TWI600428B - 使用ｔｏｒ激酶抑制劑之癌症治療 - Google Patents

使用ｔｏｒ激酶抑制劑之癌症治療 Download PDF

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Publication number
TWI600428B
TWI600428B TW102109153A TW102109153A TWI600428B TW I600428 B TWI600428 B TW I600428B TW 102109153 A TW102109153 A TW 102109153A TW 102109153 A TW102109153 A TW 102109153A TW I600428 B TWI600428 B TW I600428B
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TW
Taiwan
Prior art keywords
substituted
pyrazine
unsubstituted
methyl
tor kinase
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TW102109153A
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English (en)
Chinese (zh)
Other versions
TW201343167A (zh
Inventor
徐水禪
克利斯坦 梅耶 黑格
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標誌製藥公司
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Publication of TW201343167A publication Critical patent/TW201343167A/zh
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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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4985—Pyrazines or piperazines 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
    • A61K31/495—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
    • A61K31/495—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
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57407—Specifically defined cancers

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Cell Biology (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Hospice & Palliative Care (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
TW102109153A 2012-03-15 2013-03-14 使用ｔｏｒ激酶抑制劑之癌症治療 TWI600428B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261611370P 2012-03-15 2012-03-15
US201261715329P 2012-10-18 2012-10-18

Publications (2)

Publication Number Publication Date
TW201343167A TW201343167A (zh) 2013-11-01
TWI600428B true TWI600428B (zh) 2017-10-01

Family

ID=47998542

Family Applications (2)

Application Number Title Priority Date Filing Date
TW102109153A TWI600428B (zh) 2012-03-15 2013-03-14 使用ｔｏｒ激酶抑制劑之癌症治療
TW106122809A TWI664968B (zh) 2012-03-15 2013-03-14 使用tor激酶抑制劑之癌症治療

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW106122809A TWI664968B (zh) 2012-03-15 2013-03-14 使用tor激酶抑制劑之癌症治療

Country Status (20)

Country Link
US (1) US20130245029A1 (enExample)
EP (1) EP2825168B1 (enExample)
JP (2) JP2015516375A (enExample)
KR (3) KR20200034818A (enExample)
CN (2) CN107137402A (enExample)
AU (1) AU2013203156C1 (enExample)
BR (1) BR112014022697A2 (enExample)
CA (1) CA2867349A1 (enExample)
EA (1) EA028434B1 (enExample)
ES (1) ES2677908T3 (enExample)
IL (2) IL234640B (enExample)
MX (1) MX360877B (enExample)
MY (1) MY182650A (enExample)
NI (1) NI201400109A (enExample)
NZ (1) NZ628421A (enExample)
PH (2) PH12014502048B1 (enExample)
SG (1) SG11201405706TA (enExample)
TW (2) TWI600428B (enExample)
WO (1) WO2013138556A1 (enExample)
ZA (1) ZA201406709B (enExample)

