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RU2018125296A - Фармацевтические композиции для лечения диабета - Google Patents

Фармацевтические композиции для лечения диабета Download PDF

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RU2018125296A
RU2018125296A RU2018125296A RU2018125296A RU2018125296A RU 2018125296 A RU2018125296 A RU 2018125296A RU 2018125296 A RU2018125296 A RU 2018125296A RU 2018125296 A RU2018125296 A RU 2018125296A RU 2018125296 A RU2018125296 A RU 2018125296A
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arg
aib
phe
pglu
glu
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RU2018125296A
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RU2018125296A3 (ru
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РОЗА Марио ДЕ
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Калейде Фармасьютикалз Аг
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Publication of RU2018125296A3 publication Critical patent/RU2018125296A3/ru

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07Tetrapeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K38/28Insulins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0021Intradermal administration, e.g. through microneedle arrays, needleless injectors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1019Tetrapeptides with the first amino acid being basic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1021Tetrapeptides with the first amino acid being acidic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Zoology (AREA)
  • Dermatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Ophthalmology & Optometry (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Claims (15)

1. Применение пептида общей формулы (I):
L1-X1-X2-X3-X4,
где:
L1 представляет собой Н, или ацил, или возможно N-ацилированную и/или N-алкилированную и/или Сα-алкилированную аминокислоту, выбранную из Glu, Gln, Pro, гидрокси-Pro, Azt (азетидиновая кислота), Pip (пипеколиновая кислота), pGlu (пироглутаминовая кислота), Aib (α-амино-изомасляная кислота), Ас4с (1-аминоциклобутан-1-карбоновая кислота), Ас5с (1-аминоциклопентан-1-карбоновая кислота), Ас6с (1-аминоциклогексан-1-карбоновая кислота);
X1 и Х3, которые могут быть одинаковыми или разными, представляют собой возможно N-алкилированную и/или Сα-алкилированную основную аминокислоту, выбранную из Arg, Orn и возможно гуанидилированного Lys, и фенилаланинов, замещенных в мета или пара положениях аминогруппой или гуанидиновой группой;
Х2 представляет собой возможно N-алкилированную аминокислоту, выбранную из Glu, Lys, α-метил-лейцина, α-метил-валина, α-метил-глутаминовой кислоты, Aib, Ас4с, Ас5с, Ас6с;
Х4 представляет собой гидрофобную аминокислоту, которая амидирована или не амидирована по С-концу и возможно Сα-алкилирована, выбранную из Phe, h-Phe (гомофенилаланин), Tyr, Trp, 1-Nal (β-1-нафтил-аланин), 2-Nal (β-2-нафтил-аланин), h-1-Nal (гомо-β-1-нафтил-аланин), h-2-Nal (гомо-β-2-нафтил-аланин), Cha (циклогексил-аланин), Chg (циклогексил-глицин), Phg (фенил-глицин);
и его солей в комбинации с инсулином для лечения глазных патологий, ассоциированных с диабетом.
