RU2001102058A - Пролекарства ингибиторов дипептидилпептидазы iv - Google Patents

Пролекарства ингибиторов дипептидилпептидазы iv

Info

Publication number
RU2001102058A
RU2001102058A RU2001102058/04A RU2001102058A RU2001102058A RU 2001102058 A RU2001102058 A RU 2001102058A RU 2001102058/04 A RU2001102058/04 A RU 2001102058/04A RU 2001102058 A RU2001102058 A RU 2001102058A RU 2001102058 A RU2001102058 A RU 2001102058A
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RU
Russia
Prior art keywords
prodrug compounds
pharmaceutical composition
treatment
composition according
preceding paragraphs
Prior art date
Application number
RU2001102058/04A
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English (en)
Other versions
RU2226533C2 (ru
Inventor
Ханс-Ульрих Демут
Торстен Хоффманн
Дагмар ШЛЕНЦИГ
Зузанне МАНХАРТ
Original Assignee
Пробиодруг Аг
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Priority claimed from DE19828113A external-priority patent/DE19828113A1/de
Application filed by Пробиодруг Аг filed Critical Пробиодруг Аг
Publication of RU2001102058A publication Critical patent/RU2001102058A/ru
Application granted granted Critical
Publication of RU2226533C2 publication Critical patent/RU2226533C2/ru

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Claims (17)

1. Соединения-пролекарства ингибиторов дипептидилпептидазы IV (ДП IV) общей формулы
А-В-С,
где А обозначает аминокислоту;
В обозначает химическую связь между А и С или аминокислоту;
С обозначает стабильный ингибитор ДП IV с отсутствующим С-концевым фосфонатным остатком.
2. Соединения-пролекарства по п.1, отличающиеся тем, что В представляет собой пролин, гидроксипролин, тиазолидинкарбоновую кислоту, дегидропролин, пипеколиновую кислоту, азетидинкарбоновую кислоту или азиридинкарбоновую кислоту.
3. Соединения-пролекарства по п.1 или 2, отличающиеся тем, что В представляет собой пролин, гидроксипролин.
4. Соединения-пролекарства по одному из предыдущих пунктов, отличающиеся тем, что С представляет собой аминоацилпирролидин, аминоацилтиазолидин или N-дипептидил, O-ацилгидроксиламин.
5. Соединения-пролекарства по одному из предыдущих пунктов, отличающиеся тем, что ингибиторы находятся в виде соли.
6. Соединения-пролекарства по одному из предыдущих пунктов, отличающиеся тем, что А-В представляет собой дипептид формулы Ile-Pro или Gly-Pro.
7. Фармацевтическая композиция, в частности, для перорального 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.
8. Соединения-пролекарства по одному из пп.1-6 для приготовления лекарственного средства для регулируемого во времени ингибирования in vivo ДП IV.
9. Соединения-пролекарства по одному из пп.1-6 для клеточного, тканевого или органоспецифического ингибирования ДП IV.
10. Соединения-пролекарства по одному из пп.1-6 для лечения заболеваний млекопитающих, излечиваемых модуляцией ДП IV-активности.
11. Соединения-пролекарства по п.9 для лечения обменных заболеваний людей.
12. Соединения-пролекарства по п.9 для лечения нарушенной толерантности к глюкозе, глюкозурии, гиперлипидемии, метаболических ацидозов, сахарного диабета, диабетической невропатии и нефропатии, а также обусловленных сахарным диабетом осложнений млекопитающих.
13. Фармацевтическая композиция по п.7 для приготовления лекарственного средства для регулируемого во времени ингибирования in vivo ДП IV.
14. Фармацевтическая композиция по п.7 для клеточного, тканевого или органоспецифического ингибирования ДП IV.
15. Фармацевтическая композиция по п.7 для лечения заболеваний млекопитающих, излечиваемых модуляцией ДП IV-активности.
16. Фармацевтическая композиция по п.9 для лечения обменных заболеваний людей.
17. Фармацевтическая композиция по п.9 для лечения нарушенной толерантности к глюкозе, глюкозурии, гиперлипидемии, метаболических ацидозов, сахарного диабета, диабетической невропатии и нефропатии, а также обусловленных сахарным диабетом осложнений млекопитающих.
RU2001102058/04A 1998-06-24 1999-06-24 Пролекарства ингибиторов дипептидилпептидазы iv RU2226533C2 (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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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) NO20006484L (ru)
NZ (1) NZ508722A (ru)
PL (1) PL345151A1 (ru)
RU (2) RU2226533C2 (ru)
WO (1) WO1999067278A1 (ru)

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