NZ541009A - Method of treating nausea, vomiting, retching or any combination thereof - Google Patents
Method of treating nausea, vomiting, retching or any combination thereofInfo
- Publication number
- NZ541009A NZ541009A NZ541009A NZ54100904A NZ541009A NZ 541009 A NZ541009 A NZ 541009A NZ 541009 A NZ541009 A NZ 541009A NZ 54100904 A NZ54100904 A NZ 54100904A NZ 541009 A NZ541009 A NZ 541009A
- Authority
- NZ
- New Zealand
- Prior art keywords
- vomiting
- retching
- nausea
- combination
- group
- Prior art date
Links
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K41/00—Medicinal preparations obtained by treating materials with wave energy or particle radiation ; Therapies using these preparations
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pyridine Compounds (AREA)
- Dental Preparations (AREA)
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| US49247803P | 2003-08-04 | 2003-08-04 | |
| PCT/US2004/000809 WO2004062624A2 (en) | 2003-01-13 | 2004-01-13 | Method of treating nausea, vomiting, retching or any combination thereof |
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| NZ541009A true NZ541009A (en) | 2007-09-28 |
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| JP (1) | JP2006516977A (enExample) |
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| BR (1) | BRPI0406748A (enExample) |
| CA (1) | CA2512022A1 (enExample) |
| DE (1) | DE602004005814T2 (enExample) |
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| NZ (1) | NZ541009A (enExample) |
| PL (1) | PL378369A1 (enExample) |
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| GB0216027D0 (en) * | 2002-07-10 | 2002-08-21 | Arachnova Therapeutics Ltd | New therapeutic use |
| US20040048874A1 (en) * | 2001-05-22 | 2004-03-11 | Bardsley Hazel Judith | New therapeutic use of 4-(2-fluorophenyl)-6-methyl-2-(1-piperazinyl)thieno[2,3-D]pyrimidine |
| EP1539172A1 (en) * | 2002-08-29 | 2005-06-15 | Arachnova Therapeutics Ltd. | New therapeutic uses of (4-(2-fluorophenyl)-6-methyl-2-(1-piperazinyl) thieno[2,3-d]pyrimidine |
| AU2004204827B2 (en) * | 2003-01-13 | 2006-06-29 | Dynogen Pharmaceuticals, Inc. | Method of treating nausea, vomiting, retching or any combination thereof |
| BRPI0406749A (pt) * | 2003-01-13 | 2005-12-20 | Dynogen Pharmaceuticals Inc | Métodos relacionados ao tratamento de distúrbios fincionais do intestino e composição farmacêutica |
| JO2735B1 (en) | 2003-01-30 | 2013-09-15 | هيلسين هيلث كير أس ايه. | Liquid pharmaceutical formations of balloonosterone |
| US8598219B2 (en) | 2003-01-30 | 2013-12-03 | Helsinn Healthcare Sa | Liquid pharmaceutical formulations of palonosetron |
| JP2006522144A (ja) * | 2003-04-04 | 2006-09-28 | ダイノゲン ファーマシューティカルズ，インコーポレイテッド | 下部尿路障害の治療方法 |
| WO2005007600A2 (en) * | 2003-07-11 | 2005-01-27 | Eisai Co., Ltd. | Novel methods using aminobenzoic acid compounds |
| US20060100290A1 (en) * | 2003-07-28 | 2006-05-11 | Dunaway Leslie J | Treatment of allergic rhinitis and asthma |
