DK191186A - Indolderivater - Google Patents

Indolderivater Download PDF

Info

Publication number
DK191186A
DK191186A DK191186A DK191186A DK191186A DK 191186 A DK191186 A DK 191186A DK 191186 A DK191186 A DK 191186A DK 191186 A DK191186 A DK 191186A DK 191186 A DK191186 A DK 191186A
Authority
DK
Denmark
Prior art keywords
alkyl
indole derivatives
alkoxy
halogen
phenyl
Prior art date
Application number
DK191186A
Other languages
English (en)
Other versions
DK170166B1 (da
DK191186D0 (da
Inventor
Francis David King
Original Assignee
Beecham Group 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26289173&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DK191186(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GB858510752A external-priority patent/GB8510752D0/en
Priority claimed from GB858525913A external-priority patent/GB8525913D0/en
Application filed by Beecham Group Plc filed Critical Beecham Group Plc
Publication of DK191186D0 publication Critical patent/DK191186D0/da
Publication of DK191186A publication Critical patent/DK191186A/da
Application granted granted Critical
Publication of DK170166B1 publication Critical patent/DK170166B1/da

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06Oxygen atoms
    • C07D451/12Oxygen atoms acylated by aromatic or heteroaromatic carboxylic acids, e.g. cocaine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/14Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/06Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing isoquinuclidine ring systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Description

z er CH eller N, og Rfl har den for R3 ovenfor definerede betydning;
Rb er til stede, når X-Y-R2 er bundet til phenylringen, og er valgt blandt hydrogen, halogen, CF3, hydroxy, Cj^.g-alkoxy og alkyl;
Ri er hydrogen, halogen, CF3, C^.g-alkyl, C^.g-alkoxy, C^.g-alkyl-thio, Cj_.y-acyl, .7 -acylamino, Ci.g-alkylsulfonylamino, N-{Ci-g-alkylsulfonyl)-N-Ci.4-alkylamino, Ci.g -alkylsulfinyl, hydroxy, nitro eller araino, aminocarbonyl, aminosulfonyl, araino-sulfonylamino eller N-(aminosulfonyl)-Ci.^-alkylamino eventuelt N-substitueret med én eller to grupper valgt blandt Ci.g-alkyl, Cj.g-eyeloalkyl, Cj.g-cycloalkyl-Ci.^-alkyl, phenyl og phenyl-Ci_4*alkyl eller eventuelt N-disubstitueret med C^.g-polymeth-ylen; R2 er en gruppe med den almene formel (a), (b) eller (c)
Figure DK191186AD00021
U)
Figure DK191186AD00022
(b)
Figure DK191186AD00023
(c) hvor n er 2 eller 3; p og q uafhængigt af hinanden er 1-3; og i:· eller R5 er C^-alkyl, Cj.g-cycloalkyl, C3.g-cycloalkyl-C1.2-alkyl eller en gruppe (CH2)tRg, hvor t er 1 eller 2, og Rg er thienyl, pyrrolyl eller furyl eventuelt substitueret med én eller to substituenter valgt blandt Cj.g-alkyl, Ci_g-alkoxy, tri-fluormethyl og halogen, eller er phenyl eventuelt substitueret med én eller to substituenter valgt blandt Ci.^-alkoxy, tri- fluormethyl, halogen, nitro, carboxy, esterificeret carboxy og C^.^-alkyl, der eventuelt er substitueret med hydroxy, C^.^-alkoxy, carboxy, esterificeret carboxy eller in vivo hydrolyserbart acyloxy, fremstilles ved forskellige fremgangsmåder. Forbindelser I har 5-HT-antagonistvirkning og/eller gastrisk motilitetsforbedrende virkning og kan anvendes som farmaceutiske midler. t
DK191186A 1985-04-27 1986-04-24 N-(endo-9-methyl-9-azabicyclo(3,3,1)non-3-yl)-1-m ethylindazol-3-carboxamid med 5-HT-antagonist-aktivitet, farmaceutiske præparater indeholdende forbindelsen, en fremgangsmåde til fremstilling af forbindelsen samt dens anvendelse som et farmaceutisk middel DK170166B1 (da)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB858510752A GB8510752D0 (en) 1985-04-27 1985-04-27 Compounds
GB8510752 1985-04-27
GB858525913A GB8525913D0 (en) 1985-10-21 1985-10-21 Compounds
GB8525913 1985-10-21

