CZ140096A3 - Pharmaceutical composition and the use thereof - Google Patents
Pharmaceutical composition and the use thereof Download PDFInfo
- Publication number
- CZ140096A3 CZ140096A3 CZ961400A CZ140096A CZ140096A3 CZ 140096 A3 CZ140096 A3 CZ 140096A3 CZ 961400 A CZ961400 A CZ 961400A CZ 140096 A CZ140096 A CZ 140096A CZ 140096 A3 CZ140096 A3 CZ 140096A3
- Authority
- CZ
- Czechia
- Prior art keywords
- nitric oxide
- progestin
- estrogen
- use according
- mammal
- Prior art date
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- 239000008194 pharmaceutical composition Substances 0.000 title claims description 5
- MWUXSHHQAYIFBG-UHFFFAOYSA-N Nitric oxide Chemical compound O=[N] MWUXSHHQAYIFBG-UHFFFAOYSA-N 0.000 claims abstract description 95
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical class C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 claims abstract description 90
- 229940011871 estrogen Drugs 0.000 claims abstract description 56
- 239000000262 estrogen Substances 0.000 claims abstract description 56
- 239000000583 progesterone congener Substances 0.000 claims abstract description 54
- 239000000758 substrate Substances 0.000 claims abstract description 37
- 229930064664 L-arginine Natural products 0.000 claims description 33
- 235000014852 L-arginine Nutrition 0.000 claims description 33
- ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 claims description 32
- 239000002840 nitric oxide donor Substances 0.000 claims description 31
- 241000124008 Mammalia Species 0.000 claims description 29
- 239000000186 progesterone Substances 0.000 claims description 24
- 229960003387 progesterone Drugs 0.000 claims description 23
- 102000008299 Nitric Oxide Synthase Human genes 0.000 claims description 17
- 108010021487 Nitric Oxide Synthase Proteins 0.000 claims description 17
- 239000000203 mixture Substances 0.000 claims description 16
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 claims description 14
- 206010027304 Menopausal symptoms Diseases 0.000 claims description 13
- SNIOPGDIGTZGOP-UHFFFAOYSA-N Nitroglycerin Chemical compound [O-][N+](=O)OCC(O[N+]([O-])=O)CO[N+]([O-])=O SNIOPGDIGTZGOP-UHFFFAOYSA-N 0.000 claims description 12
- 238000002657 hormone replacement therapy Methods 0.000 claims description 12
- RSEPBGGWRJCQGY-RBRWEJTLSA-N Estradiol valerate Chemical compound C1CC2=CC(O)=CC=C2[C@@H]2[C@@H]1[C@@H]1CC[C@H](OC(=O)CCCC)[C@@]1(C)CC2 RSEPBGGWRJCQGY-RBRWEJTLSA-N 0.000 claims description 11
- 229960005309 estradiol Drugs 0.000 claims description 11
- 229960003711 glyceryl trinitrate Drugs 0.000 claims description 11
- WWYNJERNGUHSAO-XUDSTZEESA-N (+)-Norgestrel Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 WWYNJERNGUHSAO-XUDSTZEESA-N 0.000 claims description 10
- 230000015572 biosynthetic process Effects 0.000 claims description 10
- 229960004400 levonorgestrel Drugs 0.000 claims description 10
- 239000000006 Nitroglycerin Substances 0.000 claims description 9
- 229930182833 estradiol Natural products 0.000 claims description 9
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- XEYBHCRIKKKOSS-UHFFFAOYSA-N disodium;azanylidyneoxidanium;iron(2+);pentacyanide Chemical group [Na+].[Na+].[Fe+2].N#[C-].N#[C-].N#[C-].N#[C-].N#[C-].[O+]#N XEYBHCRIKKKOSS-UHFFFAOYSA-N 0.000 claims description 5
- 229940083618 sodium nitroprusside Drugs 0.000 claims description 5
- NCGICGYLBXGBGN-UHFFFAOYSA-N 3-morpholin-4-yl-1-oxa-3-azonia-2-azanidacyclopent-3-en-5-imine;hydrochloride Chemical compound Cl.[N-]1OC(=N)C=[N+]1N1CCOCC1 NCGICGYLBXGBGN-UHFFFAOYSA-N 0.000 claims description 4
