WO1993007147A1 - Derives de 3,9-diazobicyclo(3.3.1)nonane presentant une activite antagoniste du recepteur 5-ht¿3? - Google Patents

Derives de 3,9-diazobicyclo(3.3.1)nonane presentant une activite antagoniste du recepteur 5-ht¿3? Download PDF

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Publication number
WO1993007147A1
WO1993007147A1 PCT/GB1992/001819 GB9201819W WO9307147A1 WO 1993007147 A1 WO1993007147 A1 WO 1993007147A1 GB 9201819 W GB9201819 W GB 9201819W WO 9307147 A1 WO9307147 A1 WO 9307147A1
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WO
WIPO (PCT)
Prior art keywords
formula
group
methyl
hydrogen
pharmaceutically acceptable
Prior art date
Application number
PCT/GB1992/001819
Other languages
English (en)
Inventor
Francis David King
Shirley Katherine Rahman
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 EP92921032A priority Critical patent/EP0607233A1/fr
Priority to JP5505561A priority patent/JPH06510990A/ja
Publication of WO1993007147A1 publication Critical patent/WO1993007147A1/fr

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08Bridged systems
    • 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

Definitions

  • CO-Y- is in the 1-position and either R 15 is in the 3-position and is
  • R 8 and R 9 are preferably both methyl groups.
  • R 15 when in the 4-position, include the following: hydrogen, chloro, bromo, methyl, ethyl, amino, methylamino, dimethylamino, phenyl, C 1-4 alkanoylamino such as formylamino, acetylamino, propionylamino, n- and wo-butyrylamino, aminosulphonyl, and amino and aminosulphonyl optionally substituted by one or two methyl, ethyl, n- or iso-propyl, n-, sec-, iso- or tert-butyl or phenyl groups; nitro, n- and iso-propory, methylthio, ethylthio, n- and iso-propylthio, hydroxy, methylsulphonyl and ethylsulphonyl or when R 15
  • Y is preferably NH.
  • X 1 ' to X 1 including any R a , R b , R c , R d, R e , R g , R h or R 10 , R 11 , R 12 , R 13 , R 14 or R 15 group to another such group, converting R'/Z', when other than R/Z, to R/Z; and optionally forming a pharmaceutically acceptable salt of the resultant compound of formula (IA).
  • leaving groups Q 1 displaceable by a nucleophile, include halogen such as chloro and bromo, C 1-4 alkoxy, such as CH 3 O and
  • the compounds of formula (IV) are known or are preparable analogously to, or routinely from, known compounds.

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

L'invention se rapporte à des composés de la formule (I), et à des sels pharmaceutiquement acceptables de ceux-ci. Dans ladite formule, X représente un groupe phényle ou un groupe hétéroaryle monocyclique pentagonal ou hexagonal, dont l'un ou l'autre groupe est éventuellement soudé à un noyau saturé ou insaturé, carbocyclique ou hétérocyclique pentagonal ou heptagonal; A représente une fraction de liaison; Z représente un groupe acyle carbocyclique; et R représente hydrogène ou méthyle. Ces composés présentent une activité antagoniste du récepteur 5-HT3.
PCT/GB1992/001819 1991-10-05 1992-10-05 Derives de 3,9-diazobicyclo(3.3.1)nonane presentant une activite antagoniste du recepteur 5-ht¿3? WO1993007147A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP92921032A EP0607233A1 (fr) 1991-10-05 1992-10-05 Derives de 3,9-diazobicyclo(3.3.1)nonane presentant une activite antagoniste du recepteur 5-ht 3?
JP5505561A JPH06510990A (ja) 1991-10-05 1992-10-05 5−ht3受容体拮抗活性を有する3,9−ジアザビシクロ(3.3.1)ノナン誘導体

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB9121170.6 1991-10-05
GB919121170A GB9121170D0 (en) 1991-10-05 1991-10-05 Pharmaceuticals

Publications (1)

Publication Number Publication Date
WO1993007147A1 true WO1993007147A1 (fr) 1993-04-15

Family

ID=10702465

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB1992/001819 WO1993007147A1 (fr) 1991-10-05 1992-10-05 Derives de 3,9-diazobicyclo(3.3.1)nonane presentant une activite antagoniste du recepteur 5-ht¿3?

Country Status (5)

Country Link
EP (1) EP0607233A1 (fr)
JP (1) JPH06510990A (fr)
AU (1) AU2688192A (fr)
GB (1) GB9121170D0 (fr)
WO (1) WO1993007147A1 (fr)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0558923A1 (fr) * 1992-01-31 1993-09-08 Nisshin Flour Milling Co., Ltd. Dérivés diazabicycliques comme antagonistes 5-HT3
US5399562A (en) * 1994-02-04 1995-03-21 G. D. Searle & Co. Indolones useful as serotonergic agents
US7589109B2 (en) 2005-02-22 2009-09-15 Pfizer Inc Oxyindole derivatives
US7595329B2 (en) 2004-06-15 2009-09-29 Pfizer Inc Benzimidazolone carboxylic acid derivatives
US7737163B2 (en) 2004-06-15 2010-06-15 Pfizer Inc. Benzimidazolone carboxylic acid derivatives

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2193633A (en) * 1986-07-30 1988-02-17 Sandoz Ltd Therapeutic use of serotonin antagonists
EP0469449A1 (fr) * 1990-07-31 1992-02-05 Nisshin Flour Milling Co., Ltd. Azabicyclo-dérivés
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2193633A (en) * 1986-07-30 1988-02-17 Sandoz Ltd Therapeutic use of serotonin antagonists
EP0469449A1 (fr) * 1990-07-31 1992-02-05 Nisshin Flour Milling Co., Ltd. Azabicyclo-dérivés
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

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0558923A1 (fr) * 1992-01-31 1993-09-08 Nisshin Flour Milling Co., Ltd. Dérivés diazabicycliques comme antagonistes 5-HT3
US5399562A (en) * 1994-02-04 1995-03-21 G. D. Searle & Co. Indolones useful as serotonergic agents
US7595329B2 (en) 2004-06-15 2009-09-29 Pfizer Inc Benzimidazolone carboxylic acid derivatives
US7705020B2 (en) 2004-06-15 2010-04-27 Pfizer Inc. Benzimidazolone carboxylic acid derivatives
US7737163B2 (en) 2004-06-15 2010-06-15 Pfizer Inc. Benzimidazolone carboxylic acid derivatives
US7589109B2 (en) 2005-02-22 2009-09-15 Pfizer Inc Oxyindole derivatives

Also Published As

Publication number Publication date
GB9121170D0 (en) 1991-11-20
EP0607233A1 (fr) 1994-07-27
AU2688192A (en) 1993-05-03
JPH06510990A (ja) 1994-12-08

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