Publications (3)

Publication Number Publication Date
DK191186D0 DK191186D0 (da) 1986-04-24
DK191186A true DK191186A (da) 1986-10-28
DK170166B1 DK170166B1 (da) 1995-06-06

Family

ID=26289173

Family Applications (1)

Application Number Title Priority Date Filing Date
DK191186A DK170166B1 (da) 1985-04-27 1986-04-24 N-(endo-9-methyl-9-azabicyclo(3,3,1)non-3-yl)-1-m ethylindazol-3-carboxamid med 5-HT-antagonist-aktivitet, farmaceutiske præparater indeholdende forbindelsen, en fremgangsmåde til fremstilling af forbindelsen samt dens anvendelse som et farmaceutisk middel

Country Status (17)

Country Link
US (2) US4886808A (da)
EP (2) EP0498466B1 (da)
JP (1) JP2696457B2 (da)
AU (1) AU594670B2 (da)
BG (1) BG61324B2 (da)
CA (1) CA1296004C (da)
CY (1) CY1721A (da)
CZ (1) CZ286325B6 (da)
DE (2) DE3687080T2 (da)
DK (1) DK170166B1 (da)
ES (1) ES8707948A1 (da)
GR (1) GR861103B (da)
HK (1) HK66993A (da)
IE (1) IE58313B1 (da)
NZ (1) NZ215945A (da)
PT (1) PT82463B (da)
SG (1) SG39393G (da)

