RU2015137757A - Производные пиридазинон-амидов - Google Patents

Производные пиридазинон-амидов Download PDF

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RU2015137757A
RU2015137757A RU2015137757A RU2015137757A RU2015137757A RU 2015137757 A RU2015137757 A RU 2015137757A RU 2015137757 A RU2015137757 A RU 2015137757A RU 2015137757 A RU2015137757 A RU 2015137757A RU 2015137757 A RU2015137757 A RU 2015137757A
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disease
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syndrome
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RU2666899C2 (ru
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Катрин Жоран-Лебрюн
Сантош КУЛКАРНИ
Стефано ГРОСИНЬЯНИ
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Мерк Патент Гмбх
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Claims (37)

1. Соединение формулы (I)
Figure 00000001
в которой
Z означает группу
Figure 00000002
в которой
X означает СН или N,
Y означает СН или N,
Ra, Rc, R1 каждый независимо означают Н, Hal или Al,
Rb означает Н или алкил
Al означает разветвленный или линейный алкил, имеющий от 1 до 12 атомов углерода, в котором один или больше, например, от 1 до 7, атомов Н могут быть заменены посредством Hal, ORb, COORb, CN или N(Rb)2 и причем одна или больше, предпочтительно от 1 до 5 СН2-группы могут быть заменены посредством О, СО, NRb или S, SO, SO2, 1,2-, 1,3- или 1,4-фенилен, -СН=СН- или -С≡С-,
и
Hal означает F, Cl, Br, I
и его фармацевтически приемлемые производные, сольваты, соли и стереоизомеры, включая их смеси во всех соотношениях.
2. Соединение формулы (I) по п. 1, причем Ra означает Hal ORd или алкил, причем Rd означает Н, алкил или СОН или СОалкил.
3. Соединение формулы (I) по п. 1 или 2, причем R1 означает Н, алкил, Hal, Оалкил, ORd, или (CH2)nCONHRb или (CH2)nCOORb, причем n означает 0, 1, 2, 3, 4, 5, или 6 и Rb является таким, как определено выше и причем Rd означает Н, алкил или CORb.
4. Соединение формулы (I) по п. 1 или 2, причем Z означает пиридинил или пиримидинил.
5. Соединение формулы (I), выбранное из следующей группы:
Figure 00000003
Figure 00000004
Figure 00000005
Figure 00000006
Figure 00000007
Figure 00000008
и его фармацевтически приемлемые производные, сольваты, соли и стереоизомеры, включая их смеси во всех соотношениях.
6. Применение соединения формулы (I) по предыдущим пунктам и его фармацевтически приемлемые производные, сольваты, таутомеры, соли, гидраты и стереоизомеры, включая их смеси во всех соотношениях, для применения в качестве лекарственного средства.
7. Применение соединения по п. 6 для применения в лечении или предупреждения воспалительного заболевания, аутоиммунного заболевания, рака или множественного склероза и связанных заболеваний.
8. Применение соединения по п. 7, причем аутоиммунное заболевание выбирают из группы, состоящей из астмы, ревматоидного артрита, острого множественного энцефаломиелита (ОМЭМ), болезни Аддисона, очаговой алопеции, анкилозирующего спондилита, синдрома антифосфолипидных антител (АФС), аутоиммунной гемолитической анемии, аутоиммунного гепатита, аутоиммунного заболевания внутреннего уха, буллезного пемфигоида, болезни Бехчета, целиакии, антитрансглутаминазы, болезни Чагаса, хронического обструктивного заболевания легких, болезни Крона, дерматомиозита, сахарного диабета 1 типа, эндометриоза, синдрома Гудпасчера, болезни Грейвса, синдрома Гийена-Барре (СГБ), тиреоидита Хашимото, гнойного гидраденита, синдрома Кавасаки, нефропатии IgA, идиопатической тромбоцитопенической пурпуры, интерстициального цистита, эритематозной волчанки, смешанной болезни соединительной ткани, кольцевидной склеродермии, множественного склероза (МС), тяжелой миастении, нарколепсии, нейромиотомии, обыкновенной пузырчатки, злокачественной анемии, псориаза, псориатического артрита, полимиозита, билиарного первичного цирроза печени, ревматоидного артрита, шизофрении, склеродермии, синдрома Шегрена, синдрома скованного человека, системного склероза, височного артериита, язвенного колита, васкулита, витилиго, гранулематоза Вегенера.
9. Применение соединения по п. 7, причем заболевание выбирают из ревматоидного артрита, псориатического артрита, остеоартрита, системной красной волчанки, волчаночного нефрита, анкилозирующего спондилоартрита, остеопороза, системного склероза, множественного склероза, псориаза, сахарного диабета I типа, сахарного диабета II типа, воспалительного заболевания кишечника (болезнь Крона и язвенный колит), гипериммуноглобулинемии D и синдрома периодической лихорадки, криопирин-связанных периодических синдромов, синдрома Шницлера, системного ювенильного идиопатического артрита, приобретенной болезни Стилла, подагры, псевдоподагры, синдрома САПГО, болезни Кастлемана, сепсиса, инсульта, атеросклероза, целиакии, DIRA (дефицит антагониста рецептора IL-1), болезни Альцгеймера, болезни Паркинсона, рака.
10. Соединение по п. 6, причем заболевание выбирают из ревматоидного артрита, волчаночного нефрита, системной красной волчанки.
11. Соединение формулы (I) по п. 1 для предупреждения и/или лечения заболеваний, связанных с повышенной экспрессией IRAK.
12. Набор, состоящий из отдельных упаковок:
(а) эффективного количества соединения формулы (I) и/или его фармацевтически приемлемых производных, сольватов, солей, гидратов и стереоизомеров, включая их смеси во всех соотношениях, и
(б) эффективного количества дополнительного действующего вещества лекарственного средства.
13. Фармацевтическая композиция, содержащая по меньшей мере одно из соединений формулы (I) по любому из пп. от 1 до 5 и/или любое его фармацевтически приемлемое производное, сольват, соль и стереоизомер, включая их смеси во всех соотношениях.
14. Фармацевтическая композиция по п. 13, дополнительно содержащая по меньшей мере одно другое лекарственное средство, применяемое в лечении воспалительных заболеваний или иммунных заболеваний.
15. Фармацевтическая композиция по п. 14, дополнительно содержащая по меньшей мере одно другое иммуномодулирующее средство.
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