CN109846884A - 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
CN109846884A
CN109846884A CN201910158858.3A CN201910158858A CN109846884A CN 109846884 A CN109846884 A CN 109846884A CN 201910158858 A CN201910158858 A CN 201910158858A CN 109846884 A CN109846884 A CN 109846884A
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CN
China
Prior art keywords
base
pyrazine
substituted
unsubstituted
phenyl
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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CN201910158858.3A
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English (en)
Chinese (zh)
Inventor
徐水蟾
克里斯汀·梅·海格
希瑟·雷蒙
辻俊哉
利萨·萨皮诺索
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Signal Pharmaceuticals LLC
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Signal Pharmaceuticals LLC
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Publication of CN109846884A publication Critical patent/CN109846884A/zh
Pending legal-status Critical Current

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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
    • A61K31/495—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
    • 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
    • G01N33/575—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57555—Immunoassay; Biospecific binding assay; Materials therefor for cancer of the prostate
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/52—Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/56—Staging of a disease; Further complications associated with the disease

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Urology & Nephrology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Physics & Mathematics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Food Science & Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Epidemiology (AREA)
  • Cell Biology (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201910158858.3A 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症 Pending CN109846884A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261611428P 2012-03-15 2012-03-15
US61/611,428 2012-03-15
US201261715327P 2012-10-18 2012-10-18
US61/715,327 2012-10-18
CN201380024216.5A CN104271138A (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
CN201380024216.5A Division CN104271138A (zh) 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症

Publications (1)

Publication Number Publication Date
CN109846884A true CN109846884A (zh) 2019-06-07

Family

ID=48045717

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201910158858.3A Pending CN109846884A (zh) 2012-03-15 2013-03-14 用tor激酶抑制剂治疗癌症
CN201380024216.5A Pending CN104271138A (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
CN201380024216.5A Pending CN104271138A (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) US20130245028A1 (https=)
EP (1) EP2825171B1 (https=)
JP (2) JP2015511964A (https=)
KR (1) KR102057357B1 (https=)
CN (2) CN109846884A (https=)
AU (2) AU2013202992B2 (https=)
BR (1) BR112014022700A2 (https=)
CA (1) CA2867174C (https=)
EA (1) EA028062B1 (https=)
ES (1) ES2668279T3 (https=)
IL (1) IL234639B (https=)
MX (1) MX359227B (https=)
MY (1) MY198666A (https=)
NI (1) NI201400110A (https=)
NZ (1) NZ628420A (https=)
PH (1) PH12014502047B1 (https=)
SG (1) SG11201405686PA (https=)
TW (1) TWI622395B (https=)
UA (1) UA114194C2 (https=)
WO (1) WO2013138560A1 (https=)
ZA (1) ZA201406708B (https=)

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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
PE20151995A1 (es) 2013-01-16 2016-01-13 Signal Pharm Llc Compuestos sustituidos de pirrolopirimidina, composiciones de los mismos, y metodos de tratamiento con los mismos
CN105377299B (zh) 2013-04-17 2018-06-12 西格诺药品有限公司 用于治疗前列腺癌的包含二氢吡嗪并-吡嗪化合物和雄激素受体拮抗剂的组合疗法
CA2908742C (en) 2013-04-17 2021-06-01 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
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
US9505764B2 (en) 2013-04-17 2016-11-29 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
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
US9630966B2 (en) 2013-04-17 2017-04-25 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
CA2909629C (en) 2013-04-17 2022-12-13 Signal Pharmaceuticals, 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
NZ629486A (en) 2013-05-29 2017-11-24 Signal Pharm Llc Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use
US9512129B2 (en) 2014-04-16 2016-12-06 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
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
ES2823756T3 (es) 2014-04-16 2021-05-10 Signal Pharm Llc Métodos para tratar el cáncer usando terapia de combinación de inhibidores de quinasa TOR
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
US20180369241A1 (en) * 2015-06-24 2018-12-27 Celgene Corporation Treatment of cancer with dnapk inhibitors
US11318139B2 (en) 2016-01-26 2022-05-03 Dana-Farber Cancer Institute, Inc. Methods for treating brain metastases using combinations of anti-P13K and anti-mTOR agents
TWI787284B (zh) 2017-06-22 2022-12-21 美商西建公司 以b型肝炎病毒感染表徵之肝細胞癌之治療

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Also Published As

Publication number Publication date
TW201343166A (zh) 2013-11-01
ZA201406708B (en) 2016-05-25
PH12014502047A1 (en) 2014-12-10
AU2013202992B2 (en) 2015-09-03
BR112014022700A2 (pt) 2020-06-30
EP2825171B1 (en) 2018-03-14
MX359227B (es) 2018-09-20
AU2013202992A1 (en) 2013-10-03
CA2867174A1 (en) 2013-09-19
JP2018058861A (ja) 2018-04-12
SG11201405686PA (en) 2014-10-30
MX2014011116A (es) 2015-04-08
EA028062B1 (ru) 2017-10-31
IL234639A0 (en) 2014-11-30
ES2668279T3 (es) 2018-05-17
JP2015511964A (ja) 2015-04-23
MY198666A (en) 2023-09-14
NZ628420A (en) 2016-04-29
PH12014502047B1 (en) 2014-12-10
CA2867174C (en) 2020-06-23
WO2013138560A1 (en) 2013-09-19
KR102057357B1 (ko) 2019-12-18
CN104271138A (zh) 2015-01-07
NI201400110A (es) 2015-01-12
JP6470822B2 (ja) 2019-02-13
HK1202247A1 (en) 2015-09-25
TWI622395B (zh) 2018-05-01
UA114194C2 (uk) 2017-05-10
KR20140138928A (ko) 2014-12-04
EA201491701A1 (ru) 2015-01-30
US20130245028A1 (en) 2013-09-19
AU2015213353A1 (en) 2015-09-03
AU2015213353B2 (en) 2017-07-27
IL234639B (en) 2020-05-31
EP2825171A1 (en) 2015-01-21

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