KR102359759B1 - 세린/트레오닌 키나제 저해제 - Google Patents

세린/트레오닌 키나제 저해제 Download PDF

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Publication number
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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (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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KR1020167017847A Expired - Fee Related KR102359759B1 (ko) 2013-12-06 2014-12-03 세린/트레오닌 키나제 저해제

Country Status (23)

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

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JP2015533151A (ja) 2012-10-16 2015-11-19 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト セリン/スレオニンキナーゼ阻害剤
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
EP3077401B1 (en) 2013-12-06 2018-04-18 Genentech, Inc. Serine/threonine kinase inhibitors
KR102379517B1 (ko) 2013-12-30 2022-03-25 제넨테크, 인크. 세린/트레오닌 키나아제 억제제
JP6642942B2 (ja) * 2013-12-30 2020-02-12 アレイ バイオファーマ、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
RS60155B1 (sr) * 2015-11-09 2020-05-29 Astrazeneca Ab Derivati dihidroimidazopirazinona korisni za upotrebu u tretmanu raka
WO2017180581A1 (en) 2016-04-15 2017-10-19 Genentech, Inc. Diagnostic and therapeutic methods for cancer
AU2018329925B2 (en) 2017-09-08 2025-05-29 F. Hoffmann-La Roche Ag Diagnostic and therapeutic methods for cancer
EP3752200A1 (en) 2018-02-13 2020-12-23 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
CN119350306A (zh) * 2018-12-13 2025-01-24 英特维特国际股份有限公司 1-[(3r,4s)-4-氰基四氢吡喃-3-基]-3-[(2-氟-6-甲氧基-4-吡啶基)氨基]吡唑-4-甲酰胺制备方法
MX2021014961A (es) * 2019-06-06 2022-01-24 Hutchison Medipharma Ltd Compuestos triciclicos y su uso.
TW202231282A (zh) * 2021-02-03 2022-08-16 大陸商上海拓界生物醫藥科技有限公司 稠三環類細胞週期蛋白-依賴性激酶抑制劑及其製備方法和醫藥用途

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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JP2005508358A (ja) * 2001-10-25 2005-03-31 デポメド・インコーポレイテッド 胃滞留型ロサルタン投与量を用いる治療方法
BRPI0615930A2 (pt) * 2005-09-15 2016-08-23 Painceptor Pharma Corp métodos de modular a interação de uma neurotrofina e um receptor de neurotrofina, de tratar dor em um indivíduo, de tratar distúrbio inflamatório em um indivíduo, de tratar um distúrbio neurológico em um indivíduo, e de tratar uma doença ou distúrbio associado aos sistemas geniturinário e/ou gastrointestinal de um indivíduo, e, composto
EP2002836B1 (en) * 2007-05-31 2010-10-20 Nerviano Medical Sciences S.r.l. Cyclocondensed azaindoles active as kinase inhibitors
PT2643322T (pt) 2010-11-23 2017-11-13 Abbvie Inc Sais e formas cristalinas de um agente indutor de apoptose
CN103635472B (zh) 2011-02-28 2018-01-12 阵列生物制药公司 丝氨酸/苏氨酸激酶抑制剂
JP6097289B2 (ja) 2011-08-04 2017-03-15 アレイ バイオファーマ、インコーポレイテッド セリン/スレオニンキナーゼインヒビターとしてのキナゾリン化合物
AR092253A1 (es) 2012-08-27 2015-04-08 Array Biopharma Inc Inhibidores de serina/treonina cinasa
JP2015533151A (ja) 2012-10-16 2015-11-19 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト セリン/スレオニンキナーゼ阻害剤
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
EP3077401B1 (en) 2013-12-06 2018-04-18 Genentech, Inc. Serine/threonine kinase inhibitors
KR102379517B1 (ko) 2013-12-30 2022-03-25 제넨테크, 인크. 세린/트레오닌 키나아제 억제제
JP6642942B2 (ja) 2013-12-30 2020-02-12 アレイ バイオファーマ、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
MY188526A (en) 2014-04-09 2021-12-18 Genentech Inc Process for the manufacturing of medicaments

Patent Citations (2)

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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

Also Published As

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

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