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RU2341527C1 - Annelated asaheterocycles including pyrimidine fragment, method of production thereof and pi3k kinase inhibitors - Google Patents

Annelated asaheterocycles including pyrimidine fragment, method of production thereof and pi3k kinase inhibitors Download PDF

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RU2341527C1
RU2341527C1 RU2007127188/04A RU2007127188A RU2341527C1 RU 2341527 C1 RU2341527 C1 RU 2341527C1 RU 2007127188/04 A RU2007127188/04 A RU 2007127188/04A RU 2007127188 A RU2007127188 A RU 2007127188A RU 2341527 C1 RU2341527 C1 RU 2341527C1
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Александр Васильевич Иващенко (US)
Александр Васильевич Иващенко
Сергей Евгеньевич Ткаченко (RU)
Сергей Евгеньевич Ткаченко
Иль Матусович Окунь (US)
Илья Матусович Окунь
Николай Филиппович Савчук (RU)
Николай Филиппович Савчук
Андрей Александрович Иващенко (RU)
Андрей Александрович Иващенко
Дмитрий Владимирович Кравченко (RU)
Дмитрий Владимирович Кравченко
Олег ШМИДТ-КИТТЛЕР (US)
Олег ШМИДТ-КИТТЛЕР
Карло РАГО (US)
Карло РАГО
Николас ПАПАДОПОУЛОС (US)
Николас ПАПАДОПОУЛОС
Виктор ВЕЛКУЕЛСКУ (US)
Виктор ВЕЛКУЕЛСКУ
Берт ВОГЕЛСТАИН (US)
Берт ВОГЕЛСТАИН
Кеннет В. КИНЗЛЕР (US)
Кеннет В. КИНЗЛЕР
Андрей Сергеевич Трифиленков (RU)
Андрей Сергеевич Трифиленков
Елена Александровна Рыжова (RU)
Елена Александровна Рыжова
Жу ДЖУКСИЯНГ (US)
Жу ДЖУКСИЯНГ
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Abstract

FIELD: medicine; pharmacology.
SUBSTANCE: new annelated asaheterocycles include pyrimidine fragment of general formula I in the form of free bases or pharmaceutically acceptable salts. Compounds of this invention possess properties of PI3 kinase inhibitors. In general formula I
Figure 00000002
X represents oxygen atom or sulphur atom; Z represents oxygen atom, R1 represents hydrogen atom or optionally substituted C1-C6alkyl, or Z represents nitrogen atom together with bound carbon atom forming through Z and R1 optionally substituted annelated imidazoline cycle; R2 represents optionally substituted C1-C6alkyl, optionally substituted C3-C8cycloalkyl, optionally substituted phenyl, possibly annelated with 5-6-term heterocyclyl containing heteroatoms chosen from oxygen and nitrogen, optionally substituted 5-6-term heterocyclyl containing heteroatoms chosen from nitrogen, oxygen and/or sulphur, possibly annelated with phenyl ring. Invention also concerns method of production of compounds, pharmaceutical compositions and medical products.
EFFECT: effective application for preparation of medical products for oncologic therapy.
14 cl, 3 dwg, 1 tbl, 4 ex

Description

Текст описания приведен в факсимильном виде.

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The text of the description is given in facsimile form.
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Claims (14)