Families Citing this family (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4937247A (en) * 1985-04-27 1990-06-26 Beecham Group P.L.C. 1-acyl indazoles
DE3687080T2 (de) * 1985-04-27 1993-03-25 Beecham Group Plc Azabicyclononyl-indazol-carboxamid mit 5-ht-antagonistischer wirkung.
GB8623142D0 (en) * 1986-09-26 1986-10-29 Beecham Group Plc Compounds
GB8515845D0 (en) * 1985-06-22 1985-07-24 Beecham Group Plc Treatment
GB8518658D0 (en) * 1985-07-24 1985-08-29 Glaxo Group Ltd Medicaments
US5204356A (en) * 1985-07-24 1993-04-20 Glaxo Group Limited Treatment of anxiety
DE3687980T2 (de) * 1986-01-07 1993-06-17 Beecham Group Plc Indolderivate mit einer azabicyclischen seitenkette, verfahren zu ihrer herstellung, zwischenprodukte und pharmazeutische zusammensetzungen.
EP0254584B1 (en) * 1986-07-25 1992-10-07 Beecham Group Plc Azabicyclic compounds, process for their preparation, and their pharmaceutical use
HU202108B (en) * 1986-07-30 1991-02-28 Sandoz Ag Process for producing pharmaceutical compositions containing serotonine antqgonistic derivatives of indol-carboxylic acid or imidazolyl-methyl-carbazol
AT396870B (de) * 1986-08-07 1993-12-27 Sandoz Ag Verfahren zur herstellung einer galenischen formulierung zur nasalen verabreichung von serotoninantagonisten
ES2036587T5 (es) * 1986-11-21 1995-10-16 Glaxo Group Ltd Medicamentos para el tratamiento o prevencion del sindrome de abstinencia.
US5200414A (en) * 1986-12-17 1993-04-06 Glaxo Group Limited Methods for the treatment of cognitive disorders
US4973594A (en) * 1986-12-17 1990-11-27 Glaxo Group Limited Medicaments
US4985437A (en) * 1986-12-17 1991-01-15 Glaxo Group Limited Medicaments
US5190954A (en) * 1986-12-17 1993-03-02 Glaxo Group Limited Methods for the treatment of cognitive disorders
GB8806990D0 (en) * 1988-03-23 1988-04-27 Beecham Group Plc Novel compounds
GB8701022D0 (en) * 1987-01-19 1987-02-18 Beecham Group Plc Treatment
DE3852145T2 (de) * 1987-02-18 1995-04-06 Beecham Group Plc Indolderivate, Verfahren zu deren Herstellung und pharmazeutische Präparate, die diese enthalten.
US4918080A (en) * 1987-04-14 1990-04-17 Glaxo Group Limited Imidazollyl containing ketone derivatives
EP0289170B1 (en) * 1987-04-25 1993-06-23 Beecham Group Plc Azabicyclic compounds, process for their preparation and pharmaceutical compositions containing them
DE3822792C2 (de) * 1987-07-11 1997-11-27 Sandoz Ag Neue Verwendung von 5HT¶3¶-Antagonisten
GB8723157D0 (en) * 1987-10-02 1987-11-04 Beecham Group Plc Compounds
DE3872872T2 (de) * 1987-11-14 1993-02-04 Beecham Group Plc 5-ht3-rezeptor-antagonisten zur behandlung von husten und bronchokonstriktion.
AU611976B2 (en) * 1987-12-24 1991-06-27 John Wyeth & Brother Limited Aroyl urea and carbamic acid derivatives of azabicyclo compounds
EP0350130A3 (en) * 1988-07-07 1991-07-10 Duphar International Research B.V New substituted 1,7-annelated 1h-indazoles
US5166341A (en) * 1988-07-29 1992-11-24 Dainippon Pharmaceutical Co., Ltd. 6-amino-1,4-hexahydro-1H-diazepine derivatives
US5017573A (en) * 1988-07-29 1991-05-21 Dainippon Pharmaceutical Co., Ltd. Indazole-3-carboxylic acid derivatives
CA2004911A1 (en) * 1988-12-22 1990-06-22 Mitsuaki Ohta 4,5,6,7-tetrahydrobenzimidazole derivatives
DK0381422T3 (da) * 1989-02-02 1997-03-10 Yamanouchi Pharma Co Ltd Tetrahydrobenzimidazolderivater
GB8904551D0 (en) * 1989-02-28 1989-04-12 Glaxo Group Ltd Chemical compounds
GB8916682D0 (en) * 1989-07-21 1989-09-06 Beecham Group Plc Pharmaceutical compounds
US5126343A (en) * 1989-09-11 1992-06-30 G. D. Searle & Co. N-azabicyclo [3.3.0]octane amides of aromatic acids
US4992461A (en) * 1989-09-11 1991-02-12 G. D. Searle & Co. N-azabicyclo(3.3.0)octane amides of aromatic acids, compositions, and methods of use thereof
US5180728A (en) * 1989-09-25 1993-01-19 Fujisawa Pharmaceutical Company, Ltd. Pyrimidoindole derivatives and processes for preparation thereof
GB2236751B (en) 1989-10-14 1993-04-28 Wyeth John & Brother Ltd Heterocyclic compounds
GB8923209D0 (en) * 1989-10-14 1989-11-29 Wyeth John & Brother Ltd Heterocyclic compounds
US5225419A (en) * 1989-10-14 1993-07-06 John Wyeth & Brother, Limited Certain 1,8-ethano or propano-1,4-dihydro-4-oxo-quinoline-3-carboxamides and derivatives thereof
GB8928837D0 (en) * 1989-12-21 1990-02-28 Beecham Group Plc Pharmaceuticals
