C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 59/147 (2006.01) C07C 35/18 (2006.01) C07C 69/74 (2006.01) C07C 323/61 (2006.01) C07D 213/55 (2006.01) C07D 233/54 (2006.01) C07D 249/08 (2006.01) C07D 303/38 (2006.01) C07D 331/02 (2006.01) C07D 521/00 (2006.01)
Patent
CA 2415169
Novel C-4 substituted all-trans retinoic acid analogs are synthesized and used to treat various cancers and dermatological diseases and conditions. These novel C-4 substituted all-trans retinoic acid analogs inhibit all-trans retinoic acid (ATRA) 4-hydroxylase activity, thereby inhibiting the catabolism of ATRA. These novel C-4 substituted ATRA analogs also have ATRA-mimetic activity. The substitutions at C-4 comprise azole, sulfur, oxygen, nitrogen, pyridyl, acetylinic, cyclopropyl-amine, ester, oxime, cyano, oxirone and aziridine groups.
L'invention concerne de nouveaux analogues de l'acide tout trans rétinoïque substitués en C-4 qui sont synthétisés et utilisés pour traiter divers cancers et maladies et conditions dermatologiques. Ces nouveaux analogues de l'acide tout trans rétinoïque substitués en C-4 inhibent l'activité 4-hydroxylase de l'acide tout trans rétinoïque (ATRA), inhibant ainsi le catabolisme d'ATRA. Ces nouveaux analogues d'ATRA substitués en C-4 présentent également une activité mimétique d'ATRA. Les substitutions au niveau C-4 comprennent des groupes azole, soufre, oxygène, azote, pyridyle, acétyle, cyclopropyl-amine, ester, oxime, cyano, oxirane et aziridine.
Brodie Angela M. H.
Njar Vincent C. O.
Nnane Ivo P.
Gowling Lafleur Henderson Llp
University Of Maryland Baltimore
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