NO328489B1 - Nye forbindelser og anvendelse av disse for fremstilling av farmasoytiske preparater for behandling av blant annet astma og diar± - Google Patents
Nye forbindelser og anvendelse av disse for fremstilling av farmasoytiske preparater for behandling av blant annet astma og diar± Download PDFInfo
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- NO328489B1 NO328489B1 NO20020979A NO20020979A NO328489B1 NO 328489 B1 NO328489 B1 NO 328489B1 NO 20020979 A NO20020979 A NO 20020979A NO 20020979 A NO20020979 A NO 20020979A NO 328489 B1 NO328489 B1 NO 328489B1
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Landscapes
- Health & Medical Sciences (AREA)
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- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
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Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15164999P | 1999-08-31 | 1999-08-31 | |
| PCT/US2000/040751 WO2001016134A1 (en) | 1999-08-31 | 2000-08-28 | Selective antagonists of a2b adenosine receptors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| NO20020979D0 NO20020979D0 (no) | 2002-02-27 |
| NO20020979L NO20020979L (no) | 2002-04-26 |
| NO328489B1 true NO328489B1 (no) | 2010-03-01 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20020979A NO328489B1 (no) | 1999-08-31 | 2002-02-27 | Nye forbindelser og anvendelse av disse for fremstilling av farmasoytiske preparater for behandling av blant annet astma og diar± |
Country Status (22)
| Country | Link |
|---|---|
| EP (1) | EP1208100B1 (de) |
| JP (1) | JP3914434B2 (de) |
| KR (1) | KR100502757B1 (de) |
| CN (1) | CN1178940C (de) |
| AR (1) | AR029178A1 (de) |
| AT (1) | ATE236160T1 (de) |
| AU (1) | AU760071B2 (de) |
| BR (1) | BR0013673A (de) |
| CA (1) | CA2383351C (de) |
| DE (1) | DE60001969T2 (de) |
| DK (1) | DK1208100T3 (de) |
| ES (1) | ES2190422T3 (de) |
| HK (1) | HK1049835B (de) |
| IL (2) | IL148366A0 (de) |
| MX (1) | MXPA02002262A (de) |
| NO (1) | NO328489B1 (de) |
| NZ (1) | NZ517546A (de) |
| PT (1) | PT1208100E (de) |
| TR (1) | TR200201132T2 (de) |
| TW (1) | TWI262921B (de) |
| WO (1) | WO2001016134A1 (de) |
| ZA (1) | ZA200201650B (de) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6403567B1 (en) | 1999-06-22 | 2002-06-11 | Cv Therapeutics, Inc. | N-pyrazole A2A adenosine receptor agonists |
| USRE47351E1 (en) | 1999-06-22 | 2019-04-16 | Gilead Sciences, Inc. | 2-(N-pyrazolo)adenosines with application as adenosine A2A receptor agonists |
| CA2671940A1 (en) | 2000-02-23 | 2001-08-30 | Cv Therapeutics, Inc. | Identification of partial agonists of the a2a adenosine receptor |
| US6770651B2 (en) | 2001-06-29 | 2004-08-03 | Venkata Palle | A2B adenosine receptor antagonists |
| US8470801B2 (en) | 2002-07-29 | 2013-06-25 | Gilead Sciences, Inc. | Myocardial perfusion imaging methods and compositions |
| JP2006528199A (ja) * | 2003-07-22 | 2006-12-14 | シーブイ・セラピューティクス・インコーポレイテッド | Ａ１アデノシン受容体拮抗薬 |
| JPWO2005053695A1 (ja) * | 2003-12-04 | 2007-12-06 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 多発性硬化症予防剤または治療剤 |
| JP5001012B2 (ja) * | 2004-02-14 | 2012-08-15 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Ｈｍ７４ａ受容体活性を有する薬剤 |
| CA2583986A1 (en) * | 2004-10-15 | 2006-04-27 | Cv Therapeutics, Inc. | Method of preventing and treating airway remodeling and pulmonary inflammation using a2b adenosine receptor antagonists |
