WO1994001095A2 - Medicaments pour le traitement de douleurs viscerales et de migraines - Google Patents

Medicaments pour le traitement de douleurs viscerales et de migraines Download PDF

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Publication number
WO1994001095A2
WO1994001095A2 PCT/GB1993/001377 GB9301377W WO9401095A2 WO 1994001095 A2 WO1994001095 A2 WO 1994001095A2 GB 9301377 W GB9301377 W GB 9301377W WO 9401095 A2 WO9401095 A2 WO 9401095A2
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WO
WIPO (PCT)
Prior art keywords
dose
receptor antagonist
treatment
composition according
active
Prior art date
Application number
PCT/GB1993/001377
Other languages
English (en)
Other versions
WO1994001095A3 (fr
Inventor
Gareth John Sanger
Stephen Edward Banner
Original Assignee
Smithkline Beecham Plc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Smithkline Beecham Plc filed Critical Smithkline Beecham Plc
Priority to CA002139440A priority Critical patent/CA2139440A1/fr
Priority to EP93914854A priority patent/EP0650355A1/fr
Priority to AU45076/93A priority patent/AU4507693A/en
Priority to JP6503078A priority patent/JPH07508530A/ja
Publication of WO1994001095A2 publication Critical patent/WO1994001095A2/fr
Publication of WO1994001095A3 publication Critical patent/WO1994001095A3/fr
Priority to KR1019940704887A priority patent/KR950702112A/ko

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Classifications

    • A—HUMAN NECESSITIES
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents

Definitions

  • This invention relates to the use of certain compounds which are 5-HT3 receptor antagonists as visceral analgesics.
  • EP-A-279512 (Beecham Group p.l.c.) describes the use of certain 5-HT3 receptor antagonists, including granisetron (KYTRIL) in the treatment of visceral pain.
  • KYTRIL granisetron
  • Visceral pain is a symptom of irritable bowel syndrome (IBS) and granisetron has been found to desensitise the rectum in IBS patients as shown by double-blind placebo-controlled studies, at doses of 120 ⁇ g/kg and 50 ⁇ g/kg, 120 ⁇ g/kg being most effective. (Prior and Read, 1990; Gut 11 (10) A1174).
  • Granisetron has been found to be active in an animal model of rectal sensitivity to distension (see method described hereafter).
  • 5-HT3 receptor antagonists which have the same effect as granisetron in this model, include zatosetron (Lilly) and metoclopramide.
  • the invention therefore relates to the use of those 5-HT3 receptor antagonists, which are active in the animal model at a dose determined as the dose at which 5-HT3 receptor antagonist activity is observed in standard tests, such as the Bezold-Jarisch model, in the treatment of visceral pain, such as the pain symptoms of IBS, and also migraine.
  • Preferred compounds are active at a lower dose than the 5-HT3 receptor antagonist dose.
  • Compounds which are approved or under clinical investigation are active at a similar dosage level to that which is used for antiemetic use.
  • 5-HT3 receptor antagonists which should be considered for this invention include those specifically and generically disclosed and referenced in EP-A-450757 (Glaxo Group Limited). Rat Model of Colo-rectal Distension
  • a 6-7 cm latex balloon was inserted intra-anally into male Wistar rats (250-650g) under halothane anaesthesia; the balloon catheter was taped to the tail. After recovery the animals were allowed unrestricted movement and were dosed with either vehicle (saline) or 5-hydroxytryptophan (5-HTP lOmgkg " ! subcutaneously).
  • vehicle saline
  • 5-hydroxytryptophan 5-hydroxytryptophan
  • 5-HT3 receptor antagonists or saline were dosed subcutaneously after 3 stable responses were achieved and within 45 min of dosing 5-HTP or vehicle.
  • the visceromotor threshold values were then recorded for a further 30 min.
  • a similar model was described by Ness & Gebhart (1988, Brain Res. 450. 153-169). Maximum percentage changes (within the 30 min post-dose period) in distension pressure were compared with the mean of the pre-dose recordings. Saline control values were then assigned the value of 1.00 and drug induced changes compared directly.
  • Intrathecal administration of granisetron also showed good analgesic activity suggesting that a site of action, of those 5-HT3 receptor antagonists that are visceral analgesics, may be in the spinal cord.
  • 5-HT3 receptor antagonists that are visceral analgesics

