TWI664968B - 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
TWI664968B
TWI664968B TW106122809A TW106122809A TWI664968B TW I664968 B TWI664968 B TW I664968B TW 106122809 A TW106122809 A TW 106122809A TW 106122809 A TW106122809 A TW 106122809A TW I664968 B TWI664968 B TW I664968B
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TW
Taiwan
Prior art keywords
substituted
unsubstituted
pyrazine
dihydropyrazino
methyl
Prior art date
Application number
TW106122809A
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English (en)
Chinese (zh)
Other versions
TW201733586A (zh
Inventor
徐水禪
Shuichan Xu
梅耶 黑格克利斯坦
Kristen Mae Hege
Original Assignee
標誌製藥公司
Signal Pharmaceuticals, Llc
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Application filed by 標誌製藥公司, Signal Pharmaceuticals, Llc filed Critical 標誌製藥公司
Publication of TW201733586A publication Critical patent/TW201733586A/zh
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Publication of TWI664968B publication Critical patent/TWI664968B/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
    • A61K31/495—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
    • A61K31/435—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
    • A61K31/505—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
    • G01N33/575—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57557—Immunoassay; Biospecific binding assay; Materials therefor for cancer of other specific parts of the body, e.g. brain

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (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)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Microbiology (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Food Science & Technology (AREA)
  • Cell Biology (AREA)
  • Biotechnology (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)
TW106122809A 2012-03-15 2013-03-14 使用tor激酶抑制劑之癌症治療 TWI664968B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201261611370P 2012-03-15 2012-03-15
US61/611,370 2012-03-15
US201261715329P 2012-10-18 2012-10-18
US61/715,329 2012-10-18

Publications (2)

Publication Number Publication Date
TW201733586A TW201733586A (zh) 2017-10-01
TWI664968B true TWI664968B (zh) 2019-07-11

Family

ID=47998542

Family Applications (2)

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
TW102109153A TWI600428B (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
TW102109153A TWI600428B (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 (https=)
EP (1) EP2825168B1 (https=)
JP (2) JP2015516375A (https=)
KR (3) KR20190058673A (https=)
CN (2) CN107137402A (https=)
AU (1) AU2013203156C1 (https=)
BR (1) BR112014022697A2 (https=)
CA (1) CA2867349A1 (https=)
EA (1) EA028434B1 (https=)
ES (1) ES2677908T3 (https=)
IL (2) IL234640B (https=)
MX (1) MX360877B (https=)
MY (1) MY182650A (https=)
NI (1) NI201400109A (https=)
NZ (1) NZ628421A (https=)
PH (2) PH12014502048B1 (https=)
SG (1) SG11201405706TA (https=)
TW (2) TWI664968B (https=)
WO (1) WO2013138556A1 (https=)
ZA (1) ZA201406709B (https=)

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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
US9937169B2 (en) 2013-04-17 2018-04-10 Signal Pharmaceuticals, Llc Methods for treating cancer using dihydropyrazino-pyrazine compound combination therapy
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
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
US9782427B2 (en) 2013-04-17 2017-10-10 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy
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
AU2014254052B2 (en) 2013-04-17 2019-06-06 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
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
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
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
EA201790189A1 (ru) 2014-07-14 2017-11-30 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Способы лечения злокачественного новообразования с использованием замещенных пирролопиримидиновых соединений, композиции на их основе
SMT202100225T1 (it) * 2016-12-20 2021-05-07 Astrazeneca Ab Composti di ammino-triazolopiridina e loro uso nel trattamento del cancro
EP3641772B1 (en) 2017-06-22 2023-08-02 Celgene Corporation Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection
HUE062437T2 (hu) * 2018-03-01 2023-11-28 Essilor Int Lencseelem
BR202019004173Y1 (pt) 2018-03-01 2024-02-20 Essilor International Dispositivo óptico
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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US7968556B2 (en) 2006-10-19 2011-06-28 Signal Pharmaceuticals, Llc Heteroaryl compounds, compositions thereof, and methods of treatment therewith
MY177695A (en) 2009-10-26 2020-09-23 Signal Pharm Llc Methods of synthesis and purification of heteroaryl compounds
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
HK1201755A1 (en) 2015-09-11
IL234640B (en) 2020-05-31
KR20140138929A (ko) 2014-12-04
MX360877B (es) 2018-11-21
US20130245029A1 (en) 2013-09-19
JP2015516375A (ja) 2015-06-11
MY182650A (en) 2021-01-27
MX2014011117A (es) 2015-04-08
TWI600428B (zh) 2017-10-01
CN104302295B (zh) 2017-06-20
AU2013203156C1 (en) 2016-02-18
ES2677908T3 (es) 2018-08-07
IL274318A (en) 2020-06-30
KR102057358B1 (ko) 2019-12-18
TW201733586A (zh) 2017-10-01
AU2013203156A1 (en) 2013-10-03
CN107137402A (zh) 2017-09-08
KR20200034818A (ko) 2020-03-31
TW201343167A (zh) 2013-11-01
CA2867349A1 (en) 2013-09-19
PH12014502048A1 (en) 2014-12-10
AU2013203156B2 (en) 2015-12-10
EA028434B1 (ru) 2017-11-30
PH12018502234B1 (en) 2021-07-23
IL234640A0 (en) 2014-11-30
EP2825168A1 (en) 2015-01-21
EP2825168B1 (en) 2018-05-09
BR112014022697A2 (pt) 2020-06-30
SG11201405706TA (en) 2014-10-30
JP6470821B2 (ja) 2019-02-13
NZ628421A (en) 2016-04-29
CN104302295A (zh) 2015-01-21
PH12014502048B1 (en) 2020-10-28
PH12018502234A1 (en) 2019-08-14
EA201491694A1 (ru) 2015-06-30
KR20190058673A (ko) 2019-05-29
WO2013138556A1 (en) 2013-09-19
NI201400109A (es) 2015-01-15
ZA201406709B (en) 2016-07-27
JP2018065820A (ja) 2018-04-26

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