MD20140047A2 - Inhibitori ai protein kinazei - Google Patents

Inhibitori ai protein kinazei Download PDF

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Publication number
MD20140047A2
MD20140047A2 MDA20140047A MD20140047A MD20140047A2 MD 20140047 A2 MD20140047 A2 MD 20140047A2 MD A20140047 A MDA20140047 A MD A20140047A MD 20140047 A MD20140047 A MD 20140047A MD 20140047 A2 MD20140047 A2 MD 20140047A2
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MD
Moldova
Prior art keywords
protein kinase
kinase inhibitors
rfrf
formula
inhibitors
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MDA20140047A
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English (en)
Russian (ru)
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MD4582B1 (ro
MD4582C1 (ro
Inventor
Теро Линнанен
Ярд ВОЛЬФАРТ
Сринивас Нандури
Рави УДДЖИНАМАТАДА
Сринивасан РАДЖАГОПАЛАН
Субхенду Мукхерджи
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Orion Corporation
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=54261175&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MD20140047(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Orion Corporation filed Critical Orion Corporation
Publication of MD20140047A2 publication Critical patent/MD20140047A2/ro
Publication of MD4582B1 publication Critical patent/MD4582B1/ro
Publication of MD4582C1 publication Critical patent/MD4582C1/ro

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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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Abstract

Invenţia se referă la compusul cu formula (I):în care R3, R4, G, B, M şi Z au semnificaţiile definite în revendicări, şi la sărurile farmaceutic acceptabile ale acestuia. Compuşii cu formula (I) acţionează ca inhibitori ai FGFR kinazei şi sunt utili în tratamentul stării, în care este dezirabilă inhibarea FGFR kinazei, cum ar fi cancerul.
MDA20140047A 2011-10-10 2012-10-09 Derivaţi ai 1-fenil-1H-benzimidazolului ca inhibitori ai protein kinazei MD4582C1 (ro)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1306KO2011 2011-10-10
PCT/FI2012/000040 WO2013053983A1 (en) 2011-10-10 2012-10-09 Protein kinase inhibitors

Publications (3)

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MD20140047A2 true MD20140047A2 (ro) 2014-09-30
MD4582B1 MD4582B1 (ro) 2018-07-31
MD4582C1 MD4582C1 (ro) 2019-02-28

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MDA20140047A MD4582C1 (ro) 2011-10-10 2012-10-09 Derivaţi ai 1-fenil-1H-benzimidazolului ca inhibitori ai protein kinazei

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EP (1) EP2766354B1 (ro)
JP (1) JP5890027B2 (ro)
CN (1) CN103958500B (ro)
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AU (1) AU2012322572B2 (ro)
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HU (1) HUE030366T2 (ro)
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IN (1) IN2014CN03159A (ro)
MD (1) MD4582C1 (ro)
ME (1) ME02453B (ro)
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MY (1) MY170823A (ro)
PE (1) PE20141827A1 (ro)
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PT (1) PT2766354T (ro)
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SG (1) SG11201400792YA (ro)
SI (1) SI2766354T1 (ro)
SM (1) SMT201600238B (ro)
TW (1) TWI567066B (ro)
UA (1) UA111382C2 (ro)
WO (1) WO2013053983A1 (ro)
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
TWI628176B (zh) * 2013-04-04 2018-07-01 奧利安公司 蛋白質激酶抑制劑
TWI649318B (zh) 2013-04-19 2019-02-01 英塞特控股公司 作為fgfr抑制劑之雙環雜環
EP3094326A4 (en) 2014-01-14 2017-07-26 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
TN2016000270A1 (en) 2014-01-14 2017-10-06 Millennium Pharm Inc Heteroaryls and uses thereof.
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US10269617B2 (en) * 2016-06-22 2019-04-23 Globalwafers Co., Ltd. High resistivity silicon-on-insulator substrate comprising an isolation region
CN115124470B (zh) 2017-03-23 2024-08-27 奥瑞基尼肿瘤有限公司 用于制备磺酰胺结构化的激酶抑制剂的方法
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3665167B1 (en) 2017-08-11 2022-11-30 Syngenta Participations AG Pesticidally active pyrazole derivatives
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
ES2991427T3 (es) 2018-05-04 2024-12-03 Incyte Corp Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas
MX2021002524A (es) * 2018-09-06 2021-04-28 Aurigene Discovery Tech Limited Star Nuevas formas de sal de clorhidrato de un inhibidor de cinasa estructurada por sulfonamida.
WO2020135878A1 (zh) * 2018-12-29 2020-07-02 南京明德新药研发有限公司 作为fgfr和vegfr双重抑制剂的咪唑并吡啶衍生物
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
CN109776436B (zh) * 2019-03-14 2020-12-18 帕潘纳(北京)科技有限公司 一种三唑类化合物的制备方法
BR112021018168B1 (pt) 2019-03-21 2023-11-28 Onxeo Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer
AU2020292664B2 (en) 2019-06-14 2023-04-13 Cgenetech (Suzhou, China) Co., Ltd. Fused ring compound as FGFR and VEGFR dual inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
GEAP202415945A (en) 2019-10-14 2024-04-25 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3159348A1 (en) 2019-11-08 2021-05-14 Inserm (Institut National De La Sante Et De La Recherche Medicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
EP4114359A1 (en) * 2020-03-05 2023-01-11 Aurigene Discovery Technologies Limited Pharmaceutical compositions of a kinase inhibitor
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN114671810B (zh) * 2022-03-21 2024-03-22 济南鸿湾生物技术有限公司 一种咪唑苯脲的制备方法
WO2024246852A2 (en) * 2023-06-01 2024-12-05 Aurigene Oncology Limited Method of treating fibrotic diseases using protein kinase inhibitor
CN117069696B (zh) * 2023-08-17 2024-04-26 中国药科大学 一种双靶点小分子抑制剂及其制备方法和应用
WO2026013198A1 (en) * 2024-07-10 2026-01-15 Universiteit Antwerpen Oxazole derivatives for oral administration

