RU2441005C2 - Новые пиразолопиримидины как ингибиторы циклинзависимых киназ - Google Patents

Новые пиразолопиримидины как ингибиторы циклинзависимых киназ Download PDF

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RU2441005C2
RU2441005C2 RU2008117295/04A RU2008117295A RU2441005C2 RU 2441005 C2 RU2441005 C2 RU 2441005C2 RU 2008117295/04 A RU2008117295/04 A RU 2008117295/04A RU 2008117295 A RU2008117295 A RU 2008117295A RU 2441005 C2 RU2441005 C2 RU 2441005C2
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lymphoma
kinase
malignant tumor
leukemia
pharmaceutically acceptable
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RU2008117295A (ru
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Тимоти Дж. ГУЗИ (US)
Тимоти Дж. ГУЗИ
Камил ПАРУХ (US)
Камил ПАРУХ
Майкл П. ДВАЙЕР (US)
Майкл П. ДВАЙЕР
Марк ЛЭЙБРОЛИ (US)
Марк ЛЭЙБРОЛИ
Картик М. КЕЕРТИКАР (US)
Картик М. КЕЕРТИКАР
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Шеринг Корпорейшн
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    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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Abstract

Изобретение относится к соединениям выбранным из группы, состоящей из соединений формулы:
Figure 00000704
Figure 00000705
Figure 00000706
Figure 00000707
и
Figure 00000709
или к их фармацевтически приемлемым солям.
Изобретение также относится к фармацевтической композиции, а также к применению, по меньшей мере, одного соединения по п.1 и/или его фармацевтически приемлемых солей.
Технический результат - получение новых биологически активных соединений, обладающих свойствами ингибиторов циклинзависимых киназ.
4 н. и 7 з.п. ф-лы, 86 табл.

Description

Текст описания приведен в факсимильном виде.
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Claims (11)

1. Соединение, выбранное из группы, состоящей из соединений формулы:
Figure 00000704
Figure 00000705
Figure 00000706

Figure 00000707
и
Figure 00000709

или их фармацевтически приемлемых солей.
2. Фармацевтическая композиция, обладающая свойствами ингибиторов циклинзависимых киназ, содержащая, по меньшей мере, одно соединение по п.1 или его фармацевтически приемлемую соль, и, по меньшей мере, один фармацевтически приемлемый носитель.
3. Применение, по меньшей мере, одного соединения по п.1 и/или его фармацевтически приемлемых солей для получения лекарственного средства, для лечения злокачественной опухоли или для ингибирования одной или нескольких циклинзависимых киназ.
4. Применение по п.3, в котором указанная злокачественная опухоль выбрана из группы, состоящей из
злокачественной опухоли мочевого пузыря, молочной железы, толстой кишки, почки, печени, легкого, мелкоклеточного рака легкого, немелкоклеточного рака легкого, злокачественной опухоли головы и шеи, пищевода, желчного пузыря, яичника, поджелудочной железы, желудка, шейки матки, щитовидной железы, предстательной железы и кожи, включая плоскоклеточную карциному;
лейкоза, острого лимфоцитарного лейкоза, острого лимфобластного лейкоза, В-клеточной лимфомы, Т-клеточной лимфомы, лимфомы Ходжкина, не-Ходжкинской лимфомы, волосатоклеточной лимфомы, лимфомы из клеток мантийной зоны, миеломы и лимфомы Беркитта;
острого и хронического миелогенных лейкозов, миелодиспластического синдрома и промиелоцитарного лейкоза;
фибросаркомы и рабдомиосаркомы;
злокачественной опухоли головы и шеи, лимфомы из клеток мантийной зоны, миеломы;
астроцитомы, нейробластомы, глиомы и шванном;
меланомы, семиномы, тератокарциномы, остеосаркомы, пигментной ксеродермы, кератоакантомы, фолликулярного рака щитовидной железы и саркомы Капоши.
5. Применение, по меньшей мере, одного соединения по п.1 и/или его фармацевтически приемлемых солей для получения лекарственного средства для лечения у пациента одного или нескольких заболеваний, ассоциированных с киназой.
6. Применение по п.5, в котором указанная киназа представляет собой циклин-зависимую киназу.
7. Применение по п.6, в котором указанная циклинзависимая киназа представляет собой CDK1, CDK2 или CDK9.
8. Применение по п.7, в котором указанная киназа представляет собой CDK2.
9. Применение по п.5, в котором указанная киназа представляет собой митоген-активируемую протеинкиназу (MAPK/ERK).
10. Применение по п.5, в котором указанная киназа представляет собой киназу-3 гликогенсинтазы (GSK3beta).
11. Применение по п.5, в котором указанное заболевание выбрано из группы, состоящей из
злокачественной опухоли мочевого пузыря, молочной железы, толстой кишки, почки, печени, легкого, мелкоклеточного рака легкого, немелкоклеточного рака легкого, злокачественной опухоли головы и шеи, пищевода, желчного пузыря, яичника, поджелудочной железы, желудка, шейки матки, щитовидной железы, предстательной железы и кожи, включая плоскоклеточную карциному;
лейкоза, острого лимфоцитарного лейкоза, острого лимфобластного лейкоза, В-клеточной лимфомы, Т-клеточной лимфомы, лимфомы Ходжкина, не-Ходжкинской лимфомы, волосатоклеточной лимфомы, лимфомы из клеток мантийной зоны, миеломы и лимфомы Беркитта;
острого и хронического миелогенных лейкозов, миелодиспластического синдрома и промиелоцитарного лейкоза;
фибросаркомы и рабдомиосаркомы;
злокачественной опухоли головы и шеи, лимфомы из клеток мантийной зоны, миеломы;
астроцитомы, нейробластомы, глиомы и шванном;
меланомы, семиномы, тератокарциномы, остеосаркомы, пигментной ксеродермы, кератоакантомы, фолликулярного рака щитовидной железы и саркомы Капоши.
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