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  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention porte sur l'utilisation des antagonistes du récepteur de 5-HT3 qui sont actifs sur un modèle rat de distension colo-rectale à une dose déterminée à laquelle on observe l'activité de l'antagoniste du récepteur de 5-HT3 dans les essais standard tels que le modèle Bezold-Jarisch, dans le traitement de douleurs viscérales telles que les symptômes douloureux du côlon irritable et de la migraine.
PCT/GB1993/001377 1992-07-03 1993-06-30 Medicaments pour le traitement de douleurs viscerales et de migraines WO1994001095A2 (fr)

Priority Applications (5)

Application Number Priority Date Filing Date Title
CA002139440A CA2139440A1 (fr) 1992-07-03 1993-06-30 Medicaments pour le traitement des douleurs viscerales et de la migraine
EP93914854A EP0650355A1 (fr) 1992-07-03 1993-06-30 Medicaments pour le traitement de douleurs viscerales et de migraines
AU45076/93A AU4507693A (en) 1992-07-03 1993-06-30 Medicaments for the treatment of visceral pain and migraine
JP6503078A JPH07508530A (ja) 1992-07-03 1993-06-30 内臓の痛みおよび偏頭痛の治療薬
KR1019940704887A KR950702112A (ko) 1992-07-03 1994-12-31 내장 진통 및 편두통의 치료 약물(Medicaments for the treatment of visceral pain and migraine)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB929214184A GB9214184D0 (en) 1992-07-03 1992-07-03 Pharmaceuticals
GB9214184.5 1992-07-03

Publications (2)

Publication Number Publication Date
WO1994001095A2 true WO1994001095A2 (fr) 1994-01-20
WO1994001095A3 WO1994001095A3 (fr) 1994-04-14

Family

ID=10718169

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB1993/001377 WO1994001095A2 (fr) 1992-07-03 1993-06-30 Medicaments pour le traitement de douleurs viscerales et de migraines

Country Status (7)

Country Link
EP (1) EP0650355A1 (fr)
JP (1) JPH07508530A (fr)
KR (1) KR950702112A (fr)
AU (1) AU4507693A (fr)
CA (1) CA2139440A1 (fr)
GB (1) GB9214184D0 (fr)
WO (1) WO1994001095A2 (fr)

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5726187A (en) * 1992-10-16 1998-03-10 Smithkline Beecham Plc N-alkylpiperidinyl-4-methyl carboxylic esters/amides of condensed ring systems as 5-HT4 receptor antagonists
US5852014A (en) * 1992-03-12 1998-12-22 Smithkline Beecham P.L.C. Condensed indole derivatives as 5HT4 -receptor antagonists
WO1999017755A2 (fr) * 1997-10-07 1999-04-15 Glaxo Group Limited Medicaments
US5998409A (en) * 1992-03-12 1999-12-07 Smithkline Beecham Plc Condensed indole derivatives as 5HT4 -receptor antagonists
WO2000048581A2 (fr) * 1999-02-18 2000-08-24 Novartis Ag Utilisation d'antagonistes du recepteur 5-ht¿3?
WO2001041748A2 (fr) * 1999-12-10 2001-06-14 Novartis Ag Combinaisons pharmaceutiques et leur utilisation dans le traitement de troubles gastro-intestinaux
US7094786B2 (en) 2003-01-13 2006-08-22 Dynogen Pharmaceuticals, Inc. Method of treating nausea, vomiting, retching or any combination thereof
US7470690B2 (en) 2002-07-10 2008-12-30 Dynogen Pharmaceuticals, Inc. 4-(2-Fluorophenyl)-6-methyl-2-(1-piperazinyl)thieno[2,3-D)pyrimidine in the treatment of functional bowel disorder
US7608282B2 (en) * 2003-02-05 2009-10-27 Strakan International Limited Transdermal granisetron
US8246981B2 (en) 2005-05-18 2012-08-21 Abeille Pharamaceuticals, Inc. Transdermal method and patch for emesis

