RU2003136759A - Пролекарства ингибиторов дипептидилпептидазы iv - Google Patents

Пролекарства ингибиторов дипептидилпептидазы iv Download PDF

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Publication number
RU2003136759A
RU2003136759A RU2003136759/04A RU2003136759A RU2003136759A RU 2003136759 A RU2003136759 A RU 2003136759A RU 2003136759/04 A RU2003136759/04 A RU 2003136759/04A RU 2003136759 A RU2003136759 A RU 2003136759A RU 2003136759 A RU2003136759 A RU 2003136759A
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pro
ile
val
pyrr
thia
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RU2003136759/04A
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Ханс-Ульрих ДЕМУТ (DE)
Ханс-Ульрих Демут
Торстен ХОФФМАНН (DE)
Торстен Хоффманн
Дагмар ШЛЕНЦИГ (DE)
Дагмар ШЛЕНЦИГ
Зузанне МАНХАРТ ( DE)
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Пробиодруг Аг (De)
Пробиодруг Аг
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Publication of RU2003136759A publication Critical patent/RU2003136759A/ru

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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
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; 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
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06173—Dipeptides with the first amino acid being heterocyclic and Glp-amino acid; 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
    • C07K5/04—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
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • 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
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • 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
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C07K5/0823—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp and Pro-amino acid; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Claims (18)

1. Соединения-пролекарства ингибиторов дипептидилпептидазы IV (ДП IV) общей формулы А-В-С, при этом
А выбран из группы, включающей Ile, Val, Phe, Pro, Ala, Gly и pGlu,
В обозначает химическую связь между А и С или аминокислоту и
С обозначает стабильный ингибитор ДП IV, выбранный из группы, включающей Ile-Thia, Ile-Pyrr, Val-Thia и Val-Pyrr.
2. Соединения-пролекарства по п. 1, в которых В представляет собой химическую связь между А и С или пролин.
3. Соединения-пролекарства по п.1 или 2, представляющие собой Ile-Pro-Ile-Thia, Pro-Pro-Ile-Thia, Gly-Pro-Ile-Thia, pGlu-Ile-Thia, Pro-Ile-Thia и Ala-Ile-Thia.
4. Соединения-пролекарства по п.1 или 2, представляющие собой Ile-Pro-Ile-Pyrr, Pro-Pro-Ile-Pyrr, Gly-Pro-Ile- Pyrr, pGlu-Ile-Pyrr, Pro-Ile-Pyrr и Ala-Ile-Pyrr.
5. Соединения-пролекарства по п.1 или 2, представляющие собой Ile-Pro-Val-Thia, Pro-Pro-Val-Thia, Gly-Pro-Val-Thia, pGlu-Val-Thia, Pro-Val-Thia и Ala-Val-Thia.
6. Соединения-пролекарства по п.1 или 2, представляющие собой Ile-Pro-Val-Pyrr, Pro-Pro-Val-Pyrr, Gly-Pro-Val- Pyrr, pGlu-Val-Pyrr, Pro-Val-Pyrr и Ala-Val-Pyrr.
7. Соединения-пролекарства по одному из предыдущих пунктов, в которых ингибиторы находятся в виде соли.
8. Фармацевтическая композиция, в частности, для орального введения, отличающаяся тем, что она содержит по меньшей мере одно соединение-пролекарство по одному из предыдущих пунктов в случае необходимости в комбинации с обычными носителями или вспомогательными веществами.
9. Применение соединений-пролекарств по одному из пп.1-7 для приготовления лекарственного средства для регулируемого во времени ингибирования ДП IV in vivo.
10. Применение по п.9 для клеточного, тканевого или органоспецифического ингибирования ДП IV.
11. Применение по п.9 для лечения заболеваний млекопитающих, излечиваемых модуляцией ДП IV-активности.
12. Применение по п.10 для лечения обменных заболеваний людей.
13. Применение по п.10 для лечения нарушенной толерантности к глюкозе, глюкозурии, гиперлипидемии, метаболических ацидозов, сахарного диабета, диабетической невропатии и нефропатии, а также обусловленных сахарным диабетом осложнений млекопитающих.
14. Применение фармацевтических композиций по п.8 для приготовления лекарственного средства для регулируемого во времени ингибирования ДП IV in vivo.
15. Применение по п.14 для клеточного, тканевого или органоспецифического ингибирования ДП IV.
16. Применение по п.14 для лечения заболеваний млекопитающих, излечиваемых модуляцией ДП IV-активности.
17. Применение по п.16 для лечения обменных заболеваний людей.
18. Применение по п.16 для лечения нарушенной толерантности к глюкозе, глюкозурии, гиперлипидемии, метаболических ацидозов, сахарного диабета, диабетической невропатии и нефропатии, а также обусловленных сахарным диабетом осложнений млекопитающих.
RU2003136759/04A 1998-06-24 2003-12-18 Пролекарства ингибиторов дипептидилпептидазы iv RU2003136759A (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19828113.7 1998-06-24
DE19828113A DE19828113A1 (de) 1998-06-24 1998-06-24 Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV

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RU2001102058/04A Division RU2226533C2 (ru) 1998-06-24 1999-06-24 Пролекарства ингибиторов дипептидилпептидазы iv

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RU2003136759A true RU2003136759A (ru) 2005-05-27

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RU2001102058/04A RU2226533C2 (ru) 1998-06-24 1999-06-24 Пролекарства ингибиторов дипептидилпептидазы iv
RU2003136759/04A RU2003136759A (ru) 1998-06-24 2003-12-18 Пролекарства ингибиторов дипептидилпептидазы iv

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US (2) US7084120B2 (ru)
EP (1) EP1087991B1 (ru)
JP (1) JP4088419B2 (ru)
KR (1) KR100529816B1 (ru)
CN (1) CN1245417C (ru)
AT (1) ATE441660T1 (ru)
AU (1) AU766726C (ru)
BR (1) BR9911468A (ru)
CA (1) CA2335992A1 (ru)
DE (2) DE19828113A1 (ru)
HU (1) HUP0102281A3 (ru)
IL (1) IL140336A0 (ru)
NO (1) NO20006484D0 (ru)
NZ (1) NZ508722A (ru)
PL (1) PL345151A1 (ru)
RU (2) RU2226533C2 (ru)
WO (1) WO1999067278A1 (ru)

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DE59915073D1 (de) 2009-10-15
HUP0102281A2 (hu) 2001-11-28
KR20010071579A (ko) 2001-07-28
CN1245417C (zh) 2006-03-15
NO20006484L (no) 2000-12-19
ATE441660T1 (de) 2009-09-15
EP1087991A1 (de) 2001-04-04
AU4900799A (en) 2000-01-10
US20020049164A1 (en) 2002-04-25
JP4088419B2 (ja) 2008-05-21
KR100529816B1 (ko) 2005-11-22
NO20006484D0 (no) 2000-12-19
US20040171555A1 (en) 2004-09-02
AU766726B2 (en) 2003-10-23
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JP2003524591A (ja) 2003-08-19
IL140336A0 (en) 2002-02-10
DE19828113A1 (de) 2000-01-05
CN1306540A (zh) 2001-08-01
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US7166579B2 (en) 2007-01-23
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CA2335992A1 (en) 1999-12-29
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