BR112017015206B1 - Processos para a preparação de 1-((r)-3-(4-amino-3-(4- fenoxifenil)-1h- pirazol[3,4-d]pirimidin-1-il)piperidin-1-il)prop-2- en-1-ona (ibrutinibe) e compostos - Google Patents

Processos para a preparação de 1-((r)-3-(4-amino-3-(4- fenoxifenil)-1h- pirazol[3,4-d]pirimidin-1-il)piperidin-1-il)prop-2- en-1-ona (ibrutinibe) e compostos Download PDF

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BR112017015206B1
BR112017015206B1 BR112017015206-1A BR112017015206A BR112017015206B1 BR 112017015206 B1 BR112017015206 B1 BR 112017015206B1 BR 112017015206 A BR112017015206 A BR 112017015206A BR 112017015206 B1 BR112017015206 B1 BR 112017015206B1
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Brazil
Prior art keywords
compound
formula
ibrutinib
scheme
acid
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Application number
BR112017015206-1A
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English (en)
Portuguese (pt)
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BR112017015206A2 (pt
Inventor
Cyril Benhaim
Wei Chen
Erick Goldman
Andras Horvath
Philip Pye
Mark S. Smyth
Erik J. Verner
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Pharmacyclics Llc
Janssen Pharmaceutica Nv
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Publication of BR112017015206A2 publication Critical patent/BR112017015206A2/pt
Publication of BR112017015206B1 publication Critical patent/BR112017015206B1/pt

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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
BR112017015206-1A 2015-01-14 2016-01-14 Processos para a preparação de 1-((r)-3-(4-amino-3-(4- fenoxifenil)-1h- pirazol[3,4-d]pirimidin-1-il)piperidin-1-il)prop-2- en-1-ona (ibrutinibe) e compostos BR112017015206B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562103507P 2015-01-14 2015-01-14
US62/103,507 2015-01-14
PCT/US2016/013424 WO2016115356A1 (en) 2015-01-14 2016-01-14 Synthesis of a bruton's tyrosine kinase inhibitor

Publications (2)

Publication Number Publication Date
BR112017015206A2 BR112017015206A2 (pt) 2018-06-19
BR112017015206B1 true BR112017015206B1 (pt) 2023-04-11

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BR112017015206-1A BR112017015206B1 (pt) 2015-01-14 2016-01-14 Processos para a preparação de 1-((r)-3-(4-amino-3-(4- fenoxifenil)-1h- pirazol[3,4-d]pirimidin-1-il)piperidin-1-il)prop-2- en-1-ona (ibrutinibe) e compostos

Country Status (16)

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US (6) US20180009814A1 (https=)
EP (1) EP3245208A4 (https=)
JP (2) JP2018502077A (https=)
KR (1) KR20170102887A (https=)
CN (2) CN113816962A (https=)
AU (2) AU2016206693A1 (https=)
BR (1) BR112017015206B1 (https=)
CA (2) CA3210320A1 (https=)
HK (1) HK1246293A1 (https=)
IL (4) IL308276A (https=)
MA (1) MA41350A (https=)
MX (2) MX366827B (https=)
RU (1) RU2017128308A (https=)
SG (2) SG10201906517VA (https=)
WO (1) WO2016115356A1 (https=)
ZA (1) ZA201704338B (https=)

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US10214532B2 (en) * 2015-02-12 2019-02-26 Shanghai Dude Medical Science and Technology Co., Ltd. Process for preparing ibrutinib
US11883404B2 (en) 2016-03-04 2024-01-30 Taiho Pharmaceuticals Co., Ltd. Preparation and composition for treatment of malignant tumors
EP3424505A4 (en) 2016-03-04 2019-10-16 Taiho Pharmaceutical Co., Ltd. PREPARATION AND COMPOSITION FOR THE TREATMENT OF MALIGNANT TUMORS
CN109206426B (zh) * 2017-07-06 2021-10-08 上海复星星泰医药科技有限公司 吡唑并嘧啶类化合物的制备方法
JP7166331B2 (ja) 2017-08-01 2022-11-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 中間体化合物及び方法
CN107814804A (zh) * 2017-10-27 2018-03-20 广州科锐特生物科技有限公司 依鲁替尼的制备方法
SG11202008435SA (en) 2018-03-19 2020-10-29 Taiho Pharmaceutical Co Ltd Pharmaceutical composition including sodium alkyl sulfate
US20210121466A1 (en) 2018-05-03 2021-04-29 Juno Therapeutics, Inc. Combination therapy of a chimeric antigen receptor (car) t cell therapy and a kinase inhibitor
JP6944496B2 (ja) * 2018-10-22 2021-10-06 ファイザー・インク ピロロ[2,3−d]ピリミジントシル酸塩、その結晶形態、ならびにその製造方法および中間体
WO2020095452A1 (ja) 2018-11-09 2020-05-14 大鵬薬品工業株式会社 ジメトキシベンゼン化合物の製造方法
CN109988175A (zh) * 2019-04-28 2019-07-09 梯尔希(南京)药物研发有限公司 一种依鲁替尼-d5的制备方法
AU2020280904A1 (en) * 2019-05-21 2021-11-18 Janssen Pharmaceutica Nv Processes and intermediates for preparing a BTK inhibitor
AU2020278162A1 (en) 2019-05-21 2021-11-18 Janssen Pharmaceutica Nv Processes and intermediates for preparing a BTK inhibitor
WO2022157250A1 (en) 2021-01-21 2022-07-28 Synthon B.V. Process for making ibrutinib
CN114853662B (zh) * 2021-02-05 2024-01-12 四川青木制药有限公司 手性肼基哌啶衍生物的制备方法
WO2023220655A1 (en) 2022-05-11 2023-11-16 Celgene Corporation Methods to overcome drug resistance by re-sensitizing cancer cells to treatment with a prior therapy via treatment with a t cell therapy
WO2023242384A1 (en) 2022-06-17 2023-12-21 Krka, D.D., Novo Mesto Crystalline form of ibrutinib

