TWI583385B - 使用tor之激酶抑制劑之癌症治療 - Google Patents

使用tor之激酶抑制劑之癌症治療 Download PDF

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Publication number
TWI583385B
TWI583385B TW102109160A TW102109160A TWI583385B TW I583385 B TWI583385 B TW I583385B TW 102109160 A TW102109160 A TW 102109160A TW 102109160 A TW102109160 A TW 102109160A TW I583385 B TWI583385 B TW I583385B
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TW
Taiwan
Prior art keywords
substituted
pyrazine
unsubstituted
methyl
tor kinase
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TW102109160A
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English (en)
Chinese (zh)
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TW201343168A (zh
Inventor
徐水禪
克利斯坦 梅耶 黑格
海瑟 雷蒙
莉麗 羅蘭安 王
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標誌製藥公司
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Publication of TW201343168A publication Critical patent/TW201343168A/zh
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Publication of TWI583385B publication Critical patent/TWI583385B/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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW102109160A 2012-03-15 2013-03-14 使用tor之激酶抑制劑之癌症治療 TWI583385B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261611361P 2012-03-15 2012-03-15
US201261715323P 2012-10-18 2012-10-18

Publications (2)

Publication Number Publication Date
TW201343168A TW201343168A (zh) 2013-11-01
TWI583385B true TWI583385B (zh) 2017-05-21

Family

ID=48014336

Family Applications (1)

Application Number Title Priority Date Filing Date
TW102109160A TWI583385B (zh) 2012-03-15 2013-03-14 使用tor之激酶抑制劑之癌症治療

Country Status (21)

Country Link
US (1) US20130245026A1 (https=)
EP (1) EP2825170B1 (https=)
JP (3) JP2015510891A (https=)
KR (3) KR102122617B1 (https=)
CN (2) CN108992446A (https=)
AU (1) AU2013203153B2 (https=)
BR (1) BR112014022703A2 (https=)
CA (1) CA2866872A1 (https=)
EA (1) EA028414B1 (https=)
ES (1) ES2677874T3 (https=)
IL (1) IL234602B (https=)
MX (1) MX360878B (https=)
MY (1) MY174022A (https=)
NI (1) NI201400111A (https=)
NZ (1) NZ628416A (https=)
PH (1) PH12014502029B1 (https=)
SG (1) SG11201405707XA (https=)
TW (1) TWI583385B (https=)
UA (1) UA114315C2 (https=)
WO (1) WO2013138557A1 (https=)
ZA (1) ZA201406706B (https=)

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CA2866872A1 (en) * 2012-03-15 2013-09-19 Signal Pharmaceuticals, Llc Treatment of cancer with tor kinase inhibitors
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
AU2014254052B2 (en) 2013-04-17 2019-06-06 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
BR112015026292B1 (pt) 2013-04-17 2022-04-12 Signal Pharmaceuticals, Llc Uso de 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 e métodos in vitro
TW201521725A (zh) 2013-04-17 2015-06-16 Signal Pharm Llc 使用tor激酶抑制劑組合療法以治療癌症之方法
BR112015026297B1 (pt) 2013-04-17 2022-08-23 Signal Pharmaceuticals, Llc Uso de um inibidor da quinase tor e quinazolinona 5-substituída, composição farmacêutica que os compreende, e kit
TW201527300A (zh) 2013-04-17 2015-07-16 Signal Pharm Llc 關於1-乙基-7-(2-甲基-6-(1H-1,2,4-三唑-3-基)吡啶-3-基)-3,4-二氫吡并[2,3-b]吡-2(1H)-酮之醫藥調配物、方法、固態型式及使用方法
US9937169B2 (en) 2013-04-17 2018-04-10 Signal Pharmaceuticals, Llc Methods for treating cancer using dihydropyrazino-pyrazine compound combination therapy
US9782427B2 (en) * 2013-04-17 2017-10-10 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy
US20140314673A1 (en) * 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
EP3003313A1 (en) 2013-05-29 2016-04-13 Signal Pharmaceuticals, LLC Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use
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
EP3131552B1 (en) 2014-04-16 2020-07-15 Signal Pharmaceuticals, LLC Methods for treating cancer using tor kinase inhibitor combination therapy
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
EA201790189A1 (ru) 2014-07-14 2017-11-30 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Способы лечения злокачественного новообразования с использованием замещенных пирролопиримидиновых соединений, композиции на их основе
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
EP3641772B1 (en) 2017-06-22 2023-08-02 Celgene Corporation Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection

