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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Publication number
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 date
Application filed by Pharmacyclics Llc, Janssen Pharmaceutica Nv filed Critical Pharmacyclics Llc
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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (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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Application Number Title Priority Date Filing Date
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)

Country Link
US (6) US20180009814A1 (enExample)
EP (1) EP3245208A4 (enExample)
JP (2) JP2018502077A (enExample)
KR (1) KR20170102887A (enExample)
CN (2) CN107108640A (enExample)
AU (2) AU2016206693A1 (enExample)
BR (1) BR112017015206B1 (enExample)
CA (2) CA2971460C (enExample)
HK (1) HK1246293A1 (enExample)
IL (4) IL322449A (enExample)
MA (1) MA41350A (enExample)
MX (2) MX366827B (enExample)
RU (1) RU2017128308A (enExample)
SG (2) SG11201705678YA (enExample)
WO (1) WO2016115356A1 (enExample)
ZA (1) ZA201704338B (enExample)

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WO2016127915A1 (zh) * 2015-02-12 2016-08-18 上海度德医药科技有限公司 伊布替尼的制备方法
US11883404B2 (en) 2016-03-04 2024-01-30 Taiho Pharmaceuticals Co., Ltd. Preparation and composition for treatment of malignant tumors
KR102793563B1 (ko) 2016-03-04 2025-04-11 다이호야쿠힌고교 가부시키가이샤 악성 종양 치료용 제제 및 조성물
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
EP4353222A1 (en) 2018-03-19 2024-04-17 Taiho Pharmaceutical Co., Ltd. Use of sodium alkyl sulfate
EP3787751A1 (en) 2018-05-03 2021-03-10 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
KR102742083B1 (ko) 2018-11-09 2024-12-16 다이호야쿠힌고교 가부시키가이샤 디메톡시벤젠 화합물의 제조 방법
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
EP3972977A1 (en) * 2019-05-21 2022-03-30 Janssen Pharmaceutica NV Processes and intermediates for preparing a btk inhibitor
US12459948B2 (en) 2019-05-21 2025-11-04 Janssen Pharmaceutica Nv Processes and intermediates for preparing a Btk inhibitor
EP4281454B1 (en) 2021-01-21 2025-03-05 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
US20250302954A1 (en) 2022-05-11 2025-10-02 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
MXPA06007326A (es) * 2003-12-23 2007-01-26 Astex Therapeutics Ltd Derivados de pirazol como moduladores de proteina cinasa.
DK2529622T3 (en) * 2006-09-22 2018-05-07 Pharmacyclics Llc INHIBITORS OF BRUTON-TYROSINKINASE
NZ579911A (en) * 2007-03-28 2012-05-25 Pharmacyclics Inc Inhibitors of bruton's tyrosine kinase
US7718662B1 (en) * 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
EP2882751B1 (en) * 2012-07-30 2018-06-27 Concert Pharmaceuticals Inc. Deuterated ibrutinib
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
EP3248979B1 (en) * 2015-01-21 2021-04-14 Hefei Institutes of Physical Science, Chinese Academy of Sciences Novel inhibitor of flt3 kinase and use thereof

Also Published As

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

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B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
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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)