210130363A1 (en) 2021-05-06

Similar Documents

Publication Publication Date Title
US12103931B2 (en) 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
HK40109095A (en) 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