RU2008131792A - Комбинация избирательного ингибитора обратного захвата норадреналина и ингибитора pdev - Google Patents
Комбинация избирательного ингибитора обратного захвата норадреналина и ингибитора pdev Download PDFInfo
- Publication number
- RU2008131792A RU2008131792A RU2008131792/15A RU2008131792A RU2008131792A RU 2008131792 A RU2008131792 A RU 2008131792A RU 2008131792/15 A RU2008131792/15 A RU 2008131792/15A RU 2008131792 A RU2008131792 A RU 2008131792A RU 2008131792 A RU2008131792 A RU 2008131792A
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- Russia
- Prior art keywords
- pharmaceutically acceptable
- solvate
- acceptable salt
- ethyl
- pain
- Prior art date
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- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 title 2
- 239000003112 inhibitor Substances 0.000 title 2
- 229960002748 norepinephrine Drugs 0.000 title 2
- SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 title 2
- 150000003839 salts Chemical class 0.000 claims abstract 18
- 239000012453 solvate Substances 0.000 claims abstract 18
- WOXKDUGGOYFFRN-IIBYNOLFSA-N tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C(C4=CC=CC=C4N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 WOXKDUGGOYFFRN-IIBYNOLFSA-N 0.000 claims abstract 8
- BNRNXUUZRGQAQC-UHFFFAOYSA-N sildenafil Chemical compound CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 BNRNXUUZRGQAQC-UHFFFAOYSA-N 0.000 claims abstract 6
- YPFZMBHKIVDSNR-UHFFFAOYSA-N 5-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylpyridin-3-yl]-3-ethyl-2-(2-methoxyethyl)-4h-pyrazolo[4,3-d]pyrimidin-7-one Chemical compound C1=C(C=2NC(=O)C3=NN(CCOC)C(CC)=C3N=2)C(OCC)=NC=C1S(=O)(=O)N1CCN(CC)CC1 YPFZMBHKIVDSNR-UHFFFAOYSA-N 0.000 claims abstract 4
- 229940099471 Phosphodiesterase inhibitor Drugs 0.000 claims abstract 4
- 239000002571 phosphodiesterase inhibitor Substances 0.000 claims abstract 4
- SECKRCOLJRRGGV-UHFFFAOYSA-N Vardenafil Chemical compound CCCC1=NC(C)=C(C(N=2)=O)N1NC=2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(CC)CC1 SECKRCOLJRRGGV-UHFFFAOYSA-N 0.000 claims abstract 3
- CBQGYUDMJHNJBX-OALUTQOASA-N (2S)-2-[(S)-(2-ethoxyphenoxy)-phenylmethyl]morpholine Chemical compound CCOC1=CC=CC=C1O[C@@H](C=1C=CC=CC=1)[C@H]1OCCNC1 CBQGYUDMJHNJBX-OALUTQOASA-N 0.000 claims abstract 2
- ZUHZNKJIJDAJFD-UHFFFAOYSA-N 1-(2-ethoxyethyl)-5-[ethyl(methyl)amino]-7-[(4-methylpyridin-2-yl)amino]-n-methylsulfonylpyrazolo[4,3-d]pyrimidine-3-carboxamide Chemical compound C=12N(CCOCC)N=C(C(=O)NS(C)(=O)=O)C2=NC(N(C)CC)=NC=1NC1=CC(C)=CC=N1 ZUHZNKJIJDAJFD-UHFFFAOYSA-N 0.000 claims abstract 2
- UCRSYBKADUKGLT-CYBMUJFWSA-N 3-ethyl-5-[(3r)-3-methylpiperazin-1-yl]-n-pyrimidin-4-yl-1-[2-(2,2,2-trifluoroethoxy)ethyl]pyrazolo[4,3-d]pyrimidin-7-amine Chemical compound N1=C(N2C[C@@H](C)NCC2)N=C2C(CC)=NN(CCOCC(F)(F)F)C2=C1NC1=CC=NC=N1 UCRSYBKADUKGLT-CYBMUJFWSA-N 0.000 claims abstract 2
- INLBUQIADGPECI-UHFFFAOYSA-N 5-(5-acetyl-2-butoxypyridin-3-yl)-3-ethyl-2-(1-ethylazetidin-3-yl)-4h-pyrazolo[4,3-d]pyrimidin-7-one Chemical compound CCCCOC1=NC=C(C(C)=O)C=C1C1=NC2=C(CC)N(C3CN(CC)C3)N=C2C(=O)N1 INLBUQIADGPECI-UHFFFAOYSA-N 0.000 claims abstract 2
