RU2006138431A - Фармацевтические композиции пиримидин-2, 4, 6-трионов - Google Patents
Фармацевтические композиции пиримидин-2, 4, 6-трионов Download PDFInfo
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- RU2006138431A RU2006138431A RU2006138431/15A RU2006138431A RU2006138431A RU 2006138431 A RU2006138431 A RU 2006138431A RU 2006138431/15 A RU2006138431/15 A RU 2006138431/15A RU 2006138431 A RU2006138431 A RU 2006138431A RU 2006138431 A RU2006138431 A RU 2006138431A
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- Prior art keywords
- group
- cyclodextrin
- trioxopyrimidine
- pyrimidin
- complex according
- Prior art date
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- HNYOPLTXPVRDBG-UHFFFAOYSA-N barbituric acid Chemical group O=C1CC(=O)NC(=O)N1 HNYOPLTXPVRDBG-UHFFFAOYSA-N 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 229920000858 Cyclodextrin Polymers 0.000 claims 19
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 claims 3
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- -1 phenyloxy, phenylthio, phenylsulfinyl Chemical group 0.000 claims 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 2
- 239000001116 FEMA 4028 Substances 0.000 claims 2
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 2
- 229960004853 betadex Drugs 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 1
- FMKQJGOROFNCGM-UHFFFAOYSA-N 5-(4-phenoxyphenyl)-5-(4-pyrimidin-2-ylpiperazin-1-yl)pyrimidine-2,4,6(2h,3h)-trione Chemical compound O=C1NC(=O)NC(=O)C1(C=1C=CC(OC=2C=CC=CC=2)=CC=1)N1CCN(C=2N=CC=CN=2)CC1 FMKQJGOROFNCGM-UHFFFAOYSA-N 0.000 claims 1
- OAYYGVNBSZDPFY-UHFFFAOYSA-N 5-[4-(3,4-dichlorophenoxy)phenyl]-5-(4-pyrimidin-2-ylpiperazin-1-yl)-1,3-diazinane-2,4,6-trione Chemical compound C1=C(Cl)C(Cl)=CC=C1OC1=CC=C(C2(N3CCN(CC3)C=3N=CC=CN=3)C(NC(=O)NC2=O)=O)C=C1 OAYYGVNBSZDPFY-UHFFFAOYSA-N 0.000 claims 1
- YEIIPFFTXIWIGO-UHFFFAOYSA-N 5-[4-(4-bromophenoxy)phenyl]-5-(4-pyrimidin-2-ylpiperazin-1-yl)-1,3-diazinane-2,4,6-trione Chemical compound C1=CC(Br)=CC=C1OC1=CC=C(C2(N3CCN(CC3)C=3N=CC=CN=3)C(NC(=O)NC2=O)=O)C=C1 YEIIPFFTXIWIGO-UHFFFAOYSA-N 0.000 claims 1
- WJNLHGBCQYNFAH-UHFFFAOYSA-N 5-[4-(4-chlorophenoxy)phenyl]-5-(4-pyrimidin-2-ylpiperazin-1-yl)-1,3-diazinane-2,4,6-trione Chemical compound C1=CC(Cl)=CC=C1OC1=CC=C(C2(N3CCN(CC3)C=3N=CC=CN=3)C(NC(=O)NC2=O)=O)C=C1 WJNLHGBCQYNFAH-UHFFFAOYSA-N 0.000 claims 1
- NJKTYSXXGARILV-UHFFFAOYSA-N 5-[4-(4-nitrophenyl)piperazin-1-yl]-5-(4-phenylphenyl)-1,3-diazinane-2,4,6-trione Chemical group C1=CC([N+](=O)[O-])=CC=C1N1CCN(C2(C(NC(=O)NC2=O)=O)C=2C=CC(=CC=2)C=2C=CC=CC=2)CC1 NJKTYSXXGARILV-UHFFFAOYSA-N 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 235000019766 L-Lysine Nutrition 0.000 claims 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 claims 1
- 229930064664 L-arginine Natural products 0.000 claims 1
- 235000014852 L-arginine Nutrition 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 claims 1
- 235000011175 beta-cyclodextrine Nutrition 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- GDSRMADSINPKSL-HSEONFRVSA-N gamma-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO GDSRMADSINPKSL-HSEONFRVSA-N 0.000 claims 1
- 229940080345 gamma-cyclodextrin Drugs 0.000 claims 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
- A61K31/515—Barbituric acids; Derivatives thereof, e.g. sodium pentobarbital
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- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
