AU2003241585B2 - Use of mGluR5 antagonists for the treatment of GERD - Google Patents
Use of mGluR5 antagonists for the treatment of GERD Download PDFInfo
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- AU2003241585B2 AU2003241585B2 AU2003241585A AU2003241585A AU2003241585B2 AU 2003241585 B2 AU2003241585 B2 AU 2003241585B2 AU 2003241585 A AU2003241585 A AU 2003241585A AU 2003241585 A AU2003241585 A AU 2003241585A AU 2003241585 B2 AU2003241585 B2 AU 2003241585B2
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- antagonist
- glutamate receptor
- metabotropic glutamate
- treatment
- acceptable salt
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- Steroid Compounds (AREA)
- Pyridine Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| SE0201943A SE0201943D0 (sv) | 2002-06-20 | 2002-06-20 | New use |
| SE0201943-8 | 2002-06-20 | ||
| PCT/US2003/016223 WO2004000316A1 (en) | 2002-06-20 | 2003-06-19 | Use of mglur5 antagonists for the treatment of gerd |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2003241585A1 AU2003241585A1 (en) | 2004-01-06 |
| AU2003241585B2 true AU2003241585B2 (en) | 2009-06-25 |
Family
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2003241585A Ceased AU2003241585B2 (en) | 2002-06-20 | 2003-06-19 | Use of mGluR5 antagonists for the treatment of GERD |
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|---|---|
| EP (1) | EP1513525B1 (https=) |
| JP (2) | JP4683920B2 (https=) |
| CN (1) | CN100430056C (https=) |
| AT (1) | ATE395059T1 (https=) |
| AU (1) | AU2003241585B2 (https=) |
| BR (1) | BR0311759A (https=) |
| CA (1) | CA2489730C (https=) |
| CY (1) | CY1107954T1 (https=) |
| DE (1) | DE60320990D1 (https=) |
| DK (1) | DK1513525T3 (https=) |
| ES (1) | ES2304510T3 (https=) |
| IL (1) | IL165138A0 (https=) |
| IS (1) | IS7654A (https=) |
| MX (1) | MXPA04012659A (https=) |
| NO (1) | NO20050154L (https=) |
| NZ (1) | NZ536559A (https=) |
| PL (1) | PL372186A1 (https=) |
| PT (1) | PT1513525E (https=) |
| RU (1) | RU2324484C2 (https=) |
| SE (1) | SE0201943D0 (https=) |
| SI (1) | SI1513525T1 (https=) |
| UA (1) | UA81627C2 (https=) |
| WO (1) | WO2004000316A1 (https=) |
| ZA (1) | ZA200409908B (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US7964609B2 (en) | 2002-06-20 | 2011-06-21 | Astrazeneca Ab | Use of mGluR5 antagonists for the treatment of gerd |
| SE0303418D0 (sv) * | 2003-12-17 | 2003-12-17 | Astrazeneca Ab | New use 1 |
| WO2005060971A1 (en) * | 2003-12-18 | 2005-07-07 | Astrazeneca Ab | Treatment of reflux-related diseases |
| WO2005060961A2 (en) * | 2003-12-18 | 2005-07-07 | Astrazeneca Ab | Treatment of transient lower esophageal sphincter relaxations (tlesrs) and gastro-esophageal reflux disease (gerd) |
| WO2005077345A1 (en) * | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Compounds for the treatment of gastro-esophageal reflux disease |
| WO2005077368A2 (en) * | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Treatment of gastro-esophageal reflux disease (gerd) |
| RU2381226C2 (ru) * | 2004-02-18 | 2010-02-10 | Астразенека Аб | Полигетероциклические соединения и их применение в качестве антагонистов метаботропного рецептора глутамата |