- 229940117229 cialis Drugs 0.000 claims abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 2
- 229960003310 sildenafil Drugs 0.000 claims abstract 2
- 229960000835 tadalafil Drugs 0.000 claims abstract 2
- 229960002381 vardenafil Drugs 0.000 claims abstract 2
- 208000002193 Pain Diseases 0.000 claims 11
- 208000023178 Musculoskeletal disease Diseases 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 208000004296 neuralgia Diseases 0.000 claims 2
- 208000021722 neuropathic pain Diseases 0.000 claims 2
- QMNWYGTWTXOQTP-UHFFFAOYSA-N 1h-triazin-6-one Chemical compound O=C1C=CN=NN1 QMNWYGTWTXOQTP-UHFFFAOYSA-N 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 208000001640 Fibromyalgia Diseases 0.000 claims 1
- 206010021639 Incontinence Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000001294 Nociceptive Pain Diseases 0.000 claims 1
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
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Abstract
1. Комбинация, состоящая из: ! (а) (S,S)-ребоксетина или его фармацевтически приемлемой соли или сольвата; и ! (б) ингибитора фосфодиэстеразы типа 5 (PDEV). ! 2. Комбинация по п.1, где ингибитор фосфодиэстеразы типа 5 (PDEV) выбран из: ! 5-[2-этокси-5-(4-метил-1-пиперазинилсульфонил)фенил]-1-метил-3-н-пропил-1,6-дигидро-7H-пиразоло[4,3-d]пиримидин-7-она (силденафил) или его фармацевтически приемлемой соли или сольвата; ! (6R,12aR)-2,3,6,7,12,12а-гексагидро-2-метил-6-(3,4-метилендиоксифенил)-пиразино[2',1':6,1]пиридо[3,4-b]индол-1,4-диона (тадалафил, IС-351, Cialis®) или его фармацевтически приемлемой соли или сольвата; ! 2-[2-этокси-5-(4-этил-пиперазин-1-ил-1-сульфонил)-фенил]-5-метил-7-пропил-3Н-имидазо[5,1-f][1,2,4]триазин-4-она (варденафил) или его фармацевтически приемлемой соли или сольвата; ! 5-[2-этокси-5-(4-этилпиперазин-1-илсульфонил)пиридин-3-ил]-3-этил-2-[2-метоксиэтил]-2,6-дигидро-7H-пиразоло[4,3-d]пиримидин-7-она или его фармацевтически приемлемой соли или сольвата; ! 5-(5-ацетил-2-бутокси-3-пиридинил)-3-этил-2-(1-этил-3-азетидинил)-2,6-дигидро-7H-пиразоло[4,3-d]пиримидин-7-она или его фармацевтически приемлемой соли или сольвата; ! 1-{6-этокси-5-[3-этил-6,7-дигидро-2-(2-метоксиэтил)-7-оксо-2Н-пиразоло[4,3-d]пиримидин-5-ил]-3-пиридилсульфонил}-4-этилпиперазина или его фармацевтически приемлемой соли или сольвата; ! N-[1-(2-этоксиэтил)-5-(N-этил-N-метиламино)-7-(4-метилпиридин-2-иламино)-1Н-пиразоло[4,3-d]пиримидин-3-карбонил]метансульфонамида или его фармацевтически приемлемой соли или сольвата; и ! {3-этил-5-[(R)-3-метил-пиперазин-1-ил]-1-[2-(2,2,2-трифторэтокси)-этил]-1Н-пиразоло[4,3-d]пиримидин-7-ил}-пиримидин-4-ил-амина или его фармацевтически приемлемой соли или сольвата. ! 3. Фармацевтическая композиция, содержащая: ! (а)комбинацию по п.1; и ! (б) ф�
Claims (14)
1. Комбинация, состоящая из:
(а) (S,S)-ребоксетина или его фармацевтически приемлемой соли или сольвата; и
(б) ингибитора фосфодиэстеразы типа 5 (PDEV).
