RU2355700C9 - Новые пептиды как ингибиторы ns3-серинпротеазы вируса гепатита с - Google Patents

Новые пептиды как ингибиторы ns3-серинпротеазы вируса гепатита с Download PDF

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RU2355700C9
RU2355700C9 RU2003105217/04A RU2003105217A RU2355700C9 RU 2355700 C9 RU2355700 C9 RU 2355700C9 RU 2003105217/04 A RU2003105217/04 A RU 2003105217/04A RU 2003105217 A RU2003105217 A RU 2003105217A RU 2355700 C9 RU2355700 C9 RU 2355700C9
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interferon
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hepatitis
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Анил К. САКСЕНА (US)
Анил К. САКСЕНА
Вийур Мупил ГИРИЯВАЛЛАБХАН (US)
Вийур Мупил ГИРИЯВАЛЛАБХАН
Реймонд Дж. ЛАВИ (US)
Реймонд Дж. ЛАВИ
Эдвин И. ДЖАО (US)
Эдвин И. ДЖАО
Фрэнк БЕННЕТ (US)
Фрэнк Беннет
КОРМИК Джинпинг Л. МАК (US)
КОРМИК Джинпинг Л. МАК
Хайян ВАНГ (US)
Хайян ВАНГ
Рассел И. ПАЙК (US)
Рассел И. ПАЙК
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Тин-Яу ЧЭН (US)
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Ф. Джордж НЬЕРОГЕ
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Хенри Э. ВАККАРО (US)
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

В настоящем изобретении раскрыты новые соединения, которые обладают способностью ингибировать протеазу HCV (вируса гепатита С), а также способы получения таких соединений. В другом варианте осуществления в настоящем изобретении раскрыты фармацевтические композиции, включающие такие соединения, а также способы их применения для лечения заболеваний, связанных с протеазой HCV. 6 н. и 17 з.п. ф-лы, 5 табл.

Description

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Claims (23)

1. Производное пептида, обладающее ингибирующей протеазу HCV активностью, выбранное из группы, включающей следующие соединения:
Figure 00000453
Figure 00000454
Figure 00000455
Figure 00000456
Figure 00000457
Figure 00000458
Figure 00000459
Figure 00000460
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Figure 00000482

Figure 00000483

Figure 00000484

Figure 00000485

Figure 00000486

Figure 00000487

Figure 00000488

Figure 00000489

и его энантиомеры, стереоизомеры, ротамеры, таутомеры, рацематы или приемлемые с фармацевтической точки зрения соли.
2. Фармацевтическая композиция, обладающая ингибирующей вирус гепатита С активностью, содержащая терапевтически эффективное количество одного или нескольких производных пептида по п.1, включая их энантиомеры, стереоизомеры, ротамеры, таутомеры, рацематы и приемлемые с фармацевтической точки зрения соли, и фармацевтически приемлемый носитель.
3. Фармацевтическая композиция по п.2, отличающаяся тем, что дополнительно содержит антивирусный агент.
4. Фармацевтическая композиция по п.3, отличающаяся тем, что в качестве антивирусного агента содержит рибавирин.
5. Фармацевтическая композиция по п.2, отличающаяся тем, что дополнительно содержит интерферон.
6. Фармацевтическая композиция по п.3 или 4, отличающаяся тем, что дополнительно содержит интерферон.
7. Фармацевтическая композиция по п.5, отличающаяся тем, что в качестве интерферона содержит α-интерферон или конъюгат α-интерферона и полиэтиленгликоля (ПЭГ).
8. Фармацевтическая композиция по п.6, отличающаяся тем, что в качестве интерферона содержит α-интерферон или конъюгат α-интерферона и полиэтиленгликоля (ПЭГ).
9. Фармацевтическая композиция по п.2, причем производное пептида выбрано из следующих соединений:
Figure 00000490

Figure 00000491

Figure 00000492

Figure 00000493

Figure 00000494

Figure 00000495

Figure 00000496

Figure 00000497

Figure 00000498

Figure 00000499
,
предпочтительно выбрано из следующих соединений:
Figure 00000500

Figure 00000501

Figure 00000502

Figure 00000503

Figure 00000504

Figure 00000505

Figure 00000506

Figure 00000507

Figure 00000508

Figure 00000509

Figure 00000510

Figure 00000511

Figure 00000512

Figure 00000513

Figure 00000514

Figure 00000515

Figure 00000516

Figure 00000517

Figure 00000518

Figure 00000519
10. Фармацевтическая композиция по п.9, отличающаяся тем, что дополнительно содержит антивирусный агент.
11. Фармацевтическая композиция по п.10, отличающаяся тем, что дополнительно содержит α-интерферон или конъюгат α-интерферона и полиэтиленгликоля (ПЭГ).
12. Фармацевтическая композиция по п.11, содержащая в качестве антивирусного агента рибавирин, а в качестве интерферона - α-интерферон.
13. Производное пептида по п.1, включая его энантиомеры, стереоизомеры, ротамеры, таутомеры, рацематы и приемлемые с фармацевтической точки зрения соли, представляющее собой ингибитор активности протеазы HCV, выбранное из
Figure 00000520

Figure 00000521

Figure 00000522

Figure 00000523

Figure 00000524

Figure 00000525

Figure 00000526

Figure 00000527

Figure 00000528

Figure 00000529
.
14. Производное пептида по п.13, выбранное из:
Figure 00000530

Figure 00000531

Figure 00000502

Figure 00000503

Figure 00000532

Figure 00000533

Figure 00000506

Figure 00000507

Figure 00000508

Figure 00000509

Figure 00000534

Figure 00000535

Figure 00000536

Figure 00000537

Figure 00000514

Figure 00000538

Figure 00000516

Figure 00000539

Figure 00000518

Figure 00000519
.
15. Применение производного пептида по п.1, включая его энантиомеры, стереоизомеры, ротамеры, таутомеры, рацематы и приемлемые с фармацевтической точки зрения соли, для приготовления лекарственного средства для лечения заболеваний, связанных с вирусом гепатита С, путем введения пациенту, нуждающемуся в таком лечении, упомянутого лекарственного средства в терапевтически эффективном количестве.
16. Применение по п.15, причем производное пептида представляет собой производное пептида по п.1 или 14.
17. Применение по п.15 или 16, причем лечение дополнительно включает введение интерферона, предпочтительно α-интерферона или пегилированного интерферона и, при необходимости, введение антивирусного агента.
18. Применение по п.17, причем лекарственное средство вводят перорально или подкожно.
19. Способ модуляции активности протеазы вируса гепатита С, включающий контактирование протеазы вируса гепатита С с одним или более производных пептида по п.1.
20. Способ по п.19, отличающийся тем, что протеаза вируса гепатита С представляет собой протеазу NS3/NS4a.
21. Способ по п.19, отличающийся тем, что производное пептида или производные пептида ингибируют протеазу вируса гепатита С NS3/NS4a.
22. Применение производного пептида по п.1, для приготовления лекарственного средства для лечения, предотвращения или уменьшения интенсивности одного или большего количества симптомов гепатита С, путем введения эффективного количества одного или более упомянутых производных пептида.
23. Способ модулирования процессинга полипептида вируса гепатита С, заключающийся в контактировании композиции, содержащей полипептид вируса гепатита С, в условиях, при которых полипептид подвергается процессингу, с одним или большим количеством соединений по п.1.
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