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- MOYKHGMNXAOIAT-JGWLITMVSA-N isosorbide dinitrate Chemical compound [O-][N+](=O)O[C@H]1CO[C@@H]2[C@H](O[N+](=O)[O-])CO[C@@H]21 MOYKHGMNXAOIAT-JGWLITMVSA-N 0.000 claims description 4
- 229960000201 isosorbide dinitrate Drugs 0.000 claims description 4
- YWXYYJSYQOXTPL-SLPGGIOYSA-N isosorbide mononitrate Chemical compound [O-][N+](=O)O[C@@H]1CO[C@@H]2[C@@H](O)CO[C@@H]21 YWXYYJSYQOXTPL-SLPGGIOYSA-N 0.000 claims description 4
- 229960003827 isosorbide mononitrate Drugs 0.000 claims description 4
- PROQIPRRNZUXQM-UHFFFAOYSA-N (16alpha,17betaOH)-Estra-1,3,5(10)-triene-3,16,17-triol Natural products OC1=CC=C2C3CCC(C)(C(C(O)C4)O)C4C3CCC2=C1 PROQIPRRNZUXQM-UHFFFAOYSA-N 0.000 claims description 3
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- 125000002059 L-arginyl group Chemical group O=C([*])[C@](N([H])[H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])C(=N[H])N([H])[H] 0.000 claims 1
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- JGMOKGBVKVMRFX-HQZYFCCVSA-N dydrogesterone Chemical compound C1=CC2=CC(=O)CC[C@@]2(C)[C@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 JGMOKGBVKVMRFX-HQZYFCCVSA-N 0.000 claims 1
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- 208000024891 symptom Diseases 0.000 abstract description 14
- GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 abstract description 3
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Claims (26)
- E N T O V 32NÁROKY1. Použití a) substrátu oxid dusnatý-syntásy,b) donoru oxidu dusnatého, nebo obou a, popřípadě, také v případě samice ¢-)-estrogenu—a ' ~ 'd) progestinu nebo, v případě samced) progestinu, pro výrobu léčiva pro ošetřování klimakteria (klimakterických symptomů) u negravidních samic nebo u samců savců.
- 2. Použití podle nároku 1, kde a) se použije v účinném množství pro zvýšení krevní hladiny cirkulujícího L-argininu o alespoň asi 10-50 nmol nad normální cirkulující hladiny50 až 100 nmol.
- 3. Použití podle nároku 1 nebo 2, kde savcem je negravidní Žena postižená menopauzálními symptomy klimakteria.
- 4. Použití podle nároku 1 nebo 2, kde savcem je negravidní žena, která vykazuje nebo je kandidátem na hormonovou náhradovou terapii.
- 5. Použití podle nároku 1 nebo 2, kde savcem je negravidní žena a kde a) je substrát oxid dusnatý-syntásy.
- 6. Použití podle nároku 5, kde substrátem oxidu dusnatého je L-arginín.
- 7. Použití podle nároku 1 nebo 2, kde savcem je negravidní žena a kde a) je donor oxidu dusnatého.
- 8. Použití podle nároku 7, kde donorem oxidu dusnatého je nitroprusid sodný, nitroglycerin, glyceryltrinitrát, SIN-1, isosorbidmononitrát nebo isosorbiddinitrát.
- 9. Použití podle nároku 7, kde donor oxidu dusnatého je pro orální podání.
- 10. Použití podle nároku 1 nebo 2, kde savcem je negravidní žena a substrát nebo donor oxidu dusnatého je pro orální podáni v kombinaci s estrogenem.
- 11. Použití podle nároku 10, kde estrogen je estradiól-valerát, konjugované koňské estrogeny,17p-estradiol, estron nebo estriol.
- 12. Použití podle nároku 1 nebo 2, kde savcem je negravidní žena a substrát nebo donor oxidu dusnatého je pro orální podání v kombinaci s progestinem.
- 13. Použití podle nároku 12, kde progestinem je progesteron, dydrogesteron, medroxyprogesteron, norethisteron, levonorgestrel, norgestrel, gestoden, desogestrel nebo 3-keto-desogestrel.
- 14. Použití podle nároku l nebo 2, kde savcem je negravidní žena pod současnou a kontinuální hormonovou náhradou estrogenem nebo progestinem.
- 15. Použití podle nároku 1 nebo 2, kde savcem je negravidní Žena pod současnou a sekvenční hormonovou náhradou estrogenem a progestinem.
- 16. Použití podle nároku 1 nebo 2, kde savcem je muž pod současnou a sekvenční hormonovou náhradou estrogenem a progestinem.