2. Комбинация по п.1, где ингибитор фосфодиэстеразы типа 5 (PDEV) выбран из:
5-[2-этокси-5-(4-метил-1-пиперазинилсульфонил)фенил]-1-метил-3-н-пропил-1,6-дигидро-7H-пиразоло[4,3-d]пиримидин-7-она (силденафил) или его фармацевтически приемлемой соли или сольвата;
(6R,12aR)-2,3,6,7,12,12а-гексагидро-2-метил-6-(3,4-метилендиоксифенил)-пиразино[2',1':6,1]пиридо[3,4-b]индол-1,4-диона (тадалафил, IС-351, Cialis®) или его фармацевтически приемлемой соли или сольвата;
2-[2-этокси-5-(4-этил-пиперазин-1-ил-1-сульфонил)-фенил]-5-метил-7-пропил-3Н-имидазо[5,1-f][1,2,4]триазин-4-она (варденафил) или его фармацевтически приемлемой соли или сольвата;
5-[2-этокси-5-(4-этилпиперазин-1-илсульфонил)пиридин-3-ил]-3-этил-2-[2-метоксиэтил]-2,6-дигидро-7H-пиразоло[4,3-d]пиримидин-7-она или его фармацевтически приемлемой соли или сольвата;
5-(5-ацетил-2-бутокси-3-пиридинил)-3-этил-2-(1-этил-3-азетидинил)-2,6-дигидро-7H-пиразоло[4,3-d]пиримидин-7-она или его фармацевтически приемлемой соли или сольвата;
1-{6-этокси-5-[3-этил-6,7-дигидро-2-(2-метоксиэтил)-7-оксо-2Н-пиразоло[4,3-d]пиримидин-5-ил]-3-пиридилсульфонил}-4-этилпиперазина или его фармацевтически приемлемой соли или сольвата;
N-[1-(2-этоксиэтил)-5-(N-этил-N-метиламино)-7-(4-метилпиридин-2-иламино)-1Н-пиразоло[4,3-d]пиримидин-3-карбонил]метансульфонамида или его фармацевтически приемлемой соли или сольвата; и
{3-этил-5-[(R)-3-метил-пиперазин-1-ил]-1-[2-(2,2,2-трифторэтокси)-этил]-1Н-пиразоло[4,3-d]пиримидин-7-ил}-пиримидин-4-ил-амина или его фармацевтически приемлемой соли или сольвата.
3. Фармацевтическая композиция, содержащая:
(а)комбинацию по п.1; и
(б) фармацевтически приемлемый эксципиент, разбавитель или носитель.
4. Применение комбинации по п.1 или 2 в изготовлении лекарственного средства для одновременного, последовательного или раздельного введения обоих агентов при лечении недержания.
5. Применение комбинации по п.1 или 2 в изготовлении лекарственного средства для одновременного, последовательного или раздельного введения обоих агентов при лечении боли.
6. Применение комбинации по п.5, где боль представляет собой острую боль.
7. Применение комбинации по п.5, где боль представляет собой хроническую боль.
8. Применение комбинации по п.5, где боль представляет собой ноцицептивную боль.
9. Применение комбинации по п.5, где боль представляет собой невропатическую боль.
