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1. WO1992015551 - ALIPHATIC PROPARGYLAMINES AS SELECTIVE MAO-B INHIBITORS AND AS NEUROPROTECTIVE AGENTS

Publication Number WO/1992/015551
Publication Date 17.09.1992
International Application No. PCT/CA1992/000090
International Filing Date 28.02.1992
Chapter 2 Demand Filed 30.09.1992
IPC
C07C 211/23 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
211Compounds containing amino groups bound to a carbon skeleton
01having amino groups bound to acyclic carbon atoms
20of an acyclic unsaturated carbon skeleton
23the carbon skeleton containing carbon-to-carbon triple bonds
C07C 215/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
215Compounds containing amino and hydroxy groups bound to the same carbon skeleton
02having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
04the carbon skeleton being saturated
06and acyclic
08with only one hydroxy group and one amino group bound to the carbon skeleton
C07C 229/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
04the carbon skeleton being acyclic and saturated
06having only one amino and one carboxyl group bound to the carbon skeleton
10the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
12to carbon atoms of acyclic carbon skeletons
CPC
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 25/24
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
24Antidepressants
A61P 25/26
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
26Psychostimulants, e.g. nicotine, cocaine
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for 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
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
C07C 211/23
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
211Compounds containing amino groups bound to a carbon skeleton
01having amino groups bound to acyclic carbon atoms
20of an acyclic unsaturated carbon skeleton
23the carbon skeleton containing carbon-to-carbon triple bonds
Applicants
  • UNIVERSITY OF SASKATCHEWAN [CA]/[CA] (AllExceptUS)
  • YU, Peter, H. [CA]/[CA] (UsOnly)
  • DAVIS, Bruce, A. [CA]/[CA] (UsOnly)
  • BOULTON, Alan, A. [CA]/[CA] (UsOnly)
Inventors
  • YU, Peter, H.
  • DAVIS, Bruce, A.
  • BOULTON, Alan, A.
Agents
  • TRUDEAU, Raymond
Priority Data
663,01801.03.1991US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ALIPHATIC PROPARGYLAMINES AS SELECTIVE MAO-B INHIBITORS AND AS NEUROPROTECTIVE AGENTS
(FR) PROPARGYLAMINES ALIPHATIQUES UTILISEES EN TANT QU'INHIBITEURS SELECTIFS DE MAO-B ET AGENTS NEUROPROTECTEURS
Abstract
(EN)
The invention relates to a series of propargylamines, their salts and pharmaceutical compositions containing a compound of formula (III) wherein R1, R3 and R4 are the same or different and represent hydrogen or a straight chain or branched lower alkyl; y is an integer ranging from 0 to 5; z is an integer ranging from 0 to 5; and R2 is a straight chain or branched alkyl, alkenyl, alkynyl, alkoxy, alkylthio or alkyl sulphinyl group having from 3 to 11 carbon atoms, said group being unsubstituted or substituted with at least one of the substituents selected from hydroxy, aldehyde, oxo, loweracyloxy, halogen, thio, sulfoxide, sulfone, phenyl, halogen-substituted phenyl, hydroxy-substituted phenyl, cycloalkyl having from 3 to 6 carbon atoms and heterocyclic substituents having between 3 and 6 atoms, of which form 1 to 3 are heteroatoms selected from O, S and/or N, and pharmaceutically acceptable salts thereof, in admixture with a pharmaceutically acceptable carrier, excipient or adjuvant. The compounds are useful as selective monoamine oxidase B inhibitors and have demonstrated neuroprotective properties in human and veterinary medicine.
(FR)
L'invention concerne une série de propargylamines, leurs sels et des compositions pharmaceutiques contenant un composé de la formule (III), dans laquelle R1, R3 et R4 sont identiques ou différents et représentent hydrogène ou un alkyle inférieur à chaîne droite ou ramifié; y est un nombre entier de 0 à 5; z est un nombre entier de 0 à 5; et R2 représente un groupe alkyle, alcényle, alcynyle, alcoxy, alkylthio ou alkylsulfinyle à chaîne droite ou ramifié présentant de 3 à 11 atomes de carbone, ledit groupe étant non substitué ou substitué par au moins l'un des substituants choisis parmi hydroxy, aldéhyde, oxo, acyloxy inférieur, halogène, thio, sulfoxyde, suflone phényle, phényle substitué par halogène, phényle substitué par hydroxy, cycloalkyle présentant de 3 à 6 atomes de carbone et des substituants hétérocycliques présentant entre 3 et 6 atomes, dont de 1 à 3 sont de hétéroatomes choisis parmi O, S et/ou N, et leurs sels pharmaceutiquement acceptables, mélangés avec un porteur, excipient ou adjuvant pharmaceutiquement acceptable. Les composés sont utiles en tant qu'inhibiteurs sélectifs de monoamine oxydase B et possèdent des propriétés neuroprotectrices prouvées dans la médecine humaine et vétérinaire.
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