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
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TW106122809A
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English (en)
Chinese (zh)
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TW201733586A (zh
Inventor
徐水禪
梅耶 黑格克利斯坦
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標誌製藥公司
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Publication of TW201733586A publication Critical patent/TW201733586A/zh
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Publication of TWI664968B publication Critical patent/TWI664968B/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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • 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
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • 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
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57407Specifically defined cancers

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Cell Biology (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Biotechnology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Microbiology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Hospice & Palliative Care (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 (OSRAM)
EP (1) EP2825168B1 (OSRAM)
JP (2) JP2015516375A (OSRAM)
KR (3) KR20190058673A (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) TWI664968B (OSRAM)
WO (1) WO2013138556A1 (OSRAM)
ZA (1) ZA201406709B (OSRAM)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
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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
US9346812B2 (en) 2013-01-16 2016-05-24 Signal Pharmaceuticals, Llc Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith
EP2986322A1 (en) 2013-04-17 2016-02-24 Signal Pharmaceuticals, LLC Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer
NZ629230A (en) 2013-04-17 2017-05-26 Signal Pharm Llc Pharmaceutical formulations, processes, solid forms and methods of use relating to 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
CA2909579A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer
NZ629332A (en) 2013-04-17 2017-05-26 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines
NZ629411A (en) 2013-04-17 2017-06-30 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines
NZ629469A (en) 2013-04-17 2017-05-26 Signal Pharm Llc Methods for treating cancer using dihydropyrazino-pyrazine compound combination therapy
MX374749B (es) 2013-04-17 2025-03-06 Signal Pharm Llc Terapia de combinacion que comprende un inhibidor de tor cinasa y un analogo de citidina para tratar cancer.
HK1223286A1 (zh) 2013-05-29 2017-07-28 西格诺药品有限公司 7-(6-(2-羟基丙-2-基)吡啶-3-基)-1-((反式)-4-甲氧基环己基)-3,4-二氢吡嗪并[2,3-b]吡嗪-2(1h)-酮的药物组合物、其固体形式及它们的使用方法
EP3131551A4 (en) 2014-04-16 2017-09-20 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
WO2015160868A1 (en) 2014-04-16 2015-10-22 Signal Pharmaceuticals, Llc Methods for treating cancer using tor kinase inhibitor combination therapy
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
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
WO2016010886A1 (en) 2014-07-14 2016-01-21 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions 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
NZ755222A (en) 2016-12-20 2022-07-01 Astrazeneca Ab Amino-triazolopyridine compounds and their use in treating cancer
MY198676A (en) 2017-06-22 2023-09-15 Celgene Corp Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection
BR112020017312B1 (pt) 2018-03-01 2023-03-14 Essilor International Elemento de lente
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

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

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ZA200902384B (en) 2006-10-19 2010-07-28 Signal Pharm Llc Heteroaryl compounds, compositions thereof, and use thereof as protein kinase inhibitors
CN105693730A (zh) * 2006-10-19 2016-06-22 西格诺药品有限公司 杂芳基化合物、其组合物以及它们作为蛋白激酶抑制剂的用途
CA2778615C (en) 2009-10-26 2019-04-23 Signal Pharmaceuticals, 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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Publication number Priority date Publication date Assignee Title
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
ZA201406709B (en) 2016-07-27
PH12014502048B1 (en) 2020-10-28
NZ628421A (en) 2016-04-29
KR20200034818A (ko) 2020-03-31
US20130245029A1 (en) 2013-09-19
CN107137402A (zh) 2017-09-08
ES2677908T3 (es) 2018-08-07
MY182650A (en) 2021-01-27
AU2013203156A1 (en) 2013-10-03
BR112014022697A2 (pt) 2020-06-30
IL274318A (en) 2020-06-30
EA028434B1 (ru) 2017-11-30
PH12014502048A1 (en) 2014-12-10
PH12018502234B1 (en) 2021-07-23
AU2013203156B2 (en) 2015-12-10
IL234640A0 (en) 2014-11-30
KR20140138929A (ko) 2014-12-04
WO2013138556A1 (en) 2013-09-19
NI201400109A (es) 2015-01-15
KR20190058673A (ko) 2019-05-29
MX2014011117A (es) 2015-04-08
HK1201755A1 (en) 2015-09-11
JP2018065820A (ja) 2018-04-26
PH12018502234A1 (en) 2019-08-14
CN104302295B (zh) 2017-06-20
KR102057358B1 (ko) 2019-12-18
EA201491694A1 (ru) 2015-06-30
EP2825168A1 (en) 2015-01-21
EP2825168B1 (en) 2018-05-09
JP6470821B2 (ja) 2019-02-13
SG11201405706TA (en) 2014-10-30
TWI600428B (zh) 2017-10-01
TW201343167A (zh) 2013-11-01
CN104302295A (zh) 2015-01-21
CA2867349A1 (en) 2013-09-19
AU2013203156C1 (en) 2016-02-18
MX360877B (es) 2018-11-21
TW201733586A (zh) 2017-10-01
IL234640B (en) 2020-05-31
JP2015516375A (ja) 2015-06-11

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