Novel compounds and medicinal use thereof

Details Novel compounds and medicinal use thereof Novel compounds and medicinal use thereof

C - Chemistry, Metallurgy

07

C

C07C 69/73 (2006.01) A61K 31/18 (2006.01) A61K 31/216 (2006.01) A61K 31/277 (2006.01) A61K 31/40 (2006.01) A61K 31/415 (2006.01) A61K 31/428 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01) A61K 38/08 (2006.01) A61P 19/02 (2006.01) A61P 37/06 (2006.01) A61P 43/00 (2006.01) C07C 59/64 (2006.01) C07C 59/84 (2006.01) C07C 65/24 (2006.01) C07C 65/34 (2006.01) C07C 65/36 (2006.01) C07C 65/38 (2006.01) C07C 65/40 (2006.01) C07C 69/738 (2006.01) C07C 69/767 (2006.01) C07C 69/94 (2006.01) C07C 205/49 (2006.01)

Patent

CA 2348763

Compounds represented by formula (I) wherein N1 represents an atom to which a donor hydrogen atom in a hydrogen bond donor group is bonded or a hydrogen bond acceptor atom in a hydrogen bond acceptor group; N3 represents a hydrogen bond acceptor atom in a hydrogen bond acceptor group; and N2, N4 and N5 represent each an arbitrary carbon atom constituting a hydrophobic group; having an atom corresponding to N3 and atoms corresponding to at least two atoms selected from N1, N2, N4 and N5 among the five atoms constituting a pharmacophore specified by the interatomic distances among N1, N2, N3, N4 and N5; and, in the optimized stereochemical structure thereof, the interatomic distances between the atom corresponding to N3 and atoms corresponding to at least two atoms selected from N1, N2, N4 and N5 fall within the scope of the pharmacophore interatomic distance, or salts thereof. Because of having an effect of inhibiting the activity of a transcription factor AP-1, these compounds are useful as preventives/remedies for diseases in which the excessive expression of AP-1 participates and as AP-1 inhibitors.

Composés de formule (I), ou leurs sels, dans laquelle N1 représente soit un atome auquel est lié un atome donneur d'hydrogène faisant partie d'un groupe donneur de liaisons hydrogène, soit un atome accepteur de liaisons hydrogène faisant partie d'un groupe accepteur de liaisons hydrogène; N3 représente un atome accepteur de liaisons hydrogène faisant partie d'un groupe accepteur de liaisons hydrogène; et N2, N4 et N5 représentent chacun un atome de carbone arbitraire constituant un groupe hydrophobe. Ces composés contiennent un atome correspondant à N3 et des atomes correspondant à au moins deux atomes choisis entre N1, N2, N4 et N5 parmi les 5 atomes constituant un pharmacophore défini par les distances interatomiques entre N1, N2, N3, N4 et N5; et, dans leur structure stéréochimique optimale, les distances interatomiques entre l'atome correspondant à N3 et les atomes correspondant aux deux atomes choisis entre N1, N2, N4 et N5 sont comprises dans la plage de distances interatomiques du pharmacophore. Les composés de l'invention étant capables d'inhiber l'activité du facteur de transcription AP-1, ils sont utiles comme agents prophylactiques ou thérapeutiques dans les maladies où intervient une expression excessive de AP-1 et comme inhibiteurs de AP-1.

Affiliated with

Also associated with

Rating

Novel compounds and medicinal use thereof does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Novel compounds and medicinal use thereof, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Novel compounds and medicinal use thereof will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-1929876