| US20050282879A1 (en) * | 2004-06-17 | 2005-12-22 | Foad Salehani | Methods and composition for treatment of migraine and symptoms thereof |
| WO2006066197A1 (en) * | 2004-12-17 | 2006-06-22 | Janssen Pharmaceutica, N.V. | Tetrahydroisoquinoline compounds for treatment of cns disorders |
| WO2006105117A2 (en) * | 2005-03-28 | 2006-10-05 | Dynogen Pharmaceuticals, Inc. | Method of treating disorders and conditions using peripherally-restricted antagonists and inhibitors |
| EP1906951A4 (en) * | 2005-07-01 | 2009-05-27 | Dynogen Pharmaceuticals Inc | COMPOSITIONS AND METHODS FOR TREATING GASTROINTESTINAL HYPOMOTILITY AND RELEVANT DISEASES |
| WO2007090113A2 (en) * | 2006-02-01 | 2007-08-09 | Weg Stuart L | Use of antifungal compositions to treat upper gastrointestinal conditions |
| US20070254899A1 (en) * | 2006-03-31 | 2007-11-01 | Dynogen Pharmaceuticals, Inc. | Soluble salts of thieno[2,3-d]pyrimidine derivatives |
| US20070259933A1 (en) * | 2006-05-04 | 2007-11-08 | Xenoport, Inc. | Compositions, dosage forms and methods of treating emesis |
| WO2008038106A1 (en) * | 2006-09-27 | 2008-04-03 | Orchid Chemicals & Pharmaceuticals Limited | Venlafaxine extended release formulations |
| KR101779991B1 (ko) * | 2009-05-20 | 2017-09-19 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 병소성 전정 질환을 치료하기 위한 세로토닌 5-ｈｔ3 수용체 길항제의 용도 |
| RU2679448C2 (ru) | 2013-03-14 | 2019-02-11 | Редхилл Байофарма Лтд. | Твердые лекарственные формы, обладающие противорвотным действием, с замедленным высвобождением |
| MX373002B (es) | 2014-03-11 | 2020-04-30 | Redhill Biopharma Ltd | Formas de dosificacion sólida de liberación extendida de ondansetrón para tratar bien sea síntomas de náusea, vómito o diarrea |
| PL3442537T3 (pl) | 2016-04-14 | 2024-07-15 | Sensorion | (+)-azasetron do zastosowania w leczeniu zaburzeń ucha |
| WO2022015628A2 (en) * | 2020-07-15 | 2022-01-20 | St. Jude Children's Research Hospital, Inc. | Obese ferret model and methods of establishing and using the same |
| WO2022232574A1 (en) | 2021-04-29 | 2022-11-03 | Tilray, Inc. | Cannabidiol-dominant formulations, methods of manufacturing, and uses thereof |
| WO2023164132A1 (en) * | 2022-02-25 | 2023-08-31 | Neuraxis, Inc. | Auricular nerve field stimulation device and methods for using the same |
Family Cites Families (59)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US36500A (en) * | 1862-09-23 | Joseph banks | ||
| US44450A (en) * | 1864-09-27 | Improvement in ore-crushers | ||
| US254172A (en) * | 1882-02-28 | Half to laweence | ||
| US107244A (en) * | 1870-09-13 | Improved manner of treating- cod-liver and castor-oils | ||
| US254171A (en) * | 1882-02-28 | Car-axle box | ||
| US48874A (en) * | 1865-07-18 | Improved extension door-knobs | ||
| US203055A (en) * | 1878-04-30 | Improvement in carpet-stretchers | ||
| US36549A (en) * | 1862-09-23 | Improvement in caps | ||
| US4225407A (en) * | 1979-04-04 | 1980-09-30 | The Dow Chemical Company | Cathodic electrodeposition of polymers onto a conductive surface |
