RU2353625C2 - Миметики человеческого глюканоподобного пептида-1 и их применение в лечении диабета и родственных состояний - Google Patents

Миметики человеческого глюканоподобного пептида-1 и их применение в лечении диабета и родственных состояний Download PDF

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RU2353625C2
RU2353625C2 RU2004114836/04A RU2004114836A RU2353625C2 RU 2353625 C2 RU2353625 C2 RU 2353625C2 RU 2004114836/04 A RU2004114836/04 A RU 2004114836/04A RU 2004114836 A RU2004114836 A RU 2004114836A RU 2353625 C2 RU2353625 C2 RU 2353625C2
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polypeptide
glucan
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peptide
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Сеша И. НАТАРАДЖАН (US)
Сеша И. НАТАРАДЖАН
Маргарита М. БЭСТОС (US)
Маргарита М. БЭСТОС
Майкл С. БЕРНАТОВИЧ (US)
Майкл С. БЕРНАТОВИЧ
Клаудио МАПЕЛЛИ (US)
Клаудио МАПЕЛЛИ
Винг ЛИ (US)
Винг ЛИ
Уилльям Р. ВВИНГ (US)
Уилльям Р. ВВИНГ
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Бристол-Маерс Сквибб Компани
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/605—Glucagons
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

Настоящее изобретение относится к биологически активным соединениям и охватывает новые пептиды, содержащие до 15 аминокислотных остатков, включающие последовательность Thr-Ser-Asp-Хаа-Хаа,
где Хаа представляет собой необязательно замещенный бифенилаланин, и обладающие активностью рецептора GLP-1. Предложенные пептиды проявляют повышенную устойчивость к протеолитическому расщеплению, что делает их кандидатами для терапии при оральном или парентальном введении. 5 н. и 1 з.п. ф-лы, 7 ил., 4 табл.

Description

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Claims (6)

1. Выделенный полипептид, имеющий активность рецептора GLP-1, содержащий до 15 аминокислотных остатков, включающий аминокислотную последовательность Thr-Ser-Asp-Xaa-Xaa, где Хаа представляет собой необязательно замещенный бифенилаланин.
2. Фармацевтическая композиция для ослабления диабетического состояния, содержащая полипептид по п.1 и фармацевтически приемлемый носитель.
3. Выделенный полипептид по п.1, отличающийся тем, что он выбран из группы последовательностей, состоящей из SEQ ID NO: 3, 11, 12, 14-23, 25-27, 31-32, 34-40, 73, 74, 76, 78, 79, 90-95, 98, 100, 102-108, 114-118, 120-134, 136-140, 142, 144, 145, 148, 150, 153-155, 157-160, 162, 164, 166, 168-171, 173-183, 192-227, 231-234, 236, 238-259, 267-271, 276-278, 281-290, 292, 294, 295, 297-309, 312-339, 343-433, 449-455 и 457-517.
4. Выделенный полипептид, выбранный из группы последовательностей, состоящей из SEQ ID NO: 3, 11, 12, 14-23, 25-27, 31-32, 34-40, 73, 74, 76, 78, 79, 90-95, 98, 100, 102-108, 114-118, 120-134, 136-140, 142, 144, 145, 148, 150, 153-155, 157-160, 162, 164, 166, 168-171, 173-183, 192-227, 231-234, 236, 238-259, 267-271, 276-278, 281-290, 292, 294, 295, 297-309, 312-339, 343-433, 449-455 и 457-517.
5. Фармацевтическая композиция для ослабления диабетического состояния, содержащая полипептид по п.4, и фармацевтически приемлемый носитель.
6. Применение выделенного полипептида по п.1 для изготовления лекарственного средства для ослабления диабетического состояния.
RU2004114836/04A 2001-10-18 2002-10-18 Миметики человеческого глюканоподобного пептида-1 и их применение в лечении диабета и родственных состояний RU2353625C2 (ru)

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