BR112014022700A2 - uso de uma quantidade eficaz de um inibidor da quinase tor, método para melhorar o critério do grupo de trabalho 2 do antígeno prostático específico (psawg2), método para a inibição da fosforilação de s6rp, 4e-bp1 e/ou de akt, método para a inibição da atividade da proteína quinase dependente do dna (dna-pk), método para a medição da inibição da fosforilação de s6rp, 4e-bp1 ou akt, método para a medição da inibição da fosforilação de dna-pk s2056 e kit - Google Patents

uso de uma quantidade eficaz de um inibidor da quinase tor, método para melhorar o critério do grupo de trabalho 2 do antígeno prostático específico (psawg2), método para a inibição da fosforilação de s6rp, 4e-bp1 e/ou de akt, método para a inibição da atividade da proteína quinase dependente do dna (dna-pk), método para a medição da inibição da fosforilação de s6rp, 4e-bp1 ou akt, método para a medição da inibição da fosforilação de dna-pk s2056 e kit Download PDF

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Publication number
BR112014022700A2
BR112014022700A2 BR112014022700-4A BR112014022700A BR112014022700A2 BR 112014022700 A2 BR112014022700 A2 BR 112014022700A2 BR 112014022700 A BR112014022700 A BR 112014022700A BR 112014022700 A2 BR112014022700 A2 BR 112014022700A2
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BR
Brazil
Prior art keywords
substituted
pyrazin
unsubstituted
tor kinase
methyl
Prior art date
Application number
BR112014022700-4A
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English (en)
Portuguese (pt)
Inventor
Shuichan Xu
Kristen Mae Hege
Heather Raymon
Toshiya Tsuji
Lisa Sapinoso
Original Assignee
Signal Pharmaceuticals, Llc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Signal Pharmaceuticals, Llc filed Critical Signal Pharmaceuticals, Llc
Publication of BR112014022700A2 publication Critical patent/BR112014022700A2/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed 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
    • A61K31/4985Pyrazines 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/502Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • 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
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12QMEASURING 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
    • C12Q1/00Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
    • 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
    • G01N33/57434Specifically defined cancers of prostate
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00Detection or diagnosis of diseases
    • G01N2800/52Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00Detection or diagnosis of diseases
    • G01N2800/56Staging 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)
  • Urology & Nephrology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biotechnology (AREA)
  • Zoology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Analytical Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Hematology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Oncology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Cell Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Food Science & Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
BR112014022700-4A 2012-03-15 2013-03-14 uso de uma quantidade eficaz de um inibidor da quinase tor, método para melhorar o critério do grupo de trabalho 2 do antígeno prostático específico (psawg2), método para a inibição da fosforilação de s6rp, 4e-bp1 e/ou de akt, método para a inibição da atividade da proteína quinase dependente do dna (dna-pk), método para a medição da inibição da fosforilação de s6rp, 4e-bp1 ou akt, método para a medição da inibição da fosforilação de dna-pk s2056 e kit BR112014022700A2 (pt)

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
PCT/US2013/031217 WO2013138560A1 (en) 2012-03-15 2013-03-14 Treatment of cancer with tor kinase inhibitors

Publications (1)

Publication Number Publication Date
BR112014022700A2 true BR112014022700A2 (pt) 2020-06-30

Family

ID=48045717

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112014022700-4A BR112014022700A2 (pt) 2012-03-15 2013-03-14 uso de uma quantidade eficaz de um inibidor da quinase tor, método para melhorar o critério do grupo de trabalho 2 do antígeno prostático específico (psawg2), método para a inibição da fosforilação de s6rp, 4e-bp1 e/ou de akt, método para a inibição da atividade da proteína quinase dependente do dna (dna-pk), método para a medição da inibição da fosforilação de s6rp, 4e-bp1 ou akt, método para a medição da inibição da fosforilação de dna-pk s2056 e kit

Country Status (21)

Country Link
US (1) US20130245028A1 (enExample)
EP (1) EP2825171B1 (enExample)
JP (2) JP2015511964A (enExample)
KR (1) KR102057357B1 (enExample)
CN (2) CN104271138A (enExample)
AU (2) AU2013202992B2 (enExample)
BR (1) BR112014022700A2 (enExample)
CA (1) CA2867174C (enExample)
EA (1) EA028062B1 (enExample)
ES (1) ES2668279T3 (enExample)
IL (1) IL234639B (enExample)
MX (1) MX359227B (enExample)
MY (1) MY198666A (enExample)
NI (1) NI201400110A (enExample)
NZ (1) NZ628420A (enExample)
PH (1) PH12014502047A1 (enExample)
SG (1) SG11201405686PA (enExample)
TW (1) TWI622395B (enExample)
UA (1) UA114194C2 (enExample)
WO (1) WO2013138560A1 (enExample)
ZA (1) ZA201406708B (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
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
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
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
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
KR102221029B1 (ko) 2013-04-17 2021-02-26 시그날 파마소티칼 엘엘씨 디하이드로피라지노-피라진을 사용한 암의 치료
NZ631082A (en) 2013-04-17 2017-06-30 Signal Pharm Llc Methods for treating cancer using tor kinase inhibitor combination therapy
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
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
CA2955009A1 (en) 2014-07-14 2016-01-21 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
JP2018519308A (ja) * 2015-06-24 2018-07-19 セルジーン コーポレイション Dnapk阻害剤でのがんの治療
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
IL271491B2 (en) 2017-06-22 2023-09-01 Celgene Corp Treatment of carcinoma of the liver characterized by hepatitis b virus infection

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Also Published As

Publication number Publication date
US20130245028A1 (en) 2013-09-19
HK1202247A1 (en) 2015-09-25
MX359227B (es) 2018-09-20
JP2018058861A (ja) 2018-04-12
NZ628420A (en) 2016-04-29
PH12014502047B1 (en) 2014-12-10
AU2015213353B2 (en) 2017-07-27
EA028062B1 (ru) 2017-10-31
EP2825171B1 (en) 2018-03-14
MY198666A (en) 2023-09-14
AU2013202992B2 (en) 2015-09-03
AU2013202992A1 (en) 2013-10-03
EA201491701A1 (ru) 2015-01-30
IL234639B (en) 2020-05-31
NI201400110A (es) 2015-01-12
ZA201406708B (en) 2016-05-25
MX2014011116A (es) 2015-04-08
CA2867174C (en) 2020-06-23
JP2015511964A (ja) 2015-04-23
ES2668279T3 (es) 2018-05-17
UA114194C2 (uk) 2017-05-10
CA2867174A1 (en) 2013-09-19
CN109846884A (zh) 2019-06-07
WO2013138560A1 (en) 2013-09-19
JP6470822B2 (ja) 2019-02-13
AU2015213353A1 (en) 2015-09-03
EP2825171A1 (en) 2015-01-21
TW201343166A (zh) 2013-11-01
TWI622395B (zh) 2018-05-01
KR102057357B1 (ko) 2019-12-18
PH12014502047A1 (en) 2014-12-10
CN104271138A (zh) 2015-01-07
IL234639A0 (en) 2014-11-30
KR20140138928A (ko) 2014-12-04
SG11201405686PA (en) 2014-10-30

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 8A ANUIDADE.

B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements
B350 Update of information on the portal [chapter 15.35 patent gazette]