| JPS60146891A (ja) * | 1984-01-05 | 1985-08-02 | Mitsubishi Chem Ind Ltd | 〔２，３−ｄ〕チエノピリミジン誘導体およびその塩 |
| DE3689974T2 (de) * | 1985-03-14 | 1994-11-03 | Beecham Group Plc | Arzneimittel zur Behandlung von Emesis. |
| GB8516083D0 (en) * | 1985-06-25 | 1985-07-31 | Glaxo Group Ltd | Heterocyclic compounds |
| GB8701022D0 (en) * | 1987-01-19 | 1987-02-18 | Beecham Group Plc | Treatment |
| EP0297651B1 (en) * | 1987-06-29 | 1993-11-03 | Duphar International Research B.V | Anellated indole derivatives |
| US5223511A (en) * | 1987-09-23 | 1993-06-29 | Boehringer Ingelheim Italia S.P.A. | Benzimidazoline-2-oxo-1-carboxylic acid compounds useful as 5-HT receptor antagonists |
| CA1304082C (en) | 1987-10-22 | 1992-06-23 | Tetsuya Tahara | Benzoxazine compounds and pharmaceutical use thereof |
| US5530008A (en) * | 1989-04-21 | 1996-06-25 | Sandoz Ltd. | Use of 5-HT3 receptor antagonists in treating panic disorders or obsessive compulsive disorders |
| US5225407A (en) * | 1990-02-22 | 1993-07-06 | Glaxo Group Limited | 5-HT3 receptor antagonists for the treatment of autism |
| JPH06508836A (ja) * | 1991-06-26 | 1994-10-06 | セプラコア，インコーポレーテッド | 光学的に純粋なｒ（＋）オンダンセトロンを使用する嘔吐、吐き気および他の障害の治療のための方法および組成物 |
| JP2699794B2 (ja) * | 1992-03-12 | 1998-01-19 | 三菱化学株式会社 | チエノ〔３，２−ｂ〕ピリジン誘導体 |
| GB9214184D0 (en) | 1992-07-03 | 1992-08-12 | Smithkline Beecham Plc | Pharmaceuticals |
| JPH0616557A (ja) * | 1992-12-21 | 1994-01-25 | Mitsubishi Kasei Corp | 脳機能障害改善剤 |
| GB9406857D0 (en) * | 1994-04-07 | 1994-06-01 | Sandoz Ltd | Improvements in or relating to organic compounds |
| US5576317A (en) * | 1994-12-09 | 1996-11-19 | Pfizer Inc. | NK-1 receptor antagonists and 5HT3 receptor antagonists for the treatment of emesis |
| HUP9901208A3 (en) * | 1995-07-28 | 2002-10-28 | Dainippon Pharmaceutical Co | (r)-5-bromo-n-(1-ethyl-4-methylhexahydro-1h-1,4-diazepin-6-yl)-2-methoxy-6-methyl-amino-3-pyridine-carboxamide, process for producing the same and medicinal composition containing the same |
| AU702594B2 (en) * | 1995-10-13 | 1999-02-25 | Duphar International Research B.V. | Process for the preparation of enantiomerically pure imidazolyl compounds |
| KR100469029B1 (ko) * | 1996-02-15 | 2005-05-27 | 얀센 파마슈티카 엔.브이. | 세로토닌재흡수억제제의위장효과를극복하기위한5ht4수용체길항제의용도 |
| DE69816060T2 (de) * | 1997-04-18 | 2004-04-22 | Janssen Pharmaceutica N.V. | Verwendung von 5ht3 antagonisten zum fördern der darmspülung |
| JPH10298078A (ja) | 1997-05-06 | 1998-11-10 | Mitsubishi Chem Corp | 抗不安薬 |
| ES2128266B1 (es) | 1997-07-08 | 2000-01-16 | Vita Invest Sa | Compuestos derivados de tiofeno y benzotiofeno y utilizacion y composicion correspondientes. |
| DE19813661A1 (de) * | 1997-08-01 | 1999-02-04 | Solvay Pharm Gmbh | Gegen Racemisierung stabilisierte pharmazeutische Zubereitungen von Cilansetron |
| DE19734444A1 (de) * | 1997-08-08 | 1999-02-11 | Basf Ag | 3-Substituierte 3,4,5,7-Tetrahydro-pyrrolo(3',4':4,5) thieno (2,3-d) pyrimidin-Derivate, ihre Herstellung und Verwendung |
