TWI557126B - 絲胺酸/蘇胺酸激酶抑制劑 - Google Patents

絲胺酸/蘇胺酸激酶抑制劑 Download PDF

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Publication number
TWI557126B
TWI557126B TW103142501A TW103142501A TWI557126B TW I557126 B TWI557126 B TW I557126B TW 103142501 A TW103142501 A TW 103142501A TW 103142501 A TW103142501 A TW 103142501A TW I557126 B TWI557126 B TW I557126B
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TW
Taiwan
Prior art keywords
methyl
pyrazol
dihydro
amine
pyrimidin
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TW103142501A
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English (en)
Chinese (zh)
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TW201522338A (zh
Inventor
亞力山德 柯利斯尼卡瓦
史帝芬 杜
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建南德克公司
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/5365—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 ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D471/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D498/12—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 three hetero rings
    • C07D498/16—Peri-condensed systems
    • 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
    • C07D513/12—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 three hetero rings
    • C07D513/16—Peri-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures 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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
TW103142501A 2013-12-06 2014-12-05 絲胺酸/蘇胺酸激酶抑制劑 TWI557126B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361912905P 2013-12-06 2013-12-06

Publications (2)

Publication Number Publication Date
TW201522338A TW201522338A (zh) 2015-06-16
TWI557126B true TWI557126B (zh) 2016-11-11

Family

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Country Status (23)

Country Link
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 (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2909206A1 (en) 2012-10-16 2015-08-26 F. Hoffmann-La Roche AG Serine/threonine kinase inhibitors
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
EA031243B1 (ru) 2013-12-06 2018-12-28 Дженентек, Инк. Ингибиторы серин/треонинкиназ
KR102379517B1 (ko) 2013-12-30 2022-03-25 제넨테크, 인크. 세린/트레오닌 키나아제 억제제
MX375902B (es) 2013-12-30 2025-03-07 Genentech Inc Inhibidores de serina/treonina cinasa.
SMT202000152T1 (it) 2015-11-09 2020-05-08 Astrazeneca Ab Derivati di diidroimidazopirazinone utili nel trattamento di cancro
AU2017249229A1 (en) 2016-04-15 2018-10-04 Genentech, Inc. Diagnostic and therapeutic methods for cancer
KR102811888B1 (ko) 2017-09-08 2025-05-27 에프. 호프만-라 로슈 아게 암의 진단 및 치료 방법
US20210008047A1 (en) 2018-02-13 2021-01-14 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
CN113227077B (zh) * 2018-12-13 2024-10-29 英特维特国际股份有限公司 一种制备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-甲酰胺的方法
PH12021553058A1 (en) * 2019-06-06 2022-07-25 Hutchison Medipharma Ltd Tricyclic compounds and their use
CN120682245A (zh) * 2021-02-03 2025-09-23 江苏恒瑞医药股份有限公司 稠三环类细胞周期蛋白-依赖性激酶抑制剂及其制备方法和医药用途

Citations (2)

* Cited by examiner, † Cited by third party
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CN101679409A (zh) * 2006-12-22 2010-03-24 Astex治疗学有限公司 新颖化合物
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
US20070099900A1 (en) 2005-09-15 2007-05-03 Painceptor Pharma Corporation Methods of modulating neurotrophin-mediated activity
DE602008003055D1 (de) * 2007-05-31 2010-12-02 Nerviano Medical Sciences Srl Zyklokondensierte Azaindole, die als Kinase-Hemmer wirken
WO2012071336A1 (en) 2010-11-23 2012-05-31 Abbott Laboratories Salts and crystalline forms of an apoptosis-inducing agent
US9133187B2 (en) 2011-02-28 2015-09-15 Array Biopharma Inc. Serine/threonine kinase inhibitors
ES2552989T3 (es) 2011-08-04 2015-12-03 Array Biopharma, Inc. Compuestos de quinazolina como inhibidores de la cinasa de serina / treonina
CA2882750A1 (en) 2012-08-27 2014-03-06 Jim Blake Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases
EP2909206A1 (en) 2012-10-16 2015-08-26 F. Hoffmann-La Roche AG Serine/threonine kinase inhibitors
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
EA031243B1 (ru) 2013-12-06 2018-12-28 Дженентек, Инк. Ингибиторы серин/треонинкиназ
KR102379517B1 (ko) 2013-12-30 2022-03-25 제넨테크, 인크. 세린/트레오닌 키나아제 억제제
MX375902B (es) 2013-12-30 2025-03-07 Genentech Inc Inhibidores de serina/treonina cinasa.
CN106659721B (zh) 2014-04-09 2021-01-01 基因泰克公司 用于制备药物的方法

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
CN101679409A (zh) * 2006-12-22 2010-03-24 Astex治疗学有限公司 新颖化合物
WO2013130976A1 (en) * 2012-03-01 2013-09-06 Array Biopharma Inc. Serine/threonine kinase inhibitors

Also Published As

Publication number Publication date
KR20160093703A (ko) 2016-08-08
MY176049A (en) 2020-07-22
US20190192534A1 (en) 2019-06-27
US20180000833A1 (en) 2018-01-04
US10842799B2 (en) 2020-11-24
MA39170A1 (fr) 2018-04-30
JP2016539153A (ja) 2016-12-15
US10278975B2 (en) 2019-05-07
US20210106593A1 (en) 2021-04-15
PH12016501071B1 (en) 2019-04-26
PE20160886A1 (es) 2016-09-14
TW201522338A (zh) 2015-06-16
CN106029672A (zh) 2016-10-12
ZA201604461B (en) 2022-05-25
CN106029672B (zh) 2019-03-29
EA031243B1 (ru) 2018-12-28
JP2019034970A (ja) 2019-03-07
US20150182537A1 (en) 2015-07-02
SG11201604573WA (en) 2016-07-28
US10517878B2 (en) 2019-12-31
WO2015085007A1 (en) 2015-06-11
AR098647A1 (es) 2016-06-01
CA2932729A1 (en) 2015-06-11
EA201691177A1 (ru) 2016-10-31
EP3077401A1 (en) 2016-10-12
AU2014360455A1 (en) 2016-07-07
UA120506C2 (uk) 2019-12-26
US11376260B2 (en) 2022-07-05
BR112016012844A2 (enExample) 2017-08-08
US9867833B2 (en) 2018-01-16
MA39170B1 (fr) 2019-05-31
CL2016001368A1 (es) 2016-12-09
EP3077401B1 (en) 2018-04-18
JP6449293B2 (ja) 2019-01-09
US20200078371A1 (en) 2020-03-12
IL246017A0 (en) 2016-08-02
MX368443B (es) 2019-10-02
MX2016007352A (es) 2016-09-08
KR102359759B1 (ko) 2022-02-09
NZ721361A (en) 2021-07-30
AU2014360455B2 (en) 2018-05-10
BR112016012844B1 (pt) 2023-01-10
CA2932729C (en) 2021-02-23
CR20160309A (es) 2016-08-25
IL246017B (en) 2019-10-31
PH12016501071A1 (en) 2016-07-25

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