2. Применение по п. 1, где пептид выбран из Ac-Arg-Glu-Arg-Phe-NH2; pGlu-Arg-Glu-Arg-Tyr-OH; Glu-Arg-Glu-Arg-Phe-NH2; Ac-Arg-Glu-Arg-Tyr-NH2; Ac-Arg-Glu-Arg-Trp-NH2; Ac-Arg-Glu-N(Me)Arg-Phe-NH2; Ac-Arg-Glu-N(Me)Arg-Tyr-NH2; Ac-Arg-Glu-N(Me)Arg-Trp-NH2; pGlu-Arg-Glu-N(Me)Arg-Phe-NH2; pGlu-Arg-Glu-N(Me)Arg-Tyr-NH2; pGlu-Arg-Glu-N(Me)Arg-Trp-NH2; pGlu-Arg-Glu-Arg-Phe-NH2; pGlu-Arg-Glu-Arg-Tyr-NH2; pGlu-Arg-Glu-Arg-Trp-NH2; Ac-Arg-Aib-Arg-Phe-NH2; Ac-Arg-Aib-Arg-Tyr-NH2; Ac-Arg-Aib-Arg-Trp-NH2; Ac-Aib-Arg-Aib-Arg-Phe-NH2; Ac-Arg-Aib-N(Me)Arg-Phe-NH2; Ac-Arg-Aib-N(Me)Arg-Tyr-NH2; Ac-Arg-Aib-N(Me)Arg-Trp-NH2; pGlu-Arg-Aib-N(Me)Arg-Phe-NH2; Glu-Arg-Aib-N(Me)Arg-Tyr-NH2; pGlu-Arg-Aib-N(Me)Arg-Trp-NH2; pGlu-Arg-Aib-Arg-Phe-NH2; pGlu-Arg-Aib-Arg-Tyr-NH2; pGlu-Arg-Aib-Arg-Trp-NH2; Ac-Arg-Ac5c-Arg-Phe-NH2; Ac-Arg-Ac5c-Arg-Tyr-NH2; Ac-Arg-Ac5c-Arg-Trp-NH2; Ac-Arg-Ac5c-N(Me)Arg-Phe-NH2; Ac-Arg-Ac5c-N(Me)Arg-Tyr-NH2; Ac-Arg-Ac5c-N(Me)Arg-Trp-NH2; pGlu-Arg-Ac5c-N(Me)Arg-Phe-NH2; pGlu-Arg-Ac5c-N(Me)Arg-Tyr-NH2; pGlu-Arg-Ac5c-N(Me)Arg-Trp-NH2; pGlu-Arg-Ac5c-Arg-Phe-NH2; pGlu-Arg-Ac5c-Arg-Tyr-NH2; pGlu-Arg-Ac5c-Arg-Trp-NH2; Ac-Arg-Glu-Arg-Phe-OH; Ac-Arg-Glu-Arg-Tyr-OH; Ac-Arg-Glu-Arg-Trp-ОН; Ac-Arg-Glu-N(Me)Arg-Tyr-OH; pGlu-Arg-Glu-N(Me)Arg-Phe-OH; pGlu-Arg-Glu-Arg-Trp-ОН; Ac-Arg-Aib-Arg-Phe-OH; Ac-Arg-Aib-N(Me)Arg-Phe-OH; pGlu-Arg-Aib-N(Me)Arg-Tyr-OH; pGlu-Arg-Aib-Arg-Тrp-ОН; Ac-Arg-Ac5c-Arg-Phe-OH; Ac-Arg-Ac5c-N(Me)Arg-Tyr-OH; pGlu-Arg-Ac5c-N(Me)Arg-Trp-OH; pGlu-Arg-Ac5c-Arg-Trp-ОН; Ac-N(Me)Arg-Aib-Arg-Phe-NH2; Ac-N(Me)Arg-Aib-N(Me)Arg-Phe-NH2; Ac-Arg-Aib-N(Me)Arg-Phe-NH2; Ac-Arg-Aib-Arg-α(Me)Phe-NH2; Ac-N(Me)Arg-Aib-Arg-α(Me)Phe-NH2; Ac-N(Me)Arg-Aib-N(Me)Arg-α(Me)Phe-NH2; Ac-Arg-Aib-N(Me)Arg-α(Me)Phe-NH2; Ac-Aib-N(Me)Arg-Aib-Arg-Phe-NH2; Ac-Aib-N(Me)Arg-Aib-N(Me)Arg-Phe-NH2; Ac-Aib-Arg-Aib-N(Me)Arg-Phe-NH2; Ac-Aib-Arg-Aib-Arg-α(Me)Phe-NH2; Ac-Aib-N(Me)Arg-Aib-Arg-α(Me)Phe-NH2; Ac-Aib-N(Me)Arg-Aib-N(Me)Arg-α(Me)Phe-NH2; Ac-Aib-Arg-Aib-N(Me)Arg-α(Me)Phe-NH2 или их солей.
3. Применение по п. 1, где пептид выбран из Ac-Arg-Aib-Arg-α(Me)Phe-NH2 или Ac-Aib-Arg-Aib-Arg-α(Me)Phe-NH2 или их солей.
4. Фармацевтическая композиция, содержащая комбинацию пептида, как он определен по любому из пп. 1-3, и инсулина в форме, подходящей для раздельного, одновременного или последовательного введения.
5. Фармацевтическая композиция по п. 4 для применения в лечении осложнений диабета, в частности диабетической ретинопатии.
6. Фармацевтическая композиция по п. 4 или 5, содержащая единичную дозу пептида в диапазоне от 1 до 200 мг в комбинации со стандартными дозами инсулина.
7. Фармацевтическая композиция по п. 4 или 5, подходящая для введения подкожным, внутримышечным, внутривенным, пероральным, назальным, сублингвальным, местным, аэрозольным или трансдермальным путем или посредством ингаляции.
8. Фармацевтическая композиция по п. 7, подходящая для подкожного введения.
RU2018125296A 2016-01-12 2017-01-11 Фармацевтические композиции для лечения диабета RU2018125296A (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
ITUB2016A009928A ITUB20169928A1 (it) 2016-01-12 2016-01-12 Formulazioni farmaceutiche per il trattamento del diabete
IT102016000002015 2016-01-12
PCT/EP2017/050495 WO2017121764A1 (en) 2016-01-12 2017-01-11 Pharmaceutical formulations for the treatment of diabetes

