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RU2011131985A - Толуидинсульфонамиды и их применение - Google Patents

Толуидинсульфонамиды и их применение Download PDF

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RU2011131985A
RU2011131985A RU2011131985/04A RU2011131985A RU2011131985A RU 2011131985 A RU2011131985 A RU 2011131985A RU 2011131985/04 A RU2011131985/04 A RU 2011131985/04A RU 2011131985 A RU2011131985 A RU 2011131985A RU 2011131985 A RU2011131985 A RU 2011131985A
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Russia
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alkyl
group
compound according
disease
cancer
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RU2011131985/04A
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English (en)
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Хорхе АЛОНСО
ЛОПЕС Аранткса ЭНСИНАС
Марсель МЮЛЬБАЙЕР
Йохен АММЕН
Бернд ВЕНДТ
Джо ЛЕВИС
Кристоф ШУЛЬТЕС
Бернд ЯНСЕН
Original Assignee
Юропиан Моулекьюлар Байолоджи Лаборатори (Юмбл)
Элара Фармасьютикалз Гмбх
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Publication of RU2011131985A publication Critical patent/RU2011131985A/ru

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    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/21—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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 with substituted hydrocarbon radicals, directly attached to ring carbon atoms
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Abstract

1. Соединение, имеющее структуру формулы I:гдеRвыбран из группы, состоящей из Н, алкила, алкенила, алкинила, -CN, галогена, -ОН, алкокси, -SH, S-алкила, -NH, NH-алкила, N-бис-алкила, NHOH, NMeOH, NMe(OMe), -NO, -CF, -OCFи гидрокси(С-С)алкила.Rпредставляет Н или C-Cалкил;Rпредставляет Н или -СН;Rпредставляет фенил или моноциклический 5- или 6-членный гетероарил, необязательно замещенный одним или более заместителями, выбранными из группы, состоящей из:алкила, алкенила, алкинила, алкокси, галогена, -CN, -CF, -OCF, C-Сгидроксиалкила, -ОН, -SH, S-алкила, -CN, N-бис-алкила, цианоацетилена, -NO, -NRR, -C(O)R, N-O (где атом азота является целой частью моноциклического 5-или 6-членного гетероарила),и двух заместителей, которые вместе образуют диоксиметиленовый мостик (-O-СН-O-);Rпредставляет Н или -СН;Rвыбран из группы, состоящей из Н, галогена, алкила, алкокси, алкенила, алкинила, S-алкила, -ОН, -NRR, -CN, N-бис-алкила, -SH, -CFи -OCF; или Rобразует вместе с Rдиоксиметиленовый мостик (-О-СН-О-);Rпредставляет собой Н или алкил;Rпредставляет собой Н или C-Cалкил; иRпредставляет собой C-Cалкил;при условии, что Rне является 3-алкокси-пиридазин-5-илом; что если Rявляется фенилом, то 2-ое и 5-ое положение фенильного кольца не могут быть замещены двумя метокси заместителями одновременно; и что Rи Rне могут быть одновременно Н.2. Соединение по п.1, имеющее структуру формулы II:3. Соединение по п.1, имеющее структуру формулы III:4. Соединение по любому из пп.1-3, где Rимеет структуру формулы IV:гдеRи Rнезависимо выбраны из группы, состоящей из Н, С-Салкила, C-Салкенила, С-Салкинила, -CN, -C(O)R, цианоацетилена, галогена, -ОН, С-Салкокси, -SH, S-(С-С)алкила, -NH, NH-(C-C)алкила, N-бис-(C-C)алкила, -NO, -CF, -OCFи гидрокси(С-С)алкила;или Rи Rвместе образуют диоксиметилен

Claims (18)

1. Соединение, имеющее структуру формулы I:
Figure 00000001
где
R1 выбран из группы, состоящей из Н, алкила, алкенила, алкинила, -CN, галогена, -ОН, алкокси, -SH, S-алкила, -NH2, NH-алкила, N-бис-алкила, NHOH, NMeOH, NMe(OMe), -NO2, -CF3, -OCF3 и гидрокси(С1-С4)алкила.
