RU2008145663A - Производное тиено[3,2-d]пиримидина в качестве ингибитора фосфатидилинозитол-3-киназы (рi3к) - Google Patents
Производное тиено[3,2-d]пиримидина в качестве ингибитора фосфатидилинозитол-3-киназы (рi3к) Download PDFInfo
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- LHNIIDJUOCFXAP-UHFFFAOYSA-N CS(N1CCN(Cc2cc(nc(-c3cccc4c3cn[nH]4)nc3N4CCOCC4)c3[s]2)CC1)(=O)=O Chemical compound CS(N1CCN(Cc2cc(nc(-c3cccc4c3cn[nH]4)nc3N4CCOCC4)c3[s]2)CC1)(=O)=O LHNIIDJUOCFXAP-UHFFFAOYSA-N 0.000 description 1
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Abstract
1. Соединение, которое представляет собой тиенопиримидин формулы (I) ! ! или его фармацевтически приемлемая соль. ! 2. Соединение по п.1, где фармацевтически приемлемая соль выбрана из солей с соляной кислотой, бромисто-водородной кислотой, йодисто-водородной кислотой, серной кислотой, азотной кислотой, фосфорной кислотой, метансульфоновой кислотой, бензолсульфоновой кислотой, муравьиной кислотой, уксусной кислотой, трифторуксусной кислотой, пропионовой кислотой, щавелевой кислотой, малоновой кислотой, янтарной кислотой, фумаровой кислотой, малеиновой кислотой, молочной кислотой, яблочной кислотой, винной кислотой, лимонной кислотой, этансульфоновой кислотой, аспарагиновой кислотой и глутаминовой кислотой. ! 3. Соединение по п.1 или 2, где фармацевтически приемлемая соль представляет собой моносоль или бис-соль. ! 4. Соединение по п.1 или 2, которое представляет собой моносоль или бис-соль с метансульфоновой кислотой, бензолсульфоновой кислотой, соляной кислотой, фосфорной кислотой и серной кислотой. ! 5. Соединение по п.1, которое представляет собой 2-(1Н-индазол-4-ил)-6-(4-метансульфонилпиперазин-1-илметил)-4-морфолин-4-илтиено[3,2-d]пиримидина бисмезилат. ! 6. Способ получения соединения, как определено в п.1, при котором (а) обрабатывают соединение формулы (III) ! ! амином формулы (V) ! ! в присутствии подходящего восстанавливающего агента, или ! (б) обрабатывают соединение формулы (VI) ! ! бороновой кислотой или ее эфиром формулы (IV) ! ! в которой каждый R15 представляет собой Н или C1-C6 алкил, либо две группы OR15 образуют вместе с атомом бора, к которому они присоединены, сложноэфирную пинаколятоборонатную группу, в присутст
Claims (14)
2. Соединение по п.1, где фармацевтически приемлемая соль выбрана из солей с соляной кислотой, бромисто-водородной кислотой, йодисто-водородной кислотой, серной кислотой, азотной кислотой, фосфорной кислотой, метансульфоновой кислотой, бензолсульфоновой кислотой, муравьиной кислотой, уксусной кислотой, трифторуксусной кислотой, пропионовой кислотой, щавелевой кислотой, малоновой кислотой, янтарной кислотой, фумаровой кислотой, малеиновой кислотой, молочной кислотой, яблочной кислотой, винной кислотой, лимонной кислотой, этансульфоновой кислотой, аспарагиновой кислотой и глутаминовой кислотой.
3. Соединение по п.1 или 2, где фармацевтически приемлемая соль представляет собой моносоль или бис-соль.
4. Соединение по п.1 или 2, которое представляет собой моносоль или бис-соль с метансульфоновой кислотой, бензолсульфоновой кислотой, соляной кислотой, фосфорной кислотой и серной кислотой.
5. Соединение по п.1, которое представляет собой 2-(1Н-индазол-4-ил)-6-(4-метансульфонилпиперазин-1-илметил)-4-морфолин-4-илтиено[3,2-d]пиримидина бисмезилат.
6. Способ получения соединения, как определено в п.1, при котором (а) обрабатывают соединение формулы (III)
амином формулы (V)
в присутствии подходящего восстанавливающего агента, или
(б) обрабатывают соединение формулы (VI)
бороновой кислотой или ее эфиром формулы (IV)
в которой каждый R15 представляет собой Н или C1-C6 алкил, либо две группы OR15 образуют вместе с атомом бора, к которому они присоединены, сложноэфирную пинаколятоборонатную группу, в присутствии катализатора Pd.
8. Фармацевтическая композиция, которая содержит фармацевтически приемлемый носитель или разбавитель и, в качестве активного ингредиента, соединение по п.1.
9. Композиция по п.8, которая приготовлена для перорального введения.
10. Способ лечения заболевания или расстройства, возникающего в результате аномального роста, функции или поведения клеток, связанного с ФИЗ киназой, при котором пациенту, нуждающемуся в этом, вводят соединение, как определено в п.1.
11. Способ по п.10, где заболевание или расстройство выбрано из группы, состоящей из рака, иммунных расстройств, сердечно-сосудистого заболевания, вирусной инфекции, воспаления, расстройств метаболизма/эндокринных расстройств и неврологических расстройств.
12. Способ по п.11, где рак выбран из глиобластомы, меланомы, рака простаты, эндометрия, яичника, молочной железы, легкого, головы, шеи, печеночно-клеточного рака, рака щитовидной железы, рака шейки матки, простаты, яичка, мочеполовых путей, пищевода, гортани, глиобластомы, нейробластомы, рака желудка, кожи, кератоакантомы, рака легкого, плоскоклеточного рака, крупноклеточного рака, немелкоклеточного рака легкого (НМКРЛ), мелкоклеточного рака, аденокарциномы легкого, рака кости, ободочной кишки, аденомы, рака поджелудочной железы, аденокарциномы, рака щитовидной железы, фолликулярной карциномы, недифференцированной карциномы, папиллярной карциномы, семиномы, меланомы, саркомы, карциномы мочевого пузыря, карциномы печени и желчных протоков, карциномы почки, миелоидных расстройств, лимфоидных расстройств, лейкозного ретикулоэндотелиоза, рака полости рта и глотки (орального), губы, языка, рта, глотки, тонкого кишечника, прямой и ободочной кишки, толстого кишечника, прямой кишки, головного мозга и центральной нервной системы, лимфомы Ходжкина и лейкоза.
13. Способ изготовления фармацевтической композиции, при котором объединяют соединение, как определено в п.1, с фармацевтически приемлемым носителем.
14. Набор для лечения состояния, опосредованного ФИЗК, содержащий:
(а) первую фармацевтическую композицию, содержащую соединение, как определено в п.1;
(б) инструкции по применению; и
(в) вторую фармацевтическую композицию, где вторая фармацевтическая композиция содержит второе соединение, обладающее антигиперпролиферативной активностью,
при этом инструкции относятся к одновременному, последовательному или отдельному введению указанной первой и второй фармацевтических композиций пациенту, нуждающемуся в этом.
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US11008333B2 (en) | 2015-12-31 | 2021-05-18 | Hanmi Pharm. Co., Ltd. | Crystalline forms of hydrochloride salts of thienopyrimidine compound |
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