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001040217A1 (en) * 1999-11-30 2001-06-07 Pfizer Products Inc. Novel benzoimidazole derivatives useful as antiproliferative agents
US6329380B1 (en) * 1999-06-30 2001-12-11 Merck & Co., Inc. SRC kinase inhibitor compounds
WO2005021531A1 (en) * 2003-08-21 2005-03-10 Osi Pharmaceuticals, Inc. N-substituted benzimidazolyl c-kit inhibitors
WO2006060381A2 (en) * 2004-12-01 2006-06-08 Osi Pharmaceuticals, Inc. N-substituted benzimidazolyl c-kit inhibitors and combinatorial benzimidazole library
WO2009019518A1 (en) * 2007-08-09 2009-02-12 Astrazeneca Ab Pyrimidine compounds having a fgfr inhibitory effect

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6465484B1 (en) 1997-09-26 2002-10-15 Merck & Co., Inc. Angiogenesis inhibitors
US6162804A (en) 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
US20060135553A1 (en) 2004-10-28 2006-06-22 Campbell David A Imidazole derivatives
MX2009006706A (es) 2006-12-22 2009-07-02 Astex Therapeutics Ltd Compuestos heterociclicos biciclicos como inhibidores del receptor del factor de crecimiento de fibroblastos.
MX2009006704A (es) * 2006-12-22 2009-06-30 Astex Therapeutics Ltd Derivados de amina triciclicos como inhibidores de proteina de tirosina cinasa.
AR067326A1 (es) 2007-05-11 2009-10-07 Novartis Ag Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido
GB0810902D0 (en) 2008-06-13 2008-07-23 Astex Therapeutics Ltd New compounds
GB0906470D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
GB0906472D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
WO2012131501A1 (en) * 2011-03-28 2012-10-04 Glenmark Pharmaceuticals S.A. Substituted benzimidazole compounds as cot kinase inhibitors

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6329380B1 (en) * 1999-06-30 2001-12-11 Merck & Co., Inc. SRC kinase inhibitor compounds
WO2001040217A1 (en) * 1999-11-30 2001-06-07 Pfizer Products Inc. Novel benzoimidazole derivatives useful as antiproliferative agents
WO2005021531A1 (en) * 2003-08-21 2005-03-10 Osi Pharmaceuticals, Inc. N-substituted benzimidazolyl c-kit inhibitors
WO2006060381A2 (en) * 2004-12-01 2006-06-08 Osi Pharmaceuticals, Inc. N-substituted benzimidazolyl c-kit inhibitors and combinatorial benzimidazole library
WO2009019518A1 (en) * 2007-08-09 2009-02-12 Astrazeneca Ab Pyrimidine compounds having a fgfr inhibitory effect

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Matthew Squires et al. Potent, Selective Inhibitors of Fibroblast Growth Factor Receptor Define Fibroblast Growth Factor Dependence in Preclinical Cancer Models. Molecular Cancer Therapeutics, 2011, vol. 10, nr. 9, p. 1542-1552 (regăsit în internet la 2017.08.29 URL: <<http://mct.aacrjournals.org/content/10/9/1542>>) *
Oriol Casanovas et al. Drug resistance by evasion of antiangiogenic targeting of VEGF signaling in late-stage pancreatic islet tumors. Cancer Cell, 2005, vol. 8, nr. 4, p. 299-309 (regăsit în internet la 2017.08.29 URL: <<http://www.cell.com/cancer-cell/fulltext/S1535-6108(05)00298-9>>) *
WenjunZhou et al. A Structure-Guided Approach to Creating Covalent FGFR Inhibitors. Chemistry & Biology, 2010, vol. 17, nr. 3, p. 285-295 (regăsit în internet la 2017.08.29 URL: <<http://www.sciencedirect.com/science/article/pii/S1074552110000761>>) *

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