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)
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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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Publication of TWI600428B publication Critical patent/TWI600428B/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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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 (OSRAM)
EP (1) EP2825168B1 (OSRAM)
JP (2) JP2015516375A (OSRAM)
KR (3) KR102057358B1 (OSRAM)
CN (2) CN104302295B (OSRAM)
AU (1) AU2013203156C1 (OSRAM)
BR (1) BR112014022697A2 (OSRAM)
CA (1) CA2867349A1 (OSRAM)
EA (1) EA028434B1 (OSRAM)
ES (1) ES2677908T3 (OSRAM)
IL (2) IL234640B (OSRAM)
MX (1) MX360877B (OSRAM)
MY (1) MY182650A (OSRAM)
NI (1) NI201400109A (OSRAM)
NZ (1) NZ628421A (OSRAM)
PH (2) PH12014502048B1 (OSRAM)
SG (1) SG11201405706TA (OSRAM)
TW (2) TWI600428B (OSRAM)
WO (1) WO2013138556A1 (OSRAM)
ZA (1) ZA201406709B (OSRAM)

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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
CN105188704B (zh) 2013-01-16 2017-09-19 西格诺药品有限公司 被取代的吡咯并嘧啶化合物、其组合物和使用其的治疗方法
KR102221029B1 (ko) 2013-04-17 2021-02-26 시그날 파마소티칼 엘엘씨 디하이드로피라지노-피라진을 사용한 암의 치료
UA115805C2 (uk) 2013-04-17 2017-12-26 Сігнал Фармасьютікалз, Елелсі Комбінована терапія, яка включає сполуку дигідропіразинопіразину й антагоніст рецептора андрогену, для лікування раку простати
US9358232B2 (en) 2013-04-17 2016-06-07 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy
PH12021552945B1 (en) 2013-04-17 2024-02-28 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines
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
EA037683B1 (ru) 2013-04-17 2021-04-29 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Фармацевтические составы, способы, твердые формы и способы применения, относящиеся к 1-этил-7-(2-метил-6-(1h-1,2,4-триазол-3-ил)пиридин-3-ил)-3,4-дигидропиразино[2,3-b] пиразин-2(1h)-ону
NZ631082A (en) 2013-04-17 2017-06-30 Signal Pharm Llc Methods for treating cancer using tor kinase inhibitor combination therapy
CN105407892B (zh) 2013-05-29 2019-05-07 西格诺药品有限公司 一种化合物的药物组合物、其固体形式及它们的使用方法
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
WO2015160882A1 (en) 2014-04-16 2015-10-22 Signal Pharmaceuticals, Llc SOLID FORMS COMPRISING 7-(6-(2-HYDROXYPROPAN-2YL) 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
WO2015160868A1 (en) 2014-04-16 2015-10-22 Signal Pharmaceuticals, Llc Methods for treating cancer using tor kinase inhibitor combination therapy
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
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
CA2955009A1 (en) 2014-07-14 2016-01-21 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
AU2017384388B2 (en) * 2016-12-20 2020-09-17 Astrazeneca Ab Amino-triazolopyridine compounds and their use in treating cancer
IL271491B2 (en) 2017-06-22 2023-09-01 Celgene Corp Treatment of carcinoma of the liver characterized by hepatitis b virus infection
SG11202008010SA (en) * 2018-03-01 2020-09-29 Essilor Int Lens element
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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Also Published As

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

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