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)
Other versions
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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    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/505Pyrimidines; 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
    • G01N33/575Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57557Immunoassay; Biospecific binding assay; Materials therefor for cancer of other specific parts of the body, e.g. brain

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  • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Food Science & Technology (AREA)
  • Cell Biology (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (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)
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 (enExample)
EP (1) EP2825168B1 (enExample)
JP (2) JP2015516375A (enExample)
KR (3) KR20190058673A (enExample)
CN (2) CN107137402A (enExample)
AU (1) AU2013203156C1 (enExample)
BR (1) BR112014022697A2 (enExample)
CA (1) CA2867349A1 (enExample)
EA (1) EA028434B1 (enExample)
ES (1) ES2677908T3 (enExample)
IL (2) IL234640B (enExample)
MX (1) MX360877B (enExample)
MY (1) MY182650A (enExample)
NI (1) NI201400109A (enExample)
NZ (1) NZ628421A (enExample)
PH (2) PH12014502048B1 (enExample)
SG (1) SG11201405706TA (enExample)
TW (2) TWI600428B (enExample)
WO (1) WO2013138556A1 (enExample)
ZA (1) ZA201406709B (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
MX2015009209A (es) 2013-01-16 2016-03-17 Signal Pharm Llc Compuestos sustituidos de pirrolopirimidina, composiciones de los mismos, y metodos de tratamiento con los mismos.
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
MX368286B (es) 2013-04-17 2019-09-27 Signal Pharm Llc Terapia de combinacion que comprende un inhibidor de tor cinasa y un compuesto de quinazolinona 5-sustituida para tratar cancer.
CA2908353C (en) 2013-04-17 2021-11-02 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
AU2014254059B2 (en) 2013-04-17 2019-06-06 Signal Pharmaceuticals, Llc Combination therapy comprising a TOR kinase inhibitor and a cytidine analog for treating cancer
CA2908957C (en) 2013-04-17 2021-05-18 Signal Pharmaceuticals, Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
US9505764B2 (en) 2013-04-17 2016-11-29 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
EA030726B1 (ru) 2013-04-17 2018-09-28 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
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
JP2017511367A (ja) 2014-04-16 2017-04-20 シグナル ファーマシューティカルズ,エルエルシー 1−エチル−7−(2−メチル−6−(1H−1,2,4−トリアゾール−3−イル)ピリジン−3−イル)−3,4−ジヒドロピラジノ[2,3−b]ピラジン−2(1H)−オン及び共形成物を含む固体形態、その組成物及び使用方法
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
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
EP3131552B1 (en) 2014-04-16 2020-07-15 Signal Pharmaceuticals, LLC Methods for treating cancer using tor kinase inhibitor combination therapy
EA201790189A1 (ru) 2014-07-14 2017-11-30 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Способы лечения злокачественного новообразования с использованием замещенных пирролопиримидиновых соединений, композиции на их основе
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
PE20191474A1 (es) 2016-12-20 2019-10-16 Astrazeneca Ab Compuestos de amino-triazolopiridina y su uso en el tratamiento del cancer
ES2959860T3 (es) 2017-06-22 2024-02-28 Celgene Corp Tratamiento del carcinoma hepatocelular caracterizado por la infección por el virus de la hepatitis B
EP3759545B1 (en) * 2018-03-01 2023-12-20 Essilor International Lens element
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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ES2383370T3 (es) 2006-10-19 2012-06-20 Signal Pharmaceuticals Llc Compuestos de heteroarilo, sus composiciones y uso de los mismos como inhibidores de proteína quinasa
US7981893B2 (en) * 2006-10-19 2011-07-19 Signal Pharmaceuticals, Llc Heteroaryl compounds, compositions thereof, and methods of treatment therewith
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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
CN104302295A (zh) 2015-01-21
IL234640A0 (en) 2014-11-30
CA2867349A1 (en) 2013-09-19
PH12014502048A1 (en) 2014-12-10
BR112014022697A2 (pt) 2020-06-30
JP6470821B2 (ja) 2019-02-13
EA201491694A1 (ru) 2015-06-30
PH12018502234B1 (en) 2021-07-23
EP2825168B1 (en) 2018-05-09
JP2018065820A (ja) 2018-04-26
NZ628421A (en) 2016-04-29
HK1201755A1 (en) 2015-09-11
ZA201406709B (en) 2016-07-27
AU2013203156A1 (en) 2013-10-03
IL234640B (en) 2020-05-31
NI201400109A (es) 2015-01-15
AU2013203156B2 (en) 2015-12-10
CN104302295B (zh) 2017-06-20
MY182650A (en) 2021-01-27
MX360877B (es) 2018-11-21
KR102057358B1 (ko) 2019-12-18
TW201343167A (zh) 2013-11-01
JP2015516375A (ja) 2015-06-11
KR20200034818A (ko) 2020-03-31
MX2014011117A (es) 2015-04-08
TW201733586A (zh) 2017-10-01
CN107137402A (zh) 2017-09-08
TWI664968B (zh) 2019-07-11
IL274318A (en) 2020-06-30
KR20190058673A (ko) 2019-05-29
US20130245029A1 (en) 2013-09-19
EP2825168A1 (en) 2015-01-21
EA028434B1 (ru) 2017-11-30
AU2013203156C1 (en) 2016-02-18
PH12014502048B1 (en) 2020-10-28
SG11201405706TA (en) 2014-10-30
WO2013138556A1 (en) 2013-09-19
PH12018502234A1 (en) 2019-08-14
ES2677908T3 (es) 2018-08-07
KR20140138929A (ko) 2014-12-04

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