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AU2013203714B2 (en) 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
EP2945636B1 (en) 2013-01-16 2017-06-28 Signal Pharmaceuticals, LLC Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith
BR112015026257B1 (pt) 2013-04-17 2022-12-20 Signal Pharmaceuticals, Llc Uso de um composto dihidropirazino-pirazina e enzalutamida, composição farmacêutica que os compreende, e kit
SG11201508527VA (en) 2013-04-17 2015-11-27 Signal Pharm Llc Pharmaceutical formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl) pyridin-3-yl) -3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one
ES2944478T3 (es) 2013-04-17 2023-06-21 Signal Pharm Llc 1-etil-7-(2-metil-6-(1H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-ona para tratar el glioblastoma multiforme
NZ629411A (en) 2013-04-17 2017-06-30 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines
AU2014254057A1 (en) 2013-04-17 2015-11-05 Signal Pharmaceuticals, Llc Combination therapy comprising a TOR kinase inhibitor and N-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer
MX368286B (es) 2013-04-17 2019-09-27 Signal Pharm Llc Terapia de combinacion que comprende un inhibidor de tor cinasa y un compuesto de quinazolinona 5-sustituida para tratar cancer.
KR102242505B1 (ko) 2013-04-17 2021-04-20 시그날 파마소티칼 엘엘씨 암 치료용 tor 키나제 억제제 및 시티딘 유사체를 포함하는 병용 요법
JP6401250B2 (ja) 2013-05-29 2018-10-10 シグナル ファーマシューティカルズ，エルエルシー ７−（６−（２−ヒドロキシプロパン−２−イル）ピリジン−３−イル）−１−（（ｔｒａｎｓ）−４−メトキシシクロヘキシル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オン、その固体形態の医薬組成物、及びその使用方法
NZ714742A (en) 2014-04-16 2017-04-28 Signal Pharm Llc Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use
US9718824B2 (en) 2014-04-16 2017-08-01 Signal Pharmaceuticals, Llc Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, and a coformer, compositions and methods of use thereof
US9737535B2 (en) 2014-04-16 2017-08-22 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy comprising administering substituted pyrazino[2,3-b]pyrazines
US9512129B2 (en) 2014-04-16 2016-12-06 Signal Pharmaceuticals, Llc Solid forms comprising 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and a coformer
AU2015289929A1 (en) 2014-07-14 2017-03-02 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
NZ629796A (en) 2014-07-14 2015-12-24 Signal Pharm Llc Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
HUE054548T2 (hu) * 2016-12-20 2021-09-28 Astrazeneca Ab Amino-triazolopiridin vegyületek és azok alkalmazása rák kezelésében
EP3641772B1 (en) 2017-06-22 2023-08-02 Celgene Corporation Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection
JP7466450B2 (ja) 2018-03-01 2024-04-12 エシロール・アンテルナシオナル レンズ要素
CN113493471B (zh) * 2020-04-03 2024-06-11 山东轩竹医药科技有限公司 杂芳环类激酶抑制剂

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TW201026702A (en) * 2008-10-27 2010-07-16 Signal Pharm Llc Mtor kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway

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ES2383370T3 (es) 2006-10-19 2012-06-20 Signal Pharmaceuticals Llc Compuestos de heteroarilo, sus composiciones y uso de los mismos como inhibidores de proteína quinasa
EP2457913B1 (en) * 2006-10-19 2017-04-19 Signal Pharmaceuticals, LLC Heteroaryl compounds, compositions thereof, and methods of treatment therewith
JP2013508456A (ja) 2009-10-26 2013-03-07 シグナル ファーマシューティカルズ， エルエルシー ヘテロアリール化合物の合成方法および精製方法
WO2011133668A2 (en) * 2010-04-20 2011-10-27 President And Fellows Of Harvard College Methods and compositions for the treatment of cancer

Patent Citations (1)

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TW201026702A (en) * 2008-10-27 2010-07-16 Signal Pharm Llc Mtor kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway

Also Published As

Publication number Publication date
CA2867349A1 (en) 2013-09-19
TWI664968B (zh) 2019-07-11
KR102057358B1 (ko) 2019-12-18
BR112014022697A2 (pt) 2020-06-30
EA028434B1 (ru) 2017-11-30
WO2013138556A1 (en) 2013-09-19
EA201491694A1 (ru) 2015-06-30
KR20140138929A (ko) 2014-12-04
HK1201755A1 (en) 2015-09-11
TW201343167A (zh) 2013-11-01
AU2013203156C1 (en) 2016-02-18
IL234640B (en) 2020-05-31
TW201733586A (zh) 2017-10-01
IL234640A0 (en) 2014-11-30
PH12014502048A1 (en) 2014-12-10
ES2677908T3 (es) 2018-08-07
JP2015516375A (ja) 2015-06-11
JP6470821B2 (ja) 2019-02-13
JP2018065820A (ja) 2018-04-26
CN107137402A (zh) 2017-09-08
NZ628421A (en) 2016-04-29
KR20200034818A (ko) 2020-03-31
AU2013203156A1 (en) 2013-10-03
AU2013203156B2 (en) 2015-12-10
MY182650A (en) 2021-01-27
MX2014011117A (es) 2015-04-08
IL274318A (en) 2020-06-30
EP2825168B1 (en) 2018-05-09
SG11201405706TA (en) 2014-10-30
EP2825168A1 (en) 2015-01-21
ZA201406709B (en) 2016-07-27
US20130245029A1 (en) 2013-09-19
MX360877B (es) 2018-11-21
CN104302295A (zh) 2015-01-21
NI201400109A (es) 2015-01-15
CN104302295B (zh) 2017-06-20
KR20190058673A (ko) 2019-05-29
PH12018502234A1 (en) 2019-08-14
PH12014502048B1 (en) 2020-10-28
PH12018502234B1 (en) 2021-07-23

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