CA2389645A1 - Composes azacycliques olefiniques d'aryle, composes azacycliques acetyleniques d'aryle, compositions pharmaceutiques les contenant et leur utilisation en tant qu'inhibiteurs de recepteurs cholinergiques nicotiniques - Google Patents

Composes azacycliques olefiniques d'aryle, composes azacycliques acetyleniques d'aryle, compositions pharmaceutiques les contenant et leur utilisation en tant qu'inhibiteurs de recepteurs cholinergiques nicotiniques Download PDF

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Publication number
CA2389645A1
CA2389645A1 CA002389645A CA2389645A CA2389645A1 CA 2389645 A1 CA2389645 A1 CA 2389645A1 CA 002389645 A CA002389645 A CA 002389645A CA 2389645 A CA2389645 A CA 2389645A CA 2389645 A1 CA2389645 A1 CA 2389645A1
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CA
Canada
Prior art keywords
compound
pyridine
nitrogen
enyl
carbon
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA002389645A
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English (en)
Inventor
Jeffrey Daniel Schmitt
Gary Maurice Dull
Balwinder Singh Bhatti
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Gyre Therapeutics Inc
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Individual
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 Individual filed Critical Individual
Publication of CA2389645A1 publication Critical patent/CA2389645A1/fr
Abandoned legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/32—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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

Abstract

La présente invention concerne le traitement de patients sensibles à/souffrant d'affections et de troubles, tels que des troubles du système nerveux central, par administration, si le patient le nécessite, de composés azacycliques oléfiniques d'aryle et de composés azacycliques acétyléniques d'aryle, notamment de cycloalkylamines oléfiniques de pyridyle et de cycloalkylamines acétyléniques de pyridyle. Des exemples de composés comprennent (S)-(E)-3-(3-pyrrolidine-2-yle-prop-1-ényle)pyridine, (S)-(E)-3-(2-pyrrolidine-2-ylvinyle)pyridine, 3-(2-pyrrolidine-2-yléthenyle)pyridine, 3-(3-pyrrolidine-2-ylprop-1-ényle)pyridine, 3-(2-(2-azétidinyle)éthényle)pyridine, 3-(3-(2-azétidinyle)prop-1-ényle)pyridine, 2-(2-(3-pyridyle)éthényle)-1-azabicyclo[3.3.0]octane, 2-(3-(3-pyridyle)prop-2-ényle)-1-azabicyclo[3.3.0]octane, 3-(2-(3-pyridyle)éthényle)-2-azabicyclo[2.2.1]heptane, 3-(3-(3-pyridyle)prop-2-ényl)-2-azabicyclo[2.2.1]heptane, 2-(2-(3-pyridyle)éthényle)-7-azabicyclo[2.2.1]heptane, 2-(3-(3-pyridyle)prop-2-ényle)-7-azabicyclo[2.2.1]heptane, 2-(2-(3-pyridyle)éthényle)quinuclidine et 2-(3-(3-pyridyle)prop-2-ényle)quinuclidine.
CA002389645A 1999-11-01 2000-06-30 Composes azacycliques olefiniques d'aryle, composes azacycliques acetyleniques d'aryle, compositions pharmaceutiques les contenant et leur utilisation en tant qu'inhibiteurs de recepteurs cholinergiques nicotiniques Abandoned CA2389645A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US43170099A 1999-11-01 1999-11-01
US09/431,700 1999-11-01
PCT/US2000/018292 WO2001032264A1 (fr) 1999-11-01 2000-06-30 Composes azacycliques olefiniques d'aryle, composes azacycliques acetyleniques d'aryle, compositions pharmaceutiques les contenant et leur utilisation en tant qu'inhibiteurs de recepteurs cholinergiques nicotiniques

Publications (1)

Publication Number Publication Date
CA2389645A1 true CA2389645A1 (fr) 2001-05-10

Family

ID=23713067

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002389645A Abandoned CA2389645A1 (fr) 1999-11-01 2000-06-30 Composes azacycliques olefiniques d'aryle, composes azacycliques acetyleniques d'aryle, compositions pharmaceutiques les contenant et leur utilisation en tant qu'inhibiteurs de recepteurs cholinergiques nicotiniques

Country Status (5)

Country Link
EP (1) EP1225955A1 (fr)
JP (1) JP2003513054A (fr)
AU (1) AU780492B2 (fr)
CA (1) CA2389645A1 (fr)
WO (1) WO2001032264A1 (fr)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6890935B2 (en) * 1999-11-01 2005-05-10 Targacept, Inc. Pharmaceutical compositions and methods for use
US6624167B1 (en) 2000-08-04 2003-09-23 Targacept, Inc. Pharmaceutical compositions and methods for use
AR036041A1 (es) * 2001-06-12 2004-08-04 Upjohn Co Compuestos aromaticos heterociclicos sustituidos con quinuclidina y composiciones farmaceuticas que los contienen
WO2004009599A1 (fr) * 2002-07-19 2004-01-29 Targacept, Inc. Composes heteroaromatiques olefiniques azacycliques a cinq elements, compositions pharmaceutiques contenant lesdits composes et leur utilisation comme inhibiteurs des recepteurs nicotiniques cholinergiques
US7098331B2 (en) * 2003-03-05 2006-08-29 Targacept, Inc. Arylvinylazacycloalkane compounds and methods of preparation and use thereof
WO2010065443A1 (fr) * 2008-12-01 2010-06-10 Targacept, Inc. Synthèse et nouvelles formes salines de la (r)-5-((e)-2-(pyrrolidin-3-ylvinyl)pyrimidine
MX2012006484A (es) 2009-12-07 2012-08-01 Targacept Inc 3,6-diazabiciclo [3.1.1] heptanos como ligandos de receptores nicotinicos neuronales de acetilcolina.

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9226573D0 (en) * 1992-12-21 1993-02-17 Ici Plc Heterocyclic compounds
CA2294990C (fr) * 1997-06-30 2007-03-06 William Scott Caldwell Compositions pharmaceutiques et methodes pour la liberation de dopamine
US6632823B1 (en) * 1997-12-22 2003-10-14 Merck & Co., Inc. Substituted pyridine compounds useful as modulators of acetylcholine receptors
US6432975B1 (en) * 1998-12-11 2002-08-13 Targacept, Inc. Pharmaceutical compositions and methods for use

Also Published As

Publication number Publication date
EP1225955A1 (fr) 2002-07-31
AU6204500A (en) 2001-05-14
AU780492B2 (en) 2005-03-24
JP2003513054A (ja) 2003-04-08
WO2001032264A1 (fr) 2001-05-10

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