10. Применение комбинации по п.9, где невропатическая боль выбрана из постгерпетической невралгии и болезненной диабетической невропатии.
11. Применение комбинации по п.5, где боль представляет собой боль при воспалении.
12. Применение комбинации по п.11, где боль является следствием скелетно-мышечного расстройства.
13. Применение комбинации по п.12, где скелетно-мышечное расстройство представляет собой фибромиалгию.
14. Набор для лечения боли, по существу состоящий из:
(а) комбинации по п.1 и
(б) средств для содержания указанных соединений.
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| GB0417777A GB0417777D0 (en) | 2004-08-10 | 2004-08-10 | Pharmaceutical combination |
| GB0417777.0 | 2004-08-10 | ||
| US60630204P | 2004-08-31 | 2004-08-31 | |
| US60/606,302 | 2004-08-31 |
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| RU2007102847/15A Division RU2349323C2 (ru) | 2004-08-10 | 2005-07-29 | Комбинация избирательного ингибитора обратного захвата норадреналина и ингибитора pdev |
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| RU2008131792/15A RU2008131792A (ru) | 2004-08-10 | 2008-08-04 | Комбинация избирательного ингибитора обратного захвата норадреналина и ингибитора pdev |
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| RU2007102847/15A RU2349323C2 (ru) | 2004-08-10 | 2005-07-29 | Комбинация избирательного ингибитора обратного захвата норадреналина и ингибитора pdev |
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| EP (1) | EP1778241A1 (ru) |
| JP (1) | JP2008509900A (ru) |
| KR (2) | KR20070036171A (ru) |
| AU (1) | AU2005270904A1 (ru) |
| BR (1) | BRPI0514296A (ru) |
| CA (1) | CA2575980A1 (ru) |
| IL (1) | IL180557A0 (ru) |
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| NO (1) | NO20066059L (ru) |
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| WO2005040169A2 (en) | 2003-09-17 | 2005-05-06 | Janssen Pharmaceutica, N.V. | Fused heterocyclic compounds as serotonin receptor modulators |
| WO2006014913A2 (en) * | 2004-07-27 | 2006-02-09 | Biocryst Pharmaceuticals, Inc. | Inhibitors of 5'-methylthioadenosine phosphorylase and 5'methylthioadenosine/s-adenosylhomocysteine nucleosidase |
| US7598255B2 (en) | 2005-08-04 | 2009-10-06 | Janssen Pharmaceutica Nv | Pyrimidine compounds as serotonin receptor modulators |
| JP2008273867A (ja) * | 2007-04-27 | 2008-11-13 | Asahi Kasei Pharma Kk | 経粘膜投与用製剤 |
| US8841300B2 (en) | 2006-10-02 | 2014-09-23 | Jerry M. Held | Treatment for Parkinson's disease—combination high dose serotonergic synaptic reuptake inhibitor with phosphodiesterase inhibitor |
| JP2010527928A (ja) * | 2007-05-18 | 2010-08-19 | ヴィヴァス・インコーポレイテッド | ホスホジエステラーゼ−５阻害剤を含む新規の組み合わせおよびそれらの使用 |
| US20090131442A1 (en) * | 2007-11-16 | 2009-05-21 | Joseph Bernstein | Method of Treating Bone Pain Caused by Osteoarthritis |
| US20130323288A1 (en) | 2010-07-08 | 2013-12-05 | Wellesley Pharmaceuticals, Llc | Pharmaceutical formulation for bedwetting and method of use thereof |
| CN102018550B (zh) * | 2010-12-01 | 2012-04-25 | 中国人民解放军第四军医大学 | 后纵韧带犁刀 |
