JP2004506009A5 - - Google Patents
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- Publication number
- JP2004506009A5 JP2004506009A5 JP2002518944A JP2002518944A JP2004506009A5 JP 2004506009 A5 JP2004506009 A5 JP 2004506009A5 JP 2002518944 A JP2002518944 A JP 2002518944A JP 2002518944 A JP2002518944 A JP 2002518944A JP 2004506009 A5 JP2004506009 A5 JP 2004506009A5
- Authority
- JP
- Japan
- Prior art keywords
- selective
- ethyl
- pharmaceutical composition
- pde5 inhibitor
- pyrazolo
- Prior art date
- Legal status (The legal status 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 status listed.)
- Withdrawn
Links
- ZOOGRGPOEVQQDX-UUOKFMHZSA-N 3',5'-cyclic GMP Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=C(NC2=O)N)=C2N=C1 ZOOGRGPOEVQQDX-UUOKFMHZSA-N 0.000 claims 9
- 229940123333 Phosphodiesterase 5 inhibitor Drugs 0.000 claims 9
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 claims 9
- DOTPSQVYOBAWPQ-UHFFFAOYSA-N pyrazolo[4,3-d]pyrimidin-3-one Chemical compound N1=CN=C2C(=O)N=NC2=C1 DOTPSQVYOBAWPQ-UHFFFAOYSA-N 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 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 6
- 239000012453 solvate Substances 0.000 claims 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 4
- 208000002705 Glucose Intolerance Diseases 0.000 claims 3
- 230000001684 chronic effect Effects 0.000 claims 3
- 201000009104 prediabetes syndrome Diseases 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 229960003310 sildenafil Drugs 0.000 claims 3
- 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 2
- 206010022489 Insulin Resistance Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- WJQXYMDJKXVKMF-UHFFFAOYSA-N 3-ethyl-5-[5-(4-ethylpiperazin-1-yl)sulfonyl-2-(2-methoxyethoxy)pyridin-3-yl]-6-methyl-2-pyridin-2-ylpyrazolo[4,3-d]pyrimidin-7-one Chemical compound C1CN(CC)CCN1S(=O)(=O)C1=CN=C(OCCOC)C(C=2N(C(=O)C3=NN(C(CC)=C3N=2)C=2N=CC=CC=2)C)=C1 WJQXYMDJKXVKMF-UHFFFAOYSA-N 0.000 claims 1
- OABVKOFQXWSACK-UHFFFAOYSA-N 3-ethyl-5-[5-(4-ethylpiperazin-1-yl)sulfonyl-2-propoxyphenyl]-6-methyl-2-pyridin-2-ylpyrazolo[4,3-d]pyrimidin-7-one Chemical compound CCCOC1=CC=C(S(=O)(=O)N2CCN(CC)CC2)C=C1C(N(C(=O)C1=N2)C)=NC1=C(CC)N2C1=CC=CC=N1 OABVKOFQXWSACK-UHFFFAOYSA-N 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- -1 4-Ethylpiperazin-1-ylsulfonyl Chemical group 0.000 claims 1
- DYHVWOAZIYHPLL-UHFFFAOYSA-N 5-[2-ethoxy-5-(2-morpholin-4-ylacetyl)phenyl]-1-ethyl-3-propyl-4h-pyrazolo[4,3-d]pyrimidin-7-one Chemical compound CCCC1=NN(CC)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1C(=O)CN1CCOCC1 DYHVWOAZIYHPLL-UHFFFAOYSA-N 0.000 claims 1
- 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 1
- 230000001154 acute effect Effects 0.000 claims 1
- 238000013270 controlled release Methods 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 230000002650 habitual effect Effects 0.000 claims 1
- 238000002638 palliative care Methods 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 229960002639 sildenafil citrate Drugs 0.000 claims 1
- DEIYFTQMQPDXOT-UHFFFAOYSA-N sildenafil citrate Chemical group OC(=O)CC(O)(C(O)=O)CC(O)=O.CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 DEIYFTQMQPDXOT-UHFFFAOYSA-N 0.000 claims 1
- 238000013268 sustained release Methods 0.000 claims 1
- 239000012730 sustained-release form Substances 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 238000011282 treatment Methods 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22492800P | 2000-08-11 | 2000-08-11 | |