R2 представляет Н или C1-C4 алкил;
R3 представляет Н или -СН3;
R4 представляет фенил или моноциклический 5- или 6-членный гетероарил, необязательно замещенный одним или более заместителями, выбранными из группы, состоящей из:
алкила, алкенила, алкинила, алкокси, галогена, -CN, -CF3, -OCF3, C1-С4 гидроксиалкила, -ОН, -SH, S-алкила, -CN, N-бис-алкила, цианоацетилена, -NO2, -NR7R8, -C(O)R20, N-O (где атом азота является целой частью моноциклического 5-или 6-членного гетероарила),
и двух заместителей, которые вместе образуют диоксиметиленовый мостик (-O-СН2-O-);
R5 представляет Н или -СН3;
R6 выбран из группы, состоящей из Н, галогена, алкила, алкокси, алкенила, алкинила, S-алкила, -ОН, -NR7R8, -CN, N-бис-алкила, -SH, -CF3 и -OCF3; или R6 образует вместе с R1 диоксиметиленовый мостик (-О-СН2-О-);
R7 представляет собой Н или алкил;
R8 представляет собой Н или C1-C4 алкил; и
R20 представляет собой C1-C4 алкил;
при условии, что R4 не является 3-алкокси-пиридазин-5-илом; что если R4 является фенилом, то 2-ое и 5-ое положение фенильного кольца не могут быть замещены двумя метокси заместителями одновременно; и что R3 и R5 не могут быть одновременно Н.
2. Соединение по п.1, имеющее структуру формулы II:
Figure 00000002
3. Соединение по п.1, имеющее структуру формулы III:
Figure 00000003
4. Соединение по любому из пп.1-3, где R4 имеет структуру формулы IV:
Figure 00000004
где
R9 и R10 независимо выбраны из группы, состоящей из Н, С1-С4алкила, C1-С4алкенила, С1-С4алкинила, -CN, -C(O)R20, цианоацетилена, галогена, -ОН, С1-С4алкокси, -SH, S-(С1-С4)алкила, -NH2, NH-(C1-C4)алкила, N-бис-(C1-C4)алкила, -NO2, -CF3, -OCF3 и гидрокси(С1-С4)алкила;
или R9 и R10 вместе образуют диоксиметиленовый мостик (-О-СН2-О-);
R11 и R12 независимо выбраны из группы, состоящей из Н, С1-С4алкила, C1-С4алкенила, С1-С4алкинила, -CN, галогена, -ОН, С1-С4алкокси, -SH, S-(С1-С4)алкила, -CF3, -OCF3, -NH2, -N(СН3)2 и гидрокси(С1-С4)алкила;
при условии, что R9 и R12 не могут быть метокси одновременно;
R20 принимает указанные выше значения; и
* обозначает связь между R4 и соединением любой из формул от (I) до (III).
5. Соединение по п.4, где R11 и R12 представляют Н.
6. Соединение по п.5, где
R3 представляет метил;
R2 представляет Н, метил или этил; и
R5 и R6 представляют Н.
7. Соединение по любому из пп.1-3, где R4 имеет структуру формулы V:
Figure 00000005
где
А, В, С и Е независимо выбраны из группы, состоящей из атома азота, CR13 и N-O;
G выбран из группы, состоящей из атома кислорода, атома серы и NR14;
R13 выбран из группы, состоящей из Н, C1-С3алкила, C1-С3алкокси, -ОН, -SH, -CF3, -OCF3, галогена, NR15R16, -NO2, -CN, -C(O)R20, ацетилена, цианоацетилена, гидрокси(С1-С4)алкила и σ (сигма) связи, связывающей R4 с соединением согласно любой из формул от (I) до (III); и
R14 выбран из группы, состоящей из Н, С1-С4алкила и σ (сигма) связи, связывающей R4 с соединением согласно любой из формул от (I) до (III);
и
R15 и R16 независимо представляют или Н или С1-С4алкил;
R20 принимает указанные выше значения; и
* обозначает связь между R4 и соединением любой из формул от (I) до (III).
8. Соединение по любому из пп.1-3, где R4 имеет структуру формуле VI:
Figure 00000006
где
L и Т независимо представляют или СН группу или атом азота, или N-O;
М, N и Q независимо выбраны из группы, состоящей из атома азота, CR17 группы и N-O;
R17 выбран из группы, состоящей из Н, C1-С3алкила, C1-С3алкокси, -CF3, -OCF3, галогена, -ОН, -NO2, -SH, S-(С1-С3)алкила, -NR15R16, гидрокси(С1-С4)алкила, -C(O)R20, ацетилена, цианоацетилена, и -CN;
R15 и R16 независимо представляют или Н или С1-С4алкил;
R20 принимает указанные выше значения;
и * показывает связь между R4 и соединением любой из формул от (I) до (III).