GB9009389D0 (en) * 1990-04-26 1990-06-20 Smith Kline French Lab Treatment
GB9009542D0 (en) * 1990-04-27 1990-06-20 Beecham Group Plc Novel compounds
AU7618991A (en) * 1990-05-14 1991-11-14 Syntex (U.S.A.) Inc. Novel tricyclic compounds
US5202318A (en) * 1990-05-14 1993-04-13 Syntex (U.S.A.) Inc. Tricyclic compounds acting at serotonin receptor subtypes
JP3122671B2 (ja) * 1990-05-23 2001-01-09 協和醗酵工業株式会社 複素環式化合物
GB9020927D0 (en) * 1990-09-26 1990-11-07 Beecham Group Plc Pharmaceuticals
US5200415A (en) * 1990-11-01 1993-04-06 Asahi Kasei Kogyo Kabushiki Kaisha Pyrazolo[1,5-a]pyridine-3-carboxylic acid derivatives and their pharmaceutical use
HU211081B (en) * 1990-12-18 1995-10-30 Sandoz Ag Process for producing indole derivatives as serotonin antagonists and pharmaceutical compositions containing the same
GB9101221D0 (en) * 1991-01-19 1991-02-27 Smithkline Beecham Plc Pharmaceuticals
US5929059A (en) * 1991-01-19 1999-07-27 Smithkline Beecham P.L.C. Pharmaceutical compositions containing granisetron and dexamethasone
US5143923B1 (en) * 1991-04-29 1993-11-02 Hoechst-Roussel Pharmaceuticals Incorporated Benzoisothiazole-and benzisoxazole-3-carboxamides
US5225412A (en) * 1991-04-29 1993-07-06 Hoechst-Roussel Pharmaceuticals Incorporated Benzoisothiazole-and benzisoxazole-3-carboxamides
US5955470A (en) * 1991-06-11 1999-09-21 Merrell Pharmaceuticals, Inc. Derivatives of amide analogs of certain methano bridged quinolizines
EP0517984A1 (en) * 1991-06-11 1992-12-16 Merrell Dow Pharmaceuticals Inc. Derivatives of amide analogs of certain methano bridged quinolizines
WO1993002677A1 (en) * 1991-08-03 1993-02-18 Smithkline Beecham Plc 5-ht4 receptor antagonists
CA2116024A1 (en) * 1991-08-20 1993-03-04 Francis David King 5-ht4 receptor antagonists
JPH0557982A (ja) * 1991-09-02 1993-03-09 Canon Inc キヤリツジ駆動方法
DE69231395T3 (de) 1991-09-20 2005-07-21 Glaxo Group Ltd., Greenford Neue medizinische Indikation für Tachykinin-Antagonisten
AU3361693A (en) * 1992-01-23 1993-09-01 Smithkline Beecham Plc Use of 5-HT4 receptor antagonists as medicaments for treating migraine
US5344831A (en) * 1992-01-31 1994-09-06 Nisshin Flour Milling Co., Ltd. Diazabicyclo derivatives
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
US5236931A (en) * 1992-03-26 1993-08-17 A. H. Robins Company, Incorporated 2-substituted benzamide and benzoate derivatives of 3-aminoquinuclidine and 3-quinuclidinol
GR1001378B (el) * 1992-10-08 1993-10-29 Smithkline Beecham Plc Ανταγωνιστές 5-ΗΤ4 πιπεριδυλαλκυλίου.
ES2056728B1 (es) * 1992-10-28 1995-05-01 Smithkline Beecham Plc Nuevos derivados de piperidilo y aminoalquilo con actividad antagonista del receptor 5-ht4
GB9305593D0 (en) * 1993-03-18 1993-05-05 Smithkline Beecham Plc Pharmaceuticals
CN1039623C (zh) * 1993-10-22 1998-09-02 中国人民解放军军事医学科学院毒物药物研究所 一种防治运动病综合征的药物组合物及其制备方法
GB9404055D0 (en) * 1994-03-03 1994-04-20 Smithkline Beecham Plc Novel process
GB9406857D0 (en) * 1994-04-07 1994-06-01 Sandoz Ltd Improvements in or relating to organic compounds
GB9412995D0 (en) * 1994-06-28 1994-10-26 Prendergast Kenneth F Safety enhancing pharmaceutical compositions of an active indazole
WO1996010006A1 (fr) * 1994-09-29 1996-04-04 Idemitsu Petrochemical Co., Ltd. Procede de production d'acides monocarboxyliques et/ou dicarboxyliques
GB9502582D0 (en) * 1995-02-10 1995-03-29 Smithkline Beecham Plc Novel process
GB9502583D0 (en) * 1995-02-10 1995-03-29 Smithkline Beecham Plc Novel process
GB9504078D0 (en) * 1995-03-01 1995-04-19 Smithkline Beecham Plc Novel process
ES2124162B1 (es) * 1995-03-01 1999-11-16 Smithkline Beecham Plc Un nuevo procedimiento para preparar compuestos farmaceuticamente activos.
GB9506119D0 (en) * 1995-03-25 1995-05-10 Smithkline Beecham Plc Chemical process
US5880121A (en) * 1996-01-05 1999-03-09 Hoechst Marion Roussel Inc. 4,5-dihydronaphth (1,2-c) isoxazoles and derivatives thereof
GB9602862D0 (en) * 1996-02-13 1996-04-10 Smithkline Beecham Plc Novel process
GB9602866D0 (en) * 1996-02-13 1996-04-10 Smithkline Beecham Plc Novel process
US6294548B1 (en) * 1998-05-04 2001-09-25 Hoffmann-La Roche Inc. Multidose vial formulations for administering endo-N-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-1-methyl-1H-indazole-3-carboxamide hydrochloride
JP2000198734A (ja) * 1998-12-30 2000-07-18 Pfizer Inc 胃運動性減弱および関連疾患の治療のための運動性増強薬
KR20010112673A (ko) * 2000-06-09 2001-12-21 김환기 트로피세트론 염산염(일반식ⅰ)의 제조방법
