EA201400595A1 - Морфолинилбензотриазины для применения в лечении рака - Google Patents
Морфолинилбензотриазины для применения в лечении ракаInfo
- Publication number
- EA201400595A1 EA201400595A1 EA201400595A EA201400595A EA201400595A1 EA 201400595 A1 EA201400595 A1 EA 201400595A1 EA 201400595 A EA201400595 A EA 201400595A EA 201400595 A EA201400595 A EA 201400595A EA 201400595 A1 EA201400595 A1 EA 201400595A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- compounds
- formula
- cancer
- relates
- morfolinylbenzotriazines
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 4
- 201000011510 cancer Diseases 0.000 title abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 6
- 239000002246 antineoplastic agent Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 206010027476 Metastases Diseases 0.000 abstract 1
- 102000009516 Protein Serine-Threonine Kinases Human genes 0.000 abstract 1
- 108010009341 Protein Serine-Threonine Kinases Proteins 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 230000033115 angiogenesis Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000005865 ionizing radiation Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 238000001959 radiotherapy Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
- A61N5/00—Radiation therapy
- A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
- C07D253/08—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/10—Compounds having one or more C—Si linkages containing nitrogen having a Si-N linkage
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pathology (AREA)
- Radiology & Medical Imaging (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Изобретение относится к соединениям формулы (I)в которой R, L и m имеют значения, указанные в формуле изобретения, и/или к их физиологически приемлемым солям, таутомерам и стереоизомерам, включая их смеси во всех соотношениях. Соединения формулы (I) могут быть применены для ингибирования серин-треонин протеинкиназ и для сенсибилизации раковых клеток к противораковым средствам и/или к ионизирующему излучению. Изобретение также относится к применению соединений формулы (I) в профилактике, лечении или контроле над прогрессированием рака, опухолей, метастазов или нарушений ангиогенеза, в комбинации с радиотерапией и/или противораковым средством. Кроме того, изобретение относится к способу получения соединений формулы (I) посредством реакции соединений формул (II) и (III) и по выбору превращения основания или кислоты соединений формулы (I) в одну из их солей.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102011118830A DE102011118830A1 (de) | 2011-11-18 | 2011-11-18 | Morpholinylbenzotriazine |
| PCT/EP2012/004542 WO2013072015A1 (de) | 2011-11-18 | 2012-10-30 | Morpholinylbenzotriazine zur anwendung in der krebstherapie |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA201400595A1 true EA201400595A1 (ru) | 2014-11-28 |
Family
ID=47143824
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201400595A EA201400595A1 (ru) | 2011-11-18 | 2012-10-30 | Морфолинилбензотриазины для применения в лечении рака |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US9187469B2 (ru) |
| EP (1) | EP2780332B1 (ru) |
| JP (1) | JP6096792B2 (ru) |
| KR (1) | KR20140097391A (ru) |
| CN (1) | CN103930408B (ru) |
| AU (1) | AU2012339196B2 (ru) |
| BR (1) | BR112014011805A2 (ru) |
| CA (1) | CA2856103C (ru) |
| DE (1) | DE102011118830A1 (ru) |
| DK (1) | DK2780332T3 (ru) |
| EA (1) | EA201400595A1 (ru) |
| ES (1) | ES2572605T3 (ru) |
| HK (1) | HK1199875A1 (ru) |
| HR (1) | HRP20160495T1 (ru) |
| HU (1) | HUE027577T2 (ru) |
| IL (1) | IL232577A (ru) |
| IN (1) | IN2014KN01287A (ru) |
| MX (1) | MX2014005838A (ru) |
| PL (1) | PL2780332T3 (ru) |
| RS (1) | RS54768B1 (ru) |
| SG (1) | SG11201402206YA (ru) |
| SI (1) | SI2780332T1 (ru) |
| WO (1) | WO2013072015A1 (ru) |
| ZA (1) | ZA201404438B (ru) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG10201704095UA (en) | 2012-04-24 | 2017-06-29 | Vertex Pharma | Dna-pk inhibitors |
| LT2970218T (lt) | 2013-03-12 | 2019-03-12 | Vertex Pharmaceuticals Incorporated | Dna-pk inhibitoriai |
| DE102013008118A1 (de) | 2013-05-11 | 2014-11-13 | Merck Patent Gmbh | Arylchinazoline |
| RU2675270C2 (ru) | 2013-10-17 | 2018-12-18 | Вертекс Фармасьютикалз Инкорпорейтед | Сокристаллы и содержащие их фармацевтические композиции |