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US4550214A (en) * 1981-01-05 1985-10-29 Polaroid Corporation Blocked vinyl biphenyl compounds
US4874822A (en) * 1988-04-07 1989-10-17 Minnesota Mining And Manufacturing Company Process for the acrylamidoacylation of alcohols
BRPI0418078A8 (pt) * 2003-12-23 2018-01-02 Astex Therapeutics Ltd composto ou um seu sal, solvato, tautômero ou n-óxido, uso de um composto, métodos para a profilaxia ou tratamento de um estado ou condição doentia mediada pela proteína quinase b e mediada pela proteína quinase a, para tratar uma doença ou condição, para inibir uma proteína quinase b e uma proteína quinase a, para modular um processo celular, para tratar um distúrbio imune em um mamífero e para induzir apoptose em uma célula cancerosa, composição farmacêutica, e, processo para a preparação de um composto
BRPI0622054B8 (pt) * 2006-09-22 2021-05-25 Oxford Amherst Llc composto e composição farmacêutica
IL295053A (en) * 2007-03-28 2022-09-01 Pharmacyclics Llc Broton tyrosine kinase inhibitors
US7718662B1 (en) * 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
CN104507946A (zh) * 2012-07-30 2015-04-08 康塞特医药品有限公司 氘代依鲁替尼
CN103121999A (zh) * 2012-08-29 2013-05-29 苏州迪飞医药科技有限公司 一种酪氨酸激酶抑制剂pci-32765的合成方法
US9156847B2 (en) * 2013-03-15 2015-10-13 Janssen Pharmaceutica Nv Processes and intermediates for preparing a medicament
US8957080B2 (en) * 2013-04-09 2015-02-17 Principia Biopharma Inc. Tyrosine kinase inhibitors
CN103626774B (zh) * 2013-11-20 2015-11-04 苏州明锐医药科技有限公司 伊鲁替尼的制备方法
CN105471823B (zh) * 2014-09-03 2018-10-26 阿里巴巴集团控股有限公司 一种敏感信息处理方法、装置、服务器及安全判定系统
US10266535B2 (en) * 2015-01-21 2019-04-23 Hefei Institutes Of Physical Science, Chinese Academy Of Sciences Inhibitor of FLT3 kinase and use thereof

Also Published As

Publication number Publication date
WO2016115356A1 (en) 2016-07-21
US20200347064A1 (en) 2020-11-05
MA41350A (fr) 2017-11-21
CN113816962A (zh) 2021-12-21
IL253020A0 (en) 2017-08-31
US20240158400A1 (en) 2024-05-16
ZA201704338B (en) 2023-10-25
SG11201705678YA (en) 2017-08-30
RU2017128308A (ru) 2019-02-14
BR112017015206A2 (pt) 2018-06-19
HK1246293A1 (zh) 2018-09-07
IL274716A (en) 2020-07-30
KR20170102887A (ko) 2017-09-12
CA3210320A1 (en) 2016-07-21
IL308276A (en) 2024-01-01
RU2017128308A3 (https=) 2019-10-24
AU2020230323A1 (en) 2020-10-01
AU2016206693A1 (en) 2017-07-13
EP3245208A1 (en) 2017-11-22
MX2019008815A (es) 2019-09-26
MX394327B (es) 2025-03-24
EP3245208A4 (en) 2018-10-17
SG10201906517VA (en) 2019-08-27
US20250197404A1 (en) 2025-06-19
JP2018502077A (ja) 2018-01-25
MX366827B (es) 2019-07-25
MX2017009154A (es) 2017-10-12
JP2021035947A (ja) 2021-03-04
CN107108640A (zh) 2017-08-29
US20190367518A1 (en) 2019-12-05
US20220098200A1 (en) 2022-03-31
CA2971460C (en) 2023-10-10
US20180009814A1 (en) 2018-01-11
CA2971460A1 (en) 2016-07-21
IL322449A (en) 2025-09-01

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Ipc: C07D 487/04 (2006.01), A61K 31/519 (2006.01), A61P

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Owner name: PHARMACYCLICS LLC (US) ; JANSSEN PHARMACEUTICA NV (BE)