CN108992446A - 用tor激酶抑制剂治疗癌症 - Google Patents

用tor激酶抑制剂治疗癌症 Download PDF

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Publication number
CN108992446A
CN108992446A CN201811057528.7A CN201811057528A CN108992446A CN 108992446 A CN108992446 A CN 108992446A CN 201811057528 A CN201811057528 A CN 201811057528A CN 108992446 A CN108992446 A CN 108992446A
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CN
China
Prior art keywords
base
pyrazine
substituted
unsubstituted
methyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
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CN201811057528.7A
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English (en)
Chinese (zh)
Inventor
徐水蟾
克里斯汀·梅·海格
希瑟·雷蒙
黄宝梨
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Signal Pharmaceuticals LLC
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Signal Pharmaceuticals LLC
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Application filed by Signal Pharmaceuticals LLC filed Critical Signal Pharmaceuticals LLC
Publication of CN108992446A publication Critical patent/CN108992446A/zh
Pending legal-status Critical Current

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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
    • 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

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201811057528.7A 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症 Pending CN108992446A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261611361P 2012-03-15 2012-03-15
US61/611,361 2012-03-15
US201261715323P 2012-10-18 2012-10-18
US61/715,323 2012-10-18
CN201380024859.XA CN104519885A (zh) 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201380024859.XA Division CN104519885A (zh) 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症

Publications (1)

Publication Number Publication Date
CN108992446A true CN108992446A (zh) 2018-12-14

Family

ID=48014336

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201380024859.XA Pending CN104519885A (zh) 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症
CN201811057528.7A Pending CN108992446A (zh) 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CN201380024859.XA Pending CN104519885A (zh) 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症

Country Status (21)

Country Link
US (1) US20130245026A1 (enExample)
EP (1) EP2825170B1 (enExample)
JP (3) JP2015510891A (enExample)
KR (3) KR20200070416A (enExample)
CN (2) CN104519885A (enExample)
AU (1) AU2013203153B2 (enExample)
BR (1) BR112014022703A2 (enExample)
CA (1) CA2866872A1 (enExample)
EA (1) EA028414B1 (enExample)
ES (1) ES2677874T3 (enExample)
IL (1) IL234602B (enExample)
MX (1) MX360878B (enExample)
MY (1) MY174022A (enExample)
NI (1) NI201400111A (enExample)
NZ (1) NZ628416A (enExample)
PH (1) PH12014502029A1 (enExample)
SG (1) SG11201405707XA (enExample)
TW (1) TWI583385B (enExample)
UA (1) UA114315C2 (enExample)
WO (1) WO2013138557A1 (enExample)
ZA (1) ZA201406706B (enExample)

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CN104519885A (zh) * 2012-03-15 2015-04-15 西格诺药品有限公司 用tor激酶抑制剂治疗癌症
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
US9358232B2 (en) 2013-04-17 2016-06-07 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy
KR102221029B1 (ko) 2013-04-17 2021-02-26 시그날 파마소티칼 엘엘씨 디하이드로피라지노-피라진을 사용한 암의 치료
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
US20140314673A1 (en) * 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
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
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
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
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
WO2015160868A1 (en) 2014-04-16 2015-10-22 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
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
IL271491B2 (en) 2017-06-22 2023-09-01 Celgene Corp Treatment of carcinoma of the liver characterized by hepatitis b virus infection

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101573360A (zh) * 2006-10-19 2009-11-04 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
WO2010022243A1 (en) * 2008-08-20 2010-02-25 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Chemoprevention of head and neck squamous cell carcinomas
CN102245611A (zh) * 2008-10-27 2011-11-16 西格诺药品有限公司 用于与 mTOR/PI3K/AKT/途径相关的肿瘤适应症和疾病的 mTOR激酶抑制剂

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101679432B (zh) 2006-10-19 2015-04-22 西格诺药品有限公司 杂芳基化合物、其组合物及其作为蛋白激酶抑制剂的用途
NZ599549A (en) 2009-10-26 2013-11-29 Signal Pharm Llc Methods of synthesis and purification of heteroaryl compounds
US20120028972A1 (en) * 2010-07-30 2012-02-02 Lilly Wong Biomarker assays for detecting or measuring inhibition of tor kinase activity
CN104519885A (zh) * 2012-03-15 2015-04-15 西格诺药品有限公司 用tor激酶抑制剂治疗癌症

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101573360A (zh) * 2006-10-19 2009-11-04 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
WO2010022243A1 (en) * 2008-08-20 2010-02-25 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Chemoprevention of head and neck squamous cell carcinomas
CN102245611A (zh) * 2008-10-27 2011-11-16 西格诺药品有限公司 用于与 mTOR/PI3K/AKT/途径相关的肿瘤适应症和疾病的 mTOR激酶抑制剂

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
AMORNPHIMOLTHAM, P.ET AL,: ""A Retroinhibition Approach Reveals a Tumor Cell-Autonomous Response to Rapamycin in Head and Neck Cancer"", 《CANCER RESEARCH》 *
BERK, L. ET AL: "Analysis of the pharmacodynamic activity of the mTOR inhibitor ridaforolimus (AP23573, MK-8669) in a phase 1 clinical trial", 《CANCER CHEMOTHERAPY AND PHARMACOLOGY》 *
CHANG,K.-Y. ET.AL: ""Novel Phosphoinositide 3-Kinase/mTOR Dual Inhibitor, NVP-BGT226, Displays Potent Growth-Inhibitory Activity against Human Head and Neck Cancer Cells In Vitro and In Vivo"", 《CLINICAL CANCER RESEARCH》 *

Also Published As

Publication number Publication date
MX360878B (es) 2018-11-21
CA2866872A1 (en) 2013-09-19
IL234602A0 (en) 2014-11-30
WO2013138557A1 (en) 2013-09-19
PH12014502029B1 (en) 2014-11-24
EP2825170B1 (en) 2018-05-09
ZA201406706B (en) 2016-05-25
KR20140138927A (ko) 2014-12-04
AU2013203153A1 (en) 2013-10-03
IL234602B (en) 2020-05-31
TW201343168A (zh) 2013-11-01
NI201400111A (es) 2015-01-15
KR102122617B1 (ko) 2020-06-12
TWI583385B (zh) 2017-05-21
MY174022A (en) 2020-03-04
SG11201405707XA (en) 2014-10-30
UA114315C2 (uk) 2017-05-25
EA028414B1 (ru) 2017-11-30
AU2013203153B2 (en) 2015-09-03
KR20200070416A (ko) 2020-06-17
EP2825170A1 (en) 2015-01-21
JP2015510891A (ja) 2015-04-13
CN104519885A (zh) 2015-04-15
JP2019108368A (ja) 2019-07-04
MX2014011077A (es) 2014-10-14
PH12014502029A1 (en) 2014-11-24
HK1201750A1 (en) 2015-09-11
ES2677874T3 (es) 2018-08-07
EA201491699A1 (ru) 2015-02-27
KR20210071101A (ko) 2021-06-15
BR112014022703A2 (pt) 2021-05-04
NZ628416A (en) 2016-04-29
US20130245026A1 (en) 2013-09-19
JP2021102637A (ja) 2021-07-15

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