| CN107261119A (zh) * | 2011-02-28 | 2017-10-20 | 独立行政法人国立循环器病研究中心 | 恶性肿瘤转移抑制用药物 |
| US20150274735A1 (en) * | 2012-10-23 | 2015-10-01 | Pfizer Inc. | Use of a tetrasubstituted pyrazolo[4, 3-d]pyrimidine compound for treating diabetic nephropathy |
| US9637470B2 (en) | 2013-02-22 | 2017-05-02 | Baylor College Of Medicine | Treatment for substance use disorders and stress disorders |
| US10792326B2 (en) | 2013-06-28 | 2020-10-06 | Wellesley Pharmaceuticals, Llc | Pharmaceutical formulation for bedwetting and method of use thereof |
| JP7689392B2 (ja) * | 2020-11-05 | 2025-06-06 | ニューロライヴ インコーポレイテッド | アルツハイマー病または認知機能障害治療のためのドネペジルおよびタダラフィル併用療法｛Ｃｏｍｂｉｎａｔｉｏｎ Ｔｈｅｒａｐｙ ｏｆ Ｄｏｎｅｐｅｚｉｌ ａｎｄ Ｔａｄａｌａｆｉｌ ｆｏｒ ｔｈｅ Ｔｒｅａｔｍｅｎｔ ｏｆ Ａｌｚｈｅｉｍｅｒ’ｓ Ｄｉｓｅａｓｅ ｏｒ Ｃｏｇｎｉｔｉｖｅ Ｉｍｐａｉｒｍｅｎｔ｝ |
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| US20020006963A1 (en) * | 1992-06-23 | 2002-01-17 | Young James W. | Method of using and compositions comprising (-) sibutramine optionally in combination with other pharmacologically active compounds |
| PT1371647E (pt) * | 1998-04-20 | 2005-10-31 | Pfizer | Derivados do acido piridina-3-carboxilico e sua utilizacao como intermediarios |
| PL196996B1 (pl) * | 1999-07-01 | 2008-02-29 | Upjohn Co | Zastosowanie optycznie czystej (S,S)-reboksetyny lub jej dopuszczalnej farmaceutycznie soli do wytwarzania leku |
| GB0219024D0 (en) * | 2002-08-15 | 2002-09-25 | Pfizer Ltd | Synergistic combinations |
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2005
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- 2005-07-29 CA CA002575980A patent/CA2575980A1/en not_active Abandoned
- 2005-07-29 AU AU2005270904A patent/AU2005270904A1/en not_active Abandoned
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- 2005-07-29 RU RU2007102847/15A patent/RU2349323C2/ru not_active IP Right Cessation
- 2005-07-29 WO PCT/IB2005/002457 patent/WO2006016262A1/en not_active Ceased
- 2005-07-29 JP JP2007525380A patent/JP2008509900A/ja not_active Withdrawn
- 2005-07-29 EP EP05769508A patent/EP1778241A1/en not_active Withdrawn
- 2005-07-29 KR KR1020087015060A patent/KR20080064911A/ko not_active Ceased
- 2005-07-29 MX MX2007000694A patent/MX2007000694A/es not_active Application Discontinuation
- 2005-07-29 BR BRPI0514296-2A patent/BRPI0514296A/pt not_active IP Right Cessation
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Also Published As
| Publication number | Publication date |
|---|---|
| MX2007000694A (es) | 2007-03-12 |
| KR20070036171A (ko) | 2007-04-02 |
| US20090227562A1 (en) | 2009-09-10 |
| AU2005270904A1 (en) | 2006-02-16 |
| RU2349323C2 (ru) | 2009-03-20 |
| BRPI0514296A (pt) | 2008-06-17 |
| IL180557A0 (en) | 2008-03-20 |
| WO2006016262A1 (en) | 2006-02-16 |
| CA2575980A1 (en) | 2006-02-16 |
| EP1778241A1 (en) | 2007-05-02 |
| RU2007102847A (ru) | 2008-09-20 |
| JP2008509900A (ja) | 2008-04-03 |
| WO2006016262A8 (en) | 2006-06-29 |
| NO20066059L (no) | 2007-01-29 |
| KR20080064911A (ko) | 2008-07-09 |
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