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19807535A1 (de) * 1998-02-21 1999-08-26 Asta Medica Ag Pharmazeutische Kombinationen mit Tramadol

Citations (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0189002A2 (fr) * 1984-12-20 1986-07-30 Sandoz Ag Traitement de maladies gastro-intestinales utilisant des 5-HT3 antagonistes
EP0254584A2 (fr) * 1986-07-25 1988-01-27 Beecham Group Plc Composés azabicycliques, procédé pour leur préparation et leur utilisation pharmaceutique
GB2192885A (en) * 1986-07-23 1988-01-27 Glaxo Group Ltd Heterocyclic compounds
EP0266899A2 (fr) * 1986-10-03 1988-05-11 Glaxo Group Limited Dérivés d'indole
EP0272876A2 (fr) * 1986-12-17 1988-06-29 Glaxo Group Limited Application des dérivés hétérocycliques pour la fabrication de médicaments
EP0279512A2 (fr) * 1987-01-19 1988-08-24 Beecham Group Plc Emploi de certains antagonistes du récépteur 5-HT3 pour le traitement des douleurs viscérales
EP0287196A1 (fr) * 1987-02-18 1988-10-19 Beecham Group Plc Dérivés de l'indole, un procédé pour leur préparation et compositions pharmaceutiques les contenant
EP0289170A2 (fr) * 1987-04-25 1988-11-02 Beecham Group Plc Composés azabicycliques, leur procédé de préparation et compositions pharmaceutiques les contenant
EP0315316A2 (fr) * 1987-10-02 1989-05-10 Beecham Group Plc Dérivés d'imidazole, procédé pour leur préparation, compositions pharmaceutiques les contenant, et leur application pharmaceutique
EP0315390A2 (fr) * 1987-11-04 1989-05-10 Beecham Group Plc Composés nouveaux de 4-oxobenzotriazine et 4-oxoquinazoline
EP0317088A1 (fr) * 1987-10-22 1989-05-24 Glaxo Group Limited Dérivés cétoniques
WO1989009217A1 (fr) * 1988-03-23 1989-10-05 Beecham Group Plc Nouveaux composes
EP0336759A1 (fr) * 1988-04-07 1989-10-11 Glaxo Group Limited Dérivés d'imidazole
EP0345956A1 (fr) * 1988-05-20 1989-12-13 Glaxo Group Limited Cétones tricycliques
EP0347229A1 (fr) * 1988-06-16 1989-12-20 Glaxo Group Limited Dérivés de l'indole
EP0351385A2 (fr) * 1988-07-12 1990-01-17 BOEHRINGER INGELHEIM ITALIA S.p.A. Dérivés d'amidino et de guanidino
EP0356098A2 (fr) * 1988-08-15 1990-02-28 Glaxo Group Limited Dérivés de lactames
EP0357416A2 (fr) * 1988-09-01 1990-03-07 Glaxo Group Limited Utilisation des antagonistes de la sérotonine dans le traitement de l'asservissement aux drogues
EP0358903A2 (fr) * 1988-07-29 1990-03-21 Dainippon Pharmaceutical Co., Ltd. Dérivés d'acide indazole-3-carboxylique
EP0361317A2 (fr) * 1988-09-27 1990-04-04 Fujisawa Pharmaceutical Co., Ltd. Dérivés de pyridoindole et leur procédé de préparation
EP0364274A1 (fr) * 1988-10-13 1990-04-18 Glaxo Group Limited Dérivés d'imidazole
EP0376624A1 (fr) * 1988-12-22 1990-07-04 Yamanouchi Pharmaceutical Co. Ltd. Dérivés de 4,5,6,7-tétrahydrobenzimidazole et leur préparation
