RU2227800C2 - Новые эффекторы дипептидилпептидазы iv - Google Patents
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- A61K31/425—Thiazoles
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P3/06—Antihyperlipidemics
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- 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
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- A—HUMAN NECESSITIES
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- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/04—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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Abstract
Изобретение относится к новым эффекторам дипептидилпептидазы IV - дипептидным миметикам (I), образованным из аминокислоты и тиазолидиновой или пирролидиновой группы, а именно: L-алло-изолейцил-тиазолидину, L-алло-изолейцил-пирролидину и их солям, к солям L-трео-изолейцил-тиазолидина и L - трео-изолейцил-пирролидина; фармацевтической композиции, обладающей способностью снижать сахар в крови, содержащей, по меньшей мере, одно из названных выше соединений (1). 3 с. и 17 з.п. ф-лы, 4 ил., 3 табл.
Description
Текст описания в факсимильном виде (см. графическую часть).
Claims (20)
1. Дипептидные миметики, образованные из аминокислоты и тиазолидиновой или пирролидиновой группы, а именно L-алло-изолейцил-тиазолидин, L-алло-изолейцил-пирролидин и их соли.
2. Дипептидные миметики по п.1, отличающиеся тем, что соли представляют собой органические соли, такие как ацетат, сукцинат, тартрат или фумарат, или содержат неорганические кислотные остатки, такие как фосфат или сульфат.
3. Дипептидные миметики по одному из п.1 или 2, отличающиеся тем, что они представляют собой соли с молярным соотношением дипептидного компонента и солевого компонента 1:1 или 2:1.
4. Дипептидные миметики по одному из предыдущих пунктов, представляющие собой соли фумаровой кислоты.
5. Дипептидные миметики по п.4, представляющие собой соль фумаровой кислоты L-алло-изолейцил-тиазолидина.
6. Соли дипептидных миметиков, образованные из аминокислоты и тиазолидиновой или пирролидиновой группы, а именно соли L-трео-изолейцил-тиазолидина и L-трео-изолейцил-пирролидина.
7. Соли по п.6, представляющие собой органические соли.
8. Соли по п.6, представляющие собой сукцинат, тартрат, фумарат и гидрохлорид.
9. Фармацевтическая композиция, обладающая способностью снижения сахара в крови, содержащая по меньшей мере одно соединение по одному из предыдущих пунктов, в случае необходимости в комбинации с одним или несколькими фармацевтически приемлемыми носителями и/или разбавителями.
10. Фармацевтическая композиция по п.9, отличающаяся тем, что она содержит носитель для парентеральных или энтеральных препаративных форм.
11. Фармацевтическая композиция по п.9, отличающаяся тем, что она представляет собой препаративную форму для перорального введения.
12. Фармацевтическая композиция по одному из пп.9-11, отличающаяся тем, что она содержит дополнительно гипогликемически действующее активное вещество.
13. Соединения по одному из пп.1-8 для приготовления лекарственного средства для уменьшения активности фермента дипептидилпептидазы IV или дипептидилпептидаза IV-аналогичной ферментативной активности.
14. Соединения по одному из пп.1-8 для приготовления лекарственного средства для снижения содержания сахара в крови при характерной для гипергликемии концентрации глюкозы в сыворотке млекопитающего.
15. Соединения по одному из пп.1-8 для приготовления лекарственного средства для лечения посредством перорального введения обменных заболеваний, связанных с сахарным диабетом.
16. Соединения по одному из пп.1-8 для приготовления лекарственного средства для лечения нарушенной толерантности к глюкозе, глюкозурии, гиперлипемии, метаболических ацидозов, сахарного диабета, диабетической невропатии и нефропатии, а также вызываемых сахарным диабетом осложнений млекопитающих.
17. Фармацевтическая композиция по одному из пп.9-12, уменьшающая активность фермента дипептидилпептидазы IV или дипептидилпептидаза IV-аналогичной ферментативной активности.
18. Фармацевтическая композиция по одному из пп.9-12 для снижения содержания сахара в крови при характерной для гипергликемии концентрации глюкозы в сыворотке млекопитающего.
19. Фармацевтическая композиция по одному из пп.9-12 для лечения посредством перорального введения обменных заболеваний, связанных с сахарным диабетом.