ES2197001B1 (es) 2002-03-26 2004-11-16 Laboratorios Vita, S.A. Procedimiento de obtencion de un compuesto farmaceuticamente activo.
PL210065B1 (pl) 2002-09-25 2011-11-30 Memory Pharm Corp Związki indazole, benzotiazole i benzoizotiazole, kompozycje farmaceutyczne je zawierające oraz zastosowanie związków
JP5690461B2 (ja) * 2002-11-15 2015-03-25 ヘルシン ヘルスケア ソシエテ アノニム 化学療法誘導嘔吐を治療するためのパロノセトロン
US8598219B2 (en) 2003-01-30 2013-12-03 Helsinn Healthcare Sa Liquid pharmaceutical formulations of palonosetron
JO2735B1 (en) 2003-01-30 2013-09-15 هيلسين هيلث كير أس ايه. Liquid pharmaceutical formations of balloonosterone
TWI355936B (en) * 2003-02-18 2012-01-11 Helsinn Healthcare Sa Uses of palonosetron hydrochloride
US7060841B2 (en) 2003-06-03 2006-06-13 Chemagis Ltd. Process for preparing 1-methylindazole-3-carboxylic acid
JP4824578B2 (ja) 2003-12-22 2011-11-30 メモリー・ファーマシューティカルズ・コーポレイション インドール類、1,2−ベンズイソオキサゾール類、および1,2−ベンゾイソチアゾール類、ならびにそれらの製造と使用
US20060167072A1 (en) * 2004-01-30 2006-07-27 Helsinn Healthcare Sa Liquid pharmaceutical formulations of palonosetron
KR101176670B1 (ko) 2004-03-25 2012-08-23 메모리 파마슈티칼스 코포레이션 인다졸, 벤조티아졸, 벤조이소티아졸, 벤즈이속사졸, 및그의 제조법 및 용도
EP1742944B1 (en) 2004-04-22 2010-11-10 Memory Pharmaceuticals Corporation Indoles, 1h-indazoles, 1,2-benzisoxazoles, 1,2-benzoisothiazoles, and preparation and uses thereof
WO2005111038A2 (en) 2004-05-07 2005-11-24 Memory Pharmaceuticals Corporation 1h-indazoles, benzothiazoles, 1,2-benzoisoxazoles, 1,2-benzoisothiazoles, and chromones and preparation and uses thereof
AU2005319248A1 (en) * 2004-12-22 2006-06-29 Memory Pharmaceuticals Corporation Nicotinic alpha-7 receptor ligands and preparation and uses thereof
RU2404179C2 (ru) * 2004-12-22 2010-11-20 Тереванс, Инк. Индазол-карбоксамидные соединения
US7868016B2 (en) 2005-07-13 2011-01-11 Baxter International Inc. Pharmaceutical formulations of endo-N-(9-methyl-9-azabicyclo[3,3.1]non-3-yl)-1-methyl-1H-indazole-3-carboxamide hydrochloride
US8106066B2 (en) 2005-09-23 2012-01-31 Memory Pharmaceuticals Corporation Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof
US8911751B2 (en) 2005-10-11 2014-12-16 Yissum Research Development Company Of The Hebrew University Of Jerusalem Compositions for nasal delivery
WO2007054784A1 (en) * 2005-11-10 2007-05-18 Orchid Chemicals & Pharmaceuticals Limited An improved process for the preparation of granisetron hydrochloride
WO2007088557A1 (en) * 2006-02-01 2007-08-09 Natco Pharma Limited Process for highly pure crystalline granisetron base
US20080004260A1 (en) * 2006-06-29 2008-01-03 Transcept Pharmaceuticals, Inc. Compositions of 5-HT3 antagonists and dopamine D2 antagonists for treatment of dopamine-associated chronic conditions
TWI367212B (en) * 2006-10-24 2012-07-01 Helsinn Healthcare Sa Dosage forms of palonosetron hydrochloride having improved stability and bioavailability
ITMI20062230A1 (it) * 2006-11-22 2008-05-23 Acraf Composto 2-alchil-indazolico procedimento per preparalo e composizione farmaceutica che lo comprende
EP2164848B1 (en) * 2007-06-13 2016-02-24 Inke, S.A. Polymorphic form of granisetron base, methods for obtaining it and formulation containing it
US20100298397A1 (en) * 2009-05-19 2010-11-25 Singh Nikhilesh N Method of treatment of obsessive compulsive disorder with ondansetron
EP2253316B1 (en) 2009-05-20 2013-08-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Serotonin 5-HT3 receptor antagonists for use in the treatment or prevention of an inner ear pathology with vestibular deficits
LT2432467T (lt) 2009-05-20 2018-04-10 INSERM (Institut National de la Santé et de la Recherche Médicale) Serotonino 5-ht3 receptoriaus antagonistai, skirti panaudoti pažeidimų sukeltų vestibiuliarinių sutrikimų gydymui
JOP20130213B1 (ar) * 2012-07-17 2021-08-17 Takeda Pharmaceuticals Co معارضات لمستقبلht3-5
US10329306B2 (en) 2014-09-29 2019-06-25 Takeda Pharmaceutical Company Limited Crystalline form of 1-(1-methyl-1H-pyrazol-4-yl)-N-((IR,5S,7S)-9-methyl-3-oxa-9-azabicyclo[3.3.1]nonan-7-yl)-1H-indole-3-carboxamide
GB201511382D0 (en) 2015-06-29 2015-08-12 Imp Innovations Ltd Novel compounds and their use in therapy
WO2017044693A1 (en) 2015-09-11 2017-03-16 Chase Pharmaceuticals Corporation Muscarinic combination and its use for combating hypocholinergic disorders of the central nervous system

