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
Application number
TW102109152A
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English (en)
Chinese (zh)
Other versions
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)
  • Public Health (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • Physics & Mathematics (AREA)
  • Hematology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Microbiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Physics & Mathematics (AREA)
  • Food Science & Technology (AREA)
  • Epidemiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Pathology (AREA)
  • Cell Biology (AREA)
  • Biophysics (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 (enExample)
EP (1) EP2825171B1 (enExample)
JP (2) JP2015511964A (enExample)
KR (1) KR102057357B1 (enExample)
CN (2) CN109846884A (enExample)
AU (2) AU2013202992B2 (enExample)
BR (1) BR112014022700A2 (enExample)
CA (1) CA2867174C (enExample)
EA (1) EA028062B1 (enExample)
ES (1) ES2668279T3 (enExample)
IL (1) IL234639B (enExample)
MX (1) MX359227B (enExample)
MY (1) MY198666A (enExample)
NI (1) NI201400110A (enExample)
NZ (1) NZ628420A (enExample)
PH (1) PH12014502047B1 (enExample)
SG (1) SG11201405686PA (enExample)
TW (1) TWI622395B (enExample)
UA (1) UA114194C2 (enExample)
WO (1) WO2013138560A1 (enExample)
ZA (1) ZA201406708B (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
SG11201505446WA (en) 2013-01-16 2015-08-28 Signal Pharm Llc Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith
WO2014172436A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer
HK1221168A1 (zh) 2013-04-17 2017-05-26 西格诺药品有限公司 用於治疗癌症的包括tor激酶抑制剂和n-(3-(5-氟-2-(4-(2-甲氧基乙氧基)苯基氨基)嘧啶-4-基氨基)苯基)丙烯醯胺的组合疗法
WO2014172425A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
MY189663A (en) * 2013-04-17 2022-02-23 Signal Pharm Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
JP6382946B2 (ja) 2013-04-17 2018-08-29 シグナル ファーマシューティカルズ，エルエルシー ジヒドロピラジノ−ピラジンによる癌治療
EP3549940A1 (en) 2013-04-17 2019-10-09 Signal Pharmaceuticals, LLC Pharmaceutical formulations, 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
CA2908742C (en) 2013-04-17 2021-06-01 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
CN107474051B (zh) 2013-05-29 2020-10-30 西格诺药品有限公司 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途
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
WO2015160880A1 (en) 2014-04-16 2015-10-22 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, COMPOSITIONS AND METHODS OF USE THEREOF
EP3131552B1 (en) 2014-04-16 2020-07-15 Signal Pharmaceuticals, LLC Methods for treating cancer using tor kinase inhibitor combination therapy
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
WO2016010886A1 (en) 2014-07-14 2016-01-21 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
US20180369241A1 (en) * 2015-06-24 2018-12-27 Celgene Corporation Treatment of cancer with dnapk inhibitors
WO2017132235A1 (en) * 2016-01-26 2017-08-03 Dana-Farber Cancer Institute, Inc. METHODS FOR TREATING BRAIN METASTASES USING COMBINATIONS OF ANTI-P13K AND ANTI-mTOR AGENTS
IL271491B2 (en) 2017-06-22 2023-09-01 Celgene Corp Treatment of carcinoma of the liver characterized by hepatitis b virus infection

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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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ES2627352T3 (es) 2006-10-19 2017-07-27 Signal Pharmaceuticals, Llc Compuestos heteroarilo, sus composiciones y su uso como inhibidores de proteínas quinasas
RU2474582C2 (ru) 2006-10-19 2013-02-10 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Гетероарильные соединения, их композиции и их применение в качестве ингибиторов протеинкиназы
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Also Published As

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

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