| BRPI0507499A (pt) * | 2004-02-18 | 2007-07-24 | Astrazeneca Ab | composto ou um sal farmaceuticamente aceitável ou hidrato dos mesmos, composição farmacêutica, uso do composto, e, métodos para tratar distúrbios mediados por mglur 5 e para inibir a ativação de receptores de mglur 5 |
| GB0514296D0 (en) * | 2005-07-12 | 2005-08-17 | Novartis Ag | Organic compounds |
| EP2468727A1 (en) * | 2006-03-29 | 2012-06-27 | F. Hoffmann-La Roche AG | Pyridine and pyrimidine derivatives as MGLUR2 antagonists |
| EP2272509A1 (en) | 2006-09-11 | 2011-01-12 | Novartis AG | New Uses of metabotropic glutamate receptors |
| JP2008245225A (ja) * | 2007-03-29 | 2008-10-09 | Kddi Corp | 波長パス経路決定装置、波長パス設定制御システム及びプログラム |
| WO2009024491A1 (en) * | 2007-08-20 | 2009-02-26 | F. Hoffmann-La Roche Ag | Use of mglur5 antagonists for the treatment of gerd |
| EP2320892A2 (en) | 2008-06-30 | 2011-05-18 | Novartis AG | Combination products |
| CN102573842A (zh) | 2009-07-23 | 2012-07-11 | 诺瓦提斯公司 | 氮杂双环烷基衍生物或吡咯烷-2-酮衍生物的用途 |
| JO3250B1 (ar) | 2009-09-22 | 2018-09-16 | Novartis Ag | إستعمال منشطات مستقبل نيكوتينيك أسيتيل كولين ألفا 7 |
| WO2011048150A1 (en) | 2009-10-20 | 2011-04-28 | Novartis Ag | Use of 1h-quinazoline-2,4-diones |
| JP2013529622A (ja) | 2010-06-24 | 2013-07-22 | ノバルティス アーゲー | １ｈ−キナゾリン−２，４−ジオンの使用 |
| KR20140003580A (ko) | 2011-01-27 | 2014-01-09 | 노파르티스 아게 | 니코틴성 아세틸콜린 수용체 알파 7 활성화제의 용도 |
| CN103889427A (zh) | 2011-09-07 | 2014-06-25 | 诺华股份有限公司 | 1h-喹唑啉-2,4-二酮用于预防或治疗光敏性癫痫的应用 |
| CN105263492B (zh) | 2013-01-15 | 2018-04-10 | 诺华有限公司 | α7烟碱型乙酰胆碱受体激动剂在治疗发作性睡病中的应用 |
| BR112015016992A8 (pt) | 2013-01-15 | 2018-01-23 | Novartis Ag | uso de agonistas do receptor alfa 7 nicotínico de acetilcolina |
| BR112022005579A2 (pt) * | 2019-11-05 | 2022-06-21 | Claes Thulin | 4-[5-[(rac)-1-[5-(3-clorofenil)-3-isoxazolil]etoxi]-4-metil-4h-1,2,4-triazol-3-il]piridina para uso na prevenção e/ou no tratamento de surmenage em um mamífero |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001012627A1 (en) * | 1999-08-19 | 2001-02-22 | Nps Pharmaceuticals, Inc. | Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0250572A1 (en) * | 1986-01-03 | 1988-01-07 | The University Of Melbourne | Gastro-oesophageal reflux composition |
| SE9603408D0 (sv) * | 1996-09-18 | 1996-09-18 | Astra Ab | Medical use |
| CA2332774A1 (en) * | 1998-05-15 | 1999-11-25 | Dov Michaeli | Method for the treatment of gastroesophageal reflux disease |
| RU2144331C1 (ru) * | 1998-11-05 | 2000-01-20 | Московский НИИ уха, горла и носа | Способ лечения хронического гиперпластического ларингита |
| CN1703403A (zh) * | 2000-10-02 | 2005-11-30 | 詹森药业有限公司 | 趋代谢的谷氨酸盐受体拮抗剂 |
-
2002
- 2002-06-20 SE SE0201943A patent/SE0201943D0/xx unknown
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2003
- 2003-06-19 JP JP2004515703A patent/JP4683920B2/ja not_active Expired - Fee Related
- 2003-06-19 NZ NZ536559A patent/NZ536559A/en not_active IP Right Cessation
- 2003-06-19 UA UA20041210177A patent/UA81627C2/ru unknown
- 2003-06-19 CA CA2489730A patent/CA2489730C/en not_active Expired - Fee Related
