DK191186A - Indolderivater - Google Patents

Indolderivater Download PDF

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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
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Prior art keywords
alkyl
indole derivatives
alkoxy
halogen
phenyl
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DK191186A
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English (en)
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DK191186D0 (da
DK170166B1 (da
Inventor
Francis David King
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Beecham Group Plc
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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

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C07D451/02—Heterocyclic 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
    • C07D451/04—Heterocyclic 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
    • 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
    • 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
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C07D451/02—Heterocyclic 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
    • C07D451/04—Heterocyclic 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
    • C07D451/06—Oxygen atoms
    • C07D451/12—Oxygen atoms acylated by aromatic or heteroaromatic carboxylic acids, e.g. cocaine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C07D451/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/06—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing isoquinuclidine ring systems

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  • 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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Anesthesiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (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) EP0200444B1 (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)

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

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