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RU2018125296A3 RU2018125296A3 (ru) 2020-05-13

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US (1) US20180326014A1 (ru)
EP (1) EP3402505B1 (ru)
JP (1) JP2019504007A (ru)
KR (1) KR20180102091A (ru)
CN (1) CN108463238A (ru)
AU (1) AU2017206624A1 (ru)
CA (1) CA3011062A1 (ru)
HK (1) HK1259373A1 (ru)
IL (1) IL260512B (ru)
IT (1) ITUB20169928A1 (ru)
RU (1) RU2018125296A (ru)
WO (1) WO2017121764A1 (ru)
ZA (1) ZA201804588B (ru)

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Publication number Priority date Publication date Assignee Title
US20250213658A1 (en) * 2022-04-01 2025-07-03 Wake Forest University Health Sciences Methods and formulations for intranasal delivery of insulin in the treatment of diabetic eye disease
IT202200007754A1 (it) 2022-04-19 2023-10-19 Iridea S R L Nuovi composti con attivita’ farmacologica

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AUPQ661800A0 (en) * 2000-03-31 2000-05-04 Metabolic Pharmaceuticals Limited Insulin-potentiating compounds
AU2002245333A1 (en) * 2001-01-31 2002-08-12 Colorado State University Research Foundation Method for treatment of diabetic retinopathy with naturally occurring insulin-like growth factors (igfs) and igf analogs
DE602004004883T2 (de) * 2003-03-28 2007-11-15 Regeneron Pharmaceuticals, Inc. Vegf-antagonisten zur behandlung von diabetes
ITMI20061607A1 (it) * 2006-08-09 2008-02-10 Maria Vincenza Carriero Peptidi con attivita farmacologica

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EP3402505A1 (en) 2018-11-21
AU2017206624A1 (en) 2018-07-26
RU2018125296A3 (ru) 2020-05-13
KR20180102091A (ko) 2018-09-14
CN108463238A (zh) 2018-08-28
JP2019504007A (ja) 2019-02-14
EP3402505B1 (en) 2020-06-17
ITUB20169928A1 (it) 2017-07-12
IL260512B (en) 2020-04-30
ZA201804588B (en) 2019-09-25
CA3011062A1 (en) 2017-07-20
HK1259373A1 (zh) 2019-11-29
WO2017121764A1 (en) 2017-07-20
US20180326014A1 (en) 2018-11-15

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