- 2003-06-19 EP EP03731333A patent/EP1513525B1/en not_active Expired - Lifetime
- 2003-06-19 DK DK03731333T patent/DK1513525T3/da active
- 2003-06-19 RU RU2005101411/15A patent/RU2324484C2/ru not_active IP Right Cessation
- 2003-06-19 MX MXPA04012659A patent/MXPA04012659A/es not_active Application Discontinuation
- 2003-06-19 PL PL03372186A patent/PL372186A1/xx not_active Application Discontinuation
- 2003-06-19 AU AU2003241585A patent/AU2003241585B2/en not_active Ceased
- 2003-06-19 PT PT03731333T patent/PT1513525E/pt unknown
- 2003-06-19 CN CNB038141760A patent/CN100430056C/zh not_active Expired - Fee Related
- 2003-06-19 WO PCT/US2003/016223 patent/WO2004000316A1/en not_active Ceased
- 2003-06-19 SI SI200331220T patent/SI1513525T1/sl unknown
- 2003-06-19 DE DE60320990T patent/DE60320990D1/de not_active Expired - Lifetime
- 2003-06-19 ES ES03731333T patent/ES2304510T3/es not_active Expired - Lifetime
- 2003-06-19 AT AT03731333T patent/ATE395059T1/de active
- 2003-06-19 BR BR0311759-6A patent/BR0311759A/pt not_active IP Right Cessation
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2004
- 2004-11-10 IL IL16513804A patent/IL165138A0/xx unknown
- 2004-12-07 ZA ZA200409908A patent/ZA200409908B/en unknown
-
2005
- 2005-01-11 NO NO20050154A patent/NO20050154L/no not_active Application Discontinuation
- 2005-01-19 IS IS7654A patent/IS7654A/is unknown
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2008
- 2008-05-21 CY CY20081100527T patent/CY1107954T1/el unknown
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2010
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001012627A1 (en) * | 1999-08-19 | 2001-02-22 | Nps Pharmaceuticals, Inc. | Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
Non-Patent Citations (2)
| Title |
|---|
| Gasparini et al. Neuropharmacology (1999) vol. 38, no. 10 pages 1493-1503 * |
| Knopfel et al. Journal of Medicinal Chemistry (1995) vol. 38, no. 9 pages 1417-1426 * |
Also Published As
| Publication number | Publication date |
|---|---|
| HK1075833A1 (en) | 2005-12-30 |
| CN1662235A (zh) | 2005-08-31 |
| DE60320990D1 (de) | 2008-06-26 |
| CA2489730A1 (en) | 2003-12-31 |
| ATE395059T1 (de) | 2008-05-15 |
| PT1513525E (pt) | 2008-06-24 |
| EP1513525A1 (en) | 2005-03-16 |
| MXPA04012659A (es) | 2006-05-25 |
| CY1107954T1 (el) | 2013-09-04 |
| SE0201943D0 (sv) | 2002-06-20 |
| CA2489730C (en) | 2011-11-22 |
| WO2004000316A1 (en) | 2003-12-31 |
| ES2304510T3 (es) | 2008-10-16 |
| JP2011068669A (ja) | 2011-04-07 |
| PL372186A1 (en) | 2005-07-11 |
| NZ536559A (en) | 2007-08-31 |
| ZA200409908B (en) | 2006-08-30 |
| EP1513525B1 (en) | 2008-05-14 |
| RU2324484C2 (ru) | 2008-05-20 |
| JP2006507225A (ja) | 2006-03-02 |
| DK1513525T3 (da) | 2008-08-11 |
| SI1513525T1 (sl) | 2008-08-31 |
| JP4683920B2 (ja) | 2011-05-18 |
| IL165138A0 (en) | 2005-12-18 |
| BR0311759A (pt) | 2005-03-08 |
| IS7654A (is) | 2005-01-19 |
| AU2003241585A1 (en) | 2004-01-06 |
| NO20050154L (no) | 2005-01-11 |
| CN100430056C (zh) | 2008-11-05 |
| UA81627C2 (ru) | 2008-01-25 |
| RU2005101411A (ru) | 2005-07-10 |
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