20. Фармацевтическая композиция по одному из пп.9-12 для лечения нарушенной толерантности к глюкозе, глюкозурии, гиперлипемии, метаболических ацидозов, сахарного диабета, диабетической невропатии и нефропатии, а также вызываемых сахарным диабетом осложнений млекопитающих.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19823831.2 | 1998-05-28 | ||
DE19823831A DE19823831A1 (de) | 1998-05-28 | 1998-05-28 | Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen |
Related Child Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2003121766/04A Division RU2309161C2 (ru) | 1998-05-28 | 1999-05-28 | Эффекторы дипептидилпептидазу iv |
RU2004101292/15A Division RU2004101292A (ru) | 1998-05-28 | 2004-01-15 | Композиции, содержащие эффектор дипептидилпептидазы iv |
Publications (2)
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RU2000133251A RU2000133251A (ru) | 2003-01-27 |
RU2227800C2 true RU2227800C2 (ru) | 2004-04-27 |
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Application Number | Title | Priority Date | Filing Date |
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RU2000133251/04A RU2227800C2 (ru) | 1998-05-28 | 1999-05-28 | Новые эффекторы дипептидилпептидазы iv |
RU2003121766/04A RU2309161C2 (ru) | 1998-05-28 | 1999-05-28 | Эффекторы дипептидилпептидазу iv |
RU2004101292/15A RU2004101292A (ru) | 1998-05-28 | 2004-01-15 | Композиции, содержащие эффектор дипептидилпептидазы iv |
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RU2003121766/04A RU2309161C2 (ru) | 1998-05-28 | 1999-05-28 | Эффекторы дипептидилпептидазу iv |
RU2004101292/15A RU2004101292A (ru) | 1998-05-28 | 2004-01-15 | Композиции, содержащие эффектор дипептидилпептидазы iv |
Country Status (24)
Country | Link |
---|---|
US (4) | US6548481B1 (ru) |
EP (6) | EP1082314B1 (ru) |
JP (1) | JP2002516318A (ru) |
KR (2) | KR100630258B1 (ru) |
CN (4) | CN1637018A (ru) |
AT (6) | ATE338546T1 (ru) |
AU (1) | AU764262B2 (ru) |
BR (1) | BR9910758A (ru) |
CA (1) | CA2333603C (ru) |
DE (10) | DE19823831A1 (ru) |
DK (2) | DK1304327T3 (ru) |
ES (5) | ES2271458T3 (ru) |
HK (3) | HK1033316A1 (ru) |
HU (1) | HUP0102001A3 (ru) |
IL (3) | IL139862A0 (ru) |
IS (3) | IS5728A (ru) |
NO (1) | NO317989B1 (ru) |
NZ (2) | NZ525799A (ru) |
PL (1) | PL344403A1 (ru) |
PT (2) | PT1214936E (ru) |
RU (3) | RU2227800C2 (ru) |
SI (2) | SI1082314T1 (ru) |
UA (1) | UA54599C2 (ru) |
WO (1) | WO1999061431A1 (ru) |
Families Citing this family (242)
Publication number | Priority date | Publication date | Assignee | Title |
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US20020006899A1 (en) * | 1998-10-06 | 2002-01-17 | Pospisilik Andrew J. | Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals |
ES2285785T3 (es) * | 1997-09-29 | 2007-11-16 | Point Therapeutics, Inc. | Estimulacion de celulas hematopoyeticas in vitro. |
DE19823831A1 (de) * | 1998-05-28 | 1999-12-02 | Probiodrug Ges Fuer Arzneim | Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen |
DE19828113A1 (de) | 1998-06-24 | 2000-01-05 | Probiodrug Ges Fuer Arzneim | Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV |
DE19834591A1 (de) * | 1998-07-31 | 2000-02-03 | Probiodrug Ges Fuer Arzneim | Verfahren zur Steigerung des Blutglukosespiegels in Säugern |
US6979697B1 (en) | 1998-08-21 | 2005-12-27 | Point Therapeutics, Inc. | Regulation of substrate activity |
US20030176357A1 (en) * | 1998-10-06 | 2003-09-18 | Pospisilik Andrew J. | Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels |
WO2000053171A1 (en) * | 1999-03-05 | 2000-09-14 | Molteni L. E C. Dei Fratelli Alitti Societa' Di Esercizio S.P.A. | Use of metformin in the preparation of pharmaceutical compositions capable of inhibiting the enzyme dipeptidyl peptidase iv |
US6548529B1 (en) | 1999-04-05 | 2003-04-15 | Bristol-Myers Squibb Company | Heterocyclic containing biphenyl aP2 inhibitors and method |
US6890904B1 (en) * | 1999-05-25 | 2005-05-10 | Point Therapeutics, Inc. | Anti-tumor agents |
DE19940130A1 (de) * | 1999-08-24 | 2001-03-01 | Probiodrug Ges Fuer Arzneim | Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung |
JP2003534239A (ja) * | 1999-12-17 | 2003-11-18 | ヴァージコア・インコーポレーテッド | 新規なスクシナート化合物、組成物、並びに使用及び調製方法 |
US20080076811A1 (en) * | 2000-01-21 | 2008-03-27 | Bork Balkan | Combinations comprising depeptidypeptidase-iv inhibitors and antidiabetic agents |