- 17. Použití podle nároku 1 nebo 2, kde savcem je muž a substrát nebo donor oxidu dusnatého je pro podání v kombinaci s p r o g e s-Μη e m-;--: ——
- 18. Farmaceutická kompozice, vyznačující se t í m, že obsahuje směs a) substrátu oxid dusnatý-syntásy,b) . donoru oxidu dusnatého, nebo obou a, takéc) estrogenu nebod) progestinu spolu s estrogenem.
- 19. Kompozice podle nároku 18, vyznačující se t í m, že (a) je substrát syntézy oxidu dusnatého.
- 20. Kompozice podle nároku 18, vyznačující se t í m, že substrát syntézy oxidu dusnatého (a) je L-arginin.
- 21. Kompozice podle nároku 18, vyznačující se t í rn, že (b) je donor oxidu dusnatého.
- 22. Kompozice podle nároku 21,vyznačuj ící se t í m, že donor oxidu dusnatého (b) je nitroprusid sodný, nitroglycerin, glyceryltrinitrid, SIN-1, isosorbidmononitrát nebo isosorbiddinitrát.
- 23. Kompozice podle nároku 18, vyznačuj ící t í m, že estrogenem (c) je estradiol-valerát.
- 24. Kompozice podle nároku 18, vyznačující se t í m, že estrogenem (c) je estradiol.
- 25. Kompozice podle nároku 18, vyznačující se t í m, že progestinem (d) je norgestrel.
- 26. Kompozice podle nároku 18, kde progestinem (d) je progesteron.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/153,345 US5595970A (en) | 1993-07-16 | 1993-11-16 | Treatment of climacteric disorders with nitric oxide synthase substrates and/or donors |
Publications (1)
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|---|---|
| CZ140096A3 true CZ140096A3 (en) | 1996-09-11 |
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ID=22546812
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| CZ961400A CZ140096A3 (en) | 1993-11-16 | 1994-11-17 | Pharmaceutical composition and the use thereof |
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| US (2) | US5595970A (cs) |
| EP (1) | EP0730445A1 (cs) |
| JP (1) | JPH09505069A (cs) |
| KR (1) | KR960705554A (cs) |
| CN (1) | CN1135177A (cs) |
| AU (1) | AU8144694A (cs) |
| BR (1) | BR9408062A (cs) |
| CA (1) | CA2176727A1 (cs) |
| CZ (1) | CZ140096A3 (cs) |
| FI (1) | FI962110A (cs) |
| HU (1) | HUT74459A (cs) |
| NO (1) | NO961994L (cs) |
| NZ (1) | NZ276106A (cs) |
| PL (1) | PL178130B1 (cs) |
| SK (1) | SK63496A3 (cs) |
| WO (1) | WO1995013800A1 (cs) |
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| US6407082B1 (en) * | 1996-09-13 | 2002-06-18 | New Life Pharmaceuticals Inc. | Prevention of ovarian cancer by administration of a vitamin D compound |
| ES2292402T3 (es) * | 1994-05-27 | 2008-03-16 | Strakan International Limited | Composicion de donador de oxido nitrico y metodo para el tratamiento de afecciones anales. |
| US5968983A (en) | 1994-10-05 | 1999-10-19 | Nitrosystems, Inc | Method and formulation for treating vascular disease |
| US20110196039A9 (en) * | 1994-10-05 | 2011-08-11 | Kaesemeyer Wayne H | Controlled release arginine formulations |
| US6425881B1 (en) | 1994-10-05 | 2002-07-30 | Nitrosystems, Inc. | Therapeutic mixture useful in inhibiting lesion formation after vascular injury |
| US6239172B1 (en) * | 1997-04-10 | 2001-05-29 | Nitrosystems, Inc. | Formulations for treating disease and methods of using same |
| US5789442A (en) * | 1996-01-18 | 1998-08-04 | Schering Aktiengesellschaft | Treatment of urinary incontinence with nitric oxide synthase substrates and/or nitric oxide donors alone or in combination with estrogen or progesterone and/or other agents |
| US5910482A (en) * | 1996-03-19 | 1999-06-08 | Board Of Regents, The University Of Texas System | Treatment or prevention of preeclampsia, eclampsia with calcitonin gene related peptide, CGRP analog, progestational agent, nitric oxide source, and cyclooxygenase inhibitor |
