RU2006120484A - Микрочастицы, содержащие аналоги соматостатина - Google Patents

Микрочастицы, содержащие аналоги соматостатина Download PDF

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RU2006120484A
RU2006120484A RU2006120484/15A RU2006120484A RU2006120484A RU 2006120484 A RU2006120484 A RU 2006120484A RU 2006120484/15 A RU2006120484/15 A RU 2006120484/15A RU 2006120484 A RU2006120484 A RU 2006120484A RU 2006120484 A RU2006120484 A RU 2006120484A
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microparticles according
microparticles
composition according
salt
agent
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Маркус АЛЬХАЙМ (DE)
Маркус АЛЬХАЙМ
Михаэль АУСБОРН (DE)
Михаэль АУСБОРН
Оливье ЛАМБЕР (FR)
Оливье Ламбер
Марк РИМЕНШНИТТЕР (DE)
Марк Рименшниттер
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Новартис АГ (CH)
Новартис Аг
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Priority claimed from GB0326602A external-priority patent/GB0326602D0/en
Priority claimed from GB0406241A external-priority patent/GB0406241D0/en
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    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/31Somatostatins
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1641Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A61K9/1647Polyesters, e.g. poly(lactide-co-glycolide)
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00Drugs for disorders of the metabolism
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    • A61P3/00Drugs for disorders of the metabolism
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    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
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    • AHUMAN NECESSITIES
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    • A61P35/00Antineoplastic agents
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    • A61P35/02Antineoplastic agents specific for leukemia
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    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
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    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
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    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/02Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S977/00Nanotechnology
    • Y10S977/70Nanostructure
    • Y10S977/788Of specified organic or carbon-based composition

Claims (13)

1. Микрочастицы, включающие аналог соматостатина, включающий последовательность аминокислот формулы I
Figure 00000001
в которой X1 обозначает радикал формулы (а) или (б)
Figure 00000002
в которой R1 представляет собой необязательно замещенный фенил, R2 обозначает -Z1-CH2-R1, -CH2-CO-O-CH2-R1,
Figure 00000003
где Z1 обозначает О или S, и
Х2 представляет собой α-аминокислоту, имеющую ароматический остаток на Сα-боковой цепи или аминокислотную группу, выбранную из Dab, Dpr, Dpm, His, (Bzl)HyPro, тиенил-Ala, циклогексил-Ala и трет-бутил-А1а, причем остаток Lys указанной последовательности соответствует остатку Lys9 нативного соматостатина-14
в свободной форме, в форме соли или защищенной форме,
погруженный в полимерную матрицу.
2. Микрочастицы по п.1, в которых аналог соматостатина представляет собой соединение формулы III
Figure 00000004
в которой конфигурация в положении С-2 представляет собой (R) или (S) или их смесь и
в которой R обозначает NR1R2-C2-6алкилен или гуанидин-С2-6алкилен и каждый из R1 и R2 независимо друг от друга обозначают Н или С1-4алкил, в свободной форме, в форме соли или защищенной форме.
3. Микрочастицы по п.2, в которых аналог соматостатина находится в форме соли памовой кислоты.
4. Микрочастицы по п.3, в которых полимерная матрица включает линейный или разветвленный полилактид-со-гликолид.
5. Микрочастицы по п.4, в которых полимерная матрица включает по меньшей мере два различных полимера.
6. Микрочастицы по п.4, дополнительно включающие поверхностно-активное вещество, агент, влияющий на пористость, и/или основную соль.
7. Фармацевтическая композиция, включающая микрочастицы по любому из предшествующих пунктов и носитель на водной основе, включающий смачивающий агент.
8. Композиция по п.7, в которой смачивающий агент включает полоксамер и/или полиоксиэтиленовый эфир сорбитана и жирной кислоты.
9. Композиция по любому из пп.7 или 8, в которой носитель включает агент тоничности.
10. Композиция по любому из пп.7 или 8, в которой носитель включает агент, повышающий вязкость.
11. Набор, включающий микрочастицы по любому из пп.1-6 и носитель на водной основе.
12. Применение микрочастиц по любому из пп.1-6 или фармацевтической композиции по любому из пп.7-10 для приготовления лекарственного препарата для лечения заболевания или нарушения с этиологией, включающей или ассоциированной с избыточной секрецией GH и/или IGF-1.
13. Способ лечения заболевания или нарушения с этиологией, включающей или ассоциированной с избыточной секрецией GH и/или IGF-1 нуждающегося в этом субъекта, включающий введение субъекту микрочастиц по любому из пп.1-6 или фармацевтической композиции по любому из пп.7-10.
RU2006120484/15A 2003-11-14 2004-11-12 Микрочастицы, содержащие аналоги соматостатина RU2404749C2 (ru)

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GB0326602.0 2003-11-14
GB0326602A GB0326602D0 (en) 2003-11-14 2003-11-14 Organic compounds
GB0406241.0 2004-03-19
GB0406241A GB0406241D0 (en) 2004-03-19 2004-03-19 Organic compounds

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AU2004289055B2 (en) 2008-10-30
SI1686964T1 (sl) 2010-05-31
KR101233892B1 (ko) 2013-02-18
PE20050581A1 (es) 2005-09-09
DE602004025271D1 (de) 2010-03-11
HK1093682A1 (en) 2007-03-09
DK1686964T3 (da) 2010-05-17
US8188037B2 (en) 2012-05-29
NO337172B1 (no) 2016-02-01
NO2016003I2 (no) 2016-02-02
AU2004289055C1 (en) 2009-05-21
TWI295178B (en) 2008-04-01
JP4682145B2 (ja) 2011-05-11
IS8480A (is) 2006-05-23
JP2007511482A (ja) 2007-05-10
NO2016003I1 (no) 2016-02-02
EP1686964B1 (en) 2010-01-20
BRPI0416227B8 (pt) 2021-05-25
CY2015011I2 (el) 2016-04-13
PT1686964E (pt) 2010-02-04
IL175286A (en) 2012-05-31
BRPI0416227A (pt) 2007-01-02
ATE455537T1 (de) 2010-02-15
ES2339026T3 (es) 2010-05-14
CY2015011I1 (el) 2016-04-13
EP1686964A1 (en) 2006-08-09
US20070212418A1 (en) 2007-09-13
BRPI0416227B1 (pt) 2019-06-18
TW200529883A (en) 2005-09-16
US20100272809A1 (en) 2010-10-28
CA2541944C (en) 2014-02-25
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RU2404749C2 (ru) 2010-11-27
PL1686964T3 (pl) 2010-06-30
ECSP066565A (es) 2006-10-17
KR20060115873A (ko) 2006-11-10
LU92701I2 (fr) 2015-11-02
AU2004289055A1 (en) 2005-05-26
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