9. Соединение по любому из пп.1-3, где R4 выбран из группы, состоящей из:
Figure 00000007
,
Figure 00000008
,
Figure 00000009
,
Figure 00000010
,
Figure 00000011
,
Figure 00000012
,
Figure 00000013
,
Figure 00000014
,
Figure 00000015
,
Figure 00000016
,
Figure 00000017
,
Figure 00000018
,
Figure 00000019
,
Figure 00000020
,
Figure 00000021
,
Figure 00000022
,
Figure 00000023
,
Figure 00000024
,
Figure 00000025
,
Figure 00000026
,
Figure 00000027
,
Figure 00000028
и
Figure 00000029
где R18 и R19 независимо выбраны из группы, состоящей из Н, C1-С3 алкила, C1-С3 алкокси, -CF3, -OCF3, галогена, -ОН, -NO2, -SH, S-(С1-С3)алкила, -NR15R16, гидрокси(С1-С4)алкила, алкинила, алкенила, -C(O)R20, цианоацетилена, и -CN;
R15, R16 и R20 принимают указанные выше значения.
10. Соединение по любому из пп.1-3, где R2 представляет Н и R4 выбран из группы, состоящей из:
Figure 00000030
,
Figure 00000031
,
Figure 00000032
,
Figure 00000033
,
Figure 00000034
,
Figure 00000035
,
Figure 00000036
,
Figure 00000037
,
Figure 00000038
,
Figure 00000039
,
Figure 00000040
,
Figure 00000041
,
Figure 00000042
,
Figure 00000043
,
Figure 00000044
,
Figure 00000045
,
Figure 00000046
,
Figure 00000047
,
Figure 00000048
,
Figure 00000049
,
Figure 00000050
,
Figure 00000051
,
Figure 00000052
,
Figure 00000053
,
Figure 00000054
,
Figure 00000055
,
Figure 00000056
,
Figure 00000057
,
Figure 00000058
,
Figure 00000059
,
Figure 00000060
,
Figure 00000061
,
Figure 00000062
,
Figure 00000063
,
Figure 00000064
,
Figure 00000065
,
Figure 00000066
,
Figure 00000067
,
Figure 00000068
,
Figure 00000069
,
Figure 00000070
,
Figure 00000071
,
Figure 00000072
,
Figure 00000073
,
Figure 00000074
,
Figure 00000075
,
Figure 00000070
,
Figure 00000076
,
Figure 00000074
,
Figure 00000077
,
Figure 00000078
,
Figure 00000079
,
Figure 00000080
,
Figure 00000081
,
Figure 00000082
,
Figure 00000083
,
Figure 00000084
,
Figure 00000085
,
Figure 00000086
,
Figure 00000087
,
Figure 00000085
,
Figure 00000088
,
Figure 00000089
,
Figure 00000090
,
Figure 00000091
,
Figure 00000092
,
Figure 00000093
,
Figure 00000094
,
Figure 00000095
,
Figure 00000096
,
Figure 00000097
,
Figure 00000098
,
Figure 00000099
,
Figure 00000100
,
Figure 00000101
,
Figure 00000102
,
Figure 00000103
,
Figure 00000104
,
Figure 00000105
,
Figure 00000106
,
Figure 00000107
,
Figure 00000108
,
Figure 00000109
,
Figure 00000101
,
Figure 00000110
,
Figure 00000111
,
Figure 00000112
,
Figure 00000113
,
Figure 00000114
,
Figure 00000115
,
Figure 00000116
,
Figure 00000117
,
Figure 00000118
,
Figure 00000119
,
Figure 00000120
,
Figure 00000121
,
Figure 00000122
,
Figure 00000123
,
Figure 00000124
,
Figure 00000125
,
Figure 00000126
,
Figure 00000127
,
Figure 00000128
,
Figure 00000129
,
Figure 00000130
,
Figure 00000131
и
Figure 00000132
где * показывает связь между R4 и соединением любой из формул от (I) до (III).
11. Соединение по любому из пп.1-3, где R2 и/или R6 представляет H.
12. Соединение по п.1 или его фармацевтически приемлемая соль для предотвращения или лечения заболевания или расстройства.
13. Фармацевтическая композиция, содержащая соединение по любому из пп.1-10 или его фармацевтически приемлемую соль и второй терапевтический агент, полезный для лечения или предотвращения заболевания или расстройства, выбранного из группы, состоящей из воспалительного заболевания, гиперпролиферативного заболевания или расстройства, связанного с гипоксией патологии, и заболевания, охарактеризованного патофизиологической гиперваскуляризацией, и необязательно фармацевтически приемлемый носитель или эксципиент.
14. Применение соединения по любому из пп.1-11 или композиции по п.13 для получения лекарственного средства для лечения или предотвращения заболевания или расстройства выбранного из группы, состоящей из воспалительного заболевания, гиперпролиферативного заболевания или расстройства, связанного с гипоксией патологии, или заболевания, охарактеризованного патофизиологической гиперваскуляризацией.
