KR102359759B1 - 세린/트레오닌 키나제 저해제 - Google Patents

세린/트레오닌 키나제 저해제 Download PDF

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KR102359759B1
KR102359759B1 KR1020167017847A KR20167017847A KR102359759B1 KR 102359759 B1 KR102359759 B1 KR 102359759B1 KR 1020167017847 A KR1020167017847 A KR 1020167017847A KR 20167017847 A KR20167017847 A KR 20167017847A KR 102359759 B1 KR102359759 B1 KR 102359759B1
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methyl
pyrazol
pyrimidin
dihydro
amine
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Korean (ko)
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KR20160093703A (ko
Inventor
알렉산드르 콜레스니코브
스티븐 도
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제넨테크, 인크.
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    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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
    • C07D471/16Peri-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
    • 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/5365Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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 three hetero rings
    • C07D498/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/12Heterocyclic 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 three hetero rings
    • C07D513/16Peri-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020167017847A 2013-12-06 2014-12-03 세린/트레오닌 키나제 저해제 Expired - Fee Related KR102359759B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361912905P 2013-12-06 2013-12-06
US61/912,905 2013-12-06
PCT/US2014/068452 WO2015085007A1 (en) 2013-12-06 2014-12-03 Serine/threonine kinase inhibitors

Publications (2)

Publication Number Publication Date
KR20160093703A KR20160093703A (ko) 2016-08-08
KR102359759B1 true KR102359759B1 (ko) 2022-02-09

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Country Status (23)

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US (5) US9867833B2 (enExample)
EP (1) EP3077401B1 (enExample)
JP (2) JP6449293B2 (enExample)
KR (1) KR102359759B1 (enExample)
CN (1) CN106029672B (enExample)
AR (1) AR098647A1 (enExample)
AU (1) AU2014360455B2 (enExample)
BR (1) BR112016012844B1 (enExample)
CA (1) CA2932729C (enExample)
CL (1) CL2016001368A1 (enExample)
CR (1) CR20160309A (enExample)
EA (1) EA031243B1 (enExample)
IL (1) IL246017B (enExample)
MA (1) MA39170B1 (enExample)
MX (1) MX368443B (enExample)
MY (1) MY176049A (enExample)
PE (1) PE20160886A1 (enExample)
PH (1) PH12016501071B1 (enExample)
SG (1) SG11201604573WA (enExample)
TW (1) TWI557126B (enExample)
UA (1) UA120506C2 (enExample)
WO (1) WO2015085007A1 (enExample)
ZA (1) ZA201604461B (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
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MX2015004615A (es) 2012-10-16 2015-07-17 Hoffmann La Roche Inhibidores de serina/treonina cinasa.
US9532987B2 (en) 2013-09-05 2017-01-03 Genentech, Inc. Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases
JP6449293B2 (ja) 2013-12-06 2019-01-09 ジェネンテック, インコーポレイテッド セリン/トレオニンキナーゼ阻害剤
WO2015103133A1 (en) 2013-12-30 2015-07-09 Genentech, Inc. Serine/threonine kinase inhibitors
EP3089980B1 (en) * 2013-12-30 2018-01-31 Array Biopharma, Inc. Serine/threonine kinase inhibitors
SI3374359T1 (sl) 2015-11-09 2020-04-30 Astrazeneca Ab Derivati dihidroimidazopirazinona uporabni pri zdravljenju raka
WO2017180581A1 (en) 2016-04-15 2017-10-19 Genentech, Inc. Diagnostic and therapeutic methods for cancer
EP3679159A1 (en) 2017-09-08 2020-07-15 H. Hoffnabb-La Roche Ag Diagnostic and therapeutic methods for cancer
WO2019158579A1 (en) 2018-02-13 2019-08-22 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
TWI879771B (zh) * 2019-06-06 2025-04-11 大陸商和記黃埔醫藥(上海)有限公司 三環類化合物及其用途
AU2022217309A1 (en) * 2021-02-03 2023-09-14 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Fused tricyclic cyclin-dependent kinase inhibitor, and preparation method therefor and pharmaceutical use thereof

Citations (2)

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US20100093718A1 (en) 2006-12-22 2010-04-15 Valerio Berdini Compounds
WO2013130976A1 (en) 2012-03-01 2013-09-06 Array Biopharma Inc. Serine/threonine kinase inhibitors