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2100909A1 (fr) * 1970-07-15 1972-03-24 Egyt Gyogyszervegyeszeti Gyar Amides de l'acide indazole-3-carboxylique et procedes de preparation
GB2100259B (en) * 1981-06-13 1984-10-31 Merrell Toraude & Co Treatment of migraine with tropyl benzoate derivatives
FR2531083B1 (fr) * 1982-06-29 1986-11-28 Sandoz Sa Nouveaux derives de la piperidine, leur preparation et leur utilisation comme medicaments
FR2548666A1 (fr) * 1983-07-08 1985-01-11 Delalande Sa Nouveaux derives du nor-tropane et du granatane, leur procede de preparation et leur application en therapeutique
CH664567A5 (de) * 1983-08-26 1988-03-15 Sandoz Ag Aromatische carbonsaeure- und sulfonsaeureester oder -amide.
GB8510752D0 (en) * 1985-04-27 1985-06-05 Beecham Group Plc Compounds
US4937247A (en) * 1985-04-27 1990-06-26 Beecham Group P.L.C. 1-acyl indazoles
GB8525913D0 (en) * 1985-10-21 1985-11-27 Beecham Group Plc Compounds
DE3687080T2 (de) * 1985-04-27 1993-03-25 Beecham Group Plc Azabicyclononyl-indazol-carboxamid mit 5-ht-antagonistischer wirkung.
GB8520616D0 (en) * 1985-08-16 1985-09-25 Beecham Group Plc Compounds

