JP2015516375A - Torキナーゼ阻害剤を用いた癌の治療 - Google Patents
Torキナーゼ阻害剤を用いた癌の治療 Download PDFInfo
- Publication number
- JP2015516375A JP2015516375A JP2015500595A JP2015500595A JP2015516375A JP 2015516375 A JP2015516375 A JP 2015516375A JP 2015500595 A JP2015500595 A JP 2015500595A JP 2015500595 A JP2015500595 A JP 2015500595A JP 2015516375 A JP2015516375 A JP 2015516375A
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- pyrazin
- tor kinase
- kinase inhibitor
- 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
Links
- 0 *C(c1nc(N)nc2c1*C*2)=O Chemical compound *C(c1nc(N)nc2c1*C*2)=O 0.000 description 7
- MVXVYAKCVDQRLW-UHFFFAOYSA-N c1c[nH]c2c1cccn2 Chemical compound c1c[nH]c2c1cccn2 MVXVYAKCVDQRLW-UHFFFAOYSA-N 0.000 description 1
- HYZJCKYKOHLVJF-UHFFFAOYSA-N c1nc2ccccc2[nH]1 Chemical compound c1nc2ccccc2[nH]1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 description 1
Images
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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- 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
-
- 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
- G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
- G01N33/57407—Specifically defined cancers
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Cell Biology (AREA)
- Microbiology (AREA)
- Biotechnology (AREA)
- Hospice & Palliative Care (AREA)
- Food Science & Technology (AREA)
- Physics & Mathematics (AREA)
- Analytical Chemistry (AREA)
- Biochemistry (AREA)
- General Physics & Mathematics (AREA)
- Pathology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Investigating Or Analysing Biological Materials (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261611370P | 2012-03-15 | 2012-03-15 | |
| US61/611,370 | 2012-03-15 | ||
| US201261715329P | 2012-10-18 | 2012-10-18 | |
| US61/715,329 | 2012-10-18 | ||
| PCT/US2013/031202 WO2013138556A1 (en) | 2012-03-15 | 2013-03-14 | Treatment of cancer with tor kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017218364A Division JP6470821B2 (ja) | 2012-03-15 | 2017-11-13 | Torキナーゼ阻害剤を用いた癌の治療 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015516375A true JP2015516375A (ja) | 2015-06-11 |
| JP2015516375A5 JP2015516375A5 (OSRAM) | 2016-04-21 |
Family
ID=47998542
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015500595A Pending JP2015516375A (ja) | 2012-03-15 | 2013-03-14 | Torキナーゼ阻害剤を用いた癌の治療 |
| JP2017218364A Active JP6470821B2 (ja) | 2012-03-15 | 2017-11-13 | Torキナーゼ阻害剤を用いた癌の治療 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017218364A Active JP6470821B2 (ja) | 2012-03-15 | 2017-11-13 | Torキナーゼ阻害剤を用いた癌の治療 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US20130245029A1 (OSRAM) |
| EP (1) | EP2825168B1 (OSRAM) |
| JP (2) | JP2015516375A (OSRAM) |
| KR (3) | KR102057358B1 (OSRAM) |
| CN (2) | CN104302295B (OSRAM) |
| AU (1) | AU2013203156C1 (OSRAM) |
| BR (1) | BR112014022697A2 (OSRAM) |
| CA (1) | CA2867349A1 (OSRAM) |
| EA (1) | EA028434B1 (OSRAM) |
| ES (1) | ES2677908T3 (OSRAM) |
| IL (2) | IL234640B (OSRAM) |
| MX (1) | MX360877B (OSRAM) |
| MY (1) | MY182650A (OSRAM) |
| NI (1) | NI201400109A (OSRAM) |
| NZ (1) | NZ628421A (OSRAM) |
| PH (2) | PH12014502048B1 (OSRAM) |
| SG (1) | SG11201405706TA (OSRAM) |
| TW (2) | TWI600428B (OSRAM) |
| WO (1) | WO2013138556A1 (OSRAM) |
| ZA (1) | ZA201406709B (OSRAM) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20190092573A (ko) * | 2016-12-20 | 2019-08-07 | 아스트라제네카 아베 | 아미노-트리아졸로피리딘 화합물 및 암 치료에서의 이의 용도 |
Families Citing this family (19)
| 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 |
| 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 |
| KR102221029B1 (ko) | 2013-04-17 | 2021-02-26 | 시그날 파마소티칼 엘엘씨 | 디하이드로피라지노-피라진을 사용한 암의 치료 |
| 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 |
| US9358232B2 (en) | 2013-04-17 | 2016-06-07 | Signal Pharmaceuticals, Llc | Methods for treating cancer using TOR kinase inhibitor combination therapy |
| 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 |
| 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 |
| 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 |
| WO2015160882A1 (en) | 2014-04-16 | 2015-10-22 | Signal Pharmaceuticals, Llc | SOLID FORMS COMPRISING 7-(6-(2-HYDROXYPROPAN-2YL) PYRIDIN-3-YL)-1-(TRANS)-4-METHOXYCYCLOHEXYL)-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 |