EP0377967A2 (fr) * 1988-12-13 1990-07-18 Beecham Group Plc Dérivés du 9-aza-3-(oxa/thia)-bicyclo[3,2,1]nonane, procédé et intermédiaires pour leur préparation et compositions pharmaceutiques les contenant
EP0381422A1 (fr) * 1989-02-02 1990-08-08 Yamanouchi Pharmaceutical Co. Ltd. Dérivés de tétrahydrobenzimidazole
EP0385722A2 (fr) * 1989-02-28 1990-09-05 Glaxo Group Limited Dérivés de tricyclique lactame et les compositions pharmaceutiques qui les contiennent
EP0387431A1 (fr) * 1989-03-14 1990-09-19 Beecham Group Plc Dérivés d'imidazole, procédés de leur préparation et leur application comme produits pharmaceutiques
WO1991001316A1 (fr) * 1989-07-21 1991-02-07 Beecham Group Plc Nouveau derive de 9-azabicyclo[3.3.1] nonane
EP0417746A2 (fr) * 1989-09-11 1991-03-20 G.D. Searle & Co. Amides d'acides aromatiques N-substituées par azabicyclo[3.3.0]octane
EP0419397A1 (fr) * 1989-09-08 1991-03-27 Novo Nordisk A/S Dérivés de l'urée, leur préparation et leur utilisation
WO1991007402A1 (fr) * 1989-11-17 1991-05-30 Pfizer Inc. Amides et esters azabicyliques antagonistes du recepteur de 5-ht¿3?
WO1991012254A1 (fr) * 1990-02-16 1991-08-22 Novo Nordisk A/S Composes d'uree substitues, preparation et utilisation des ces composes
EP0450757A2 (fr) * 1990-02-22 1991-10-09 Glaxo Group Limited Utilisation des antagonistes du 5-hydroxytryptamine pour le traitement des maladies mentales dès l'origine de l'enfance
EP0451538A2 (fr) * 1990-03-19 1991-10-16 Fujisawa Pharmaceutical Co., Ltd. Utilisation des dérivés du pyridoindole dans le traitement des troubles ischémiques
EP0454121A2 (fr) * 1990-04-27 1991-10-30 G.D. Searle & Co. Composés azatétracycliques
WO1992005174A1 (fr) * 1990-09-26 1992-04-02 Beecham Group Plc Derives de 3,9-diazabicyclo (3.3.1) nonan-7-yl, procede et intermediaires de preparation et compositions pharmaceutiques les contenant
US5126343A (en) * 1989-09-11 1992-06-30 G. D. Searle & Co. N-azabicyclo [3.3.0]octane amides of aromatic acids
WO1992011259A1 (fr) * 1990-12-19 1992-07-09 Beecham Group Plc Amides azabicycliques ou esters d'acides benzoïques halogenes
WO1992012149A1 (fr) * 1991-01-09 1992-07-23 Smithkline Beecham Plc Derives azabicydiques et azatricydiques, leurs procedes et intermediaires de preparation et compositions pharmaceutiques les contenant
US5137893A (en) * 1991-03-07 1992-08-11 G. D. Searle & Co. Pharmaceutically useful meso-azacyclic amides of imidazopyridine carboxylic acids and analogs thereof
WO1992014733A1 (fr) * 1991-02-23 1992-09-03 Smithkline Beecham P.L.C. Produits pharmaceutiques
EP0504679A1 (fr) * 1991-03-07 1992-09-23 G.D. Searle & Co. Imidazopyridines comme antagonistes 5-HT3 sérotonergiques
EP0518767A2 (fr) * 1991-06-11 1992-12-16 Merrell Pharmaceuticals Inc. Dérivés d'analogues d'amide de quinolizines à pont méthano
EP0554794A1 (fr) * 1992-02-04 1993-08-11 Eisai Co., Ltd. Dérivés d'acides aminobenzoiques