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Claims (10)
1. Комплекс триоксопиримидин-циклодекстрин, образованный из производного триоксопиримидина или его соли и растворимого в воде циклодекстрина, в котором производное триоксопиримидина описывается формулой (I)
в которой R1 обозначает С3-С20алкил, которые необязательно может включать одну или несколько групп -S-, -О- или -NH-; или
группу W-V, в которой
W обозначает химическую связь или фенил; и
V обозначает фенил, фенилоксигруппу, фенилтиогруппу, фенилсульфинил, фенилсульфонил или фениламиногруппу, и эти фенильные фрагменты могут быть незамещенными или один или несколько раз замещенными галогеном, гидроксигруппой, C1-С6алкилом, C1-С6алкоксигруппой, C1-С6-алкилтиогруппой, C1-С6алкилсульфинилом, C1-С6-алкиламиногруппой, цианогруппой, нитрогруппой или C1-С6-алкилсульфонилом; и
R2 обозначает C1-С10алкил, и эта алкильная группа является незамещенной или один или два раза замещенной гидроксигруппой или аминогруппой и необязательно может включать одну или несколько групп -S-, -О- или -NH-; бензоильную группу, которая может быть незамещенной или один или несколько раз замещенной галогеном, гидроксигруппой, нитрогруппой, C1-С6-алкоксигруппой, C1-С6-алкиламиногруппой, C1-С6-алкилтиогруппой, C1-С6-алкилсульфинилом, C1-С6-алкилсульфонилом, амидосульфонилом, C1-С6-алкиламидосульфонилом, бис-C1-С6-алкиламидосульфонилом; гетероароматическую ацильную группу; или
фенильную или гетероарильную группу, которые являются незамещенными или один или несколько раз замещенными галогеном, гидроксигруппой, C1-С6-алкоксигруппой, C1-С6-алкиламиногруппой, C1-С6-диалкиламиногруппой, цианогруппой, C1-С6-алкилом, C2-С6-алкенилом, C2-С6-алкинилом, C1-С6-ацилом, C1-С6-алкилтиогруппой, C1-С6-алкилсульфонилом, C1-С6-алкилсульфинилом, C1-С6-алкиламинокарбонилом, аминокарбонилом, C1-С6-алкиламидосульфонилом, амидосульфонилом, бис-C1-С6-алкиламидосульфонилом, нитрогруппой, C1-С6-алкоксикарбонилом, карбоксигруппой.
2. Комплекс триоксопиримидин-циклодекстрин по п.1, к которому в качестве вспомогательного вещества прибавлен L-лизин или L-аргинин.
3. Комплекс триоксопиримидин-циклодекстрин по п.1, в котором производное триоксопиримидина представляет собой
5-бифенил-4-ил-5-[4-(4-нитрофенил)-пиперазин-1-ил]пиримидин-2,4,6-трион;
5-(4-феноксифенил)-5-(4-пиримидин-2-илпиперазин-1-ил)-пиримидин-2,4,6-трион;
5-[4-(4-хлорфенокси)-фенил]-5-(4-пиримидин-2-илпиперазин-1-ил)-пиримидин-2,4,6-трион;
5-[4-(3,4-дихлорфенокси)-фенил]-5-(4-пиримидин-2-илпиперазин-1-ил)-пиримидин-2,4,6-трион;
5-[4-(4-бромфенокси)-фенил]-5-(4-пиримидин-2-илпиперазин-1-ил)-пиримидин-2,4,6-трион
или его соль.
4. Комплекс триоксопиримидин-циклодекстрин по п.1, в котором растворимым в воде циклодекстрином является β-циклодекстрин.
5. Комплекс триоксопиримидин-циклодекстрин по п.1, в котором растворимым в воде циклодекстрином является гидроксипропилированный циклодекстрин.
6. Комплекс триоксопиримидин-циклодекстрин по п.1, в котором растворимым в воде циклодекстрином является статистически метилированный циклодекстрин.
7. Комплекс триоксопиримидин-циклодекстрин по п.1, в котором растворимым в воде циклодекстрином является сульфобутил-β-циклодекстрин.
8. Комплекс триоксопиримидин-циклодекстрин по п.1, в котором растворимым в воде циклодекстрином является γ-циклодекстрин.
9. Фармацевтический препарат, содержащий комплекс триоксопиримидин-циклодекстрин по любому из пп.1-8.
