Some content of this application is unavailable at the moment.
If this situation persist, please contact us atFeedback&Contact
1. (WO1997018192) AROMATIC CARBOXYLIC ACID ESTERS, THE PRODUCTION OF SAME AND USE OF SAME AS MEDICAMENTS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/018192 International Application No.: PCT/CH1996/000390
Publication Date: 22.05.1997 International Filing Date: 05.11.1996
Chapter 2 Demand Filed: 24.05.1997
IPC:
A61K 31/44 (2006.01) ,C07D 213/80 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78
Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
79
Acids; Esters
80
in position 3
Applicants:
F. HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124 CH-4070 Basel, CH
Inventors:
KLAUS, Michael; DE
MOHR, Peter; CH
Priority Data:
3249/9516.11.1995CH
Title (DE) AROMATISCHE CARBONSÄUREESTER, IHRE HERSTELLUNG UND VERWENDUNG ALS HEILMITTEL
(EN) AROMATIC CARBOXYLIC ACID ESTERS, THE PRODUCTION OF SAME AND USE OF SAME AS MEDICAMENTS
(FR) ESTERS CARBOXYLIQUES AROMATIQUES, LEUR PRODUCTION ET LEUR UTILISATION COMME MEDICAMENTS
Abstract:
(DE) Verbindungen der Formel (I), worin R1 Wasserstoff oder C1-6-Alkyl; R2 C1-6-Alkyl oder Adamantyl; R3 C1-6-Alkyl oder Hydroxy; oder R2 und R3 zusammen -(CR6R7)n-; R4 C2-8-Alkyl, C2-8-Alkenyl, C2-8-Alkinyl, -OCH2R5 oder C2-8-Alkanoyl; und, falls R3 Hydroxy ist, Wasserstoff; R5 C1-6-Alkyl; C2-6-Alkenyl oder C2-6-Alkinyl; R6 und R7 unabhängig voneinander Wasserstoff oder C1-6-Alkyl; Y Sauerstoff oder Schwefel; und n 3, 4 oder 5 bedeuten, und pharmazeutisch anwendbare Salze von Carbonsäuren der Formel (I) wirken als selektive Liganden des Retinsäure-$g(g)-Rezeptors und können zur Behandlung von Epithelläsionen Verwendung finden.
(EN) Disclosed are compounds of formula (I) in which R1 stands for hydrogen or C1-6-alkyl, R2 stands for C1-6-alkyl or adamantyl, R3 stands for C1-6-alkyl or hydroxy or R2 and R3 together represent -(CR6R7)n-, R4 stands for C2-8-alkyl, C2-8-alkenyl, C2-8-alkinyl, -OCH2R5 or C2-8-alkanoyl and, if R3 is hydroxy, hydrogen, R5 stands for C1-6-alkyl, C2-6-alkenyl or C2-6-alkinyl, R6 and R7 independently of one another represent hydrogen or C1-6-alkyl, Y represents oxygen or sulphur, and n is 3, 4 or 5. These compounds and pharmaceutically usable salts of carboxylic acids of formula (I) act as selective ligands of the retinoic acid $g(g) receptor and can be used for treating of epithelial lesions.
(FR) L'invention concerne les composés de la formule (I) où R1 représente hydrogène ou alkyle C1-6, R2 représente alkyle C1-6 ou adamantyle, R3 représente alkyle C1-6 ou hydroxy, ou bien R2 et R3 représentent ensemble -(CR6R7)n-, R4 représente alkyle C2-8, alcényle C2-8, alkinyle C2-8, -OCH2R5 ou alcanoyle C2-8, et hydrogène si R3 représente hydroxy, R5 représente alkyle C1-6, alcényle C2-6 ou alkinyle C2-6, R6 et R7 représentent indépendamment l'un de l'autre hydrogène ou alkyle C1-6, Y représente oxygène ou soufre, et n vaut 3, 4 ou 5. Ces composés et les sels d'acides carboxyliques de la formule (I), pharmaceutiquement utilisables, agissent comme ligands sélectifs du récepteur d'acide rétinoïque $g(g) et peuvent être utilisés pour le traitement de lésions épithéliales.
Designated States: AL, AU, BA, BB, BG, BR, CA, CN, CZ, EE, GE, HU, IL, IS, JP, KP, KR, LK, LR, LT, LV, MG, MK, MN, MX, NO, NZ, PL, RO, SG, SI, SK, TR, TT, UA, UZ, VN
African Regional Intellectual Property Organization (ARIPO) (KE, LS, MW, SD, SZ, UG)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: German (DE)
Filing Language: German (DE)
Also published as:
TR1998/00870MXPA/a/1998/003829EP0862554JPH11500452CN1202154CA2237313
KR1019990067645AU1996072759DK0862554