TWI622395B - 使用ｔｏｒ之激酶抑制劑之癌症治療 - Google Patents
使用ｔｏｒ之激酶抑制劑之癌症治療 Download PDFInfo
- Publication number
- TWI622395B TWI622395B TW102109152A TW102109152A TWI622395B TW I622395 B TWI622395 B TW I622395B TW 102109152 A TW102109152 A TW 102109152A TW 102109152 A TW102109152 A TW 102109152A TW I622395 B TWI622395 B TW I622395B
- Authority
- TW
- Taiwan
- Prior art keywords
- substituted
- unsubstituted
- methyl
- pyrazine
- dihydropyrazino
- Prior art date
Links
Classifications
-
- 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
-
- 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
- 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
-
- 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
Landscapes
- 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)
Applications Claiming Priority (4)
| 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW201343166A TW201343166A (zh) | 2013-11-01 |
| TWI622395B true TWI622395B (zh) | 2018-05-01 |
Family
ID=48045717
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW102109152A TWI622395B (zh) | 2012-03-15 | 2013-03-14 | 使用ｔｏｒ之激酶抑制劑之癌症治療 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US20130245028A1 (enExample) |
| EP (1) | EP2825171B1 (enExample) |
| JP (2) | JP2015511964A (enExample) |
| KR (1) | KR102057357B1 (enExample) |
| CN (2) | CN109846884A (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) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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. |
| 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 |
| 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 |
| 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 |
| CA2908353C (en) | 2013-04-17 | 2021-11-02 | Signal Pharmaceuticals, Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| 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 |
| 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. |
| 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 |
| 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 |
| 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 |
| 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 |
| WO2016210046A1 (en) * | 2015-06-24 | 2016-12-29 | 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 |
| 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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| EP2299474B1 (en) * | 2008-07-10 | 2013-01-23 | JX Nippon Mining & Metals Corporation | Hybrid silicon wafer and method for manufacturing same |
| 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 |
| EP2349984A1 (en) * | 2008-10-17 | 2011-08-03 | Merck & Co. | Combination therapy |
| JP2012509058A (ja) * | 2008-11-20 | 2012-04-19 | オンコセラピー・サイエンス株式会社 | 前立腺癌を診断または治療するための方法 |
| EP2430013B1 (en) * | 2009-05-13 | 2014-10-15 | Amgen Inc. | Heteroaryl compounds as pikk inhibitors |
| NZ618135A (en) | 2009-10-26 | 2015-05-29 | Signal Pharm Llc | Methods of synthesis and purification of heteroaryl compounds |
| AR078793A1 (es) * | 2009-10-27 | 2011-12-07 | Orion Corp | Derivados de carboxamidas no esteroidales y acil hidrazona moduladores de receptores androgenicos de tejido selectivo (sarm), composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer de prostata entre otros |
-
2013
- 2013-03-14 MY MYPI2014702599A patent/MY198666A/en unknown
- 2013-03-14 EA EA201491701A patent/EA028062B1/ru not_active IP Right Cessation
- 2013-03-14 MX MX2014011116A patent/MX359227B/es active IP Right Grant
- 2013-03-14 KR KR1020147028708A patent/KR102057357B1/ko active Active
- 2013-03-14 EP EP13714092.7A patent/EP2825171B1/en active Active
- 2013-03-14 CN CN201910158858.3A patent/CN109846884A/zh active Pending
- 2013-03-14 US US13/803,317 patent/US20130245028A1/en not_active Abandoned
- 2013-03-14 JP JP2015500599A patent/JP2015511964A/ja active Pending
- 2013-03-14 AU AU2013202992A patent/AU2013202992B2/en active Active
- 2013-03-14 SG SG11201405686PA patent/SG11201405686PA/en unknown
- 2013-03-14 TW TW102109152A patent/TWI622395B/zh active
- 2013-03-14 NZ NZ628420A patent/NZ628420A/en unknown
- 2013-03-14 ES ES13714092.7T patent/ES2668279T3/es active Active
- 2013-03-14 WO PCT/US2013/031217 patent/WO2013138560A1/en not_active Ceased
- 2013-03-14 BR BR112014022700-4A patent/BR112014022700A2/pt not_active Application Discontinuation
- 2013-03-14 CN CN201380024216.5A patent/CN104271138A/zh active Pending
- 2013-03-14 UA UAA201411214A patent/UA114194C2/uk unknown
- 2013-03-14 CA CA2867174A patent/CA2867174C/en active Active
-
2014
- 2014-09-12 NI NI201400110A patent/NI201400110A/es unknown
- 2014-09-12 ZA ZA2014/06708A patent/ZA201406708B/en unknown
- 2014-09-14 IL IL234639A patent/IL234639B/en active IP Right Grant
- 2014-09-15 PH PH12014502047A patent/PH12014502047A1/en unknown
-
2015
- 2015-08-13 AU AU2015213353A patent/AU2015213353B2/en active Active
-
2017
- 2017-11-13 JP JP2017218388A patent/JP6470822B2/ja active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
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