RU2012141590A - Соединения для лечения рака - Google Patents
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- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
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- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D277/24—Radicals substituted by oxygen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D277/28—Radicals substituted by nitrogen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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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
- C07D417/02—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 two hetero rings
- C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Abstract
1. Соединение, представленное структурой формулы (II):гдеВ представляет собой-(имидазол);R, R, R, R, Rи Rнезависимо представляют собой атом водорода, O-алкил, O-галогеналкил, F, Cl, Br, I, галогеналкил, CF, CN, -CHCN, NH, гидроксил, -(СН)NHCH, -(CH)NH, -(CH)N(CH), -ОС(O)CF, C-Cлинейный или разветвленный алкил, галогеналкил, алкиламино, аминоалкил, -OCHPh, -NHCO-алкил, СООН, -C(O)Ph, C(O)O-алкил, С(O)Н, -C(O)NHили NO;Rи Rнезависимо представляют собой атом водорода, O-алкил, O-галогеналкил, F, Cl, Br, I, галогеналкил, CF, CN, -CHCN, NH, гидроксил, -(CH)NHCH, -(CH)NH, -(CH)N(CH), -ОС(O)CF, C-Cлинейный или разветвленный алкил, галогеналкил, алкиламино, аминоалкил, -OCHPh, -NHCO-алкил, СООН, -C(O)Ph, С(O)O-алкил, С(O)Н, -C(O)NHили NO;Х представляет собой связь, C-Cуглеводород или О;Y представляет собой связь, -С=О, -C=S, -C=N-NH, -C=N-OH, -СН-ОН, -С=СН-CN; -C=N-CN, -СН=СН-, -С=С(СН), -C=N-OMe, -(C=O)-NH, -NH-(C=O), -(C=O)-O, -O-(С=O), -(CH)-(C=O), (C=O)-(CH), -(SO)-NH-, -NH-(SO)-, SO, SO или S;i представляет собой целое число от 0 до 5;1 представляет собой целое число от 1 до 2;n представляет собой целое число от 1 до 3; иm представляет собой целое число от 1 до 3;2. Соединение по п.1, где указанное соединение представлено структурой формулы V:где R, R, R, n и В соответствуют определениям по п.1.3. Соединение по п.1, где указанное соединение представлено структурой формулы (XVI):где Rи Rнезависимо представляют собой Н, O-алкил, I, Br, Cl, F, алкил, галогеналкил, аминоалкил, -(СН)NHCH, -(CH)NH, -(CH)N(CH), OCHPh, ОН, CN, NO, -NHCO-алкил, COOH, С(O)O-алкил или С(O)Н;Rпредставляет собой I, Br, Cl или F;i представляет собой целое число от 0 до 5; иn равно 1-4.4. Соединение по п.3, где указанный Rпредставляет собой F.5. Соединение по п.3, где указанный Rпредставляет собой Cl.6. Соединение по п.3, где указанный Rпредставляет собой Cl.7. Соединение по п.3, где указанный Rпредставляет собой ОСН.8. Соеди
Claims (24)
1. Соединение, представленное структурой формулы (II):
где
В представляет собой
R1, R2, R3, R4, R5 и R6 независимо представляют собой атом водорода, O-алкил, O-галогеналкил, F, Cl, Br, I, галогеналкил, CF3, CN, -CH2CN, NH2, гидроксил, -(СН2)iNHCH3, -(CH2)iNH2, -(CH2)iN(CH3)2, -ОС(O)CF3, C1-C5 линейный или разветвленный алкил, галогеналкил, алкиламино, аминоалкил, -OCH2Ph, -NHCO-алкил, СООН, -C(O)Ph, C(O)O-алкил, С(O)Н, -C(O)NH2 или NO2;
R10 и R11 независимо представляют собой атом водорода, O-алкил, O-галогеналкил, F, Cl, Br, I, галогеналкил, CF3, CN, -CH2CN, NH2, гидроксил, -(CH2)iNHCH3, -(CH2)iNH2, -(CH2)iN(CH3)2, -ОС(O)CF3, C1-C5 линейный или разветвленный алкил, галогеналкил, алкиламино, аминоалкил, -OCH2Ph, -NHCO-алкил, СООН, -C(O)Ph, С(O)O-алкил, С(O)Н, -C(O)NH2 или NO2;
Х представляет собой связь, C1-C5 углеводород или О;
Y представляет собой связь, -С=О, -C=S, -C=N-NH2, -C=N-OH, -СН-ОН, -С=СН-CN; -C=N-CN, -СН=СН-, -С=С(СН3)2, -C=N-OMe, -(C=O)-NH, -NH-(C=O), -(C=O)-O, -O-(С=O), -(CH2)1-5-(C=O), (C=O)-(CH2)1-5, -(SO2)-NH-, -NH-(SO2)-, SO2, SO или S;
i представляет собой целое число от 0 до 5;
1 представляет собой целое число от 1 до 2;
n представляет собой целое число от 1 до 3; и
m представляет собой целое число от 1 до 3;
3. Соединение по п.1, где указанное соединение представлено структурой формулы (XVI):
где R4 и R5 независимо представляют собой Н, O-алкил, I, Br, Cl, F, алкил, галогеналкил, аминоалкил, -(СН2)iNHCH3, -(CH2)iNH2, -(CH2)iN(CH3)2, OCH2Ph, ОН, CN, NO2, -NHCO-алкил, COOH, С(O)O-алкил или С(O)Н;
R3 представляет собой I, Br, Cl или F;
i представляет собой целое число от 0 до 5; и
n равно 1-4.
4. Соединение по п.3, где указанный R3 представляет собой F.