Patent Citations (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0189002A2 (fr) * 1984-12-20 1986-07-30 Sandoz Ag Traitement de maladies gastro-intestinales utilisant des 5-HT3 antagonistes
GB2192885A (en) * 1986-07-23 1988-01-27 Glaxo Group Ltd Heterocyclic compounds
EP0254584A2 (fr) * 1986-07-25 1988-01-27 Beecham Group Plc Composés azabicycliques, procédé pour leur préparation et leur utilisation pharmaceutique
EP0266899A2 (fr) * 1986-10-03 1988-05-11 Glaxo Group Limited Dérivés d'indole
EP0272876A2 (fr) * 1986-12-17 1988-06-29 Glaxo Group Limited Application des dérivés hétérocycliques pour la fabrication de médicaments
EP0279512A2 (fr) * 1987-01-19 1988-08-24 Beecham Group Plc Emploi de certains antagonistes du récépteur 5-HT3 pour le traitement des douleurs viscérales
EP0287196A1 (fr) * 1987-02-18 1988-10-19 Beecham Group Plc Dérivés de l'indole, un procédé pour leur préparation et compositions pharmaceutiques les contenant
EP0289170A2 (fr) * 1987-04-25 1988-11-02 Beecham Group Plc Composés azabicycliques, leur procédé de préparation et compositions pharmaceutiques les contenant
EP0315316A2 (fr) * 1987-10-02 1989-05-10 Beecham Group Plc Dérivés d'imidazole, procédé pour leur préparation, compositions pharmaceutiques les contenant, et leur application pharmaceutique
EP0317088A1 (fr) * 1987-10-22 1989-05-24 Glaxo Group Limited Dérivés cétoniques
EP0315390A2 (fr) * 1987-11-04 1989-05-10 Beecham Group Plc Composés nouveaux de 4-oxobenzotriazine et 4-oxoquinazoline
WO1989009217A1 (fr) * 1988-03-23 1989-10-05 Beecham Group Plc Nouveaux composes
EP0336759A1 (fr) * 1988-04-07 1989-10-11 Glaxo Group Limited Dérivés d'imidazole
EP0345956A1 (fr) * 1988-05-20 1989-12-13 Glaxo Group Limited Cétones tricycliques
EP0347229A1 (fr) * 1988-06-16 1989-12-20 Glaxo Group Limited Dérivés de l'indole
EP0351385A2 (fr) * 1988-07-12 1990-01-17 BOEHRINGER INGELHEIM ITALIA S.p.A. Dérivés d'amidino et de guanidino
EP0358903A2 (fr) * 1988-07-29 1990-03-21 Dainippon Pharmaceutical Co., Ltd. Dérivés d'acide indazole-3-carboxylique
EP0356098A2 (fr) * 1988-08-15 1990-02-28 Glaxo Group Limited Dérivés de lactames
EP0357416A2 (fr) * 1988-09-01 1990-03-07 Glaxo Group Limited Utilisation des antagonistes de la sérotonine dans le traitement de l'asservissement aux drogues
EP0361317A2 (fr) * 1988-09-27 1990-04-04 Fujisawa Pharmaceutical Co., Ltd. Dérivés de pyridoindole et leur procédé de préparation
EP0364274A1 (fr) * 1988-10-13 1990-04-18 Glaxo Group Limited Dérivés d'imidazole
EP0377967A2 (fr) * 1988-12-13 1990-07-18 Beecham Group Plc Dérivés du 9-aza-3-(oxa/thia)-bicyclo[3,2,1]nonane, procédé et intermédiaires pour leur préparation et compositions pharmaceutiques les contenant