| CA2583185A1 (en) | 2004-10-20 | 2006-04-27 | Cv Therapeutics, Inc. | Use of a2a adenosine receptor agonists |
| ES2270715B1 (es) | 2005-07-29 | 2008-04-01 | Laboratorios Almirall S.A. | Nuevos derivados de pirazina. |
| ES2274712B1 (es) | 2005-10-06 | 2008-03-01 | Laboratorios Almirall S.A. | Nuevos derivados imidazopiridina. |
| ES2273599B1 (es) | 2005-10-14 | 2008-06-01 | Universidad De Barcelona | Compuestos para el tratamiento de la fibrilacion auricular. |
| KR101494125B1 (ko) | 2006-02-03 | 2015-02-16 | 길리애드 사이언시즈, 인코포레이티드 | Ａ2ａ-아데노신 수용체 효능제 및 이의 다형체의 제조 방법 |
| US7795427B2 (en) * | 2006-02-14 | 2010-09-14 | New York University | Methods for inhibiting osteoclast differentiation, formation, or function and for increasing bone mass |
| DE102011005232A1 (de) | 2011-03-08 | 2012-09-13 | AristoCon GmbH & Co. KG | Adenosin und seine Derivate zur Verwendung in der Schmerztherapie |
| US11370792B2 (en) | 2015-12-14 | 2022-06-28 | Raze Therapeutics, Inc. | Caffeine inhibitors of MTHFD2 and uses thereof |
| CA3126735A1 (en) | 2019-01-11 | 2020-07-16 | Omeros Corporation | Methods and compositions for treating cancer |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE7810946L (sv) * | 1978-10-20 | 1980-04-21 | Draco Ab | Metod att behandla kronisk obstruktiv luftvegssjukdom |
| DE4019892A1 (de) * | 1990-06-22 | 1992-01-02 | Boehringer Ingelheim Kg | Neue xanthinderivate |
| CA2098846A1 (en) * | 1990-12-21 | 1992-06-22 | David G. Smith | Xanthine derivatives |
| GB9210839D0 (en) * | 1992-05-21 | 1992-07-08 | Smithkline Beecham Plc | Novel compounds |
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2000
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- 2000-08-28 KR KR10-2002-7002718A patent/KR100502757B1/ko not_active IP Right Cessation
- 2000-08-28 DK DK00971055T patent/DK1208100T3/da active
- 2000-08-28 DE DE60001969T patent/DE60001969T2/de not_active Expired - Lifetime
- 2000-08-28 ES ES00971055T patent/ES2190422T3/es not_active Expired - Lifetime
- 2000-08-28 BR BR0013673-5A patent/BR0013673A/pt not_active Application Discontinuation
- 2000-08-28 AT AT00971055T patent/ATE236160T1/de not_active IP Right Cessation
- 2000-08-28 NZ NZ517546A patent/NZ517546A/en unknown
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| ZA200201650B (en) | 2003-05-28 |
| IL148366A (en) | 2006-12-10 |
| DK1208100T3 (da) | 2003-06-30 |
| TWI262921B (en) | 2006-10-01 |
| JP3914434B2 (ja) | 2007-05-16 |
| WO2001016134A1 (en) | 2001-03-08 |
| CA2383351A1 (en) | 2001-03-08 |
| CA2383351C (en) | 2005-11-01 |
| AU8034800A (en) | 2001-03-26 |
| HK1049835B (zh) | 2005-04-08 |
| DE60001969T2 (de) | 2004-02-05 |
| NO20020979L (no) | 2002-04-26 |
| KR20020041419A (ko) | 2002-06-01 |
| ATE236160T1 (de) | 2003-04-15 |
| JP2003508398A (ja) | 2003-03-04 |
| IL148366A0 (en) | 2002-09-12 |
| EP1208100A1 (de) | 2002-05-29 |
| HK1049835A1 (en) | 2003-05-30 |
| BR0013673A (pt) | 2002-05-28 |
| AR029178A1 (es) | 2003-06-18 |
| TR200201132T2 (tr) | 2002-08-21 |
| NZ517546A (en) | 2003-10-31 |
| PT1208100E (pt) | 2003-07-31 |
| NO20020979D0 (no) | 2002-02-27 |
| EP1208100B1 (de) | 2003-04-02 |
| KR100502757B1 (ko) | 2005-07-22 |
| CN1377352A (zh) | 2002-10-30 |
| MXPA02002262A (es) | 2002-09-30 |
| DE60001969D1 (de) | 2003-05-08 |
| CN1178940C (zh) | 2004-12-08 |
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