| GB0030649A GB0030649D0 (en) | 2000-12-15 | 2000-12-15 | Treatment of the insulin resistance syndrome |
| US26608301P | 2001-02-02 | 2001-02-02 | |
| GB0106468A GB0106468D0 (en) | 2001-03-15 | 2001-03-15 | Treatment of diabetes mellitus |
| GB0106465A GB0106465D0 (en) | 2001-03-15 | 2001-03-15 | Treatment of the insulin resistance syndrome |
| GB0117134A GB0117134D0 (en) | 2001-07-13 | 2001-07-13 | Treatment of the insulin resistance syndrome |
| PCT/IB2001/001428 WO2002013798A2 (en) | 2000-08-11 | 2001-08-06 | Treatment of the insulin resistance syndrome with selective cgmp pde5 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004506009A JP2004506009A (ja) | 2004-02-26 |
| JP2004506009A5 true JP2004506009A5 (https=) | 2005-02-24 |
Family
ID=27546614
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002518944A Withdrawn JP2004506009A (ja) | 2000-08-11 | 2001-08-06 | インスリン抵抗性症候群の治療 |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP1307183A2 (https=) |
| JP (1) | JP2004506009A (https=) |
| KR (1) | KR20030023747A (https=) |
| CN (1) | CN1446084A (https=) |
| AU (1) | AU2001276607A1 (https=) |
| CA (1) | CA2419033A1 (https=) |
| HU (1) | HUP0300725A3 (https=) |
| IL (1) | IL154158A0 (https=) |
| WO (1) | WO2002013798A2 (https=) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA03006936A (es) * | 2001-02-02 | 2003-11-18 | Pfizer | Tratamiento de diabetes mellitus. |
| US6933127B2 (en) | 2001-07-05 | 2005-08-23 | Eucro European Contract Research Gmbh & Co. Kg | Substrate for PP2C |
| DE10135815A1 (de) * | 2001-07-23 | 2003-02-06 | Bayer Ag | Verwendung von 2-Alkoxyphenyl-substituierten Imidazotriazinonen |
| US7019010B2 (en) | 2001-09-27 | 2006-03-28 | Novertis Ag | Combinations |
| US20030114469A1 (en) * | 2001-09-27 | 2003-06-19 | Cohen David Saul | Combinations |
| JP2005508978A (ja) | 2001-11-02 | 2005-04-07 | ファイザー・プロダクツ・インク | Ｐｄｅ９阻害薬によるインスリン抵抗性症候群及び２型糖尿病の治療 |
| US20030181461A1 (en) * | 2002-01-25 | 2003-09-25 | Lautt Wilfred Wayne | Use of phosphodiesterase antagonists to treat insulin resistance |
| JP2005519927A (ja) * | 2002-02-07 | 2005-07-07 | ファイザー・インク | 多嚢胞性卵巣症候群の処置における、シルデナフィル如きｐｄｅ５インヒビターの使用 |
| JP2004018524A (ja) * | 2002-06-13 | 2004-01-22 | Eucro European Contract Research Gmbh & Co Kg | 動脈硬化症を処置するための方法 |
| GB0214784D0 (en) * | 2002-06-26 | 2002-08-07 | Pfizer Ltd | Novel combination |
| BRPI0408500A (pt) * | 2003-03-17 | 2006-03-07 | Pfizer Prod Inc | tratamento do diabetes do tipo 1 com inibidores de pde5 |
| UA80871C2 (en) * | 2003-04-29 | 2007-11-12 | Pfizer Ltd | 5,7-diaminopyrazolo[4,3-d]pyrimidines useful in the treatment of hypertension |
| OA13050A (en) | 2003-04-29 | 2006-11-10 | Pfizer Ltd | 5,7-diaminopyrazolo [4,3-D] pyrimidines useful in the treatment of hypertension. |
| JP2007504201A (ja) | 2003-09-05 | 2007-03-01 | アルタナ ファルマ アクチエンゲゼルシャフト | 真性糖尿病の治療のためのｐｄｅ４阻害剤の使用 |
| US7572799B2 (en) | 2003-11-24 | 2009-08-11 | Pfizer Inc | Pyrazolo[4,3-d]pyrimidines as Phosphodiesterase Inhibitors |
| CA2562251C (en) | 2004-04-07 | 2009-04-28 | Pfizer Inc. | Pyrazolo'4,3-d pyrimidines |
| EP1874308A1 (en) | 2005-03-08 | 2008-01-09 | Nycomed GmbH | Roflumilast for the treatment of diabetes mellitus |
| WO2007010337A2 (de) * | 2005-07-15 | 2007-01-25 | Proxomed Medizintechnik Gmbh | Verwendung von phosphodiesterase typ 5-hemmern für die prävention und behandlung von adipositas, sowie abgabesysteme für dieselben |
| WO2008028914A1 (en) | 2006-09-07 | 2008-03-13 | Nycomed Gmbh | Combination treatment for diabetes mellitus |