EP0376624A1 (fr) * 1988-12-22 1990-07-04 Yamanouchi Pharmaceutical Co. Ltd. Dérivés de 4,5,6,7-tétrahydrobenzimidazole et leur préparation
EP0381422A1 (fr) * 1989-02-02 1990-08-08 Yamanouchi Pharmaceutical Co. Ltd. Dérivés de tétrahydrobenzimidazole
EP0385722A2 (fr) * 1989-02-28 1990-09-05 Glaxo Group Limited Dérivés de tricyclique lactame et les compositions pharmaceutiques qui les contiennent
EP0387431A1 (fr) * 1989-03-14 1990-09-19 Beecham Group Plc Dérivés d'imidazole, procédés de leur préparation et leur application comme produits pharmaceutiques
WO1991001316A1 (fr) * 1989-07-21 1991-02-07 Beecham Group Plc Nouveau derive de 9-azabicyclo[3.3.1] nonane
EP0419397A1 (fr) * 1989-09-08 1991-03-27 Novo Nordisk A/S Dérivés de l'urée, leur préparation et leur utilisation
US5126343A (en) * 1989-09-11 1992-06-30 G. D. Searle & Co. N-azabicyclo [3.3.0]octane amides of aromatic acids
EP0417746A2 (fr) * 1989-09-11 1991-03-20 G.D. Searle & Co. Amides d'acides aromatiques N-substituées par azabicyclo[3.3.0]octane
WO1991007402A1 (fr) * 1989-11-17 1991-05-30 Pfizer Inc. Amides et esters azabicyliques antagonistes du recepteur de 5-ht¿3?
WO1991012254A1 (fr) * 1990-02-16 1991-08-22 Novo Nordisk A/S Composes d'uree substitues, preparation et utilisation des ces composes
EP0450757A2 (fr) * 1990-02-22 1991-10-09 Glaxo Group Limited Utilisation des antagonistes du 5-hydroxytryptamine pour le traitement des maladies mentales dès l'origine de l'enfance
EP0451538A2 (fr) * 1990-03-19 1991-10-16 Fujisawa Pharmaceutical Co., Ltd. Utilisation des dérivés du pyridoindole dans le traitement des troubles ischémiques
EP0454121A2 (fr) * 1990-04-27 1991-10-30 G.D. Searle & Co. Composés azatétracycliques
WO1992005174A1 (fr) * 1990-09-26 1992-04-02 Beecham Group Plc Derives de 3,9-diazabicyclo (3.3.1) nonan-7-yl, procede et intermediaires de preparation et compositions pharmaceutiques les contenant
WO1992011259A1 (fr) * 1990-12-19 1992-07-09 Beecham Group Plc Amides azabicycliques ou esters d'acides benzoïques halogenes
WO1992012149A1 (fr) * 1991-01-09 1992-07-23 Smithkline Beecham Plc Derives azabicydiques et azatricydiques, leurs procedes et intermediaires de preparation et compositions pharmaceutiques les contenant
WO1992014733A1 (fr) * 1991-02-23 1992-09-03 Smithkline Beecham P.L.C. Produits pharmaceutiques
US5137893A (en) * 1991-03-07 1992-08-11 G. D. Searle & Co. Pharmaceutically useful meso-azacyclic amides of imidazopyridine carboxylic acids and analogs thereof
EP0504679A1 (fr) * 1991-03-07 1992-09-23 G.D. Searle & Co. Imidazopyridines comme antagonistes 5-HT3 sérotonergiques
EP0518767A2 (fr) * 1991-06-11 1992-12-16 Merrell Pharmaceuticals Inc. Dérivés d'analogues d'amide de quinolizines à pont méthano
EP0554794A1 (fr) * 1992-02-04 1993-08-11 Eisai Co., Ltd. Dérivés d'acides aminobenzoiques