| US6156771A (en) * | 1997-08-28 | 2000-12-05 | Rubin; Walter | Method for alleviation of lower gastrointestinal disorders in a human patient |
| US6117879A (en) * | 1997-09-16 | 2000-09-12 | Solvay Pharmaceuticals Gmbh | Methods of using moxonidine to inhibit nociceptive pain |
| EP0901790B1 (en) * | 1997-09-16 | 2001-05-30 | Solvay Pharmaceuticals GmbH | Use of moxonidine for the Treatment of neuropathic pain |
| GB9721139D0 (en) * | 1997-10-07 | 1997-12-03 | Glaxo Group Ltd | Medicaments |
| FR2781671A1 (fr) | 1998-07-28 | 2000-02-04 | Synthelabo | Compositions pharmaceutiques contenant un inhibiteur de la recapture de la serotonine et leur application en therapeutique |
| US6376550B1 (en) * | 1999-02-09 | 2002-04-23 | Asta Medica Ag | Pharmaceutical compositions containing tramadol for migraine |
| AU3422800A (en) * | 1999-02-18 | 2000-09-04 | Novartis Ag | Use of 5-ht3 receptor antagonists |
| US6362202B1 (en) * | 1999-03-02 | 2002-03-26 | Sepracor Inc. | Methods and compositions using (−) norcisapride in combination with proton pump inhibitors or H2 receptor antagonists |
| US6353005B1 (en) | 1999-03-02 | 2002-03-05 | Sepracor, Inc. | Method and compositions using (+) norcisapride in combination with proton pump inhibitors or H2 receptor antagonist |
| US6589570B1 (en) * | 1999-04-12 | 2003-07-08 | University Of Madras | Pharmaceutical formulation useful for the treatment of hepatitis B, hepatitis C and other viral infections of the liver and a process for its preparation |
| DE19929197A1 (de) * | 1999-06-25 | 2000-12-28 | Novosis Pharma Ag | Transdermalsysteme zur Abgabe von 5-HT3-Rezeptor-Antagonisten und ihre Verwendung zur antiemitischen Behandlung |
| ES2247572T3 (es) * | 1999-07-01 | 2006-03-01 | PHARMACIA & UPJOHN COMPANY LLC | (s,s)-reboxetina para tratar las cefaleas migrañosas. |
| GB2355191A (en) * | 1999-10-12 | 2001-04-18 | Laxdale Ltd | Combination formulations for fatigue, head injury and strokes |
| TWI263496B (en) | 1999-12-10 | 2006-10-11 | Novartis Ag | Pharmaceutical combinations and their use in treating gastrointestinal disorders |
| ES2188344B1 (es) | 2000-11-29 | 2004-09-16 | Laboratorios Vita, S.A. | Compuestos derivados de benzotiofeno, su procedimiento de obtencion y utilizacion de los mismos. |
| US20020107244A1 (en) * | 2001-02-02 | 2002-08-08 | Howard Harry R. | Combination treatment for depression |
| US20040048874A1 (en) * | 2001-05-22 | 2004-03-11 | Bardsley Hazel Judith | New therapeutic use of 4-(2-fluorophenyl)-6-methyl-2-(1-piperazinyl)thieno[2,3-D]pyrimidine |
| GB0112494D0 (en) | 2001-05-22 | 2001-07-11 | Arachnova Therapeutics Ltd | New therapeutic use |
| GB0216027D0 (en) * | 2002-07-10 | 2002-08-21 | Arachnova Therapeutics Ltd | New therapeutic use |
| CA2473392A1 (en) * | 2002-01-18 | 2003-07-31 | Aryx Therapeutics | 5-ht3 receptor antagonists and methods of use |
| GB0202265D0 (en) * | 2002-01-31 | 2002-03-20 | Arachnova Therapeutics Ltd | New therapeutic use |