15. Применение по п.14, где воспалительное заболевание выбрано из группы, состоящей из атеросклероза, ревматоидного артрита, астмы, воспалительного заболевания пищеварительного тракта, псориаза, в частности псориаза обыкновенного, псориаза волосяного, каплевидного псориаза, псориаза кожных складок; нейродерматита; ихтиоза; гнездной алопеции; тотальной алопеции; субтотальной алопеции; общей алопеции; диффузной алопеции; атопического дерматита; красной волчанки кожи; кожного дерматомиозита; атопической экземы; кольцевидной склеродермии; склеродермии; краевой формы гнездной алопеции; андрогенной алопеции; аллергического дерматита; раздражающего контактного дерматита; контактного дерматита; пузырчатки обыкновенной; пузырчатки листовидной; пузырчатки вегетирующей; рубцующего пимфегоида слизистой оболочки; буллезного пемфигоида; пемфигоида слизистой оболочки; дерматита; герпетиформного дерматита Дюринга; крапивницы; липоидного некробиоза; эритемы узловатой; симплексного пруриго; узловатого пруриго; острого пруриго; линейного IGA дерматоза; полиморфного фото дерматоза; солнечной эритемы; кожной экзантемы; лекарственной экзантемы; прогрессирующей хронической пурпуры; дисгидротической экземы; экземы; постоянной лекарственной экзантемы; фотоаллергической реакции кожи и периорального дерматита.
16. Применение по п.14, где гиперпролиферативное заболевание выбрано из группы, состоящей из опухолевого или ракового заболевания, предракового заболевания, дисплазии, гистиоцитоза, васкулярного пролиферативного заболевания и вирус-индуцированного пролиферативного заболевания.
17. Применение по п.16, где гиперпролиферативное заболевание представляет опухолевое или раковое заболевание, выбранное из группы, состоящей из диффузной В-клеточной лимфомы (DLBCL), Т-клеточной лимфомы или лейкемии, например, кожной Т-клеточной лимфомы (CTCL), некожной периферической Т-клеточной лимфомы, лимфомы связанной с человеческим Т-клеточным лимфотрофическим вирусом (HTLV), Т-клеточной лейкемии/лимфомы взрослых, а также острой лимфоцитарной лейкемии, острой нелимфоцитарной лейкемии, острой миелоидной лейкемии, хронической лимфоцитарной лейкемии, хронической миелогенной лейкемии, заболевания Ходжкина, не-Ходжкина заболевания, миеломы, множественной миеломы, мезотиеломы, детской солидной опухоли, глиомы, рака кости и саркомы мягких тканей, имеющей общее происхождение, солидной опухоли взрослых, такой как рак головы и шеи (например, внутриротовой, ларингеальный и пищеводный), рака мочеполовой системы (например, простаты, мочевого пузыря, почечный (в частности, злокачественная почечная клеточная карцинома (RCC)), маточный, яичниковый, тестикулярный, рак прямой кишки и толстой кишки), рака легких (например, мелкоклеточная карцинома и немелкоклеточная карцинома легкого, включающая плоскоклеточную карциному и аденокарциному), рака молочной железы, рака поджелудочной железы, меланомы и других видов рака кожи, базальной клеточной карциномы, метастатической карциномы кожи, плоскоклеточной карциномы как язвенного, так и папиллярного типа, рака желудка, рака головного мозга, рака печени, рака надпочечников, рака почки, рака щитовидной железы, медуллярной карциномы, остеосаркомы, саркомы мягких тканей, саркомы Юинга, ретикулярно-клеточной саркомы и саркомы Капоши, фибросаркомы, миксосаркомы, липосаркомы, хондросаркомы остеогенной саркомы, хордомы, ангиосаркомы, эндотелиальной саркомы, лимфагиомной саркомы, лимфагиоэндотелиальной саркомы, синовиомы, мезотелиомы, лейомиосаркомы, рабдомиосаркомы, плоскоклеточной карциномы, базальной клеточной карциномы, аденокарциномы, карциномы потовой железы, карциномы сальной железы, папиллярной карциномы, папиллярной аденокарциномы, цистаденокарциномы, медуллярной карциномы, бронхогенной карциномы, семиномы, эмбриональной карциномы, опухоли Вильмса, мелкоклеточной карциномы легкого, эпителиальной карциномы, астроцитомы, медуллобластомы, опухоли кармана Ратке, эпендимальной глиомы, пинеаломы, гемангиобластомы, акустической невриномы, олигодендроглиомы, менингиомы, нейробластомы, ретинобластомы, глаукомы, гемангиомы, тяжелой цепи заболеваний и метастазов.
18. Способ лечения гиперпролиферативного заболевания или расстройства, включающий введение соединения по любому из пп.1-11 или композиции по п.13 пациенту до, во время и/или после того, как он был подвержен радиационной терапии, химиотерапии, иммунотерапии или генной терапии с использованием антисмысловой ДНК и/или РНК.
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