| 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 |
| 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 |
| SG11202008010SA (en) * | 2018-03-01 | 2020-09-29 | Essilor Int | Lens element |
| CN113493471B (zh) * | 2020-04-03 | 2024-06-11 | 山东轩竹医药科技有限公司 | 杂芳环类激酶抑制剂 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010062571A1 (en) * | 2008-10-27 | 2010-06-03 | Signal Pharmaceuticals, Llc | Mtor kinase inhibitors for oncology indications and diseases associated with the mtor/p13k/akt pathway |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101504669B1 (ko) | 2006-10-19 | 2015-03-20 | 시그날 파마소티칼 엘엘씨 | 헤테로아릴 화합물, 이들의 조성물 그리고 단백질 키나아제 억제제로서의 이들의 용도 |
| 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 |
| WO2011133668A2 (en) * | 2010-04-20 | 2011-10-27 | President And Fellows Of Harvard College | Methods and compositions for the treatment of cancer |
-
2013
- 2013-03-14 AU AU2013203156A patent/AU2013203156C1/en not_active Ceased
- 2013-03-14 NZ NZ628421A patent/NZ628421A/en not_active IP Right Cessation
- 2013-03-14 KR KR1020147028710A patent/KR102057358B1/ko active Active
- 2013-03-14 SG SG11201405706TA patent/SG11201405706TA/en unknown
- 2013-03-14 BR BR112014022697-0A patent/BR112014022697A2/pt not_active Application Discontinuation
- 2013-03-14 KR KR1020197014135A patent/KR20190058673A/ko not_active Ceased
- 2013-03-14 US US13/803,323 patent/US20130245029A1/en not_active Abandoned
- 2013-03-14 CN CN201380025102.2A patent/CN104302295B/zh active Active
- 2013-03-14 ES ES13712647.0T patent/ES2677908T3/es active Active
- 2013-03-14 MX MX2014011117A patent/MX360877B/es active IP Right Grant
- 2013-03-14 TW TW102109153A patent/TWI600428B/zh active
- 2013-03-14 EP EP13712647.0A patent/EP2825168B1/en active Active
- 2013-03-14 WO PCT/US2013/031202 patent/WO2013138556A1/en not_active Ceased
- 2013-03-14 JP JP2015500595A patent/JP2015516375A/ja active Pending
- 2013-03-14 CA CA2867349A patent/CA2867349A1/en not_active Abandoned
- 2013-03-14 KR KR1020207008188A patent/KR20200034818A/ko not_active Ceased
- 2013-03-14 CN CN201710422322.9A patent/CN107137402A/zh active Pending
- 2013-03-14 TW TW106122809A patent/TWI664968B/zh active
- 2013-03-14 MY MYPI2014702606A patent/MY182650A/en unknown
- 2013-03-14 EA EA201491694A patent/EA028434B1/ru not_active IP Right Cessation
-
2014
- 2014-09-12 ZA ZA2014/06709A patent/ZA201406709B/en unknown
- 2014-09-12 NI NI201400109A patent/NI201400109A/es unknown
- 2014-09-14 IL IL234640A patent/IL234640B/en active IP Right Grant
- 2014-09-15 PH PH12014502048A patent/PH12014502048B1/en unknown
-
2017
- 2017-11-13 JP JP2017218364A patent/JP6470821B2/ja active Active
-
2018
- 2018-10-18 PH PH12018502234A patent/PH12018502234B1/en unknown
-
2020
- 2020-04-28 IL IL274318A patent/IL274318A/en unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010062571A1 (en) * | 2008-10-27 | 2010-06-03 | Signal Pharmaceuticals, Llc | Mtor kinase inhibitors for oncology indications and diseases associated with the mtor/p13k/akt pathway |
Non-Patent Citations (3)
| Title |
|---|
| BERK L, ET AL.: "Analysis of the pharmacodynamic activity of the mTOR inhibitor ridaforolimus (AP23573, MK-8669) in a", CANCER CHEMOTHERAPY AND PHARMACOLOGY, vol. 69, no. 5, JPN6016045332, 10 January 2012 (2012-01-10), pages 1369 - 1377, ISSN: 0003446444 * |
| MATEO-LOZANO S, ET AL.: "Combined transcriptional and translational targeting of EWS/FLI-1 in Ewing's sarcoma", CLINICAL CANCER RESEARCH, vol. 12, no. 22, JPN6016045330, 15 November 2006 (2006-11-15), pages 6781 - 6790, ISSN: 0003446443 * |
| MATEO-LOZANO S, ET AL.: "Rapamycin induces the fusion-type independent downregulation of the EWS/FLI-1 proteins and inhibits", ONCOGENE, vol. 22, no. 58, JPN6016045327, 2003, pages 9282 - 9287, ISSN: 0003446442 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20190092573A (ko) * | 2016-12-20 | 2019-08-07 | 아스트라제네카 아베 | 아미노-트리아졸로피리딘 화합물 및 암 치료에서의 이의 용도 |
| JP2020504107A (ja) * | 2016-12-20 | 2020-02-06 | アストラゼネカ・アクチエボラーグAstrazeneca Aktiebolag | アミノ−トリアゾロピリジン化合物および癌の治療におけるその使用 |
| KR102220971B1 (ko) | 2016-12-20 | 2021-02-25 | 아스트라제네카 아베 | 아미노-트리아졸로피리딘 화합물 및 암 치료에서의 이의 용도 |
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