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EP1438027A1 (en) * 2001-10-25 2004-07-21 DepoMed, Inc. Methods of treatment using a gastric retained losartan dosage
CN101304973A (zh) * 2005-09-15 2008-11-12 佩因赛普托药物公司 调节神经营养蛋白介导的活性的方法
EP2002836B1 (en) * 2007-05-31 2010-10-20 Nerviano Medical Sciences S.r.l. Cyclocondensed azaindoles active as kinase inhibitors
AU2011332043C1 (en) 2010-11-23 2016-11-10 Abbvie Inc. Salts and crystalline forms of an apoptosis-inducing agent
CA2828478C (en) 2011-02-28 2019-12-31 Array Biopharma Inc. Serine/threonine kinase inhibitors
WO2013020062A1 (en) 2011-08-04 2013-02-07 Array Biopharma Inc. Quinazoline compounds as serine/threonine kinase inhibitors
BR112015004548A2 (pt) 2012-08-27 2017-08-08 Array Biopharma Inc inibidores de serina/treonina para tratamento de doenças hiperproliferativas
MX2015004615A (es) 2012-10-16 2015-07-17 Hoffmann La Roche Inhibidores de serina/treonina cinasa.
US9532987B2 (en) 2013-09-05 2017-01-03 Genentech, Inc. Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases
JP6449293B2 (ja) 2013-12-06 2019-01-09 ジェネンテック, インコーポレイテッド セリン/トレオニンキナーゼ阻害剤
EP3089980B1 (en) 2013-12-30 2018-01-31 Array Biopharma, Inc. Serine/threonine kinase inhibitors
WO2015103133A1 (en) 2013-12-30 2015-07-09 Genentech, Inc. Serine/threonine kinase inhibitors
PL3129025T3 (pl) 2014-04-09 2019-11-29 Genentech Inc Sposób wytwarzania środków leczniczych

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100093718A1 (en) 2006-12-22 2010-04-15 Valerio Berdini Compounds
WO2013130976A1 (en) 2012-03-01 2013-09-06 Array Biopharma Inc. Serine/threonine kinase inhibitors

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AU2014360455B2 (en) 2018-05-10
JP2016539153A (ja) 2016-12-15
JP2019034970A (ja) 2019-03-07
AR098647A1 (es) 2016-06-01
EA031243B1 (ru) 2018-12-28
SG11201604573WA (en) 2016-07-28
PH12016501071A1 (en) 2016-07-25
US10517878B2 (en) 2019-12-31
US11376260B2 (en) 2022-07-05
UA120506C2 (uk) 2019-12-26
US20180000833A1 (en) 2018-01-04
IL246017B (en) 2019-10-31
MY176049A (en) 2020-07-22
MX368443B (es) 2019-10-02
CN106029672A (zh) 2016-10-12
CL2016001368A1 (es) 2016-12-09
AU2014360455A1 (en) 2016-07-07
EA201691177A1 (ru) 2016-10-31
BR112016012844B1 (pt) 2023-01-10
MA39170A1 (fr) 2018-04-30
WO2015085007A1 (en) 2015-06-11
US20190192534A1 (en) 2019-06-27
EP3077401B1 (en) 2018-04-18
US10278975B2 (en) 2019-05-07
TWI557126B (zh) 2016-11-11
US20200078371A1 (en) 2020-03-12
US20150182537A1 (en) 2015-07-02
JP6449293B2 (ja) 2019-01-09
IL246017A0 (en) 2016-08-02
PH12016501071B1 (en) 2019-04-26
MX2016007352A (es) 2016-09-08
NZ721361A (en) 2021-07-30
US10842799B2 (en) 2020-11-24
ZA201604461B (en) 2022-05-25
CA2932729A1 (en) 2015-06-11
CA2932729C (en) 2021-02-23
US9867833B2 (en) 2018-01-16
PE20160886A1 (es) 2016-09-14
CR20160309A (es) 2016-08-25
US20210106593A1 (en) 2021-04-15
MA39170B1 (fr) 2019-05-31
EP3077401A1 (en) 2016-10-12
CN106029672B (zh) 2019-03-29
TW201522338A (zh) 2015-06-16
KR20160093703A (ko) 2016-08-08
BR112016012844A2 (enExample) 2017-08-08

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