DE122008000018I1 (de) * | 2000-01-21 | 2008-08-14 | Novartis Pharma Ag | Zusammensetzungen bestehend aus Dipeptidylpeptidase-IV Inhibitoren und Antidiabetica |
AU2001233622A1 (en) * | 2000-02-25 | 2001-09-03 | Novo-Nordisk A/S | Inhibition of beta cell degeneration |
WO2001072290A2 (en) * | 2000-03-31 | 2001-10-04 | Probiodrug Ag | Method for the improvement of islet signaling in diabetes mellitus and for its prevention |
GB0010183D0 (en) * | 2000-04-26 | 2000-06-14 | Ferring Bv | Inhibitors of dipeptidyl peptidase IV |
US7078397B2 (en) | 2000-06-19 | 2006-07-18 | Smithkline Beecham Corporation | Combinations of dipeptidyl peptidase IV inhibitors and other antidiabetic agents for the treatment of diabetes mellitus |
GB0014969D0 (en) | 2000-06-19 | 2000-08-09 | Smithkline Beecham Plc | Novel method of treatment |
NZ524618A (en) | 2000-08-10 | 2004-08-27 | Mitsubishi Pharma Corp | Proline derivatives and use thereof as drugs |
IL155157A0 (en) * | 2000-10-27 | 2003-10-31 | Probiodrug Ag | Pharmaceutical compositions containing an attractin inhibitor |
US7132104B1 (en) | 2000-10-27 | 2006-11-07 | Probiodrug Ag | Modulation of central nervous system (CNS) dipeptidyl peptidase IV (DPIV) -like activity for the treatment of neurological and neuropsychological disorders |
EP1891948A1 (en) * | 2000-10-27 | 2008-02-27 | Probiodrug AG | Treatment of neurological and neuropsychological disorders |
EP1354882A1 (en) * | 2000-12-27 | 2003-10-22 | Kyowa Hakko Kogyo Co., Ltd. | Dipeptidyl peptidase iv inhibitor |
MEP59808A (en) * | 2001-02-24 | 2011-05-10 | Boehringer Ingelheim Pharma | Xanthine derivative, production and use thereof as a medicament |
US20070293426A1 (en) * | 2001-04-02 | 2007-12-20 | Hans-Ulrich Demuth | Methods for improving islet signaling in diabetes mellitus and for its prevention |
US6890905B2 (en) | 2001-04-02 | 2005-05-10 | Prosidion Limited | Methods for improving islet signaling in diabetes mellitus and for its prevention |
GB0109146D0 (en) * | 2001-04-11 | 2001-05-30 | Ferring Bv | Treatment of type 2 diabetes |
HUP0600232A2 (en) | 2001-04-11 | 2006-08-28 | Bristol Myers Squibb Co | Amino acid complexes of c-aryl glucosides for treatment of diabetes and method |
US6944925B2 (en) * | 2001-06-13 | 2005-09-20 | Ttx Company | Articulated connector reconditioning process and apparatuses |
CA2418543A1 (en) * | 2001-06-27 | 2003-01-09 | Probiodrug Ag | New dipeptidyl peptidase iv inhibitors and their uses as anti-cancer agents |
ES2339813T3 (es) * | 2001-06-27 | 2010-05-25 | Glaxosmithkline Llc | Fluoropirrolidinas como inhibidores de dipeptidil peptidasas. |
DE10150203A1 (de) | 2001-10-12 | 2003-04-17 | Probiodrug Ag | Peptidylketone als Inhibitoren der DPIV |
ES2291477T3 (es) | 2001-06-27 | 2008-03-01 | Smithkline Beecham Corporation | Fluoropirrolidinas como inhibidores de dipeptidil peptidasa. |
US7196201B2 (en) | 2001-06-27 | 2007-03-27 | Smithkline Beecham Corporation | Pyrrolidines as dipeptidyl peptidase inhibitors |
US7368421B2 (en) | 2001-06-27 | 2008-05-06 | Probiodrug Ag | Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis |
US20030130199A1 (en) | 2001-06-27 | 2003-07-10 | Von Hoersten Stephan | Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents |
UA74912C2 (en) | 2001-07-06 | 2006-02-15 | Merck & Co Inc | Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes |
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2001
- 2001-06-11 HK HK01103972A patent/HK1033316A1/xx not_active IP Right Cessation
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2002
- 2002-12-06 HK HK02108901.9A patent/HK1047887B/zh not_active IP Right Cessation
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2003
- 2003-02-10 US US10/361,956 patent/US20030134802A1/en not_active Abandoned
- 2003-07-14 HK HK03105067.4A patent/HK1052708B/zh not_active IP Right Cessation
- 2003-12-02 US US10/727,209 patent/US20050203030A1/en not_active Abandoned
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2004
- 2004-01-15 RU RU2004101292/15A patent/RU2004101292A/ru not_active Application Discontinuation
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2005
- 2005-03-21 IS IS7764A patent/IS2130B/xx unknown
- 2005-03-21 IS IS7763A patent/IS2089B/is unknown
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2006
- 2006-05-04 IL IL175407A patent/IL175407A0/en unknown
- 2006-05-30 US US11/443,389 patent/US20080182798A1/en not_active Abandoned
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