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
ALIMENT.PHARMACOL.THER., vol.6, no.3, June 1992 pages 273 - 289 N.J.TALLEY 'REVIEW ARTICLE: 5-HYDROXYTRYPTAMINE AGONISTA AND ANTAGONISTS IN THE MODULATION OF GASTROINTESTINAL MOTILITY AND SENSATION: CLIMICAL IMPLICATIONS' *
GUT, vol.31, no.10, 1990 page A1174 A. PRIOR ET AL. 'REDUCTION OF RECTAL SENSITIVITY AND POST-PRANDIAL MOTILITY BY GRANISETRON, A 5-HT3 RECEPTOR ANTAGONIST, IN PATIENTS WITH IRRITABLE BOWEL SYNDROME (IBS)' cited in the application *
R.BERKOW, ED. 'THE MERCK MANUAL OF DIAGNOSIS AND THERAPY, 15TH EDITION' , MERCK & CO. , RAHWAY, N.J. see page 808 - page 810 *

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US5852014A (en) * 1992-03-12 1998-12-22 Smithkline Beecham P.L.C. Condensed indole derivatives as 5HT4 -receptor antagonists
US5998409A (en) * 1992-03-12 1999-12-07 Smithkline Beecham Plc Condensed indole derivatives as 5HT4 -receptor antagonists
US5726187A (en) * 1992-10-16 1998-03-10 Smithkline Beecham Plc N-alkylpiperidinyl-4-methyl carboxylic esters/amides of condensed ring systems as 5-HT4 receptor antagonists
US6284770B1 (en) 1997-10-07 2001-09-04 Glaxo Wellcome Inc. Medicaments for the treatment of non-constipated female irritable bowel syndrome
WO1999017755A2 (fr) * 1997-10-07 1999-04-15 Glaxo Group Limited Medicaments
WO1999017755A3 (fr) * 1997-10-07 1999-09-23 Glaxo Group Ltd Medicaments
US6593336B2 (en) 1997-10-07 2003-07-15 Smithkline Beecham Corporation Methods for treating irritable bowel syndrome
US6429209B2 (en) 1997-10-07 2002-08-06 Smithkline Beecham Corporation Methods for treating irritable bowel syndrome
WO2000048581A3 (fr) * 1999-02-18 2001-01-11 Novartis Ag Utilisation d'antagonistes du recepteur 5-ht¿3?
WO2000048581A2 (fr) * 1999-02-18 2000-08-24 Novartis Ag Utilisation d'antagonistes du recepteur 5-ht¿3?
US6462065B2 (en) 1999-02-18 2002-10-08 Novartis Ag Use of 5-HT3 receptor antagonists for treating musculoeskeletal diseases
US7393857B2 (en) 1999-02-18 2008-07-01 Novasearch Ag Use of 5-HT3 receptor antagonists for treating musculoskeletal diseases
CN1310644C (zh) * 1999-12-10 2007-04-18 诺瓦提斯公司 药物组合产品及其在治疗胃肠疾病中的应用
EP1488788A1 (fr) * 1999-12-10 2004-12-22 Novartis AG Combinaisons pharmaceutiques et leur utilisation pour le traitement de troubles gastro-intestinaux
WO2001041748A2 (fr) * 1999-12-10 2001-06-14 Novartis Ag Combinaisons pharmaceutiques et leur utilisation dans le traitement de troubles gastro-intestinaux
WO2001041748A3 (fr) * 1999-12-10 2002-12-19 Novartis Ag Combinaisons pharmaceutiques et leur utilisation dans le traitement de troubles gastro-intestinaux
SG152025A1 (en) * 1999-12-10 2009-05-29 Novartis Ag Pharmaceutical combinations and their use in treating gastrointestinal disorders
CZ300690B6 (cs) * 1999-12-10 2009-07-15 Novartis Ag Farmaceutická kombinace obsahující tegaserod a omeprazol pro lécení refluxní nemoci jícnu
US7470690B2 (en) 2002-07-10 2008-12-30 Dynogen Pharmaceuticals, Inc. 4-(2-Fluorophenyl)-6-methyl-2-(1-piperazinyl)thieno[2,3-D)pyrimidine in the treatment of functional bowel disorder
US7094786B2 (en) 2003-01-13 2006-08-22 Dynogen Pharmaceuticals, Inc. Method of treating nausea, vomiting, retching or any combination thereof
US7608282B2 (en) * 2003-02-05 2009-10-27 Strakan International Limited Transdermal granisetron
US20100008974A1 (en) * 2003-02-05 2010-01-14 Strakan International Limited Transdermal granisetron
US20120258164A1 (en) * 2003-02-05 2012-10-11 Strakan International Limited Transdermal granisetron
US8246981B2 (en) 2005-05-18 2012-08-21 Abeille Pharamaceuticals, Inc. Transdermal method and patch for emesis

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GB9214184D0 (en) 1992-08-12
EP0650355A1 (fr) 1995-05-03
KR950702112A (ko) 1995-06-19
WO1994001095A3 (fr) 1994-04-14
AU4507693A (en) 1994-01-31
JPH07508530A (ja) 1995-09-21
CA2139440A1 (fr) 1994-01-20

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