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
Application number
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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Publication date
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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Classifications

    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (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)
  • 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
CN201811057528.7A Pending CN108992446A (zh) 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症
CN201380024859.XA Pending CN104519885A (zh) 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症

Family Applications After (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) CN108992446A (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) PH12014502029B1 (enExample)
SG (1) SG11201405707XA (enExample)
TW (1) TWI583385B (enExample)
UA (1) UA114315C2 (enExample)
WO (1) WO2013138557A1 (enExample)
ZA (1) ZA201406706B (enExample)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2825170B1 (en) * 2012-03-15 2018-05-09 Signal Pharmaceuticals, LLC Treatment of cancer with tor kinase inhibitors
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
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
US20140314673A1 (en) * 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
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
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
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.
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
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
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
WO2015160868A1 (en) 2014-04-16 2015-10-22 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
MY198676A (en) 2017-06-22 2023-09-15 Celgene Corp Treatment of hepatocellular carcinoma 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

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA200902384B (en) 2006-10-19 2010-07-28 Signal Pharm Llc Heteroaryl compounds, compositions thereof, and use thereof as protein kinase inhibitors
CA2778615C (en) 2009-10-26 2019-04-23 Signal Pharmaceuticals, 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
EP2825170B1 (en) * 2012-03-15 2018-05-09 Signal Pharmaceuticals, LLC Treatment of cancer with tor kinase inhibitors

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

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