10. Фармацевтический препарат по п.9, содержащий фармацевтически приемлемую добавку.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04007921 | 2004-04-01 | ||
| EP04007921.2 | 2004-04-01 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2006138431A true RU2006138431A (ru) | 2008-06-10 |
| RU2411043C2 RU2411043C2 (ru) | 2011-02-10 |
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| Application Number | Title | Priority Date | Filing Date |
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| RU2006138431/15A RU2411043C2 (ru) | 2004-04-01 | 2005-03-31 | Фармацевтические композиции пиримидин-2,4,6-трионов |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US20070191404A1 (ru) |
| EP (1) | EP1735007A2 (ru) |
| JP (1) | JP4787240B2 (ru) |
| KR (1) | KR100771411B1 (ru) |
| CN (1) | CN1950110B (ru) |
| AU (1) | AU2005230380B2 (ru) |
| BR (1) | BRPI0509583A (ru) |
| CA (1) | CA2561660C (ru) |
| MX (1) | MXPA06011031A (ru) |
| RU (1) | RU2411043C2 (ru) |
| WO (1) | WO2005097058A2 (ru) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070191404A1 (en) | 2004-04-01 | 2007-08-16 | Pierre Bartsch | Pharmaceutical compositions of pyrimidine-2,4,6-triones |
| US10653899B2 (en) | 2009-12-31 | 2020-05-19 | Sol-Gel Technologies Ltd. | Core stabilized microcapsules, method of their preparation and uses thereof |
| KR20220156931A (ko) * | 2020-03-23 | 2022-11-28 | 잡 리써치 앤드 디벨롭먼트, 엘엘씨 | 경구 테르펜 사이클로덱스트린 봉입물 복합 비히클 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| DE1018340B (de) * | 1954-01-13 | 1957-10-24 | Takeo Takagi | Vorrichtung zum Reissen und Strecken eines Buendels aus endlosen Kunstfaeden nach dem Doppelstrecksystem |
| DE19548624A1 (de) * | 1995-12-23 | 1997-06-26 | Boehringer Mannheim Gmbh | Neue Barbitursäure-Derivate, Verfahren zu deren Herstellung und diese Verbindungen enthaltende Arzneimittel |
| DE19726427A1 (de) * | 1997-06-23 | 1998-12-24 | Boehringer Mannheim Gmbh | Pyrimidin-2,4,6-trion-Derivate, Verfahren zu deren Herstellung und diese Verbindungen enthaltende Arzneimittel |
| US6048736A (en) * | 1998-04-29 | 2000-04-11 | Kosak; Kenneth M. | Cyclodextrin polymers for carrying and releasing drugs |
| US6350786B1 (en) * | 1998-09-22 | 2002-02-26 | Hoffmann-La Roche Inc. | Stable complexes of poorly soluble compounds in ionic polymers |
| IT1304190B1 (it) * | 1998-12-18 | 2001-03-08 | Euphar Group Srl | Clatrati di deidroepiandrosterone e relative composizionifarmaceutiche |
| ATE249218T1 (de) * | 1999-01-06 | 2003-09-15 | Tecnimede Sociedade Tecnico Medicinal Sa | Cyclodextrin einschlusskomplexe mit aminosäuresalzen von benzimidazolderivaten, deren herstellung, sowie diese enthaltende pharmazeutische zusammensetzungen |
| AR033651A1 (es) * | 1999-10-01 | 2004-01-07 | Hoffmann La Roche | Derivados de pirimidina-2,4,6-triona, composiciones farmaceuticas que contienen dichos compuestos y el empleo de los mismos para la manufactura de un medicamento |
| WO2002089824A1 (en) * | 2001-05-03 | 2002-11-14 | F. Hoffmann-La Roche Ag | Combination of a gelatinase inhibitor and an anti-tumor agent, and uses thereof |
| US20070191404A1 (en) | 2004-04-01 | 2007-08-16 | Pierre Bartsch | Pharmaceutical compositions of pyrimidine-2,4,6-triones |
-
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- 2005-03-31 KR KR1020067020529A patent/KR100771411B1/ko not_active IP Right Cessation
- 2005-03-31 RU RU2006138431/15A patent/RU2411043C2/ru not_active IP Right Cessation
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- 2005-03-31 WO PCT/EP2005/003348 patent/WO2005097058A2/en active Application Filing
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Also Published As
| Publication number | Publication date |
|---|---|
| US20100261672A1 (en) | 2010-10-14 |
| JP4787240B2 (ja) | 2011-10-05 |
| JP2007530628A (ja) | 2007-11-01 |
| AU2005230380A1 (en) | 2005-10-20 |
| US8044035B2 (en) | 2011-10-25 |
| CA2561660C (en) | 2012-10-30 |
| WO2005097058A3 (en) | 2006-08-17 |
| KR100771411B1 (ko) | 2007-10-30 |
| CN1950110A (zh) | 2007-04-18 |
| US20070191404A1 (en) | 2007-08-16 |
| RU2411043C2 (ru) | 2011-02-10 |
| MXPA06011031A (es) | 2007-03-21 |
| KR20070027528A (ko) | 2007-03-09 |
| CN1950110B (zh) | 2012-11-21 |
| EP1735007A2 (en) | 2006-12-27 |
| AU2005230380B2 (en) | 2010-09-23 |
| CA2561660A1 (en) | 2005-10-20 |
| WO2005097058A2 (en) | 2005-10-20 |
| BRPI0509583A (pt) | 2007-10-09 |
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