| AU2003225837B2 (en) * | 2002-03-15 | 2008-11-06 | Forest Laboratories Holdings Limited | NE and 5-HT reuptake inhibitors for treating visceral pain syndromes |
| AU2003255712B2 (en) | 2002-07-10 | 2007-03-15 | Arachnova Therapeutics Ltd. | 4-(2-fluorophenyl)-6-methyl-2(1-piperazinyl)thieno(2,3-D) pyrimidine in the treatment of functional bowel disorder |
| EP1539172A1 (en) * | 2002-08-29 | 2005-06-15 | Arachnova Therapeutics Ltd. | New therapeutic uses of (4-(2-fluorophenyl)-6-methyl-2-(1-piperazinyl) thieno[2,3-d]pyrimidine |
| AU2003290363A1 (en) | 2002-12-24 | 2004-07-22 | Amedis Pharmaceuticals Ltd. | Therapeutic use of selective noradrenaline reuptake inhibitors |
| AU2004204827B2 (en) * | 2003-01-13 | 2006-06-29 | Dynogen Pharmaceuticals, Inc. | Method of treating nausea, vomiting, retching or any combination thereof |
| BRPI0406749A (pt) * | 2003-01-13 | 2005-12-20 | Dynogen Pharmaceuticals Inc | Métodos relacionados ao tratamento de distúrbios fincionais do intestino e composição farmacêutica |
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2004
- 2004-01-13 AU AU2004204827A patent/AU2004204827B2/en not_active Ceased
- 2004-01-13 KR KR1020057012925A patent/KR20050094843A/ko not_active Withdrawn
- 2004-01-13 MX MXPA05007379A patent/MXPA05007379A/es active IP Right Grant
- 2004-01-13 WO PCT/US2004/000809 patent/WO2004062624A2/en not_active Ceased
- 2004-01-13 AT AT04701830T patent/ATE359079T1/de not_active IP Right Cessation
- 2004-01-13 JP JP2006500937A patent/JP2006516977A/ja active Pending
- 2004-01-13 ES ES04701830T patent/ES2285407T3/es not_active Expired - Lifetime
- 2004-01-13 CA CA002512022A patent/CA2512022A1/en not_active Abandoned
- 2004-01-13 BR BR0406748-7A patent/BRPI0406748A/pt not_active IP Right Cessation
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- 2004-01-13 EP EP04701830A patent/EP1567163B1/en not_active Expired - Lifetime
- 2004-01-13 US US10/757,981 patent/US20040147510A1/en not_active Abandoned
- 2004-05-14 US US10/846,978 patent/US20040254171A1/en not_active Abandoned
- 2004-05-14 US US10/846,979 patent/US7094786B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| EP1567163B1 (en) | 2007-04-11 |
| DE602004005814D1 (de) | 2007-05-24 |
| US20040254172A1 (en) | 2004-12-16 |
| PL378369A1 (pl) | 2006-04-03 |
| AU2004204827B2 (en) | 2006-06-29 |
| US7094786B2 (en) | 2006-08-22 |
| JP2006516977A (ja) | 2006-07-13 |
| WO2004062624A2 (en) | 2004-07-29 |
| US20040254171A1 (en) | 2004-12-16 |
| EP1567163A2 (en) | 2005-08-31 |
| ATE359079T1 (de) | 2007-05-15 |
| US20040147510A1 (en) | 2004-07-29 |
| KR20050094843A (ko) | 2005-09-28 |
| CA2512022A1 (en) | 2004-07-29 |
| WO2004062624A3 (en) | 2005-04-07 |
| EP1567163A4 (en) | 2006-01-18 |
| DE602004005814T2 (de) | 2008-01-10 |
| ES2285407T3 (es) | 2007-11-16 |
| MXPA05007379A (es) | 2006-02-10 |
| BRPI0406748A (pt) | 2005-12-20 |
| AU2004204827A1 (en) | 2004-07-29 |
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