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1. WO1996040126 - 1H-4(5)-SUBSTITUTED IMIDAZOLE DERIVATIVES

Publication Number WO/1996/040126
Publication Date 19.12.1996
International Application No. PCT/US1996/009498
International Filing Date 06.06.1996
Chapter 2 Demand Filed 03.01.1997
IPC
A61K 31/4164 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41641,3-Diazoles
A61K 31/422 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
42Oxazoles
422not condensed and containing further heterocyclic rings
C07D 233/54 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
C07D 413/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
CPC
A61K 31/4164
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41641,3-Diazoles
A61K 31/422
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
42Oxazoles
422not condensed and containing further heterocyclic rings
C07D 233/64
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
64with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
C07D 413/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
04directly linked by a ring-member-to-ring-member bond
Applicants
  • GLIATECH, INC. [US]/[US] (AllExceptUS)
  • PHILLIPS, James, G. [US]/[US] (UsOnly)
  • KHAN, Amin, Mohammed [IN]/[US] (UsOnly)
  • TEDFORD, Clark, E. [US]/[US] (UsOnly)
Inventors
  • PHILLIPS, James, G.
  • KHAN, Amin, Mohammed
  • TEDFORD, Clark, E.
Agents
  • KATZ, Martin, L.
Priority Data
08/479,92507.06.1995US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 1H-4(5)-SUBSTITUTED IMIDAZOLE DERIVATIVES
(FR) DERIVES D'IMIDAZOLE A SUBSTITUTION 1H-4(5)
Abstract
(EN)
The present invention is directed to 1H-4(5)-substituted imidazole derivates of formula (I), wherein A is (a); (b); or (c) where R1 is lower alkyl or lower alkoxy; R2, R3, R4, R5, R7 and R8 are each independently hydrogen or lower alkyl; R6 is hydrogen, lower alkyl or lower alkoxy and R5 and R6 can be joined to form a 4, 5 or 6 membered ring. The compounds of formula (I) have H3 histamine receptor agonist activity. The pharmaceutically acceptable salts, and individual stereoisomers of compounds of formula (I) above, as well as mixtures thereof, are also contemplated as falling within the scope of the present invention. The present invention also provides pharmaceutical compositions comprising a pharmaceutically acceptable carrier in combination with an effective amount of a compound of formula (I). The present invention also provides a method of treating conditions in which activation of histamine H3 receptors may be of therapeutic importance such as allergy, inflammation, cardio or cerebrovascular disease (i.e., hyper or hypotension, ischemia, stroke, migraine), gastrointestinal disorders (acid secretion, motility) and CNS disorders involving psychiatric disorders (i.e., including anxiety, manic/depressive disorder, schizophrenia, obsessive-compulsive disorders, etc.).
(FR)
La présente invention concerne des dérivés d'imidazole à substitution 1H-4(5) représentés par la formule générale (I). Dans cette formule, A représente (a), (b) ou (c), où R1 est alkyle inférieur ou alcoxy inférieur; R2, R3, R4, R5, R7 et R8 sont chacun indépendamment hydrogène ou alkyle inférieur; R6 est hydrogène, alkyle inférieur ou alcoxy inférieur, et R5 et R6 peuvent être reliés de façon à former un cycle à 4, 5 ou 6 chaînons. Les composés représentés par la formule (I) présentent une activité agoniste par rapport au récepteur H3 de l'histamine. L'invention concerne également des sels acceptables sur le plan pharmaceutique et des stéréoisomères individuels des composés représentés par la formule (I), ainsi que certains de leurs mélanges. L'invention concerne par ailleurs des compositions pharmaceutiques comprenant un excipient acceptable sur le plan pharmaceutique, en combinaison avec une quantité suffisante d'un des composés représentés par la formule (I). De plus, l'invention concerne un procédé de traitement des états dans lesquels l'activation des récepteurs H3 de l'histamine peut présenter une importance thérapeutique. Ces affections peuvent être des allergies, des inflammations, des affections cardio-vasculaires ou cérébro-vasculaires (telles que l'hypertension ou l'hypotension, l'ischémie, l'ictus, la migraine), des troubles gastro-intestinaux (tels que la sécrétion acide, les troubles de la motilité) et des troubles du système nerveux central, y compris des troubles de nature psychiatrique (tels que notamment, l'anxiété, les troubles maniaco-dépressifs, la schizophrénie, la psychonévrose obsessionnelle).
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