5. Соединение по п.3, где указанный R3 представляет собой Cl.
6. Соединение по п.3, где указанный R4 представляет собой Cl.
7. Соединение по п.3, где указанный R4 представляет собой ОСН3.
8. Соединение по п.3, где указанный R5 представляет собой атом водорода.
13. Соединение по любому из пп.1-12 или его изомер, фармацевтически приемлемая соль, фармацевтический продукт, таутомер, гидрат, N-оксид или их комбинации.
14. Фармацевтическая композиция, содержащая соединение по п.13 и фармацевтически приемлемый носитель.
15. Способ лечения, подавления, уменьшения тяжести, снижения риска или ингибирования рака, включающий введение соединения по п.13 субъекту, страдающему от рака, в условиях, обеспечивающих эффективное лечение рака.
16. Способ по п.15, в котором указанный рак выбран из группы, состоящей из рака предстательной железы, рака груди, рака яичника, рака кожи, меланомы, рака легких, рака толстой кишки, лейкемии, рака почки, рака ЦНС и их комбинаций.
17. Способ по п.16, в котором указанный рак представляет собой меланому или метастатическую меланому.
18. Способ по п.16, в котором указанный рак представляет собой рак предстательной железы или рак яичника.
19. Способ по п.15, в котором указанное введение осуществляется в комбинации с другим типом противораковой терапии.
20. Способ лечения лекарственно-устойчивой опухоли или опухолей, включающий введение соединения по п.13 субъекту, страдающему от рака, в условиях, обеспечивающих эффективное лечение лекарственно-устойчивой опухоли или опухолей.
21. Способ по п.20, в котором указанная опухоль представляет собой раковую опухоль при меланоме или опухоль при метастатической меланоме.
22. Способ по п.20, в котором указанная опухоль представляет собой опухоль при раке предстательной железы или опухоль при раке яичника.
23. Способ по п.20, в котором указанное введение осуществляется в комбинации с альтернативными типами терапии рака.
24. Способ разрушения раковой клетки, включающий получение соединения по п.13 и контактирование раковой клетки с данным соединением в условиях, обеспечивающих эффективное уничтожение раковой клетки.
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US30936010P | 2010-03-01 | 2010-03-01 | |
US61/309,360 | 2010-03-01 | ||
US31579010P | 2010-03-19 | 2010-03-19 | |
US61/315,790 | 2010-03-19 | ||
US37667510P | 2010-08-24 | 2010-08-24 | |
US61/376,675 | 2010-08-24 | ||
PCT/US2010/062418 WO2011109059A1 (en) | 2010-03-01 | 2010-12-29 | Compounds for treatment of cancer |
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RU2012141590A true RU2012141590A (ru) | 2014-04-10 |
RU2581367C2 RU2581367C2 (ru) | 2016-04-20 |
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RU2012141590/04A RU2581367C2 (ru) | 2010-03-01 | 2010-12-29 | Соединения для лечения рака |
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US (1) | US9334242B2 (ru) |
EP (2) | EP2542081A4 (ru) |
JP (1) | JP5879273B2 (ru) |
KR (2) | KR20120130777A (ru) |
CN (2) | CN104592205A (ru) |
AU (1) | AU2010347233B2 (ru) |
CA (1) | CA2791738C (ru) |
IL (3) | IL221710A (ru) |
MX (1) | MX2012010115A (ru) |
RU (1) | RU2581367C2 (ru) |
WO (1) | WO2011109059A1 (ru) |
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2010
- 2010-12-29 KR KR1020127025893A patent/KR20120130777A/ko active Application Filing
- 2010-12-29 JP JP2012556056A patent/JP5879273B2/ja not_active Expired - Fee Related
- 2010-12-29 CA CA2791738A patent/CA2791738C/en not_active Expired - Fee Related
- 2010-12-29 RU RU2012141590/04A patent/RU2581367C2/ru active
- 2010-12-29 CN CN201410729973.9A patent/CN104592205A/zh active Pending
- 2010-12-29 AU AU2010347233A patent/AU2010347233B2/en not_active Ceased
- 2010-12-29 EP EP10847161.6A patent/EP2542081A4/en not_active Withdrawn
- 2010-12-29 CN CN201080066561.1A patent/CN102883607B/zh not_active Expired - Fee Related
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- 2010-12-29 WO PCT/US2010/062418 patent/WO2011109059A1/en active Application Filing
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Also Published As
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CN104592205A (zh) | 2015-05-06 |
KR20180038079A (ko) | 2018-04-13 |
IL261852A (en) | 2018-10-31 |
IL239672A0 (en) | 2015-08-31 |
EP3064204A1 (en) | 2016-09-07 |
CA2791738C (en) | 2020-06-09 |
US9334242B2 (en) | 2016-05-10 |
AU2010347233B2 (en) | 2015-06-18 |
KR20120130777A (ko) | 2012-12-03 |
EP2542081A4 (en) | 2013-07-31 |
MX2012010115A (es) | 2013-02-26 |
WO2011109059A1 (en) | 2011-09-09 |
CN102883607B (zh) | 2015-07-22 |
US20110257196A1 (en) | 2011-10-20 |
IL221710A (en) | 2015-06-30 |
CN102883607A (zh) | 2013-01-16 |
JP5879273B2 (ja) | 2016-03-08 |
KR101939704B1 (ko) | 2019-01-17 |
RU2581367C2 (ru) | 2016-04-20 |
EP2542081A1 (en) | 2013-01-09 |
IL261852B (en) | 2020-09-30 |
AU2010347233A1 (en) | 2012-09-27 |
JP2013521281A (ja) | 2013-06-10 |
CA2791738A1 (en) | 2011-09-09 |
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