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CN102245611A (zh) * 2008-10-27 2011-11-16 西格诺药品有限公司 用于与 mTOR/PI3K/AKT/途径相关的肿瘤适应症和疾病的 mTOR激酶抑制剂

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ATE543819T1 (de) * 2006-10-19 2012-02-15 Signal Pharm Llc Heteroarylverbindungen, zusammensetzungen daraus und behandlungsverfahren damit
US7968556B2 (en) 2006-10-19 2011-06-28 Signal Pharmaceuticals, Llc Heteroaryl compounds, compositions thereof, and methods of treatment therewith
CA2734828C (en) * 2008-08-20 2018-07-24 J. Silvio Gutkind Chemoprevention of head and neck squamous cell carcinomas
MY177695A (en) 2009-10-26 2020-09-23 Signal Pharm Llc Methods of synthesis and purification of heteroaryl compounds
US20120028972A1 (en) * 2010-07-30 2012-02-02 Lilly Wong Biomarker assays for detecting or measuring inhibition of tor kinase activity
CA2866872A1 (en) * 2012-03-15 2013-09-19 Signal Pharmaceuticals, Llc Treatment of cancer with tor kinase inhibitors

Patent Citations (1)

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CN102245611A (zh) * 2008-10-27 2011-11-16 西格诺药品有限公司 用于与 mTOR/PI3K/AKT/途径相关的肿瘤适应症和疾病的 mTOR激酶抑制剂

Non-Patent Citations (1)

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Bryan T. Hennessy et al., Exploiting the PI3K/AKT pathway for cancer drug discovery, Nature reviews Drug Discovery, 2005, Vol.4, 988-1004 *

Also Published As

Publication number Publication date
EA028414B1 (ru) 2017-11-30
UA114315C2 (uk) 2017-05-25
KR20210071101A (ko) 2021-06-15
CA2866872A1 (en) 2013-09-19
MX2014011077A (es) 2014-10-14
PH12014502029A1 (en) 2014-11-24
JP2021102637A (ja) 2021-07-15
IL234602A0 (en) 2014-11-30
HK1201750A1 (en) 2015-09-11
JP2019108368A (ja) 2019-07-04
ZA201406706B (en) 2016-05-25
KR20200070416A (ko) 2020-06-17
ES2677874T3 (es) 2018-08-07
NI201400111A (es) 2015-01-15
TW201343168A (zh) 2013-11-01
SG11201405707XA (en) 2014-10-30
AU2013203153B2 (en) 2015-09-03
BR112014022703A2 (pt) 2021-05-04
CN104519885A (zh) 2015-04-15
EP2825170A1 (en) 2015-01-21
IL234602B (en) 2020-05-31
JP2015510891A (ja) 2015-04-13
CN108992446A (zh) 2018-12-14
MY174022A (en) 2020-03-04
KR20140138927A (ko) 2014-12-04
EA201491699A1 (ru) 2015-02-27
MX360878B (es) 2018-11-21
AU2013203153A1 (en) 2013-10-03
EP2825170B1 (en) 2018-05-09
WO2013138557A1 (en) 2013-09-19
NZ628416A (en) 2016-04-29
PH12014502029B1 (en) 2014-11-24
US20130245026A1 (en) 2013-09-19
KR102122617B1 (ko) 2020-06-12

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