| KR101560844B1 (ko) | 2007-06-04 | 2015-10-15 | 벤-구리온 유니버시티 오브 더 네게브 리서치 앤드 디벨럽먼트 어쏘러티 | 트라이-아릴계 화합물 및 이를 포함하는 조성물 |
| AT512084A1 (de) | 2011-10-20 | 2013-05-15 | Univ Wien Tech | Diazabicyclo- und diazaspiro-alkanderivate als phosphodiesterase-5 inhibitoren |
| US20130315891A1 (en) | 2012-05-25 | 2013-11-28 | Matthew Charles | Formulations of human tissue kallikrein-1 for parenteral delivery and related methods |
| US20130323222A1 (en) | 2012-06-04 | 2013-12-05 | Matthew Charles | Human tissue kallikrein 1 glycosylation isoforms |
| SG10201709195TA (en) * | 2012-11-13 | 2017-12-28 | Nusirt Sciences Inc | Compositions and methods for increasing energy metabolism |
| US9840547B2 (en) | 2013-05-14 | 2017-12-12 | Scimar Ltd. | Hepatic insulin sensitizing substance and test meal for insulin sensitization |
| MX2016005995A (es) | 2013-11-05 | 2016-08-17 | Ben-Gurion Univ Of The Negev Res And Dev Authority | Compuestos para el tratamiento de diabetes y complicaciones de la enfermedad derivadas de la misma. |
| AU2018230478B2 (en) | 2017-03-09 | 2025-01-23 | Diamedica Inc. | Dosage forms of tissue kallikrein 1 |
| MX2017016930A (es) * | 2017-12-19 | 2019-06-20 | Malesil Research & Tech Llc | Uso del maleato de sildenafil en el tratamiento de ulceras de pie diabetico. |
| KR102068299B1 (ko) * | 2018-12-21 | 2020-01-20 | 한국기초과학지원연구원 | Cyp4a 저해 화합물을 유효성분으로 포함하는 대사질환의 예방 또는 치료용 조성물 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9013750D0 (en) * | 1990-06-20 | 1990-08-08 | Pfizer Ltd | Therapeutic agents |
| GB9511220D0 (en) * | 1995-06-02 | 1995-07-26 | Glaxo Group Ltd | Solid dispersions |
| WO1997024334A1 (en) * | 1995-12-28 | 1997-07-10 | Fujisawa Pharmaceutical Co., Ltd. | Benzimidazole derivatives |
| US6723719B1 (en) * | 1997-04-25 | 2004-04-20 | Pfizer Inc | Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3′,5′—monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction |
| AU745081B2 (en) * | 1997-06-27 | 2002-03-14 | Fujisawa Pharmaceutical Co., Ltd. | Sulfonamide compounds and medicinal use thereof |
| KR20010052235A (ko) * | 1998-04-06 | 2001-06-25 | 후지야마 아키라 | 인돌 유도체 |
| HK1044154A1 (zh) * | 1998-12-04 | 2002-10-11 | 藤泽药品工业株式会社 | 磺酰胺化合物及其药物用途 |
| AU765128B2 (en) * | 1999-03-22 | 2003-09-11 | Bristol-Myers Squibb Company | Fused pyridopyridazine inhibitors of cGMP phosphodiesterase |
| DE19944161A1 (de) * | 1999-09-15 | 2001-03-22 | Bayer Ag | Neue Kombination zur Behandlung von sexueller Dysfunktion |
| ATE257480T1 (de) * | 1999-09-30 | 2004-01-15 | Pfizer Prod Inc | Bicyclische pyrrolylamide als glycogenphosphorylase-inhibitoren |
| US6503908B1 (en) * | 1999-10-11 | 2003-01-07 | Pfizer Inc | Pharmaceutically active compounds |
| US6774128B2 (en) * | 2000-04-19 | 2004-08-10 | Johns Hopkins University | Methods for prevention and treatment of gastrointestinal disorders |
-
2001
- 2001-08-06 AU AU2001276607A patent/AU2001276607A1/en not_active Abandoned
- 2001-08-06 CA CA002419033A patent/CA2419033A1/en not_active Abandoned
- 2001-08-06 WO PCT/IB2001/001428 patent/WO2002013798A2/en not_active Ceased
- 2001-08-06 KR KR10-2003-7001961A patent/KR20030023747A/ko not_active Ceased
- 2001-08-06 HU HU0300725A patent/HUP0300725A3/hu unknown
- 2001-08-06 EP EP01954266A patent/EP1307183A2/en not_active Withdrawn
- 2001-08-06 CN CN01814039A patent/CN1446084A/zh active Pending
- 2001-08-06 JP JP2002518944A patent/JP2004506009A/ja not_active Withdrawn
- 2001-08-06 IL IL15415801A patent/IL154158A0/xx unknown
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