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1. (WO1992010495) NOVEL 14-(N-SUBSTITUTED AMINOMETHYL)EBURNANE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING THEM
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1992/010495 International Application No.: PCT/HU1991/000051
Publication Date: 25.06.1992 International Filing Date: 06.12.1991
IPC:
C07D 461/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
461
Heterocyclic compounds containing indolo [3, 2, 1-d, e] pyrido [3, 2, 1-i, j] [1, 5]-naphthyridine ring systems, e.g. vincamine
Applicants:
RICHTER GEDEON VEGYÉSZETI GYÁR RT. [HU/HU]; Gyömro^"i út 19-21 H-1475 Budapest, HU (AllExceptUS)
SZPORNY, László [HU/HU]; HU (UsOnly)
KISS, Béla [HU/HU]; HU (UsOnly)
KÁRPÁTI, Egon [HU/HU]; HU (UsOnly)
PÁLOSI, Éva [HU/HU]; HU (UsOnly)
SZOMBATHELYI, Zsolt [HU/HU]; HU (UsOnly)
SARKADI, Ádám [HU/HU]; HU (UsOnly)
GERE, Anikó [HU/HU]; HU (UsOnly)
BODÓ, Mihály [HU/HU]; HU (UsOnly)
CSOMOR, Katalin [HU/HU]; HU (UsOnly)
LASZY, Judit [HU/HU]; HU (UsOnly)
SZENTIRMAY, Zsolt [HU/HU]; HU (UsOnly)
LAPIS, Erzsébet [HU/HU]; HU (UsOnly)
SZABÓ, Sándor [HU/HU]; HU (UsOnly)
KREIDL, János [HU/HU]; HU (UsOnly)
VISKY, György [HU/HU]; HU (UsOnly)
CZIBULA, László [HU/HU]; HU (UsOnly)
NEMES, András [HU/HU]; HU (UsOnly)
Inventors:
SZPORNY, László; HU
KISS, Béla; HU
KÁRPÁTI, Egon; HU
PÁLOSI, Éva; HU
SZOMBATHELYI, Zsolt; HU
SARKADI, Ádám; HU
GERE, Anikó; HU
BODÓ, Mihály; HU
CSOMOR, Katalin; HU
LASZY, Judit; HU
SZENTIRMAY, Zsolt; HU
LAPIS, Erzsébet; HU
SZABÓ, Sándor; HU
KREIDL, János; HU
VISKY, György; HU
CZIBULA, László; HU
NEMES, András; HU
Agent:
DANUBIA; P.O. Box 198 H-1368 Budapest, HU
Priority Data:
8107/9007.12.1990HU
Title (EN) NOVEL 14-(N-SUBSTITUTED AMINOMETHYL)EBURNANE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING THEM
(FR) NOUVEAUX DERIVES DE 14-(AMINOMETHYLE N-SUBSTITUE)EBURBANE, LEUR PROCEDE DE PREPARATION ET COMPOSITIONS LES CONTENANT
Abstract:
(EN) The invention relates to novel, optically active $i(cis) and $i(trans) 14-(N-substituted aminomethyl)eburnane derivatives of formula (I), wherein R1 stands for hydrogen, a C1-6alkyl or C2-6alkenyl group; R2 means a C1-6alkyl, C2-6alkenyl or a hydroxy-C1-6alkyl group; or R1 and R2 represent together with the adjacent nitrogen atom to which they are attached, a 5 to 7-membered saturated ring, optionally containing one oxygen atom and/or one optionally substituted nitrogen atom as heteroatom; and n is 2 or 3, as well as pharmaceutically acceptable salts of these compounds. The compounds of the invention possess an antioxidative (lipid peroxidation-inhibiting) effect and therefore, they are useful for treating diseases connected with lipid peroxidation, such as ischaemic intestinal diseases, myocardial ischaemia, ischaemic cerebrovascular disturbances as well as some diseases of connective tissues, e.g. rheumatoid arthritis. The compounds of the invention are also suitable for treating or preventing cognitive disorders.
(FR) Nouveaux dérivés $i(cis) et $i(trans) optiquement actifs de 14-(aminométhyle N-substitué)éburbane répondant à la formule (I), dans laquelle R1 représente hydrogène, ou un groupe alkyle C1-6 ou alcényle C2-6; R2 représente un groupe alkyle C1-6, alcényle C2-6 ou hydroxyalkyle C1-6; ou R1 et R2 représentent, conjointement avec l'atome d'azote voisin auquel ils sont liés, un cycle saturé penta- ou heptogonal renfermant éventuellement un atome d'oxygène et/ou un atome d'azote éventuellement substitué à titre d'hétéroatome; et n est 2 ou 3 ; ainsi que les sels pharmaceutiquement acceptables de ces composés. Lesdits composés présentent un effet antioxydant (inhibiteur de la peroxydation lipidique) et sont donc utiles au traitement des maladies associées à la peroxydation lipidique, par exemple les maladies intestinales ischémiques, l'ischémie myocardique, les troubles cérébro-vasculaires ischémiques ainsi que certaines maladies des tissus conjonctifs, par exemple la polyarthrite rhumatismale. Ces composés sont également utiles au traitement ou à la prophylaxie des troubles cognitifs.
Designated States: AU, CA, FI, JP, KR, LK, NO, US
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, MC, NL, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
AU1991090500