EA027561B1 - Алкилированные соединения пиперазина в качестве ингибиторов тирозинкиназы брутона - Google Patents

Алкилированные соединения пиперазина в качестве ингибиторов тирозинкиназы брутона Download PDF

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Publication number
EA027561B1
EA027561B1 EA201490859A EA201490859A EA027561B1 EA 027561 B1 EA027561 B1 EA 027561B1 EA 201490859 A EA201490859 A EA 201490859A EA 201490859 A EA201490859 A EA 201490859A EA 027561 B1 EA027561 B1 EA 027561B1
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EA
Eurasian Patent Office
Prior art keywords
methyl
oxo
mmol
fluoro
pyridin
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EA201490859A
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English (en)
Russian (ru)
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EA201490859A1 (ru
Inventor
Джеймс Джон Кроуфорд
Венди Б. Янг
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Ф.Хоффманн-Ля Рош Аг
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Application filed by Ф.Хоффманн-Ля Рош Аг filed Critical Ф.Хоффманн-Ля Рош Аг
Publication of EA201490859A1 publication Critical patent/EA201490859A1/ru
Publication of EA027561B1 publication Critical patent/EA027561B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/495—Heterocyclic 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/33—Heterocyclic compounds
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
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    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
EA201490859A 2011-11-03 2012-11-02 Алкилированные соединения пиперазина в качестве ингибиторов тирозинкиназы брутона EA027561B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161555395P 2011-11-03 2011-11-03
PCT/US2012/063198 WO2013067277A1 (en) 2011-11-03 2012-11-02 Alkylated piperazine compounds as inhibitors of btk activity

Publications (2)

Publication Number Publication Date
EA201490859A1 EA201490859A1 (ru) 2014-09-30
EA027561B1 true EA027561B1 (ru) 2017-08-31

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EA201490859A EA027561B1 (ru) 2011-11-03 2012-11-02 Алкилированные соединения пиперазина в качестве ингибиторов тирозинкиназы брутона

Country Status (23)

Country Link
US (3) US8729072B2 (enExample)
EP (1) EP2773639B1 (enExample)
JP (2) JP5976828B2 (enExample)
KR (1) KR101716011B1 (enExample)
CN (1) CN104024255B (enExample)
AR (1) AR088642A1 (enExample)
AU (1) AU2012332368A1 (enExample)
BR (1) BR112014010439A2 (enExample)
CA (1) CA2853970A1 (enExample)
CL (1) CL2014001158A1 (enExample)
CO (1) CO6950475A2 (enExample)
CR (1) CR20140187A (enExample)
EA (1) EA027561B1 (enExample)
IL (1) IL232280A0 (enExample)
IN (1) IN2014CN03265A (enExample)
MA (1) MA35725B1 (enExample)
MX (1) MX2014005289A (enExample)
PE (1) PE20141686A1 (enExample)
PH (1) PH12014500966A1 (enExample)
SG (1) SG11201401993RA (enExample)
TW (1) TW201326171A (enExample)
WO (1) WO2013067277A1 (enExample)
ZA (1) ZA201403158B (enExample)

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TW201326171A (zh) * 2011-11-03 2013-07-01 Genentech Inc 烷基化哌□化合物
UA111756C2 (uk) * 2011-11-03 2016-06-10 Ф. Хоффманн-Ля Рош Аг Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона
HK1214820A1 (zh) 2013-07-03 2016-08-05 豪夫迈．罗氏有限公司 杂芳基吡啶酮和氮杂-吡啶酮酰胺化合物
CN105793251B (zh) 2013-12-05 2018-10-12 豪夫迈·罗氏有限公司 具有亲电子官能性的杂芳基吡啶酮和氮杂-吡啶酮化合物
USRE50030E1 (en) 2013-12-13 2024-07-02 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
EP3079682A4 (en) 2013-12-13 2017-08-30 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
WO2015151006A1 (en) 2014-03-29 2015-10-08 Lupin Limited Substituted purine compounds as btk inhibitors
KR102359214B1 (ko) 2014-04-04 2022-02-07 델 마 파마슈티컬스 폐의 비소세포 암종 및 난소암을 치료하기 위한 디안하이드로갈락티톨 및 이의 유사체 또는 유도체
WO2015170266A1 (en) 2014-05-07 2015-11-12 Lupin Limited Substituted pyrimidine compounds as btk inhibitors
WO2016050921A1 (en) 2014-10-02 2016-04-07 F. Hoffmann-La Roche Ag Pyrazole carboxamide compounds for use in the treament of disorders mediated by bruton's tyrosine kinase (btk)
CA2965178C (en) 2014-10-22 2023-09-26 Dana-Farber Cancer Institute, Inc. Thiazolyl-containing compounds for treating proliferative diseases
CN107108604B (zh) 2014-10-27 2020-07-24 豪夫迈·罗氏有限公司 制备三环内酰胺化合物的方法
CN105837576B (zh) 2015-01-14 2019-03-26 湖北生物医药产业技术研究院有限公司 Btk抑制剂
KR102894264B1 (ko) * 2015-03-10 2025-12-02 오리진 온콜로지 리미티드 면역조절제로서의 1,2,4-옥사다이아졸 및 티아다이아졸 화합물
PL4049660T3 (pl) 2016-02-29 2025-06-09 F. Hoffmann-La Roche Ag Kompozycje postaci dawkowania zawierające inhibitor kinazy tyrozynowej Brutona
US11590167B2 (en) 2016-12-03 2023-02-28 Juno Therapeutic, Inc. Methods and compositions for use of therapeutic T cells in combination with kinase inhibitors
SI3555099T1 (sl) * 2016-12-15 2021-11-30 F. Hoffmann-La Roche Ag Postopek priprave zaviralcev BTK
CN107445981B (zh) * 2017-08-25 2018-06-22 牡丹江医学院 一种用于防治宫颈炎的活性化合物
US12637467B2 (en) 2019-02-25 2026-05-26 Newave Pharmaceutical Inc. Inhibitor of BTK and mutants thereof
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
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