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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Publication of TW201522338A publication Critical patent/TW201522338A/zh
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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
    • A61K31/495Heterocyclic 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
    • 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
    • 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
    • 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
    • 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)
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

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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
Publication number Priority date Publication date Assignee Title
CA2884766A1 (en) 2012-10-16 2014-04-24 Daniel Jon Burdick 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
CN105980387B (zh) 2013-12-30 2019-04-19 阵列生物制药公司 丝氨酸/苏氨酸激酶抑制剂
CA2934679C (en) 2013-12-30 2023-02-28 Genentech, Inc. Serine/threonine kinase inhibitors
SG11201803066VA (en) 2015-11-09 2018-05-30 Astrazeneca Ab Dihydroimidazopyrazinone derivatives useful in the treatment of cancer
CN109072311A (zh) 2016-04-15 2018-12-21 豪夫迈·罗氏有限公司 用于癌症的诊断和治疗方法
WO2019051296A1 (en) 2017-09-08 2019-03-14 Genentech, Inc. DIAGNOSTIC AND THERAPEUTIC METHODS OF CANCER
WO2019158579A1 (en) 2018-02-13 2019-08-22 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
AU2020288273B2 (en) * 2019-06-06 2025-11-13 Hutchison Medipharma Limited Tricyclic compounds and their use
MX2023008896A (es) * 2021-02-03 2023-08-09 Tuojie Biotech Shanghai Co Ltd Inhibidor triciclico fusionado de la cinasa dependiente de ciclina, y metodo de preparacion del mismo y uso farmaceutico del mismo.

Citations (2)

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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
CA2622571A1 (en) 2005-09-15 2007-03-22 Painceptor Pharma Corporation Methods of modulating neurotrophin-mediated activity
EP2002836B1 (en) 2007-05-31 2010-10-20 Nerviano Medical Sciences S.r.l. Cyclocondensed azaindoles active as kinase inhibitors
SG190361A1 (en) 2010-11-23 2013-06-28 Abbvie Inc Salts and crystalline forms of an apoptosis-inducing agent
RU2013143839A (ru) 2011-02-28 2015-04-10 Эррэй Биофарма Инк. Ингибиторы сериновых/треониновых киназ
MX340756B (es) 2011-08-04 2016-07-25 Array Biopharma Inc Compuestos de quinazolina como inhibidores de serina/treonina quinasa.
HK1210174A1 (en) 2012-08-27 2016-04-15 Array Biopharma, Inc. Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases
CA2884766A1 (en) 2012-10-16 2014-04-24 Daniel Jon Burdick 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
CN105980387B (zh) 2013-12-30 2019-04-19 阵列生物制药公司 丝氨酸/苏氨酸激酶抑制剂
CA2934679C (en) 2013-12-30 2023-02-28 Genentech, Inc. Serine/threonine kinase inhibitors
CN112645927A (zh) 2014-04-09 2021-04-13 基因泰克公司 用于制备药物的方法

Patent Citations (2)

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

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