| US5898038A (en) * | 1996-03-19 | 1999-04-27 | Board Of Regents, The University Of Texas System | Treatment of osteoporosis and metabolic bone disorders with nitric oxide substrate and/or donors |
| AU771012B2 (en) * | 1996-05-07 | 2004-03-11 | Board Of Regents, The University Of Texas System | Improvement of implantation rates after in vitro fertilization |
| US6040340A (en) * | 1996-05-07 | 2000-03-21 | Schering Aktiengesellschaft | Implantation rates after in vitro fertilization, treatment of infertility and early pregnancy loss with a nitric oxide donor alone or in combination with progesterone, and a method for contraception with nitric oxide inhibitors |
| US6232434B1 (en) | 1996-08-02 | 2001-05-15 | Duke University Medical Center | Polymers for delivering nitric oxide in vivo |
| AUPO203996A0 (en) * | 1996-08-30 | 1996-09-26 | Novogen Research Pty Ltd | Therapeutic uses |
| US6765002B2 (en) | 2000-03-21 | 2004-07-20 | Gustavo Rodriguez | Prevention of ovarian cancer by administration of products that induce transforming growth factor-β and/or apoptosis in the ovarian epithelium |
| US6034074A (en) | 1996-09-13 | 2000-03-07 | New Life Pharmaceuticals Inc. | Prevention of ovarian cancer by administration of a Vitamin D compound |
| US6511970B1 (en) | 1996-09-13 | 2003-01-28 | New Life Pharmaceuticals Inc. | Prevention of ovarian cancer by administration of products that induce transforming growth factor-beta and/or apoptosis in the ovarian epithelium |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5508045A (en) * | 1992-10-09 | 1996-04-16 | The Regents Of The University Of California | Method and agents for control and management of labor during pregnancy |
-
1993
- 1993-11-16 US US08/153,345 patent/US5595970A/en not_active Expired - Lifetime
-
1994
- 1994-11-17 SK SK634-96A patent/SK63496A3/sk unknown
- 1994-11-17 PL PL94314466A patent/PL178130B1/pl unknown
- 1994-11-17 CN CN94194167A patent/CN1135177A/zh active Pending
- 1994-11-17 JP JP7514225A patent/JPH09505069A/ja active Pending
- 1994-11-17 CZ CZ961400A patent/CZ140096A3/cs unknown
- 1994-11-17 AU AU81446/94A patent/AU8144694A/en not_active Abandoned
- 1994-11-17 KR KR1019960702551A patent/KR960705554A/ko not_active Application Discontinuation
- 1994-11-17 WO PCT/EP1994/003818 patent/WO1995013800A1/en not_active Application Discontinuation
- 1994-11-17 HU HU9601301A patent/HUT74459A/hu unknown
- 1994-11-17 BR BR9408062A patent/BR9408062A/pt not_active Application Discontinuation
- 1994-11-17 NZ NZ276106A patent/NZ276106A/en unknown
- 1994-11-17 CA CA002176727A patent/CA2176727A1/en not_active Abandoned
- 1994-11-17 EP EP95900760A patent/EP0730445A1/en not_active Withdrawn
-
1995
- 1995-06-06 US US08/466,538 patent/US5958878A/en not_active Expired - Fee Related
-
1996
- 1996-05-15 NO NO961994A patent/NO961994L/no not_active Application Discontinuation
- 1996-05-17 FI FI962110A patent/FI962110A/fi unknown
Also Published As
| Publication number | Publication date |
|---|---|
| HUT74459A (en) | 1996-12-30 |
| FI962110A (fi) | 1996-07-15 |
| HU9601301D0 (en) | 1996-07-29 |
| NO961994D0 (no) | 1996-05-15 |
| BR9408062A (pt) | 1996-11-24 |
| CN1135177A (zh) | 1996-11-06 |
| WO1995013800A1 (en) | 1995-05-26 |
| FI962110A0 (fi) | 1996-05-17 |
| US5958878A (en) | 1999-09-28 |
| NO961994L (no) | 1996-07-16 |
| CA2176727A1 (en) | 1995-05-26 |
| EP0730445A1 (en) | 1996-09-11 |
| PL178130B1 (pl) | 2000-03-31 |
| PL314466A1 (en) | 1996-09-16 |
| SK63496A3 (en) | 1997-03-05 |
| KR960705554A (ko) | 1996-11-08 |
| NZ276106A (en) | 1998-05-27 |
| AU8144694A (en) | 1995-06-06 |
| US5595970A (en) | 1997-01-21 |
| JPH09505069A (ja) | 1997-05-20 |
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