1. Аннелированные азагетероциклы, включающие пиримидиновый фрагмент общей формулы I в форме свободных оснований или фармацевтически приемлемых солей1. Annelated azaheterocycles comprising the pyrimidine moiety of general formula I in the form of free bases or pharmaceutically acceptable salts
Figure 00000144
Figure 00000144
 где Х представляет атом кислорода или атом серы;where X represents an oxygen atom or a sulfur atom; Z представляет собой атом кислорода, R1 представляет собой атом водорода или необязательно замещенный C1-С6 алкил, илиZ represents an oxygen atom, R1 represents a hydrogen atom or an optionally substituted C 1 -C 6 alkyl, or Z представляет собой атом азота, который вместе с атомом углерода, с которым он связан, образуют через Z и R1 необязательно замещенный аннелированный имидазолиновый цикл;Z represents a nitrogen atom which, together with the carbon atom to which it is bonded, form through Z and R1 an optionally substituted annelated imidazoline ring; R2 представляет собой необязательно замещенный C1-С6алкил, необязательно замещенный С3-С8циклоалкил, необязательно замещенный фенил, возможно аннелированный с 5-6-членным гетероциклилом, содержащим гетероатомы, выбранные из кислорода и азота, необязательно замещенный 5-6-членный гетероциклил, содержащий гетероатомы, выбранные из азота, кислорода и/или серы, возможно аннелированный с фенильным кольцом.R2 is optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted phenyl, optionally annelated with a 5-6 membered heterocyclyl containing heteroatoms selected from oxygen and nitrogen, optionally substituted with 5-6- a heterocyclyl member containing heteroatoms selected from nitrogen, oxygen and / or sulfur, possibly annelated with a phenyl ring. 2. Соединения по п.1, представляющие собой замещенные амиды 4-оксо-3,4-дигидрофуро[2,3-b]пиримидин-5-карбоновых кислот общей формулы I.1, замещенные амиды 4-оксо-3,4-дигидротиено[2,3-b]пиримидин-5-карбоновых кислот общей формулы I.2 и замещенные амиды 2,3-дигидрофуро[3,2-е]имидазо[1,2-с]пиримидин-9-карбоновых кислот общей формулы I.3 или их фармацевтически приемлемые соли2. The compounds according to claim 1, which are substituted amides of 4-oxo-3,4-dihydrofuro [2,3-b] pyrimidine-5-carboxylic acids of the general formula I.1, substituted amides of 4-oxo-3,4- dihydrothieno [2,3-b] pyrimidine-5-carboxylic acids of the general formula I.2 and substituted amides of 2,3-dihydrofuro [3,2-e] imidazo [1,2-c] pyrimidine-9-carboxylic acids of the general formula I.3 or their pharmaceutically acceptable salts
Figure 00000145
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 где R1 и R2 имеют вышеуказанные значения; R3а и R3b независимо друг от друга представляют собой атом водорода или низший алкил.where R1 and R2 have the above meanings; R 3 a and R 3 b independently represent a hydrogen atom or lower alkyl. 3. Способ получения соединений общих формул I.1, I.2, I.3 по п.1 или 2 взаимодействием соответствующих кислот общих формул F1, F2, H3 с аминами общей формулы F11 в присутствии конденсирующих реагентов3. A method for producing compounds of general formulas I.1, I.2, I.3 according to claim 1 or 2 by reacting the corresponding acids of general formulas F1, F2, H3 with amines of general formula F11 in the presence of condensing reagents
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 где R1, R2, R3а и R3b имеют вышеуказанные значения.where R1, R2, R 3 a and R 3 b have the above meanings. 4. Ингибиторы PI3 киназ, представляющие собой соединения общей формулы I по п.1.4. Inhibitors of PI3 kinases, which are compounds of General formula I according to claim 1. 5. Селективные ингибиторы по п.4 изоформы р110-альфа PI3 киназ, представляющие собой соединения общей формулы I по п.1.5. Selective inhibitors according to claim 4 of the isoform of p110-alpha PI3 kinases, which are compounds of general formula I according to claim 1. 6. Селективные ингибиторы по п.4 изоформы р110-бета PI3 киназ, представляющие собой соединения общей формулы I по п.1.6. Selective inhibitors according to claim 4 of the isoform of p110-beta PI3 kinases, which are compounds of general formula I according to claim 1. 7. Селективные ингибиторы по п.4 изоформы р110-гамма PI3 киназ, представляющие собой соединения общей формулы I по п.1.7. Selective inhibitors according to claim 4 of the isoform of p110-gamma PI3 kinases, which are compounds of general formula I according to claim 1. 8. Селективные ингибиторы по п.4 изоформы р110-дельта PI3 киназ, представляющие собой соединения общей формулы I по п.1.8. Selective inhibitors according to claim 4 of the isoform of p110-delta PI3 kinases, which are compounds of general formula I according to claim 1. 9. Селективные ингибиторы по п.5 изоформы р110-альфа PI3 киназ с мутацией в эксоне 20 (H1047R), представляющие собой соединения общей формулы I по п.1.9. Selective inhibitors according to claim 5 of the isoform of p110-alpha PI3 kinases with mutation in exon 20 (H1047R), which are compounds of the general formula I according to claim 1. 10. Соединения общей формулы I по п.1 в качестве биологически активного начала для получения лекарственных средств для лечения онкологических заболеваний.10. The compounds of General formula I according to claim 1 as a biologically active principle for the production of drugs for the treatment of cancer. 11. Фармацевтическая композиция, предназначенная для лечения онкологических заболеваний, содержащая в качестве биологически активного начала, по крайней мере, одно соединение общей формулы I по п.1, или соединения по п.2, или их фармацевтически приемлемые соли в эффективном количестве.11. A pharmaceutical composition for the treatment of cancer, containing, as a biologically active principle, at least one compound of general formula I according to claim 1, or a compound according to claim 2, or pharmaceutically acceptable salts thereof in an effective amount. 12. Фармацевтическая композиция по п.11, содержащая в качестве активного начала, по крайней мере, одно соединение общих формул I.1, I.2, I.3 по п.2 или их фармацевтически приемлемые соли в эффективном количестве.12. The pharmaceutical composition according to claim 11, containing as an active principle, at least one compound of the general formulas I.1, I.2, I.3 according to claim 2 or their pharmaceutically acceptable salts in an effective amount. 13. Способ получения фармацевтической композиции по п.11 или 12 смешением активного начала, представляющего собой, по крайней мере, одно соединение общей формулы I по п.1 или его фармацевтически приемлемую соль, с инертными наполнителями и/или растворителями.13. The method of obtaining the pharmaceutical composition according to claim 11 or 12, mixing the active principle, which is at least one compound of general formula I according to claim 1 or a pharmaceutically acceptable salt thereof, with inert excipients and / or solvents. 14. Лекарственное средство в форме таблеток, капсул или инъекций, помещенных в фармацевтически приемлемую упаковку, включающее ингибитор PI3 киназ по любому из пп.4-9 или фармацевтическую композицию по любому из пп.11 и 12 в эффективном количестве.14. A drug in the form of tablets, capsules or injections in a pharmaceutically acceptable package, comprising a PI3 kinase inhibitor according to any one of claims 4 to 9 or a pharmaceutical composition according to any one of claims 11 and 12 in an effective amount.
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