Also Published As

Publication number Publication date
AU594670B2 (en) 1990-03-15
JPH05194508A (ja) 1993-08-03
NZ215945A (en) 1990-04-26
EP0200444B1 (en) 1992-11-11
EP0200444A2 (en) 1986-11-05
DK170166B1 (da) 1995-06-06
US4886808A (en) 1989-12-12
ES554405A0 (es) 1987-09-01
BG61324B2 (bg) 1997-05-30
EP0498466A1 (en) 1992-08-12
DE3687080T2 (de) 1993-03-25
US5034398A (en) 1991-07-23
ES8707948A1 (es) 1987-09-01
PT82463A (en) 1986-05-01
SG39393G (en) 1993-06-11
DE3687080D1 (de) 1992-12-17
IE58313B1 (en) 1993-09-08
EP0498466B1 (en) 2002-07-24
DE3650772D1 (de) 2002-08-29
JP2696457B2 (ja) 1998-01-14
DK191186D0 (da) 1986-04-24
GR861103B (en) 1986-08-11
PT82463B (pt) 1988-10-14
AU5657986A (en) 1986-11-06
EP0200444A3 (en) 1988-12-14
HK66993A (en) 1993-07-16
CA1296004C (en) 1992-02-18
IE861099L (en) 1986-10-27
CZ286325B6 (cs) 2000-03-15
DE3650772T2 (de) 2003-04-03
CS332391A3 (en) 1992-06-17
CY1721A (en) 1994-05-06

Similar Documents

Publication Publication Date Title
DK191186A (da) Indolderivater
SE7908443L (sv) Heterocykliska foreningar
LV11035A (lv) Jauni benzimidazolin-2-okso-1-karbonskabes atvasinajumi kuri pielietojami ka serotonina (5-HT) receptoru antagonisti
GB1088531A (en) Substituted benzamides
RU95113593A (ru) Замещенные, гетероциклические соединения, способ их получения, промежуточные соединения, гербицидная композиция и способ борьбы с нежелательными растениями
ATE73797T1 (de) Heterocyclisch substituierte indole, zwischenprodukte, verfahren zu ihrer herstellung und arzneimittel.
RU2004120553A (ru) Производные никотинамида, полезные в качестве р38-ингибиторов
EP0093488A3 (en) Nortropyl benzopyrrolinone compounds, process for their preparation and pharmaceutical compositions containing them
EA199800794A1 (ru) Новые производные арилглициламида, способ их получения и фармацевтическая композиция, содержащая эти соединения
CA2324418A1 (en) Novel opiate compounds, methods of making and methods of use
EP0096524A3 (en) Bicyclic benzamides or anilides, process for their preparation, and pharmaceutical compositions containing them
PE20050420A1 (es) Fenacilo 2-hidroxi-3-diaminoalcanos
ATE268752T1 (de) Aralkyl-1,2-diaminen mit calcimimetischer wirkung und verfahren zu ihrer herstellung
ES8307244A1 (es) Un procedimiento para la preparacion de nuevos derivados de benzamida.
AR023111A1 (es) Derivados de sulfonamida utiles como antagonistas del receptor 5-ht7, un procedimiento para su preparacion y composicion farmaceutica que los comprenden
DE69936572D1 (de) Benzisoxazolderivate mit d4-antagonistischer wirkung
EA200100825A1 (ru) Новые 1-арил-4-тиотриазины
EA200401077A1 (ru) 2-оксазоламины и их применение в качестве антагонистов рецептора 5-ht2b
HUP9700954A2 (hu) Szubsztituált 1-naftoil-guanidin-származékok, előállításuk, valamint az e vegyületeket tartalmazó gyógyszerkészítmények
NO802325L (no) Fremgangsmaate ved fremstilling av 3-amino-1-benzoxepin-derivater
ATE29877T1 (de) Mittel zur senkung der herzfrequenz.
SE7609385L (sv) Foreningar med antidepressiv aktivitet
RU2011107205A (ru) Пирролидинилалкиламидные производные, их получение и терапевтическое применение в качестве лигандов рецептора ccr3
ES8201541A1 (es) Un procedimiento para la preparacion de nuevas guanilamidi- nas
DE602008001452D1 (de) Verwendung einer Zusammensetzung für die Färbung von Keratinfasern, die einen halochromen Bestandteil und/oder den Farbstoff enthält, der diesem Bestandteil entspricht

Legal Events

Date Code Title Description
B1 Patent granted (law 1993)
PUP Patent expired