TWI622395B - 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
TWI622395B
TWI622395B TW102109152A TW102109152A TWI622395B TW I622395 B TWI622395 B TW I622395B TW 102109152 A TW102109152 A TW 102109152A TW 102109152 A TW102109152 A TW 102109152A TW I622395 B TWI622395 B TW I622395B
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TW
Taiwan
Prior art keywords
substituted
unsubstituted
methyl
pyrazine
dihydropyrazino
Prior art date
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TW102109152A
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English (en)
Chinese (zh)
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TW201343166A (zh
Inventor
徐水禪
Shuichan Xu
克利斯坦 梅耶 黑格
Kristen Mae Hege
海瑟 雷蒙
Heather Raymon
十俊也
Toshiya Tsuji
麗莎 沙賓諾索
Lisa SAPINOSO
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 TW201343166A publication Critical patent/TW201343166A/zh
Application granted granted Critical
Publication of TWI622395B publication Critical patent/TWI622395B/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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
    • 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
    • G01N33/57555—Immunoassay; Biospecific binding assay; Materials therefor for cancer of the prostate
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/52—Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/56—Staging of a disease; Further complications associated with the disease

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Public Health (AREA)
  • Biochemistry (AREA)
  • Analytical Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Biotechnology (AREA)
  • Biomedical Technology (AREA)
  • Physics & Mathematics (AREA)
  • Hematology (AREA)
  • Microbiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Food Science & Technology (AREA)
  • Epidemiology (AREA)
  • Cell Biology (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Pathology (AREA)
  • Biophysics (AREA)
  • General Physics & Mathematics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW102109152A 2012-03-15 2013-03-14 使用ｔｏｒ之激酶抑制劑之癌症治療 TWI622395B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201261611428P 2012-03-15 2012-03-15
US61/611,428 2012-03-15
US201261715327P 2012-10-18 2012-10-18
US61/715,327 2012-10-18

Publications (2)

Publication Number Publication Date
TW201343166A TW201343166A (zh) 2013-11-01
TWI622395B true TWI622395B (zh) 2018-05-01

Family

ID=48045717

Family Applications (1)

Application Number Title Priority Date Filing Date
TW102109152A TWI622395B (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) US20130245028A1 (https=)
EP (1) EP2825171B1 (https=)
JP (2) JP2015511964A (https=)
KR (1) KR102057357B1 (https=)
CN (2) CN104271138A (https=)
AU (2) AU2013202992B2 (https=)
BR (1) BR112014022700A2 (https=)
CA (1) CA2867174C (https=)
EA (1) EA028062B1 (https=)
ES (1) ES2668279T3 (https=)
IL (1) IL234639B (https=)
MX (1) MX359227B (https=)
MY (1) MY198666A (https=)
NI (1) NI201400110A (https=)
NZ (1) NZ628420A (https=)
PH (1) PH12014502047A1 (https=)
SG (1) SG11201405686PA (https=)
TW (1) TWI622395B (https=)
UA (1) UA114194C2 (https=)
WO (1) WO2013138560A1 (https=)
ZA (1) ZA201406708B (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
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
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
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
EP3131552B1 (en) 2014-04-16 2020-07-15 Signal Pharmaceuticals, LLC Methods for treating cancer using tor kinase inhibitor combination therapy
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
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
US20180369241A1 (en) * 2015-06-24 2018-12-27 Celgene Corporation Treatment of cancer with dnapk inhibitors
US11318139B2 (en) 2016-01-26 2022-05-03 Dana-Farber Cancer Institute, Inc. Methods for treating brain metastases using combinations of anti-P13K and anti-mTOR agents
EP3641772B1 (en) 2017-06-22 2023-08-02 Celgene Corporation Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection

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Also Published As

Publication number Publication date
ZA201406708B (en) 2016-05-25
JP6470822B2 (ja) 2019-02-13
EA028062B1 (ru) 2017-10-31
BR112014022700A2 (pt) 2020-06-30
JP2018058861A (ja) 2018-04-12
CN104271138A (zh) 2015-01-07
EP2825171A1 (en) 2015-01-21
UA114194C2 (uk) 2017-05-10
MX2014011116A (es) 2015-04-08
US20130245028A1 (en) 2013-09-19
CA2867174A1 (en) 2013-09-19
EP2825171B1 (en) 2018-03-14
IL234639A0 (en) 2014-11-30
PH12014502047B1 (en) 2014-12-10
KR20140138928A (ko) 2014-12-04
SG11201405686PA (en) 2014-10-30
KR102057357B1 (ko) 2019-12-18
NI201400110A (es) 2015-01-12
WO2013138560A1 (en) 2013-09-19
CA2867174C (en) 2020-06-23
AU2013202992A1 (en) 2013-10-03
IL234639B (en) 2020-05-31
ES2668279T3 (es) 2018-05-17
NZ628420A (en) 2016-04-29
PH12014502047A1 (en) 2014-12-10
EA201491701A1 (ru) 2015-01-30
AU2015213353B2 (en) 2017-07-27
TW201343166A (zh) 2013-11-01
MY198666A (en) 2023-09-14
MX359227B (es) 2018-09-20
AU2013202992B2 (en) 2015-09-03
JP2015511964A (ja) 2015-04-23
AU2015213353A1 (en) 2015-09-03
CN109846884A (zh) 2019-06-07
HK1202247A1 (en) 2015-09-25

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