| RU2758669C2 (ru) | 2016-09-27 | 2021-11-01 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с применением сочетания днк-поражающих агентов и ингибиторов днк-пк |
| CN107793373B (zh) * | 2017-10-31 | 2019-09-17 | 广西师范大学 | 2-取代苯并三嗪酮衍生物及其制备方法 |
| AU2019209293B2 (en) | 2018-01-17 | 2023-07-27 | Vertex Pharmaceuticals Incorporated | DNA-PK inhibitors |
| JOP20220100A1 (ar) | 2019-11-01 | 2023-01-30 | Syngenta Crop Protection Ag | مركبات هتيروماتية ثنائية الحلقة مندمجة نشطة من الناحية المبيدة للآفات |
| CA3221180A1 (en) | 2021-06-24 | 2022-12-29 | Syngenta Crop Protection Ag | 2-[3-[1 [(quinazolin-4-yl)amino]ethyl]pyrazin-2-yl]thiazole-5-carbonitrile derivatives and similar compounds as pesticides |
| WO2023247360A1 (en) | 2022-06-21 | 2023-12-28 | Syngenta Crop Protection Ag | Pesticidally active fused bicyclic heteroaromatic compounds |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR930702292A (ko) | 1990-11-06 | 1993-09-08 | 알렌 제이. 스피겔 | 종양 치료 활성을 증대시키기 위한 퀴나졸린 유도체 |
| WO2000061186A1 (en) | 1999-04-08 | 2000-10-19 | Arch Development Corporation | Use of anti-vegf antibody to enhance radiation in cancer therapy |
| US7179912B2 (en) * | 2000-09-01 | 2007-02-20 | Icos Corporation | Materials and methods to potentiate cancer treatment |
| US7291733B2 (en) * | 2003-10-10 | 2007-11-06 | Boehringer Ingelheim Pharmaceuticals, Inc. | Substituted tricyclic heterocycles and their uses |
| CN101230045B (zh) * | 2008-02-14 | 2013-04-10 | 沈阳药科大学 | 芳环并三嗪类衍生物及其应用 |
| US9126952B2 (en) * | 2010-03-16 | 2015-09-08 | Merck Patent Gmbh | Morpholinylquinazolines |
-
2011
- 2011-11-18 DE DE102011118830A patent/DE102011118830A1/de not_active Withdrawn
-
2012
- 2012-10-30 EP EP12783121.2A patent/EP2780332B1/de active Active
- 2012-10-30 SI SI201230559A patent/SI2780332T1/sl unknown
- 2012-10-30 ES ES12783121.2T patent/ES2572605T3/es active Active
- 2012-10-30 CA CA2856103A patent/CA2856103C/en active Active
- 2012-10-30 CN CN201280056504.4A patent/CN103930408B/zh active Active
- 2012-10-30 SG SG11201402206YA patent/SG11201402206YA/en unknown
- 2012-10-30 IN IN1287KON2014 patent/IN2014KN01287A/en unknown
- 2012-10-30 EA EA201400595A patent/EA201400595A1/ru unknown
- 2012-10-30 PL PL12783121T patent/PL2780332T3/pl unknown
- 2012-10-30 BR BR112014011805A patent/BR112014011805A2/pt not_active Application Discontinuation
- 2012-10-30 RS RS20160351A patent/RS54768B1/sr unknown
- 2012-10-30 AU AU2012339196A patent/AU2012339196B2/en active Active
- 2012-10-30 KR KR1020147016518A patent/KR20140097391A/ko not_active Application Discontinuation
- 2012-10-30 DK DK12783121.2T patent/DK2780332T3/en active
- 2012-10-30 HU HUE12783121A patent/HUE027577T2/en unknown
- 2012-10-30 WO PCT/EP2012/004542 patent/WO2013072015A1/de active Application Filing
- 2012-10-30 JP JP2014541555A patent/JP6096792B2/ja active Active
- 2012-10-30 US US14/351,773 patent/US9187469B2/en active Active
- 2012-10-30 MX MX2014005838A patent/MX2014005838A/es not_active Application Discontinuation
-
2014
- 2014-05-12 IL IL232577A patent/IL232577A/en active IP Right Grant
- 2014-06-17 ZA ZA2014/04438A patent/ZA201404438B/en unknown
-
2015
- 2015-01-12 HK HK15100269.7A patent/HK1199875A1/xx unknown
-
2016
- 2016-05-09 HR HRP20160495TT patent/HRP20160495T1/hr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SG11201402206YA (en) | 2014-11-27 |
| IN2014KN01287A (ru) | 2015-10-16 |
| AU2012339196A1 (en) | 2014-07-03 |
| RS54768B1 (sr) | 2016-10-31 |
| EP2780332A1 (de) | 2014-09-24 |
| DK2780332T3 (en) | 2016-05-30 |
| KR20140097391A (ko) | 2014-08-06 |
| HK1199875A1 (en) | 2015-07-24 |
| US20140275072A1 (en) | 2014-09-18 |
| MX2014005838A (es) | 2014-07-30 |
| CA2856103A1 (en) | 2013-05-23 |
| AU2012339196B2 (en) | 2017-04-27 |
| BR112014011805A2 (pt) | 2017-05-16 |
| JP6096792B2 (ja) | 2017-03-15 |
| IL232577A0 (en) | 2014-06-30 |
| CN103930408B (zh) | 2016-09-07 |
| HUE027577T2 (en) | 2016-10-28 |
| DE102011118830A1 (de) | 2013-05-23 |
| PL2780332T3 (pl) | 2016-07-29 |
| SI2780332T1 (sl) | 2016-06-30 |
| US9187469B2 (en) | 2015-11-17 |
| JP2015502926A (ja) | 2015-01-29 |
| WO2013072015A1 (de) | 2013-05-23 |
| CN103930408A (zh) | 2014-07-16 |
| CA2856103C (en) | 2020-08-25 |
| EP2780332B1 (de) | 2016-02-24 |
| ES2572605T3 (es) | 2016-06-01 |
| IL232577A (en) | 2017-05-29 |
| ZA201404438B (en) | 2015-12-23 |
| HRP20160495T1 (hr) | 2016-06-03 |
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